Cycloalkano(1,2-B) indole-sulponamides
    6.
    发明授权
    Cycloalkano(1,2-B) indole-sulponamides 失效
    环咯烷(1,2-B)吲哚磺胺

    公开(公告)号:US4988820A

    公开(公告)日:1991-01-29

    申请号:US556592

    申请日:1990-07-20

    摘要: Cycloalkano[1,2-b]indole-sulphonamides of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, trifluoromethyl, carboxyl or alkoxycarbonyl, represents a group of the formula --S(O).sub.m R.sup.3, in which R.sup.3 denotes alkyl or aryl, and m denotes one of the numbers 0, 1 or 2, represents a group of the formula ##STR2## in which R.sup.4 and R.sup.5 are identical or different and represent hydrogen, alkyl, aryl, aralkyl or acetyl, represents a group of the formula --OR.sup.6, in which R.sup.6 denotes hydrogen, alkyl, aryl, aralkyl, alkyl-SO.sub.2 --, aryl--SO.sub.2 --, aralkyl--SO.sub.2 -- or trifluoromethyl, or represents alkyl, alkenyl or cycloalkyl, each of which is optionally substituted by carboxyl, alkoxycarbonyl, halogen, hydroxyl, alkoxy, alkylthio or cyano, R.sup.2 represents aryl which is optionally substituted up to 5 times by halogen, cyano, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, alkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxy, alkylthio, hydroxyl, carboxyl, alkoxycarbonyl, phenyl, phenoxy, benzyloxy, benzylthio or a group of the formula ##STR3## in which R.sup.4 and R.sup.5 have the abovementioned meaning, x represents the number 1, 2 or 3, and y represents the number 0 or 1, where appropriate in an isomeric form, and their salts are disclosed. These compounds are useful to inhibit platelet aggregation and to antagonize thromboxane A.sub.2.

    摘要翻译: 其中R 1表示氢,卤素,三氟甲基,羧基或烷氧基羰基的式[IMAGE]的环烷基[1,2-b]吲哚磺酰胺代表式-S(O)m R 3的基团,其中R 3表示烷基或 芳基,m表示数字0,1或2中的一个,表示其中R 4和R 5相同或不同并且表示氢,烷基,芳基,芳烷基或乙酰基的式“IMAGE”的基团,表示 其中R 6表示氢,烷基,芳基,芳烷基,烷基-SO 2 - ,芳基-SO 2 - ,芳烷基-SO 2 - 或三氟甲基,或表示烷基,烯基或环烷基,其各自任选被羧基, 氰基,三氟甲基,三氟甲氧基,三氟甲硫基,烷基,羧基烷基,烷氧基羰基烷基,烷氧基,烷硫基,羟基,羧基,烷氧基羰基,烷氧基羰基,烷硫基, 苯基,苯氧基,苄氧基,苄硫基 或其中R 4和R 5具有上述含义的式“IMAGE”的基团,x表示数字1,2或3,并且y代表数字0或1,其中适当的是异构体形式,并且其公开的盐 。 这些化合物可用于抑制血小板聚集和拮抗血栓素A2。

    Indolylpropionic acids, compositions of, and use thereof to inhibit
thrombocyte aggregation
    7.
    发明授权
    Indolylpropionic acids, compositions of, and use thereof to inhibit thrombocyte aggregation 失效
    吲哚丙酸,其组合物及其用途,用于抑制血小板聚集

    公开(公告)号:US4843091A

    公开(公告)日:1989-06-27

    申请号:US58489

    申请日:1987-06-05

    摘要: An N-sulphonamidoethyl-indole of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl, alkoxy, alkylthio, halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, difluoromethoxy, aryl, arylthio, aralkyl, aralkoxy, aralkylthio, acyl or a group of the formula ##STR2## in which R.sup.5 and R.sup.6 are identical or different and denote hydrogen, alkyl, aryl, aralkyl or acyl, andR.sup.3 represents hydrogen, alkyl, aryl, pyridyl, thienyl or furyl, andR.sup.4 represents hydrogen, alkyl, alkoxy, alkylthio, halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, aryl, aryloxy, arylthio, aralkyl, aralkoxy, aralkylthio, acl or a group of the formula ##STR3## in which R.sup.7 and R.sup.8 are identical or different and denote hydrogen, alkyl, aryl, aralkyl or acyl,R.sup.5 represents hydrogen, ##STR4## or a pharmacologically acceptable salt of ##STR5## and R.sup.2 represents hydrogen, alkyl or aryl.The compounds were R.sup.5 is ##STR6## or a salt thereof inhibit the aggregation of thrombocytes.

    摘要翻译: 其中R 1表示氢,烷基,烷氧基,烷硫基,卤素,三氟甲基,三氟甲氧基,三氟甲硫基,二氟甲氧基,芳基,芳硫基,芳烷基,芳烷氧基,芳烷硫基,酰基或一组基团的N-磺酰氨基乙基 - 吲哚 式中,R 5和R 6相同或不同,表示氢,烷基,芳基,芳烷基或酰基,R 3表示氢,烷基,芳基,吡啶基,噻吩基或呋喃基,R 4表示氢,烷基,烷氧基,烷硫基 卤素,三氟甲基,三氟甲氧基,三氟甲硫基,芳基,芳氧基,芳硫基,芳烷基,芳烷氧基,芳烷硫基,acl或其中R 7和R 8相同或不同并表示氢,烷基,芳基,芳烷基或 酰基,R 5表示氢,或者是IMA IMA的药理学上可接受的盐,R 2表示氢,烷基或芳基。 化合物是R5是抑制凝血细胞聚集的盐或其盐。

    N-dihydroindolylethyl-sulphonamides
    9.
    发明授权
    N-dihydroindolylethyl-sulphonamides 失效
    N-二氢吲哚基乙基磺酰胺

    公开(公告)号:US4806551A

    公开(公告)日:1989-02-21

    申请号:US39395

    申请日:1987-04-16

    CPC分类号: C07D209/16

    摘要: New N-dihydroindolylethyl-sulphonamides are prepared from the corresponding N-indolylethyl-sulphonamides by oxidation or hydrogenation and are useful as active compounds in medicaments. These compounds exhibit a platelet aggregation-inhibiting and thromboxan A.sub.2 -antagonistic action.The N-dihydroindolylethyl-sulphonamides have the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, trifluoromethyl, carboxyl or alkoxycarbonyl, or represents a group of the formula --S(O).sub.m R.sup.5,whereinR.sup.5 denotes alkyl or aryl andm denotes one of the numbers 0, 1 or 2, orR.sup.1 represents a group of the formula ##STR2## or R.sup.1 represents a group of the formula --OR.sup.8, orR.sup.1 represents optionally substituted alkyl, alkenyl or cycloalkyl,R.sup.2 represents aryl, which is optionally substituted by up to 5 substituents,R.sup.3 represents hydrogenor alkyl andR.sup.4 represents hydrogen, orR.sup.3 and R.sup.4 together bond a carbonyl oxygen.

    摘要翻译: 通过氧化或氢化由相应的N-吲哚基乙基磺酰胺制备新的N-二氢吲哚基乙基磺酰胺,并且可用作药物中的活性化合物。 这些化合物表现出血小板聚集抑制和血栓素A2拮抗作用。 N-二氢吲哚基乙基磺酰胺具有式“IMAGE”,其中R 1表示氢,卤素,三氟甲基,羧基或烷氧基羰基,或表示式-S(O)m R 5的基团,其中R 5表示烷基或芳基,m表示一个 数字0,1或2,或者R1表示式“IMAGE”或R1表示式-OR8的基团,或R1表示任选取代的烷基,烯基或环烷基,R 2表示芳基,其任选被取代 最多5个取代基,R 3表示氢或烷基,R 4表示氢,或者R 3和R 4一起键合羰基氧。

    Novel norbornane- and norbornene-carboxylic acid amides thromboxan
antagonists
    10.
    发明授权
    Novel norbornane- and norbornene-carboxylic acid amides thromboxan antagonists 失效
    新型降冰片烷和降冰片烯 - 羧酸酰胺血栓素拮抗剂

    公开(公告)号:US4622339A

    公开(公告)日:1986-11-11

    申请号:US691088

    申请日:1985-01-11

    CPC分类号: C07C59/46

    摘要: Norbornane- and norbornene-carboxylic acid amides of the formula ##STR1## in which ##STR2## represents the part structure ##STR3## A represents a ##STR4## or --CH.sub.2 --CH.sub.2 -- group, R.sup.1 and R.sup.2 each independently is hydrogen or an alkyl radical with 1-6 carbon atoms,R.sup.3 is alkyl or alkenyl which has 1-8 carbon atoms and is optionally substituted by halogen or alkyl with 1 or 2 carbon atoms, cycloalkyl or cycloalkeny wtih 3 to 7 carbon atoms, an aromatic radical which has 6 or 10 carbon atoms and and is optionally substituted by halogen, by alkyl with 1 or 2 carbon atoms or by halogenoalkyl with 1 or 2 carbon atoms, or is a five-membered or six-membered heteroaromatic radical,R.sup.4 is hydrogen or a hydroxyl group,R.sup.5 and R.sup.6 each independently is hydrogen or alkyl with 1 to 4 carbon atoms, andn is a number from 2 to 6,and, if R.sup.1 is hydrogen, also physiologically acceptable salts thereof, perform as thromboxan antagonists.

    摘要翻译: 其中代表部分结构的降冰片烯 - 和降冰片烯 - 羧酸酰胺代表“IMAGE”或-CH 2 -CH 2 - 基团,R 1和R 2各自独立地是氢或烷基 具有1-6个碳原子的基团,R3是具有1-8个碳原子并且任选地被卤素或具有1或2个碳原子的烷基取代的烷基或烯基,具有3至7个碳原子的环烷基或环烯基,具有 6或10个碳原子,并且任选被卤素,具有1或2个碳原子的烷基或具有1或2个碳原子的卤代烷基取代,或者是五元或六元杂芳族基团,R 4是氢或羟基 基团,R 5和R 6各自独立地是氢或具有1至4个碳原子的烷基,n是2至6的数,并且如果R 1是氢,则其生理上可接受的盐也作为血栓素拮抗剂进行。