UY27202A1 - AMIDAS OF CARBOXYLIC ACIDS ANTITROMBÓTICAS, ITS PREPARATION AND ITS EMPLOYMENT AS MEDICATIONS - Google Patents

AMIDAS OF CARBOXYLIC ACIDS ANTITROMBÓTICAS, ITS PREPARATION AND ITS EMPLOYMENT AS MEDICATIONS

Info

Publication number
UY27202A1
UY27202A1 UY27202A UY27202A UY27202A1 UY 27202 A1 UY27202 A1 UY 27202A1 UY 27202 A UY27202 A UY 27202A UY 27202 A UY27202 A UY 27202A UY 27202 A1 UY27202 A1 UY 27202A1
Authority
UY
Uruguay
Prior art keywords
preparation
antitrombóticas
amidas
medications
employment
Prior art date
Application number
UY27202A
Other languages
Spanish (es)
Inventor
Dr Uwe Ries
Dr Henning Priepke
Dr Herbert Nar
Dr Wolfgang Wienen
Dr Jean Marie Stassen
Original Assignee
Boehringer Ingelheim Pharma
Co Kg
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 Boehringer Ingelheim Pharma, Co Kg filed Critical Boehringer Ingelheim Pharma
Publication of UY27202A1 publication Critical patent/UY27202A1/en

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 presente invención se refiere a amidas de ácidos carboxílicos de la fórmula (I), en la que R1a R4, Het, Z1, A, Ar y m se definen como en la reivindicación 1. A sus tautómeros, sus estereoisómeros, sus mezclas, sus profármacos y sus sales, que presentan valiosas propiedades. Los compuestos de la fórmula I anterior, en los que R4 representa un grupo ciano, representan valiosos productos intermedios para la preparación de los restantes compuestos de la fórmula general I, y los compuestos de la fórmula general I, en los que R4 representa uno de los grupos amidino mencionados en la reivindicación 1 presentan valiosas propiedades farmacológicas, en particular un efecto antitrombótico y un efecto inhibidor del factor Xa.The present invention relates to carboxylic acid amides of the formula (I), wherein R1a R4, Het, Z1, A, Ar and m are defined as in claim 1. To their tautomers, their stereoisomers, their mixtures, their prodrugs and their salts, which have valuable properties. The compounds of the formula I above, in which R4 represents a cyano group, represent valuable intermediates for the preparation of the remaining compounds of the general formula I, and the compounds of the general formula I, in which R4 represents one of the amidino groups mentioned in claim 1 have valuable pharmacological properties, in particular an antithrombotic effect and a factor Xa inhibitory effect.

UY27202A 2001-03-13 2002-03-11 AMIDAS OF CARBOXYLIC ACIDS ANTITROMBÓTICAS, ITS PREPARATION AND ITS EMPLOYMENT AS MEDICATIONS UY27202A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10111842A DE10111842A1 (en) 2001-03-13 2001-03-13 Antithrombotic carboxylic acid amides, their preparation and their use as pharmaceuticals

Publications (1)

Publication Number Publication Date
UY27202A1 true UY27202A1 (en) 2002-10-31

Family

ID=7677159

Family Applications (1)

Application Number Title Priority Date Filing Date
UY27202A UY27202A1 (en) 2001-03-13 2002-03-11 AMIDAS OF CARBOXYLIC ACIDS ANTITROMBÓTICAS, ITS PREPARATION AND ITS EMPLOYMENT AS MEDICATIONS

Country Status (7)

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

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20040804A1 (en) 2002-12-19 2004-12-31 Boehringer Ingelheim Pharma CARBOXAMID DERIVATIVES AS INHIBITORS OF THE Xa FACTOR
CN1784388B (en) * 2003-03-13 2012-02-22 出光兴产株式会社 Nitrogen-containing heterocyclic derivative and organic electroluminescent element using same
AU2004283196B2 (en) 2003-09-17 2011-08-25 Janssen Pharmaceutica, N.V. Fused heterocyclic compounds
US7371743B2 (en) 2004-02-28 2008-05-13 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments
DE102004027821A1 (en) * 2004-06-08 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Benzimidazoles, process for their preparation and their use as medicaments
CA2577608A1 (en) * 2004-09-06 2006-03-16 F. Hoffmann-La Roche Ag 4-aminomethyl benzamidine derivatives and their use as factor viia inhibitors
CN101277700B (en) * 2005-08-04 2013-02-20 詹森药业有限公司 Pyrimidine compounds as serotonin receptor modulators
US7598255B2 (en) 2005-08-04 2009-10-06 Janssen Pharmaceutica Nv Pyrimidine compounds as serotonin receptor modulators
TW201444798A (en) 2013-02-28 2014-12-01 必治妥美雅史谷比公司 Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors
EP2961746B1 (en) 2013-02-28 2018-01-03 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors
MA54823A (en) 2019-01-24 2022-04-27 Takeda Pharmaceuticals Co HETEROCYCLIC COMPOUND AND ITS USE
JP2021050161A (en) 2019-09-25 2021-04-01 武田薬品工業株式会社 Heterocyclic compound and use thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6358960B1 (en) * 1998-02-17 2002-03-19 Ono Pharmaceutical Co., Ltd. Amidino derivatives and drugs containing the same as the active ingredient
DE19912690A1 (en) * 1999-03-20 2000-09-21 Boehringer Ingelheim Pharma New benzimidazolyl amidine or nitrile compounds, useful as thrombin inhibitors or antithrombotic agents, for treating deep leg vein thrombosis
DE19929787A1 (en) * 1999-06-29 2001-01-04 Bayer Ag New 4- (2-oxodihydrooxadiazinylphenyl) amides and their use
DE19937494A1 (en) * 1999-08-07 2001-02-08 Boehringer Ingelheim Pharma New carboxylic acid amides are Factor Xa and serine protease inhibitors, useful for the treatment and prevention of thrombotic disorders, tumors and fibrin-dependent inflammation

Also Published As

Publication number Publication date
CA2439231A1 (en) 2002-09-19
EP1370540A1 (en) 2003-12-17
MXPA03008186A (en) 2004-01-29
JP2004529905A (en) 2004-09-30
WO2002072558A1 (en) 2002-09-19
DE10111842A1 (en) 2002-09-19

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Legal Events

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Effective date: 20141126