CA2277273A1 - Integrin antagonists - Google Patents

Integrin antagonists Download PDF

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Publication number
CA2277273A1
CA2277273A1 CA002277273A CA2277273A CA2277273A1 CA 2277273 A1 CA2277273 A1 CA 2277273A1 CA 002277273 A CA002277273 A CA 002277273A CA 2277273 A CA2277273 A CA 2277273A CA 2277273 A1 CA2277273 A1 CA 2277273A1
Authority
CA
Canada
Prior art keywords
beta
alpha
antagonists
vitronectin receptor
integrin antagonists
Prior art date
Legal status (The legal status 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 status listed.)
Granted
Application number
CA002277273A
Other languages
French (fr)
Other versions
CA2277273C (en
Inventor
Mark E. Duggan
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck & Co., Inc.
Mark E. Duggan
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 claimed from GBGB9702788.2A external-priority patent/GB9702788D0/en
Priority claimed from GBGB9725996.4A external-priority patent/GB9725996D0/en
Application filed by Merck & Co., Inc., Mark E. Duggan filed Critical Merck & Co., Inc.
Publication of CA2277273A1 publication Critical patent/CA2277273A1/en
Application granted granted Critical
Publication of CA2277273C publication Critical patent/CA2277273C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61K31/66—Phosphorus compounds
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, viral disease, and tumor growth.
CA002277273A 1997-01-17 1998-01-13 Integrin antagonists Expired - Fee Related CA2277273C (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US3561497P 1997-01-17 1997-01-17
US60/035,614 1997-01-17
GB9702788.2 1997-02-11
GBGB9702788.2A GB9702788D0 (en) 1997-02-11 1997-02-11 Alpha v beta 3 antagonists
US6259497P 1997-10-20 1997-10-20
US60/062,594 1997-10-20
GBGB9725996.4A GB9725996D0 (en) 1997-12-09 1997-12-09 Intergrin antagonists
GB9725996.4 1997-12-09
PCT/US1998/000617 WO1998031359A1 (en) 1997-01-17 1998-01-13 Integrin antagonists

Publications (2)

Publication Number Publication Date
CA2277273A1 true CA2277273A1 (en) 1998-07-23
CA2277273C CA2277273C (en) 2008-03-25

Family

ID=27451601

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002277273A Expired - Fee Related CA2277273C (en) 1997-01-17 1998-01-13 Integrin antagonists

Country Status (5)

Country Link
EP (1) EP1007026A4 (en)
JP (1) JP2001509176A (en)
AU (1) AU729869B2 (en)
CA (1) CA2277273C (en)
WO (1) WO1998031359A1 (en)

Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19629816A1 (en) 1996-07-24 1998-01-29 Hoechst Ag New cycloalkyl derivatives as inhibitors of bone resorption and vitronectin receptor antagonists
US6017926A (en) * 1997-12-17 2000-01-25 Merck & Co., Inc. Integrin receptor antagonists
US6048861A (en) 1997-12-17 2000-04-11 Merck & Co., Inc. Integrin receptor antagonists
US6066648A (en) 1997-12-17 2000-05-23 Merck & Co., Inc. Integrin receptor antagonists
US6211191B1 (en) 1997-12-17 2001-04-03 Merck & Co., Inc. Integrin receptor antagonists
US6313119B1 (en) 1998-01-23 2001-11-06 Adventis Pharma Deutschland Gmbh Sulfonamide derivatives as inhibitors of bone resorption and as inhibitors of cell adhesion
US6372719B1 (en) * 1998-03-04 2002-04-16 Jay Cunningham ανβ3 integrin antagonists in combination with chemotherapeutic agents
GB9805655D0 (en) 1998-03-16 1998-05-13 Celltech Therapeutics Ltd Chemical compounds
US6521626B1 (en) 1998-03-24 2003-02-18 Celltech R&D Limited Thiocarboxamide derivatives
GB9814414D0 (en) 1998-07-03 1998-09-02 Celltech Therapeutics Ltd Chemical compounds
US6984400B2 (en) 1998-07-14 2006-01-10 Yissum Research Development Company Of The Hebrew University Of Jerusalem Method of treating restenosis using bisphosphonate nanoparticles
IL125336A0 (en) * 1998-07-14 1999-03-12 Yissum Res Dev Co Compositions for inhibition and treatment of restinosis
US7008645B2 (en) 1998-07-14 2006-03-07 Yissum Research Development Company Of The Hebrew University Of Jerusalem Method of inhibiting restenosis using bisphosphonates
JP2002521450A (en) * 1998-07-29 2002-07-16 メルク エンド カムパニー インコーポレーテッド Integrin receptor antagonist
DE19842415A1 (en) * 1998-09-16 2000-03-23 Merck Patent Gmbh Pharmaceutical preparation for treating e.g. tumors, thrombosis or inflammation, contains cyclic pentapeptide integrin inhibitor and chemotherapeutic agent and/or angiogenesis inhibitor
GB9821061D0 (en) 1998-09-28 1998-11-18 Celltech Therapeutics Ltd Chemical compounds
GB9826174D0 (en) 1998-11-30 1999-01-20 Celltech Therapeutics Ltd Chemical compounds
KR20010110310A (en) * 1998-12-23 2001-12-12 로저 에이. 윌리암스 Method of using a cyclooxygenase-2 inhibitor and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia
CN1208323C (en) 1999-04-06 2005-06-29 三共株式会社 Alpha-substituted carboxylic acid derivatives
GB9908355D0 (en) * 1999-04-12 1999-06-09 Rhone Poulenc Rorer Ltd Chemical compounds
GB9910394D0 (en) * 1999-05-05 1999-07-07 Rhone Poulenc Rorer Ltd Chemical compounds
US6518283B1 (en) 1999-05-28 2003-02-11 Celltech R&D Limited Squaric acid derivatives
CA2373937A1 (en) 1999-06-02 2000-12-07 Merck & Co., Inc. Alpha v integrin receptor antagonists
WO2000075129A1 (en) * 1999-06-07 2000-12-14 Shire Biochem Inc. Thiophene integrin inhibitors
EP1065207A1 (en) 1999-07-02 2001-01-03 Aventis Pharma Deutschland GmbH Naphthyridine derivatives, processes for their preparation, their use, and pharmaceutical compositions comprising them
EP1065208A1 (en) * 1999-07-02 2001-01-03 Aventis Pharma Deutschland GmbH Substituted purine derivatives as inhibitors of cell adhesion
CN1374863A (en) * 1999-07-21 2002-10-16 惠氏公司 Bicyclic antagonists selective for the alpha beta integrin
US6750219B1 (en) 1999-08-05 2004-06-15 Meiji Seika Kaisha, Ltd. Ω-amino-α-hydroxycarboxylic acid derivatives having integrin ανβ3 antagonistic activity
US6534513B1 (en) 1999-09-29 2003-03-18 Celltech R&D Limited Phenylalkanoic acid derivatives
US6455539B2 (en) 1999-12-23 2002-09-24 Celltech R&D Limited Squaric acid derivates
ATE375330T1 (en) 2000-04-17 2007-10-15 Ucb Pharma Sa ENAMINE DERIVATIVES AS CELL ADHESION MOLECULES
US6545013B2 (en) 2000-05-30 2003-04-08 Celltech R&D Limited 2,7-naphthyridine derivatives
US6403608B1 (en) 2000-05-30 2002-06-11 Celltech R&D, Ltd. 3-Substituted isoquinolin-1-yl derivatives
EP1289960A2 (en) 2000-06-15 2003-03-12 Pharmacia Corporation Cycloalkyl alkanoic acids as integrin receptor antagonists
JP2004503540A (en) 2000-06-15 2004-02-05 ファルマシア・コーポレーション Dihydrostilbene alkanoic acid derivatives useful as integrin antagonists
AU2001268607A1 (en) 2000-06-21 2002-01-02 Bristol-Myers Squibb Company Piperidine amides as modulators of chemokine receptor activity
AU2001267753A1 (en) 2000-07-07 2002-01-21 Celltech R And D Limited Squaric acid derivatives containing a bicyclic heteroaromatic ring as integrin antagonists
WO2002010136A1 (en) 2000-08-02 2002-02-07 Celltech R & D Limited 3-substituted isoquinolin-1-yl derivatives
US6531494B1 (en) 2001-08-29 2003-03-11 Pharmacia Corporation Gem-substituted αvβ3 antagonists
RU2316337C2 (en) 2001-04-24 2008-02-10 Мерк Патент Гмбх Combined therapy by using antiangiogenic agents and tnf-alpha
US7153822B2 (en) 2002-01-29 2006-12-26 Wyeth Compositions and methods for modulating connexin hemichannels
US7365209B2 (en) 2003-02-11 2008-04-29 Pharmacopeia, Inc. Nitrogen heterocycle biaryls for osteoporosis and other diseases
US10517883B2 (en) 2003-06-27 2019-12-31 Zuli Holdings Ltd. Method of treating acute myocardial infarction
CA2539230A1 (en) * 2003-09-23 2005-03-31 Novartis Ag Combinations of a vegf receptor inhibitor with other therapeutic agents
CA2637387A1 (en) 2006-01-18 2007-07-26 Simon Goodman Specific therapy using integrin ligands for treating cancer
ES2348829T3 (en) 2006-03-31 2010-12-15 Janssen Pharmaceutica Nv BENZIMIDAZOL-2-IL-PYRIMIDINES AND MODULATING PIRAZINS OF THE H4 HISTAMINE RECEIVER.
ES2349237T3 (en) 2006-03-31 2010-12-29 Janssen Pharmaceutica Nv BENZOIMIDAZOL-2-IL PYRIMIDINS AS MODULATORS OF THE HISTAMINE RECEIVER H4.
EA017864B1 (en) 2007-01-18 2013-03-29 Мерк Патент Гмбх Specific therapy and medicament using integrin ligands for treating cancer
WO2009079001A1 (en) 2007-12-18 2009-06-25 Janssen Pharmaceutica N.V. Bicyclic heteroaryl-substituted imidazoles as modulators of the histamine h4 receptor
US9371311B2 (en) 2008-06-30 2016-06-21 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyrimidine derivatives
CN102448497A (en) 2009-05-25 2012-05-09 默克专利有限公司 Continuous administration of integrin ligands for treating cancer
BR112015021463A8 (en) 2013-03-06 2019-11-19 Janssen Pharmaceutica Nv h4 histamine receptor benzoimidazol-2-pyrimidine modulators, their use and pharmaceutical composition
US9993427B2 (en) 2013-03-14 2018-06-12 Biorest Ltd. Liposome formulation and manufacture
ES2957460T3 (en) 2013-09-24 2024-01-19 Fujifilm Corp Pharmaceutical composition of a nitrogen-containing compound or a salt thereof, or metal complex thereof
AU2015265571A1 (en) 2014-05-30 2016-11-17 Pfizer Inc. Carbonitrile derivatives as selective androgen receptor modulators
EP3509590A4 (en) 2016-09-07 2020-12-02 Pliant Therapeutics, Inc. N-acyl amino acid compounds and methods of use
WO2023275715A1 (en) 2021-06-30 2023-01-05 Pfizer Inc. Metabolites of selective androgen receptor modulators

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5648368A (en) * 1992-12-01 1997-07-15 Merck & Co., Inc. Fibrinogen receptor antagonists
US5563158A (en) * 1993-12-28 1996-10-08 The Dupont Merck Pharmaceutical Company Aromatic compounds containing basic and acidic termini useful as fibrinogen receptor antagonists
CA2190870A1 (en) * 1994-05-27 1995-12-07 George D. Hartman Compounds for inhibiting osteoclast-mediated bone resorption

Also Published As

Publication number Publication date
EP1007026A1 (en) 2000-06-14
CA2277273C (en) 2008-03-25
JP2001509176A (en) 2001-07-10
AU729869B2 (en) 2001-02-15
AU6023198A (en) 1998-08-07
WO1998031359A1 (en) 1998-07-23
EP1007026A4 (en) 2002-08-07

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