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17 条记录 (耗时 0.077 秒)

    Sulfur-containing isoquinoline derivatives in pharmaceutical compositions and methods of use
    11.
    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。

    Derivatives of bicyclic lactols
    12.
    发明授权
    Derivatives of bicyclic lactols 失效
    双环乳糖的衍生物

    公开(公告)号：US4257962A

    公开(公告)日：1981-03-24

    申请号：US942819

    申请日：1978-09-15

    申请人： Tibor Szabo ,  Laszlo Institoris ,  Gabor Kovacs ,  Gyula Dalmadi ,  Bela Koszegi ,  Istvan Stadler

    发明人： Tibor Szabo ,  Laszlo Institoris ,  Gabor Kovacs ,  Gyula Dalmadi ,  Bela Koszegi ,  Istvan Stadler

    IPC分类号： C07C405/00 ,  A61K31/34 ,  A61K31/343 ,  A61P7/02 ,  A61P25/02 ,  A61P35/00 ,  C07D307/935

    CPC分类号： C07D307/935

    摘要： Racemic or optically active compounds with antitumor activity of the formula: ##STR1## wherein X is oxygen or sulfur;R.sup.1 is hydrogen, C.sub.1 to C.sub.4 alkanoyl, benzoyl or phenyl-substituted benzoyl;R.sup.2 is hydrogen or C.sub.1 to C.sub.4 alkanoyl;R.sup.3 is C.sub.2 to C.sub.40 straight or branched chain alkyl substituted by hydroxy, epoxy, amino, C.sub.1 to C.sub.6 alkylamino, C.sub.1 to C.sub.6 dialkylamino, C.sub.1 to C.sub.6 alkanoyloxy or, C.sub.1 to C.sub.4 alkoxycarbonyl; cyclohexyl, phenyl unsubstituted or substituted by halogen, amino, C.sub.1 to C.sub.4 alkyl-substituted amino, C.sub.1 to C.sub.4 alkoxy, nitro, or hydroxy; C.sub.1 to C.sub.6 alkanoyl; allyl or phenyl-C.sub.1 to C.sub.4 alkyl unsubstituted or substituted by a C.sub.2 to C.sub.6 alkene group; or where X is sulfur R.sup.3 is as defined above or is C.sub.1 to C.sub.40 straight or branched chain alkyl; and.about. represents the exo- or endo-steric position in the ring and indicates an .alpha.- or .beta.-steric position in the side chain are disclosed.

    摘要翻译： 具有下式的抗肿瘤活性的外消旋或光学活性化合物：其中X是氧或硫; R1是氢，C1至C4烷酰基，苯甲酰基或苯基取代的苯甲酰基; R2是氢或C1-C4烷酰基; R3为C2至C40被羟基，环氧基，氨基，C1至C6烷基氨基，C1至C6二烷基氨基，C1至C6烷酰氧基或C1至C4烷氧基羰基取代的直链或支链烷基; 环己基，未取代或被卤素取代的苯基，氨基，C1至C4烷基取代的氨基，C1至C4烷氧基，硝基或羟基; C1至C6烷酰基; 烯丙基或未被取代或被C2至C6烯基取代的苯基-C1至C4烷基; 或其中X为硫的R 3如上所定义或为C 1至C 40直链或支链烷基; 而DIFFERENCE表示环中的外 - 或内 - 立体位置，并且表示侧链中的α或β-甾族位置。

    7-Oxo-PGI.sub.2 -derivatives and process for the preparation thereof and pharmaceutical compositions containing same
    14.
    发明授权
    7-Oxo-PGI.sub.2 -derivatives and process for the preparation thereof and pharmaceutical compositions containing same 失效
    7-氧代-PGI2-衍生物及其制备方法和含有它们的药物组合物

    公开(公告)号：US4330553A

    公开(公告)日：1982-05-18

    申请号：US205292

    申请日：1980-11-10

    申请人： Vilmos Simonidesz ,  Agnes Papp nee Behr ,  Gabor Kovacs ,  Jozsef Ivanics ,  Julia Der nee Foldvary ,  Istvan Stadler ,  Istvan Pallagi

    发明人： Vilmos Simonidesz ,  Agnes Papp nee Behr ,  Gabor Kovacs ,  Jozsef Ivanics ,  Julia Der nee Foldvary ,  Istvan Stadler ,  Istvan Pallagi

    IPC分类号： C07D307/937 ,  A61K31/34 ,  A61K31/557 ,  C07D307/935

    CPC分类号： C07D307/937

    摘要： New PGI.sub.2 derivatives and a process for their preparation are disclosed of the formula (I) ##STR1## wherein Q is hydrogen, a pharmacologically acceptable cation, or lower alkyl;A is cis or trans --CH.dbd.CH--, --C.tbd.C--, or --CH.sub.2 --CH.sub.2 --;R.sup.13 is hydrogen or a C.sub.1 to C.sub.4 alkanoyl or is a blockinggroup of the formula R.sup.7 R.sup.8 R.sup.9 Si or ##STR2## wherein R.sup.7, R.sup.8 and R.sup.9 are the same or different and can be straight or branched chain alkyl groups having 1 to 4 carbon atoms and R.sup.10 and R.sup.11 are the same or different and can be hydrogen or methyl, and R.sup.12 represents methyl or ethyl, or is tetrahydropyran-2-yl;R.sup.4 is hydrogen or lower alkyl inthe .alpha. or .beta. steric position;R.sup.1 and R.sup.2 are each hydrogen or lower alkyl;Y is methylene, oxygen or an --NH-- group; andR.sup.3 is lower alkyl or phenyl which can be monosubstituted phenyl. The compounds are useful as antiaggregation or thrombus-dissolving agents, stomach juice secretion inhibiting agents and antiasthmatic agents.

    摘要翻译： 公开了新的PGI 2衍生物及其制备方法，式（I）其中Q为氢，药理学可接受的阳离子或低级烷基; A是顺式或反式-CH = CH - ， - C 3BOND C - 或-CH 2 -CH 2 - ; R 13是氢或C 1至C 4烷酰基或是式R 7 R 8 R 9 Si或其中R 7，R 8和R 9相同或不同并且可以是具有1至4个碳原子的直链或支链烷基和R 10和 R 11相同或不同，可以是氢或甲基，R 12表示甲基或乙基，或是四氢吡喃-2-基; R4是氢或在α或β位置的低级烷基; R1和R2各自为氢或低级烷基; Y是亚甲基，氧或-NH-基团; 并且R 3是可以是单取代的苯基的低级烷基或苯基。 该化合物可用作抗凝聚剂或血栓溶解剂，胃液分泌抑制剂和抗哮喘剂。