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501 条记录 (耗时 0.021 秒)

    3-Aminopiperidine derivatives and related nitrogen containing heterocycles
    93.
    发明公开
    3-Aminopiperidine derivatives and related nitrogen containing heterocycles 失效
    3-Aminopiperidinderivate und verwandte Nitrogen-enthaltende Heterozyklen。

    公开(公告)号：EP0436334A2

    公开(公告)日：1991-07-10

    申请号：EP90313680.2

    申请日：1990-12-14

    申请人： PFIZER INC.

    发明人： Desai, Manoj C. ,  Rosen, Terry J.

    IPC分类号： C07D207/14 ,  C07D211/56 ,  C07D223/12 ,  C07D221/20 ,  A61K31/40 ,  A61K31/445 ,  A61K31/55

    CPC分类号： C07D221/20 ,  C07D211/56 ,  C07D409/04 ,  C07D409/14

    摘要： The present invention relates to novel 3-aminopiperidine derivatives and related nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula

    wherein R¹, R², R³, R⁴, R⁵, R⁶, R⁷, R⁸, Y and Z are as defined below. These novel compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders. The invention also relates to novel intermediates used in the synthesis of compounds of the formula I.

    摘要翻译： 本发明涉及新的3-氨基哌啶衍生物和相关的含氮杂环化合物，具体地说，涉及式的化合物，其中R 1，R 2，R 3，R 4，R R 5，R 6，R 7，R 8，Y和Z如下所定义。 这些新型化合物可用于治疗炎性和中枢神经系统疾病以及其他疾病。 本发明还涉及用于合成式I化合物的新型中间体。

    Cycloalkyl-substituted glutaramide diuretic agents
    95.
    发明公开
    Cycloalkyl-substituted glutaramide diuretic agents 失效
    环烷基磺酸酯谷氨酰胺

    公开(公告)号：EP0343911A2

    公开(公告)日：1989-11-29

    申请号：EP89305180.5

    申请日：1989-05-23

    申请人： Pfizer Limited ,  PFIZER INC.

    发明人： James, Keith, Dr. ,  Danilewicz, John Christopher, Dr.

    IPC分类号： C07C103/737 ,  A61K31/215 ,  C07K5/06 ,  C07D213/82 ,  A61K31/455 ,  C07D295/18 ,  A61K31/40 ,  C07D207/14

    CPC分类号： C07D213/82 ,  A61K38/00 ,  C07C233/63 ,  C07C235/40 ,  C07C237/24 ,  C07C271/22 ,  C07C311/06 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D277/06 ,  C07D295/185 ,  C07K5/0207 ,  C07K5/06086

    摘要： Compounds having the formula:
    wherein A completes a 4 to 7 membered carbocyclic ring which may be saturated or mono-unsaturated and which may optionally be fused to a further carbocyclic ring; B is (CH 2 ) m wherein m is 1 to 3; R and R 4 are H, C 1 -C 6 alkyl, benzyl or biolabile ester-forming groups; R 1 is H or C 1 -C 4 alkyl; R 2 and R 3 are each H, OH, C 1 -C 6 alkyl or C 1 -C 6 alkoxy, or are linked together and are (CH 2 ) r wherein r is 1 to 4; Y is an optional alkylene group of from 1 to 6 carbon atoms which may be straight or branched-chain;

    and R 5 is R 6 CONR 9- , R 6 SO 2 NR 9 -, R 6 CO 2 -, R 6 CO-, R 6 SOq-, R 7 NR 9 CO-, R 7 NR 9 S0 2 - or R 7 0CO-; wherein R 6 is a group of the formula R 8 (R 1O R 11 C-CONR 9 ) n R 1O R 11 C-; R 7 is a group of the formula R 10 R 11 R 12 C- and R 9 is H, C 1 -C 6 alkyl, aryl, C 3 -C 7 cycloalkyl, heterocyclyl, aryl(C 1 -C 6 alkyl) or heterocyclyl(C 1 -C 6 alkyl); wherein R 8 is R 9 CONR 9 -, R 9 SO 2 NR 9 -, R 13 R 14 -N-(CH 2 ) p -, or R 9 0-, R 10 and R 11 are H or C 1 -C 6 alkyl; or R 10 is H and R 11 is C 1 -C 6 alkyl which is substituted by OH, SH, SCH 3 , NH 2 , aryl(C 1 -C 6 alkyl)OCONH-, NH 2 CO-, C0 2 H, guanidino, aryl, or heterocyclyl; or the two groups R 10 and R 11 are joined to form a five or 6 membered carbocyclic ring which may be saturated, mono-unsaturated, optionally substituted by C 1 -C 4 alkyl or fused to a further carbocylic ring; or R 8 and R 11 are linked to form a 2-(N-COR 9- 4-aminopyrrolidinyl) group; R 12 is R 13 R 14 NCO-, R 9 0CO-, R 9 0CH 2 - or heterocyclyl, R 13 and R 14 are H, C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, aryl, aryl(C 1 -C 6 alkyl), C 2 -C s alkoxyalkyl, amino (C 1 -C 6 alkyl), heterocyclyl or heterocyclyl(C 1 -C 6 alkyl); or the two groups R 13 and R 14 form a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C 1 -C 4 alkyl) piperazinyl, pyrrolyl, imidazolyl, pyrazolyl or triazolyl group; n is 0 or 1; p is 0 or 1 to 6; and q is 0, 1 or 2; and pharmaceutically acceptable salts thereof and bioprecursors therefor, are diuretic agents of value in the treatment of hypertension, heart failure and renal insufficiency.

    摘要翻译： 具有下式的化合物：其中A完成4至7元碳环，其可以是饱和或单不饱和的，并且可任选地与另外的碳环稠合; B是（CH 2）m，其中m是1至3; R和R 4是H，C 1 -C 6烷基，苄基或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各自为H，OH，C 1 -C 6烷基或C 1 -C 6烷氧基，或连接在一起并且为（CH 2）r，其中r为1至4; Y是可以是直链或支链的1-6个碳原子的任选的亚烷基; R 5是R 6 CONR 9 - ，R 6 SO 2 NR 9 - ，R 6 CO 2 - ，R 6 CO-，R 6 SOQ-，R 7 NR 9，CO - ，R 7 NR 9 SO 2 - 或R 7 OCO-; 其中R 6是式R 8的基团（R 1）R 1 C-CONR 9）n R 1 R 1 > C-; R 7是式R 1，R 1，R 2，C和R 9是H，C 1 -C 6烷基，芳基，C 3 -C 6环烷基， C7环烷基，杂环基，芳基（C1-C6烷基）或杂环基（C1-C6烷基）; 其中R 8是R 9 CONR 9 - ，R 9 SO 2 NR 9 - ，R 1，R 3，N - （CH 2）p - 或R O，R 1，O和R 1是H或C 1 -C 6烷基; 或R 1为H且R 1为被OH，SH，SCH 3，NH 2，芳基（C 1 -C 6烷基）OCONH-，NH 2 CO-，CO 2 H， 胍基，芳基或杂环基; 或两个基团R 1和R 1连接形成五元或六元碳环，其可以是饱和的，单不饱和的，任选地被C 1 -C 4烷基取代或稠合到 进一步的碳环; 或R 8和R 1'连接形成2-（N-COR 9-14-氨基吡咯烷基）基团; R 1是R 1，R 3，R 3，NCO-，R 9 OCO-，R 9 OCH 2 - 或杂环基，R 1和R 3 C 1 -C 6烷基，C 1 -C 6烷基，C 2 -C 6烷氧基烷基，氨基（C 1 -C 6烷基），杂环基或杂环基（C 1 -C 6烷基） ; 或两个基团R 1，R 3和R 4形成吡咯烷基，哌啶子基，吗啉代，哌嗪基，N-（C 1 -C 4烷基）哌嗪基，吡咯基，咪唑基，吡唑基或三唑基; n为0或1; p为0或1至6; q为0,1或2; 及其药学上可接受的盐及其生物前体是治疗高血压，心力衰竭和肾功能不全的利尿剂。