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1. 发明授权

US4373104A Sulfur-containing isoquinoline derivatives, process for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：含硫异喹啉衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4373104A
公开(公告)日：1983-02-08
申请号：US164939
申请日：1980-07-01
申请人： Kalman Takacs , Maria H. Papp , Gabor Kovacs , Ilona K. Ajzert , Antal Simay , Peter L. Nagy , Marian E. Puskas , Gyula Sebestyen , Istvan Stadler , Zoltan Sumeghy
发明人： Kalman Takacs , Maria H. Papp , Gabor Kovacs , Ilona K. Ajzert , Antal Simay , Peter L. Nagy , Marian E. Puskas , Gyula Sebestyen , Istvan Stadler , Zoltan Sumeghy
IPC分类号： C07D217/00 , A61K31/47 , A61K31/472 , A61P7/08 , A61P7/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , A61P29/00 , A61P43/00 , C07D217/14 , C07D217/16 , C07D513/04
CPC分类号： C07D513/04 , C07D217/14 , Y10S514/869
摘要： Isoquinolines are disclosed of the formula (I) ##STR1## wherein R independently represents hydrogen, hydroxyl or alkoxy having 1 to 4 carbon atoms,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms and optionally substituted with phenyl, phenyl optionally substituted with one or more halogen or alkoxy group, cyano or carbomoyl,R.sup.2 is phenyl optionally substituted with one or more halogen, alkoxy or carboxyl, or a group of the general formula A ##STR2## wherein R.sup.3 is hydrogen, a straight or branched chained alkyl having 1 to 4 carbon atoms or phenyl,m and n independently represent 0, 1 or 2, with the proviso that m+n is at least 1,R.sup.4 is hydrogen, phenyl, hydroxyl, acyloxy, carboxyl, alkoxycarbonyl having 1 to 6 carbon atoms, carbamoyl, carbazoyl or dialkylamino containing 1 to 6 carbon atoms in the alkyl moiety, orR.sup.2 is a straight or branched chained alkylene group having 1 to 6 carbon atoms, andthe dotted line stands for a further carbon-carbon bond or hydrogen atoms in the 3- and 4-positions of the ring,or salts thereof. The new compounds are potent diuretic agents.
摘要翻译：公开了式（I）的异喹啉（I）其中R独立地表示氢，羟基或具有1至4个碳原子的烷氧基，R 1是氢，具有1至4个碳原子的烷基，任选被苯基取代，苯基任选地被一个或多个卤素或烷氧基取代，氰基或甲酰甲酰基，R 2是任选被一个或多个卤素，烷氧基或羧基取代的苯基或通式A的基团，其中R 3是氢，直链或支链具有1至4个碳原子的烷基或苯基，m和n独立地表示0,1或2，条件是m + n至少为1，R4为氢，苯基，羟基，酰氧基，羧基，具有1至6个碳原子的烷氧基羰基碳原子，氨基甲酰基，咔唑基或在烷基部分含有1至6个碳原子的二烷基氨基，或者R2是具有1至6个碳原子的直链或支链链烯基，虚线代表另外的碳 - 碳键或氢原子在3-和环的4-位，或其盐。新化合物是有效的利尿剂。

2. 发明授权

US4425349A Sulfur-containing isoquinoline derivatives in pharmaceutical compositions and methods of use 失效
标题翻译：含硫异喹啉衍生物在药物组合物和使用方法中的应用
公开(公告)号：US4425349A
公开(公告)日：1984-01-10
申请号：US381775
申请日：1982-05-25
申请人： Kalman Takacs , Maria H. Papp , Gabor Kovacs , Ilona K. Ajzert , Antal Simay , Peter Literati Nagy , Marian E. Puskas , Gyula Sebestyen , Istvan Stadler , Zoltan Sumeghy
发明人： Kalman Takacs , Maria H. Papp , Gabor Kovacs , Ilona K. Ajzert , Antal Simay , Peter Literati Nagy , Marian E. Puskas , Gyula Sebestyen , Istvan Stadler , Zoltan Sumeghy
IPC分类号： C07D217/14 , C07D513/04 , A61K31/47
CPC分类号： C07D513/04 , C07D217/14 , Y10S514/826 , Y10S514/869
摘要： The invention concerns new sulfur-containing isoquinoline derivatives. More particularly, the invention relates to isoquinoline derivatives of the general formula (I) ##STR1## wherein R independently represents hydrogen, hydroxyl or alkoxy having 1 to 4 carbon atoms,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms and optionally substituted with phenyl, phenyl optionally substituted with one or more halogen or alkoxy group, cyano or carbamoyl,R.sup.2 is phenyl optionally substituted with one or more halogen, alkoxy or carboxyl, or a group of the general formula A ##STR2## wherein R.sup.3 is hydrogen, a straight or branched chained alkyl having 1 to 4 carbon atoms or phenyl,m and n independently represent 0, 1 or 2, with the proviso that m+n is at least 1,R.sup.4 is hydrogen, phenyl, hydroxyl, acyloxy, carboxyl, alkoxycarbonyl having 1 to 6 carbon atoms, carbamoyl, carbazoyl or dialkylamino containing 1 to 6 carbon atoms in the alkyl moiety, orR.sup.2 is a straight or branched chained alkylene group having 1 to 6 carbon atoms, andthe dotted line stands for a further carbon-carbon bond or hydrogen atoms in the 3- and 4-positions of the ring,and salts and cyclic amides thereof.The new compounds possess valuable pharmaceutical activities, more particularly, are potent diuretic, antiasthmatic, hypotensive and antiinflammatory agents. Thus another aspect of the invention is a pharmaceutical composition which comprises as active ingredient a pharmaceutically effective amount of at least one compound of the general formula (I) with at least one pharmaceutically inert carrier or diluent. The invention also relates to a process for preparing these compounds.
摘要翻译：本发明涉及新的含硫异喹啉衍生物。更具体地说，本发明涉及通式（I）的异喹啉衍生物，其中R独立地表示氢，羟基或具有1至4个碳原子的烷氧基，R 1是氢，具有1至4个碳原子的烷基和任选地被苯基取代，任选被一个或多个卤素或烷氧基取代的苯基，氰基或氨基甲酰基，R 2是任选被一个或多个卤素，烷氧基或羧基取代的苯基或通式A的基团，其中R 3是氢，具有1至4个碳原子的直链或支链烷基或苯基，m和n独立地表示0,1或2，条件是m + n至少为1，R4为氢，苯基，羟基，酰氧基，羧基，具有1至6个碳原子的烷氧基羰基，在烷基部分含有1至6个碳原子的氨基甲酰基，咔唑基或二烷基氨基，或者是具有1至6个碳原子的直链或支链的亚烷基，虚线代表进一步c 环的3-和4-位的碳 - 碳键或氢原子，及其盐和环状酰胺。新化合物具有有价值的药物活性，特别是有效的利尿，止喘，降压和抗炎药。因此，本发明的另一方面是药物组合物，其包含作为活性成分的药学有效量的至少一种通式（I）的化合物与至少一种药学上惰性的载体或稀释剂。本发明还涉及制备这些化合物的方法。

3. 再颁专利

USRE32519E Sulfur-containing isoquinoline derivatives, process for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：含硫异喹啉衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：USRE32519E
公开(公告)日：1987-10-13
申请号：US524023
申请日：1983-08-17
申请人： Kalman Takacs , Maria H. Papp , Gabor Kovaacs , Ilona K. Ajzert , Antal Simay , Peter L. Nagy , Marian E. Puskas , Gyula Sebestyen , Istvan Stadler , Zoltan Sumeghy
发明人： Kalman Takacs , Maria H. Papp , Gabor Kovaacs , Ilona K. Ajzert , Antal Simay , Peter L. Nagy , Marian E. Puskas , Gyula Sebestyen , Istvan Stadler , Zoltan Sumeghy
IPC分类号： C07D217/14 , C07D513/04
CPC分类号： C07D513/04 , C07D217/14
摘要： Isoquinolines are disclosed of the formula (I) ##STR1## wherein R independently represents hydrogen, hydroxyl or alkoxy having 1 to 4 carbon atoms,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms and optionally substituted with phenyl, phenyl optionally substituted with one or more halogen or alkoxy group, cyano or carbomoyl,R.sup.2 is phenyl optionally substituted with one or more halogen, alkoxy or carboxyl, or a group of the general formula A ##STR2## wherein R.sup.3 is hydrogen, a straight or branched chained alkyl having 1 to 4 carbon atoms or phenyl,m and n independently represent 0, 1 or 2, with the proviso that m+n is at least 1,R.sup.4 is hydrogen, phenyl, hydroxyl, acyloxy, carboxyl, alkoxycarbonyl having 1 to 6 carbon atoms, carbamoyl, carbazoyl or dialkylamino containing 1 to 6 carbon atoms in the alkyl moiety, orR.sup.2 is a straight or branched chained alkylene group having 1 to 6 carbon atoms, andthe dotted line stands for a further carbon-carbon bond or hydrogen atoms in the 3- and 4-positions of the ring,or salts thereof. The new compounds are potent diuretic agents.

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