WO2005117876A8 - Dual small molecule inhibitors of cancer and angiogenesis - Google Patents

Dual small molecule inhibitors of cancer and angiogenesis

Info

Publication number
WO2005117876A8
WO2005117876A8 PCT/US2005/019244 US2005019244W WO2005117876A8 WO 2005117876 A8 WO2005117876 A8 WO 2005117876A8 US 2005019244 W US2005019244 W US 2005019244W WO 2005117876 A8 WO2005117876 A8 WO 2005117876A8
Authority
WO
WIPO (PCT)
Prior art keywords
angiogenesis
cancer
small molecule
molecule inhibitors
present
Prior art date
Application number
PCT/US2005/019244
Other languages
French (fr)
Other versions
WO2005117876A1 (en
Inventor
Milton L Brown
Original Assignee
Univ Virginia
Milton L Brown
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
Priority to EP05756099.7A priority Critical patent/EP1750706B1/en
Priority to KR1020067027847A priority patent/KR101258298B1/en
Application filed by Univ Virginia, Milton L Brown filed Critical Univ Virginia
Priority to JP2007515530A priority patent/JP4991527B2/en
Priority to CA2568622A priority patent/CA2568622C/en
Priority to US11/628,209 priority patent/US8178545B2/en
Priority to NZ551775A priority patent/NZ551775A/en
Priority to AU2005249527A priority patent/AU2005249527B2/en
Priority to BRPI0511748-8A priority patent/BRPI0511748A/en
Priority to ES05756099.7T priority patent/ES2604197T3/en
Priority to CN2005800245756A priority patent/CN1988907B/en
Publication of WO2005117876A1 publication Critical patent/WO2005117876A1/en
Priority to IL179714A priority patent/IL179714A/en
Priority to US11/613,663 priority patent/US8298512B2/en
Publication of WO2005117876A8 publication Critical patent/WO2005117876A8/en
Priority to US13/366,726 priority patent/US8642610B2/en
Priority to US14/166,200 priority patent/US9133136B2/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/001—Preparation for luminescence or biological staining
    • A61K49/0013—Luminescence
    • A61K49/0017—Fluorescence in vivo
    • A61K49/0019—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules
    • A61K49/0021—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules the fluorescent group being a small organic molecule
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/24—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16—Benzazepines; Hydrogenated benzazepines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D245/00—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
    • C07D245/04—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D245/00—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
    • C07D245/04—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C07D245/06—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods of treating cancers comprising mutant p53.
PCT/US2005/019244 2004-06-01 2005-06-01 Dual small molecule inhibitors of cancer and angiogenesis WO2005117876A1 (en)

Priority Applications (14)

Application Number Priority Date Filing Date Title
ES05756099.7T ES2604197T3 (en) 2004-06-01 2005-06-01 Double small molecule inhibitors of cancer and angiogenesis
BRPI0511748-8A BRPI0511748A (en) 2004-06-01 2005-06-01 pharmaceutical composition, methods for treating cancer and a disease or disorder associated with angiogenesis in an individual in need, to inhibit proliferation of vascular and cancer endothelial cells, and to prepare sc-2-71 and analogs thereof, sc photoaffinity label -2-71, method for disrupting microtubule polymerization in a cell, and for identifying an analog, analog, and kit for administering a pharmaceutical composition to an individual
JP2007515530A JP4991527B2 (en) 2004-06-01 2005-06-01 Bipartite low molecular weight cancer and angiogenesis inhibitors
KR1020067027847A KR101258298B1 (en) 2004-06-01 2005-06-01 Dual small molecule inhibitors of cancer and angiogenesis
US11/628,209 US8178545B2 (en) 2004-06-01 2005-06-01 Dual small molecule inhibitors of cancer and angiogenesis
NZ551775A NZ551775A (en) 2004-06-01 2005-06-01 Dual small molecule inhibitors of cancer and angiogenesis
CN2005800245756A CN1988907B (en) 2004-06-01 2005-06-01 Dual small molecule inhibitors of cancer and angiogenesis
EP05756099.7A EP1750706B1 (en) 2004-06-01 2005-06-01 Dual small molecule inhibitors of cancer and angiogenesis
CA2568622A CA2568622C (en) 2004-06-01 2005-06-01 Dual small molecule inhibitors of cancer and angiogenesis
AU2005249527A AU2005249527B2 (en) 2004-06-01 2005-06-01 Dual small molecule inhibitors of cancer and angiogenesis
IL179714A IL179714A (en) 2004-06-01 2006-11-30 Pharmaceutical composition comprising derivatives of 2-biphenyl-4-yl-2,3-dihydro-1h-quinazolin-4-one and use thereof in the manufacture of medicaments for treating cancer and angiogenesis
US11/613,663 US8298512B2 (en) 2004-06-01 2006-12-20 Methods of determining β-III tubulin expression
US13/366,726 US8642610B2 (en) 2004-06-01 2012-02-06 Dual small molecule inhibitors of cancer and angiogenesis
US14/166,200 US9133136B2 (en) 2004-06-01 2014-01-28 Dual small molecule inhibitors of cancer and angiogenesis

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US57592704P 2004-06-01 2004-06-01
US60/575,927 2004-06-01

Related Child Applications (3)

Application Number Title Priority Date Filing Date
US11/628,209 A-371-Of-International US8178545B2 (en) 2004-06-01 2005-06-01 Dual small molecule inhibitors of cancer and angiogenesis
US11/613,663 Continuation-In-Part US8298512B2 (en) 2004-06-01 2006-12-20 Methods of determining β-III tubulin expression
US13/366,726 Division US8642610B2 (en) 2004-06-01 2012-02-06 Dual small molecule inhibitors of cancer and angiogenesis

Publications (2)

Publication Number Publication Date
WO2005117876A1 WO2005117876A1 (en) 2005-12-15
WO2005117876A8 true WO2005117876A8 (en) 2007-03-01

Family

ID=35462720

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2005/019244 WO2005117876A1 (en) 2004-06-01 2005-06-01 Dual small molecule inhibitors of cancer and angiogenesis

Country Status (12)

Country Link
US (4) US8178545B2 (en)
EP (1) EP1750706B1 (en)
JP (1) JP4991527B2 (en)
KR (1) KR101258298B1 (en)
CN (1) CN1988907B (en)
AU (1) AU2005249527B2 (en)
BR (1) BRPI0511748A (en)
CA (1) CA2568622C (en)
ES (1) ES2604197T3 (en)
IL (1) IL179714A (en)
NZ (1) NZ551775A (en)
WO (1) WO2005117876A1 (en)

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9034330B2 (en) 1999-02-22 2015-05-19 Georgetown University Preparation of antibody or an antibody fragment-targeted immunoliposomes for systemic administration of therapeutic or diagnostic agents and uses thereof
AU2004275718B2 (en) 2003-09-23 2008-02-07 Merck Sharp & Dohme Corp. Quinazoline potassium channel inhibitors
SG150533A1 (en) 2003-11-20 2009-03-30 Janssen Pharmaceutica Nv 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2- quinoxalinones as poly(adp-ribose) polymerase inhibitors
SG150534A1 (en) 2003-11-20 2009-03-30 Janssen Pharmaceutica Nv 7-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(adp- ribose) polymerase inhibitors
BRPI0511748A (en) 2004-06-01 2008-01-02 Univ Virginia pharmaceutical composition, methods for treating cancer and a disease or disorder associated with angiogenesis in an individual in need, to inhibit proliferation of vascular and cancer endothelial cells, and to prepare sc-2-71 and analogs thereof, sc photoaffinity label -2-71, method for disrupting microtubule polymerization in a cell, and for identifying an analog, analog, and kit for administering a pharmaceutical composition to an individual
US20050283097A1 (en) * 2004-06-18 2005-12-22 Ultrastop Ltd. Devices and methodologies useful in non invasive termination of pregnancy
KR101211950B1 (en) 2004-06-30 2012-12-13 얀센 파마슈티카 엔.브이. Phthalazine derivatives as parp inhibitors
EA011552B1 (en) 2004-06-30 2009-04-28 Янссен Фармацевтика Н.В. Quinazolinedione derivatives as parp inhibitors
UA85593C2 (en) 2004-06-30 2009-02-10 Янссен Фармацевтика Н.В. Quinazolinone derivatives as parp inhibitors
WO2006020049A2 (en) 2004-07-15 2006-02-23 Amr Technology, Inc. Aryl-and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
US20060257337A1 (en) * 2005-04-28 2006-11-16 David Sherris Compositions and methods to treat skin diseases characterized by cellular proliferation and angiogenesis
ATE542799T1 (en) 2007-03-08 2012-02-15 Janssen Pharmaceutica Nv QUINOLINONE DERIVATIVES AS PARP AND TANK INHIBITORS
NZ584330A (en) * 2007-10-04 2013-01-25 Bionomics Ltd Markers of endothelial cells and uses thereof
PL2215075T3 (en) 2007-10-26 2014-04-30 Janssen Pharmaceutica Nv Quinolinone derivatives as parp inhibitors
WO2009118382A1 (en) 2008-03-27 2009-10-01 Janssen Pharmaceutica Nv Tetrahydrophenanthridinones and tetrahydrocyclopentaquinolinones as parp and tubulin polymerization inhibitors
WO2009118384A1 (en) * 2008-03-27 2009-10-01 Janssen Pharmaceutica Nv Quinazolinone derivatives as tubulin polymerization inhibitors
US9156812B2 (en) 2008-06-04 2015-10-13 Bristol-Myers Squibb Company Crystalline form of 6-[(4S)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine
AU2008363295B2 (en) 2008-10-20 2015-05-07 Forschungsverbund Berlin E.V. Low molecular weight thyroid stimulating hormone receptor (TSHR) agonists
BRPI1008955A2 (en) 2009-03-13 2015-09-01 Abraxis Bioscience Llc Combination therapy with thiocolchicine derivatives.
JP5739415B2 (en) 2009-05-12 2015-06-24 ブリストル−マイヤーズ スクウィブ カンパニー (S) -7-([1,2,4] triazolo [1,5-a] pyridin-6-yl) -4- (3,4-dichlorophenyl) -1,2,3,4-tetrahydroisoquinoline Crystal forms and uses thereof
KR20120034644A (en) 2009-05-12 2012-04-12 알바니 몰레큘라 리써치, 인크. Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof
DK2429296T3 (en) * 2009-05-12 2018-03-12 Albany Molecular Res Inc 7 - ([1,2,4,] TRIAZOLO [1,5, -A] PYRIDIN-6-YL) -4- (3,4-DICHLORPHENYL) -1,2,3,4- TETRAHYDROISOQUINOLINE AND USE thereof
US20100291201A1 (en) * 2009-05-14 2010-11-18 Cerovene, Inc. Coated pharmaceutical capsule dosage form
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
EP3168226A3 (en) 2010-05-31 2017-07-26 London Health Sciences Centre Research Inc. Rhamm binding peptides
CN101935318A (en) * 2010-08-17 2011-01-05 上海医药集团股份有限公司 2,3-dihydro-4(1H)- quinazolone derivative and application thereof
US9381187B2 (en) 2011-02-16 2016-07-05 Paloma Pharmaceuticals, Inc. Radiation countermeasure agents
UA110640C2 (en) * 2011-05-05 2016-01-25 Янссен Фармацевтика Нв Antifungal 5,6-dihydro-4h-pyrrolo-[l,2-a][l,4]benzodiazepines and 6h-pyrrolo[1,2-a][l,4]benzodiazepines substituted with heterocyclic derivatives
EP2721007B1 (en) 2011-06-20 2015-04-29 Novartis AG Cyclohexyl isoquinolinone compounds
US8859535B2 (en) 2011-06-20 2014-10-14 Novartis Ag Hydroxy substituted isoquinolinone derivatives
EP2855483B1 (en) 2012-05-24 2017-10-25 Novartis AG Pyrrolopyrrolidinone compounds
US9695156B2 (en) * 2012-07-16 2017-07-04 Brown University Compounds for the treatment and prevention of infections
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
WO2014080291A2 (en) * 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
MX2015007921A (en) 2012-12-21 2016-03-03 Zenith Epigenetics Corp Novel heterocyclic compounds as bromodomain inhibitors.
EP2948453B1 (en) 2013-01-22 2017-08-02 Novartis AG Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the p53/mdm2 interaction
WO2014115077A1 (en) 2013-01-22 2014-07-31 Novartis Ag Substituted purinone compounds
CA2913697A1 (en) 2013-05-27 2014-12-04 Novartis Ag Imidazopyrrolidinone derivatives and their use in the treatment of disease
MX2015016425A (en) 2013-05-28 2016-03-03 Novartis Ag Pyrazolo-pyrrolidin-4-one derivatives and their use in the treatment of disease.
PT3004108T (en) 2013-05-28 2018-01-24 Novartis Ag Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease
JP6599852B2 (en) 2013-06-21 2019-10-30 ゼニス・エピジェネティクス・リミテッド Novel substituted bicyclic compounds as bromodomain inhibitors
BR112015031073B1 (en) 2013-06-21 2022-11-29 Zenith Epigenetics Ltd BICYCLIC BROMODIMANIUM INHIBITORS AND PHARMACEUTICAL COMPOSITION CONTAINING SAID COMPOUNDS
EA201690087A1 (en) 2013-07-31 2016-08-31 Зенит Эпидженетикс Корп. NEW QUINAZOLINONS AS BROMOMODENIAL INHIBITORS
KR20160086930A (en) 2013-11-21 2016-07-20 노파르티스 아게 Pyrrolopyrrolone derivatives and their use as bet inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
US10179125B2 (en) 2014-12-01 2019-01-15 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
JP2017537946A (en) 2014-12-11 2017-12-21 ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． Substituted heterocycles as bromodomain inhibitors
CN107406438B (en) 2014-12-17 2021-05-14 恒翼生物医药科技(上海)有限公司 Inhibitors of bromodomains
GB201510010D0 (en) 2015-06-09 2015-07-22 King S College London PDD and BPD compounds
US20180339985A1 (en) 2015-08-21 2018-11-29 Femtogenix Limited Pdd compounds
GB201514928D0 (en) 2015-08-21 2015-10-07 King S College London PDD compounds
US10781203B2 (en) 2016-07-20 2020-09-22 The Penn State Research Foundation Nontoxic compounds for the treatment and prevention of herpesvirus infections
CN115433134A (en) * 2022-09-16 2022-12-06 哈尔滨工业大学（深圳） Catalytic enantioselective synthesis method of dihydro quinazolinone
CN115677600A (en) * 2022-11-04 2023-02-03 武汉大学人民医院（湖北省人民医院） 2, 3-dihydroquinazoline-4 (1H) -ketone derivative and preparation method and application thereof

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4160452A (en) 1977-04-07 1979-07-10 Alza Corporation Osmotic system having laminated wall comprising semipermeable lamina and microporous lamina
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
GB8329361D0 (en) 1983-11-03 1983-12-07 Wiggins Teape Group Ltd Record material
JPS62258368A (en) * 1986-03-10 1987-11-10 Agency Of Ind Science & Technol Production of quinazolin-4-one
JP3136724B2 (en) 1991-01-16 2001-02-19 東ソー株式会社 Tetrahydroisoquinoline derivative, method for producing the same, and fungicide containing the same as an active ingredient
DE69220389T2 (en) 1991-01-16 1998-01-29 Tosoh Corp Tetrahydroisoquinoline derivatives, process for their preparation and fungicidal compositions containing them
DE69219236T2 (en) * 1991-02-19 1997-08-07 Fujitsu Ltd SEMICONDUCTOR ARRANGEMENT WITH A AREA ENRICHED WITH OXYGEN AND THEIR PRODUCTION METHOD
US5480883A (en) * 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
WO1998023620A1 (en) 1996-11-28 1998-06-04 Cheil Jedang Corporation Cathecol derivatives and a method for the preparation thereof and a pharmaceutical composition containing the same
US20020028813A1 (en) * 1997-09-03 2002-03-07 Paul F. Jackson Thioalkyl compounds, methods, and compositions for inhibiting parp activity
WO2000027831A1 (en) 1998-11-09 2000-05-18 Chemrx Advanced Technologies, Inc. Process for the synthesis of quinazolinones
US6716614B1 (en) 1999-09-02 2004-04-06 Lexicon Genetics Incorporated Human calcium dependent proteases, polynucleotides encoding the same, and uses thereof
DE10034606B4 (en) 2000-07-20 2004-02-26 Stefan Gleis Method for providing manufacturing-related data in a series production of manufacturing objects, in particular motor vehicles
US6967251B2 (en) 2000-10-02 2005-11-22 Molecular Probes, Inc. Reagents for labeling biomolecules having aldehyde or ketone moieties
PT1370553E (en) * 2001-03-23 2006-09-29 Bayer Corp RHOQUINASE INHIBITORS
EP1389103A4 (en) 2001-04-23 2005-09-14 Univ Virginia Synthesis and evaluation of novel phthalimide mimics as anti-angiogenic agents
DE10246140A1 (en) 2002-10-01 2004-04-15 Basf Ag Reaction products of 2-propylheptanol with 1-halogen-2,3-epoxypropanes and 1-hydroxy-2,3-epoxypropane
TW200408393A (en) 2002-10-03 2004-06-01 Ono Pharmaceutical Co Antagonist of lysophosphatidine acid receptor
US20050214807A1 (en) 2003-11-19 2005-09-29 Iain Johnson Environmental sensitive fluorogenic compounds and their application for singlet oxygen and protein detection
US20050130897A1 (en) 2003-12-11 2005-06-16 Ma Jian-Xing Compounds useful in inhibiting vascular leakage, inflammation and fibrosis and methods of making and using same
BRPI0511748A (en) 2004-06-01 2008-01-02 Univ Virginia pharmaceutical composition, methods for treating cancer and a disease or disorder associated with angiogenesis in an individual in need, to inhibit proliferation of vascular and cancer endothelial cells, and to prepare sc-2-71 and analogs thereof, sc photoaffinity label -2-71, method for disrupting microtubule polymerization in a cell, and for identifying an analog, analog, and kit for administering a pharmaceutical composition to an individual

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