CA2491271A1 - 2-(phenyl)-2h-pyrazole-3-carboxylic acid-n-4-(thioxo-heterocyclyl)-phenyl-amide derivatives and corresponding imino-heterocyclyl derivatives and relates compounds for use as inhibitors of the coagulation factors xa and/or viia for treating thromboses - Google Patents

2-(phenyl)-2h-pyrazole-3-carboxylic acid-n-4-(thioxo-heterocyclyl)-phenyl-amide derivatives and corresponding imino-heterocyclyl derivatives and relates compounds for use as inhibitors of the coagulation factors xa and/or viia for treating thromboses Download PDF

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Publication number
CA2491271A1
CA2491271A1 CA002491271A CA2491271A CA2491271A1 CA 2491271 A1 CA2491271 A1 CA 2491271A1 CA 002491271 A CA002491271 A CA 002491271A CA 2491271 A CA2491271 A CA 2491271A CA 2491271 A1 CA2491271 A1 CA 2491271A1
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CA
Canada
Prior art keywords
phenyl
formula
compounds
disubstituted
monosubstituted
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.)
Abandoned
Application number
CA002491271A
Other languages
English (en)
French (fr)
Inventor
Bertram Cezanne
Dieter Dorsch
Werner Mederski
Christos Tsaklakidis
Johannes Gleitz
Christopher Barnes
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 Patent GmbH
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2491271A1 publication Critical patent/CA2491271A1/en
Abandoned legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433—Thidiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine 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
    • 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
    • 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
    • A61P9/08—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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA002491271A 2002-06-28 2003-06-05 2-(phenyl)-2h-pyrazole-3-carboxylic acid-n-4-(thioxo-heterocyclyl)-phenyl-amide derivatives and corresponding imino-heterocyclyl derivatives and relates compounds for use as inhibitors of the coagulation factors xa and/or viia for treating thromboses Abandoned CA2491271A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10229070A DE10229070A1 (de) 2002-06-28 2002-06-28 Phenylderivate 5
DE10229070.9 2002-06-28
PCT/EP2003/005898 WO2004002477A1 (de) 2002-06-28 2003-06-05 2-(phenyl)-2h-pyrazol-3-carbonsäure-n-4-(thioxo-heterocyclyl)-phenyl-amid derivate und entsprechende imino-heterocyclyl derivate sowie verwandte verbindungen als inhibitoren der koagulationsfaktoren xa und/oder viia zur behandlung bon thrombosen

Publications (1)

Publication Number Publication Date
CA2491271A1 true CA2491271A1 (en) 2004-01-08

Family

ID=29723536

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002491271A Abandoned CA2491271A1 (en) 2002-06-28 2003-06-05 2-(phenyl)-2h-pyrazole-3-carboxylic acid-n-4-(thioxo-heterocyclyl)-phenyl-amide derivatives and corresponding imino-heterocyclyl derivatives and relates compounds for use as inhibitors of the coagulation factors xa and/or viia for treating thromboses

Country Status (8)

Country Link
US (1) US20050203127A1 (https=)
EP (2) EP1679073A1 (https=)
JP (1) JP2005535630A (https=)
AR (1) AR040472A1 (https=)
AU (1) AU2003238475A1 (https=)
CA (1) CA2491271A1 (https=)
DE (1) DE10229070A1 (https=)
WO (1) WO2004002477A1 (https=)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002006234A1 (en) * 2000-07-17 2002-01-24 Takeda Chemical Industries, Ltd. Sulfone derivatives, process for their production and use thereof
AU2003284596A1 (en) * 2002-11-22 2004-06-18 Takeda Pharmaceutical Company Limited Imidazole derivative, process for producing the same, and use
TWI396686B (zh) * 2004-05-21 2013-05-21 Takeda Pharmaceutical 環狀醯胺衍生物、以及其製品和用法
DE102004051277A1 (de) * 2004-10-21 2006-04-27 Merck Patent Gmbh Heterocyclische Carbonylverbindungen
US7446210B2 (en) 2004-10-26 2008-11-04 Janssen Pharmaceutica N.V. Factor Xa compounds
DE102005038947A1 (de) 2005-05-18 2006-11-30 Grünenthal GmbH Substituierte Benzo[d]isoxazol-3-yl-amin-Verbindungen und deren Verwendung in Arzneimitteln
DE102005045115A1 (de) * 2005-09-21 2007-04-05 Siemens Ag Verfahren und Vorrichtung zum Betrieb eines Kommunikationsendgeräts
US8338367B2 (en) 2008-10-15 2012-12-25 Boehringer Ingelheim International Gmbh Fused heteroaryl diamide compounds useful as MMP-13 inhibitors
US8785489B2 (en) 2008-10-17 2014-07-22 Boehringer Ingelheim International Gmbh Heteroaryl substituted indole compounds useful as MMP-13 inhibitors
JP6155187B2 (ja) 2010-03-30 2017-06-28 ヴァーセオン コーポレイション トロンビンの阻害剤としての多置換芳香族化合物
HK1214252A1 (zh) 2013-03-15 2016-07-22 Verseon Corporation 作為凝血酶抑制劑的鹵代吡唑
CN110179795A (zh) 2013-03-15 2019-08-30 维颂公司 作为丝氨酸蛋白酶抑制剂的多取代芳族化合物的制药用途
JP6223563B2 (ja) 2013-10-14 2017-11-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 選択的に置換されたキノリン化合物
CN105636945B (zh) 2013-10-14 2017-11-17 卫材R&D管理有限公司 选择性取代的喹啉化合物
CN106257976B (zh) 2014-03-07 2021-02-02 拜奥克里斯特制药公司 人类血浆激肽释放酶抑制剂
US10189810B2 (en) 2014-09-17 2019-01-29 Verseon Corporation Pyrazolyl-substituted pyridone compounds as serine protease inhibitors
CN107405333A (zh) 2015-02-27 2017-11-28 维颂公司 作为丝氨酸蛋白酶抑制剂的被取代的吡唑化合物

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1246847A (zh) * 1996-12-23 2000-03-08 杜邦药品公司 作为Xa因子抑制剂的含氮杂芳族化合物
US6020357A (en) * 1996-12-23 2000-02-01 Dupont Pharmaceuticals Company Nitrogen containing heteroaromatics as factor Xa inhibitors
KR20010013977A (ko) * 1997-06-19 2001-02-26 블레어 큐. 퍼거슨 중성 ｐ1 특이성 기를 갖는 인자 ｘａ의 억제제
ZA985247B (en) * 1997-06-19 1999-12-17 Du Pont Merck Pharma Guanidine mimics as factor Xa inhibitors.
US5998424A (en) * 1997-06-19 1999-12-07 Dupont Pharmaceuticals Company Inhibitors of factor Xa with a neutral P1 specificity group

Also Published As

Publication number Publication date
AR040472A1 (es) 2005-04-06
EP1517685A1 (de) 2005-03-30
WO2004002477A8 (de) 2004-04-15
DE10229070A1 (de) 2004-01-15
JP2005535630A (ja) 2005-11-24
US20050203127A1 (en) 2005-09-15
WO2004002477A1 (de) 2004-01-08
EP1679073A1 (de) 2006-07-12
AU2003238475A1 (en) 2004-01-19

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Legal Events

Date Code Title Description
FZDE Discontinued