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216 条记录 (耗时 0.022 秒)

    4-substituted-N-(piperidinyl or pyrrolidinyl)alkyl benzenesulfonamides
    31.
    发明授权
    4-substituted-N-(piperidinyl or pyrrolidinyl)alkyl benzenesulfonamides 失效
    4-取代-N-（哌啶基或吡咯烷基）烷基苯磺酰胺

    公开(公告)号：US4734510A

    公开(公告)日：1988-03-29

    申请号：US916984

    申请日：1986-10-09

    申请人： John T. A. Boyle ,  Richard S. Todd

    发明人： John T. A. Boyle ,  Richard S. Todd

    IPC分类号： C07D207/09 ,  C07D215/44 ,  C07D237/28 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D211/28

    CPC分类号： C07D401/12 ,  C07D207/09 ,  C07D215/44 ,  C07D237/28 ,  C07D239/94 ,  C07D403/12

    摘要： Novel quinazoline and cinnoline derivatives having the formula ##STR1## (wherein one of A and B is CH and the other one of A and B is N; X.sub.1 is halogen or CF.sub.3 and X.sub.3 is one of the groups II, III, IV or V ##STR2## where Q is lower alkylene; R.sub.1 is hydrogen or lower alkyl; R.sub.2 and R.sub.3 are independently lower alkyl or R.sub.2 and R.sub.3 are a divalent radical such that HNR.sub.2 R.sub.3 is a secondary cyclic amine with 5 to 7 ring atoms; R.sub.4 is lower alkyl; n is 0 or 1; the rings shown in formulae III and IV are piperidine or pyrrolidine optionally substituted by lower alkyl; and the ring shown in formula V is piperazine optionally substituted by lower alkyl) and their pharmaceutically acceptable salts are useful as pharmaceuticals particularly as anti-hypertensives. Novel intermediates are also described including the corresponding sulphonic acids of formula I (where A, B and X.sub.1 are defined above and X.sub.3 is OH).

    摘要翻译： 具有式（I）的新型喹唑啉和噌啉衍生物（其中A和B中的一个为CH，A和B中的一个为N; X 1为卤素或CF 3，X 3为II，III， （IV）其中Q是低级亚烷基; R1是氢或低级烷基; R2和R3独立地是低级烷基或R2和R3是 二价基团，使得HNR2R3是具有5-7个环原子的仲环状胺; R4是低级烷基; n是0或1;式III和IV中所示的环是任选被低级烷基取代的哌啶或吡咯烷;并且环 式V中所示的化合物是任选被低级烷基取代的哌嗪）及其药学上可接受的盐可用作特别是抗高血压药物的药物。 还描述了新的中间体，包括相应的式I的磺酸（其中A，B和X 1如上定义，X​​ 3是OH）。

    N-(-2-Pyrimidinyl)-4-aryl-4-[N'-(alkylamino alkyl)]-piperidinamide
    33.
    发明授权
    N-(-2-Pyrimidinyl)-4-aryl-4-[N'-(alkylamino alkyl)]-piperidinamide 失效
    N - （ - 2-嘧啶基）-4-芳基-4- [N' - （烷基氨基烷基）] - 哌啶酰胺

    公开(公告)号：US4329345A

    公开(公告)日：1982-05-11

    申请号：US144469

    申请日：1980-04-28

    申请人： James R. Shroff ,  Rohit Desai

    发明人： James R. Shroff ,  Rohit Desai

    IPC分类号： C07D211/64 ,  C07D211/28 ,  A61K31/44

    CPC分类号： C07D211/64 ,  Y10S514/821

    摘要： Compounds of the formula ##STR1## wherein R is hydrogen, alkyl, alkoxy, halo, amino, alkylamino, dialkylamino, hydroxy, nitro, trifluoromethyl, mercapto, or alkylmercapto, and may be the same or different,n is an integer from 2 to 4, andR.sub.1 and R.sub.2 are hydrogen or alkyl and may be the same or different, or R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached may be pyrrolidino, piperidino or morpholinoand their pharmaceutically acceptable, non-toxic acid addition salts have anti-arrhythmic activity.

    摘要翻译： 其中R是氢，烷基，烷氧基，卤素，氨基，烷基氨基，二烷基氨基，羟基，硝基，三氟甲基，巯基或烷基巯基，并且可以相同或不同，n是2- 4，R 1和R 2是氢或烷基，并且可以相同或不同，或者R 1和R 2与它们所连接的氮一起可以是吡咯烷子基，哌啶子基或吗啉代及其药学上可接受的无毒酸加成盐 有抗心律失常活动。

    1-Alkyl-4-(10[1-p iperidyl]-5H-dibenzo-[a,d]cyclohepten-5-ylidene)piperidine compounds
    34.
    发明授权
    1-Alkyl-4-(10[1-p iperidyl]-5H-dibenzo-[a,d]cyclohepten-5-ylidene)piperidine compounds 失效
    1-烷基-4-（10 {8 1-哌啶基{9 -5H-二苯并 - {8a，d {9环庚烯-5-亚基）哌啶化合物

    公开(公告)号：US3981876A

    公开(公告)日：1976-09-21

    申请号：US280697

    申请日：1972-08-14

    申请人： John D. Prugh

    发明人： John D. Prugh

    IPC分类号： A61K31/445 ,  C07D211/68 ,  C07D211/28

    CPC分类号： C07D211/68 ,  A61K31/445

    摘要： The new 1-alkyl-4-(10-oxo or -hydroxy-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidine compounds are prepared from the corresponding 10-desoxy compounds having a double bond at the 10,11-position by a process involving bromination, dehydrobomination of the resulting dibromo compound, followed by enamine formation and hydrolysis to give the desired 10-oxo compound. The compounds prepared in this manner are active as antihistamines and as appetite stimulants.

    摘要翻译： 从相应的10-脱氧化合物制备新的1-烷基-4-（10-氧代或 - 羟基-10,11-二氢-5H-二苯并[a，d]环庚烯-5-亚基） - 哌啶化合物，其具有 通过涉及溴化的方法在10,11位双键，得到的二溴化合物脱氢，然后进行烯胺形成和水解，得到所需的10-氧代化合物。 以这种方式制备的化合物作为抗组胺剂和作为食欲兴奋剂是有活性的。