WO2001070678A3 - Substituierte biphenylderivate - Google Patents

Substituierte biphenylderivate Download PDF

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Publication number
WO2001070678A3
WO2001070678A3 PCT/EP2001/003375 EP0103375W WO0170678A3 WO 2001070678 A3 WO2001070678 A3 WO 2001070678A3 EP 0103375 W EP0103375 W EP 0103375W WO 0170678 A3 WO0170678 A3 WO 0170678A3
Authority
WO
WIPO (PCT)
Prior art keywords
con
compounds
optionally substituted
substituted biphenyl
biphenyl derivatives
Prior art date
Application number
PCT/EP2001/003375
Other languages
English (en)
French (fr)
Other versions
WO2001070678A2 (de
Inventor
Horst Juraszyk
Dieter Dorsch
Werner Mederski
Christos Tsaklakidis
Christopher Barnes
Johannes Gleitz
Original Assignee
Merck Patent Gmbh
Horst Juraszyk
Dieter Dorsch
Werner Mederski
Christos Tsaklakidis
Christopher Barnes
Johannes Gleitz
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, Horst Juraszyk, Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Christopher Barnes, Johannes Gleitz filed Critical Merck Patent Gmbh
Priority to EP01927797A priority Critical patent/EP1268413A2/de
Priority to JP2001568890A priority patent/JP2003528077A/ja
Priority to CA002403500A priority patent/CA2403500A1/en
Priority to US10/239,397 priority patent/US6946489B2/en
Publication of WO2001070678A2 publication Critical patent/WO2001070678A2/de
Publication of WO2001070678A3 publication Critical patent/WO2001070678A3/de

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C317/34—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring
    • C07C317/38—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring with the nitrogen atom of at least one amino group being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfones
    • C07C317/40—Y being a hydrogen or a carbon atom
    • 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
    • A61P9/08—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
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (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)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)

Abstract

Die Erfindung betrifft Verbindungen der Formel (I), worin R1: durch -C(=NH)NH¿2?, das auch einfach durch -COA, -CO-, [C(R?7)¿2]n-Ar', -COOA, OR7, OCOA, OCO-[C(R7)2]n2-Ar', -OH oder durch eine konventionelle Aminoschutzgruppe substituiert sein kann, -NHC(=NH)-NH2', -CON=C(NH2)2, substituiertes Phenyl oder Naphthyl, das gegebenenfalls durch -A, OR?6, -N(R6)¿2, -NO2, -CN, -Hal, -NR5COA, -NR5COAr', -NR6So2A, -NR5SO2Ar', -COOR5, -CON(R5)2, -COR7, -COAr', oder S(O)¿n?A substituiert sein kann; R?2¿: -S(O)¿n?A, -CF3, -COOR?7¿, -OA; bedeuten, und worin R?3, R4, R5, R7¿, A und X die im Text angegebene Bedeutung haben. Die Verbindungen wirken als Inhibitoren der Faktoren Xa und VIIa und können daher zur Bekämpfung und Verhütung von thromboembolischen Erkrankungen wie Thrombose, myocardialem Infarkt, Arteriosklerose, Entzündungen, Apoplexie, Angina pectoris, Restenose nach Angioplastie und Claudicatio intermittens eingsetzt werden.
PCT/EP2001/003375 2000-03-24 2001-03-23 Substituierte biphenylderivate WO2001070678A2 (de)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP01927797A EP1268413A2 (de) 2000-03-24 2001-03-23 Substituierte biphenylderivate
JP2001568890A JP2003528077A (ja) 2000-03-24 2001-03-23 置換ビフェニル誘導体
CA002403500A CA2403500A1 (en) 2000-03-24 2001-03-23 Substituted biphenyl derivatives
US10/239,397 US6946489B2 (en) 2000-03-24 2001-03-23 Substituted biphenyl derivatives

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10014645A DE10014645A1 (de) 2000-03-24 2000-03-24 Substituierte Biphenylderivate
DE10014645.7 2000-03-24

Publications (2)

Publication Number Publication Date
WO2001070678A2 WO2001070678A2 (de) 2001-09-27
WO2001070678A3 true WO2001070678A3 (de) 2002-04-04

Family

ID=7636185

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2001/003375 WO2001070678A2 (de) 2000-03-24 2001-03-23 Substituierte biphenylderivate

Country Status (6)

Country Link
US (1) US6946489B2 (de)
EP (1) EP1268413A2 (de)
JP (1) JP2003528077A (de)
CA (1) CA2403500A1 (de)
DE (1) DE10014645A1 (de)
WO (1) WO2001070678A2 (de)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1332131A2 (de) * 2000-11-07 2003-08-06 Bristol-Myers Squibb Company Säurederivate und ihre verwendung als inhibitoren von serinproteasen
US6906192B2 (en) 2000-11-07 2005-06-14 Bristol Myers Squibb Company Processes for the preparation of acid derivatives useful as serine protease inhibitors
AU2002231235A1 (en) * 2000-11-07 2002-05-21 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
JP4886948B2 (ja) * 2001-09-28 2012-02-29 キッセイ薬品工業株式会社 ビフェニルエチルアミン誘導体およびその製造方法
DE10204072A1 (de) * 2002-01-31 2003-08-14 Morphochem Ag Komb Chemie Neue Verbindungen, die Faktor Xa-Aktivität inhibieren
AU2003205461B2 (en) * 2002-02-15 2006-08-31 Endorecherche, Inc. Biphenyl Derivatives and their Use as Antiandrogenic Agents
ZA200407802B (en) * 2002-03-20 2006-11-29 Metabolex Inc Substituted phenylacetic acids
EP1479675A1 (de) 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Indazolderivate als Faktor Xa-Inhibitoren
CA2536954C (en) 2003-08-29 2012-11-27 Exelixis, Inc. C-kit modulators and methods of use
JP4585522B2 (ja) * 2003-12-22 2010-11-24 メルク・シャープ・エンド・ドーム・コーポレイション ブラジキニン拮抗物質又は逆作用物質としてのアルファ−ヒドロキシアミド
DE102004060542A1 (de) 2004-12-16 2006-07-06 Sanofi-Aventis Deutschland Gmbh Hydroxybiphenyl-Carbonsäuren und Derivate, Verfahren zu deren Herstellung und deren Verwendung
US7693868B2 (en) * 2005-12-30 2010-04-06 Sap Ag Separation of employee data for different applications
US8044242B2 (en) * 2006-03-09 2011-10-25 Bristol-Myers Squibb Company 2-(aryloxy) acetamide factor VIIa inhibitors useful as anticoagulants
DE102014203011A1 (de) * 2014-02-19 2015-08-20 Beiersdorf Ag Kosmetische oder dermatologische Zubereitungen mit einem Gehalt an einem oder mehreren Biphenylamin-Derivaten und Verwendung von einem oder mehreren Biphenylamin-Derivaten zur Bräunung der Haut

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0540051A1 (de) * 1991-10-31 1993-05-05 Daiichi Pharmaceutical Co., Ltd. Aromatische Amidinderivate und ihre Salze
WO1999041231A1 (fr) * 1998-02-17 1999-08-19 Ono Pharmaceutical Co., Ltd. Derives amidino utilises comme ingredients actifs et medicaments les contenant
WO2000071512A1 (en) * 1999-05-24 2000-11-30 Cor Therapeutics, Inc. INHIBITORS OF FACTOR Xa

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1185508A2 (de) * 1999-05-24 2002-03-13 Cor Therapeutics, Inc. Inhibitoren von faktor xa
WO2000071507A2 (en) * 1999-05-24 2000-11-30 Cor Therapeutics, Inc. INHIBITORS OF FACTOR Xa

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0540051A1 (de) * 1991-10-31 1993-05-05 Daiichi Pharmaceutical Co., Ltd. Aromatische Amidinderivate und ihre Salze
WO1999041231A1 (fr) * 1998-02-17 1999-08-19 Ono Pharmaceutical Co., Ltd. Derives amidino utilises comme ingredients actifs et medicaments les contenant
EP1078917A1 (de) * 1998-02-17 2001-02-28 Ono Pharmaceutical Co., Ltd. Amidinoderivate und medikamente die diese als aktiven bestandteil enthalten
WO2000071512A1 (en) * 1999-05-24 2000-11-30 Cor Therapeutics, Inc. INHIBITORS OF FACTOR Xa

Also Published As

Publication number Publication date
WO2001070678A2 (de) 2001-09-27
DE10014645A1 (de) 2001-09-27
US20040220241A1 (en) 2004-11-04
CA2403500A1 (en) 2002-09-18
JP2003528077A (ja) 2003-09-24
EP1268413A2 (de) 2003-01-02
US6946489B2 (en) 2005-09-20

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