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20 条记录 (耗时 0.027 秒)

    1,2,4-Oxadiazine derivatives, process for their preparation and pharmaceutical compositions containing them
    3.
    发明授权
    1,2,4-Oxadiazine derivatives, process for their preparation and pharmaceutical compositions containing them 失效
    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。

    Sulfur-containing isoquinoline derivatives in pharmaceutical compositions and methods of use
    6.
    发明授权
    Sulfur-containing isoquinoline derivatives in pharmaceutical compositions and methods of use 失效
    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。

    Thiazoloisoquinolines with coronary and respiratory effects
    10.
    发明授权
    Thiazoloisoquinolines with coronary and respiratory effects 失效
    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。