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WO2003011222A3 - Thrombin inhibitors - Google Patents

Thrombin inhibitors 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
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.)
Ceased
Application number
PCT/US2002/024219
Other languages
French (fr)
Other versions
WO2003011222A2 (en
Inventor
Philippe G Nantermet
Harold G Selnick
James C Barrow
Christina L Di Newton
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
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Priority to AU2002322802A priority Critical patent/AU2002322802A1/en
Publication of WO2003011222A2 publication Critical patent/WO2003011222A2/en
Anticipated expiration legal-status Critical
Publication of WO2003011222A3 publication Critical patent/WO2003011222A3/en
Ceased legal-status Critical Current

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

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: e.g. .
PCT/US2002/024219 2001-07-27 2002-07-23 Thrombin inhibitors Ceased WO2003011222A2 (en)

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 (en) 2003-02-13
WO2003011222A3 true WO2003011222A3 (en) 2004-03-18

Family

ID=23193395

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/024219 Ceased WO2003011222A2 (en) 2001-07-27 2002-07-23 Thrombin inhibitors

Country Status (2)

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

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR058380A1 (en) * 2005-12-23 2008-01-30 Bristol Myers Squibb Co INHIBITORS OF THE VIEW MACROCICLIC FACTOR USEFUL AS ANTICOAGULANTS
PE20081775A1 (en) * 2006-12-20 2008-12-18 Bristol Myers Squibb Co MACROCYCLIC COMPOUNDS AS INHIBITORS OF FACTOR VIIA
TW201311689A (en) 2011-08-05 2013-03-16 必治妥美雅史谷比公司 Novel macrocyclic compounds as factor XIA inhibitors
TW201319068A (en) * 2011-08-05 2013-05-16 必治妥美雅史谷比公司 Cyclic P1 linkers as factor XIa inhibitors
ES2625256T3 (en) 2011-10-14 2017-07-19 Bristol-Myers Squibb Company Tetrahydroisoquinoline compounds substituted as XIA factor inhibitors
PE20150639A1 (en) 2012-10-12 2015-05-11 Bristol Myers Squibb Co CRYSTAL FORMS OF XIA FACTOR INHIBITOR
EP2906552B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
WO2014059214A1 (en) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
US9738655B2 (en) 2013-03-25 2017-08-22 Bristol-Myers Squibb Company Tetrahydroisoquinolines containing substituted azoles as factor XIa inhibitors
PE20210470A1 (en) * 2014-01-31 2021-03-08 Bristol Myers Squibb Co MACROCYCLES WITH P2 'HETEROCYCLIC GROUPS AS INHIBITORS OF THE XIA FACTOR
NO2760821T3 (en) 2014-01-31 2018-03-10
US10081623B2 (en) 2014-09-04 2018-09-25 Bristol-Myers Squibb Company Diamide macrocycles that are FXIa inhibitors
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
MX386680B (en) 2015-07-06 2025-03-19 Turning Point Therapeutics Inc DIARYL MACROCYCLE POLYMORPHOUS.
WO2017049383A1 (en) * 2015-09-24 2017-03-30 Cyclenium Pharma Inc. Libraries of heteroaryl-containing macrocyclic compounds and methods of making and using the same

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 (en) 2003-02-13
AU2002322802A1 (en) 2003-02-17

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