+

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

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/06Peri-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/06Peri-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 (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200745062A (en) 2005-12-23 2007-12-16 Bristol Myers Squibb Co Macrocyclic factor VIIA inhibitors useful as anticoagulants
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
SI2766346T1 (sl) 2011-10-14 2017-05-31 Bristol-Myers Squibb Company Substituirane tetrahidroizokinolinske spojine kot faktor xia inhibitorji
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
CA2888100A1 (fr) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Formes cristallines d'un inhibiteur de facteur xia
US9315519B2 (en) 2012-10-12 2016-04-19 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
JP6479763B2 (ja) 2013-03-25 2019-03-06 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 第xia因子阻害剤としての置換アゾール含有のテトラヒドロイソキノリン
SG10201908467RA (en) * 2014-01-31 2019-10-30 Bristol Myers Squibb Co Macrocycles with hetrocyclic p2' groups as factor xia inhibitors
NO2760821T3 (fr) 2014-01-31 2018-03-10
ES2714283T3 (es) 2014-09-04 2019-05-28 Bristol Myers Squibb Co Macrociclos de diamida que son inhibidores de FXIa
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
WO2017049383A1 (fr) * 2015-09-24 2017-03-30 Cyclenium Pharma Inc. Bibliothèques de composés macrocycliques contenant hétéroaryle et procédés 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 *

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
WO2003011222A2 (fr) 2003-02-13
AU2002322802A1 (en) 2003-02-17

Similar Documents

Publication Publication Date Title
DE69709727D1 (de) Parazinon thrombin inhibitoren
AU2002250394A1 (en) Rho-kinase inhibitors
AU2002245709A1 (en) Rho-kinase inhibitors
WO2003088897A3 (fr) Inhibiteurs de fab i
WO2003059296A3 (fr) Compositions a base de collagene et procedes d'utilisation
EP1628530B8 (fr) Procedes et compositions pour la prevention et le traitement de la sepsie
WO2003011222A3 (fr) Inhibiteurs de la thrombine
AU1624801A (en) Plasminogen activator inhibitor antagonists related applications
GB0125445D0 (en) Protease Inhibitors
HK1070008A1 (en) Combination of cytochome p 450 dependent protease inhibitors
AU2001245764A1 (en) Novel compounds and compositions as protease inhibitors
AU2002345796A1 (en) Compositions and methods for inhibiting platelet activation and thrombosis
AU2002306734A1 (en) Inhibitors of plasmepsins
WO2002070457A8 (fr) Inhibiteur de la capture de la monoamine
AU2002351076A1 (en) Thrombin inhibitors
AU2001278997A1 (en) Thrombin inhibitors
AU2002342682A1 (en) Protease inhibitors
AU2001251057A1 (en) Multi-domain proteinase inhibitor
AU2002315398A1 (en) Methods and compositions useful for the prediction of blood-brain barrier permeation
AU2002305868A1 (en) Inhibitors of reggamma
AU2002363791A1 (en) Protease enzyme inhibitors
GB0109278D0 (en) Enzyme inhibitors
AU2002247158A1 (en) Thrombin inhibitors
AU2002317322A1 (en) Processes for the manufacture of thrombin inhibitors and n-pyridin-4-yl-oxazolidin-2-ones as intermediate therefor
AU2003247401A1 (en) Compositions and methods involving inhibiting or enhancing the deubiquitylation of an enzyme

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BY BZ CA CH CN CO CR CU CZ DE DM DZ EC EE ES FI GB GD GE GH HR HU ID IL IN IS JP KE KG KR KZ LK LR LS LT LU LV MA MD MG MK MW MX MZ NO NZ OM PH PL PT RO SD SE SG SI SK SL TJ TM TN TR TT UA UG US UZ VN YU ZA ZM

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ OM PH PL PT RO RU SD SE SG SI SK SL TJ TM TN TR TT TZ UA UG US UZ VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR IE IT LU MC NL PT SE SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ UG ZM ZW AM AZ BY KG KZ RU TJ TM AT BE BG CH CY CZ DK EE ES FI FR GB GR IE IT LU MC PT SE SK TR BF BJ CF CG CI GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: JP

WWW Wipo information: withdrawn in national office

Country of ref document: JP

点击 这是indexloc提供的php浏览器服务,不要输入任何密码和下载