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    Spiro-subsituted glutaramide diuretic agents
    1.
    发明公开
    Spiro-subsituted glutaramide diuretic agents 失效
    螺旋替代物戊二酰胺

    公开(公告)号：EP0274234A2

    公开(公告)日：1988-07-13

    申请号：EP87310784.1

    申请日：1987-12-08

    申请人： Pfizer Limited

    发明人： Barnish, Ian Thompson, Dr. ,  James, Keith, Dr. ,  Terrett, Nicholas Kenneth, Dr. ,  Danilewicz, John Christopher, Dr. ,  Samuels, Gillian Mary Ryder, Dr. ,  Wythes, Martin James, Dr.

    IPC分类号： C07C233/57 ,  C07D207/327 ,  C07D295/14 ,  A61K31/16 ,  A61K31/445 ,  A61K31/535 ,  A61K31/40 ,  A61K31/495 ,  C07C311/01 ,  C07C311/15

    CPC分类号： C07D241/12 ,  C07D209/46 ,  C07D213/56 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D261/10 ,  C07D277/36 ,  C07D277/46 ,  C07D295/185 ,  C07D307/16 ,  C07D307/68 ,  C07D321/08 ,  C07D333/34

    摘要： Compounds of the formula
    wherein A completes a 4 or 7 membered carbocyclic ring which may be saturated or mono-unsaturated and which may optionally be fused to a further saturated or unsaturated 5 or 6 membered carbocyclic ring; B is (CH 2 ) m wherein m is an integer of from 1 to 3; each of R and R 4 is independently H, C 1 -C 6 alkyl, benzyl or an alternative biolabile ester-forming group; R 1 is H or C 1 -C 4 alkyl; R 2 and R 3 are each independently H, OH, C 1 -C 4 alkyl or C 1 -C 4 alkoxy; and R 5 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, aryl(C 2 -C 6 alkynyl), C 3 -C 7 cycloalkyl, C 3 -C 7 cycloalkenyl, C 1 -C 6 alkoxy, -NR 6 R 7 , -NR 8 COR 9 , -NR 8 SO 2 R 9 or a saturated heterocyclic group; or C 1 -C 6 alkyl substituted by one or more substituents chosen from halo, hydroxy, C 1 -C 6 alkoxy, C 2 -C 6 hydroxyalkoxy, C 1 -C 6 alkoxy(C 1 -C 6 alkoxy), C 3 -C 7 cycloalkyl, C 3 -C 7 cycloalkenyl, aryl, aryloxy, arlyoxy(C I -C 4 alkoxy), heterocyclyl, heterocyclyloxy, -NR 6 R 7 , -NR8COR9, -NR 8 SO 2 R 9 , -CONR 6 R 7 , -SH, -S(O) p R 10 , -COR 11 or -CO 2 R 12 ; wherein R 6 and R 7 are each independently H, C 1 -C 4 alkyl, C 3 -C 7 cycloalkyl (optionally substituted by hydroxy or C 1 -C 4 alkoxy), aryl, aryl(C 1 -C 4 alkyl), CrCs alkoxyalkyl, or heterocyclyl; or the two groups R 6 and R 7 are taken together with the nitrogen to which they are attached to form a pyrrolidinyl, piperidino, morpholino, piperazinyl or N-(C 1 -C 4 alkyl)-piperazinyl group; R 8 is H or C 1 -C 4 alkyl; R 9 is C 1 -C 4 alkyl, CF 3 , aryl, aryl(C I -C 4 alkyl), aryl(C 1 -C 4 alkoxy), heterocycyl, C 1 -C 4 alkoxy or NR 6 R 7 wherein R 6 and R 7 are as previously defined; R 10 is C 1 -C 4 alkyl, aryl, heterocyclyl or NR 6 R 7 wherein R 6 and R 7 are as previously defined; R 11 is C 1 -C 4 alkyl, C 3 -C 7 cycloalkyl, aryl or heterocyclyl; R 12 is H or Ci-C 4 alkyl; and p is 0, 1 or 2; or a pharmaceutically acceptable salts thereof or bioprecursor therefor are diuretic agents having utility in the treatment of hypertension, heart failure, renal insufficiency and in other disorders.

    摘要翻译： 其中A完成4或7元碳环，其可以是饱和或单不饱和的，并且可以任选地与另外的饱和或不饱和的5或6元碳环稠合; B是（CH 2）m，其中m是1至3的整数; R和R 4中的每一个独立地是H，C 1 -C 6烷基，苄基或替代的生物不稳定酯形成基团; R 1是H或C 1 -C 4烷基; R 2和R 3各自独立地为H，OH，C 1 -C 4烷基或C 1 -C 4烷氧基; 并且R 5是C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，芳基（C 2 -C 6炔基），C 3 -C 7环烷基，C 3 -C 7环烯基，C 1 -C 6烷氧基，-NR 6 R -NR 8 COR 9，-NR 8 SO 2 R 9或饱和杂环基; 或被一个或多个选自卤素，羟基，C 1 -C 6烷氧基，C 2 -C 6羟基烷氧基，C 1 -C 6烷氧基（C 1 -C 6烷氧基），C 3 -C 7环烷基，C 3 -C 7环烯基，芳基， 芳氧基，芳氧基（C 1 -C 4烷氧基），杂环基，杂环氧基，-NR 6 R 7，-NR 8 COR 9，-NR 8 SO 2 R 9，-CONR 6 R -SH，-S（O）pR 1 O，-COR 1或-CO 2 R 1; 其中R 6和R 7各自独立地为H，C 1 -C 4烷基，C 3 -C 7环烷基（任选被羟基或C 1 -C 4烷氧基取代），芳基，芳基（C 1 -C 4烷基），C 2 -C 6烷氧基烷基 ，或杂环基; 或两个基团R 6和R 7与它们所连接的氮一起形成吡咯烷基，哌啶子基，吗啉代，哌嗪基或N-（C 1 -C 4烷基） - 哌嗪基; R 8是H或C 1 -C 4烷基; R 9是C 1 -C 4烷基，CF 3，芳基，芳基（C 1 -C 4烷基），芳基（C 1 -C 4烷氧基），杂环基，C 1 -C 4烷氧基或NR 6 R 7其中R 6， 和R 7如前所定义; R 1是C 1 -C 4烷基，芳基，杂环基或NR 6 R 7，其中R 6和R 7如前所定义; R 1是C 1 -C 4烷基，C 3 -C 7环烷基，芳基或杂环基; R 1是H或C 1 -C 4烷基; p为0,1或2; 或其药学上可接受的盐或其生物前体是具有用于治疗高血压，心力衰竭，肾功能不全和其它病症的利尿剂。

    Spiro-subsituted glutaramide diuretic agents
    3.
    发明公开
    Spiro-subsituted glutaramide diuretic agents 失效
    SPIRO替代的谷氨酰胺代用剂

    公开(公告)号：EP0274234A3

    公开(公告)日：1988-10-19

    申请号：EP87310784

    申请日：1987-12-08

    申请人： Pfizer Limited

    发明人： Barnish, Ian Thompson, Dr. ,  James, Keith, Dr. ,  Terrett, Nicholas Kenneth, Dr. ,  Danilewicz, John Christopher, Dr. ,  Samuels, Gillian Mary Ryder, Dr. ,  Wythes, Martin James, Dr.

    IPC分类号： C07C103/737 ,  C07D207/327 ,  C07D295/14 ,  A61K31/16 ,  A61K31/445 ,  A61K31/535 ,  A61K31/40 ,  A61K31/495 ,  C07C143/74 ,  C07C143/78

    CPC分类号： C07D241/12 ,  C07D209/46 ,  C07D213/56 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D261/10 ,  C07D277/36 ,  C07D277/46 ,  C07D295/185 ,  C07D307/16 ,  C07D307/68 ,  C07D321/08 ,  C07D333/34

    摘要： Compounds of the formula wherein A completes a 4 or 7 membered carbocyclic ring which may be saturated or mono-unsaturated and which may optionally be fused to a further saturated or unsaturated 5 or 6 membered carbocyclic ring; B is (CH 2 ) m wherein m is an integer of from 1 to 3; each of R and R 4 is independently H, C 1 -C 6 alkyl, benzyl or an alternative biolabile ester-forming group; R 1 is H or C 1 -C 4 alkyl; R 2 and R 3 are each independently H, OH, C 1 -C 4 alkyl or C 1 -C 4 alkoxy; and R 5 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, aryl(C 2 -C 6 alkynyl), C 3 -C 7 cycloalkyl, C 3 -C 7 cycloalkenyl, C 1 -C 6 alkoxy, -NR 6 R 7 , -NR 8 COR 9 , -NR 8 SO 2 R 9 or a saturated heterocyclic group; or C 1 -C 6 alkyl substituted by one or more substituents chosen from halo, hydroxy, C 1 -C 6 alkoxy, C 2 -C 6 hydroxyalkoxy, C 1 -C 6 alkoxy(C 1 -C 6 alkoxy), C 3 -C 7 cycloalkyl, C 3 -C 7 cycloalkenyl, aryl, aryloxy, arlyoxy(C I -C 4 alkoxy), heterocyclyl, heterocyclyloxy, -NR 6 R 7 , -NR8COR9, -NR 8 SO 2 R 9 , -CONR 6 R 7 , -SH, -S(O) p R 10 , -COR 11 or -CO 2 R 12 ; wherein R 6 and R 7 are each independently H, C 1 -C 4 alkyl, C 3 -C 7 cycloalkyl (optionally substituted by hydroxy or C 1 -C 4 alkoxy), aryl, aryl(C 1 -C 4 alkyl), CrCs alkoxyalkyl, or heterocyclyl; or the two groups R 6 and R 7 are taken together with the nitrogen to which they are attached to form a pyrrolidinyl, piperidino, morpholino, piperazinyl or N-(C 1 -C 4 alkyl)-piperazinyl group; R 8 is H or C 1 -C 4 alkyl; R 9 is C 1 -C 4 alkyl, CF 3 , aryl, aryl(C I -C 4 alkyl), aryl(C 1 -C 4 alkoxy), heterocycyl, C 1 -C 4 alkoxy or NR 6 R 7 wherein R 6 and R 7 are as previously defined; R 10 is C 1 -C 4 alkyl, aryl, heterocyclyl or NR 6 R 7 wherein R 6 and R 7 are as previously defined; R 11 is C 1 -C 4 alkyl, C 3 -C 7 cycloalkyl, aryl or heterocyclyl; R 12 is H or Ci-C 4 alkyl; and p is 0, 1 or 2; or a pharmaceutically acceptable salts thereof or bioprecursor therefor are diuretic agents having utility in the treatment of hypertension, heart failure, renal insufficiency and in other disorders.