CA2439231A1 - Amides d'acide carboxylique antithrombotiques, leur preparation et leur utilisation comme medicaments - Google Patents

Amides d'acide carboxylique antithrombotiques, leur preparation et leur utilisation comme medicaments Download PDF

Info

Publication number
CA2439231A1
CA2439231A1 CA002439231A CA2439231A CA2439231A1 CA 2439231 A1 CA2439231 A1 CA 2439231A1 CA 002439231 A CA002439231 A CA 002439231A CA 2439231 A CA2439231 A CA 2439231A CA 2439231 A1 CA2439231 A1 CA 2439231A1
Authority
CA
Canada
Prior art keywords
group
phenyl
denotes
methyl
amidino
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
CA002439231A
Other languages
English (en)
Inventor
Henning Priepke
Herbert Nar
Jean Marie Stassen
Uwe Ries
Wolfgang Wienen
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.)
Boehringer Ingelheim Pharma GmbH and Co KG
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 CA2439231A1 publication Critical patent/CA2439231A1/fr
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • 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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/70—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08—Radicals containing only hydrogen and carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/14—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/26—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical

Landscapes

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

Abstract

La présente invention concerne des amides d'acide carboxylique de la formule (I), où R1 à R4, het, Z1, A, Ar, et m ont la définition donnée dans la 1ère revendication, leurs tautomères, leurs stéréoisomères, leurs mélanges, leurs prodrogues et leurs sels, qui ont de précieuses propriétés. Les composés de la formule I susmentionnée, où R4 représente un groupe cyano, constituent de précieux produits intermédiaires pour la production des composés susmentionnés de la formule générale I, et les composés de la formule générale (I) susmentionnée, où R4 représente un des groupes amidino mentionnés dans la 1ère revendication, ont de précieuses propriétés pharmacologiques, notamment une action antithrombotique et une action d'inhibition du facteur Xa.
CA002439231A 2001-03-13 2002-03-09 Amides d'acide carboxylique antithrombotiques, leur preparation et leur utilisation comme medicaments Abandoned CA2439231A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10111842A DE10111842A1 (de) 2001-03-13 2001-03-13 Antithrombotische Carbonsäureamide, deren Herstellung und deren Verwendung als Arzneimittel
DE10111842.2 2001-03-13
PCT/EP2002/002615 WO2002072558A1 (fr) 2001-03-13 2002-03-09 Amides d'acide carboxylique antithrombotiques, leur production et leur utilisation comme medicaments

Publications (1)

Publication Number Publication Date
CA2439231A1 true CA2439231A1 (fr) 2002-09-19

Family

ID=7677159

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002439231A Abandoned CA2439231A1 (fr) 2001-03-13 2002-03-09 Amides d'acide carboxylique antithrombotiques, leur preparation et leur utilisation comme medicaments

Country Status (7)

Country Link
EP (1) EP1370540A1 (fr)
JP (1) JP2004529905A (fr)
CA (1) CA2439231A1 (fr)
DE (1) DE10111842A1 (fr)
MX (1) MXPA03008186A (fr)
UY (1) UY27202A1 (fr)
WO (1) WO2002072558A1 (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7326791B2 (en) 2002-12-19 2008-02-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg Carboxylic acid amides, the preparation thereof, and their use as pharmaceutical compositions
US7371743B2 (en) 2004-02-28 2008-05-13 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments
US12630509B2 (en) 2019-11-14 2026-05-19 Takeda Pharmaceutical Company Limited Heterocyclic NMDA antagonists
US12637418B2 (en) 2019-01-24 2026-05-26 Takeda Pharmaceutical Company Limited Heterocyclic compounds as antagonist of NMDA

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004080975A1 (fr) * 2003-03-13 2004-09-23 Idemitsu Kosan Co., Ltd. Derive heterocyclique contenant de l'azote et element electroluminescent organique utilisant ce derive
SG146683A1 (en) 2003-09-17 2008-10-30 Janssen Pharmaceutica Nv Fused heterocyclic compounds as serotonin receptor modulators
DE102004027821A1 (de) * 2004-06-08 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Benzimidazole, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
JP2008512364A (ja) * 2004-09-06 2008-04-24 エフ．ホフマン−ラ ロシュ アーゲー ４−アミノメチルベンズアミジン誘導体及び第ＶＩＩａ因子阻害剤としてのその使用
EP1928461B1 (fr) * 2005-08-04 2012-01-04 Janssen Pharmaceutica NV Composes de pyrimidine utiles comme modulateurs des recepteurs de la serotonine
US7598255B2 (en) 2005-08-04 2009-10-06 Janssen Pharmaceutica Nv Pyrimidine compounds as serotonin receptor modulators
EP2961746B1 (fr) 2013-02-28 2018-01-03 Bristol-Myers Squibb Company Dérivés de phénylpyrazole en tant que puissants inhibiteurs de rock1 et rock2
AR094929A1 (es) 2013-02-28 2015-09-09 Bristol Myers Squibb Co Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2
JP2021050161A (ja) 2019-09-25 2021-04-01 武田薬品工業株式会社 複素環化合物及びその用途

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2300699A (en) * 1998-02-17 1999-08-30 Ono Pharmaceutical Co. Ltd. Amidino derivatives and drugs containing the same as the active ingredient
DE19912690A1 (de) * 1999-03-20 2000-09-21 Boehringer Ingelheim Pharma Benzimidazole, deren Herstellung und deren Verwendung als Arzneimittel
DE19929787A1 (de) * 1999-06-29 2001-01-04 Bayer Ag Neue 4-(2-Oxodihydrooxadiazinylphenyl)amide und ihre Verwendung
DE19937494A1 (de) * 1999-08-07 2001-02-08 Boehringer Ingelheim Pharma Carbonsäureamide, deren Herstellung und deren Verwendung als Arzneimittel

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7326791B2 (en) 2002-12-19 2008-02-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg Carboxylic acid amides, the preparation thereof, and their use as pharmaceutical compositions
US7371743B2 (en) 2004-02-28 2008-05-13 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments
US7947700B2 (en) 2004-02-28 2011-05-24 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments
US8445525B2 (en) 2004-02-28 2013-05-21 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments
US8791103B2 (en) 2004-02-28 2014-07-29 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments
US12637418B2 (en) 2019-01-24 2026-05-26 Takeda Pharmaceutical Company Limited Heterocyclic compounds as antagonist of NMDA
US12630509B2 (en) 2019-11-14 2026-05-19 Takeda Pharmaceutical Company Limited Heterocyclic NMDA antagonists

Also Published As

Publication number Publication date
UY27202A1 (es) 2002-10-31
EP1370540A1 (fr) 2003-12-17
WO2002072558A1 (fr) 2002-09-19
MXPA03008186A (es) 2004-01-29
DE10111842A1 (de) 2002-09-19
JP2004529905A (ja) 2004-09-30

Similar Documents

Publication Publication Date Title
AU763094B2 (en) Benzimidazoles, production thereof and use thereof as medicaments
US8445525B2 (en) Carboxylic acid amides, the preparation thereof and their use as medicaments
US20040220169A1 (en) Carboxylic acid amides, the preparation thereof, and their use as pharmaceutical compositions
US6114532A (en) Bicyclic heterocycles, the preparation thereof, and their use as pharmaceuticals
US6593355B2 (en) Benzimidazoles with antithrombotic activity
US20020183519A1 (en) Antithrombotic carboxylic acid amides
US6248770B1 (en) Benzimidazoles having antithrombotic activity
US20040248897A1 (en) Substituted N-acylaniline derivatives, the preparation thereof, and their use as pharmaceutical compositions
JP2004529905A (ja) 抗血栓性カルボン酸アミド、それらの調製及び医薬組成物としてのそれらの使用
US7425641B2 (en) Carboxylic acid amides, the preparation thereof and their use as pharmaceutical compositions
CA2393916A1 (fr) Benzimidazoles, leur preparation et leur utilisation dans les compositions pharmaceutiques
CA2435492A1 (fr) Composes antithrombotiques, leur preparation et leur utilisation comme produits pharmaceutiques
US20020151534A1 (en) Antithrombotic compounds
US20020151595A1 (en) Carboxylic acid amides having antithrombotic activity
US20080015178A1 (en) Benzimidazoles, process for their preparation and use thereof as medicament
US6838565B2 (en) Substituted benzoic acid amides, their preparation and their use as pharmaceutical compositions
CA2436837A1 (fr) Amides d'acide carboxylique, leur preparation et leur utilisation comme produit pharmaceutique
US20040077729A1 (en) New carboxylic acid amides, the preparation thereof and their use as pharmaceutical compositions
US7005437B2 (en) Substituted aryl and heteroaryl derivatives, the preparation thereof and the use therof as pharmaceutical compositions
CA2445571A1 (fr) Derives aryliques et heteroaryliques substitues, methode de preparation connexe et utilisation desdits derives comme compositions pharmaceutiques
DE10104598A1 (de) Carbonsäureamide, deren Herstellung und deren Verwendung als Arzneimittel
DE10234057A1 (de) Neue Carbonsäureamide, deren Herstellung und deren Verwendung als Arzneimittel

Legal Events

Date Code Title Description
FZDE Dead