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    Sulfur-containing isoquinoline derivatives in pharmaceutical compositions and methods of use
    2.
    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。

    Pharmaceutical compositions containing hydroximic acid derivatives
    10.
    发明授权
    Pharmaceutical compositions containing hydroximic acid derivatives 失效

    公开(公告)号：US06306878B1

    公开(公告)日：2001-10-23

    申请号：US08722499

    申请日：1996-09-27

    申请人： Balazs Sumegi ,  Peter Literati Nagy ,  Laszlo Vigh ,  Bruno Maresca

    发明人： Balazs Sumegi ,  Peter Literati Nagy ,  Laszlo Vigh ,  Bruno Maresca

    IPC分类号： A61K31445

    CPC分类号： A61K31/5395 ,  A61K31/15 ,  A61K31/4545 ,  A61K31/455 ,  A61K31/539

    摘要： The invention refers to pharmaceutical compositions suitable for the protection of the mitochondrial genom and/or mitochondrium from damages or for the treatment of diseases connected with such damages, said compositions comprising a hydroximic acid derivative of the formula: wherein R1 represents a hydrogen or a C1-5 alkyl group, R2 stands for a hydrogen, a C1-5 alkyl group, a C3-8 cycloalkyl group or a phenyl group optionally substituted by a hydroxy or a phenyl group, or R1 or R2 together with the nitrogen atom they are attached to form a 5 to 8 membered ring optionally containing one or more further nitrogen, oxygen or sulfur atom(s) and said ring can be condensed with another alicyclic or heterocyclic ring, preferably a benzene, naphthalene, quinoline, isoquinoline, pyridine or pyrazoline ring, furthermore, if desired and chemically possible, the nitrogen and/or sulfur heteroatom(s) are present in the form of an oxide or dioxide, R3 means a hydrogen, a phenyl group, a naphthyl group or a pyridyl group wherein said groups can be substituted by one or more halo atom(s) or C1-4 alkoxy group(s), Y is a hydrogen, a hydroxy group, a C1-24 alkoxy group optionally substituted by an amino group, a C2-24 polyalkenyl-oxy group containing 1 to 6 double bond(s), a C1-25 alkanoyl group, C3-9 alkenoyl group or a group of the formula R7—COO—, wherein R7 represents a C2-30 polyalkenyl group containing 1 to 6 double bond(s), X stands for a halo, an amino group, a C1-4 alkoxy group, or X forms with B an oxygen atom, or X and Y together with the carbon atoms they are attached to and the —NR—O—CH2 group being between said carbon atoms form a ring of the formula wherein Z represents an oxygen or a nitrogen, R stands for a hydrogen or R forms with B a chemical bond, A is a C1-4 alkylene group or a chemical bond or a group of the formula wherein R4 represents a hydrogen, a C1-5 alkyl group, a C3-8 cycloalkyl group or a phenyl group optionally substituted by a halo, a C1-4 alkoxy group or a C1-5 alkyl group, R5 stands for a hydrogen, a C1-4 alkyl group or a phenyl group, m has a value of 0, 1 or 2, n has a value of 0, 1 or 2, or a pharmaceutically acceptable acid addition salt thereof as the active ingredient.