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1. 发明授权

US4760064A Carbostyril compounds, compositions containing same and processes for preparing same 失效
标题翻译：碳青霉烯化合物，含有它们的组合物及其制备方法
公开(公告)号：US4760064A
公开(公告)日：1988-07-26
申请号：US808420
申请日：1985-12-13
申请人： Michiaki Tominaga , Takafumi Fujioka , Kazuyoshi Nagami , Kazuyuki Nakagawa
发明人： Michiaki Tominaga , Takafumi Fujioka , Kazuyoshi Nagami , Kazuyuki Nakagawa
IPC分类号： C07D215/38 , A61K31/495 , C07D401/04
CPC分类号： C07D215/38
摘要： A carbostyril compound of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are as defined or its pharmaceutically acceptable salt, composition containing the compound and processes for preparing the same are disclosed.The compound is useful as a cardiotonic agent.
摘要翻译：公开了式（I）的喹诺酮化合物：其中R 1和R 2如上所定义或其药学上可接受的盐，含该化合物的组合物及其制备方法。该化合物可用作强心剂。

2. 发明授权

US4593035A Carbostyril derivatives 失效
标题翻译：卡波他汀衍生物
公开(公告)号：US4593035A
公开(公告)日：1986-06-03
申请号：US679632
申请日：1984-12-10
申请人： Michiaki Tominaga , Hidenori Ogawa , Takafumi Fujioka , Yung-hsiung Yang , Kazuyuki Nakagawa
发明人： Michiaki Tominaga , Hidenori Ogawa , Takafumi Fujioka , Yung-hsiung Yang , Kazuyuki Nakagawa
IPC分类号： A61K31/47 , A61P9/08 , A61P9/10 , A61P9/12 , C07D215/38 , C07D407/12
CPC分类号： C07D407/12 , C07D215/38
摘要： Novel carbostyril derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen atom or a lower alkyl group, R.sup.2 is a lower alkyl group or a group of the formula: ##STR2## R.sup.3 is a lower alkylthio group, a lower alkyl group, a lower alkoxy group, phenoxy group, a phenyl(lower)alkoxy group, a lower alkenyloxy group, a phenyl group which may have a substituent selected from a lower alkoxy and a lower alkylenedioxy group on the phenyl ring, or a group of the formula: --NR.sup.4 R.sup.5 (R.sup.4 and R.sup.5 are the same or different and are each hydrogen atom or a lower alkyl group), and X is oxygen atom or sulfur atom, provided that when R.sup.1 is hydrogen atom and R.sup.2 is the group of the formula: ##STR3## X is not oxygen atom and R.sup.3 is not a lower alkyl group, and a pharmaceutically acceptable salt thereof, which show excellent pharmacological activities, such as myocardial contract increasing activity and coronary blood flow increasing activity and are useful for the treatment of heart diseases such as congestive heart failure.
摘要翻译：式（1）的新型喹诺酮衍生物：其中R 1是氢原子或低级烷基，R 2是低级烷基或下式的基团：R 3是低级烷硫基，低级烷基基团，低级烷氧基，苯氧基，苯基（低级）烷氧基，低级烯氧基，可具有选自苯环上的低级烷氧基和低级亚烷基二氧基的取代基的苯基，或一组式-NR4R5（R4和R5相同或不同，各自为氢原子或低级烷基），X为氧原子或硫原子，条件是当R 1为氢原子且R 2为式：X不是氧原子，R 3不是低级烷基，其药学上可接受的盐，其具有优异的药理活性，例如心肌收缩增加活性和冠状动脉血流增加活性，并且可用于治疗心脏病如充血性他艺术失败。

3. 发明授权

US5266577A Method of treating congestive heart failure using carbostyril derivatives 失效
标题翻译：使用喹诺酮衍生物治疗充血性心力衰竭的方法
公开(公告)号：US5266577A
公开(公告)日：1993-11-30
申请号：US734958
申请日：1991-07-24
申请人： Takafumi Fujioka , Shuji Teramoto , Michiaki Tominaga , Yoichi Yabuuchi
发明人： Takafumi Fujioka , Shuji Teramoto , Michiaki Tominaga , Yoichi Yabuuchi
IPC分类号： A61K31/47 , C07D215/22 , C07D215/227 , C07D215/54 , C07D401/12 , C07D409/12 , C07D215/16
CPC分类号： C07D215/227 , A61K31/47 , C07D215/54 , C07D401/12 , C07D409/12
摘要： Method for the treatment of congestive heart failure or paroxymal frequent heart pulse using a carbostyril derivative of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cycloalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonylalkyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoylalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of -A-NR.sup.4 R.sup.5 (R.sup.4 and R.sup.5 are each alkyl or phenyl having optionally substituents of halogen or alkoxy on phenyl ring, and A is alkylene which may be interrupted with O), and a salt thereof, and novel carbostyril derivatives, and pharmaceutical composition for prophylaxis and treatment of heart diseases containing said novel carbostyril derivative.
摘要翻译：使用下式的喹诺酮衍生物治疗充血性心力衰竭或阵发性频繁心脏脉搏的方法：其中R1是H或CN，R2和R3各自为H，任选地被OH，环烷基，烯基，苯基，在烷基部分上具有烷氧基烷氧基，卤素，烷氧基，NO2，烷基，CN，烷硫基或烷基亚磺酰基的任意取代基的苯基烷基，在苯环上具有任选烷氧基取代基的苯基磺酰基烷基，苯硫基烷基，具有卤素取代基的苯基亚磺酰基烷基或苯基环上的烷氧基，在苯环上具有卤素或烷氧基的任意取代基的苯氧基烷基，在吡啶环上具有卤素或烷氧基的任意取代基的吡啶基烷基，噻吩烷基，苯甲酰基烷基，苯硫基硫代羰基，苯甲酰基，吡啶基，苯基烯基或-A-NR4R5基团（ R4和R5各自为苯基上的烷基或具有卤素或烷氧基的任意取代基的苯基，A为a 可被O取代的亚烷基及其盐，以及新的喹诺酮衍生物，以及用于预防和治疗含有所述新型喹诺酮衍生物的心脏病的药物组合物。

4. 发明授权

US5760058A Peripheral vasodilating agent containing piperidine derivative as active ingredient 失效
标题翻译：含有哌啶衍生物作为活性成分的外周血管舒张剂
公开(公告)号：US5760058A
公开(公告)日：1998-06-02
申请号：US794322
申请日：1997-02-03
申请人： Takafumi Fujioka , Shuji Teramoto , Michinori Tanaka , Hiroshi Shimizu , Fujio Tabusa , Michiaki Tominaga
发明人： Takafumi Fujioka , Shuji Teramoto , Michinori Tanaka , Hiroshi Shimizu , Fujio Tabusa , Michiaki Tominaga
IPC分类号： C07D211/58 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D417/06 , C07D521/00 , A61K31/445
CPC分类号： C07D231/12 , C07D211/58 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D417/06
摘要： Peripheral vasodilating agents containing as an active ingredient, a piperidine derivative or pharmaceutically acceptable salt thereof having excellent peripheral vasodilating activity, said piperidine derivative or pharmaceutically acceptable salt thereof being represented by the general formula (1) ##STR1## wherein R, R.sup.1 and R.sup.2 are as defined herein.
摘要翻译：含有作为活性成分的外周血管舒张剂，具有优异的外周血管扩张活性的哌啶衍生物或其药学上可接受的盐，所述哌啶衍生物或其药学上可接受的盐由通式（1）表示。其中R，R 1 和R2如本文所定义。

5. 发明授权

US5053514A Cardiotonics 失效
标题翻译：心脏病
公开(公告)号：US5053514A
公开(公告)日：1991-10-01
申请号：US391305
申请日：1989-08-09
申请人： Takafumi Fujioka , Shuji Teramoto , Michiaki Tominaga , Yoichi Yabuuchi
发明人： Takafumi Fujioka , Shuji Teramoto , Michiaki Tominaga , Yoichi Yabuuchi
IPC分类号： C07D215/22 , A61K31/47 , A61P9/04 , C07D215/227 , C07D215/48 , C07D215/54 , C07D401/12 , C07D409/12
CPC分类号： C07D215/227 , A61K31/47 , C07D215/54 , C07D401/12 , C07D409/12 , Y10S514/929
摘要： Method for prophylaxis and treatment of heart diseases using a carbostyril derivative of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cyclocalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoyalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of --A--NR.sup.4 R.sup.5 (R.sup.4 and R.sup.5 are each alkyl or phenyl having optionally substituents of halogen or alkoxy on phenyl ring, and A is alkylene which may be interrupted with O), and a salt thereof, and novel carbostyril derivatives, and pharmaceutical composition of prophylaxis and treatment of heart diseases containing said novel carbostyril derivative.

6. 发明授权

US5532253A Agent for treating thrombosis and phosphodiesterase inhibitor 失效
标题翻译：治疗血栓形成和磷酸二酯酶抑制剂的药剂
公开(公告)号：US5532253A
公开(公告)日：1996-07-02
申请号：US352835
申请日：1994-12-02
申请人： Takafumi Fujioka , Shuji Teramoto , Michiaki Tominaga , Yoichi Yabuuchi
发明人： Takafumi Fujioka , Shuji Teramoto , Michiaki Tominaga , Yoichi Yabuuchi
IPC分类号： A61K31/47 , A61P7/02 , A61P43/00 , C07D215/22 , C07D215/227
CPC分类号： C07D215/227 , A61K31/47
摘要： A pharmaceutical preparation comprising at least one compound selected from the group consisting of carbostyril derivatives having the general formula: ##STR1## wherein R.sup.1 is hydrogen or a lower alkyl group optionally having hydroxy group as a substituent; R.sup.2 is a phenyl(lower alkyl) group optionally having 1 to 3 substituents selected from the group consisting of a lower alkoxy group and a halogen atom on the phenyl ring, pyridyl(lower alkyl) group, or a group of the formula --A--NR.sup.3 R.sup.4 (wherein A is a lower alkylene group, R.sup.3 and R.sup.4 are the same or different and represent a lower alkyl group or phenyl group), and a salt thereof, which is useful as an agent for treating thrombosis, more particularly, as an agent for inhibiting platelet aggregation, an agent for platelet aggregate dissociation, an ameliorant of cerebral circulation and a phosphodiesterase inhibitor.
摘要翻译：一种药物制剂，其包含至少一种选自具有以下通式的喹诺酮衍生物的化合物：其中R 1为氢或任选具有羟基作为取代基的低级烷基; R2是任选具有1〜3个选自苯环上的低级烷氧基和卤素原子的取代基的苯基（低级烷基），吡啶基（低级烷基）或式-A- NR3R4（其中A为低级亚烷基，R3和R4相同或不同，表示低级烷基或苯基）及其盐，其可用作治疗血栓形成的药剂，更特别是作为药剂用于抑制血小板聚集，血小板聚集体解离剂，脑循环改善剂和磷酸二酯酶抑制剂。

7. 发明授权

US5385914A Cardiotonic carbostyril agents for treating heart ailments 失效
标题翻译：用于治疗心脏病的强心性喹诺酮类药物
公开(公告)号：US5385914A
公开(公告)日：1995-01-31
申请号：US150792
申请日：1993-11-12
申请人： Takafumi Fujioka , Shuji Teramoto , Michiaki Tominaga , Yoichi Yabuuchi
发明人： Takafumi Fujioka , Shuji Teramoto , Michiaki Tominaga , Yoichi Yabuuchi
IPC分类号： C07D215/22 , A61K31/47 , A61P9/04 , C07D215/227 , C07D215/48 , C07D215/54 , C07D401/12 , C07D409/12
CPC分类号： C07D215/227 , A61K31/47 , C07D215/54 , C07D401/12 , C07D409/12 , Y10S514/929
摘要： Method for prophylaxis and treatment of heart diseases using a carbostyril derivative-of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cycloalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonylalkyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoylalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of --A--NR.sup.4 R.sup.5 (R.sup.4 and R.sup.5 are each alkyl or phenyl having optionally substituents of halogen or alkoxy on phenyl ring, and A is alkylene which may be interrupted with O), and a salt thereof, and novel carbostyril derivatives, and pharmaceutical composition for prophylaxis and treatment of heart diseases containing said novel carbostyril derivative.
摘要翻译：使用喹诺酮衍生物预防和治疗心脏病的方法：其中R1是H或CN，R2和R3各自为H，任选地被OH，环烷基，烯基，苯基，具有任选取代基的苯基烷基取代的烷基苯基环上烷氧基烷氧基，卤素，烷氧基，NO2，烷基，CN，烷硫基或烷基亚磺酰基，并且在烷基部分上具有任选的OH-取代基，在苯环上具有任选的烷氧基取代基的苯基磺酰基烷基，苯基硫代烷基，具有卤素或苯基上烷氧基的苯基亚磺酰基烷基环，苯基环上具有卤素或烷氧基的任意取代基的苯氧基烷基，吡啶环上具有卤素或烷氧基的任意取代基的吡啶基烷基，噻吩基烷基，苯甲酰基烷基，苯硫基硫代羰基，苯甲酰基，吡啶基，苯基烯基或-A-NR4R5基团（R4和R5是每个烷基或苯基在苯环上具有任选的卤素或烷氧基的取代基，A是可被中断的亚烷基与O）及其盐，以及新的喹诺酮衍生物，以及用于预防和治疗含有所述新型喹诺酮衍生物的心脏病的药物组合物。

8. 发明授权

US5198448A Cardiotonics 失效
标题翻译：强心剂
公开(公告)号：US5198448A
公开(公告)日：1993-03-30
申请号：US734957
申请日：1991-07-24
申请人： Takafumi Fujioka , Shuji Teramoto , Michiaki Tominaga , Yoichi Yabuuchi
发明人： Takafumi Fujioka , Shuji Teramoto , Michiaki Tominaga , Yoichi Yabuuchi
IPC分类号： A61K31/47 , C07D215/22 , C07D215/227 , C07D215/54 , C07D401/12 , C07D409/12
CPC分类号： C07D215/227 , A61K31/47 , C07D215/54 , C07D401/12 , C07D409/12
摘要： Method for prophylaxis and treatment of heart diseases using a carbostyril derivative of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cycloalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonylalkyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoylalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of --A-NR.sup.4 R.sup.5 (R.sup.4 and R.sup.5 are each alkyl or phenyl having optionally substituents of halogen or alkoxy on phenyl ring, and A is alkylene which may be interrupted with O), and a salt thereof, and novel carbostyril derivatives, and pharmaceutical composition for prophylaxis and treatment of heart diseases containing said novel carbostyril derivative.
摘要翻译：使用下式的喹诺酮衍生物预防和治疗心脏病的方法：其中R1是H或CN，R2和R3各自为H，任选地被OH，环烷基，烯基，苯基，任选地被烷氧基烷氧基，卤素，烷氧基，NO 2，烷基，CN，烷硫基或烷基亚磺酰基，并且在烷基部分上具有任选的OH-取代基，在苯环上具有任选烷氧基取代基的苯基磺酰基烷基，苯基硫基烷基，苯基环上具有卤素或烷氧基的苯基亚磺酰基烷基，具有任意取代基在苯环上具有卤素或烷氧基的苯氧基烷基，在吡啶环上具有卤素或烷氧基的任意取代基的吡啶基烷基，噻吩基烷基，苯甲酰基烷基，苯硫基硫代羰基，苯甲酰基，吡啶基，苯基烯基或-A-NR4R5基团（R4和R5各自为烷基或在苯环上具有卤素或烷氧基的任意取代基的苯基，A是可被中断的亚烷基与O）及其盐，以及新的喹诺酮衍生物，以及用于预防和治疗含有所述新型喹诺酮衍生物的心脏病的药物组合物。

9. 发明授权

US5656642A Peripheral vasodilating agent containing piperidine derivative as active ingredient 失效
标题翻译：含有哌啶衍生物作为活性成分的外周血管舒张剂
公开(公告)号：US5656642A
公开(公告)日：1997-08-12
申请号：US347454
申请日：1994-12-06
申请人： Takafumi Fujioka , Shuji Teramoto , Michinori Tanaka , Hiroshi Shimizu , Fujio Tabusa , Michiaki Tominaga
发明人： Takafumi Fujioka , Shuji Teramoto , Michinori Tanaka , Hiroshi Shimizu , Fujio Tabusa , Michiaki Tominaga
IPC分类号： C07D211/58 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D417/06 , C07D521/00 , A61K31/445
CPC分类号： C07D231/12 , C07D211/58 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D417/06
摘要： The present invention relates to novel peripheral vasodilating agents characterized by each containing as an active ingredient, a piperidine derivative or pharmaceutically acceptable salt thereof having excellent peripheral vasodilating activity.Said piperidine derivative or pharmaceutically acceptable salt thereof is represented by the general formula (1): ##STR1## (wherein R, R.sup.1 and R.sup.2 are the same as defined above.
摘要翻译： PCT No.PCT / JP94 / 00549 Sec。 371日期1994年12月6日第 102（e）日期1994年12月6日PCT 1994年4月4日PCT PCT。第WO94 / 22826号公报日期：1994年10月13日本发明涉及新颖的外周血管扩张剂，其特征在于每种含有作为活性成分的哌啶衍生物或其药学上可接受的盐具有优异的外周血管扩张活性。所述哌啶衍生物或其药学上可接受的盐由通式（1）表示：其中R，R 1和R 2与上述定义相同。

10. 发明授权

US5654317A Antiarrhythmic agent 失效
标题翻译：抗心律失常药
公开(公告)号：US5654317A
公开(公告)日：1997-08-05
申请号：US403891
申请日：1995-03-17
申请人： Takafumi Fujioka , Shuji Teramoto , Michiaki Tominaga , Yoichi Yabuuchi
发明人： Takafumi Fujioka , Shuji Teramoto , Michiaki Tominaga , Yoichi Yabuuchi
IPC分类号： A61K31/47 , A61K31/4704
CPC分类号： A61K31/4704 , A61K31/47
摘要： An antiarrhythmic agent which comprises as an active ingredient a carbostyril derivative of the formula: ##STR1## wherein R.sub.1 is hydrogen atom or a lower alkyl group, and R.sub.2 is a phenyl-lower alkyl group which has optionally 1 to 3 substituents of a lower alkoxy group on the phenyl ring, or a pharmaceutically acceptable salt thereof.
摘要翻译： PCT No.PCT / JP93 / 01294 Sec。 371日期1995年3月17日 102（e）1995年3月17日PCT 1993年9月10日PCT公布。出版物WO94 / 06427 日期：1994年3月31日一种抗心律失常药，其包含下式的喹诺酮衍生物作为活性成分：其中R1是氢原子或低级烷基，R2是具有任选的苯基 - 低级烷基苯基环上1至3个低级烷氧基的取代基，或其药学上可接受的盐。

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