WO2006127899A3 - (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use - Google Patents

(r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use Download PDF

Info

Publication number
WO2006127899A3
WO2006127899A3 PCT/US2006/020233 US2006020233W WO2006127899A3 WO 2006127899 A3 WO2006127899 A3 WO 2006127899A3 US 2006020233 W US2006020233 W US 2006020233W WO 2006127899 A3 WO2006127899 A3 WO 2006127899A3
Authority
WO
WIPO (PCT)
Prior art keywords
synthesis
methylnaltrexone
processes
pharmaceutical use
mntx
Prior art date
Application number
PCT/US2006/020233
Other languages
French (fr)
Other versions
WO2006127899A2 (en
Inventor
Harold D Doshan
Julio Perez
Original Assignee
Progenics Pharm Inc
Harold D Doshan
Julio Perez
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=36997886&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2006127899(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to PL06771163T priority Critical patent/PL1913001T3/en
Priority to JP2008513707A priority patent/JP5213704B2/en
Priority to CA2609662A priority patent/CA2609662C/en
Priority to MX2007014880A priority patent/MX2007014880A/en
Priority to AU2006249911A priority patent/AU2006249911C1/en
Application filed by Progenics Pharm Inc, Harold D Doshan, Julio Perez filed Critical Progenics Pharm Inc
Priority to EP06771163.0A priority patent/EP1913001B1/en
Priority to CN200680022957XA priority patent/CN101208344B/en
Priority to DK06771163.0T priority patent/DK1913001T3/en
Priority to SI200631663T priority patent/SI1913001T1/en
Priority to ES06771163T priority patent/ES2429160T3/en
Priority to BRPI0611162-9A priority patent/BRPI0611162A2/en
Publication of WO2006127899A2 publication Critical patent/WO2006127899A2/en
Publication of WO2006127899A3 publication Critical patent/WO2006127899A3/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • A61P5/04—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/08—Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/02—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
    • C07D489/04—Salts; Organic complexes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/06—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with a hetero atom directly attached in position 14
    • C07D489/08—Oxygen atom
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/15—Medicinal preparations ; Physical properties thereof, e.g. dissolubility
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
    • Y10T436/00—Chemistry: analytical and immunological testing
    • Y10T436/14—Heterocyclic carbon compound [i.e., O, S, N, Se, Te, as only ring hetero atom]
    • Y10T436/141111—Diverse hetero atoms in same or different rings [e.g., alkaloids, opiates, etc.]

Abstract

This invention relates to stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use.
PCT/US2006/020233 2005-05-25 2006-05-25 (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use WO2006127899A2 (en)

Priority Applications (11)

Application Number Priority Date Filing Date Title
BRPI0611162-9A BRPI0611162A2 (en) 2005-05-25 2006-05-25 (r) -n-methylnaltrexone, process for its synthesis and pharmaceutical use
CN200680022957XA CN101208344B (en) 2005-05-25 2006-05-25 (R)-N-methylnaltrexone, processes for its synthesis and its pharmaceutical use
CA2609662A CA2609662C (en) 2005-05-25 2006-05-25 (r)-n-methylnaltrexone, process for its synthesis and its pharmaceutical use
MX2007014880A MX2007014880A (en) 2005-05-25 2006-05-25 (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use.
AU2006249911A AU2006249911C1 (en) 2005-05-25 2006-05-25 (R)-N-methylnaltrexone, processes for its synthesis and its pharmaceutical use
PL06771163T PL1913001T3 (en) 2005-05-25 2006-05-25 (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use
EP06771163.0A EP1913001B1 (en) 2005-05-25 2006-05-25 (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use
JP2008513707A JP5213704B2 (en) 2005-05-25 2006-05-25 (R) -N-methylnaltrexone, synthesis method thereof and pharmaceutical use thereof
DK06771163.0T DK1913001T3 (en) 2005-05-25 2006-05-25 (R) -N-METHYLNALTREXON, METHODS OF SYNTHESIS AND PHARMACEUTICAL APPLICATION
SI200631663T SI1913001T1 (en) 2005-05-25 2006-05-25 (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use
ES06771163T ES2429160T3 (en) 2005-05-25 2006-05-25 (R) -N-methylnaltrexone, processes for its synthesis and pharmaceutical use

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US68461605P 2005-05-25 2005-05-25
US60/684,616 2005-05-25

Publications (2)

Publication Number Publication Date
WO2006127899A2 WO2006127899A2 (en) 2006-11-30
WO2006127899A3 true WO2006127899A3 (en) 2007-02-08

Family

ID=36997886

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2006/020233 WO2006127899A2 (en) 2005-05-25 2006-05-25 (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use

Country Status (20)

Country Link
US (6) US7674904B2 (en)
EP (3) EP3219717A1 (en)
JP (4) JP5213704B2 (en)
CN (2) CN101208344B (en)
AR (1) AR057035A1 (en)
AU (1) AU2006249911C1 (en)
BR (1) BRPI0611162A2 (en)
CA (1) CA2609662C (en)
DK (1) DK1913001T3 (en)
ES (1) ES2429160T3 (en)
GT (1) GT200600226A (en)
HK (1) HK1244267A1 (en)
HN (1) HN2006019068A (en)
MX (1) MX2007014880A (en)
MY (1) MY151036A (en)
PL (1) PL1913001T3 (en)
PT (1) PT1913001E (en)
SI (1) SI1913001T1 (en)
TW (1) TWI383984B (en)
WO (1) WO2006127899A2 (en)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8524731B2 (en) 2005-03-07 2013-09-03 The University Of Chicago Use of opioid antagonists to attenuate endothelial cell proliferation and migration
US9518062B2 (en) 2009-07-16 2016-12-13 Mallinckrodt Llc Compounds and compositions for use in phototherapy and in treatment of ocular neovascular disease and cancers
US9526723B2 (en) 2008-03-21 2016-12-27 The University Of Chicago Treatment with opioid antagonists and mTOR inhibitors

Families Citing this family (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030158220A1 (en) * 1997-11-03 2003-08-21 Foss Joseph F. Use of methylnaltrexone and related compounds to treat chronic opioid use side effects
DK2368553T3 (en) 2003-04-08 2015-02-09 Progenics Pharm Inc Pharmaceutical preparation comprising methylnaltrexone
US20050004155A1 (en) * 2003-04-08 2005-01-06 Boyd Thomas A. Use of methylnaltrexone to treat irritable bowel syndrome
RU2005134364A (en) * 2003-04-08 2006-06-10 Проджиникс Фармасьютикалз, Инк. (Us) COMBINED TREATMENT FOR CONSTIPATION
BRPI0606587A2 (en) * 2005-01-20 2009-07-07 Progenics Pharmaceuticais Inc use of methylnaltrexone and related compounds to treat postoperative gastrointestinal dysfunction
CN101171010B (en) * 2005-03-07 2014-09-17 芝加哥大学 Use of opioid antagonists to attenuate endothelial cell proliferation and migration
US8518962B2 (en) 2005-03-07 2013-08-27 The University Of Chicago Use of opioid antagonists
US9662325B2 (en) 2005-03-07 2017-05-30 The University Of Chicago Use of opioid antagonists to attenuate endothelial cell proliferation and migration
US7767388B2 (en) * 2005-05-16 2010-08-03 Nutech Ventures Method for monitoring the stereoselectivity and relative rate of organic chemical reactions
AR057035A1 (en) * 2005-05-25 2007-11-14 Progenics Pharm Inc SYNTHESIS OF (R) -N-METHYLNTREXONE, PHARMACEUTICAL COMPOSITIONS AND USES
AR057325A1 (en) 2005-05-25 2007-11-28 Progenics Pharm Inc SYNTHESIS OF (S) -N-METHYLNTREXONE, PHARMACEUTICAL COMPOSITIONS AND USES
US20080194611A1 (en) * 2005-06-03 2008-08-14 Alverdy John C Modulation of Cell Barrier Dysfunction
MX2008014794A (en) 2006-05-26 2009-04-08 Pharmacofore Inc Controlled release of phenolic opioids.
TWI489984B (en) 2006-08-04 2015-07-01 Wyeth Corp Formulations for parenteral delivery of compounds and uses thereof
TW200815451A (en) * 2006-08-04 2008-04-01 Wyeth Corp 6-carboxy-normorphinan derivatives, synthesis and uses thereof
TW200817048A (en) * 2006-09-08 2008-04-16 Wyeth Corp Dry powder compound formulations and uses thereof
NZ575620A (en) 2006-09-20 2010-11-26 Mallinckrodt Inc Preparation of substituted morphinan-6-ones and salts and intermediates thereof
BRPI0719587A2 (en) * 2006-11-22 2013-12-17 Progenics Pharm Inc (S) - 7,8-SATURATED-4,5-EPOXY-MORFINAN ANALOG STEREO ISOMERS
CA2670136A1 (en) * 2006-11-22 2008-05-29 Progenics Pharmaceuticals, Inc. 7,8-saturated-4,5-epoxy-morphinanium analogs
US9040726B2 (en) 2007-03-06 2015-05-26 Mallinckrodt Llc Process for the preparation of quaternary N-alkyl morphinan alkaloid salts
EP2137189B1 (en) * 2007-03-06 2015-05-06 Mallinckrodt LLC Process for the preparation of quaternary n-alkyl morphinan alkaloid salts
CA2865389A1 (en) * 2007-03-29 2008-10-09 Progenics Pharmaceuticals, Inc. Crystal forms and uses thereof
TWI553009B (en) * 2007-03-29 2016-10-11 普吉尼製藥公司 Peripheral opioid receptor antagonists and uses thereof
HUE025662T2 (en) 2007-03-29 2016-04-28 Wyeth Llc Peripheral opioid receptor and antagonists and uses thereof
AU2014201056B2 (en) * 2007-03-29 2016-06-09 Progenics Pharmaceuticals, Inc. Crystal forms of (r) -n-methylnaltrexone bromide and uses thereof
BRPI0809205B8 (en) 2007-03-29 2021-05-25 Daiichi Sankyo Co Ltd pharmaceutical composition
WO2008138383A1 (en) 2007-05-16 2008-11-20 Cilag Ag Method for the production of n-methyl naltrexone bromide
WO2009009292A2 (en) * 2007-07-11 2009-01-15 Mallinckrodt Inc. Crystalline forms of naltrexone methobromide
US8159331B2 (en) * 2007-07-17 2012-04-17 Psion Teklogix Inc. Method and system for radiated power control for short range RFID tag reading
EP2240489A1 (en) 2008-02-06 2010-10-20 Progenics Pharmaceuticals, Inc. Preparation and use of (r),(r)-2,2'-bis-methylnaltrexone
WO2009099410A1 (en) * 2008-02-06 2009-08-13 Progenics Pharmaceuticals, Inc. Preparation and use of (r)-8-keto-methylnaltrexone
ES2549904T3 (en) 2008-05-27 2015-11-03 Mallinckrodt Llc Processes and compounds for the preparation of normorphinans
CN101607963B (en) 2008-06-20 2013-04-03 重庆医药工业研究院有限责任公司 Morphinan derivatives and preparation method thereof
US9458109B2 (en) 2008-09-03 2016-10-04 Mallinckrodt Llc Substituted berbines and processes for their synthesis
CN101685084B (en) * 2008-09-22 2013-09-25 重庆医药工业研究院有限责任公司 Method for detecting methylnaltrexone bromide and impurity thereof by chromatography
CA2676881C (en) 2008-09-30 2017-04-25 Wyeth Peripheral opioid receptor antagonists and uses thereof
CN101732243B (en) * 2008-11-26 2012-12-05 重庆医药工业研究院有限责任公司 Stable methyl naltrexone injection and preparation method thereof
CA2747427C (en) 2008-12-17 2015-10-13 Daiichi Sankyo Company, Limited Method for producing diamine derivative
EP2383272A4 (en) 2009-01-13 2012-07-25 Daiichi Sankyo Co Ltd Active blood coagulation factor inhibitor
WO2010096788A1 (en) * 2009-02-23 2010-08-26 Mallinckrodt Inc. (+)-morphinanium quaternary salts and processes for their production
CN102325777B (en) 2009-02-23 2015-08-12 马林克罗特公司 (+)-morphinan * N-oxide compound and preparation method thereof
US8946419B2 (en) 2009-02-23 2015-02-03 Mallinckrodt Llc (+)-6-hydroxy-morphinan or (+)-6-amino-morphinan derivatives
JP2012518652A (en) 2009-02-23 2012-08-16 マリンクロッド インコーポレイテッド (+)-6-hydroxy-morphinan or (+)-6-amino-morphinan derivatives
WO2010104078A1 (en) 2009-03-10 2010-09-16 第一三共株式会社 Process for producing diamine derivative
CN102348680B (en) 2009-03-13 2014-11-05 第一三共株式会社 Method for producing optically active diamine derivative
JP5824448B2 (en) * 2009-04-24 2015-11-25 ブロック ユニバーシティ Preparation of morphinan and morphinone compounds
WO2010131663A1 (en) * 2009-05-15 2010-11-18 第一三共株式会社 Oxamide derivative
MY155256A (en) 2009-06-18 2015-09-30 Daiichi Sankyo Co Ltd Pharmaceutical composition having improved solubility
CN101845047B (en) * 2009-12-31 2011-12-07 南京臣功制药有限公司 Method for preparing methylnaltrexone bromide
CN107308125B (en) * 2010-03-11 2021-07-16 惠氏有限责任公司 Oral formulations and lipophilic salts of methylnaltrexone
KR101792299B1 (en) 2010-03-19 2017-10-31 다이이찌 산쿄 가부시키가이샤 Method for improving dissolution of anticoagulant agent
BR112012023649B1 (en) 2010-03-19 2021-06-08 Daiichi Sankyo Company, Limited METHOD FOR PRODUCING FORM II CRYSTALS OF N1 -(5-CHLOROPIRIDIN-2-YL)-N2 -((1S,2R,4S)-4-[(DIMETHYLAMINO)CARBONYL]-2-{[(5- METHYL-4,5,6,7-TETRAHYDROTHIAZOLE[5,4-C]PYRIDIN-2-YL) CARBONYL] AMINO}CYCLOHEXYL)ETHANEDIAMIDE P-TOLUENESULFONATE
CA2859191C (en) 2010-07-02 2016-05-17 Daiichi Sankyo Company, Limited Process for preparation of optically active diamine derivative salt
CN102336760B (en) * 2010-07-23 2016-04-06 重庆医药工业研究院有限责任公司 The preparation method of bromized morphinan quaternary ammonium salt
CN102565203B (en) * 2010-12-07 2015-01-07 重庆医药工业研究院有限责任公司 Method for separating and determining methyhaaltrexone bromide and impurities thereof with liquid chromatography
CN102565205B (en) * 2010-12-17 2014-04-09 北大方正集团有限公司 Quality detection method of methyhaaltrexone bromide
CN102558189B (en) * 2010-12-17 2014-09-03 北大方正集团有限公司 Refining method of methyhaaltrexone bromide
CN102558190B (en) * 2010-12-30 2014-10-22 天津康鸿医药科技发展有限公司 (R)-N-brooethyl naltrexone crystal form compound and preparation method, combination and application thereof
KR101940840B1 (en) 2011-08-10 2019-01-21 다이이찌 산쿄 가부시키가이샤 Pharmaceutical composition containing diamine derivative
CN103917543A (en) 2011-09-08 2014-07-09 马林克罗特有限公司 Production of alkaloids without the isolation of intermediates
CN103172640A (en) * 2011-12-22 2013-06-26 天津康鸿医药科技发展有限公司 Preparation method of (R)-N-bromine-methyl naltrexone and naltrexone derivatives
US10485798B2 (en) 2012-08-22 2019-11-26 Aptapharma Inc. Methylnaltrexone nasal formulations, methods of making, and use thereof
US8987289B2 (en) 2012-12-14 2015-03-24 Trevi Therapeutics, Inc. Methods for treating pruritus
US20140179727A1 (en) 2012-12-14 2014-06-26 Trevi Therapeutics, Inc. Methods for treating pruritus
US8637538B1 (en) 2012-12-14 2014-01-28 Trevi Therapeutics, Inc. Methods for treatment of pruritis
WO2015095644A1 (en) 2013-12-20 2015-06-25 AntiOP, Inc. Intranasal naloxone compositions and methods of making and using same
CN104224734A (en) * 2014-08-15 2014-12-24 南京优科生物医药有限公司 Dezocine freeze-dried powder injection and preparation method thereof
CA3002137A1 (en) 2014-10-17 2016-04-21 Salix Pharmaceuticals, Inc. Use of methylnaltrexone to attenuate tumor progression
CN105985348B (en) * 2015-02-12 2019-02-01 正大天晴药业集团股份有限公司 A kind of preparation method of methylnaltrexone bromide
US20160256451A1 (en) * 2015-03-06 2016-09-08 Develco Pharma Schweiz Ag Dosage of naloxone
US20160256453A1 (en) * 2015-03-06 2016-09-08 Develco Pharma Schweiz Ag Opioid receptor antagonist for use in treating patients with severe constipation induced by high opiate dosage regimen
WO2016193456A2 (en) * 2015-06-03 2016-12-08 Develco Pharma Schweiz Ag Opioid receptor antagonist for use in treating patients with severe constipation
CN107782820A (en) * 2016-08-31 2018-03-09 江苏正大丰海制药有限公司 The assay method of genetoxic impurity ethyl p-toluenesulfonate in a kind of brufen
CN112703000A (en) 2018-07-23 2021-04-23 特雷维治疗股份有限公司 Treatment of chronic cough, shortness of breath and dyspnea
MX2021013488A (en) 2019-05-07 2021-12-10 Bausch Health Ireland Ltd Liquid oral dosage formulations of methylnaltrexone.
CA3142214A1 (en) 2019-06-03 2020-12-10 Bausch Health Ireland Limited Use of methylnaltrexone and rifaximin for treatment of increased gut permeability or associated disorders
CN111487336B (en) * 2020-04-13 2022-08-19 司法鉴定科学研究院 Method for analyzing 37 fentanyl novel psychoactive substances in hair
WO2021224138A1 (en) 2020-05-02 2021-11-11 Bausch Health Ireland Limited Methods of reducing mortality risk in subjects suffering from an underlying disease or condition by administration of methylnaltrexone
CN114152699A (en) * 2021-12-22 2022-03-08 北京金城泰尔制药有限公司 Method for determining content of glyceryl monostearate and glyceryl distearate in promestrene cream

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4176186A (en) * 1978-07-28 1979-11-27 Boehringer Ingelheim Gmbh Quaternary derivatives of noroxymorphone which relieve intestinal immobility
WO2004043964A2 (en) * 2002-11-08 2004-05-27 Mallinckrodt Inc. Process for the preparation of quaternary n-alkyl morphinan alkaloid salts

Family Cites Families (254)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1420015B1 (en) * 1959-10-16 1971-08-26 Boehringer Sohn Ingelheim 2'-Hydroxy-5,9-dimethyl-6,7-benzomorphane
GB1202148A (en) 1968-03-06 1970-08-12 Sankyo Co Pharmaceutical compositions
US3854480A (en) 1969-04-01 1974-12-17 Alza Corp Drug-delivery system
US3884916A (en) * 1971-03-30 1975-05-20 Janssen Pharmaceutica Nv 2,2-Diaryl-4-(4-aryl-4-hydroxy-piperidino)-butyramides
US3714159A (en) * 1971-03-30 1973-01-30 Janssen Pharmaceutica Nv 2,2-diaryl-4-(4'-aryl-4'-hydroxy-piper-idino)-butyramides
US4025652A (en) 1975-03-31 1977-05-24 William H. Rorer, Inc. Amidinoureas
US4326074A (en) * 1972-09-22 1982-04-20 William H. Rorer, Inc. Amidinoureas
US3937801A (en) * 1973-07-10 1976-02-10 American Home Products Corporation Reducing the incidence of gastrointestinal side effects during the treatment of inflammatory conditions with antiinflammatory drugs
US4060635A (en) 1975-03-31 1977-11-29 William H. Rorer, Inc. Amidinoureas for treating diarrhea
US4203920A (en) * 1975-03-31 1980-05-20 William H. Rorer, Inc. Amidinoureas
US4072686A (en) * 1975-04-16 1978-02-07 G. D. Searle & Co. 1-(3,3,3-Triarylalkyl)-4-phenyl-piperidinealkanols
US4066654A (en) * 1975-04-16 1978-01-03 G. D. Searle & Co. 1-triarylalkyl-4-phenyl-4-piperidine carboxylic acids and derivatives
US3996214A (en) 1976-02-23 1976-12-07 G. D. Searle & Co. 5-(1,1-Diphenyl-4-(cyclic amino) but-2-trans-en-1-yl)-2-alkyl-1,3,4-oxadiazoles and intermediates thereto
US4013668A (en) * 1976-03-10 1977-03-22 G. D. Searle & Co. 5-(1,1-diphenyl-3-(5- or 6-hydroxy-2-azabicyclo(2.2.2)oct-2-yl)propyl)-2-alkyl-1,3,4-oxadiazoles and related compounds
US4012393A (en) * 1976-03-22 1977-03-15 G. D. Searle & Co. 2-[5-(CYCLIC AMINO) ETHYL-10,11-DIHYDRO-5H-dibenzo[a,d]-cyclohepten-5- yl]-5
US4115400A (en) 1976-05-27 1978-09-19 Eli Lilly And Company 1-Azoniabicyclo[3.1.0]hexanes
GB1593191A (en) 1977-03-23 1981-07-15 Reckitt & Colmann Prod Ltd Derivatives of morphine
US4125531A (en) 1977-04-18 1978-11-14 G. D. Searle & Co. 2-Substituted-1-azabicyclo[2.2.2]octanes
US4069223A (en) * 1977-05-02 1978-01-17 G. D. Searle & Co. 4-Aminomethyl-1-(3,3,3-triarylpropyl)-4-arylpiperidine and derivatives thereof
US4116963A (en) 1977-05-23 1978-09-26 G.D. Searle & Co. 3,3,3-triarylalkyl-4-phenylalkyl-4-hydroxy piperidines and related compounds
US4194045A (en) * 1977-12-27 1980-03-18 G. D. Searle & Co. 1-(3,3-Diaryl-3-oxadiazolalkyl)-4-phenyl-4-piperidinomethanols and related compounds
JPS5535031A (en) * 1978-09-04 1980-03-11 Shin Etsu Chem Co Ltd Enteric coating composition
US4311833A (en) * 1979-03-06 1982-01-19 Daicel Chemical Industries Ltd. Process for preparing ethylcarboxymethylcellulose
US4277605A (en) 1980-03-07 1981-07-07 Bristol-Myers Company Chemical compounds
US4322426A (en) * 1980-04-28 1982-03-30 E. I. Du Pont De Nemours And Company 17-Substituted-6-desoxy-7,8-dihydro-6α-methylnoroxymorphone narcotic antagonists
US4675189A (en) 1980-11-18 1987-06-23 Syntex (U.S.A.) Inc. Microencapsulation of water soluble active polypeptides
US4466968A (en) 1980-11-24 1984-08-21 Dermall, Ltd. Method for prophylaxis or treatment of emesis and nausea
US4427676A (en) * 1980-12-19 1984-01-24 John Wyeth & Brother Ltd. Thiomorpholine derivatives
US4377568A (en) * 1981-08-12 1983-03-22 Merck Sharp & Dohme (I.A.) Corp. Preparation of aqueous alcoholic dispersions of pH sensitive polymers and plasticizing agents and a method of enteric coating dosage forms using same
DK150008C (en) * 1981-11-20 1987-05-25 Benzon As Alfred PROCEDURE FOR THE PREPARATION OF A PHARMACEUTICAL ORAL POLYDEPOT PREPARATION
US4987136A (en) * 1982-03-16 1991-01-22 The Rockefeller University Method for controlling gastrointestinal dysmotility
EP0103636B1 (en) 1982-03-16 1990-09-12 Rockefeller University Use of opium antagonists for the manufacture of medicaments for controlling gastrointestinal dysmotility
US4870084A (en) 1982-03-16 1989-09-26 Pfizer Inc. Bicyclic benzo fused pyran compounds used for nausea treatment and prevention
JPS58142090U (en) 1982-03-20 1983-09-24 幸和産業株式会社 Interlocking prize ball feeder for pachinko machines
US4430327A (en) * 1982-05-18 1984-02-07 Eli Lilly And Company Method for treating pregnant females for pain and anxiety
US4457907A (en) * 1982-08-05 1984-07-03 Clear Lake Development Group Composition and method for protecting a therapeutic drug
US4533739A (en) 1982-10-12 1985-08-06 G. D. Searle & Co. 2-[(Aminophenyl and amidophenyl)amino]-1-azacycloalkanes having antidiarrheal activity
US4518433A (en) * 1982-11-08 1985-05-21 Fmc Corporation Enteric coating for pharmaceutical dosage forms
US4452775A (en) 1982-12-03 1984-06-05 Syntex (U.S.A.) Inc. Cholesterol matrix delivery system for sustained release of macromolecules
US4462839A (en) * 1983-06-16 1984-07-31 Fmc Corporation Enteric coating for pharmaceutical dosage forms
US4556552A (en) 1983-09-19 1985-12-03 Colorcon, Inc. Enteric film-coating compositions
EP0143949B1 (en) * 1983-11-01 1988-10-12 TERUMO KABUSHIKI KAISHA trading as TERUMO CORPORATION Pharmaceutical composition containing urokinase
US4689332A (en) 1984-04-09 1987-08-25 Research Corporation Growth regulation and related applications of opioid antagonists
US5266574A (en) * 1984-04-09 1993-11-30 Ian S. Zagon Growth regulation and related applications of opioid antagonists
US4666716A (en) 1984-09-04 1987-05-19 Richardson-Vicks Inc. Antidiarrheal compositions and use thereof
JPS6229515A (en) * 1985-07-30 1987-02-07 Shinjiro Tsuji Method for film-coating of hard capsule
JPH0676314B2 (en) 1985-09-30 1994-09-28 花王株式会社 Suppository base and suppository
US4824853A (en) * 1985-10-11 1989-04-25 Janssen Pharmaceutica N.V. α,α-diaryl-4-aryl-4-hydroxy-1-piperidinebutanamide, N-oxides and method of treating diarrhea
US4806556A (en) * 1985-12-12 1989-02-21 Regents Of The University Of Minnesota Gut-selective opiates
US4730048A (en) * 1985-12-12 1988-03-08 Regents Of The University Of Minnesota Gut-selective opiates
US4861781A (en) * 1986-03-07 1989-08-29 The University Of Chicago Quaternary derivatives of noroxymorphone which relieve nausea and emesis
US4719215A (en) 1986-03-07 1988-01-12 University Of Chicago Quaternary derivatives of noroxymorphone which relieve nausea and emesis
DE3609073C2 (en) 1986-03-18 1995-08-10 Hans J Prof Dr Rer Nat Schmitt Measuring device for non-invasive detection of peripheral drainage and flow disorders in human extremities
US4990521A (en) * 1986-07-03 1991-02-05 Janssen Pharmaceutica 4-(aroylamino)piperidine-butanimide derivatives
EP0319545B1 (en) * 1986-08-28 1992-03-18 Enzacor Properties Limited Animal growth promotant
US5597564A (en) * 1986-08-28 1997-01-28 Enzacor Properties Limited Method of administering a microgranular preparation to the intestinal region of animals
US4888346A (en) * 1986-10-07 1989-12-19 Bernard Bihari Method for the treatment of persons infected with HTLV-III (AIDS) virus
US4765978A (en) 1986-12-16 1988-08-23 Schering Corporation Novel vaginal suppository
FR2609632B1 (en) 1987-01-21 1991-03-29 Shelly Marc NOVEL THERAPEUTIC APPLICATION OF 17- (CYCLOPROPYLMETHYL) -4,5-EPOXY-3,14-DIHYDROXYMORPHINON-6-ONE AND PHARMACEUTICAL COMPOSITIONS FOR THIS USE
NL8700842A (en) 1987-04-10 1988-11-01 Duphar Int Res
US4891379A (en) * 1987-04-16 1990-01-02 Kabushiki Kaisha Kobe Seikosho Piperidine opioid antagonists
US4857833A (en) * 1987-08-27 1989-08-15 Teradyne, Inc. Diagnosis of faults on circuit board
CA1315689C (en) 1987-09-03 1993-04-06 Leon I. Goldberg Quarternary derivatives of noroxymorphone which relieve nausea and emesis
ES2051742T3 (en) 1987-09-10 1994-07-01 Univ Chicago QUARTERLY DERIVATIVES OF NOROXI-MORPHINE THAT MITIGATE NAUSEA AND EMESIS.
US4912114A (en) * 1988-03-18 1990-03-27 Sandoz Ltd. Morphinan derivatives
ES2085865T3 (en) * 1988-06-30 1996-06-16 Astra Ab DERMORPHINE ANALOGS, THEIR PREPARATION METHODS, PHARMACEUTICAL COMPOSITIONS, AND THERAPEUTIC TREATMENT METHODS THAT USE THEM.
EP0352361A1 (en) 1988-07-29 1990-01-31 The Rockefeller University Method of treating patients suffering from chronic pain or chronic cough
US4999342A (en) 1988-08-16 1991-03-12 Ortho Pharmaceutical Corporation Long lasting contraceptive suppository composition and methods of use
US4857533A (en) 1988-12-15 1989-08-15 Baker Cummins Pharmaceuticals, Inc. Method of treatment for autoimmune diseases
US4863928A (en) 1989-01-04 1989-09-05 Baker Cummins Pharmaceuticals, Inc. Method of treatment for arthritic and inflammatory diseases
US5102887A (en) * 1989-02-17 1992-04-07 Arch Development Corporation Method for reducing emesis and nausea induced by the administration of an emesis causing agent
US5116868A (en) 1989-05-03 1992-05-26 The Johns Hopkins University Effective ophthalmic irrigation solution
US5133974A (en) 1989-05-05 1992-07-28 Kv Pharmaceutical Company Extended release pharmaceutical formulations
US4965269A (en) * 1989-12-20 1990-10-23 Ab Hassle Therapeutically active chloro substituted benzimidazoles
US5236947A (en) 1990-02-28 1993-08-17 Jouveinal S.A. Propanamines, their pharmacological properties and their application as an antidiarrheal
JPH0813748B2 (en) 1990-04-23 1996-02-14 帝國製薬株式会社 Colon disintegrating polypeptide oral preparation
KR970005839B1 (en) 1990-05-11 1997-04-21 화이자 인코포레이티드 Synergistic therapeutic composition and method
US5366979A (en) * 1990-06-07 1994-11-22 Pharmaco Development Partners Orally active nonaddicting analgesics
JP3160862B2 (en) 1990-11-15 2001-04-25 雪印乳業株式会社 Bone-fortified foods, feeds and pharmaceuticals
JPH04230625A (en) * 1990-12-27 1992-08-19 Standard Chem & Pharmaceut Corp Ltd Method for production of finely dispersed tablet composition consisting of microcapsule containing sprayed and dried sodium dichlofenac and having enteric coating
EP0573565B1 (en) 1991-02-25 2000-07-19 Trustees Of Boston University Opiate receptor antagonist modulates hyperkinetic movement disorder
JP2916290B2 (en) 1991-03-22 1999-07-05 帝國製薬株式会社 Colon-disintegrating oral preparation containing bioactive polypeptide
US5250542A (en) 1991-03-29 1993-10-05 Eli Lilly And Company Peripherally selective piperidine carboxylate opioid antagonists
CA2064373C (en) 1991-03-29 2005-08-23 Buddy Eugene Cantrell Piperidine derivatives
US5159081A (en) 1991-03-29 1992-10-27 Eli Lilly And Company Intermediates of peripherally selective n-carbonyl-3,4,4-trisubstituted piperidine opioid antagonists
US5270328A (en) * 1991-03-29 1993-12-14 Eli Lilly And Company Peripherally selective piperidine opioid antagonists
US5220017A (en) 1991-04-10 1993-06-15 Merck & Co., Inc. Cholecystokinin antagonists
EP0590060B1 (en) * 1991-06-21 1997-09-17 University Of Cincinnati Orally administrable therapeutic proteins and method of making
JPH0550863A (en) 1991-08-19 1993-03-02 Aisin Aw Co Ltd Electric motor device for vehicle
US5407686A (en) * 1991-11-27 1995-04-18 Sidmak Laboratories, Inc. Sustained release composition for oral administration of active ingredient
US5614219A (en) * 1991-12-05 1997-03-25 Alfatec-Pharma Gmbh Oral administration form for peptide pharmaceutical substances, in particular insulin
US5256154A (en) 1992-01-31 1993-10-26 Sterling Winthrop, Inc. Pre-filled plastic syringes and containers and method of terminal sterilization thereof
JPH05213763A (en) 1992-02-10 1993-08-24 Sanwa Kagaku Kenkyusho Co Ltd Readily absorbable activated calcium preparation
NL9220019A (en) 1992-04-10 1994-04-05 Vnii Med Polimerov PHARMACEUTICAL COMPOSITION.
US5686072A (en) 1992-06-17 1997-11-11 Board Of Regents, The University Of Texas Epitope-specific monoclonal antibodies and immunotoxins and uses thereof
US6096756A (en) * 1992-09-21 2000-08-01 Albert Einstein College Of Medicine Of Yeshiva University Method of simultaneously enhancing analgesic potency and attenuating dependence liability caused by morphine and other bimodally-acting opioid agonists
US5512578A (en) 1992-09-21 1996-04-30 Albert Einstein College Of Medicine Of Yeshiva University, A Division Of Yeshiva University Method of simultaneously enhancing analgesic potency and attenuating dependence liability caused by exogenous and endogenous opiod agonists
USRE36547E (en) * 1992-09-21 2000-02-01 Albert Einstein College Of Medicine Of Yeshiva University Method of simultaneously enhancing analgesic potency and attenuating dependence liability caused by exogenous and endogenous opioid agonists
US5580876A (en) 1992-09-21 1996-12-03 Albert Einstein College Of Medicine Of Yeshiva University, A Division Of Yeshiva University Method of simultaneously enhancing analgesic potency and attenuating dependence liability caused by morphine and other bimodally-acting opioid agonists
US5472943A (en) * 1992-09-21 1995-12-05 Albert Einstein College Of Medicine Of Yeshiva University, Method of simultaneously enhancing analgesic potency and attenuating dependence liability caused by morphine and other opioid agonists
BR9207175A (en) 1992-10-28 1995-12-12 Genentech Inc Composition containing vascular endothelial cell growth factor antagonist polypeptide monoclonal antibody amino acid sequence and method of treatment of tumor in mammal
ES2095001T5 (en) * 1992-12-22 2001-03-16 Univ Cincinnati AN ORALALLY ADMINISTRABLE THERAPEUTIC COMPOSITION AND ITS METHOD OF OBTAINING.
DE4303214A1 (en) 1993-02-04 1994-08-11 Wolfgang Marks Treatment of diseases of viral, viroidal or oncogenic origin by steroid saponins or their aglycones
US5585348A (en) 1993-02-10 1996-12-17 Albert Einstein College Of Medicine Of Yeshiva University, A Division Of Yeshiva University Use of excitatory opioid receptor antagonists to prevent growth factor-induced hyperalgesia
US5656290A (en) * 1993-02-26 1997-08-12 The Procter & Gamble Company Bisacodyl dosage form with multiple enteric polymer coatings for colonic delivery
US5391372A (en) 1993-06-28 1995-02-21 Campbell; Elizabeth Methods of treating colic and founder in horses
WO1995003308A1 (en) 1993-07-23 1995-02-02 Toray Industries, Inc. Morphinan derivative and medicinal use
GB2281205A (en) 1993-08-24 1995-03-01 Euro Celtique Sa Oral opioid analgesic
SE9303744D0 (en) * 1993-11-12 1993-11-12 Astra Ab Pharmaceutical emulsion
US5434171A (en) 1993-12-08 1995-07-18 Eli Lilly And Company Preparation of 3,4,4-trisubstituted-piperidinyl-N-alkylcarboxylates and intermediates
US6190691B1 (en) * 1994-04-12 2001-02-20 Adolor Corporation Methods for treating inflammatory conditions
AU2360195A (en) * 1994-05-05 1995-11-29 Beckman Instruments, Inc. Oligonucleotide repeat arrays
IT1269826B (en) 1994-05-24 1997-04-15 Paolo Minoia USE OF OPTIACEAN ANTAGONISTS AND CALCIUM SALTS FOR THE PREPARATION OF MEDICATIONS FOR THE TREATMENT OF ENDORPHINE-MEDIATED PATHOLOGICAL FORMS
US5536507A (en) * 1994-06-24 1996-07-16 Bristol-Myers Squibb Company Colonic drug delivery system
US5866154A (en) * 1994-10-07 1999-02-02 The Dupont Merck Pharmaceutical Company Stabilized naloxone formulations
US5614222A (en) * 1994-10-25 1997-03-25 Kaplan; Milton R. Stable aqueous drug suspensions and methods for preparation thereof
US5965161A (en) * 1994-11-04 1999-10-12 Euro-Celtique, S.A. Extruded multi-particulates
US5578725A (en) 1995-01-30 1996-11-26 Regents Of The University Of Minnesota Delta opioid receptor antagonists
ES2094694B1 (en) * 1995-02-01 1997-12-16 Esteve Quimica Sa NEW PHARMACEUTICALLY STABLE FORMULATION OF A COMPOUND OF BENZMIDAZOLE AND ITS PROCESS OF OBTAINING.
US6096763A (en) 1995-02-23 2000-08-01 Merck & Co., Inc. α1a adrenergic receptor antagonists
US6025154A (en) * 1995-06-06 2000-02-15 Human Genome Sciences, Inc. Polynucleotides encoding human G-protein chemokine receptor HDGNR10
US5714586A (en) * 1995-06-07 1998-02-03 American Cyanamid Company Methods for the preparation of monomeric calicheamicin derivative/carrier conjugates
US5821219A (en) 1995-08-11 1998-10-13 Oregon Health Sciences University Opioid antagonists and methods of their use
GB9517001D0 (en) 1995-08-18 1995-10-18 Denny William Enediyne compounds
US5804595A (en) * 1995-12-05 1998-09-08 Regents Of The University Of Minnesota Kappa opioid receptor agonists
ATE208760T1 (en) 1995-12-21 2001-11-15 Syngenta Participations Ag 3-AMINO-2-MERCAPTOBENZOIC ACID DERIVATIVES AND METHOD FOR THE PRODUCTION THEREOF
DE69725345T2 (en) 1996-02-15 2004-08-19 Janssen Pharmaceutica N.V. USE OF 5-HT4 ANTAGONISTS TO OVERCOME THE GASTROINTESTINAL DAMAGE CAUSED BY SEROTONIN REINVISION INHIBITORS
ES2168610T3 (en) 1996-03-12 2002-06-16 Alza Corp COMPOSITION AND GALENIC FORM CONTAINING AN OPIOID ANTAGONIST.
US6136780A (en) 1996-03-29 2000-10-24 The Penn State Research Foundation Control of cancer growth through the interaction of [Met5 ]-enkephalin and the zeta (ζ) receptor
US20040024006A1 (en) * 1996-05-06 2004-02-05 Simon David Lew Opioid pharmaceutical compositions
DE19651551C2 (en) 1996-12-11 2000-02-03 Klinge Co Chem Pharm Fab Opioid antagonist-containing galenic formulation
US20010036469A1 (en) 1997-01-13 2001-11-01 Gooberman Lance L. Opiate antagonist implant and process for preparation therefor
US6884879B1 (en) * 1997-04-07 2005-04-26 Genentech, Inc. Anti-VEGF antibodies
GB9801231D0 (en) * 1997-06-05 1998-03-18 Merck & Co Inc A method of treating cancer
HU9701081D0 (en) * 1997-06-23 1997-08-28 Gene Research Lab Inc N Pharmaceutical composition of antitumoral activity
US6525038B1 (en) * 1997-06-24 2003-02-25 Werner Kreutz Synergistic compositions for the selective control of tumor tissue
US6353004B1 (en) * 1997-07-14 2002-03-05 Adolor Coporation Peripherally acting anti-pruritic opiates
US6096764A (en) 1997-08-21 2000-08-01 Eli Lilly And Company Methods for inhibiting detrimental side-effects due to GnRH of GnRH agonist administration
US6099853A (en) 1997-09-04 2000-08-08 Protein Express Vaginal suppository vaccine for urogenital infections
US6559158B1 (en) 1997-11-03 2003-05-06 Ur Labs, Inc. Use of methylnaltrexone and related compounds to treat chronic opioid use side affects
AU2003204844B2 (en) 1997-11-03 2007-06-07 Arch Development Corporation Use of methylnaltrexone and related compounds
US6274591B1 (en) * 1997-11-03 2001-08-14 Joseph F. Foss Use of methylnaltrexone and related compounds
US5972954A (en) 1997-11-03 1999-10-26 Arch Development Corporation Use of methylnaltrexone and related compounds
US20030158220A1 (en) * 1997-11-03 2003-08-21 Foss Joseph F. Use of methylnaltrexone and related compounds to treat chronic opioid use side effects
US6777534B1 (en) 1997-12-09 2004-08-17 Children's Medical Center Corporation Peptide antagonists of vascular endothelial growth factor
SI2266564T1 (en) * 1997-12-22 2013-07-31 Euro-Celtique S.A. Pharmaceutical oral dosage form comprising a combination of an opioid agonist and an opioid antagonist
EP0930334A1 (en) 1998-01-16 1999-07-21 Quest International B.V. Polysaccharide conjugate capable of binding cellulose
GB9802251D0 (en) 1998-02-03 1998-04-01 Ciba Geigy Ag Organic compounds
CN1140272C (en) * 1998-04-03 2004-03-03 味之素株式会社 Antitumor agents
US6359111B1 (en) * 1998-05-28 2002-03-19 Neorx Corporation Opioid receptor targeting
HN1999000149A (en) * 1998-09-09 2000-01-12 Pfizer Prod Inc DERIVATIVES OF 4,4-BIARILPIPERIDINA
US20010010919A1 (en) 1998-10-13 2001-08-02 David K. Grandy Opioid antagonists and methods of their use
US6194382B1 (en) * 1999-03-03 2001-02-27 Albert Einstein College Of Medicine Of Yeshiva University Method and composition for treating irritable bowel syndrome using low doses of opioid receptor antagonists
JP4049477B2 (en) 1999-03-23 2008-02-20 大鵬薬品工業株式会社 Side effect reducing agent
US7129265B2 (en) 1999-04-23 2006-10-31 Mason R Preston Synergistic effects of amlodipine and atorvastatin metabolite as a basis for combination therapy
US6171620B1 (en) 1999-04-27 2001-01-09 Health Research, Inc. Method of enhancing the efficacy of anti-tumor agents
AU4564200A (en) 1999-04-29 2000-11-17 Aventis Pharma S.A. Method for treating cancer using camptothecin derivatives and 5-fluorouracil
US6833349B2 (en) 1999-06-08 2004-12-21 Regeneron Pharmaceuticals, Inc. Methods of treating inflammatory skin diseases
US20020068712A1 (en) 1999-07-23 2002-06-06 Troy Stevens Use of decreasing levels of functional transient receptor potential gene product
US20030105121A1 (en) 1999-07-27 2003-06-05 Bernard Bihari Method of preventing lipodystrophy syndrome or reversing a pre-existing syndrome in HIV-infected patients being treated with antiretroviral agents
AU6934400A (en) 1999-08-25 2001-03-19 Barrett R. Cooper Compositions and methods for treating opiate intolerance
NZ517559A (en) 1999-08-31 2004-08-27 Gruenenthal Chemie Sustained release pharmaceutical composition containing tramadol saccharinate
US6451806B2 (en) * 1999-09-29 2002-09-17 Adolor Corporation Methods and compositions involving opioids and antagonists thereof
ATE275402T1 (en) 1999-11-01 2004-09-15 John Rhodes MEDICINAL PRODUCTS FOR THE TREATMENT OF INTESTINAL CONSTITUTION AND irritable colon
EP1097720B1 (en) * 1999-11-04 2005-10-12 Institut Gustave Roussy Antiviral agent in combination with radiation therapy for use in treatment of cancer
MXPA02005336A (en) 1999-11-29 2003-01-28 Adolor Corp Novel methods for the treatment and prevention of ileus.
US6384044B1 (en) 1999-11-29 2002-05-07 Bernard Bihari Method of treating cancer of the prostate
PT1244447E (en) 1999-11-29 2007-02-28 Adolor Corp Novel methods and compositions involving opioids and antagonists thereof
WO2001041705A2 (en) 1999-11-29 2001-06-14 Adolor Corporation Novel methods for the treatment and prevention of dizziness and pruritus
US6469030B2 (en) 1999-11-29 2002-10-22 Adolor Corporation Methods for the treatment and prevention of ileus
US6545010B2 (en) 2000-03-17 2003-04-08 Aventis Pharma S.A. Composition comprising camptothecin or a camptothecin derivative and a platin derivative for the treatment of cancer
US20010046968A1 (en) 2000-03-23 2001-11-29 Zagon Ian S. Opioid growth factor modulates angiogenesis
US6967075B2 (en) * 2000-04-07 2005-11-22 Schering Corporation HCV replicase complexes
CA2408106A1 (en) 2000-05-05 2001-11-15 Pain Therapeutics, Inc. Opioid antagonist compositions and dosage forms
DE60139689D1 (en) * 2000-06-22 2009-10-08 Univ Iowa Res Found Combination of CpG and antibodies against CD19, CD20, CD22 or CD40 for the prevention or treatment of cancer.
EP1175905A1 (en) 2000-07-24 2002-01-30 Societe Des Produits Nestle S.A. Nutritional Composition
FI116089B (en) * 2000-07-27 2005-09-15 Johan Tore Karlstroem Device and procedures for controls
EP1307264B1 (en) 2000-07-28 2004-10-20 F. Hoffmann-La Roche Ag New pharmaceutical composition
NZ507152A (en) * 2000-09-27 2001-06-29 Hiltive Pty Ltd Wall cladding assembly with cladding having recesses along opposite sides to engage with flanges of support members
AU2002249885A1 (en) 2000-11-17 2002-08-12 Adolor Corporation Delta agonist analgesics
US6967016B2 (en) 2000-12-04 2005-11-22 Primagen Holding B.V. Method of determining therapeutic activity and/or possible side-effects of a medicament
MXPA03005135A (en) 2000-12-13 2003-12-04 Lilly Co Eli Chronic treatment regimen using glucagon-like insulinotropic peptides.
US6693125B2 (en) * 2001-01-24 2004-02-17 Combinatorx Incorporated Combinations of drugs (e.g., a benzimidazole and pentamidine) for the treatment of neoplastic disorders
TW574512B (en) * 2001-03-14 2004-02-01 Koninkl Philips Electronics Nv Electrophoretic display device
MXPA03008623A (en) 2001-03-23 2004-05-21 Shire Biochem Inc Pharmaceutical combinations for the treatment of cancer.
US20040242523A1 (en) 2003-03-06 2004-12-02 Ana-Farber Cancer Institue And The Univiersity Of Chicago Chemo-inducible cancer gene therapy
WO2002080987A1 (en) 2001-04-09 2002-10-17 Progenics Pharmaceuticals, Inc. Anti-cd19 immunotoxins
BR0209198A (en) * 2001-04-26 2004-06-08 Control Delivery Sys Inc Synthesis methods of phenol-containing compounds
US20030022909A1 (en) 2001-06-05 2003-01-30 University Of Chicago Use of methylnaltrexone to treat immune suppression
US8012517B2 (en) 2001-08-31 2011-09-06 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Inhibition of angiogenesis and destruction of angiogenic vessels with extracts of noni juice Morinda citrifolia
DK2939696T3 (en) 2001-10-18 2016-05-23 Nektar Therapeutics Polymer Conjugates of Opioid Antagonists
US20030144312A1 (en) 2001-10-30 2003-07-31 Schoenhard Grant L. Inhibitors of ABC drug transporters in multidrug resistant cancer cells
WO2003037365A1 (en) * 2001-11-01 2003-05-08 The Johns Hopkins University Methods and compositions for treating vascular leak using hepatocyte growth factor
WO2003059904A1 (en) * 2001-12-21 2003-07-24 Merck & Co., Inc. Heteroaryl substituted pyrrole modulators of metabotropic glutamate receptor-5
US20050011468A1 (en) * 2002-02-04 2005-01-20 Jonathan Moss Use of methylnaltrexone in treating gastrointestinal dysfunction in equines
CA2475305A1 (en) 2002-02-04 2004-02-19 Jonathan Moss Use of methylnaltrexone in treating gastrointestinal dysfunction in equines
EP2319540A1 (en) * 2002-02-22 2011-05-11 Shire LLC Sustained release pharmaceutical compounds to prevent abuse of controlled substances
US7074825B2 (en) 2002-03-07 2006-07-11 Huanbiao Mo Composition and method for treating cancer
CN1652752A (en) 2002-03-14 2005-08-10 欧罗赛铁克股份有限公司 Naltrexone hydrochloride compositions
US20030191147A1 (en) * 2002-04-09 2003-10-09 Barry Sherman Opioid antagonist compositions and dosage forms
US7355081B2 (en) 2002-04-17 2008-04-08 The University Of North Carolina At Chapel Hill Curcumin analogues and uses thereof
US7329642B2 (en) 2002-05-17 2008-02-12 Board Of Regents, University Of Texas System β-2-glycoprotein is an inhibitor of angiogenesis
US7012100B1 (en) * 2002-06-04 2006-03-14 Avolix Pharmaceuticals, Inc. Cell migration inhibiting compositions and methods and compositions for treating cancer
US6986901B2 (en) * 2002-07-15 2006-01-17 Warner-Lambert Company Llc Gastrointestinal compositions
US20040010997A1 (en) * 2002-07-17 2004-01-22 Oren Close Guides to align masonry walls defining apertures, and methods of use
US7160913B2 (en) * 2002-09-13 2007-01-09 Thomas Jefferson University Methods and kit for treating Parkinson's disease
US7691374B2 (en) * 2002-10-23 2010-04-06 Health Research, Inc. Method for increasing the efficacy of anti-tumor agents by anti-endoglin antibody
WO2004054511A2 (en) 2002-12-13 2004-07-01 The Regents Of The University Of California Analgesic combination comprising nalbuphine
WO2004054569A1 (en) * 2002-12-16 2004-07-01 Council Of Scientific And Industrial Research Pharmaceutical composition containing brevifoliol for use in chemotherapeutic treatment of human beings
JP2006519855A (en) 2003-03-07 2006-08-31 イーライ リリー アンド カンパニー Opioid receptor antagonist
RU2005134364A (en) 2003-04-08 2006-06-10 Проджиникс Фармасьютикалз, Инк. (Us) COMBINED TREATMENT FOR CONSTIPATION
US20050004155A1 (en) 2003-04-08 2005-01-06 Boyd Thomas A. Use of methylnaltrexone to treat irritable bowel syndrome
DK2368553T3 (en) 2003-04-08 2015-02-09 Progenics Pharm Inc Pharmaceutical preparation comprising methylnaltrexone
KR101167579B1 (en) 2003-04-29 2012-07-27 오렉시젠 세러퓨틱스 인크. Compositions for affecting weight loss
US6992193B2 (en) 2003-06-10 2006-01-31 Adolor Corporation Sulfonylamino phenylacetamide derivatives and methods of their use
CA2529307C (en) * 2003-06-13 2013-12-24 Microbia, Inc. Methods and compositions for the treatment of gastrointestinal disorders
US7494979B2 (en) 2003-06-13 2009-02-24 Ironwood Pharmaceuticals, Inc. Method for treating congestive heart failure and other disorders
AU2003903387A0 (en) 2003-07-02 2003-07-17 Sirtex Medical Limited Combination therapy for treatment of neoplasia
EP1682006A4 (en) * 2003-10-29 2011-01-26 Physiosonics Inc Method and apparatus for determining an ultrasound fluid flow centerline
US6984403B2 (en) * 2003-12-04 2006-01-10 Pfizer Inc. Azithromycin dosage forms with reduced side effects
US8946262B2 (en) 2003-12-04 2015-02-03 Adolor Corporation Methods of preventing and treating gastrointestinal dysfunction
US20070082044A1 (en) * 2004-03-10 2007-04-12 Trustees Of Tufts College Synergistic effect of compositions comprising carotenoids selected from lutein, beta-carotene and lycopene
TW200533339A (en) 2004-03-16 2005-10-16 Bristol Myers Squibb Co Therapeutic synergy of anti-cancer compounds
US6946556B1 (en) 2004-05-21 2005-09-20 Acura Pharmaceuticals, Inc. Preparation of opioid analgesics by a one-pot process
US7725072B2 (en) * 2004-06-30 2010-05-25 Glenayre Electronics, Inc. Provision of messaging services from a video messaging system based on ANI and CLID
US7094775B2 (en) 2004-06-30 2006-08-22 Bone Care International, Llc Method of treating breast cancer using a combination of vitamin D analogues and other agents
US7388008B2 (en) * 2004-08-02 2008-06-17 Ambrilia Biopharma Inc. Lysine based compounds
US20060063792A1 (en) * 2004-09-17 2006-03-23 Adolor Corporation Substituted morphinans and methods of their use
US20060204512A1 (en) 2004-09-23 2006-09-14 Vasgene Therapeutics, Inc. Polypeptide compounds for inhibiting angiogenesis and tumor growth
CN101061073A (en) 2004-09-30 2007-10-24 贝克顿·迪金森公司 Method for reducing or eliminating residue in a glass medical container and container made in accordance therewith
BRPI0606587A2 (en) * 2005-01-20 2009-07-07 Progenics Pharmaceuticais Inc use of methylnaltrexone and related compounds to treat postoperative gastrointestinal dysfunction
US8524731B2 (en) 2005-03-07 2013-09-03 The University Of Chicago Use of opioid antagonists to attenuate endothelial cell proliferation and migration
CN101171010B (en) 2005-03-07 2014-09-17 芝加哥大学 Use of opioid antagonists to attenuate endothelial cell proliferation and migration
AR057035A1 (en) 2005-05-25 2007-11-14 Progenics Pharm Inc SYNTHESIS OF (R) -N-METHYLNTREXONE, PHARMACEUTICAL COMPOSITIONS AND USES
AR057325A1 (en) 2005-05-25 2007-11-28 Progenics Pharm Inc SYNTHESIS OF (S) -N-METHYLNTREXONE, PHARMACEUTICAL COMPOSITIONS AND USES
WO2007053194A2 (en) 2005-06-03 2007-05-10 The University Of Chicago Modulation of cell barrier dysfunction
CA2610951A1 (en) 2005-06-03 2006-12-14 The University Of Chicago Modulation of microbial pathogen-host cell interactions
US20080194611A1 (en) 2005-06-03 2008-08-14 Alverdy John C Modulation of Cell Barrier Dysfunction
CA2611105A1 (en) 2005-06-09 2006-12-21 Mallinckrodt Inc. Method for separation and purification of naltrexone by preparative chromatography
PE20070207A1 (en) * 2005-07-22 2007-03-09 Genentech Inc COMBINED TREATMENT OF TUMORS THAT EXPRESS HER
CA2627158A1 (en) * 2005-08-30 2007-03-08 Queen's University At Kingston Potentiation of the therapeutic action of an opioid receptor agonist and/or inhibition or reversal of tolerance to an opioid receptoi agonists using an ultralow dose of an alpha-2receptor antagonist
PL116330U1 (en) 2005-10-31 2007-04-02 Alza Corp Method for the reduction of alcohol provoked rapid increase in the released dose of the orally administered opioide with prolonged liberation
US20070259939A1 (en) 2006-05-04 2007-11-08 Accelerated Technologies Using naltrexone as a multi-purpose health supplement to improve the human condition and preventing multiple diseases and infirmities by stimulating immune system vitality and robustness
WO2008011596A2 (en) * 2006-07-21 2008-01-24 Lab International Srl Hydrophilic abuse deterrent delivery system
TW200815451A (en) 2006-08-04 2008-04-01 Wyeth Corp 6-carboxy-normorphinan derivatives, synthesis and uses thereof
TWI489984B (en) 2006-08-04 2015-07-01 Wyeth Corp Formulations for parenteral delivery of compounds and uses thereof
TW200817048A (en) 2006-09-08 2008-04-16 Wyeth Corp Dry powder compound formulations and uses thereof
CA2670136A1 (en) 2006-11-22 2008-05-29 Progenics Pharmaceuticals, Inc. 7,8-saturated-4,5-epoxy-morphinanium analogs
WO2008064150A1 (en) 2006-11-22 2008-05-29 Progenics Pharmaceuticals, Inc. Processes for synthesizing quaternary 4,5-epoxy-morphinan analogs and isolating their n-stereoisomers
US20080234306A1 (en) 2006-11-22 2008-09-25 Progenics Pharmaceuticals, Inc. N-Oxides of 4,5-Epoxy-Morphinanium Analogs
HUE025662T2 (en) 2007-03-29 2016-04-28 Wyeth Llc Peripheral opioid receptor and antagonists and uses thereof
CA2865389A1 (en) 2007-03-29 2008-10-09 Progenics Pharmaceuticals, Inc. Crystal forms and uses thereof
TWI553009B (en) 2007-03-29 2016-10-11 普吉尼製藥公司 Peripheral opioid receptor antagonists and uses thereof
CA2676881C (en) 2008-09-30 2017-04-25 Wyeth Peripheral opioid receptor antagonists and uses thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4176186A (en) * 1978-07-28 1979-11-27 Boehringer Ingelheim Gmbh Quaternary derivatives of noroxymorphone which relieve intestinal immobility
WO2004043964A2 (en) * 2002-11-08 2004-05-27 Mallinckrodt Inc. Process for the preparation of quaternary n-alkyl morphinan alkaloid salts

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
BIANCHETTI A ET AL: "QUATERNARY DERIVATIVES OF NARCOTIC ANTAGONISTS : STEREOCHEMICAL REQUIREMENTS AT THE CHIRAL NITROGEN FOR IN VITRO AND VIVO ACTIVITY", LIFE SCIENCES, PERGAMON PRESS, OXFORD, GB, vol. 33, no. SUPPL 1, 1983, pages 415 - 418, XP000980615, ISSN: 0024-3205 *
DE PONTI F: "METHYLNALTREXONE PROGENICS", CURRENT OPINION IN INVESTIGATIONAL DRUGS, PHARMAPRESS, US, vol. 3, no. 4, April 2002 (2002-04-01), pages 614 - 620, XP009066298, ISSN: 1472-4472 *
FUNKE, CAREL W. ET AL: "A proton and carbon-13 nuclear magnetic resonance study of three quaternary salts of naloxone and oxymorphone", JOURNAL OF THE CHEMICAL SOCIETY, PERKIN TRANSACTIONS 2: PHYSICAL ORGANIC CHEMISTRY (1972-1999) , (5), 735-8 CODEN: JCPKBH; ISSN: 0300-9580, 1986, XP009072982 *
IORIO, MARIA A. ET AL: "Narcotic agonist/antagonist properties of quaternary diastereoisomers derived from oxymorphone and naloxone", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY , 19(4), 301-3 CODEN: EJMCA5; ISSN: 0223-5234, 1984, XP009072981 *
KOBYLECKI R J: "N-METHYLNALORPHINE: DEFINITION OF N-ALLYL CONFORMATION FOR ANTAGONISM AT THE OPIATE RECEPTOR", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 25, no. 11, 1982, pages 1278 - 1280, XP000978843, ISSN: 0022-2623 *
YUAN CHUN-SU: "Clinical status of methylnaltrexone, a new agent to prevent and manage opioid-induced side effects./TRIALS SO FAR SHOW THAT THIS PERIPHERAL OPIOID RECEPTOR ANTAGONIST CAN PREVENT OPIOID-INDUCED CONSTIPATION WITHOUT DIMINISHING PAIN PALLIATION", JOURNAL OF SUPPORTIVE ONCOLOGY, BIOLINK COMMUNICATIONS,, US, vol. 2, no. 2, March 2004 (2004-03-01), pages 111 - 117, XP002390438, ISSN: 1544-6794 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8524731B2 (en) 2005-03-07 2013-09-03 The University Of Chicago Use of opioid antagonists to attenuate endothelial cell proliferation and migration
US9526723B2 (en) 2008-03-21 2016-12-27 The University Of Chicago Treatment with opioid antagonists and mTOR inhibitors
US9518062B2 (en) 2009-07-16 2016-12-13 Mallinckrodt Llc Compounds and compositions for use in phototherapy and in treatment of ocular neovascular disease and cancers
US9527858B2 (en) 2009-07-16 2016-12-27 Mallinckrodt Llc Compounds and compositions for use in phototherapy and in treatment of ocular neovascular disease and cancers

Also Published As

Publication number Publication date
JP2015129190A (en) 2015-07-16
GT200600226A (en) 2007-01-12
US20150290187A1 (en) 2015-10-15
EP3219717A1 (en) 2017-09-20
US20170143700A1 (en) 2017-05-25
AU2006249911A1 (en) 2006-11-30
AR057035A1 (en) 2007-11-14
DK1913001T3 (en) 2013-10-21
TWI383984B (en) 2013-02-01
JP2008542287A (en) 2008-11-27
US20130323286A1 (en) 2013-12-05
CN101208344A (en) 2008-06-25
JP5769693B2 (en) 2015-08-26
HK1244267A1 (en) 2018-08-03
WO2006127899A2 (en) 2006-11-30
CA2609662C (en) 2016-08-16
ES2429160T3 (en) 2013-11-13
AU2006249911B2 (en) 2012-05-17
US7674904B2 (en) 2010-03-09
EP2450359A2 (en) 2012-05-09
CN102721756A (en) 2012-10-10
JP2017137346A (en) 2017-08-10
JP5213704B2 (en) 2013-06-19
US20070099946A1 (en) 2007-05-03
AU2006249911C1 (en) 2012-12-20
MY151036A (en) 2014-03-31
JP2013075905A (en) 2013-04-25
US20150057303A1 (en) 2015-02-26
US20100311781A1 (en) 2010-12-09
EP2450359A3 (en) 2012-08-22
PT1913001E (en) 2013-10-08
US8343992B2 (en) 2013-01-01
PL1913001T3 (en) 2013-12-31
EP1913001B1 (en) 2013-09-04
MX2007014880A (en) 2008-02-15
EP1913001A2 (en) 2008-04-23
BRPI0611162A2 (en) 2010-08-17
HN2006019068A (en) 2011-03-02
US9597327B2 (en) 2017-03-21
SI1913001T1 (en) 2013-11-29
CA2609662A1 (en) 2006-11-30
TW200716647A (en) 2007-05-01
CN101208344B (en) 2012-10-24

Similar Documents

Publication Publication Date Title
WO2006127899A3 (en) (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use
WO2006127898A3 (en) (s)-n-methylnaltrexone, process for its synthesis and its pharmaceutical use
WO2005112938A3 (en) Disalt inhibitors of il-12 production
WO2007127841A3 (en) Compositions and methods of preparation thereof
WO2008017029A3 (en) Drug carriers, their synthesis, and methods of use thereof
WO2005108358A3 (en) Pyrrolidine derivatives useful as bace inhibitors
WO2006092213A8 (en) Pyrazolylcarboxanilides
WO2006023627A8 (en) Rapamycin polymorph ii and uses thereof
WO2008005877A3 (en) Inhibitors of c-kit and uses thereof
WO2007022459A3 (en) Processes and intermediates
WO2008151170A3 (en) Process for the synthesis of ramelteon and its intermediates
WO2006075095A3 (en) Use of purine derivatives as hsp90 protein inhibitors and for treatment of cancer
WO2008013990A3 (en) Processes for the synthesis of o-desmethylvenlafaxine
WO2007062370A3 (en) Calcilytic compounds
IL188919A (en) Process for the preparation of mandipropamid and derivatives thereof and intermediates therefor
WO2007067784A3 (en) Liposomal compositions
WO2007047671A3 (en) Tetrahydroquinolines, synthesis thereof, and intermediates thereto
WO2004106322A3 (en) Polymorphs of aripiprazole
WO2009137714A3 (en) Forms of lapatinib ditosylate and processes for preparation thereof
WO2007016029A3 (en) Diazepinoquinolines, synthesis thereof, and intermediates thereto
WO2007098273A3 (en) Novel crystalline forms of armodafinil and preparation thereof
WO2007061878A3 (en) 17-allylamino-17-demethoxygeldanamycin polymorphs and formulations
WO2007016609A3 (en) Method for the synthesis of quinoliνe derivatives
WO2009155403A3 (en) Processes for the preparation of varenicline and intermediates thereof
WO2009111785A3 (en) Treatment of sepsis with 5-ethyl-1-phenyl-2(1h)-pyridone and novel methods for synthesis

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: 200680022957.X

Country of ref document: CN

121 Ep: the epo has been informed by wipo that ep was designated in this application
ENP Entry into the national phase

Ref document number: 2609662

Country of ref document: CA

WWE Wipo information: entry into national phase

Ref document number: MX/a/2007/014880

Country of ref document: MX

ENP Entry into the national phase

Ref document number: 2008513707

Country of ref document: JP

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 4550/KOLNP/2007

Country of ref document: IN

NENP Non-entry into the national phase

Ref country code: DE

WWE Wipo information: entry into national phase

Ref document number: 2006771163

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 2006249911

Country of ref document: AU

NENP Non-entry into the national phase

Ref country code: RU

ENP Entry into the national phase

Ref document number: 2006249911

Country of ref document: AU

Date of ref document: 20060525

Kind code of ref document: A

ENP Entry into the national phase

Ref document number: PI0611162

Country of ref document: BR

Kind code of ref document: A2