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1. 发明授权

US4329468A 3,4-Dihydrocarbostyril derivatives 失效
标题翻译： 3,4-二氢喹诺酮衍生物
公开(公告)号：US4329468A
公开(公告)日：1982-05-11
申请号：US162353
申请日：1980-06-24
申请人： Kazuyuki Nakagawa , Nanami Murakami , Shiro Yoshizaki , Hideo Mori , Michiaki Tominaga
发明人： Kazuyuki Nakagawa , Nanami Murakami , Shiro Yoshizaki , Hideo Mori , Michiaki Tominaga
IPC分类号： C07D215/22 , C07D215/227 , C07D215/26
CPC分类号： C07D215/227 , C07D215/26
摘要： Novel compounds represented by the formula ##STR1## wherein R.sup.1, R.sup.2, R' and R" are defined as hereinafter, having a blocking activity on .beta.-adrenergic nerves, novel intermediates useful for synthesis thereof and processes for preparing the same are disclosed. When substitution is at the 5-position and R.sup.1 and R.sup.2 are hydrogen, R' and R" are not simultaneously hydrogen and a 1 to 4 carbon atom alkyl group in the claimed compound.
摘要翻译：由式（I）表示的新型化合物，其中R1，R2，R'和R“定义如下，对β-肾上腺素能神经具有阻断活性，可用于其合成的新中间体及其制备方法被披露。当取代为5位且R 1和R 2为氢时，R'和R“不是所要求保护的化合物中的氢和1至4个碳原子的烷基。

2. 发明授权

US4256890A 3,4-Dihydrocarbostyril derivatives and process for producing the same 失效
标题翻译： 3,4-二氢喹诺酮衍生物及其制备方法
公开(公告)号：US4256890A
公开(公告)日：1981-03-17
申请号：US886373
申请日：1978-03-14
申请人： Kazuyuki Nakagawa , Nanami Murakami , Shiro Yoshizaki , Hideo Mori , Michiaki Tominaga
发明人： Kazuyuki Nakagawa , Nanami Murakami , Shiro Yoshizaki , Hideo Mori , Michiaki Tominaga
IPC分类号： C07D215/22 , C07D215/227 , C07D215/26
CPC分类号： C07D215/227 , C07D215/26
摘要： Novel compounds represented by the formula ##STR1## wherein R.sup.1, R.sup.2, and R' and R" are defined as hereinafter, having a blocking activity on .beta.-adrenergic nerves, novel intermediates useful for synthesis thereof and processes for preparing the same are disclosed. When substitution is at the 5-position and R.sup.1 and R.sup.2 are hydrogen, R' and R" are not simultaneously hydrogen and a 1 to 4 carbon atom alkyl group in the claimed compound.
摘要翻译：由式（I）表示的新型化合物，其中R1，R2和R'和R“定义如下，对β-肾上腺素能神经具有阻断活性，可用于其合成的新中间体和制备同样披露。当取代为5位且R 1和R 2为氢时，R'和R“不是所要求保护的化合物中的氢和1至4个碳原子的烷基。

3. 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。

4. 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。

5. 发明授权

US4585774A Aniline derivatives and cardiotonic composition 失效
标题翻译：苯胺衍生物和强心组成
公开(公告)号：US4585774A
公开(公告)日：1986-04-29
申请号：US432902
申请日：1982-09-29
申请人： Michiaki Tominaga , Yung-hsiung Yang , Hidenori Ogawa , Kazuyuki Nakagawa
发明人： Michiaki Tominaga , Yung-hsiung Yang , Hidenori Ogawa , Kazuyuki Nakagawa
IPC分类号： A61K31/495 , A61K31/496 , A61P9/04 , C07D295/10 , C07D295/15 , C07D295/16 , C07D295/18 , C07D295/192
CPC分类号： C07D295/192 , C07C255/00 , C07D295/15
摘要： Aniline derivatives of the formula: ##STR1## wherein R.sup.0, R.sup.1 and R.sup.2 are the same or different and each is a hydrogen atom, a halogen atom, a nitro group, an amino group, a carboxy group, a cyano group, a hydroxy group, a sulfonamido group, a lower alkyl group, a lower alkoxycarbonyl group, a lower alkoxy group, a lower alkanoyl group, a lower alkylamino group, a lower alkylthio group, a lower alkanoylamino group or a group of the formula ##STR2## wherein R.sup.5 and R.sup.6 are the same or different and each is a hydrogen atom, a lower alkyl group or a C.sub.3 to C.sub.8 cycloalkyl group or together with the nitrogen atom a morpholino, piperidino, piperazino or pyrrolidino group; R.sup.3 is a cyano group, a nitro group, a halogen atom, a lower alkyl group or a lower alkoxy group; m is an integer of 1 to 3; R.sup.4 is a hydrogen atom or a lower alkyl group; and A is a lower alkylene group. The derivatives are useful as cardiotonics.
摘要翻译： PCT No.PCT / JP82 / 00152 Sec。 371日期：1982年9月29日 102（e）日期1982年9月29日PCT提交1982年5月4日PCT公布。出版物WO82 / 03861 日本11月11日，下式的苯胺衍生物：其中R 0，R 1和R 2相同或不同，各自为氢原子，卤素原子，硝基，氨基，羧基，氰基，羟基，亚磺酰氨基，低级烷基，低级烷氧基羰基，低级烷氧基，低级烷酰基，低级烷基氨基，低级烷硫基，低级烷酰基氨基或低级烷氧基其中R 5和R 6相同或不同，并且各自为氢原子，低级烷基或C 3至C 8环烷基，或与氮原子一起形成吗啉代，哌啶子基，哌嗪基或吡咯烷基; R3是氰基，硝基，卤素原子，低级烷基或低级烷氧基; m为1〜3的整数。 R4是氢原子或低级烷基; A为低级亚烷基。衍生物可用作强心剂。

6. 发明授权

US4487772A Carbostyril derivatives and their salts 失效
标题翻译：卡波他汀衍生物及其盐
公开(公告)号：US4487772A
公开(公告)日：1984-12-11
申请号：US348709
申请日：1982-02-16
申请人： Michiaki Tominaga , Yung-hsiung Yang , Hidenori Ogawa , Kazuyuki Nakagawa
发明人： Michiaki Tominaga , Yung-hsiung Yang , Hidenori Ogawa , Kazuyuki Nakagawa
IPC分类号： C07C215/06 , A61K31/44 , A61K31/4704 , A61P9/04 , C07C205/57 , C07D215/20 , C07D215/227 , C07D215/48 , C07D265/16 , C07D295/04 , C07D403/06 , C07D413/12 , C07D401/06 , A61K31/495
CPC分类号： C07D215/48 , C07C205/57
摘要： Carbostyril derivatives of the general formula ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a phenyl-lower alkyl group and R.sup.2 and R.sup.3 may be the same or different and each is a substituted or unsubstituted lower alkyl group, or R.sup.2 and R.sup.3 may form, together with the adjacent nitrogen atom, a 5- or 6-membered saturated heterocyclic ring which may be substituted or unsubstituted. The derivatives are useful as the active ingredient in cardiotonic compositions.
摘要翻译：其中R1是氢原子，低级烷基，低级烯基，低级炔基或苯基 - 低级烷基的通式为“IMAGE”的卡波他特尔衍生物，R 2和R 3可以相同或不同，取代或未取代的低级烷基，或R 2和R 3可与相邻的氮原子一起形成可被取代或未取代的5或6元饱和杂环。该衍生物可用作强心剂组合物中的活性成分。

7. 发明授权

US4454130A Morpholino and oxazoline substituted carbostyril derivatives, process for producing the same and cardiotonic compositions containing the same 失效
标题翻译：吗啉代和恶唑啉取代的喹诺酮衍生物，其制备方法和含有它们的强心组合物
公开(公告)号：US4454130A
公开(公告)日：1984-06-12
申请号：US525812
申请日：1983-08-22
申请人： Michiaki Tominaga , Yung-hsiung Yang , Hidenori Ogawa , Kazuyuki Nakagawa
发明人： Michiaki Tominaga , Yung-hsiung Yang , Hidenori Ogawa , Kazuyuki Nakagawa
IPC分类号： C07C215/06 , A61K31/44 , A61K31/4704 , A61P9/04 , C07C205/57 , C07D215/20 , C07D215/227 , C07D215/48 , C07D265/16 , C07D295/04 , C07D403/06 , C07D413/12 , A61K31/47 , A61K31/535
CPC分类号： C07D215/48 , C07C205/57
摘要： Novel carbostyril derivatives and their pharmaceutically acceptable salts represented by the formula (1). ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a phenyl-lower alkyl group, R.sup.2 and R.sup.3 form, together with the adjacent nitrogen atom and further with an additional oxygen atom, a 5- or 6-membered saturated heterocyclic ring which may have a lower alkyl group or a phenyl-lower alkyl group as the substituent; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton being a single or double bond. The derivatives are useful as the active ingredient in cardiotonic compositions.
摘要翻译：新型喹诺酮衍生物及其由式（1）表示的药学上可接受的盐。（1）其中R1是氢原子，低级烷基，低级烯基，低级炔基或苯基 - 低级烷基，R2和R3与相邻的氮原子一起形成，进一步与另外的氧原子，可以具有低级烷基或苯基 - 低级烷基作为取代基的5-或6-元饱和杂环; 喹诺酮骨架中3-和4-位之间的碳 - 碳键是单键或双键。该衍生物可用作强心剂组合物中的活性成分。

8. 发明授权

US4514401A Carbostyril derivatives 失效
标题翻译：卡波他汀衍生物
公开(公告)号：US4514401A
公开(公告)日：1985-04-30
申请号：US407099
申请日：1982-08-11
申请人： Michiaki Tominaga , Yung-hsiung Yang , Hidenori Ogawa , Kazuyuki Nakagawa
发明人： Michiaki Tominaga , Yung-hsiung Yang , Hidenori Ogawa , Kazuyuki Nakagawa
IPC分类号： C07D401/12 , C07D215/22 , C07D215/227 , C07D405/12 , C07D215/00 , A61K31/47
CPC分类号： C07D215/227 , C07D405/12
摘要： Novel carbostyril derivatives represented by the general formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a phenyl-lower alkyl group; R.sup.2 is a lower alkanoyl group, a lower alkoxycarbonyl group, a furoyl group, a lower alkane-sulfonyl group, a substituted benzoyl group, a substituted phenyl-lower alkenylcarbonyl group, a phenoxy-lower alkyl group, or a substituted phenylsulfonyl group; A is a lower alkylene group; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or double bond; and the substituted position of the side-chain of the formula, ##STR2## may be of 5-, 6-, 7- or 8-position in the carbostyril skeleton; and acid addition salts thereof.The carbostyril derivatives of the general formula (1) of the present invention and acid addition salts thereof have myocardial contraction increasing activity (positive inotropic activity), coronary blood flow increasing activity and hypotensive activity. They are useful as cardiotonics for curing various heart diseases such as congestive heart failure, mitralism, auricular fibrillation, auricular flutter, paroxysmal atrial tachycardia and the like.
摘要翻译：由通式（1）表示的新型喹诺酮衍生物，其中R1是氢原子，低级烷基，低级烯基，低级炔基或苯基低级烷基; R2是低级烷酰基，低级烷氧基羰基，糠酰基，低级链烷磺酰基，取代苯甲酰基，取代苯基 - 低级烯基羰基，苯氧基 - 低级烷基或取代的苯基磺酰基。 A是低级亚烷基; 喹诺酮骨架中3-和4-位之间的碳 - 碳键是单键或双键; 并且式VIII的侧链的取代位置可以在喹诺酮骨架中为5-，6-，7-或8-位; 及其酸加成盐。本发明的通式（1）的喹诺酮衍生物及其酸加成盐具有心肌收缩增加活性（正性肌力活性），冠状血流增加活性和降血压活性。它们可用作治疗各种心脏疾病如心力衰竭，二尖瓣，耳颤，耳颤，阵发性房性心动过速等的心力学。

9. 发明授权

US4415572A Piperazinylcarbostyril compounds 失效
标题翻译：哌嗪腈基稳定剂化合物
公开(公告)号：US4415572A
公开(公告)日：1983-11-15
申请号：US316572
申请日：1981-10-30
申请人： Michiaki Tominaga , Yung h. Yang , Hidenori Ogawa , Kazuyuki Nakagawa
发明人： Michiaki Tominaga , Yung h. Yang , Hidenori Ogawa , Kazuyuki Nakagawa
IPC分类号： C07D401/10 , A61K31/4704 , A61K31/495 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , C07D215/38 , C07D215/40 , C07D295/155 , C07D295/18 , C07D295/192 , C07D401/04 , C07D405/12 , C07D401/00
CPC分类号： C07D295/192 , C07D215/38 , C07D215/40 , C07D295/155 , C07D405/12
摘要： A piperazinylcarbostyril compound of the formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, or a phenyl-lower alkyl group;R.sup.2 represents a hydrogen atom or a lower alkoxy group;R.sup.3 represents a hydrogen atom, a lower alkanoyl group, a furoyl group, a pyridylcarbonyl group, a lower alkanesulfonyl group, a lower alkoxycarbonyl group, a lower alkoxycarbonyl-lower alkyl group, a phenylsulfonyl group which may be substituted with a lower alkyl group on the benzene ring thereof, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a phenylcarbonyl group, a phenyl-lower alkyl group or a phenyl-lower alkanoyl group where each of said phenylcarbonyl group, phenyl-lower alkyl group and phenyl-lower alkanoyl group may be substituted with 1 to 3 of a lower alkoxy group, a halogen atom, a lower alkyl group, a cyano group, a nitro group, an amino group, a hydroxy group, a lower alkanoylamino group, a lower alkylthio group and a lower alkanoyloxy group, or with a lower alkylenedioxy group on the benzene ring thereof; andthe bonding between the 3- and 4-positions of the carbostyril nucleus is a single bond or a double bond; or its pharmaceutically acceptable salt, useful as a cardiotonic agent.
摘要翻译：式（I）的哌嗪基卡必维尔化合物其中R 1表示氢原子，低级烷基，低级烯基，低级炔基或苯基低级烷基; R2表示氢原子或低级烷氧基; R3表示氢原子，低级烷酰基，糠酰基，吡啶基羰基，低级链烷磺酰基，低级烷氧基羰基，低级烷氧羰基 - 低级烷基，可被低级烷基取代的苯磺酰基，其苯环，低级烷基，低级烯基，低级炔基，苯基羰基，苯基 - 低级烷基或苯基 - 低级烷酰基，其中所述苯基羰基，苯基 - 低级烷基和苯基 - 低级烷酰基可以被1〜3个低级烷氧基，卤素原子，低级烷基，氰基，硝基，氨基，羟基，低级烷酰基氨基，低级烷硫基和低级烷酰氧基，或在其苯环上具有低亚烷基二氧基; 并且喹诺酮环的3-和4-位之间的键合是单键或双键; 或其药学上可接受的盐，可用作强心剂。

10. 发明授权

US4289883A Carbostyril compounds 失效
标题翻译：碳青霉烯化合物
公开(公告)号：US4289883A
公开(公告)日：1981-09-15
申请号：US965535
申请日：1978-11-30
申请人： Michiaki Tominaga , Hitoshi Tone , Kazuyuki Nakagawa
发明人： Michiaki Tominaga , Hitoshi Tone , Kazuyuki Nakagawa
IPC分类号： C07D215/24 , C07D215/26 , C07D215/32 , C07D401/12 , C07D405/12 , C07D413/12 , C07D215/22 , A61K31/47
CPC分类号： C07D215/32 , C07D215/26 , Y10S514/821 , Y10S514/826
摘要： Carbostyril compounds represented by the formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group or a phenylalkyl group, R.sub.2 represents an alkenyl group, an alkoxyalkyl group, a hydroxyalkyl group, a carboxyalkyl group, an alkylcarbonyl group, a cycloalkylcarbonyl group, an alkylcarbonylalkyl group, an alkoxycarbonylalkyl group, an alkynyl group or a carbamoylalkyl group, R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen atom, an alkyl group, a cycloalkyl group, an alkoxyalkyl group, an alkenyl group, a phenylalkyl group, a phenoxyalkyl group or a phenyl group, and the 3,4-bond of the carbostyril nucleus represents a single or double bond, pharmaceutically acceptable salts thereof, and a process for preparing the same.
摘要翻译：由式（I）表示的卡博司坦化合物其中R1表示氢原子，烷基或苯基烷基，R2表示烯基，烷氧基烷基，羟烷基，羧基烷基，烷基羰基基团，环烷基羰基，烷基羰基烷基，烷氧基羰基烷基，炔基或氨基甲酰基烷基，可以相同或不同的R 3和R 4各自表示氢原子，烷基，环烷基，烷氧基烷基基团，烯基，苯基烷基，苯氧基烷基或苯基，喹诺酮环的3,4-键表示单键或双键，其药学上可接受的盐及其制备方法。

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