KR960031461A - 디옥소피롤로-피롤 유도체 - Google Patents

디옥소피롤로-피롤 유도체 Download PDF

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KR960031461A
KR960031461A KR1019960004620A KR19960004620A KR960031461A KR 960031461 A KR960031461 A KR 960031461A KR 1019960004620 A KR1019960004620 A KR 1019960004620A KR 19960004620 A KR19960004620 A KR 19960004620A KR 960031461 A KR960031461 A KR 960031461A
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South Korea
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lower alkyl
aryl
substd
opt
substituted
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KR1019960004620A
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KR100456927B1 (ko
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디데리히 프랑스와
옵스트 울리케
발바움 사빈
붸버 루츠
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프리돌린 크라우스너·롤란드 보러
에프. 호프만-라 롯슈 아크티엔게젤샤프트
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P9/08—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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14—Ortho-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

본 발명은 혈장중의 트롬빈-유도성 또는 Xa 인자-유도성 혈소판 응집 및 피브리노겐 응혈을 저해하는 하기 일반식(Ⅰ)의 신규한 디옥소피롤로-피롤 유도체 및 이들의 수화물 또는 용매화물에 관한 것이다.
상기 식에서, R1내지 R6은 특허 청구 범위 제1항에서 정의한 바와 같다. 이들은 R2에 의해 N-치환된 상응 하는 말레이미드; 일반식 HN(R2)CH(R4)COOH의 α-아미노 카복실산 또는 그의 작용성 유도체; 및 일반식 R5C(O)R6의 케톤 또는 아데하이드로부터 출발하여 제조할 수 있다.

Description

디옥소피롤로-피롤 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (2)

  1. 하기 일반식(Ⅰ)의 옥타하이드로-1,3-디옥소-피롤로[3,4-c]피롤 유도체, 및 이들의 수화물 또는 용매화물 및 생리적으로 사용가능한 염;
    상기 식에서, R1및 R2는 각각 독립적으로 H, 저급알킬, 아릴, 헤테로아릴, 사이클로알킬, 또는 CONH2또는 COO-저급알킬 및/또는 아릴, 헤테로아릴 또는 사이클로알킬에 의해 치환된 저급알킬이고, R2는 저급-알카노일이고, R3는 H, COOH, CONH2, COO-저급알킬, CONH-저급알킬 또는 CON(저급알킬)2이고, R4, R5및 R6은 각각 독립적으로 H, 저급알킬, 아릴, 아르알킬 또는 사이클로알킬이거나 또는 R4및/또는 R5와 R6중 하나는 OH, SO2H, SO3H, 구아니디노, 아릴-저급알콕시 또는 저급알킬-(O 또는 S)에 의해 치환된 헤테로아릴 또는 저급알킬이거나 또는 R2와 R4는 함께 트리- 또는 테트라메틸렌 기(G)를 형성하고, 이 때 a) 메틸렌 기들 중 하나는 S, SO 또는 SO2로 대체되거나 또는 OH, 저급알킬, 저급알케닐 또는 카복시-저급 알킬에 의해 치환되거나, 또는 b) 메틸렌 기들 중 하나는 저급알케닐에 의해 치환될 수 있고 다른 하나는 저급 알킬-COOH에 의해 치환될 수 있으며, 단, R1, R2, R4, R5및 R6중 하나 이상은 아미노, 아미디노, 구아니디노 또는 N-하드록시아미디노에 의해 치환된 기이다.
  2. 활성 성분으로서 제1항에 따른 화합물을 함유하는 약학 제제.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960004620A 1995-02-27 1996-02-26 디옥소피롤로-피롤유도체 KR100456927B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CH55295 1995-02-27
CH552/95 1995-02-27
CH3457/95 1995-12-07
CH345795 1995-12-07

Publications (2)

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KR960031461A true KR960031461A (ko) 1996-09-17
KR100456927B1 KR100456927B1 (ko) 2005-04-19

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US (1) US5686459A (ko)
EP (1) EP0728758B1 (ko)
JP (1) JP2885682B2 (ko)
KR (1) KR100456927B1 (ko)
CN (1) CN1056844C (ko)
AT (1) ATE252100T1 (ko)
DE (1) DE59610771D1 (ko)
DK (1) DK0728758T3 (ko)
ES (1) ES2207657T3 (ko)

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IT1292424B1 (it) * 1996-07-18 1999-02-08 Hoffmann La Roche Ossopirrolo-pirrolderivati
WO2000017206A1 (en) * 1998-09-18 2000-03-30 Cubist Pharmaceuticals, Inc. Tetracyclic heterocycles as antimicrobial agents
SE0100326D0 (sv) 2001-02-02 2001-02-02 Astrazeneca Ab New compounds
SK302004A3 (sk) * 2001-06-28 2005-07-01 Pliva, D.D. Heterocyklické zlúčeniny a ich použitie ako inhibítory D-Ala-D-Ala ligázy
US7479502B2 (en) 2002-12-03 2009-01-20 Pharmacyclics, Inc. 2-(2-hydroxybiphenyl-3-yl)-1H-benzoimidazole-5-carboxamidine derivatives as factor VIIA inhibitors
DE602005004144T2 (de) * 2004-06-09 2009-01-29 F. Hoffmann-La Roche Ag Octahydropyrroloä3,4-cüpyrrolderivate und deren verwendung als antivirale mittel
MX2007005408A (es) * 2004-11-09 2007-05-16 Hoffmann La Roche Compuestos de aminoquinazolinas.
ATE449097T1 (de) * 2005-07-21 2009-12-15 Hoffmann La Roche Pyridoä2,3-düpyrimidin-2,4-diamin-verbindungen als ptpib-hemmer
CN101486714B (zh) * 2009-02-09 2013-03-20 沈阳药科大学 新噁嗪类化合物及其抗血小板聚集的用途
CN101486713B (zh) * 2009-02-09 2013-05-15 沈阳药科大学 呋喃并[2,3-h]色烯类化合物及其抗血小板聚集的用途
WO2017117239A1 (en) * 2015-12-30 2017-07-06 Flatley Discovery Lab, Llc Compounds and methods for the treatment of cystic fibrosis

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CH544763A (de) * 1970-03-26 1974-01-15 Siegfried Ag Verfahren zur Herstellung von Spiro-Additionsprodukten aus N-haltigen Heterocyclen und Maleinimiden
CH529152A (de) * 1970-03-26 1972-10-15 Siegfried Ag Verfahren zur Herstellung von Spiro-Verbindungen aus Schiff'schen Basen
CH546776A (de) * 1971-03-11 1974-03-15 Siegfried Ag Verfahren zur herstellung neuer cycloadditions-verbindungen.
DE3833008A1 (de) * 1988-09-29 1990-04-05 Goedecke Ag Pyrrolocarbozol-derivate, verfahren zu deren herstellung und deren verwendung als arzneimittel
JPH08505150A (ja) * 1992-12-23 1996-06-04 メルク エンド カンパニー インコーポレーテッド スピロインダニルショウノウスルホニルオキシトシンアンタゴニストのヒダントイン及びスクシンイミド置換誘導体

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JP2885682B2 (ja) 1999-04-26
CN1136567A (zh) 1996-11-27
DK0728758T3 (da) 2004-02-23
CN1056844C (zh) 2000-09-27
US5686459A (en) 1997-11-11
EP0728758A1 (de) 1996-08-28
DE59610771D1 (de) 2003-11-20
KR100456927B1 (ko) 2005-04-19
JPH08245624A (ja) 1996-09-24
EP0728758B1 (de) 2003-10-15
ES2207657T3 (es) 2004-06-01
ATE252100T1 (de) 2003-11-15

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