DE60035779T2 - Alpha v integrin-rezeptor antagonisten - Google Patents

Alpha v integrin-rezeptor antagonisten Download PDF

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Publication number
DE60035779T2
DE60035779T2 DE60035779T DE60035779T DE60035779T2 DE 60035779 T2 DE60035779 T2 DE 60035779T2 DE 60035779 T DE60035779 T DE 60035779T DE 60035779 T DE60035779 T DE 60035779T DE 60035779 T2 DE60035779 T2 DE 60035779T2
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DE
Germany
Prior art keywords
alkyl
oxo
alkylamino
tetrahydro
inhibitor
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
DE60035779T
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German (de)
English (en)
Other versions
DE60035779D1 (de
Inventor
Paul J. Rahway COLEMAN
Mark E. Rahway DUGGAN
Wasyl Rahway HALCZENKO
George D. Rahway HARTMAN
John H. Rahway HUTCHINSON
Robert S. Rahway MEISSNER
Michael A. Rahway PATANE
James J. Rahway PERKINS
Jiabing Rahway WANG
Michael J. Rahway BRESLIN
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
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Merck and Co Inc
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Publication date
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Publication of DE60035779D1 publication Critical patent/DE60035779D1/de
Publication of DE60035779T2 publication Critical patent/DE60035779T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
DE60035779T 1999-06-02 2000-05-30 Alpha v integrin-rezeptor antagonisten Expired - Fee Related DE60035779T2 (de)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US13710199P 1999-06-02 1999-06-02
US137101P 1999-06-02
US17921600P 2000-01-31 2000-01-31
US179216P 2000-01-31
PCT/US2000/014901 WO2000072801A2 (en) 1999-06-02 2000-05-30 Alpha v integrin receptor antagonists

Publications (2)

Publication Number Publication Date
DE60035779D1 DE60035779D1 (de) 2007-09-13
DE60035779T2 true DE60035779T2 (de) 2008-04-30

Family

ID=26834930

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60035779T Expired - Fee Related DE60035779T2 (de) 1999-06-02 2000-05-30 Alpha v integrin-rezeptor antagonisten

Country Status (28)

Country Link
US (1) US6410526B1 (enExample)
EP (1) EP1187592B1 (enExample)
JP (3) JP3808707B2 (enExample)
KR (1) KR20020021380A (enExample)
CN (1) CN1589145A (enExample)
AT (1) ATE368462T1 (enExample)
AU (1) AU749351B2 (enExample)
BG (1) BG106232A (enExample)
BR (1) BR0011108A (enExample)
CA (1) CA2373937A1 (enExample)
CY (1) CY1107746T1 (enExample)
CZ (1) CZ20014308A3 (enExample)
DE (1) DE60035779T2 (enExample)
DK (1) DK1187592T3 (enExample)
DZ (1) DZ3263A1 (enExample)
EA (1) EA200101272A1 (enExample)
EE (1) EE200100642A (enExample)
ES (1) ES2288861T3 (enExample)
HR (1) HRP20010895A2 (enExample)
HU (1) HUP0302468A2 (enExample)
IL (1) IL146378A0 (enExample)
IS (1) IS6157A (enExample)
NO (1) NO323906B1 (enExample)
PL (1) PL353364A1 (enExample)
PT (1) PT1187592E (enExample)
SK (1) SK17442001A3 (enExample)
TR (1) TR200103431T2 (enExample)
WO (1) WO2000072801A2 (enExample)

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AU7793501A (en) * 2000-07-26 2002-02-05 Merck & Co Inc Alpha v integrin receptor antagonists
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AU2001296439A1 (en) * 2000-10-04 2002-04-15 Merck & Co., Inc. Phosphoric acid salt of an integrin receptor antagonist
AU2002246757B2 (en) * 2001-01-03 2006-02-02 Merck & Co., Inc. Methods and compositions for treating periodontal disease
CN1247258C (zh) 2001-04-24 2006-03-29 默克专利有限公司 使用抗血管生成剂和TNFα的联合疗法
CA2478317A1 (en) * 2002-03-04 2003-09-18 Medimmune, Inc. Methods of preventing or treating disorders by administering an integrin .alpha.v.beta.3 antagonist in combination with an hmg-coa reductase inhibitor or a bisphosphonate
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US20040224986A1 (en) 2002-08-16 2004-11-11 Bart De Corte Piperidinyl targeting compounds that selectively bind integrins
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US7288655B2 (en) * 2003-03-07 2007-10-30 Merck & Co., Inc. α v integrin receptor antagonists
US8604185B2 (en) 2004-07-20 2013-12-10 Genentech, Inc. Inhibitors of angiopoietin-like 4 protein, combinations, and their use
KR20080089489A (ko) 2006-01-18 2008-10-06 메르크 파텐트 게엠베하 인테그린 리간드를 사용하는 암치료용 특이적 요법
EA017864B1 (ru) 2007-01-18 2013-03-29 Мерк Патент Гмбх Специфическая терапия и лекарственное средство на основе интегриновых лигандов для лечения рака
CL2008000467A1 (es) * 2007-02-14 2008-08-22 Janssen Pharmaceutica Nv Compuestos derivados de 2-aminopirimidina, moduladores del receptor histamina h4; su procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar un trastorno inflamatorio seleccionado de alegia, asma
EP2730282A1 (en) 2007-11-08 2014-05-14 The General Hospital Corporation Methods and compositions for the treatment of proteinuric diseases
AU2010252280A1 (en) 2009-05-25 2012-01-19 Merck Patent Gmbh Continuous administration of cilengitide in cancer treatments
EP3266782B1 (en) * 2013-02-07 2019-10-30 SciFluor Life Sciences, Inc. Fluorinated integrin antagonists
US8901144B2 (en) 2013-02-07 2014-12-02 Scifluor Life Sciences, Llc Fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives
GB201305668D0 (en) 2013-03-28 2013-05-15 Glaxosmithkline Ip Dev Ltd Avs6 Integrin Antagonists
DK3929196T3 (da) 2013-09-24 2023-09-25 Fujifilm Corp Farmaceutisk sammensætning af en nitrogenholdig forbindelse eller salt deraf, eller metalkompleks deraf
GB201417011D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
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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
CN110167934B (zh) * 2016-11-08 2022-06-10 百时美施贵宝公司 作为αV整联蛋白抑制剂的含有环丁烷和含有氮杂环丁烷的单环和螺环化合物
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US11046685B2 (en) 2017-02-28 2021-06-29 Morphic Therapeutic, Inc. Inhibitors of (α-v)(β-6) integrin
EP4159727B1 (en) 2017-02-28 2026-04-08 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
PT3844162T (pt) 2018-08-29 2025-03-28 Morphic Therapeutic Inc Inibidores da integrina alfa v beta6
AU2019327475B2 (en) 2018-08-29 2025-06-05 Morphic Therapeutic, Inc. INHIBITING αV β6 INTEGRIN
WO2020047208A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
TW202615058A (zh) 2024-06-12 2026-04-16 美商艾拉倫製藥股份有限公司 失養強直性肌肉蛋白質激酶（ｄｍｐｋ）ｉｒｎａ組成物及其使用方法
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Also Published As

Publication number Publication date
EE200100642A (et) 2003-02-17
IS6157A (is) 2001-11-13
JP2006206604A (ja) 2006-08-10
ES2288861T3 (es) 2008-02-01
CN1589145A (zh) 2005-03-02
CY1107746T1 (el) 2013-04-18
SK17442001A3 (sk) 2002-03-05
EP1187592A2 (en) 2002-03-20
BG106232A (en) 2002-06-28
NO323906B1 (no) 2007-07-16
HRP20010895A2 (en) 2003-08-31
BR0011108A (pt) 2002-03-19
AU5724600A (en) 2000-12-18
US6410526B1 (en) 2002-06-25
IL146378A0 (en) 2002-07-25
WO2000072801A3 (en) 2007-10-11
CA2373937A1 (en) 2000-12-07
JP3808707B2 (ja) 2006-08-16
HUP0302468A2 (hu) 2003-11-28
CZ20014308A3 (cs) 2002-03-13
PT1187592E (pt) 2007-10-19
ATE368462T1 (de) 2007-08-15
WO2000072801A2 (en) 2000-12-07
EP1187592A4 (en) 2002-11-06
DE60035779D1 (de) 2007-09-13
DZ3263A1 (fr) 2000-12-07
NO20015858L (no) 2002-02-04
DK1187592T3 (da) 2007-11-05
JP2004500326A (ja) 2004-01-08
AU749351B2 (en) 2002-06-27
EP1187592B1 (en) 2007-08-01
JP2006232844A (ja) 2006-09-07
KR20020021380A (ko) 2002-03-20
PL353364A1 (en) 2003-11-17
NO20015858D0 (no) 2001-11-30
TR200103431T2 (tr) 2002-06-21
EA200101272A1 (ru) 2002-06-27

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