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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)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Hematology (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)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20071132A1 (es) * 2005-12-23 2007-12-14 Bristol Myers Squibb Co Compuestos macrociclicos como inhibidores del factor viia
PE20081775A1 (es) * 2006-12-20 2008-12-18 Bristol Myers Squibb Co Compuestos macrociclicos como inhibidores del factor viia
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
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
EP3309148A1 (fr) 2011-10-14 2018-04-18 Bristol-Myers Squibb Company Composés de tétrahydroisiquinoline substitués en tant qu'inhibiteurs du facteur xia
WO2014059214A1 (fr) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Composés de tétrahydroisoquinoléine à substitution guanidine et amine utilisés comme inhibiteurs du facteur xia
EP2906552B1 (fr) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Composés de tetrahydroisoquinoline substitués par guanidine en tant qu'inhibiteurs de factor xia
PE20150639A1 (es) 2012-10-12 2015-05-11 Bristol Myers Squibb Co Formas cristalinas de inhibidor del factor 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
NO2760821T3 (fr) 2014-01-31 2018-03-10
ES2687498T3 (es) * 2014-01-31 2018-10-25 Bristol-Myers Squibb Company Macrociclos con grupos P2¿ heterocíclicos como inhibidores del factor XIa
EP3189047B1 (fr) 2014-09-04 2018-12-26 Bristol-Myers Squibb Company Diamides macrocycliques qui sont des inhibiteurs de fxia
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
US10294242B2 (en) 2015-07-06 2019-05-21 Tp Therapeutics, Inc. Diaryl macrocycle polymorph
CA2998885C (fr) * 2015-09-24 2020-09-01 Cyclenium Pharma Inc. Bibliotheques de composes macrocycliques contenant heteroaryle et procedes pour leur fabrication et leur utilisation

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 *

Also Published As

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

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