BR9813477A - Derivados de benzamidina - Google Patents

Derivados de benzamidina

Info

Publication number
BR9813477A
BR9813477A BR9813477-9A BR9813477A BR9813477A BR 9813477 A BR9813477 A BR 9813477A BR 9813477 A BR9813477 A BR 9813477A BR 9813477 A BR9813477 A BR 9813477A
Authority
BR
Brazil
Prior art keywords
benzamidine derivatives
benzamidine
derivatives
thromboembolic
prophylaxis
Prior art date
Application number
BR9813477-9A
Other languages
English (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 BR9813477A publication Critical patent/BR9813477A/pt

Links

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
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • 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
    • 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (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)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Vascular Medicine (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (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)

Abstract

Patente de Invenção: <B>"DERIVADOS DE BENZAMIDINA"<D>. Novos compostos da fórmula I na qual X, Y, R¹, R², R³ e R^ 4^ são como definidos na Reivindicação 1 de Patente, são inibidores de fator Xa de coagulação e podem ser empregados para a profilaxia e/ou terapia de distúrbios tromboembólicos.
BR9813477-9A 1997-12-12 1998-11-27 Derivados de benzamidina BR9813477A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19755268A DE19755268A1 (de) 1997-12-12 1997-12-12 Benzamidinderivate
PCT/EP1998/007673 WO1999031092A1 (de) 1997-12-12 1998-11-27 Benzamidinderivate als koagulationsfaktor-xa-hemmer

Publications (1)

Publication Number Publication Date
BR9813477A true BR9813477A (pt) 2000-10-24

Family

ID=7851688

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9813477-9A BR9813477A (pt) 1997-12-12 1998-11-27 Derivados de benzamidina

Country Status (16)

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

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CA2340100A1 (en) * 1998-08-11 2000-02-24 Daiichi Pharmaceutical Co., Ltd. Novel sulfonyl derivatives
SE9902987D0 (sv) 1999-08-24 1999-08-24 Astra Pharma Prod Novel compounds
DE19962924A1 (de) * 1999-12-24 2001-07-05 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
AU2004202422B2 (en) * 1999-12-24 2007-11-22 Bayer Intellectual Property Gmbh Substituted oxazolidinones and their use in the field of blood coagulation
CO5300399A1 (es) 2000-02-25 2003-07-31 Astrazeneca Ab Heterocicliocs que contienen nitrogeno, proceso para su preparacion y composiciones farmaceuticas que los contienen
DE10027024A1 (de) * 2000-05-31 2001-12-06 Merck Patent Gmbh Carbaminsäureester
US7005439B2 (en) 2000-06-20 2006-02-28 Astrazeneca Ab Compounds
AR028948A1 (es) 2000-06-20 2003-05-28 Astrazeneca Ab Compuestos novedosos
DE10105989A1 (de) * 2001-02-09 2002-08-14 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
GB0104050D0 (en) 2001-02-19 2001-04-04 Astrazeneca Ab Chemical compounds
AR035230A1 (es) 2001-03-19 2004-05-05 Astrazeneca Ab Compuestos de bencimidazol, proceso para su preparacion, composicion farmaceutica, proceso para la preparacion de dicha composicion farmaceutica, y usos de estos compuestos para la elaboracion de medicamentos
GB0107228D0 (en) 2001-03-22 2001-05-16 Astrazeneca Ab Chemical compounds
SE0101038D0 (sv) 2001-03-23 2001-03-23 Astrazeneca Ab Novel compounds
DE10129725A1 (de) * 2001-06-20 2003-01-02 Bayer Ag Kombinationstherapie substituierter Oxazolidinone
SE0103818D0 (sv) 2001-11-15 2001-11-15 Astrazeneca Ab Chemical compounds
DE10159453A1 (de) * 2001-12-04 2003-06-18 Merck Patent Gmbh Verwendung von 1-Phenyl-oxazolidin-2-on-Verbindungen als Protease
US7479502B2 (en) 2002-12-03 2009-01-20 Pharmacyclics, Inc. 2-(2-hydroxybiphenyl-3-yl)-1H-benzoimidazole-5-carboxamidine derivatives as factor VIIA inhibitors
DE10300111A1 (de) 2003-01-07 2004-07-15 Bayer Healthcare Ag Verfahren zur Herstellung von 5-Chlor-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophencarboxamid
SE0301369D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Chemical compounds
DE10322469A1 (de) * 2003-05-19 2004-12-16 Bayer Healthcare Ag Heterocyclische Verbindungen
AU2004252102A1 (en) * 2003-06-23 2005-01-06 Gilead Palo Alto, Inc. Urea derivatives of piperazines and piperidines as fatty acid oxidation inhibitors
DE10355461A1 (de) 2003-11-27 2005-06-23 Bayer Healthcare Ag Verfahren zur Herstellung einer festen, oral applizierbaren pharmazeutischen Zusammensetzung
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 (de) 2005-09-23 2007-03-29 Bayer Healthcare Ag 2-Aminoethoxyessigsäure-Derivate und ihre Verwendung
SG166126A1 (en) 2005-10-04 2010-11-29 Bayer Schering Pharma Ag Novel polymorphous form and the amorphous form of 5-chloro-n-({(5s)-2-oxo- 3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidine-5-yl}-methyl)-2-thiophene carboxamide
DE102005047561A1 (de) 2005-10-04 2007-04-05 Bayer Healthcare Ag Feste, oral applizierbare pharmazeutische Darreichungsformen mit schneller Wirkstofffreisetzung
JP5102781B2 (ja) 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 新規のベンズアミジン誘導体、その製造方法およびそれを含む薬学組成物
DE102007018662A1 (de) 2007-04-20 2008-10-23 Bayer Healthcare Ag Oxazolidinone zur Behandlung und Prophylaxe von pulmonaler Hypertonie
KR101009594B1 (ko) 2007-05-09 2011-01-20 주식회사 레고켐 바이오사이언스 Ｐ4 위치에 사이클릭 아미딘을 가지는 ＦＸａ 저해제, 이의유도체, 제조방법 및 이를 함유하는 의약 조성물
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
DE102007028318A1 (de) 2007-06-20 2008-12-24 Bayer Healthcare Ag Oxazolidinone zur Behandlung und Prophylaxe von Sepsis
KR101047614B1 (ko) * 2007-07-27 2011-07-07 동화약품주식회사 신규한 벤즈아미딘 유도체, 이의 제조방법 및 이를포함하는 골다공증의 예방 또는 치료용 약학 조성물
EP2138178A1 (en) 2008-06-28 2009-12-30 Bayer Schering Pharma Aktiengesellschaft Oxazolidninones for the treatment fo chronic obstructive pulmonary disease (COPD) and/or asthma
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Also Published As

Publication number Publication date
PL341008A1 (en) 2001-03-12
SK8572000A3 (en) 2001-07-10
EP1056743A1 (de) 2000-12-06
WO1999031092A1 (de) 1999-06-24
NO20002958D0 (no) 2000-06-09
AU744002B2 (en) 2002-02-14
AU1964799A (en) 1999-07-05
CN1281451A (zh) 2001-01-24
DE19755268A1 (de) 1999-06-17
HUP0004353A3 (en) 2002-04-29
RU2203897C2 (ru) 2003-05-10
NO20002958L (no) 2000-08-11
KR20010032963A (ko) 2001-04-25
CA2313651A1 (en) 1999-06-24
JP2002508370A (ja) 2002-03-19
HUP0004353A2 (hu) 2002-03-28
ZA9811339B (en) 1999-07-08
AR017844A1 (es) 2001-10-24

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Legal Events

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B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 6A,7A E 8A ANUIDADES.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 1910 DE 14/08/2007.