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    Cycloaliphatic prostaglandin analogues
    3.
    发明授权
    Cycloaliphatic prostaglandin analogues 失效
    环脂类前列腺素类似物

    公开(公告)号：US4341789A

    公开(公告)日：1982-07-27

    申请号：US962057

    申请日：1978-11-20

    Applicant: Frederick Cassidy ,  Gordon Wootton

    Inventor： Frederick Cassidy ,  Gordon Wootton

    IPC: C07D207/27 ,  A61K31/40 ,  A61K31/4015 ,  A61P43/00 ,  C07C405/00 ,  C07D207/26 ,  C07D207/273 ,  C07D207/38

    CPC classification number: C07D207/273 ,  C07C405/00 ,  C07D207/38 ,  Y10S514/822 ,  Y10S514/826 ,  Y10S514/878

    Abstract: Compounds of formula (I): ##STR1## wherein: m is 1 or 2; n is 4 to 8; X is CO, protected CO, or CROH wherein R is hydrogen or C.sub.1-4 alkyl and wherein the OH moiety may be protected; R.sub.1 is hydrogen or CO.sub.2 R.sub.1 represents an ester group in which the R.sub.1 moiety contains from 1 to 12 carbon atoms; R.sub.3 is hydroxy, or protected hydroxy; R.sub.2 and R.sub.4 are separately hydrogen, C.sub.1-9 alkyl, C.sub.5-8 cycloalkyl, C.sub.5-8 cycloalkyl-C.sub.1-6 alkyl, phenyl, phenyl C.sub.1-6 alkyl, naphthyl, naphthyl C.sub.1-6 alkyl, any of which phenyl or naphthyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or nitro groups; or R.sub.2 and R.sub.4 taken with the carbon atom to which they are joined represent a C.sub.5-8 cycloalkyl group; and salts thereof; except that when one of R.sub.2 and R.sub.4 is hydrogen or C.sub.1-4 alkyl then the other of R.sub.2 and R.sub.4 cannot be hydrogen or C.sub.1-9 alkyl; have useful pharmacological properties including antigastric secretion, bronchodilator and platelet aggregration inhibition activities.

    Abstract translation: 式（I）化合物：其中：m为1或2; n为4至8; X是CO，保护的CO或CROH，其中R是氢或C 1-4烷基，并且其中OH部分可以被保护; R 1是氢或CO 2 R 1表示其中R 1部分含有1至12个碳原子的酯基; R3是羟基或被保护的羟基; R2和R4分别是氢，C1-9烷基，C5-8环烷基，C5-8环烷基C1-6烷基，苯基，苯基C1-6烷基，萘基，萘基C1-6烷基，其中任何苯基或萘基部分 可以被一个或多个卤素，三氟甲基，C 1-6烷基，C 1-6烷氧基或硝基取代; 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; 及其盐; 除了当R 2和R 4中的一个是氢或C 1-4烷基时，R 2和R 4中的另一个不能是氢或C 1-19烷基; 具有抗胃分泌，支气管扩张剂和血小板聚集抑制活性等有用的药理学特性。

    Oxy-alkylamino carboxylic esters
    4.
    发明授权
    Oxy-alkylamino carboxylic esters 失效
    氧基 - 烷基氨基羧酸酯

    公开(公告)号：US4299970A

    公开(公告)日：1981-11-10

    申请号：US181432

    申请日：1980-08-25

    Applicant: Frederick Cassidy ,  Gordon Wootton

    Inventor： Frederick Cassidy ,  Gordon Wootton

    IPC: C07D223/10 ,  C07C405/00 ,  C07D207/26 ,  C07D207/27 ,  C07D207/36 ,  C07D211/42 ,  C07D211/74 ,  C07D211/86 ,  C07D211/90 ,  C07D491/10 ,  C07C101/20

    CPC classification number: C07D207/26 ,  C07C405/00 ,  C07D207/36 ,  C07D211/42 ,  C07D211/74 ,  C07D211/86 ,  C07D491/10

    Abstract: Compounds of formula (I): ##STR1## wherein: X is CO, protected CO, CROH in which R is hydrogen or C.sub.1-4 alkyl and in which the OH moiety may be protected;Y is CH.sub.2 CH.sub.2 or CH.dbd.CH;Z is CO or CH.sub.2 ;n is 1 to 8;m is 1, 2 or 3;R.sub.1 is hydrogen, CH.sub.2 OH, CH.sub.2 OH in which the OH moiety is protected, CO.sub.2 W wherein W is hydrogen or CO.sub.2 W represents an ester group in which the ester moiety contains from 1 to 12 carbon atoms, or CONH.sub.2 ;R.sub.2 is hydrogen, C.sub.1-4 alkyl, or taken together with R.sub.3 and the carbon atom to which it is attached represents a carbonyl group;R.sub.3 is hydrogen, hydroxy or protected hydroxy;R.sub.4 is hydrogen or C.sub.1-9 alkyl;and salts thereof--have useful pharmacological properties.

    Abstract translation: 式（I）化合物：其中：X为CO，保护的CO，CROH，其中R为氢或C1-4烷基，其中OH部分可被保护; Y是CH 2 CH 2或CH = CH; Z是CO或CH 2; n为1至8; m为1,2或3; R1是其中OH部分被保护的氢，CH 2 OH，CH 2 OH，其中W是氢的CO 2 W或CO 2 W表示酯部分含有1至12个碳原子的酯基或CONH 2; R 2是氢，C 1-4烷基，或与R 3一起并且与它相连的碳原子代表羰基; R3是氢，羟基或被保护的羟基; R 4是氢或C 1-8烷基; 及其盐具有有用的药理学性质。

    Aromatic prostaglandin analogues
    6.
    发明授权
    Aromatic prostaglandin analogues 失效
    芳香族前列腺素类似物

    公开(公告)号：US4177283A

    公开(公告)日：1979-12-04

    申请号：US903143

    申请日：1978-05-05

    Applicant: Frederick Cassidy ,  Gordon Wootton

    Inventor： Frederick Cassidy ,  Gordon Wootton

    IPC: C07C405/00 ,  C07D207/26 ,  C07D207/273 ,  C07D207/38 ,  A61K31/40

    CPC classification number: C07D207/273 ,  C07C405/00 ,  C07D207/38

    Abstract: Compounds of formula (I): ##STR1## wherein: m is 1 or 2; n is 4 to 8; X is CO, protected CO, or CROH wherein R is hydrogen or C.sub.1-4 alkyl and wherein the OH moiety may be protected; R.sub.1 is hydrogen or CO.sub.2 R.sub.1 represents an ester group in which the R.sub.1 moiety contains from 1 to 12 carbon atoms; R.sub.3 is hydroxy, or protected hydroxy; R.sub.2 and R.sub.4 are separately hydrogen, C.sub.1-9 alkyl, C.sub.5-8 cycloalkyl, C.sub.5-8 cycloalkyl-C.sub.1-6 alkyl, phenyl, phenyl C.sub.1-6 alkyl, naphthyl, naphthyl C.sub.1-6 alkyl, any of which phenyl or naphthyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or nitro groups; or R.sub.2 and R.sub.4 taken with the carbon atom to which they are joined represent a C.sub.5-8 cycloalkyl group; and salts thereof; except that when one of R.sub.2 and R.sub.4 is hydrogen or C.sub.1-4 alkyl then the other of R.sub.2 and R.sub.4 cannot be hydrogen or C.sub.1-9 alkyl; have useful pharmacological properties including anti-gastric secretion, bronchodilator and platelet aggregation inhibition activities.

    Abstract translation: 式（I）化合物：其中：m为1或2; n为4至8; X是CO，保护的CO或CROH，其中R是氢或C 1-4烷基，其中OH部分可以被保护; R 1是氢或CO 2 R 1表示其中R 1部分含有1至12个碳原子的酯基; R3是羟基或被保护的羟基; R2和R4分别是氢，C1-9烷基，C5-8环烷基，C5-8环烷基C1-6烷基，苯基，苯基C1-6烷基，萘基，萘基C1-6烷基，其中任何苯基或萘基部分 可以被一个或多个卤素，三氟甲基，C 1-6烷基，C 1-6烷氧基或硝基取代; 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; 及其盐; 除了当R 2和R 4中的一个是氢或C 1-4烷基时，R 2和R 4中的另一个不能是氢或C 1-19烷基; 具有抗胃分泌，支气管扩张剂和血小板聚集抑制活性等有用的药理学特性。

    Pharmaceutically active compounds, preparation thereof, intermediates useful in such preparation and compositions containing the compounds
    7.
    发明授权
    Pharmaceutically active compounds, preparation thereof, intermediates useful in such preparation and compositions containing the compounds 失效
    药物活性化合物，其制备，可用于这种制备的中间体和含有该化合物的组合物

    公开(公告)号：US4156730A

    公开(公告)日：1979-05-29

    申请号：US796701

    申请日：1977-05-13

    Applicant: Richard W. Moore ,  Frederick Cassidy ,  Gordon Wootton

    Inventor： Richard W. Moore ,  Frederick Cassidy ,  Gordon Wootton

    IPC: C07D207/27 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/495 ,  A61P43/00 ,  C07D207/26 ,  C07D207/273 ,  C07D207/36 ,  C07D211/76 ,  C07D317/28 ,  C07D317/30 ,  C07F7/18 ,  C07D207/32 ,  C07D207/20

    CPC classification number: C07D207/273 ,  C07D207/36 ,  C07D317/28 ,  C07D317/30 ,  C07F7/1852

    Abstract: A compound of formula (I): ##STR1## wherein: M IS 0 OR 1;N is 4 to 8;A is hydrogen, and when m is 0 and R.sub.5 is methyl it may also be methyl or a group CO.sub.2 B wherein B is hydrogen or CO.sub.2 B represents an ester group in which the B moiety contains from 1 to 12 carbon atoms;X is CO, protected CO, CROH in which R is hydrogen or C.sub.1-4 alkyl and in which the OH moiety may be protected; R.sub.1 is hydrogen, or CO.sub.2 R.sub.1 represents an ester group in which the R.sub.1 moiety contains 1 to 12 carbon atoms;R.sub.4 is hydrogen, C.sub.1-9 alkyl, C.sub.5-8 cycloalkyl, C.sub.5-8 cycloalkyl-C.sub.1-6 alkyl, phenyl, phenyl C.sub.1-6 alkyl, naphthyl, naphthyl C.sub.1-6 alkyl, any of which phenyl or naphthyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, or nitro groups;D is a group --CH.sub.2 --CH(R.sub.6)--CH(R.sub.7)--C(R.sub.2)(R.sub.3)--, a group--CH.sub.2 --CH(R.sub.6)--CH(R.sub.7)--CH(R.sub.8)--C(R.sub.2)(R.sub.3)--, a group--CH.sub.2 --CH(R.sub.6)--CH(R.sub.7)--CH(R.sub.8)--CH(R.sub.8.sup.1)--C(R.sub.2)(R.sub.3)-- or a group--CH.sub.2 --C(R.sub.10)(R.sub.3)--wherein R.sub.2 is hydrogen, C.sub.1-4 alkyl or phenyl;R.sub.3 is hydroxy or protected hydroxy; R.sub.6, R.sub.7, R.sub.8 andR.sub.8.sup.1 are hydrogen, C.sub.1-4 alkyl or phenyl; and R.sub.10 is hydrogen, C.sub.1-4 alkyl or phenyl; andR.sub.5 is hydrogen, and when m is 0 it may also be methyl; and salts thereof; have a range of pharmacological activities similar to those shown by the natural prostaglandins, but these activities tend to be rather more selective.

    Abstract translation: 式（I）的化合物：其中：

    2,4 Pyrrolidinediones
    8.
    发明授权
    2,4 Pyrrolidinediones 失效
    2,4吡咯烷二酮

    公开(公告)号：US4138407A

    公开(公告)日：1979-02-06

    申请号：US732726

    申请日：1976-10-15

    Applicant: Frederick Cassidy ,  Gordon Wootton

    Inventor： Frederick Cassidy ,  Gordon Wootton

    IPC: C07D207/27 ,  A61K31/40 ,  A61K31/4015 ,  A61P43/00 ,  C07C405/00 ,  C07D207/26 ,  C07D207/273 ,  C07D207/38 ,  C07D207/40

    CPC classification number: C07D207/273 ,  C07C405/00 ,  C07D207/38 ,  Y10S514/822 ,  Y10S514/826 ,  Y10S514/878

    Abstract: Compounds of formula (I): ##STR1## wherein: m is 1 or 2; n is 4 to 8; X is CO, protected CO, or CROH wherein R is hydrogen or C.sub.1-4 alkyl and wherein the OH moiety may be protected; R.sub.1 is hydrogen or CO.sub.2 R.sub.1 represents an ester group in which the R.sub.1 moiety contains from 1 to 12 carbon atoms; R.sub.3 is hydroxy, or protected hydroxy; R.sub.2 and R.sub.4 are separately hydrogen, C.sub.1-9 alkyl, C.sub.5-8 cycloalkyl, C.sub.5-8 cycloalkyl-C.sub.1-6 alkyl, phenyl, phenyl C.sub.1-6 alkyl, naphthyl, naphthyl C.sub.1-6 alkyl, any of which phenyl or naphthyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or nitro groups; or R.sub.2 and R.sub.4 taken with the carbon atom to which they are joined represent a C.sub.5-8 cycloalkyl group; and salts thereof; except that when one of R.sub.2 and R.sub.4 is hydrogen or C.sub.1-4 alkyl when the other of R.sub.2 and R.sub.4 cannot be hydrogen or C.sub.1-9 alkyl; have useful pharmacological properties including antigastric secretion, bronchodilator and platelet aggregation inhibition activities.

    Abstract translation: 式（I）化合物：其中：m为1或2; n为4至8; X是CO，保护的CO或CROH，其中R是氢或C 1-4烷基，并且其中OH部分可以被保护; R 1是氢或CO 2 R 1表示其中R 1部分含有1至12个碳原子的酯基; R3是羟基或被保护的羟基; R2和R4分别是氢，C1-9烷基，C5-8环烷基，C5-8环烷基C1-6烷基，苯基，苯基C1-6烷基，萘基，萘基C1-6烷基，其中任何苯基或萘基部分 可以被一个或多个卤素，三氟甲基，C 1-6烷基，C 1-6烷氧基或硝基取代; 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; 及其盐; 当R 2和R 4中的另一个不能为氢或C 1-19烷基时，R 2和R 4之一为氢或C 1-4烷基; 具有抗胃分泌，支气管扩张剂和血小板聚集抑制活性等有用的药理学特性。

    Active compounds
    9.
    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。

    Anti-hypertensive chromanol derivatives
    10.
    发明授权
    Anti-hypertensive chromanol derivatives 失效

    公开(公告)号：US4575511A

    公开(公告)日：1986-03-11

    申请号：US610626

    申请日：1984-05-16

    Applicant: John M. Evans ,  Frederick Cassidy

    Inventor： John M. Evans ,  Frederick Cassidy

    IPC: A61K31/35 ,  A61K31/352 ,  A61P9/12 ,  C07D311/68 ,  C07D311/02

    CPC classification number: C07D311/68

    Abstract: Compounds of formula (I): ##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, C.sub.1-6 alkyl-thiolmethyl, 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 alkoxysulphinylamino, C.sub.1-6 alkoxysulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or 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 one or two C.sub.1-6 alkyl groups or 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.3 and R.sub.4 together are C.sub.2-5 polymethylene;either R.sub.5 is hydrogen, hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy and R.sub.6 is hydrogen or R.sub.5 and R.sub.6 together are a bond;R.sub.7 is selected from the class consisting of C.sub.1-6 alkyl substituted by amino optionally substituted by one or two C.sub.1-6 alkyl groups which may be the same or different; amino optionally substituted by a C.sub.1-6 alkyl or C.sub.1-6 alkenyl group or a C.sub.1-6 alkanoyl group optionally substituted by up to three halo atoms or by a phenyl group optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen; or C.sub.1-6 alkoxy, or phenoxy optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen; or, when X is oxygen, R.sub.7 is further selected from the class of carboxy, C.sub.1-6 alkoxycarbonyl, or aminocarbonyl optionally substituted by one or two C.sub.1-6 alkyl groups which may be the same or different;R.sub.8 is hydrogen or C.sub.1-6 alkyl; andX is oxygen or sulphur;the R.sub.8 --N--CX--R.sub.7 group being trans to the R.sub.5 group when R.sub.5 and R.sub.6 together are not a bond;or when the compound of formula (I) contains a salifiable group, pharmaceutically acceptable salts thereof, having pharmacological activity, a process for preparing them, pharmaceutical compositions containing them, and their use in the treatment of mammals.

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