WO2002008222A3 - HETEROARYL-β-ALANINE DERIVATIVES AS ALPHA 4 INTEGRIN INHIBITORS - Google Patents

HETEROARYL-β-ALANINE DERIVATIVES AS ALPHA 4 INTEGRIN INHIBITORS Download PDF

Info

Publication number
WO2002008222A3
WO2002008222A3 PCT/US2001/023096 US0123096W WO0208222A3 WO 2002008222 A3 WO2002008222 A3 WO 2002008222A3 US 0123096 W US0123096 W US 0123096W WO 0208222 A3 WO0208222 A3 WO 0208222A3
Authority
WO
WIPO (PCT)
Prior art keywords
heteroaryl
alpha
alanine derivatives
integrin inhibitors
alanine
Prior art date
Application number
PCT/US2001/023096
Other languages
French (fr)
Other versions
WO2002008222A2 (en
Inventor
Andrei W Konradi
Michael A Pleiss
Eugene D Thorsett
Susan Ashwell
Gregory S Welmaker
Anthony Kreft
Dimitrios Sarantakis
Darren B Dressen
Francine S Grant
Christopher Semko
Ying-Zi Xu
Original Assignee
Elan Pharm Inc
American Home Prod
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
Application filed by Elan Pharm Inc, American Home Prod filed Critical Elan Pharm Inc
Priority to AU2001276027A priority Critical patent/AU2001276027A1/en
Publication of WO2002008222A2 publication Critical patent/WO2002008222A2/en
Publication of WO2002008222A3 publication Critical patent/WO2002008222A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/26—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
    • C07D251/40—Nitrogen atoms
    • C07D251/42—One nitrogen atom
    • C07D251/46—One nitrogen atom with oxygen or sulfur atoms attached to the two other ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

Disclosed are a series of heteroaryl-β-alanine derivatives, compositions containing them, processes for their preparation and their use in medicine.
PCT/US2001/023096 2000-07-21 2001-07-20 HETEROARYL-β-ALANINE DERIVATIVES AS ALPHA 4 INTEGRIN INHIBITORS WO2002008222A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2001276027A AU2001276027A1 (en) 2000-07-21 2001-07-20 Heteroaryl-beta-alanine derivatives as alpha 4 integrin inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22012800P 2000-07-21 2000-07-21
US60/220,128 2000-07-21

Publications (2)

Publication Number Publication Date
WO2002008222A2 WO2002008222A2 (en) 2002-01-31
WO2002008222A3 true WO2002008222A3 (en) 2002-06-13

Family

ID=22822184

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/023096 WO2002008222A2 (en) 2000-07-21 2001-07-20 HETEROARYL-β-ALANINE DERIVATIVES AS ALPHA 4 INTEGRIN INHIBITORS

Country Status (3)

Country Link
US (1) US7015216B2 (en)
AU (1) AU2001276027A1 (en)
WO (1) WO2002008222A2 (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6048861A (en) * 1997-12-17 2000-04-11 Merck & Co., Inc. Integrin receptor antagonists
AU780988B2 (en) * 2000-01-24 2005-04-28 Merck & Co., Inc. Alpha V integrin receptor antagonists
US6960597B2 (en) * 2000-06-30 2005-11-01 Orth-Mcneil Pharmaceutical, Inc. Aza-bridged-bicyclic amino acid derivatives as α4 integrin antagonists
WO2004007444A2 (en) 2002-07-11 2004-01-22 Vicuron Pharmaceuticals, Inc. N-hydroxyamide derivatives possessing antibacterial activity
US20050176755A1 (en) * 2003-10-31 2005-08-11 Dyatkin Alexey B. Aza-bridged-bicyclic amino acid derivatives as alpha4 integrin antagonists
WO2005077915A1 (en) * 2004-02-10 2005-08-25 Janssen Pharmaceutica, N.V. Pyridazinones as antagonists of a4 integrins
US20050209232A1 (en) * 2004-02-10 2005-09-22 Kent Barbay Pyridazinone ureas as antagonists of alpha4 integrins
EP1984344B1 (en) * 2005-12-29 2012-09-26 Lexicon Pharmaceuticals, Inc. Multicyclic amino acid derivatives and methods of their use
EP2124996A4 (en) 2007-02-20 2010-03-24 Merrimack Pharmaceuticals Inc Methods of treating multiple sclerosis by administration of alpha-fetoprotein in combination with an integrin antagonist
WO2009126920A2 (en) 2008-04-11 2009-10-15 Merrimack Pharmaceuticals, Inc. Human serum albumin linkers and conjugates thereof
KR20110112301A (en) 2008-11-18 2011-10-12 메리맥 파마슈티컬즈, 인크. Human serum albumin linkers and conjugates thereof
EP2769223A1 (en) 2011-10-17 2014-08-27 Westfälische Wilhelms-Universität Münster Assessment of pml risk and methods based thereon
WO2014036520A1 (en) 2012-08-30 2014-03-06 Merrimack Pharmaceuticals, Inc. Combination therapies comprising anti-erbb3 agents

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997036859A1 (en) * 1996-03-29 1997-10-09 G.D. Searle & Co. Para-substituted phenylpropanoic acid derivatives as integrin antagonists
WO1999037618A1 (en) * 1998-01-27 1999-07-29 Celltech Therapeutics Limited Phenylalanine derivatives useful as pharmaceutical agents
WO1999043642A1 (en) * 1998-02-26 1999-09-02 Celltech Therapeutics Limited Phenylalanine derivatives as inhibitors of alpha4 integrins
WO2000018759A1 (en) * 1998-09-28 2000-04-06 Celltech Therapeutics Limited Phenylalanine derivatives as alpha 4 integrin inhibitors
WO2000020396A1 (en) * 1998-10-01 2000-04-13 Celltech Therapeutics Limited Phenylalkanoic acid derivatives as inhibitors of alpha4 integrins

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997036859A1 (en) * 1996-03-29 1997-10-09 G.D. Searle & Co. Para-substituted phenylpropanoic acid derivatives as integrin antagonists
WO1999037618A1 (en) * 1998-01-27 1999-07-29 Celltech Therapeutics Limited Phenylalanine derivatives useful as pharmaceutical agents
WO1999043642A1 (en) * 1998-02-26 1999-09-02 Celltech Therapeutics Limited Phenylalanine derivatives as inhibitors of alpha4 integrins
WO2000018759A1 (en) * 1998-09-28 2000-04-06 Celltech Therapeutics Limited Phenylalanine derivatives as alpha 4 integrin inhibitors
WO2000020396A1 (en) * 1998-10-01 2000-04-13 Celltech Therapeutics Limited Phenylalkanoic acid derivatives as inhibitors of alpha4 integrins

Also Published As

Publication number Publication date
US7015216B2 (en) 2006-03-21
WO2002008222A2 (en) 2002-01-31
AU2001276027A1 (en) 2002-02-05
US20020086882A1 (en) 2002-07-04

Similar Documents

Publication Publication Date Title
HUP0303722A3 (en) Urea derivatives as integrin alpha 4 antanists, process for their preparation and pharmaceutical compositions containing them
HUP0400837A3 (en) 2-phenyl-thiazole derivatives, their use and pharmaceutical compositions containing them
HUP0200347A3 (en) N-cyanomethylamides as protease inhibitors, pharmaceutical compositions containing them and their use
HUP0204474A3 (en) 1h-imidazopyridine derivatives, pharmaceutical compositions containing them and their use
HUP0300207A3 (en) 1,2,3,4-tetrahydroisquinoline derivatives, pharmaceutical compositions containing them and their preparation processes
AU2001237526A1 (en) Pharmaceutical compositions containing 3-amino-azetidine derivatives, novel derivatives and preparation thereof
IL151209A0 (en) Pharmaceutical compositions containing 3-aminoazetidine derivatives, novel derivatives and their preparation
HUP0301069A3 (en) Novel biarylcarboxamides, process for their preparation, pharmaceutical compositions containing them and their use
HUP0301315A3 (en) Benzothiazole derivatives, process for their preparation, their use and pharmaceutical compositions containing them
HUP0300565A3 (en) 8-quinolinxanthine and 8-isoquinolinxanthine derivatives as pde 5 inhibitors, their use, process for their preparation and pharmaceutical compositions containing them
HUP0204410A3 (en) Pyrimidine-4-one derivatives, process for their preparation, pharmaceutical compositions containing them and their use
HUP0200396A3 (en) Gluckokinase activators, process for their preparation, pharmaceutical compositions containing them and their use
HUP0300616A3 (en) Adamantane derivatives, process for their preparation, their use and pharmaceutical compositions containing them
HUP0300909A3 (en) 2-guanidino-4-arylchinazolines as nhe-3 inhibitors, pharmaceutical compositions containing them and their use
AU2001269198A1 (en) Novel 1,3-dihydro-2h-indol-one derivatives, method for preparing same and pharmaceutical compositions containing them
HUP0400832A3 (en) New amidoalkyl-piperidine and amidoalkyl-piperazine derivatives, and pharmaceutical compositions containing such derivatives as active ingredients
WO2002008222A3 (en) HETEROARYL-β-ALANINE DERIVATIVES AS ALPHA 4 INTEGRIN INHIBITORS
HUP0401403A3 (en) 2,4-diaminothiazole derivatives, their use and pharmaceutical compositions containing them
HUP0204354A3 (en) Novel heterocyclic derivatives, preparation method and pharmaceutical compositions containing same and their use
IL143987A (en) Amidinobenzylamine derivatives, processes for their preparation, pharmaceutical compositions containing them and use of such compositions in the preparation of a medicament for the inhibition of thrombin
GEP20063972B (en) Streptogramin derivatives, preparation and compositions containing them
AU2841199A (en) Novel bis-benzamide derivatives, method for making same pharmaceutical compositions containing them and use thereof as medicine
HUP0302753A3 (en) Urea and urethane derivatives as integrin inhibitors, process for their preparation, their use and pharmaceutical compositions containing them
HUP0303195A3 (en) O-substituted 6-methyl-tramadol derivatives, process for their preparation and pharmaceutical compositions containing them
HUP0203859A3 (en) Aminomethyl-phenyl-cyclohexanone derivatives, process for their preparation, pharmaceutical compositions containing them and their use

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
AK Designated states

Kind code of ref document: A3

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: JP