WO2003011222A3 - Inhibiteurs de la thrombine - Google Patents

Inhibiteurs de la thrombine Download PDF

Info

Publication number
WO2003011222A3
WO2003011222A3 PCT/US2002/024219 US0224219W WO03011222A3 WO 2003011222 A3 WO2003011222 A3 WO 2003011222A3 US 0224219 W US0224219 W US 0224219W WO 03011222 A3 WO03011222 A3 WO 03011222A3
Authority
WO
WIPO (PCT)
Prior art keywords
thrombin inhibitors
thrombin
compounds
useful
following structure
Prior art date
Application number
PCT/US2002/024219
Other languages
English (en)
Other versions
WO2003011222A2 (fr
Inventor
Philippe G Nantermet
Harold G Selnick
James C Barrow
Christina L Di Newton
Original Assignee
Merck & Co Inc
Philippe G Nantermet
Harold G Selnick
James C Barrow
Newton Randall C
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
Application filed by Merck & Co Inc, Philippe G Nantermet, Harold G Selnick, James C Barrow, Newton Randall C filed Critical Merck & Co Inc
Priority to AU2002322802A priority Critical patent/AU2002322802A1/en
Publication of WO2003011222A2 publication Critical patent/WO2003011222A2/fr
Publication of WO2003011222A3 publication Critical patent/WO2003011222A3/fr

Links

Classifications

    • 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
    • C07D487/06—Peri-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/06—Peri-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

L'invention concerne des composés utiles pour inhiber la thrombine et les occlusions thrombotiques associées, représentés par la formule (I), par exemple un composé de formule (II).
PCT/US2002/024219 2001-07-27 2002-07-23 Inhibiteurs de la thrombine WO2003011222A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002322802A AU2002322802A1 (en) 2001-07-27 2002-07-23 Thrombin inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US30829801P 2001-07-27 2001-07-27
US60/308,298 2001-07-27

Publications (2)

Publication Number Publication Date
WO2003011222A2 WO2003011222A2 (fr) 2003-02-13
WO2003011222A3 true WO2003011222A3 (fr) 2004-03-18

Family

ID=23193395

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/024219 WO2003011222A2 (fr) 2001-07-27 2002-07-23 Inhibiteurs de la thrombine

Country Status (2)

Country Link
AU (1) AU2002322802A1 (fr)
WO (1) WO2003011222A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7212713B2 (ja) 2015-07-06 2023-01-25 ターニング・ポイント・セラピューティクス・インコーポレイテッド ジアリール大環状多形

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR058380A1 (es) 2005-12-23 2008-01-30 Bristol Myers Squibb Co Inhibidores del factor viia macrociclicos utiles como anticoagulantes
PE20081775A1 (es) * 2006-12-20 2008-12-18 Bristol Myers Squibb Co Compuestos macrociclicos como inhibidores del factor viia
TW201311689A (zh) 2011-08-05 2013-03-16 必治妥美雅史谷比公司 作為因子ｘｉａ抑制劑之新穎巨環化合物
TW201319068A (zh) * 2011-08-05 2013-05-16 必治妥美雅史谷比公司 作為ｘｉａ因子抑制劑之環狀ｐ１接合劑
HUE034857T2 (en) 2011-10-14 2018-03-28 Bristol Myers Squibb Co Substituted tetrahydroisoquinoline compounds are inhibitors of factor XIA
US9315519B2 (en) 2012-10-12 2016-04-19 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
US9403774B2 (en) 2012-10-12 2016-08-02 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
WO2014059203A1 (fr) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Formes cristallines d'un inhibiteur de facteur xia
CN105228996B (zh) 2013-03-25 2017-11-28 百时美施贵宝公司 作为因子XIa抑制剂的含取代唑类的四氢异喹啉
PE20210470A1 (es) 2014-01-31 2021-03-08 Bristol Myers Squibb Co Macrociclos con grupos p2' heterociclicos como inhibidores del factor xia
NO2760821T3 (fr) 2014-01-31 2018-03-10
CN107074821B (zh) 2014-09-04 2020-05-22 百时美施贵宝公司 为fxia抑制剂的二酰胺大环化合物
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
BROWN ET AL.: "Design of orally active, non-peptidic inhibitors of human leukocyte elastase", JOURNAL OF MEDICINAL CHEMISTRY, vol. 37, no. 9, 29 April 1994 (1994-04-29), pages 1259 - 1261, XP002916793 *
EDWARDS ET AL.: "Design, synthesis and kinetic evaluation of a unique class of elastase inhibitors, the peptidyl alpha-ketobenzoxazoles and the X-ray crystal structure of the covalent complex between procine pancreatic elastase and Ac-Ala-Pro-Val-2-benzoxazole", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 114, no. 5, 26 February 1992 (1992-02-26), pages 1854 - 1863, XP002915297 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7212713B2 (ja) 2015-07-06 2023-01-25 ターニング・ポイント・セラピューティクス・インコーポレイテッド ジアリール大環状多形
KR102623734B1 (ko) 2015-07-06 2024-01-10 터닝 포인트 테라퓨틱스, 인크. 디아릴 매크로사이클 다형체

Also Published As

Publication number Publication date
AU2002322802A1 (en) 2003-02-17
WO2003011222A2 (fr) 2003-02-13

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