Alkylamine derivatives of dihydropyridine NPY antagonists
    7.
    发明授权
    Alkylamine derivatives of dihydropyridine NPY antagonists 有权
    二氢吡啶NPY拮抗剂的烷基胺衍生物

    公开(公告)号:US06479482B2

    公开(公告)日:2002-11-12

    申请号:US09852983

    申请日:2001-05-10

    IPC分类号: C07D41714

    CPC分类号: C07D401/12 C07D211/90

    摘要: A series of non-peptidergic antagonists of NPY have been synthesized and are comprises of amino and piperazine derivatives of 4-phenyl-1,4-dihydropyridines of Formula 1. where X is CH or N As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

    摘要翻译: 已经合成了一系列NPY的非肽能拮抗剂,其由式1的4-苯基-1,4-二氢吡啶的氨基和哌嗪衍生物组成。其中X是NPY诱导行为的CH或NAs拮抗剂,这些化合物是 预期在促进减肥和治疗进食障碍中起到有效的厌氧剂的作用。

    Dihydropyrimidone derivatives as NPY antagonists
    8.
    发明授权
    Dihydropyrimidone derivatives as NPY antagonists 失效
    作为NPY拮抗剂的二氢嘧啶酮衍生物

    公开(公告)号:US5889016A

    公开(公告)日:1999-03-30

    申请号:US9534

    申请日:1998-01-20

    IPC分类号: C07D401/12 A61K31/505

    CPC分类号: C07D401/12

    摘要: The present invention provides a series of non-peptidergic antagonists of NPY comprising piperidine derivatives of 4-phenyl-1,4-dihydropyrimidinones of the Formula I ##STR1## wherein R, R.sup.1 and R.sup.2 are defined herein. As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

    摘要翻译: 本发明提供了一系列包含式I的4-苯基-1,4-二氢嘧啶酮的哌啶衍生物的NPY的非肽能拮抗剂,其中R,R 1和R 2在本文中定义。 作为NPY诱导的饲养行为的拮抗剂,预期这些化合物可用作促进减肥和治疗进食障碍的有效厌氧剂。

    Dihydro-3,5-dicarboxylates
    10.
    发明授权
    Dihydro-3,5-dicarboxylates 失效
    二氢-3,5-二羧酸二乙酯

    公开(公告)号:US4814455A

    公开(公告)日:1989-03-21

    申请号:US852856

    申请日:1986-04-16

    CPC分类号: C07D401/12 C07D211/90

    摘要: A series of compounds of the 1,4-dihydropyridine class with a 3-carboxylate group linked to an alkyleneaminoalkylene heteroatom have been prepared possessing the general formula ##STR1## wherein R.sup.2, R.sup.5 and R.sup.6 are independently selected from lower (C.sub.1-4)alkyl, hydroxy-lower-alkylene, lower alkoxy-lower-alkylene, lower alkylamino-lower-alkylene or lower dialkyl-amino-lower-alkylene; R.sup.7 is selected from hydrogen, lower alkyl, phenyl-lower-alkylene, or phenylthio-lower-alkylene; n is the integer 2 or 3; X is a chemical bond, --O--, --S--, ##STR2## or --NR.sup.9 -- wherein R.sup.9 is hydrogen, lower alkyl, phenyl, or phenyl-lower-alkylene with the proviso that when X is a chemical bond, Z is a 3-indolyl ring; and Z is selected from the group consisting of phenyl substituted with 1 to 3 substituents independently chosen from among hydrogen, lower alkyl, or lower alkoxy, phenyl-lower-alkylene, or 3-indolyl.Compounds of this series possess calcium channel blocking properties, afford protection against ischemia and inhibit aggregation of blood platelets.

    摘要翻译: 已经制备了一系列具有与亚烷基氨基亚烷基杂原子连接的3-羧酸酯基的1,4-二氢吡啶类的化合物,其具有通式“IMAGE”,其中R 2,R 5和R 6独立地选自低级(C 1-4)烷基 ,羟基 - 低级 - 亚烷基,低级烷氧基 - 低级 - 亚烷基,低级烷基氨基 - 低级 - 亚烷基或低级二烷基 - 氨基 - 低级 - 亚烷基; R 7选自氢,低级烷基,苯基 - 低级亚烷基或苯硫基 - 低级 - 亚烷基; n是整数2或3; 其中R为氢,低级烷基,苯基或苯基 - 低级亚烷基,条件是当X为化学键时,Z为化学键,-O - , - S-, 3-吲哚基环; 并且Z选自被1至3个独立地选自氢,低级烷基或低级烷氧基,苯基 - 低级亚烷基或3-吲哚基的取代基取代的苯基。 该系列化合物具有钙通道阻断性质,提供防止缺血和抑制血小板聚集的保护作用。