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1. 发明授权

US4308270A 1,2,4-Oxadiazine derivatives, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译： 1,2,4-恶二嗪衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4308270A
公开(公告)日：1981-12-29
申请号：US196034
申请日：1980-10-10
申请人： Kalman Takacs , Antal Simay , Ilona Kiss nee Ajzert , Peter L. Nagy , Maria Hetyey nee Papp , Marian Escery nee Puskas , Jozsef Szegy , Sandor Virag , Sandor J. Nagy
发明人： Kalman Takacs , Antal Simay , Ilona Kiss nee Ajzert , Peter L. Nagy , Maria Hetyey nee Papp , Marian Escery nee Puskas , Jozsef Szegy , Sandor Virag , Sandor J. Nagy
IPC分类号： A61K31/535 , A61P7/10 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P29/00 , C07D273/04 , C07D413/06
CPC分类号： C07D273/04 , Y10S514/821 , Y10S514/869
摘要： The invention concerns new compounds of the general formula (I) ##STR1## wherein R.sup.1 is hydrogen or phenyl optionally substituted by one or more of the following substituents: alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro;R.sup.2 is alkyl having 1 to 4 carbon atoms, cycloalkyl having 5 to 7 carbon atoms or phenyl, optionally substituted with one or more of the following groups: alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro; or R.sup.2 is a naphthyl group;R.sup.3 is alkyl having 1 to 4 carbon atoms, acyl or hydrogen;R.sup.4 hydrogen or alkyl having 1 to 4 carbon atoms;R.sup.5 is cycloalkyl having 5 to 7 carbon atoms, alkyl having 1 to 6 carbon atoms, phenyl-(C.sub.1-4 -alkyl) in which the phenyl moiety may optionally be substituted with alkoxy having 1 to 4 carbon atoms, halogen or nitro;or R.sup.4 and R.sup.5 together represent a group of the general formula (V) ##STR2## wherein R.sup.6 is hydrogen or alkoxy having 1 to 4 carbon atoms, m and n stand for 0, 1 or 2and acid addition and quaternary salts thereof.The compounds of the general formula (I) are potent peripheral vasodilators and hypotensive agents. They increase the coronary blood flow and in addition to their slight antiinflammatory and diuretic acidivity possess strong antiarrhythmic properties.A process for the preparation of these compounds and pharmaceutical compositions containing them are also within the scope of the invention.
摘要翻译：本发明涉及通式（I）的新化合物其中R 1为氢或任选被一个或多个下述取代基取代的苯基：具有1-4个碳原子的烷基，卤素，具有1-4个碳原子的烷氧基碳原子或硝基; R 2是具有1至4个碳原子的烷基，具有5至7个碳原子的环烷基或苯基，任选被一个或多个下列基团取代：具有1至4个碳原子的烷基，卤素，具有1至4个碳原子的烷氧基或硝基 ; 或R 2为萘基; R3是具有1-4个碳原子的烷基，酰基或氢; R4是氢或具有1-4个碳原子的烷基; R5是具有5至7个碳原子的环烷基，具有1至6个碳原子的烷基，苯基部分可任选地被具有1至4个碳原子的烷氧基取代的苯基 - （C 1-4 - 烷基），卤素或硝基; 或者R 4和R 5一起表示通式（V）的基团，其中R 6是氢或具有1至4个碳原子的烷氧基，m和n代表0,1或2，酸加成和季盐其中。通式（I）的化合物是有效的外周血管扩张剂和降压药。它们增加冠状动脉血流量，除了其轻微的抗炎和利尿酸性之外，具有强烈的抗心律失常性质。制备这些化合物的方法和含有它们的药物组合物也在本发明的范围内。

2. 发明授权

US4365064A 1,2,4-Oxadiazolin-5-one derivatives, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译： 1,2,4-恶二唑啉-5-酮衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4365064A
公开(公告)日：1982-12-21
申请号：US196583
申请日：1980-10-14
申请人： Kalman Takacs , Ilona Kiss nee Ajzert , Antal Simay , Peter Literati Nagy , Maria Hetyey nee Papp , Marian Ecsery nee Puskas , Laszlo Szekeres , Gyula Papp , Sandor Viragh , Eva Udvardy
发明人： Kalman Takacs , Ilona Kiss nee Ajzert , Antal Simay , Peter Literati Nagy , Maria Hetyey nee Papp , Marian Ecsery nee Puskas , Laszlo Szekeres , Gyula Papp , Sandor Viragh , Eva Udvardy
IPC分类号： C07D413/06 , A61K20060101 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/435 , A61K31/47 , A61K31/475 , A61P9/08 , C07D20060101 , C07D217/00 , C07D217/04 , C07D217/16 , C07D271/00 , C07D271/06 , C07D273/04 , C07D401/06
CPC分类号： A61K31/41 , A61K31/415 , A61K31/42 , A61K31/435 , A61K31/47 , A61K31/475 , C07D217/00 , C07D217/04 , C07D217/16 , C07D271/00 , C07D271/06 , C07D273/04 , C07D401/06 , C07D413/06 , Y10S514/929 , Y10S514/96 , Y10S514/962
摘要： The invention concerns new compounds of the formula (I) ##STR1## wherein R.sup.1 is hydrogen, phenyl or phenyl substituted with at least one alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro;R.sup.2 is alkyl having 1 to 4 carbon atoms, cycloalkyl having 5 to 7 carbon atoms, phenyl, or phenyl substituted with at least one alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro;R.sup.3 is alkoxy having 1 to 4 carbon atoms or hydrogen,R.sup.4 is hydrogen, alkyl having 1 to 4 carbon atoms unsubstituted or substituted with alkoxy having 1 to 4 carbon atoms, benzyloxy or cyano, phenyl, or phenyl substituted with at least one alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro, or phenyl-(C.sub.1-4 alkyl)-alkyl, in which the phenyl moiety may bear an alkoxy substituent having 1 to 4 carbon atoms or a halogen;m and n are each 0, 1 or 2 or a pharmaceutically acceptable acid addition or quaternary salt thereof.The compounds are potent vasodilators and exert a favorable influence on the extremital blood flow. They also show a heart function influencing activity.Methods for the preparation of said compounds and pharmaceutical compositions containing them are also the subject of the invention.
摘要翻译：本发明涉及新的式（I）化合物，其中R 1是氢，苯基或被至少一个具有1-4个碳原子的烷基取代的苯基，卤素，具有1-4个碳原子的烷氧基或硝基; R2是具有1至4个碳原子的烷基，具有5至7个碳原子的环烷基，苯基或被至少一个具有1至4个碳原子的烷基取代的苯基，卤素，具有1至4个碳原子的烷氧基或硝基; R3为具有1-4个碳原子的烷氧基或氢，R4为氢，未取代或未被取代或未被取代或未被取代的具有1-4个碳原子的烷氧基的烷基，苄氧基或氰基，苯基或被至少一个具有至少一个烷基 1至4个碳原子，卤素，具有1至4个碳原子的烷氧基或硝基，或苯基 - （C 1-4烷基） - 烷基，其中苯基部分可以带有具有1至4个碳原子的烷氧基取代基或卤素; m和n各自为0,1或2，或其药学上可接受的酸加成盐或季盐。这些化合物是有效的血管扩张剂，对前列腺血流量有很好的影响。它们也显示出影响活动的心脏功能。制备所述化合物的方法和含有它们的药物组合物也是本发明的主题。

3. 发明授权

US4187220A New O-(3-amino-2-hydroxy-propyl)-amidoxime derivatives, process for the preparation thereof and pharmaceutical compositions containing same 失效
标题翻译：新的O-（3-氨基-2-羟基 - 丙基） - 偕胺肟衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4187220A
公开(公告)日：1980-02-05
申请号：US829148
申请日：1977-08-30
申请人： Kalman Takacs , Peter N. Literati , Ilona Kiss nee Ajzert , Antal Simay , Matyas Szentivanyi , Sandor Virag , Katalin Farago
发明人： Kalman Takacs , Peter N. Literati , Ilona Kiss nee Ajzert , Antal Simay , Matyas Szentivanyi , Sandor Virag , Katalin Farago
IPC分类号： C07C259/14 , C07C259/18 , C07D211/28 , C07D213/42 , C07D215/12 , C07D217/14 , C07D231/12 , C07D295/088 , C07D295/14 , C07D401/12 , C07D403/12
CPC分类号： C07D231/12 , C07C259/14 , C07C259/18 , C07D211/28 , C07D213/42 , C07D215/12 , C07D217/14 , C07D295/088
摘要： A compound effective in the treatment of diabetic angiopathy, i.e. a selective .beta.-receptor blocker has the formula ##STR1## wherein: R.sup.2 is a hydrogen or alkyl having one to five carbon atoms, R.sup.3 is alkyl having one to five carbon atoms, cycloalkyl or phenyl optionally substituted with hydroxyl or phenyl, or R.sup.2 and R.sup.3 together form a five- to eight-membered ring optionally containing also other heteroatoms and/or fused with an other ring, preferably phenyl, naphthyl, quinolyl, isoquinolyl, pyridyl, pyrazolyl, R.sup.5 is hydrogen or alkyl having one to four carbon atoms, cycloalkyl or phenyl optionally substituted with halogen, alkoxy having one to four carbon atoms or alkyl having one to four carbon atoms, R.sup.6 is hydrogen, alkyl having one to four carbon atoms or phenyl, m=0, 1 or 2, and n=0, 1 or 2.
摘要翻译：治疗糖尿病性血管病的化合物，即选择性β-受体阻断剂具有下式（I）其中：R 2是氢或具有1至5个碳原子的烷基，R 3是具有1至5个碳原子的烷基任选地被羟基或苯基取代的环烷基或苯基，或者R 2和R 3一起形成任选地还含有其它杂原子和/或与另一个环稠合的五至八元环，优选苯基，萘基，喹啉基，异喹啉基，吡啶基，吡唑基，R5是氢或具有1-4个碳原子的烷基，环烷基或任选被卤素取代的苯基，具有1-4个碳原子的烷氧基或具有1-4个碳原子的烷基，R6是氢，具有1-4个碳原子的烷基或苯基，m = 0,1或2，n = 0,1或2。

4. 发明授权

US4308399A O-(3-Amino-2-hydroxy-propyl)-amidoxime derivatives, process for the preparation thereof and pharmaceutical compositions containing same 失效
标题翻译： O-（3-氨基-2-羟基 - 丙基） - 氨基肟衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4308399A
公开(公告)日：1981-12-29
申请号：US54791
申请日：1979-07-05
申请人： Kalman Takacs , Peter N. Literati , Ilona Kiss nee Ajzert , Antal Simay , Matyas Szentivanyi , Sandor Virag , Katalin Farago
发明人： Kalman Takacs , Peter N. Literati , Ilona Kiss nee Ajzert , Antal Simay , Matyas Szentivanyi , Sandor Virag , Katalin Farago
IPC分类号： C07C259/14 , C07C259/18 , C07D211/28 , C07D213/42 , C07D215/12 , C07D217/14 , C07D231/12 , C07D295/088 , C07D295/14 , C07D401/12 , C07D403/12
CPC分类号： C07D231/12 , C07C259/14 , C07C259/18 , C07D211/28 , C07D213/42 , C07D215/12 , C07D217/14 , C07D295/088
摘要： A compound effective in the treatment of diabetic angiopathy, i.e. a selective .beta.-receptor blocker has the formula ##STR1## wherein: R.sup.2 is a hydrogen or alkyl having one to five carbon atoms,R.sup.3 is alkyl having one to five carbon atoms, cycloalkyl or phenyl optionally substituted with hydroxyl or phenyl, or R.sup.2 and R.sup.3 together form a five- to eight-membered ring optionally containing also other heteroatoms and/or fused with another ring, preferably phenyl, naphthyl, quinolyl, isoquinolyl, pyridyl, pyrazolyl,R.sup.5 is hydrogen or alkyl having one to four carbon atoms, cycloalkyl or phenyl optionally substituted with halogen, alkoxy having one to four carbon atoms or alkyl having one to four carbons,R.sup.6 is hydrogen, alkyl having one to four carbon atoms or phenyl, m=0, 1 or 2, and n=0, 1 or 2.
摘要翻译：治疗糖尿病性血管病的化合物，即选择性β-受体阻断剂具有下式（I）其中：R 2是氢或具有1至5个碳原子的烷基，R 3是具有1至5个碳原子的烷基，任选被羟基或苯基取代的环烷基或苯基，或者R 2和R 3一起形成任选地还含有其它杂原子和/或与另一个环稠合的五至八元环，优选苯基，萘基，喹啉基，异喹啉基，吡啶基，吡唑基 R5是氢或具有1-4个碳原子的烷基，环烷基或任选被卤素取代的苯基，具有1-4个碳原子的烷氧基或具有1-4个碳原子的烷基，R6是氢，具有1-4个碳原子的烷基或苯基， m = 0,1或2，n = 0,1或2。

5. 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。

6. 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.

7. 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。

8. 发明申请

US20080108673A1 Prevention and Treatment of Obesity 失效
标题翻译：预防和治疗肥胖
公开(公告)号：US20080108673A1
公开(公告)日：2008-05-08
申请号：US11687945
申请日：2007-03-19
申请人： Peter Literati Nagy , Zoltan Szilvassy , Kalman Tory , Laszlo Vigh , Kalman Takacs , Jozsef Mandl , Balazs Sumegi , Sandor Bernath , Attila Kolonics , Gabor Balogh , Janos Egri
发明人： Peter Literati Nagy , Zoltan Szilvassy , Kalman Tory , Laszlo Vigh , Kalman Takacs , Jozsef Mandl , Balazs Sumegi , Sandor Bernath , Attila Kolonics , Gabor Balogh , Janos Egri
IPC分类号： A61K31/44 , A61P3/04
CPC分类号： A61K31/4545 , Y10S514/909
摘要： O-(3-piperidino-2-hydroxypropyl)-nicotinic amidoxime or a pharmaceutically suitable acid addition salt thereof (BGP-15) can be used for the prevention or reduction of weight gain or the reduction of the rate of body weight.
摘要翻译： O-（3-哌啶子基-2-羟丙基） - 烟酰胺肟或其药学上合适的酸加成盐（BGP-15）可以用于预防或减轻体重增加或减轻体重。

9. 发明授权

US5179089A Isoquinoline compounds, compositions and use 失效
标题翻译：异喹啉化合物，组合物和用途
公开(公告)号：US5179089A
公开(公告)日：1993-01-12
申请号：US792255
申请日：1991-11-14
申请人： Kalman Takacs , Iloma Kiss neAjzert , Istvan Hermecz , Janos Ori , Maria H. Pap , Zsolt Bencze , Peter S. Kormoczy , Maria Szabo , Judit Szeredy nee Varga , Csaba Vertesi , Lorand Debreczeni , Jozsef Gaal , Zoltan Kapui
发明人： Kalman Takacs , Iloma Kiss neAjzert , Istvan Hermecz , Janos Ori , Maria H. Pap , Zsolt Bencze , Peter S. Kormoczy , Maria Szabo , Judit Szeredy nee Varga , Csaba Vertesi , Lorand Debreczeni , Jozsef Gaal , Zoltan Kapui
IPC分类号： A61K31/47 , A61K31/33 , A61K31/472 , A61K31/4725 , A61P11/08 , A61P29/00 , A61P37/08 , C07D217/12 , C07D217/16 , C07D217/26
CPC分类号： C07D217/16
摘要： The invention relates to novel compounds of the general formula (I), ##STR1## wherein R means hydrogen or a straight or branched chain C.sub.1-6 alkoxy group;R.sup.1 stands for hydrogen or a straight or branched chain C.sub.1-6 alkyl group;R.sup.2 represents hydrogen or a straight or branched chain C.sub.1-6 alkyl group;R.sup.3 means hydrogen, a straight or branched chain C.sub.1-6 alkyl group optionally substituted by one or two hydroxyl and/or one or two straight or branched chain C.sub.1-4 alkoxy group(s); or a C.sub.4-7 cycloalkyl group;R.sup.4 stands for hydrogen or a straight or branched chain C.sub.1-6 alkyl group optionally substituted by one or two hydroxyl and/or one or two straight or branched chain C.sub.1-4 alkoxy group(s); or a C.sub.4-7 cycloalkyl group; orR.sup.3 and R.sup.4 together with the nitrogen atom, to which they are attached form a 4 to 8-membered cyclic group of formula ##STR2## optionally substituted by one or two straight or branched chain C.sub.1-4 alkoxy and/or one or two straight or branched chain C.sub.1-4 alkyl group(s), where optionally an oxygen or sulfur atom or an N-R.sup.5 group may be substituted for a ring carbon atom, where R.sup.5 means hydrogen or a straight or branched chain C.sub.1-6 aliphatic alkyl group, the 4- to 8-membered cycle optionally being condensed with a benzene ring;R.sup.6 stands for hydrogen or a C.sub.1-10 acyl group and the salts and hydrates thereof as well as pharmaceutical compositions containing these compounds.The compounds of the invention antagonize the effects of constrictive mediators, e.g. histamine, acetylcholine or serotonin; they show an antiallergic action and possess an antiinflammatory effect. Thus, these compounds can therapeutically be used as bronchodilators as well as antiallergic or antiinflammatory drugs, particularly in the treatment of bronchial asthma.

10. 发明授权

US4163786A Thiazoloisoquinolines with coronary and respiratory effects 失效
标题翻译：具有冠状动脉和呼吸道作用的噻唑并喹啉
公开(公告)号：US4163786A
公开(公告)日：1979-08-07
申请号：US869791
申请日：1978-01-16
申请人： Kalman Harsanyi , Kalman Takacs , Pal Kiss , Laszlo Szekeres , Gyula Papp , Eva Benedek
发明人： Kalman Harsanyi , Kalman Takacs , Pal Kiss , Laszlo Szekeres , Gyula Papp , Eva Benedek
IPC分类号： C07D513/04 , A61K31/47
CPC分类号： C07D513/04
摘要： The invention relates to new thiazoloisoquinolines of the formula (I), or pharmaceutically acceptable salts thereof, ##STR1## wherein R.sup.1 is hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.2 is hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.3 is hydrogen, cyano, alkyl, aryl, nitro, carboxy, carboalkoxy or carboxamido, andY is oxygen, sulfur, or a group of the formula .dbd.N--R.sup.4, wherein R.sup.4 stands for hydrogen, alkyl, aryl, acyl, alkyl-sulfonyl or arysulfonyl.These new compounds can be used in practice as heart medicines or respiratory analeptics.
摘要翻译：本发明涉及式（I）的新型噻唑并喹啉或其药学上可接受的盐，其中R 1是氢，羟基，烷氧基或芳烷氧基，R 2是氢，羟基，烷氧基或芳烷氧基，R 3是氢，氰基，烷基，芳基，硝基，羧基，烷氧基或甲酰胺基，Y是氧，硫或式= N-R4的基团，其中R4代表氢，烷基，芳基，酰基，烷基磺酰基或芳磺酰基。

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