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    Tricyclic ketones useful as HT.sub.3 -receptor antagonists
    2.
    发明授权
    Tricyclic ketones useful as HT.sub.3 -receptor antagonists 失效
    TRICYCLIC KETONES有用作为HT3受体拮抗剂

    公开(公告)号：US5202343A

    公开(公告)日：1993-04-13

    申请号：US887607

    申请日：1992-05-22

    申请人： Ian H. Coates ,  John Bradshaw ,  James A. Bell ,  David C. Humber ,  George B. Ewan ,  William L. Mitchell ,  Barry J. Price

    发明人： Ian H. Coates ,  John Bradshaw ,  James A. Bell ,  David C. Humber ,  George B. Ewan ,  William L. Mitchell ,  Barry J. Price

    IPC分类号： C07D403/06

    CPC分类号： C07D403/06

    摘要： The invention relates to compounds of the general formula (I): ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 ;R.sup.5 and R.sup.6, which may be the same or different, each represents a hydrogen atom, a C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl group, or a phenyl or phenylC.sub.1-4 alkyl group, in which the phenyl group is optionally substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy groups or halogen atoms, with the proviso that R.sup.5 does not represent a hydrogen atom when R.sup.1 represents a group --CO.sub.2 R.sup.5 or --SO.sub.2 R.sup.5 ;one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;Q represents a hydrogen or a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenylC.sub.1-3 alkoxy or C.sub.1-6 alkyl group or a group --NR.sup.7 R.sup.8 or --CONR.sup.7 R.sup.8 ;R.sup.7 and R.sup.8, which may be the same or different, each represents a hydrogen atom or a C.sub.1-4 alkyl or C.sub.3-4 alkenyl group, or together with the nitrogen atom to which they are attached form a saturated 5 to 7 membered ring;n represents 1, 2 or 3; andA-B represents the group CH--CH.sub.2 or C.dbd.CH; and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.

    摘要翻译： 本发明涉及通式（I）的化合物：其中Im表示下式的咪唑基：R1表示氢原子或选自C1-6烷基，C3-6烯基， C 3-10炔基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基，苯基C 1-3烷基，-CO 2 R 5，-COR 5，-CONR 5 R 6或-SO 2 R 5; R 5和R 6可以相同或不同，表示氢原子，C 1-6烷基或C 3-7环烷基或苯基或苯基C 1-4烷基，其中苯基任选被一个或多个C 1 -4-烷基，C 1-4烷氧基或羟基或卤素原子，条件是当R 1表示-CO 2 R 5或-SO 2 R 5基团时，R 5不表示氢原子; 由R 2，R 3和R 4表示的基团之一是氢原子或C 1-6烷基，C 3-7环烷基，C 3-6烯基，苯基或苯基C 1-3烷基，其它两个基团可以相同或 不同的是氢原子或C1-6烷基; Q表示氢或卤素原子，或羟基，C 1-4烷氧基，苯基C 1-3烷氧基或C 1-6烷基或基团-NR 7 R 8或-CONR 7 R 8; R 7和R 8可以相同或不同，各自表示氢原子或C 1-4烷基或C 3-4烯基，或与它们所连接的氮原子一起形成饱和的5至7元环; n表示1,2或3; A-B表示基团CH-CH 2或C = CH; 及其生理上可接受的盐和溶剂合物。 这些化合物是5-HT在5-HT 3受体上的作用的有效和选择性拮抗剂，可用于治疗精神病，焦虑和恶心和呕吐。

    Lactam derivatives
    3.
    发明授权
    Lactam derivatives 失效
    内酰胺衍生物

    公开(公告)号：US5183820A

    公开(公告)日：1993-02-02

    申请号：US691814

    申请日：1991-04-26

    申请人： Ian H. Coates ,  Alexander W. Oxford ,  Peter C. North ,  Barry J. Price

    发明人： Ian H. Coates ,  Alexander W. Oxford ,  Peter C. North ,  Barry J. Price

    IPC分类号： C07D471/04 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The invention provides potent and selective antagonists of 5-HT at 5-HT.sub.3 receptors which are tricyclic lactams of the formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 ;one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;Y represents the group CH.dbd.CH or (CH.sub.2).sub.n, wherein n represents 2 or 3;Q represents a halogen atom, or a group selected from hydroxy, C.sub.1-4 alkoxy, phenylC.sub.1-3 alkoxy, C.sub.1-6 alkyl, cyano, phenyl which may be unsubstituted or substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy groups or halogen atoms, --NR.sup.7 R.sup.8, --CONR.sup.7 R.sup.8 , --(CH.sub.2).sub.p CONR.sup.7 R.sup.8, --(CH.sub.2).sub.q NR.sup.9 R.sup.10 or --(CH.sub.2).sub.2 CO.sub.2 R.sup.11 ;Q' represents a hydrogen or a fluorine atom;and physiologically acceptable salts and solvates thereof.

    摘要翻译： 本发明提供5-HT受体的有效和选择性拮抗剂，其为作为式（I）的三环内酰胺的5-HT 3受体，其中Im表示下式的咪唑基：其中R1表示氢 原子或选自C 1-6烷基，C 3-6烯基，C 3-10炔基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基，苯基C 1-3烷基，-CO 2 R 5，-COR 5，-CONR 5 R 6或-SO 2 R 5中的基团; 由R 2，R 3和R 4表示的基团之一是氢原子或C 1-6烷基，C 3-7环烷基，C 3-6烯基，苯基或苯基C 1-3烷基，其它两个基团可以相同或不同 表示氢原子或C 1-6烷基; Y表示基团CH = CH或（CH 2）n，其中n表示2或3; Q表示卤原子，或选自羟基，C 1-4烷氧基，苯基C 1-3烷氧基，C 1-6烷基，氰基，可未被取代或被一个或多个C 1-4烷基，C 1-4烷氧基或羟基或卤素取代的苯基的基团 原子，-NR 7 R 8，-CONR 7 R 8， - （CH 2）p CONR 7 R 8， - （CH 2）q NR 9 R 10或 - （CH 2）2 CO 2 R 11; Q'表示氢或氟原子; 及其生理上可接受的盐和溶剂合物。

    1,2,4-Triazole-3,5-diamine derivatives
    4.
    发明授权
    1,2,4-Triazole-3,5-diamine derivatives 失效
    1,2,4-三唑-3,5-二胺衍生物

    公开(公告)号：US4318913A

    公开(公告)日：1982-03-09

    申请号：US33508

    申请日：1979-04-26

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

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

    IPC分类号： C07D209/48 ,  C07D249/14 ,  C07D307/52 ,  C07D317/12 ,  A61K31/445 ,  A61K31/41 ,  C07D403/12 ,  C07D403/14

    CPC分类号： C07D209/48 ,  C07D249/14 ,  C07D307/52 ,  C07D317/12 ,  Y10S514/926 ,  Y10S514/927

    摘要： The invention relates to compounds of the formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichR.sub.1 and R.sub.2 represent hydrogen, an aliphatic or cycloaliphatic group, or R.sub.1 and R.sub.2 together with the nitrogen atom form a 5 to 10 membered heterocyclic ring:Alk represents a straight or branched alkylene chain;Q represents furan, thiophen or benzene ring which is incorporated into the rest of the molecule;X represents --CH.sub.2 --, ##STR2## --O-- or --S-- whereR.sub.6 represents hydrogen or methyl;n represents zero, 1 or 2;m represents 2, 3 or 4;R.sub.3 represents hydrogen, a substituted or unsubstituted aliphatic or aryl group and;R.sub.4 and R.sub.5, which may be the same or different, each represent hydrogen, a substituted or unsubstituted aliphatic, aryl, or together with the nitrogen atom form a heterocyclic group.

    摘要翻译： 本发明涉及式（I）化合物及其生理学上可接受的盐，水合物和生物前体，其中R 1和R 2表示氢，脂族或脂环族基团，或R 1和R 2与氮原子一起 形成5至10元杂环：Alk表示直链或支链亚烷基链; Q表示呋喃，噻吩或苯环，其结合到分子的其余部分中; X表示-CH 2 - ， -O-或-S-，其中R 6表示氢或甲基; n表示0，1或2; m表示2,3或4; R 3表示氢，取代或未取代的脂族或芳基， R 4和R 5可以相同或不同，各自表示氢，取代或未取代的脂族基，芳基或与氮原子一起形成杂环基。

    Aminoalkyl furan derivatives
    5.
    发明授权
    Aminoalkyl furan derivatives 失效
    氨基烷基呋喃衍生物

    公开(公告)号：US4128658A

    公开(公告)日：1978-12-05

    申请号：US818762

    申请日：1977-07-25

    申请人： Barry J. Price ,  John W. Clitherow ,  John Bradshaw

    发明人： Barry J. Price ,  John W. Clitherow ,  John Bradshaw

    IPC分类号： C07C323/25 ,  A61K31/34 ,  A61K31/341 ,  A61P43/00 ,  C07C67/00 ,  C07C313/00 ,  C07D207/08 ,  C07D233/64 ,  C07D275/02 ,  C07D275/03 ,  C07D307/38 ,  C07D307/52 ,  C07D307/54 ,  C07D307/64 ,  C07D405/06 ,  C07D405/12 ,  C07D413/14 ,  A01N9/12 ,  A01N9/20

    CPC分类号： C07D275/03 ,  A61K31/34 ,  C07D207/08 ,  C07D307/38 ,  C07D307/52 ,  C07D307/64

    摘要： Compounds of the general formula I: ##STR1## and physiologically acceptable salts thereof and N-oxides and hydrates, in which R.sub.1 and R.sub.2 which may be the same or different represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group ##STR2## in which R.sub.4 represents hydrogen or lower alkyl or R.sub.1 and R.sub.2 may, together with the nitrogen atom to which they are attached, form a heterocyclic ring which may contain other heteroatoms selected from O and ##STR3## R.sub.3 is hydrogen, lower alkyl, lower alkenyl or alkoxyalkyl; X is --CH.sub.2 --, O or S;Y represents .dbd. S, .dbd. O, .dbd. NR.sub.5 or .dbd. CHR.sub.6 ;Alk denotes a straight or branched alkylene chain of 1 to 6 carbon atoms;R.sub.5 is H, nitro, cyano, lower alkyl, aryl, alkylsulphonyl, or arylsulphonyl;R.sub.6 represents nitro, arylsulphonyl or alkylsulphonyl;M is an integer from 2 to 4; andN is 1 or 2; or when X .dbd. S, or --CH.sub.2 --, n is zero, 1 or 2.These compounds have H.sub.2 -antagonist activity. Intermediates in the production thereof are also provided.

    摘要翻译： 通式I的化合物及其生理上可接受的盐和N-氧化物和水合物，其中可以相同或不同的R 1和R 2表示氢，低级烷基，环烷基，低级烯基，芳烷基或 被氧原子间隔的低级烷基或其中R 4表示氢或低级烷基或R 1和R 2的基团可以与它们所连接的氮原子一起形成杂环，该杂环可以含有选自O 且R 3为氢，低级烷基，低级烯基或烷氧基烷基; X是-CH 2 - ，O或S; Y表示= S，= O，= NR5或= CHR6; Alk表示1〜6个碳原子的直链或支链亚烷基链; R5是H，硝基，氰基，低级烷基，芳基，烷基磺酰基或芳基磺酰基; R6表示硝基，芳基磺酰基或烷基磺酰基; M是从2到4的整数; 和N是1或2; 或当X = S或-CH 2 - 时，n为0,1或2。

    Heterocyclic derivatives
    7.
    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.

    Furan derivatives having selective action on histamine receptors
    8.
    发明授权
    Furan derivatives having selective action on histamine receptors 失效
    呋喃衍生物对组胺受体具有选择性作用

    公开(公告)号：US4255440A

    公开(公告)日：1981-03-10

    申请号：US951026

    申请日：1978-10-13

    申请人： Barry J. Price ,  John W. Clitherow ,  John Bradshaw

    发明人： Barry J. Price ,  John W. Clitherow ,  John Bradshaw

    IPC分类号： C07C323/25 ,  A61K31/34 ,  A61K31/341 ,  A61P43/00 ,  C07C67/00 ,  C07C313/00 ,  C07D207/08 ,  C07D233/64 ,  C07D275/02 ,  C07D275/03 ,  C07D307/38 ,  C07D307/52 ,  C07D307/54 ,  C07D307/64 ,  C07D405/06 ,  C07D405/12 ,  C07D413/14 ,  A61K31/40 ,  A61K31/535 ,  C07D413/06

    CPC分类号： C07D275/03 ,  A61K31/34 ,  C07D207/08 ,  C07D307/38 ,  C07D307/52 ,  C07D307/64

    摘要： Compounds of the general formula I: ##STR1## and physiologically acceptable salts thereof and N-oxides and hydrates, in which R.sub.1 and R.sub.2 which may be the same or different represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group ##STR2## in which R.sub.4 represents hydrogen or lower alkyl or R.sub.1 and R.sub.2 may, together with the nitrogen atom to which they are attached, form a heterocyclic ring which may contain other heteroatoms selected from O and ##STR3## R.sub.3 is hydrogen, lower alkyl, lower alkenyl or alkoxyalkyl; X is --CH.sub.2 --, O-- or --S--;Y represents .dbd.S, .dbd.O, .dbd.NR.sub.5 or .dbd.CHR.sub.6 ;Alk denotes a straight or branched alkylene chain of 1 to 6 carbon atoms;R.sub.5 is H, nitro, cyano, lower alkyl, aryl, alkylsulphonyl, or arylsulphonyl;R.sub.6 represents nitro, arylsulphonyl or alkylsulphonyl;m is an integer from 2 to 4; andn is 1 or 2; or when X is --S-- or --CH.sub.2 --, n is zero, 1 or 2.These compounds have H.sub.2 -antagonist activity. Intermediates in the production thereof are also provided.

    摘要翻译： 通式I的化合物及其生理上可接受的盐和N-氧化物和水合物，其中可以相同或不同的R 1和R 2表示氢，低级烷基，环烷基，低级烯基，芳烷基或 被氧原子间隔的低级烷基或其中R 4表示氢或低级烷基或R 1和R 2的基团可以与它们所连接的氮原子一起形成杂环，该杂环可以含有选自O 且R 3为氢，低级烷基，低级烯基或烷氧基烷基; X是-CH 2 - ，O-或-S-; Y表示= S，= O，= NR5或= CHR6; Alk表示1〜6个碳原子的直链或支链亚烷基链; R5是H，硝基，氰基，低级烷基，芳基，烷基磺酰基或芳基磺酰基; R6表示硝基，芳基磺酰基或烷基磺酰基; m为2〜4的整数; n为1或2; 或当X为-S-或-CH 2 - 时，n为0,1或2.这些化合物具有H 2 - 拮抗剂活性。 还提供了其生产中的中间体。

    1H-1,2,4-Triazole-3,5-diamine derivatives and use as selective histamine H.sub.2 -antagonists
    9.
    发明授权
    1H-1,2,4-Triazole-3,5-diamine derivatives and use as selective histamine H.sub.2 -antagonists 失效

    公开(公告)号：US4442110A

    公开(公告)日：1984-04-10

    申请号：US324440

    申请日：1981-11-24

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

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

    IPC分类号： C07D209/48 ,  C07D249/14 ,  C07D307/52 ,  C07D317/12 ,  A01N43/64

    CPC分类号： C07D209/48 ,  C07D249/14 ,  C07D307/52 ,  C07D317/12 ,  Y10S514/926 ,  Y10S514/927

    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 or different, each represent hydrogen, C.sub.1-10 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 alicyclic heterocyclic 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;Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms;Q represents a furan or thiophen 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.7 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.7 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 --, ##STR2## --O-- or --S-- whereR.sub.6 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 having at least two carbon atoms, alkoxyalkyl or aryl; andR.sub.4 and R.sub.5, which may be the same or different, each represent hydrogen, alkyl, alkyl substituted by hydroxy or C.sub.1-3 alkoxy, alkenyl, aralkyl or heteroaralkyl or R.sub.4 and R.sub.5 may together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain another heteroatom, or the group ##STR3## or R.sub.4 and R.sub.5 taken together may represent the group .dbd.CR.sub.8 R.sub.9 where R.sub.8 represents aryl or heteroaryl and R.sub.9 represents hydrogen or alkyl.Preferably when X represents an oxygen atom or ##STR4## and n is zero, then Q only represents a benzene ring. The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -antagonists.

    Substituted furan compounds and pharmaceutical compositions containing them
    10.
    发明授权
    Substituted furan compounds and pharmaceutical compositions containing them 失效
    取代的呋喃化合物和含有它们的药物组合物

    公开(公告)号：US4288443A

    公开(公告)日：1981-09-08

    申请号：US124115

    申请日：1980-02-25

    申请人： Duncan B. Judd ,  John W. Clitherow ,  Barry J. Price ,  John Bradshaw

    发明人： Duncan B. Judd ,  John W. Clitherow ,  Barry J. Price ,  John Bradshaw

    IPC分类号： A61K31/34 ,  A61K31/341 ,  A61P1/04 ,  C07D307/52 ,  C07D307/56 ,  C07D307/68 ,  C07D307/54

    CPC分类号： C07D307/56 ,  C07D307/52 ,  C07D307/68

    摘要： The invention relates to compounds of the general formula ##STR1## and physiologically acceptable salts and N-oxides, hydrates and bioprecursors thereof, in which R.sub.1 and R.sub.2 which may be the same or different each represent hydrogen, C.sub.1-8 alkyl, C.sub.4-8 cycloalkyl, C.sub.3-6 alkenyl, aralkyl with 1 to 4 carbon atoms in the alkyl residue or C.sub.1-8 alkyl interrupted by an oxygen atom or a group ##STR2## in which R.sub.5 represents hydrogen or C.sub.1-8 alkyl, or R.sub.1 and R.sub.2 may together with the nitrogen atom to which they are attached, form a saturated monocyclic 5 to 7 membered heterocyclic ring which may additionally contain the heterofunction O or ##STR3## R.sub.3 represents straight or branched chain C.sub.1-8 alkyl, alkoxyalkyl with 1 to 8 carbon atoms in each alkyl residue, C.sub.1-8 hydroxyalkyl, C.sub.1-8 alkoxycarbonyl, alkyl thioalkyl with 1 to 8 carbon atoms in each alkyl residue, halogen or aryl;R.sub.4 represents hydrogen, C.sub.1-8 alkyl, C.sub.3-6 alkenyl or alkoxyalkyl with 1 to 8 carbon atoms in each alkyl residue;X represents --O-- or --S--;Y represents .dbd.S, .dbd.O, .dbd.NR.sub.6 or .dbd.CHNO.sub.2 where R.sub.6 represents hydrogen, nitro, cyano, C.sub.1-8 alkyl, aryl, C.sub.1-8 alkylsulphonyl or arylsulphonyl;m represents an integer from 2 to 4 inclusive; andn represents an integer which is 1 or 2, or additionally when X is --S-- n may also be zero.The invention also relates to processes for the production of such compounds, pharmaceutical compositions containing them and certain novel intermediates used in their production, i.e. amines of the formula ##STR4## and alcohols of the formula ##STR5## The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -antagonists.

    摘要翻译： 本发明涉及通式为（I）的化合物及其生理上可接受的盐和N-氧化物，水合物和生物前体，其中可以相同或不同的R 1和R 2各自表示氢，C 1-8烷基， C4-8环烷基，C3-6烯基，在烷基中具有1至4个碳原子的芳烷基或被氧原子间断的C1-8烷基或其中R5表示氢或C1-8烷基的基团，或R1 并且R 2可以与它们所连接的氮原子一起形成饱和的单环5至7元杂环，其可另外含有杂官能O，或者R 3表示直链或支链C 1-8烷基，烷氧基烷基与1至 每个烷基残基中的8个碳原子，C 1-8羟基烷基，C 1-8烷氧基羰基，每个烷基残基中具有1至8个碳原子的烷基硫代烷基，卤素或芳基; R4表示氢，C1-8烷基，C3-6烯基或每个烷基残基具有1至8个碳原子的烷氧基烷基; X表示-O-或-S-; Y表示= S，= O，= NR6或= CHNO2，其中R6表示氢，硝基，氰基，C1-8烷基，芳基，C1-8烷基磺酰基或芳基磺酰基; m表示2〜4的整数， 并且n表示1或2的整数，或者当X是-S-n时也可以为零。 本发明还涉及生产这种化合物的方法，含有它们的药物组合物和它们生产中使用的某些新型中间体，即式（III）的胺和式的醇（VIII）。化合物 式（I）表示作为选择性组胺H2拮抗剂的药理学活性。