NO20002958L - Benzamidine derivatives as coagulation factor Xa inhibitors - Google Patents

Benzamidine derivatives as coagulation factor Xa inhibitors

Info

Publication number
NO20002958L
NO20002958L NO20002958A NO20002958A NO20002958L NO 20002958 L NO20002958 L NO 20002958L NO 20002958 A NO20002958 A NO 20002958A NO 20002958 A NO20002958 A NO 20002958A NO 20002958 L NO20002958 L NO 20002958L
Authority
NO
Norway
Prior art keywords
inhibitors
coagulation factor
benzamidine derivatives
benzamidine
derivatives
Prior art date
Application number
NO20002958A
Other languages
Norwegian (no)
Other versions
NO20002958D0 (en
Inventor
Dieter Dorsch
Horst Juraszyk
Hanns Wurziger
Joachim Gante
Werner Mederski
Hans-Peter Buchstaller
Soheila Anzali
Sabine Bernotat-Danielowski
Guido Melzer
Original Assignee
Merck Patent Gmbh
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 Patent Gmbh filed Critical Merck Patent Gmbh
Publication of NO20002958D0 publication Critical patent/NO20002958D0/en
Publication of NO20002958L publication Critical patent/NO20002958L/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • 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
    • 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
    • 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
    • A61P9/10—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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C311/05—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/18—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26—Sulfur atoms
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic 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
    • C07D417/14—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 three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Nye forbindelser med formel (1) hvor X, Y, W, R1, R2, R3 og R4 har de i patentkrav l angitte betydninger, er inhibitorer for koagulasjonsfaktor Xa og kan anvendes til profylakse og/eller behandling av tromboemboliske syk- dommer .New compounds of formula (1) wherein X, Y, W, R1, R2, R3 and R4 have the meanings set forth in claim 1, are inhibitors of coagulation factor Xa and can be used for the prophylaxis and / or treatment of thromboembolic diseases.

NO20002958A 1997-12-12 2000-06-09 Benzamidine derivatives as coagulation factor Xa inhibitors NO20002958L (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19755268A DE19755268A1 (en) 1997-12-12 1997-12-12 Benzamidine derivatives
PCT/EP1998/007673 WO1999031092A1 (en) 1997-12-12 1998-11-27 Benzamine derivatives

Publications (2)

Publication Number Publication Date
NO20002958D0 NO20002958D0 (en) 2000-06-09
NO20002958L true NO20002958L (en) 2000-08-11

Family

ID=7851688

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20002958A NO20002958L (en) 1997-12-12 2000-06-09 Benzamidine derivatives as coagulation factor Xa inhibitors

Country Status (16)

Country Link
EP (1) EP1056743A1 (en)
JP (1) JP2002508370A (en)
KR (1) KR20010032963A (en)
CN (1) CN1281451A (en)
AR (1) AR017844A1 (en)
AU (1) AU744002B2 (en)
BR (1) BR9813477A (en)
CA (1) CA2313651A1 (en)
DE (1) DE19755268A1 (en)
HU (1) HUP0004353A3 (en)
NO (1) NO20002958L (en)
PL (1) PL341008A1 (en)
RU (1) RU2203897C2 (en)
SK (1) SK8572000A3 (en)
WO (1) WO1999031092A1 (en)
ZA (1) ZA9811339B (en)

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SE9902987D0 (en) 1999-08-24 1999-08-24 Astra Pharma Prod Novel compounds
DE19962924A1 (en) * 1999-12-24 2001-07-05 Bayer Ag Substituted oxazolidinones and their use
AU2004202422B2 (en) * 1999-12-24 2007-11-22 Bayer Intellectual Property Gmbh Substituted oxazolidinones and their use in the field of blood coagulation
CO5300399A1 (en) 2000-02-25 2003-07-31 Astrazeneca Ab HETEROCICLIOCS CONTAINING NITROGEN, PROCESS FOR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
DE10027024A1 (en) * 2000-05-31 2001-12-06 Merck Patent Gmbh Carbamic acid ester
US7005439B2 (en) 2000-06-20 2006-02-28 Astrazeneca Ab Compounds
AR028948A1 (en) 2000-06-20 2003-05-28 Astrazeneca Ab NEW COMPOUNDS
DE10105989A1 (en) 2001-02-09 2002-08-14 Bayer Ag Substituted oxazolidinones and their use
GB0104050D0 (en) 2001-02-19 2001-04-04 Astrazeneca Ab Chemical compounds
AR035230A1 (en) 2001-03-19 2004-05-05 Astrazeneca Ab BENCIMIDAZOL COMPOUNDS, PROCESS FOR PREPARATION, PHARMACEUTICAL COMPOSITION, PROCESS FOR THE PREPARATION OF SUCH PHARMACEUTICAL COMPOSITION, AND USES OF THESE COMPOUNDS FOR THE PREPARATION OF MEDICINES
GB0107228D0 (en) 2001-03-22 2001-05-16 Astrazeneca Ab Chemical compounds
SE0101038D0 (en) 2001-03-23 2001-03-23 Astrazeneca Ab Novel compounds
DE10129725A1 (en) * 2001-06-20 2003-01-02 Bayer Ag Combination therapy of substituted oxazolidinones
SE0103818D0 (en) 2001-11-15 2001-11-15 Astrazeneca Ab Chemical compounds
DE10159453A1 (en) * 2001-12-04 2003-06-18 Merck Patent Gmbh Use of 1-phenyl-oxazolidin-2-one compounds as a protease
EP1569912B1 (en) 2002-12-03 2015-04-29 Pharmacyclics, Inc. 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors
PL209135B1 (en) * 2002-03-06 2011-07-29 Toyama Chemical Co Ltd Novel arylamidine derivative or salt thereof
DE10300111A1 (en) 2003-01-07 2004-07-15 Bayer Healthcare Ag Process for the preparation of 5-chloro-N - ({(5S) -2-oxo-3- [4- (3-oxo-4-morpholinyl) phenyl] -1,3-oxazolidin-5-yl} methyl ) -2-thiophenecarboxamide
SE0301369D0 (en) 2003-05-09 2003-05-09 Astrazeneca Ab Chemical compounds
DE10322469A1 (en) * 2003-05-19 2004-12-16 Bayer Healthcare Ag Heterocyclic compounds
KR20060065586A (en) 2003-06-23 2006-06-14 씨브이 쎄러퓨틱스, 인코포레이티드 Urea derivatives of piperazine and piperidine as fatty acid oxidation inhibitors
DE10355461A1 (en) 2003-11-27 2005-06-23 Bayer Healthcare Ag Solid, high bioavailabilty oral formulations of N-substituted 5-chloro-2-thiophene-carboxamide derivative in hydrophilized form, useful for combating thrombo-embolic diseases
EP1685841A1 (en) 2005-01-31 2006-08-02 Bayer Health Care Aktiengesellschaft Prevention and treatment of thromboembolic disorders
TW200738634A (en) 2005-08-02 2007-10-16 Astrazeneca Ab New salt
DE102005045518A1 (en) 2005-09-23 2007-03-29 Bayer Healthcare Ag New 5-thienylaminocarbonylmethyl-oxazolidin-2-one derivatives, useful for treating and preventing thromboembolic disease, are selective inhibitors of coagulation factor Xa
DE102005047561A1 (en) 2005-10-04 2007-04-05 Bayer Healthcare Ag Drug delivery system, useful to treat and/or prevent e.g. thromboembolic disease, comprises 5-chloro-N-(((5S)-2-oxo-3-(4-(3-oxo-4-morpholinyl)-phenyl)-1,3-oxazolidine-5-yl)-methyl)-2-thiophene carboxamide with fast release active substance
CA2823159C (en) 2005-10-04 2014-10-21 Bayer Intellectual Property Gmbh Polymorphic form of 5-chloro-n-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide
JP5102781B2 (en) * 2006-01-31 2012-12-19 ドン ファ ファーマシューティカル カンパニー リミテッド NOVEL BENZAMIDINE DERIVATIVE, PROCESS FOR PRODUCING THE SAME AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
DE102007018662A1 (en) 2007-04-20 2008-10-23 Bayer Healthcare Ag Oxazolidinone for the treatment and prophylaxis of pulmonary hypertension
KR101009594B1 (en) 2007-05-09 2011-01-20 주식회사 레고켐 바이오사이언스 FFA inhibitor having cyclic amidine at P4 position, derivative thereof, preparation method and pharmaceutical composition containing same
WO2008140220A1 (en) * 2007-05-09 2008-11-20 Legochem Bioscience Ltd. Fxa inhibitors with cyclic amidines as p4 subunit, processes for their preparations, and pharmaceutical compositions and derivatives thereof
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NZ582700A (en) * 2007-07-27 2011-04-29 Dong Wha Pharm Co Ltd Novel benzamidine derivatives, process for the preparation thereof and pharmaceutical composition for preventing or treating osteoporosis comprising the same
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Also Published As

Publication number Publication date
SK8572000A3 (en) 2001-07-10
NO20002958D0 (en) 2000-06-09
RU2203897C2 (en) 2003-05-10
KR20010032963A (en) 2001-04-25
HUP0004353A2 (en) 2002-03-28
BR9813477A (en) 2000-10-24
AU1964799A (en) 1999-07-05
AR017844A1 (en) 2001-10-24
PL341008A1 (en) 2001-03-12
CN1281451A (en) 2001-01-24
WO1999031092A1 (en) 1999-06-24
CA2313651A1 (en) 1999-06-24
AU744002B2 (en) 2002-02-14
ZA9811339B (en) 1999-07-08
DE19755268A1 (en) 1999-06-17
HUP0004353A3 (en) 2002-04-29
EP1056743A1 (en) 2000-12-06
JP2002508370A (en) 2002-03-19

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