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    Active compounds
    2.
    发明授权
    Active compounds 失效
    活性化合物

    公开(公告)号：US4987138A

    公开(公告)日：1991-01-22

    申请号：US231183

    申请日：1988-08-11

    Applicant: Frederick Cassidy ,  Geoffrey Stemp

    Inventor： Frederick Cassidy ,  Geoffrey Stemp

    IPC: C07C49/245 ,  A61K31/165 ,  A61K31/215 ,  A61K31/22 ,  A61K31/265 ,  A61K31/275 ,  A61K31/35 ,  A61K31/352 ,  A61K31/443 ,  A61K31/445 ,  A61K31/47 ,  A61P1/00 ,  A61P9/00 ,  A61P9/12 ,  A61P11/00 ,  A61P25/02 ,  C07C45/00 ,  C07C49/252 ,  C07C49/255 ,  C07C49/83 ,  C07C49/84 ,  C07C67/00 ,  C07C201/00 ,  C07C239/00 ,  C07C301/00 ,  C07C303/26 ,  C07C303/30 ,  C07C303/36 ,  C07C303/40 ,  C07C309/28 ,  C07C313/00 ,  C07C313/04 ,  C07C313/06 ,  C07C317/24 ,  C07C317/46 ,  C07C323/25 ,  C07D215/20 ,  C07D215/48 ,  C07D311/58 ,  C07D405/04

    CPC classification number: C07D405/04 ,  C07D215/48 ,  C07D311/58

    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, 1-mercapto C.sub.2-7 alkyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl(NOH) or --C(C.sub.1-6 alkyl)NNH.sub.2 or, when Y is oxygen, one of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl and the other is methoxy or amino optionally substituted by C.sub.2-7 alkanoyl;one of R.sub.3 and R.sub.4 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.2 and R.sub.3 together are C.sub.2-5 polymethylene;R.sub.5 is hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy;R.sub.6 is hydrogen or C.sub.1-6 alkyl;R.sub.7 is NR.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 are independently C.sub.1-6 alkyl, R.sub.8 is hydrogen and R.sub.9 is C.sub.1-6 alkyl or R.sub.8 and R.sub.9 together are C.sub.4-5 polymethylene; or R.sub.6 and R.sub.8 together are --(CH.sub.2).sub.n --wherein n is 2 or 3, and R.sub.9 is hydrogen or C.sub.1-6 alkyl; or R.sub.7 is CH.sub.2 R.sub.10 wherein R.sub.10 is hydrogen or C.sub.1-5 alkyl optionally substituted by halo, hydroxy or C.sub.1-6 alkoxy; or R.sub.6 and R.sub.10 are ---(CH.sub.2).sub.m -- wherein m is 2 or 3;X is oxygen or sulphur; andY is oxygen, CH.sub.2 or NH;the R.sub.6 --CH--CX--R.sub.7 group being trans to the R.sub.5 group; having blood pressure lowering activity, a process for their preparation and their use as pharmaceuticals.

    Abstract translation: 式（I）化合物及其药学上可接受的盐：其中：R 1和R 2中的任一个是氢，另一个选自C 1-6烷基羰基，C 1-6烷氧基羰基，C 1-6 烷基羰氧基，C 1-6烷基羟甲基，硝基，氰基，氯，三氟甲基，C 1-6烷基亚磺酰基，C 1-6烷基磺酰基，C 1-6烷氧基亚磺酰基，C 1-6烷氧基磺酰基，C 1-6烷基羰基氨基，C 1-6烷氧基羰基氨基，C 1-6烷基 - 硫代羰基，C 1-6烷氧基 - 硫代羰基，C 1-6烷基 - 硫代羰基氧基，1-巯基C 2-7烷基，甲酰基或氨基亚磺酰基，氨基磺酰基或氨基羰基，氨基部分任选被一个或两个C 1-6烷基取代，或C 1 -6烷基亚磺酰氨基，C 1-6烷基磺酰基氨基C 1-6烷氧基亚磺酰基氨基或被C 1-6烷基羰基，硝基或氰基末端取代的C 1-6烷氧基磺酰基氨基或乙烯基，或-C（C 1-6烷基（NOH）或-C ）NNH 2，或者当Y为氧时，R 1和R 2中的一个为硝基，氰基或C 1-3烷基羰基，另一个为I 任选被C 2-7烷酰基取代的羟基或氨基; R3和R4之一是氢或C1-4烷基，另一个是C1-4烷基或R2和R3一起是C2-5聚亚甲基; R5是羟基，C1-6烷氧基或C1-7酰氧基; R6是氢或C1-6烷基; R7是NR8R9，其中R8和R9独立地是C1-6烷基，R8是氢，R9是C1-6烷基或R8和R9一起是C4-5聚亚甲基; 或R 6和R 8一起为 - （CH 2）n - ，其中n为2或3，并且R 9为氢或C 1-6烷基; 或R 7为CH 2 R 10，其中R 10为氢或任选被卤素，羟基或C 1-6烷氧基取代的C 1-5烷基; 或R 6和R 10为 - （CH 2）m - ，其中m为2或3; X是氧或硫; Y是氧，CH 2或NH; R6-CH-CX-R7基团反应到R5基团; 具有降血压活性，其制备方法及其作为药物的用途。

    3,4-dihydro-2H-1-benzopyrans useful as anti-hypertensive agents
    5.
    发明授权
    3,4-dihydro-2H-1-benzopyrans useful as anti-hypertensive agents 失效
    3,4-二氢-2H-1-苯并吡喃可用作抗高血压药

    公开(公告)号：US4782083A

    公开(公告)日：1988-11-01

    申请号：US902428

    申请日：1986-08-29

    Applicant: Frederick Cassidy ,  Geoffrey Stemp ,  John M. Evans

    Inventor： Frederick Cassidy ,  Geoffrey Stemp ,  John M. Evans

    IPC: A61K31/35 ,  A61K31/352 ,  A61P9/12 ,  C07D311/68 ,  C07D311/70 ,  A61K31/40 ,  A61K31/445 ,  C07D405/04

    CPC classification number: C07D311/70 ,  C07D311/68

    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: one of R.sub.1 and R.sub.2 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.1 and R.sub.2 together are C.sub.2-5 -polymethylene;either R.sub.3 is hydrogen, hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy and R.sub.4 is hydrogen or R.sub.3 and R.sub.4 together are a bond;R.sub.5 is hydrogen C.sub.1-6 alkyl optionally substituted by halogen hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, carboxy or amino optionally substituted by one or two independent C.sub.1-6 alkyl groups, or C.sub.2-6 alkenyl, amino optionally substituted by a C.sub.1-6 alkyl or C.sub.1-6 alkenyl group or by a C.sub.1-6 alkanoyl group optionally substituted by up to three halo atoms, by a phenyl group optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen, or aryl or hetroaryl, either being optionally substituted by one or more groups or atoms selected from the class of C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halogen, trifluoromethyl, nitro, cyano, C.sub.1-12 carboxylic acyl, or amino or aminocarbonyl optionally substituted by one or two C.sub.1-6 alkyl groups and R.sub.6 is hydrogen or C.sub.1-6 alkyl, or R.sub.5 and R.sub.6 together are --CH.sub.2 --(CH.sub.2).sub.n --Z--(CH.sub.2).sub.m -- wherein m and n are 0 to 2 such that m+n is 1 or 2 and Z is CH.sub.2, O, S or NR wherein R is hydrogen, C.sub.1-9 alkyl, C.sub.2-7 alkanoyl, phenyl C.sub.1-4 -alkyl, naphthylcarbonyl, phenylcarbonyl or benzylcarbonyl optionally substituted in the phenyl or naphthyl ring by one or two of C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen; mono- or bi-cyclic- heteroarylcarbonyl;X is oxygen or sulphur;Y and Q are electron withdrawing groups; andthe nitrogen-containing group in the 4-position being trans to the R.sub.3 group when R.sub.3 is hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy; having blood pressure lowering activity, a process and intermediates for their preparation and their use as pharmaceuticals.

    Abstract translation: 式（I）化合物及其药学上可接受的盐：其中：R 1和R 2之一为氢或C 1-4烷基，另一个为C 1-4烷基或R 1和R 2一起为C 2-5 - 聚亚甲基 R3是氢，羟基，C1-6烷氧基或C1-7酰氧基，R4是氢或R3和R4一起是一个键; R5是任选被卤素羟基，C 1-6烷氧基，C 1-6烷氧基羰基，羧基或任选被一个或两个独立的C 1-6烷基取代的氨基或C 2-6烯基的任选取代的C 1-6烷基，任选被 C 1-6烷基或C 1-6烯基或被任选被至多三个卤原子取代的C 1-6烷酰基，被任选被C 1-6烷基，C 1-6烷氧基或卤素取代的苯基或芳基或杂芳基 任选被一个或多个选自C 1-6烷基，C 1-6烷氧基，羟基，卤素，三氟甲基，硝基，氰基，C 1-12羧基酰基或氨基或氨基羰基中的一个或多个基团或原子取代，任选地被 一个或两个C 1-6烷基，R 6是氢或C 1-6烷基，或者R 5和R 6一起是-CH 2 - （CH 2）n Z-（CH 2）m - ，其中m和n是0-2，使得m + n 是1或2，Z是CH 2，O，S或NR，其中R是氢，C 1-8烷基，C 2-7烷酰基，苯基C 1-4 - 烷基，萘基羰基，苯基羰基或苄基羰基 任选地在苯基或萘基环中被一个或两个C 1-6烷基，C 1-6烷氧基或卤素取代; 单环或双环杂芳基羰基; X是氧或硫; Y和Q是吸电子基团; 当R3为羟基，C1-6烷氧基或C1-7酰氧基时，4-位的含氮基团反向R3基团; 具有降血压活性，其制备方法和中间体及其作为药物的用途。

    Prostaglandin analogues
    8.
    发明授权
    Prostaglandin analogues 失效
    前列腺素类似物

    公开(公告)号：US4241074A

    公开(公告)日：1980-12-23

    申请号：US48514

    申请日：1979-06-14

    Applicant: Frederick Cassidy ,  Alexander C. Goudie

    Inventor： Frederick Cassidy ,  Alexander C. Goudie

    IPC: A61K31/415 ,  A61K31/4166 ,  A61P43/00 ,  B67C3/26 ,  C07C45/67 ,  C07D233/32 ,  C07D233/70 ,  C07D233/76 ,  C07D233/78 ,  C07D233/86 ,  C07D233/40

    CPC classification number: C07D233/86 ,  C07C45/673 ,  C07D233/32 ,  C07D233/76

    Abstract: A compound of the formula (I): ##STR1## wherein: X is O, S or H;Y is --CH.sub.2 --CH--, --CH.dbd.CH-- or --C.dbd.C--;n is 1 to 7;R.sub.1 is C.sub.1-4 alkyl;R.sub.3 is hydroxy or protected hydroxy;R.sub.4 is C.sub.1-9 alkyl, C.sub.3-8 cycloalkyl or C.sub.3-8 cycloalkyl--C.sub.1-6 alkyl; orR.sub.2 and R.sub.4 taken with the carbon atom to which they are joined represent a C.sub.5-8 cycloalkyl group; andR.sub.5 is hydrogen or C.sub.1-6 alkyl; and salts thereof has useful pharmaceutical activity including bronchodilator activity.

    Abstract translation: 式（I）的化合物：其中：X为O，S或H; Y是-CH 2 -CH-，-CH = CH-或-C = C-; n为1〜7; R1是C1-4烷基; R3是羟基或被保护的羟基; R4是C1-9烷基，C3-8环烷基或C3-8环烷基C1-6烷基; 或与其连接的碳原子取代的R 2和R 4表示C 5-8环烷基; R5是氢或C1-6烷基; 其盐具有有用的药物活性，包括支气管扩张剂活性。

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