CN1589145A - αv整联蛋白受体拮抗剂 - Google Patents

αv整联蛋白受体拮抗剂 Download PDF

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Publication number
CN1589145A
CN1589145A CNA00811157XA CN00811157A CN1589145A CN 1589145 A CN1589145 A CN 1589145A CN A00811157X A CNA00811157X A CN A00811157XA CN 00811157 A CN00811157 A CN 00811157A CN 1589145 A CN1589145 A CN 1589145A
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China
Prior art keywords
tetrahydro
oxo
nonanoic acid
pyrimidin
naphthyridin
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Pending
Application number
CNA00811157XA
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English (en)
Chinese (zh)
Inventor
P·J·科莱曼
M·E·杜甘
W·哈尔岑科
G·D·哈特曼
J·H·胡钦森
R·S·梅斯纳
M·A·帕塔尼
J·J·珀金斯
王家炳
M·J·布雷斯林
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Merck and Co Inc
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Merck and Co Inc
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Filing date
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Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of CN1589145A publication Critical patent/CN1589145A/zh
Pending legal-status Critical Current

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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (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)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Obesity (AREA)
  • Immunology (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)
CNA00811157XA 1999-06-02 2000-05-30 αv整联蛋白受体拮抗剂 Pending CN1589145A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US13710199P 1999-06-02 1999-06-02
US60/137,101 1999-06-02
US17921600P 2000-01-31 2000-01-31
US60/179,216 2000-01-31

Publications (1)

Publication Number Publication Date
CN1589145A true CN1589145A (zh) 2005-03-02

Family

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Family Applications (1)

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CNA00811157XA Pending CN1589145A (zh) 1999-06-02 2000-05-30 αv整联蛋白受体拮抗剂

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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)
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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)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105246889A (zh) * 2013-02-07 2016-01-13 赛弗卢尔生命科学公司 氟化整联蛋白拮抗剂
US9593114B2 (en) 2013-02-07 2017-03-14 Scifluor Life Sciences, Inc. Fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives
CN107531699A (zh) * 2015-02-19 2018-01-02 赛弗卢尔生命科学公司 氟化四氢萘啶基壬酸衍生物及其用途
CN109476632A (zh) * 2016-07-05 2019-03-15 洛克菲勒大学 四氢萘啶戊酰胺整联蛋白拮抗剂
CN110167934A (zh) * 2016-11-08 2019-08-23 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
CN110167933A (zh) * 2016-11-08 2019-08-23 百时美施贵宝公司 作为αV整联蛋白抑制剂的唑酰胺和胺
US12497399B2 (en) 2023-06-21 2025-12-16 Ocuterra Therapeutics, Inc. Fluorinated integrin antagonists

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DE60126496T2 (de) * 2000-07-26 2007-11-15 Merck & Co., Inc. Alpha v integrin-rezeptor-antagonisten
AU2001290772A1 (en) * 2000-09-14 2002-03-26 Merck And Co., Inc. Alpha v integrin receptor antagonists
WO2002028395A1 (en) * 2000-10-04 2002-04-11 Merck & Co., Inc. Phosphoric acid salt of an integrin receptor antagonist
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KR20080089489A (ko) 2006-01-18 2008-10-06 메르크 파텐트 게엠베하 인테그린 리간드를 사용하는 암치료용 특이적 요법
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GB201417002D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compound
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TW201823208A (zh) 2016-09-07 2018-07-01 美商普萊恩醫療公司 N－醯基胺基酸化合物及其使用方法
EP3589285A4 (en) 2017-02-28 2020-08-12 Morphic Therapeutic, Inc. INHIBITORS OF INTEGRIN (ALPHA-V) (BETA-6)
CN116283977A (zh) 2017-02-28 2023-06-23 莫菲克医疗股份有限公司 αvβ6整合蛋白的抑制剂
SG11202101913PA (en) 2018-08-29 2021-03-30 Morphic Therapeutic Inc INHIBITING aV ß6 INTEGRIN

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Cited By (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105246889B (zh) * 2013-02-07 2018-07-31 赛弗卢尔生命科学公司 氟化整联蛋白拮抗剂
US11685737B2 (en) 2013-02-07 2023-06-27 Ocuterra Therapeutics, Inc. Fluorinated integrin antagonists
US9593114B2 (en) 2013-02-07 2017-03-14 Scifluor Life Sciences, Inc. Fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives
US9717729B2 (en) 2013-02-07 2017-08-01 Scifluor Life Sciences, Inc. Fluorinated integrin antagonists
US9802933B2 (en) 2013-02-07 2017-10-31 Scifluor Life Sciences, Inc. Fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives
CN108690022B (zh) * 2013-02-07 2021-08-17 赛弗卢尔生命科学公司 氟化整联蛋白拮抗剂
US10106537B2 (en) 2013-02-07 2018-10-23 Scifluor Life Sciences, Inc. Fluorinated integrin antagonists
CN108690022A (zh) * 2013-02-07 2018-10-23 赛弗卢尔生命科学公司 氟化整联蛋白拮抗剂
US9518053B2 (en) 2013-02-07 2016-12-13 Scifluor Life Sciences, Inc. Fluorinated integrin antagonists
US10155758B2 (en) 2013-02-07 2018-12-18 Scifluor Life Sciences, Inc. Fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives
CN105246889A (zh) * 2013-02-07 2016-01-13 赛弗卢尔生命科学公司 氟化整联蛋白拮抗剂
US12286432B2 (en) 2015-02-19 2025-04-29 Ocuterra Therapeutics, Inc. Fluorinated tetrahydronaphthyridinyl nonanoic acid derivatives and uses thereof
US11685738B2 (en) 2015-02-19 2023-06-27 Ocuterra Therapeutics, Inc. Fluorinated tetrahydronaphthyridinyl nonanoic acid derivatives and uses thereof
CN107531699A (zh) * 2015-02-19 2018-01-02 赛弗卢尔生命科学公司 氟化四氢萘啶基壬酸衍生物及其用途
CN109476632A (zh) * 2016-07-05 2019-03-15 洛克菲勒大学 四氢萘啶戊酰胺整联蛋白拮抗剂
CN110167933B (zh) * 2016-11-08 2022-06-21 百时美施贵宝公司 作为αV整联蛋白抑制剂的唑酰胺和胺
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
CN110167933A (zh) * 2016-11-08 2019-08-23 百时美施贵宝公司 作为αV整联蛋白抑制剂的唑酰胺和胺
CN110167934A (zh) * 2016-11-08 2019-08-23 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
US12497399B2 (en) 2023-06-21 2025-12-16 Ocuterra Therapeutics, Inc. Fluorinated integrin antagonists

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EP1187592B1 (en) 2007-08-01
TR200103431T2 (tr) 2002-06-21
WO2000072801A3 (en) 2007-10-11
EP1187592A2 (en) 2002-03-20
WO2000072801A2 (en) 2000-12-07
AU5724600A (en) 2000-12-18
EP1187592A4 (en) 2002-11-06
EA200101272A1 (ru) 2002-06-27
AU749351B2 (en) 2002-06-27
BG106232A (en) 2002-06-28
SK17442001A3 (sk) 2002-03-05
HRP20010895A2 (en) 2003-08-31
CZ20014308A3 (cs) 2002-03-13
NO323906B1 (no) 2007-07-16
DE60035779D1 (de) 2007-09-13
DZ3263A1 (fr) 2000-12-07
IS6157A (is) 2001-11-13
DK1187592T3 (da) 2007-11-05
ES2288861T3 (es) 2008-02-01
CA2373937A1 (en) 2000-12-07
DE60035779T2 (de) 2008-04-30
PL353364A1 (en) 2003-11-17
IL146378A0 (en) 2002-07-25
US6410526B1 (en) 2002-06-25
HUP0302468A2 (hu) 2003-11-28
PT1187592E (pt) 2007-10-19
NO20015858D0 (no) 2001-11-30
JP2004500326A (ja) 2004-01-08
NO20015858L (no) 2002-02-04
CY1107746T1 (el) 2013-04-18
ATE368462T1 (de) 2007-08-15
JP2006206604A (ja) 2006-08-10
EE200100642A (et) 2003-02-17
KR20020021380A (ko) 2002-03-20
BR0011108A (pt) 2002-03-19
JP2006232844A (ja) 2006-09-07
JP3808707B2 (ja) 2006-08-16

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