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    Heterocyclic derivatives, processes for the use thereof and pharmaceutical compositions containing them
    1.
    发明授权
    Heterocyclic derivatives, processes for the use thereof and pharmaceutical compositions containing them 失效
    杂环衍生物，其使用方法和含有它们的药物组合物

    公开(公告)号：US4777179A

    公开(公告)日：1988-10-11

    申请号：US789578

    申请日：1985-10-21

    申请人： John Bradshaw ,  Duncan B. Judd ,  Barry J. Price ,  John W. Clitherow ,  John W. M. Mackinnon ,  Linda Carey ,  Roger Hayes

    发明人： John Bradshaw ,  Duncan B. Judd ,  Barry J. Price ,  John W. Clitherow ,  John W. M. Mackinnon ,  Linda Carey ,  Roger Hayes

    IPC分类号： C07D249/14 ,  C07D333/20 ,  C07D333/28 ,  C07D333/32 ,  C07D333/34 ,  C07D333/42 ,  A61K31/445 ,  A61K31/41 ,  C07D401/10 ,  C07D403/12 ,  C07D403/14 ,  C07D413/10

    CPC分类号： C07D333/32 ,  C07D333/20 ,  C07D333/28 ,  C07D333/34 ,  C07D333/42

    摘要： The invention provides compounds of the general formula ##STR1## and physiologically acceptable salts and hydrates thereof, in which one of R.sub.1 and R.sub.2 represents hydrogen, halogen or a C.sub.1-4 alkyl group which may be optionally substituted by hydroxy or C.sub.1-4 alkoxy, and the other represents the group R.sub.4 R.sub.5 NAlk-- in which Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms;R.sub.3, which may be in either the 2 or 3-position, represents the ##STR2## where X represents --CH.sub.2 --, --O-- or --S--; n represents zero, 1 or 2;m represents 2, 3 or 4; andR.sub.7 represents hydrogen, alkyl, alkenyl, aralkyl, or C.sub.2-6 alkyl substituted by hydroxy or alkoxy; andR.sub.8 represents hydrogen, alkyl, alkenyl, aralkyl, hydroxyalkyl, acyloxyalkyl, alkoxyalkyl, aryloxyalkyl, aralkyloxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, hydroxy or alkoxy, or the group NR.sub.10 R.sub.11 ; with the provisos thatwhere R.sub.2 represents the group R.sub.4 R.sub.5 Nalk then R.sub.3 is in the 2-position;where R.sub.2 represents hydrogen then R.sub.3 is in the 3-position; andwhere R.sub.2 represents halogen or C.sub.1-4 alkyl optionally substituted by hydroxy or C.sub.1-4 alkoxy, and R.sub.3 is in the 2-position, then R.sub.8 cannot represent amino C.sub.1-6 alkyl, C.sub.1-6 alkylamino C.sub.1-6 alkyl, di-C.sub.1-6 alkylamino C.sub.1-6 alkyl or a group NR.sub.10 R.sub.11.The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -antagonists.

    摘要翻译： 本发明提供了通式（I）的化合物及其生理上可接受的盐和水合物，其中R 1和R 2中的一个表示氢，卤素或C 1-4烷基，其可任选被羟基或C1- 4烷氧基，另一个表示R4R5NAlk-基团，其中Alk表示1至6个碳原子的直链或支链亚烷基链; 可以在2或3位的R3表示其中X表示-CH 2 - ， - O-或-S-的。 n表示0，1或2; m表示2,3或4; 并且R 7表示氢，烷基，烯基，芳烷基或被羟基或烷氧基取代的C 2-6烷基; 芳基烷氧基烷基，芳氧基烷基，芳烷氧基烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基，羟基或烷氧基，或基团NR10R11; R10代表氢，烷基，烯基，芳烷基， 条件是其中R2表示基团R4R5Nalk，则R3为2-位; 其中R2表示氢，R3表示3-位; 并且其中R 2表示卤素或任选被羟基或C 1-4烷氧基取代的C 1-4烷基，且R 3在2-位，那么R 8不能代表氨基C 1-6烷基，C 1-6烷基氨基C 1-6烷基， C 1-6烷基氨基C 1-6烷基或基团NR 10 R 11。 式（I）化合物显示作为选择性组胺H2拮抗剂的药理活性。

    Triazole acylamines, pharmaceutical compositions thereof and method of use thereof
    2.
    发明授权
    Triazole acylamines, pharmaceutical compositions thereof and method of use thereof 失效

    公开(公告)号：US4323566A

    公开(公告)日：1982-04-06

    申请号：US125847

    申请日：1980-02-29

    申请人： John W. Clitherow ,  Barry J. Price ,  John Bradshaw ,  Michael Martin-Smith ,  John W. M. MacKinnon ,  Duncan B. Judd ,  Linda Carey

    发明人： John W. Clitherow ,  Barry J. Price ,  John Bradshaw ,  Michael Martin-Smith ,  John W. M. MacKinnon ,  Duncan B. Judd ,  Linda Carey

    IPC分类号： C07D249/14 ,  C07D295/096 ,  C07D307/52 ,  C07D317/22 ,  C07D333/36 ,  C07D403/12 ,  A61K31/41 ,  C07D403/14

    CPC分类号： C07D295/096 ,  C07D249/14 ,  C07D307/52 ,  C07D317/22 ,  C07D333/36

    摘要： The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichR.sub.1 and R.sub.2, which may be the same of different, each represent hydrogen, C.sub.1 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl, or alkyl substituted by hydroxy, alkoxy, amino alkylamino dialkylamino or cycloalkyl or R.sub.1 and R.sub.2 may together with the nitrogen atom to which they are attached form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C.sub.1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom which is oxygen or sulphur;Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms,Q represents a furan or thiophene ring in which incorporation into the rest of the molecule is through bonds at the 2- and 5- positions, the furan ring optionally bearing a further substituent R.sub.6 adjacent to the group R.sub.1 R.sub.2 N-Alk, or Q represents a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1- and 3- or 1- and 4- positions;R.sub.6 represents halogen or C.sub.1-4 alkyl which may be substituted by hydroxy or C.sub.1-4 alkoxy;x represents --CH.sub.2 --, --O--, --S--or ##STR2## where R.sub.5 represents hydrogen or methyl; n represents zero, 1 or 2;m represents 2, 3 or 4;R.sub.3 represents hydrogen, alkyl, alkenyl, aralkyl, hydroxyalkyl with at least two carbon atoms, alkoxyalkyl, or aryl, andR.sub.4 represents hydrogen, alkyl, alkenyl or aralkyl and R.sub.7 represents the group COR.sub.8 where R.sub.8 represents hydrogen, alkyl, aryl, aralkyl, alkoxy, heteroaryl or monocyclic heteroarylalkyl or R.sub.7 represents the group SO.sub.2 R.sub.9 where R.sub.9 represents alkyl or aryl, or R.sub.7 represents the group ##STR3## where Y is oxygen or sulphur and R.sub.10 represents hydrogen, alkyl, cycloalkyl, aryl or aralkyl.The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 - antagonists.

    Heterocyclic derivatives
    6.
    发明授权
    Heterocyclic derivatives 失效

    公开(公告)号：US4410523A

    公开(公告)日：1983-10-18

    申请号：US199522

    申请日：1980-10-22

    申请人： William D. Ollis ,  Barry J. Price ,  Linda Carey ,  Roger Hayes ,  John W. Clitherow ,  John Bradshaw ,  John W. M. Mackinnon

    发明人： William D. Ollis ,  Barry J. Price ,  Linda Carey ,  Roger Hayes ,  John W. Clitherow ,  John Bradshaw ,  John W. M. Mackinnon

    IPC分类号： C07D249/14 ,  A61K31/395 ,  C07D249/10

    CPC分类号： C07D249/14 ,  Y10S514/927

    摘要： The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichR.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen, C.sub.1-10 alkyl, cycloalkyl, alkenyl, aralkyl, trifluoroalkyl, heteroaralkyl, or alkyl substituted by hydroxy, alkoxy, amino, alkylamino, dialkyamino or cycloalkyl, or R.sub.1 and R.sub.2 may together with the nitrogen atom to which they are attached form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C.sub.1-3 alkyl groups, or a hydroxy group and/or may contain another heteroatom selected from oxygen and sulphur;Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms and is attached to the cyclohexadiene ring at either the 4- or 5- position;X represents --CH.sub.2 or --O--;m represents 2, 3, 4 or 5 and when X is --O-- the chain (CH.sub.2).sub.m may be interrupted by an oxygen atom provided that there are at least two methylene groups between any two heteroatoms in the moiety --X(CH.sub.2).sub.m NH--;R.sub.3 represents hydrogen, alkyl, alkenyl, aralkyl, or C.sub.2-6 alkyl substituted by hydroxy or alkoxy; andR.sub.4 represents hydrogen, alkyl, alkenyl, aralkyl, hydroxyalkyl, acyloxyalkyl, alkoxyalkyl, aryloxyalkyl, aralkyloxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, hydroxy or alkoxy or the group NR.sub.5 R.sub.6 whereR.sub.5 represents hydrogen, alkyl, alkyl substituted by hydroxy or C.sub.1-3 alkoxy, alkenyl, aralkyl or heteroaralkyl and R.sub.6 represents any of the groups defined for R.sub.5 or may represent the group COR.sub.7 where R.sub.7 represents hydrogen, alkyl, aryl, aralkyl, alkoxy, heteroaryl or monocyclic heteroaralkyl or R.sub.6 represents the group SO.sub.2 R.sub.8 where R.sub.8 represents alkyl or aryl, or R.sub.6 represents the group ##STR2## where Y is oxygen or sulphur and R.sub.9 represents hydrogen, alkyl, cycloalkyl, aryl or aralkyl,or R.sub.5 and R.sub.6 taken together may represent the group .dbd.CR.sub.10 R.sub.11 where R.sub.10 represents aryl or heteroaryl and R.sub.11 represents hydrogen or alkyl.The compounds show activity as selective histamine H.sub.2 -antagonists.