KR920018037A - 4-아릴-티아졸 또는 이미다졸 유도체 - Google Patents

4-아릴-티아졸 또는 이미다졸 유도체 Download PDF

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Publication number
KR920018037A
KR920018037A KR1019920004745A KR920004745A KR920018037A KR 920018037 A KR920018037 A KR 920018037A KR 1019920004745 A KR1019920004745 A KR 1019920004745A KR 920004745 A KR920004745 A KR 920004745A KR 920018037 A KR920018037 A KR 920018037A
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South Korea
Prior art keywords
thiazole
aryl
pharmaceutically acceptable
derivative
acceptable salt
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KR1019920004745A
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English (en)
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헨리 픽 존
토마스 로간 로버트
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에프.지.엠.헤르만스·에이.지.제이.베르미렌
악조 엔. 브이
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Application filed by 에프.지.엠.헤르만스·에이.지.제이.베르미렌, 악조 엔. 브이 filed Critical 에프.지.엠.헤르만스·에이.지.제이.베르미렌
Publication of KR920018037A publication Critical patent/KR920018037A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • A61P11/08—Bronchodilators
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Paints Or Removers (AREA)
  • Polyurethanes Or Polyureas (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

내용 없음

Description

4-아릴-티아졸 또는 이미다졸 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (8)

  1. 하기 일반식(Ⅰ)의 4-아릴-티아졸 또는 이미다졸 유도체; 또는 그것의 약학적 허용염)단 4-(4-클로로페닐)-티아졸-2-카스복스아미드는 제외) :
    상기 식중, X는 O또는 NOH이고, Y는 S또는 NR3이고, Ar는 페닐, 나프틸, 테트라히드로나프닐, 및 비페닐 중에서 선택된 기이고, R은 각각 수소, 히드록시, 저급 알킬, 저급 알콕시, 저급 티오알킬, 시클로알킬, 할로겐, CF3, NO2및 O-ALK-NR1R2중에서 선택된 1내지 4개의 치환체로서, 여기에서 ALK는 C2내지 C6의 포화지방족탄화수소기이며, R1및 R2는 각각 수소 또는 저급 알킬이거나, 또는 그들이 결합되어 있는 질소 원자와 함께 헤테로시클릭 고리를 형성하고, R3는 수소 또는 저급 알킬이다.
  2. 제 1항에 있어서, X가 NOH이고, Y가 S또는 NH이며, Ar이 페닐인 유도체, 또는 그것의 약학적 혀용염.
  3. 제 1항에 있어서, X가 NOH이고, Y가 S또는 NH이며, Ar이 페닐이고, 치환체 R중 최소한 하나가 메틸, 메톡시, 또는 염소인 유도체, 또는 그것의 약학적 허용염.
  4. 제 1항의 4-(3-클로로-4,5-디메톡시페닐)-N-히드록시-티아졸-2-카르복시이미다미드, 4-(3,4-디클로로페닐)-N-히드록시티아졸-2-카르복시이미다미드, N-히드록시-4-(4,5-디메톡시페닐)-티아졸-2-카르복시이미다미드, 또는 N-히드록시-4-(3,4-디메틸페닐)-1H-이미다졸-2-카르복스이미다미드, 또는 그것의 약학적 허용염.
  5. 하기 일반식(Ⅱ)의 4-아릴-티아졸 또는 이미다졸 유도체를 암모니아와 축합시킨 후, 획득된 X가 O인 제 1항의 유도체를 임의적으로 X가 NOH인 제 1항의 유도체로 전환시키고/또는 약학적 허용염으로 전환시키는 것을 특징으로 하는, 제 1항의 4-아릴-티아졸 또는 이미다졸 유도체를 제조하기 위한 방법.
    상기 식중, R, Ar 및 Y는 상기 정의한 의미를 지니고, L은 이탈기이다.
  6. 4-(4-클로로페닐-티아졸-2-카르복스아미드 또는 제 1항의 4-아릴-티아졸 또는 이미다졸 유도체, 또는 그것의 약학적 허용염을 약학적 허용 보조제와 혼합된 형태로 포함하는 약학적 조성물.
  7. 임상 치료용으로 사용하기 위한 4-(4-클로로페닐)-티아졸-카르복스아미드 또는 제 1항의 4-아릴-티아졸 또는 이미다졸 유도체.
  8. 심장병 천식의 치료용 의약품을 제조하는데, 4-(4-클로로페닐)-티아졸-2-카르복스아미드 또는 제 1항의 4-아릴-티아졸 또는 이미다졸 유도체, 또는 그것의 약학적 허용염을 사용하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920004745A 1991-03-25 1992-03-23 4-아릴-티아졸 또는 이미다졸 유도체 KR920018037A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP91302573 1991-03-25
GB91302573.0 1991-03-25

Publications (1)

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KR920018037A true KR920018037A (ko) 1992-10-21

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US (2) US5254575A (ko)
EP (1) EP0506194B1 (ko)
JP (1) JPH0597816A (ko)
KR (1) KR920018037A (ko)
AT (1) ATE141597T1 (ko)
AU (1) AU648394B2 (ko)
CA (1) CA2063172A1 (ko)
DE (1) DE69212870T2 (ko)
DK (1) DK0506194T3 (ko)
ES (1) ES2093765T3 (ko)
FI (1) FI921262A (ko)
GR (1) GR3021260T3 (ko)
IE (1) IE73235B1 (ko)
MX (1) MX9203810A (ko)
NO (1) NO301929B1 (ko)
NZ (1) NZ242095A (ko)
ZA (1) ZA921781B (ko)

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USRE37234E1 (en) 1996-11-01 2001-06-19 Nitromed, Inc. Nitrosated and nitrosylated phosphodiestrase inhibitor compounds, compositions and their uses
JP2001504457A (ja) * 1996-11-01 2001-04-03 ニトロメド インコーポレーテッド ニトロソ化およびニトロシル化ホスホジエステラーゼ阻害剤化合物、組成物及びその使用法
US6331543B1 (en) * 1996-11-01 2001-12-18 Nitromed, Inc. Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use
US5958926A (en) 1996-11-01 1999-09-28 Nitromed, Inc. Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses
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US6472425B1 (en) 1997-10-31 2002-10-29 Nitromed, Inc. Methods for treating female sexual dysfunctions
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AU2004226353A1 (en) 2003-04-01 2004-10-14 Laboratoires Serono Sa Inhibitors of phosphodiesterases in infertility
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TWI336697B (en) * 2003-09-19 2011-02-01 Solvay Pharm Bv Thiazole derivatives as cannabinoid receptor modulators
PE20070530A1 (es) * 2005-10-26 2007-05-31 Smithkline Beecham Corp Compuestos derivados de tiazoles sustituidos como agentes de apertura de canales de potasio activados por calcio de alta conductancia
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
WO2008151257A2 (en) 2007-06-04 2008-12-11 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
EP2328910B1 (en) 2008-06-04 2014-08-06 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
AU2009270833B2 (en) 2008-07-16 2015-02-19 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
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JP6499591B2 (ja) 2013-02-25 2019-04-10 シナジー ファーマシューティカルズ インコーポレイテッド 結腸洗浄において用いるためのグアニル酸シクラーゼ受容体アゴニスト
EP2968439A2 (en) 2013-03-15 2016-01-20 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
CA2905438A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
US10011637B2 (en) 2013-06-05 2018-07-03 Synergy Pharmaceuticals, Inc. Ultra-pure agonists of guanylate cyclase C, method of making and using same
KR102456567B1 (ko) 2013-08-09 2022-10-19 알데릭스, 인코포레이티드 인산염 수송을 억제하기 위한 화합물 및 방법
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JPH02262562A (ja) * 1988-10-20 1990-10-25 Ishihara Sangyo Kaisha Ltd イミダゾール系化合物

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DE69212870T2 (de) 1997-01-16
MX9203810A (es) 1992-07-31
NZ242095A (en) 1994-04-27
IE920734A1 (en) 1992-10-07
FI921262A0 (fi) 1992-03-24
AU1291592A (en) 1992-10-01
EP0506194B1 (en) 1996-08-21
ES2093765T3 (es) 1997-01-01
NO921156L (no) 1992-09-28
JPH0597816A (ja) 1993-04-20
NO921156D0 (no) 1992-03-24
GR3021260T3 (en) 1997-01-31
DK0506194T3 (da) 1996-12-23
CA2063172A1 (en) 1992-09-26
EP0506194A1 (en) 1992-09-30
US5254575A (en) 1993-10-19
IE73235B1 (en) 1997-05-21
ZA921781B (en) 1992-11-25
US5462959A (en) 1995-10-31
FI921262A (fi) 1992-09-26
NO301929B1 (no) 1997-12-29
DE69212870D1 (de) 1996-09-26
AU648394B2 (en) 1994-04-21
ATE141597T1 (de) 1996-09-15

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