KR960704854A - 축합 피리다진계 화합물 (fused pyridazine compound) - Google Patents
축합 피리다진계 화합물 (fused pyridazine compound)Info
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- KR960704854A KR960704854A KR1019960701845A KR19960701845A KR960704854A KR 960704854 A KR960704854 A KR 960704854A KR 1019960701845 A KR1019960701845 A KR 1019960701845A KR 19960701845 A KR19960701845 A KR 19960701845A KR 960704854 A KR960704854 A KR 960704854A
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Abstract
하기 일반식(Ⅰ)으로 표시되는 사이클릭 GMP-포스포디에스테라제(이하 cGMP-PDE라 함) 저해작용을 갖는 축합 피리다진계 화합물 및 그 약리학적으로 허용되는 염에 관한 것이다.
본 발명 화합물군은 협심증, 심근경색, 만성 및 급성 심부전 등의 허혈성 심질환, 폐고혈합중, 동맥경화증, 기관지천식 등, cGMP-PDE 저해작용이 유효한 질환의 예방ㆍ치료제로서 유용하다.
Description
「발명의 명칭」
축합 피리다진계 화합물(FUSED PYRIDAZINE COMPOUND)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (13)
- 일반식{고리 C는 헤테로원자를 가지고 있어도 좋은 5~6원 고리를 의미한다. n은 0또는 1~4의 정수를 의미한다. R1은 할로겐 원자, 치환기를 가지고 있어도 좋은 저급알킬기, 치환기를 가지고 있어도 좋은 저급알콕시기. 치환기를 가지고 있어도 좋은 시클로알킬기, 니트로기, 시아노기, 식-NR2R3(식중, R2, R3은 동일 또는 상이한 수소원자, 치환기를 가지고 있어도 좋은 저급알콕시, 아실기, 치환기를 가지고 있어도 좋은 아릴알킬기 또는 치환기를 가지고 있어도 좋은 헤테로아릴알킬기를 의미한다. 또, R2와 R3은 결합하고 있는 질소원자와 함께 고리를 형성하여도 좋다. 또한, 이 고리는 치환기를 가지고 있어도 좋다.) 으로 표시되는 기, 식 -O-R9(식중 R9는 수소원자, 치환기를 가지고 있어도 좋은 저급알킬기, 아실기, 치환기를 가지고 있어도 좋은 아릴알킬기, 치환기를 가지고 있어도 좋은 헤테로아릴알킬기를 의미한다.)로 표시되는 기, 식 ~S-R10(식중)R10은 수소원자, 치환기르르 가지고 있어도 좋은 지급알킬기, 아실기, 치환기를 가지고 있어도 좋은 아릴알킬기, 치환기를 가지고 있어도 좋은 아릴알킬기, 치환기를 가지고 있어도 좋은 헤테로아릴알킬기를 의미한다.)으로 표시되는 기, 식.(식중 R11은 수소원자, 저급알킬기, 아미노기를 의미한다. m은 0 또는 1~2의 정수를 의미한다.)으로 표시되는 기, 보호되어 있어도 좋은 카르복실기를 의미한다. 단, n이 2~4인 경우, 각 R1은 독립하여 상기 치환기를 취할 수 있다.A는 수소원자, 할로겐원자, 식 -NR4R5(식중, R4, R5는 동일 또는 상이한 수소원자, 치환기를 가지고 있어도 좋은 저급알킬기, 아실기, 치환기를 가지고 있어도 좋은 아릴알킬기, 치환기를 가지고 있어도 좋은 헤테로아릴알킬기를 의미한다. 또 R4와 R5는 결합하고 있는 질소원자와 함께 고리를 형성하고 있어도 좋다. 또한, 이 고리는 치환기를 가지고 있어도 좋다.)로 표시되는 기, 치환기를 가지고 있어도 좋은 아릴기, 치환기를 가지고 있어도 좋은 헤테로아릴기, 치환기를 가지고 있어도 좋은 아릴알킬기, 치환기를 가지고 있어도 좋은 헤테로아릴알킬기를 의미한다.X는 식 -NR6-(식중 R6은 수소원자, 치환기를 가지고 있어도 좋은 저급알킬기, 치환기를 가지고 있어도 좋은 아릴알킬기, 치환기를 가지고 있어도 좋은 헤테로아릴알킬기를 의미한다.)으로 표시되는 기, 또는 식 -N=으로 표시되는 기를 의미한다.Y는 식 -CO-로 표시되는 기 또는 식-CB=[식중 B는 수소원자, 할로겐원자, 식 -NR7R8(식중 R7및 R8은 동일 또는 상이한 수소원자, 치환기를 가지고 있어도 좋은 저급알킬기, 아실기, 치환기를 가지고 있어도 좋은 아릴알킬기, 치환기를 가지고 있어도 좋은 헤테로아릴알킬기를 의미한다. 또 R7과 R8은 결합하고 있는 질소원자와 함께 고리를 형성하고 있어도 좋다. 또, 이고리는 치환기를 가지고 있어도 좋다.)로 표시되는 기, 식 -O-R12(식중 R12는 수소원자, 치환기를 가지고 있어도 좋은 저급알킬기, 아실기, 치환기를 가지고 있어도 좋은 헤테로아릴알킬기를 의미한다.)으로 표시되는 기, 식-S-R13(식중)R13은 수소원자, 치환기를 가지고 있어도 좋은 저급알킬기, 아실기, 치환기를 가지고 있어도 좋은 아릴알킬기, 치환기를 가지고 있어도 좋은 아릴알킬기, 치환기를 가지고 있어도 좋은 헤테로아릴알킬기를 의미한다.)으로 표시되는기, 치환기를 가지고 있어도 좋은 아릴기, 치환기를 가지고 있어도 좋은 헤테로아릴기, 치환기를 가지고 있어도 좋은 아릴알킬기, 치환기를 가지고 있어도 좋은 헤테로아릴알킬기를 의미한다.]로 표시되는 기를 의미한다.은 이중결합 또는 단일결합을 의미한다.단 고리가 벤젠고리일 경우, n이 0일때를 제외하는 것으로 한다.]으로 표시되는 축합 피리다진계 화합물 또는 그 약리학적으로 허용되는 염.
- 일반식(Ⅱ)(식중 R1, A, n, Z 및 Y는 상기 의를 갖는다.은 단일결합 또는 이중결합을 의미한다.)으로 표시되는 축합 피라다진계 화합물 또는 그 약리학적으로 허용되는 염.
- 일반식(Ⅲ)식중 R1a는 할로겐 원자, 치환기를 가지고 있어도 좋은 저급알킬기, 치환기를 가지고 있어도 좋은 저급알콕시기, 치환기를 가지고 있어도 좋은 시클로알킬기, 니트로기, 시아노기, 식 -NR2R3(식중 R2, R3은 동일 또는 상이한 수소원자, 치환기를 가지고 있어도 좋은 저급 알킬기, 아실기, 치환기를 가지고 있어도 좋은 아릴알킬기 또는 치환기를 가지고 있어도 좋은 헤테로아릴알킬기를 의미한다. 또 R2와3은 결합하고 있는 질소원자와 함께 고리를 형성하여도 좋다. 또한 이 고리는 치환기를 가지고 있어도 좋다.)으로 표시되는 기를 의미한다.R1, A 및 B는 상기 의미를 갖는다.n′는 1~3의 정수를 의미한다.]
- 일반식(Ⅳ)(식중 R1, R6, R1a, n′,A 및 B는 상기 의미를 갖는다.)으로 표시되는 축합 피리다진계 화합물 또는 그 약리학적으로 허용되는 염.
- 일반식(Ⅴ)(식중 R1a및 B는 상기 의미를 갖는다. R12, R13및 R14는 동일 또는 상이한 수소원자, 할로겐원자, 치환기를 가지고 있어도 좋은 저급알킬기, 치환기를 가지고 있어도 좋은 저급알콕시기를 의미한다. 또한, R12, R13및 R14중 인접한 탄소원자에 결합한 2개의 치환기를 함께 메틸렌디옥시 또는 에틸렌디옥시를 형성할 수 있다.)으로 표시되는 축합 피리다진계 화합물 또는 그 약리학적으로 허용되는 염.
- 일반식(Ⅵ)(식중 R1a및 R6은 상기 의미를 갖는다. R12, R13및 R14는 동일 또는 상이한 수소원자, 할로겐원자, 치환기를 가지고 있어도 좋은 저급알킬기, 치환기를 가지고 있어도 좋은 저급알콕시기를 의미한다. 또한, R12, R13및 R14중 인접한 탄소원자에 결합한 2개의 치환기는 함께 메틸렌디옥시 또는 에틸렌디옥실 형성할 수 있다.)으로 표시되는 축합 피리다진계 화합물 또는 그 약리학적으로 허용되는 염.
- 제1항 기재의 축합 피리다진계 화합물 또는 그 약리학적으로 허용되는 염을 유효성분으로 하는 사이클럭 GMP 포스포디에스테라제 저해작용이 유효한 질환의 예방ㆍ치료제.
- 제1항 기재의 축합 피리다진계 화합물 또는 그 약리학적으로 허용되는 염을 유효성분으로 하는 항혈소판 작용이 유효한 질환의 예방ㆍ치료제.
- 제1항 기재의 축합 피리다진계 화합물 또는 그 약리학적으로 허용되는 염을 유효성분으로 하는 사이클릭 GMP 포스포디에스테라제 저해제.
- 제1항 기재의 축합 피리다진계 화합물 또는 그 약리학적으로 허용되는 염을 유효성분으로 하는 항혈소판제.
- 제1항 기재의 축합 피리다진계 화합물 또는 그 약리학적으로 허용되는 염을 유효성분으로 하는 고혈압증 예방ㆍ치료제.
- 제1항 기재의 축합 피리다진계 화합물 또는 그 약리학적으로 허용되는 염을 유효성분으로 하는 폐고혈압증 예방ㆍ치료제.
- 제1항 기재의 축합 피리다진계 화합물 또는 그 약리학적으로 허용되는 염을 유효성분으로 하는 협심증 예방ㆍ치료제.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP94-187128 | 1994-08-09 | ||
JP18712894 | 1994-08-09 | ||
JP94-316337 | 1994-12-20 | ||
JP31633794 | 1994-12-20 | ||
PCT/JP1995/001575 WO1996005176A1 (fr) | 1994-08-09 | 1995-08-08 | Compose de pyridazine condense |
Publications (2)
Publication Number | Publication Date |
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KR960704854A true KR960704854A (ko) | 1996-10-09 |
KR100189865B1 KR100189865B1 (ko) | 1999-06-01 |
Family
ID=26504157
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019960701845A KR100189865B1 (ko) | 1994-08-09 | 1995-08-08 | 축합 피리다진계 화합물 |
Country Status (15)
Country | Link |
---|---|
US (2) | US5849741A (ko) |
EP (1) | EP0722936B1 (ko) |
KR (1) | KR100189865B1 (ko) |
CN (1) | CN1151136C (ko) |
AT (1) | ATE267174T1 (ko) |
AU (1) | AU705229B2 (ko) |
CA (1) | CA2173493C (ko) |
DE (1) | DE69533057T2 (ko) |
ES (1) | ES2224130T3 (ko) |
FI (1) | FI111841B (ko) |
HU (1) | HU219864B (ko) |
MX (1) | MX9601310A (ko) |
NO (1) | NO309378B1 (ko) |
NZ (1) | NZ290952A (ko) |
WO (1) | WO1996005176A1 (ko) |
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GB0111078D0 (en) * | 2001-05-04 | 2001-06-27 | Novartis Ag | Organic compounds |
SI1427420T1 (sl) * | 2001-09-12 | 2006-12-31 | Novartis Ag | Uporaba kombinacije, ki vsebuje 4-piridilmetilftalazine za zdravljenje raka |
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JP2006504665A (ja) * | 2002-08-13 | 2006-02-09 | ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー | マトリックスメタロプロテイナーゼ阻害剤としてのアザイソキノリン誘導体 |
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US8506934B2 (en) | 2005-04-29 | 2013-08-13 | Robert I. Henkin | Methods for detection of biological substances |
JP2009514969A (ja) | 2005-11-09 | 2009-04-09 | コンビナトアールエックス インコーポレーティッド | 医学的状態を治療するための方法、組成物、およびキット |
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US8772481B2 (en) | 2008-10-10 | 2014-07-08 | Amgen Inc. | Aza- and diaza-phthalazine compounds as P38 map kinase modulators and methods of use thereof |
WO2010042649A2 (en) | 2008-10-10 | 2010-04-15 | Amgen Inc. | PHTHALAZINE COMPOUNDS AS p38 MAP KINASE MODULATORS AND METHODS OF USE THEREOF |
CN102443031B (zh) * | 2011-09-20 | 2014-03-05 | 山东大学 | 一种c-di-GMP的分离纯化方法 |
EP2804603A1 (en) | 2012-01-10 | 2014-11-26 | President and Fellows of Harvard College | Beta-cell replication promoting compounds and methods of their use |
WO2014055801A1 (en) | 2012-10-05 | 2014-04-10 | Henkin Robert I | Phosphodiesterase inhibitors for treating taste and smell disorders |
CN106233141B (zh) | 2014-02-18 | 2018-08-21 | 罗伯特·I·汉金 | 用于诊断和治疗味觉或嗅觉的损失和/或失真的方法和组合物 |
RU2649140C2 (ru) * | 2015-04-20 | 2018-03-30 | государственное бюджетное образовательное учреждение высшего профессионального образования "Пермская государственная фармацевтическая академия" Министерства здравоохранения Российской Федерации (ГБОУ ВПО ПГФА Минздрава России) | 2-гидрокси-4-оксо-4-(4'-хлорфенил)-бут-2-еноат 4-метил-2-пиридиламмония, обладающий прямым антикоагулянтным действием |
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-
1995
- 1995-08-08 AT AT95927990T patent/ATE267174T1/de active
- 1995-08-08 HU HU9600933A patent/HU219864B/hu not_active IP Right Cessation
- 1995-08-08 CA CA002173493A patent/CA2173493C/en not_active Expired - Fee Related
- 1995-08-08 ES ES95927990T patent/ES2224130T3/es not_active Expired - Lifetime
- 1995-08-08 NZ NZ290952A patent/NZ290952A/en not_active IP Right Cessation
- 1995-08-08 DE DE69533057T patent/DE69533057T2/de not_active Expired - Lifetime
- 1995-08-08 US US08/619,621 patent/US5849741A/en not_active Expired - Lifetime
- 1995-08-08 AU AU31919/95A patent/AU705229B2/en not_active Ceased
- 1995-08-08 KR KR1019960701845A patent/KR100189865B1/ko not_active IP Right Cessation
- 1995-08-08 CN CNB951908626A patent/CN1151136C/zh not_active Expired - Fee Related
- 1995-08-08 EP EP95927990A patent/EP0722936B1/en not_active Expired - Lifetime
- 1995-08-08 WO PCT/JP1995/001575 patent/WO1996005176A1/ja active IP Right Grant
-
1996
- 1996-04-03 FI FI961510A patent/FI111841B/fi not_active IP Right Cessation
- 1996-04-08 MX MX9601310A patent/MX9601310A/es unknown
- 1996-04-09 NO NO19961397A patent/NO309378B1/no not_active IP Right Cessation
-
1998
- 1998-09-29 US US09/161,946 patent/US6218392B1/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
HU9600933D0 (en) | 1996-07-29 |
EP0722936B1 (en) | 2004-05-19 |
AU705229B2 (en) | 1999-05-20 |
HUT76067A (en) | 1997-06-30 |
DE69533057T2 (de) | 2005-06-16 |
EP0722936A1 (en) | 1996-07-24 |
NO309378B1 (no) | 2001-01-22 |
CA2173493A1 (en) | 1996-02-22 |
FI961510A0 (fi) | 1996-04-03 |
NO961397L (no) | 1996-06-06 |
DE69533057D1 (de) | 2004-06-24 |
FI111841B (fi) | 2003-09-30 |
WO1996005176A1 (fr) | 1996-02-22 |
CN1151136C (zh) | 2004-05-26 |
AU3191995A (en) | 1996-03-07 |
US6218392B1 (en) | 2001-04-17 |
FI961510A (fi) | 1996-05-29 |
NO961397D0 (no) | 1996-04-09 |
CA2173493C (en) | 2008-03-25 |
EP0722936A4 (en) | 1996-12-11 |
MX9601310A (es) | 1998-11-30 |
NZ290952A (en) | 1998-05-27 |
ATE267174T1 (de) | 2004-06-15 |
HU219864B (hu) | 2001-08-28 |
US5849741A (en) | 1998-12-15 |
CN1135210A (zh) | 1996-11-06 |
KR100189865B1 (ko) | 1999-06-01 |
ES2224130T3 (es) | 2005-03-01 |
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