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    Aryl alkenoic acid derivatives as leukotriene antagonists
    66.
    发明授权
    Aryl alkenoic acid derivatives as leukotriene antagonists 失效
    芳基烯酸衍生物作为白三烯拮抗剂

    公开(公告)号：US5266713A

    公开(公告)日：1993-11-30

    申请号：US928693

    申请日：1992-08-12

    Applicant: Trevor S. Abram ,  Peter Norman ,  Stephen R. Tudhope ,  Harold C. Kluender ,  Robert N. Schut ,  Heinrich Meier ,  Ulrich Rosentreter

    Inventor： Trevor S. Abram ,  Peter Norman ,  Stephen R. Tudhope ,  Harold C. Kluender ,  Robert N. Schut ,  Heinrich Meier ,  Ulrich Rosentreter

    IPC: C07C323/56 ,  C07C323/60 ,  C07C323/62 ,  C07C235/00

    CPC classification number: C07C323/56 ,  C07C323/60 ,  C07C323/62

    Abstract: Aryl alkenoic acid derivatives, and physiologically acceptable salts thereof, are provided which are potent leukotriene antagonists and may be used for the treatment of circulatory diseases and preferably for respiratory diseases such as asthma. The derivatives have a general formula I ##STR1## in which X is --S--,W is CH.dbd.CH;o is 1 to 4;n is 2 to 6;m is 0 to 2;T and Z, same or different, represent oxygen or a direct bond;R.sup.2 and R.sup.3, represent hydrogen, or fluorine;A represents carboxyl, CO.sub.2 R.sub.4.sup.4, wherein R.sup.4 is lower alkylR is ##STR2## wherein Y represents carboxyl, CO.sub.2 R.sup.4, wherein R.sup.4 is lower alkylR.sup.7 and R.sup.8, same or different, represent H or lower alkyl;R.sup.9 represents --OH, --O-alkyl, NH.sub.2 or a NHCH.sub.2 CO.sub.2 H group; andR.sup.10 R3 is H.

    Abstract translation: 提供了芳基链烯酸衍生物及其生理上可接受的盐，它们是有效的白三烯拮抗剂，可用于治疗循环系统疾病，优选用于呼吸系统疾病如哮喘。 衍生物具有通式I（I）其中X是-S-，W是CH = CH; o是1到4; n为2〜6; m为0〜2; T和Z相同或不同，代表氧或直接键; R2和R3代表氢或氟; A表示羧基，CO 2 R 44，其中R 4是低级烷基R 3是其中Y表示羧基，CO 2 R 4，其中R 4是低级烷基，R 7和R 8相同或不同，表示H或低级烷基; R9表示-OH，-O-烷基，NH2或NHCH2CO2H基团; R10 R3为H.

    Cycloalkano(1,2-B) indole-sulponamides
    69.
    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

    Applicant: Horst Boshagen ,  Ulrich Rosentreter ,  Folker Lieb ,  Hermann Oediger ,  Friedel Seuter ,  Elisabeth Perzborn ,  Volker-Bernd Fiedler

    Inventor： Horst Boshagen ,  Ulrich Rosentreter ,  Folker Lieb ,  Hermann Oediger ,  Friedel Seuter ,  Elisabeth Perzborn ,  Volker-Bernd Fiedler

    IPC: C07D209/80 ,  C07D209/86 ,  C07D209/88 ,  C07D491/10

    CPC classification number: C07D209/80 ,  C07D209/86 ,  C07D209/88 ,  C07D491/10

    Abstract: 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.

    Abstract translation: 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
    70.
    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

    Applicant: Ulrich Rosentreter ,  Horst Boshagen ,  Folker Lieb ,  Hermann Oediger ,  Volker-Bernd Fiedler ,  Elisabeth Perzborn ,  Friedel Seuter

    Inventor： Ulrich Rosentreter ,  Horst Boshagen ,  Folker Lieb ,  Hermann Oediger ,  Volker-Bernd Fiedler ,  Elisabeth Perzborn ,  Friedel Seuter

    IPC: A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61P7/02 ,  C07D209/08 ,  C07D209/18 ,  C07D209/24 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04

    CPC classification number: C07D401/04 ,  C07D209/08 ,  C07D209/24 ,  C07D405/04 ,  C07D409/04

    Abstract: 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.

    Abstract translation: 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。

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