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公开(公告)号:EP0619316A1
公开(公告)日:1994-10-12
申请号:EP94105380.3
申请日:1994-04-07
发明人: Shimada, Junichi , Kuwabara, Takashi , Yasuzawa, Tohru , Magara, Hiroshi , Nonaka, Hiromi , Kusaka, Hideaki , Suzuki, Fumio
IPC分类号: C07D473/04 , A61K31/52
CPC分类号: C07D473/04 , Y10S514/869
摘要: There is provided a novel xanthine Compound(I)
wherein R¹ and R² are the same or different and each represent hydroxy-substituted, oxo-substituted or unsubstituted lower alkyl, Y is a single bond or alkylene, and Q is
wherein R³ and R⁴ are the same or different and each represent hydrogen or hydroxy, n is 0 or 1; provided that when both of R³ and R⁴ are hydrogen, at least one of R¹ and R² is hydroxy-substituted or oxo-substituted lower alkyl; or a pharmaceutically acceptable salt thereof.
The xanthine compound has adenosine A₁ receptor antagonizing activity, and thus shows diuretic effect, renal-protecting effect, bronchodilatory effect, cerebral function improving effect and anti-dementia effect.摘要翻译: 提供了一种新颖的黄嘌呤化合物(I)
其中R 1和R 2相同或不同,各自表示羟基取代的,取代或未取代的低级烷基,Y是单键或亚烷基 且Q为 ,其中R 3和R 4相同或不同,各自表示氢或羟基,n为0或1; 条件是当R 3和R 4都是氢时,R 1和R 2中的至少一个是羟基取代的或氧代取代的低级烷基; 或其药学上可接受的盐。 黄嘌呤化合物具有腺苷A1受体拮抗活性,因此具有利尿作用,肾保护作用,支气管扩张作用,脑功能改善作用和抗痴呆作用。 -
公开(公告)号:EP0619316B1
公开(公告)日:1998-08-12
申请号:EP94105380.3
申请日:1994-04-07
发明人: Shimada, Junichi , Kuwabara, Takashi , Yasuzawa, Tohru , Magara, Hiroshi , Nonaka, Hiromi , Kusaka, Hideaki , Suzuki, Fumio
IPC分类号: C07D473/04 , A61K31/52
CPC分类号: C07D473/04 , Y10S514/869
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公开(公告)号:EP0607607B1
公开(公告)日:1996-09-18
申请号:EP93120842.5
申请日:1993-12-23
发明人: Suzuki, Fumio , Shimada, Junichi , Koike, Nobuaki , Kase, Hiroshi , Nakamura, Joji , Shiozaki, Shizuo , Nonaka, Hiromi
IPC分类号: C07D473/06 , A61K31/52
CPC分类号: C07D473/06
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公开(公告)号:EP0607607A1
公开(公告)日:1994-07-27
申请号:EP93120842.5
申请日:1993-12-23
发明人: Suzuki, Fumio , Shimada, Junichi , Koike, Nobuaki , Kase, Hiroshi , Nakamura, Joji , Shiozaki, Shizuo , Nonaka, Hiromi
IPC分类号: C07D473/06 , A61K31/52
CPC分类号: C07D473/06
摘要: Disclosed are xanthine derivatives represented by the following Formula (I):
in which R¹, R², and R³ independently represent hydrogen or lower alkyl;
Q¹, Q², and Q³ independently represent hydrogen, lower alkyl, lower alkoxy, or halogen;
and X represents -COR⁴ (in which R⁴ represents hydrogen, hydroxy, lower alkyl, or lower alkoxy) or -SO₂R⁵ {in which R⁵ represents hydroxy, lower alkoxy, trifluoromethyl,
in which R⁶ and R⁷ independently represent hydrogen, hydroxy-substituted or unsubstituted lower alkyl, aryl, or
(in which m represents an integer of 1 to 3; and R⁸ and R⁹ independently represent hydrogen or lower alkyl), or
(in which Y represents a single bond, oxygen, or N-R¹⁰ in which R¹⁰ represents hydrogen or lower alkyl; and n1 and n2 independently represent an integer of 1 to 3 )}, and pharmaceutically acceptable salts thereof.摘要翻译: 公开了由下式(I)表示的黄嘌呤衍生物:其中R 1,R 2和R 3独立地表示氢或低级烷基的
Q 1,Q 2和Q 3独立地表示氢,低级烷基,低级烷氧基或卤素; 并且X表示-COR 4(其中R 4表示氢,羟基,低级烷基或低级烷氧基)或-SO 2 R 5(其中R 5表示羟基,低级烷氧基,三氟甲基,CHEM 其中R 6和R 7独立地表示氢,羟基取代或未取代的低级烷基,芳基或 (其中m表示1至3的整数;并且R 8和R 8' 或其中Y表示单键,氧或NR 1,其中R 1表示氢或低级烷基;和n1 和n2独立地表示1〜3的整数)}及其药学上可接受的盐。 -
公开(公告)号:EP0415456A2
公开(公告)日:1991-03-06
申请号:EP90116791.6
申请日:1990-08-31
发明人: Suzuki, Fumio , Shimada, Junichi , Ishii, Akio , Ohno, Tetsuji , Karasawa, Akira , Kubo, Kazuhiro , Nonaka, Hiromi
IPC分类号: C07D473/06 , C07D473/08 , C07D473/20 , C07D473/22 , A61K31/52
CPC分类号: C07D473/06 , C07D473/08 , C07D473/20 , C07D473/22
摘要: Novel xanthine compounds represented by the following formula:
wherein each of R¹, R² and R³ independently represents a hydrogen atom or a lower alkyl group;
each of X¹ and X² independently represents an oxygen or sulfur atom;
represents a single bond or a double bond;
Y represents a single bond or an alkylene group, n represents 0 or 1, each of W¹ and W² independently represents a hydrogen atom, a lower alkyl or amino group, Z represents -CH₂-, -O-, -S- or -NH-residues; provided that when Q is
then R¹, R² and R³ are not simultaneously methyl; and physiologically acceptable salts thereof have a diuretic effect, a renal-protecting effect and/or a bronchodilatory effect.
The compounds are useful as a diuretic, a renal-protecting agent and /or bronchodilator.摘要翻译: 由下式表示的新型黄嘌呤化合物:
其中R 1,R 2和R 3各自独立地表示氢原子或低级烷基; X 1和X 2各自独立地表示氧或硫原子; 表示单键或双键; Y表示单键或亚烷基,n表示0或1,W 1和W 2各自独立地表示氢原子,低级烷基或氨基,Z表示-CH 2 - , - O-, -S-或-NH-残基; 条件是当Q为 则R 1,R 2和R 3不同时为甲基; 和其生理上可接受的盐具有利尿作用,肾保护作用和/或支气管扩张作用。 该化合物可用作利尿剂,肾保护剂和/或支气管扩张剂。 -
公开(公告)号:EP0415456B1
公开(公告)日:1996-06-26
申请号:EP90116791.6
申请日:1990-08-31
发明人: Suzuki, Fumio , Shimada, Junichi , Ishii, Akio , Ohno, Tetsuji , Karasawa, Akira , Kubo, Kazuhiro , Nonaka, Hiromi
IPC分类号: C07D473/06 , C07D473/08 , C07D473/20 , C07D473/22 , A61K31/52
CPC分类号: C07D473/06 , C07D473/08 , C07D473/20 , C07D473/22
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公开(公告)号:EP0386675B1
公开(公告)日:1996-06-05
申请号:EP90104201.0
申请日:1990-03-05
发明人: Suzuki, Fumio , Shimada, Junichi , Kubo, Kazuhiro , Ohno, Tetsuji , Karasawa, Akira , Ishii, Akio , Nonaka, Hiromi
IPC分类号: C07D473/06 , C07D473/22 , A61K31/52
CPC分类号: C07D473/04 , C07D473/06 , C07D473/22
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公开(公告)号:EP0560354A1
公开(公告)日:1993-09-15
申请号:EP93103926.7
申请日:1993-03-11
发明人: Suzuki, Fumio , Shimada, Junichi , Karasawa, Akira , Mizumoto, Hideaki , Kase, Hiroshi , Nonaka, Hiromi
IPC分类号: C07D473/06 , A61K31/52
CPC分类号: C07D473/06
摘要: A xanthine derivative of the formula (I):
wherein R¹ and R² are the same or different and are substituted or unsubstituted alicyclic alkyl; m1 and m2 are the same or different and represent an integer of 0 to 2; and Q represents
(in which R³ and R⁴ are the same or different and are substituted or unsubstituted alicyclic alkyl) or
(in which n is 0 or 1, and Y is a single bond or alkylene); or a pharmaceutically acceptable salt thereof is disclosed.
This derivative has diuretic activity and renal protecting activity.摘要翻译: 式(I)的黄嘌呤衍生物:
其中R 1和R 2相同或不同,为取代或未取代的脂环族烷基; m1和m2相同或不同,表示0〜2的整数。 和Q表示 (其中R 3和R 4相同或不同,为取代或未取代的脂环族烷基)或 (其中n为0或1,Y为单键 或亚烷基); 或其药学上可接受的盐。 该衍生物具有利尿活性和肾脏保护活性。 -
公开(公告)号:EP0386675A3
公开(公告)日:1992-01-15
申请号:EP90104201.0
申请日:1990-03-05
发明人: Suzuki, Fumio , Shimada, Junichi , Kubo, Kazuhiro , Ohno, Tetsuji , Karasawa, Akira , Ishii, Akio , Nonaka, Hiromi
IPC分类号: C07D473/06 , C07D473/22 , A61K31/52
CPC分类号: C07D473/04 , C07D473/06 , C07D473/22
摘要: Novel xanthine compounds represented by the following formula:
and pharmaceutically acceptable salts thereof have a diuretic action, a renal-protecting action and a vasodilative action. The compounds are useful as a diuretic, a renal-protecting agent and an antihypertensive agent.摘要翻译: 由下式表示的新型黄嘌呤化合物及其药学上可接受的盐具有利尿作用,肾脏保护作用和血管舒张作用。 该化合物可用作利尿剂,肾保护剂和抗高血压剂。
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公开(公告)号:EP0415456A3
公开(公告)日:1991-05-29
申请号:EP90116791.6
申请日:1990-08-31
发明人: Suzuki, Fumio , Shimada, Junichi , Ishii, Akio , Ohno, Tetsuji , Karasawa, Akira , Kubo, Kazuhiro , Nonaka, Hiromi
IPC分类号: C07D473/06 , C07D473/08 , C07D473/20 , C07D473/22 , A61K31/52
CPC分类号: C07D473/06 , C07D473/08 , C07D473/20 , C07D473/22
摘要: Novel xanthine compounds represented by the following formula:
wherein each of R¹, R² and R³ independently represents a hydrogen atom or a lower alkyl group;
each of X¹ and X² independently represents an oxygen or sulfur atom;
represents a single bond or a double bond;
Y represents a single bond or an alkylene group, n represents 0 or 1, each of W¹ and W² independently represents a hydrogen atom, a lower alkyl or amino group, Z represents -CH₂-, -O-, -S- or -NH-residues; provided that when Q is
then R¹, R² and R³ are not simultaneously methyl; and physiologically acceptable salts thereof have a diuretic effect, a renal-protecting effect and/or a bronchodilatory effect. The compounds are useful as a diuretic, a renal-protecting agent and /or bronchodilator.
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