CA2277273C - Antagonistes d'integrine - Google Patents

Antagonistes d'integrine Download PDF

Info

Publication number
CA2277273C
CA2277273C CA002277273A CA2277273A CA2277273C CA 2277273 C CA2277273 C CA 2277273C CA 002277273 A CA002277273 A CA 002277273A CA 2277273 A CA2277273 A CA 2277273A CA 2277273 C CA2277273 C CA 2277273C
Authority
CA
Canada
Prior art keywords
pharmaceutically acceptable
compound
alkyl
inhibition
acceptable salt
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.)
Expired - Fee Related
Application number
CA002277273A
Other languages
English (en)
Other versions
CA2277273A1 (fr
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 and Co Inc
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 and Co Inc filed Critical Merck and Co Inc
Publication of CA2277273A1 publication Critical patent/CA2277273A1/fr
Application granted granted Critical
Publication of CA2277273C publication Critical patent/CA2277273C/fr
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)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

L'invention concerne certains nouveaux composés et leurs derivés, leur synthèse et leur utilisation comme antagonistes de récepteur vitronectine. Les composés antagonistes de récepteur de vitronectine décrits sont des antagonistes alpha v beta 3, des antagonistes alpha v beta 5 ou des antagonistes doubles alpha v beta 3/ alpha v beta 5, utiles pour inhiber la résorption osseuse, traiter et prévenir l'ostéoporose et inhiber la resténose, la rétinopathie diabétique, la dégénérescence maculaire, l'angiogénèse, l'athérosclérose, l'inflammation, les maladies virales et la croissance tumorale.
CA002277273A 1997-01-17 1998-01-13 Antagonistes d'integrine Expired - Fee Related CA2277273C (fr)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US3561497P 1997-01-17 1997-01-17
US60/035,614 1997-01-17
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
GB9702788.2 1997-12-09
GBGB9725996.4A GB9725996D0 (en) 1997-12-09 1997-12-09 Intergrin antagonists
GB9725996.4 1997-12-09
PCT/US1998/000617 WO1998031359A1 (fr) 1997-01-17 1998-01-13 Antagonistes d'integrine

Publications (2)

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

Family

ID=27451601

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002277273A Expired - Fee Related CA2277273C (fr) 1997-01-17 1998-01-13 Antagonistes d'integrine

Country Status (5)

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

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19629816A1 (de) 1996-07-24 1998-01-29 Hoechst Ag Neue Cycloalkyl-Derivate als Inhibitoren der Knochenresorption und Vitronectinrezeptor-Antagonisten
US6066648A (en) 1997-12-17 2000-05-23 Merck & Co., Inc. Integrin receptor antagonists
US6048861A (en) * 1997-12-17 2000-04-11 Merck & Co., Inc. Integrin receptor antagonists
US6211191B1 (en) 1997-12-17 2001-04-03 Merck & Co., Inc. Integrin receptor antagonists
US6017926A (en) * 1997-12-17 2000-01-25 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
US7008645B2 (en) 1998-07-14 2006-03-07 Yissum Research Development Company Of The Hebrew University Of Jerusalem Method of inhibiting restenosis using bisphosphonates
IL125336A0 (en) * 1998-07-14 1999-03-12 Yissum Res Dev Co Compositions for inhibition and treatment of restinosis
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
WO2000006169A1 (fr) * 1998-07-29 2000-02-10 Merck & Co., Inc. Antagonistes des recepteurs de l'integrine
DE19842415A1 (de) * 1998-09-16 2000-03-23 Merck Patent Gmbh Pharmazeutische Zubereitung
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
CN1398189A (zh) * 1998-12-23 2003-02-19 G.D.西尔公司 用于治疗肿瘤形成的放疗与cox－2抑制剂的联合治疗
BR0009593A (pt) 1999-04-06 2002-06-18 Sankyo Co Agente melhorador de resistência à insulina, agente hipoglicêmico, agente imunorregulador, inibidor de aldose redutase, inibidor de 5-lipoxigenase, supressor de produção de lipìdios peroxidados, ativador de ppar, antagonista de leucotrienos, promotor de formação hidroxiadipocelular ou antagonista de cálcio, agente preventivo e/ou terapêutico, derivados de ácido carboxìlico, medicamento, composição farmacêutica, e, uso de um composto
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
BR0011108A (pt) 1999-06-02 2002-03-19 Merck & Co Inc Composto, composição farmacêutica, e, processos de eliciar um efeito antagonizante do receptor da integrina, de tratamento ou prevenção da osteoporose, de tratamento ou prevenção de uma condição mediada por antagonismo de um receptor de integrina, de inibição da reabsorção óssea em um mamìfero em necessidade do mesmo, e de tratamento do desenvolvimento tumoral
WO2000075129A1 (fr) * 1999-06-07 2000-12-14 Shire Biochem Inc. Inhibiteurs d'integrine thiophene
EP1065207A1 (fr) 1999-07-02 2001-01-03 Aventis Pharma Deutschland GmbH Dérivées de la naphthyridine, procédés pour leur preparation, leur utilisation, et compositions pharmaceutique les contenant
EP1065208A1 (fr) * 1999-07-02 2001-01-03 Aventis Pharma Deutschland GmbH Dérivés substitués de la purine inhibiteurs de l'adhésion cellulaire
WO2001007036A1 (fr) * 1999-07-21 2001-02-01 American Home Products Corporation Antagonistes bicycliques selectifs contre l'integrine $g(a)v$g(b)¿3?
EP1209152A4 (fr) 1999-08-05 2003-03-12 Meiji Seika Kaisha Derives d'acide omega-amino-alpha-hydroxycarboxylique possedant un antagonisme alpha v beta 3 d'integrine
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 (de) 2000-04-17 2007-10-15 Ucb Pharma Sa Enamin-derivate als zell-adhäsionsmoleküle
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
EP1289959A1 (fr) 2000-06-15 2003-03-12 Pharmacia Corporation Derives d'acide alkanoique dihydrostilbene utilises comme antagonistes de la vitronectine
UY26780A1 (es) 2000-06-15 2002-01-31 Pharmacia Corp Cicloalquil avb3 antagonistas
EP1296949A2 (fr) 2000-06-21 2003-04-02 Bristol-Myers Squibb Pharma Company Amides de piperidine utilises comme modulateurs de l'activite des recepteurs des chimiokines
EP1301488A1 (fr) 2000-07-07 2003-04-16 Celltech R&D Limited Derives d'acide squarique contenant un noyau heteroaromatique bicyclique comme antagonistes d'integrine
WO2002010136A1 (fr) 2000-08-02 2002-02-07 Celltech R & D Limited Derives d'isoquinoline-1-yl substitues en 3
US6531494B1 (en) 2001-08-29 2003-03-11 Pharmacia Corporation Gem-substituted αvβ3 antagonists
ATE510557T1 (de) 2001-04-24 2011-06-15 Merck Patent Gmbh Kombinationstherapie mit antiangiogenen mitteln und tnfalpha
EA006860B1 (ru) 2002-01-29 2006-04-28 Уайт Композиции и способы модулирования гемиканалов коннексина
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
JP2007505939A (ja) * 2003-09-23 2007-03-15 ノバルティス アクチエンゲゼルシャフト Ｖｅｇｆ受容体阻害剤と他の治療剤の組み合わせ
WO2007084670A2 (fr) 2006-01-18 2007-07-26 Merck Patent Gmbh Traitement specifique utilisant des ligands de l’integrine destine a traiter un cancer
AU2007235577B2 (en) 2006-03-31 2011-09-15 Janssen Pharmaceutica N.V. Benzoimidazol-2-yl pyridines as modulators of the histamine H4 receptor
EA016264B1 (ru) 2006-03-31 2012-03-30 Янссен Фармацевтика Н.В. Бензоимидазол-2-илпиримидины и пиразины в качестве модуляторов рецептора гистамина н
ES2399159T3 (es) 2007-01-18 2013-03-26 Merck Patent Gmbh Terapia y medicamento específicos usando ligandos de integrinas para el tratamiento del cáncer
US8084466B2 (en) 2007-12-18 2011-12-27 Janssen Pharmaceutica Nv 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
CA2763275A1 (fr) 2009-05-25 2010-12-02 Merck Patent Gmbh Administration continue de ligands d'integrines pour le traitement du cancer
PL2964229T3 (pl) 2013-03-06 2020-05-18 Janssen Pharmaceutica Nv Benzoimidazol-2-ilo pirymidynowe modulatory receptora histaminowego H<sub>4</sub>
US9993427B2 (en) 2013-03-14 2018-06-12 Biorest Ltd. Liposome formulation and manufacture
PL3050878T3 (pl) 2013-09-24 2022-01-24 Fujifilm Corporation Zawierający atom azotu związek lub jego sól, lub ich kompleks z metalem
MX2016015467A (es) 2014-05-30 2017-03-23 Pfizer Derivados de carbonitrilo como moduladores selectivos del receptor de androgenos.
CN109996541A (zh) 2016-09-07 2019-07-09 普利安特治疗公司 N-酰基氨基酸化合物及其使用方法
US12036286B2 (en) 2021-03-18 2024-07-16 Seagen Inc. Selective drug release from internalized conjugates of biologically active compounds
WO2023275715A1 (fr) 2021-06-30 2023-01-05 Pfizer Inc. Métabolites de modulateurs sélectifs du récepteur des androgènes

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU675689B2 (en) * 1992-12-01 1997-02-13 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
JPH10501222A (ja) * 1994-05-27 1998-02-03 メルク エンド カンパニー インコーポレーテッド 破骨細胞仲介骨吸収を抑制するための化合物

Also Published As

Publication number Publication date
CA2277273A1 (fr) 1998-07-23
WO1998031359A1 (fr) 1998-07-23
AU729869B2 (en) 2001-02-15
EP1007026A1 (fr) 2000-06-14
AU6023198A (en) 1998-08-07
EP1007026A4 (fr) 2002-08-07
JP2001509176A (ja) 2001-07-10

Similar Documents

Publication Publication Date Title
CA2277273C (fr) Antagonistes d&#39;integrine
AU722360B2 (en) Integrin antagonists
US6017925A (en) Integrin antagonists
AU717283B2 (en) Integrin antagonists
AU748621B2 (en) Integrin receptor antagonists
AU747784B2 (en) Integrin receptor antagonists
US5919792A (en) Integrin antagonists
AU720758B2 (en) Alphavbeta3 antagonists
US6413955B1 (en) Integrin receptor antagonists
US5952341A (en) Integrin antagonists
AU747503B2 (en) Benzazepine derivatives as alpha-V integrin receptor antagonists
AU1912899A (en) Integrin receptor antagonists
EP1194151A1 (fr) Antagonistes des recepteurs de l&#39;integrine
US5925655A (en) αv β3 antagonists
US6211184B1 (en) Integrin antagonists
US6294549B1 (en) Method for eliciting an αvβ5 or dual αvβ3/αvβ5 antagonizing effect
US6916810B2 (en) αν integrin receptor antagonists
CA2268916A1 (fr) Antagonistes de l&#39;integrine
Duggan et al. α v β 3 antagonists

Legal Events

Date Code Title Description
EEER Examination request
MKLA Lapsed