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    Novel tricyclic derivatives which are agonists of cholinergic receptors, and drugs in which they are present
    1.
    发明授权
    Novel tricyclic derivatives which are agonists of cholinergic receptors, and drugs in which they are present 失效
    作为胆碱能受体的激动剂的新型三环衍生物及其存在的药物

    公开(公告)号：US4977152A

    公开(公告)日：1990-12-11

    申请号：US471680

    申请日：1990-01-25

    申请人： Kathleen Biziere ,  Camille G. Wermuth ,  Paul Worms ,  Jean-Jacques Bourguignon

    发明人： Kathleen Biziere ,  Camille G. Wermuth ,  Paul Worms ,  Jean-Jacques Bourguignon

    IPC分类号： A61K31/50 ,  A61K31/502 ,  A61K31/535 ,  A61P25/28 ,  C07D237/26 ,  C07D237/36 ,  C07D403/12 ,  C07D413/12

    CPC分类号： C07D403/12 ,  C07D237/26 ,  C07D237/36 ,  C07D413/12

    摘要： The invention relates to novel tricyclic derivatives which are agonists of cholinergic receptors and to drugs containing them.These derivatives have the following formula: ##STR1## in which: X represents a group (CH.sub.2).sub.n, n representing an integer equal to 2, 3 or 4, or alternatively a vinylene group or a methylvinylene group;R.sub.1 and R.sub.2, considered independently, represent hydrogen or a substituent occupying one of the free positions of the benzene ring and selected from the group comprising halogens, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a thiol group, a nitro group and an optionally substituted amino group;Y represents oxygen, sulfur or a group --NH--; andR.sub.3 is an amino groupApplication: agonists of the cholinergic receptors.

    摘要翻译： 本发明涉及作为胆碱能受体的激动剂的新型三环衍生物和含有它们的药物。 这些衍生物具有下式：其中：X表示基团（CH 2）n，n表示等于2,3或4的整数，或者可选地是亚乙烯基或甲基亚乙烯基; 独立地考虑的R 1和R 2表示氢或占据苯环的一个游离位置的取代基，并且选自卤素，低级烷基，低级烷氧基，羟基，硫醇基，硝基 基团和任选取代的氨基; Y表示氧，硫或基团-NH-; 并且R3是氨基应用：胆碱能受体的激动剂。

    Tricyclic cholinergic receptor agonists
    2.
    发明授权
    Tricyclic cholinergic receptor agonists 失效
    三环胆碱能受体激动剂

    公开(公告)号：US4983603A

    公开(公告)日：1991-01-08

    申请号：US288861

    申请日：1988-12-23

    申请人： Camille G. Wermuth ,  Paul Worms ,  Jean-Jacques Bourguignon ,  Roger Brodin

    发明人： Camille G. Wermuth ,  Paul Worms ,  Jean-Jacques Bourguignon ,  Roger Brodin

    IPC分类号： A61K31/50 ,  A61P25/02 ,  C07D491/04 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04

    CPC分类号： C07D491/04 ,  C07D495/04

    摘要： The invention relates to novel tricyclic derivatives which are agonists of cholinergic receptors.These derivatives have the formula ##STR1## in which X=O, S, --OCH.sub.2 -- or --SCH.sub.2 --; R.sub.1 =H or halogen; and R.sub.2 = ##STR2## in which Alk is an alkylene group and R.sub.3, an R.sub.4, which are identical or different, are hydrogen or a lower alkyl group, or R.sub.3 and R.sub.4, with the nitrogen atom to which they are bonded, form a 5- or 6-membered cyclic amino group optionally containing a second heteroatom; or R.sub.2 is a group ##STR3## where R.sub.5 =C.sub.1 -C.sub.4 -alkyl. Application: agonists of cholinergic receptors.

    摘要翻译： 本发明涉及作为胆碱能受体激动剂的新型三环衍生物。 这些衍生物具有其中X = O，S，-OCH 2 - 或-SCH 2 - 的式（I） R1 = H或卤素; 和其中Alk是亚烷基的R 2 =＆lt; IMAGE＆gt; R 3，相同或不同的R 4是氢或低级烷基，或者R 3和R 4与它们相连的氮原子形成 任选地含有第二杂原子的5-或6-元环氨基; 或R 2为基团，其中R 5 = C 1 -C 4 - 烷基。 应用：胆碱能受体的激动剂。

    Imidazo[1,2-]pyridazines for cortical cholinergic deficiencies
    4.
    发明授权
    Imidazo[1,2-]pyridazines for cortical cholinergic deficiencies 失效
    咪唑并[1,2]哒嗪类皮质胆碱能缺陷

    公开(公告)号：US4910199A

    公开(公告)日：1990-03-20

    申请号：US238488

    申请日：1988-08-31

    申请人： Jean-Jacques Bourguignon ,  Camille G. Wermuth ,  Paul Worms

    发明人： Jean-Jacques Bourguignon ,  Camille G. Wermuth ,  Paul Worms

    IPC分类号： A61K31/50 ,  A61P25/02 ,  A61P25/28 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： The present invention relates to imidazo[1,2-b]-pyridazines having the formula: ##STR1## in which: R.sub.1 represents hydrogen, a halogen atom, a C.sub.1 -C.sub.4 alkoxy group or a C.sub.1 -C.sub.4 alkyl group occupying one of the free positions of the benzene ring; R.sub.2 represents hydrogen, a C.sub.1 -C.sub.4 alkyl group or a phenyl group; R.sub.3 denotes hydrogen, a C.sub.1 -C.sub.4 alkyl group or a phenyl group; and R.sub.4 R.sub.5 represent hydrogen or a C.sub.1 -C.sub.4 alkyl group, or R.sub.4 and R.sub.5 form, together with the nitrogen atom to which they are bonded, a 5-membered or 6-membered heterocycle optionally containing a second heteroatom. Application: drugs, especially for the treatment of cortical cholinergic deficiencies.

    摘要翻译： 本发明涉及具有下式的咪唑并[1,2-b] - 哒嗪，其中：R 1表示氢，卤素原子，C 1 -C 4烷氧基或C 1 -C 4烷基占据 苯环的自由位置之一; R2代表氢，C1-C4烷基或苯基; R3表示氢，C1-C4烷基或苯基; 并且R 4 R 5表示氢或C 1 -C 4烷基，或者R 4和R 5与它们所键合的氮原子一起形成任选含有第二杂原子的5元或6元杂环。 应用：药物，特别是用于治疗皮质胆碱能缺陷。

    Imidazo [1,2-c] quinazoline compounds
    9.
    发明授权
    Imidazo [1,2-c] quinazoline compounds 失效
    咪唑（1,2-C）喹唑啉化合物

    公开(公告)号：US5128338A

    公开(公告)日：1992-07-07

    申请号：US666802

    申请日：1991-03-08

    申请人： Jean-Jacques Bourguignon ,  Camille-Georges Wermuth ,  de la Faverie; Jean-Francois Renaud ,  Catherine Thollon ,  Alain Lombet

    发明人： Jean-Jacques Bourguignon ,  Camille-Georges Wermuth ,  de la Faverie; Jean-Francois Renaud ,  Catherine Thollon ,  Alain Lombet

    IPC分类号： A61K31/505 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： New imidazo [1,2-c] quinazoline compounds useful as coronary smooth muscle relaxants and corresponding to the formula: ##STR1## in which: Y is oxygen or sulfur;R.sub.1 is (C.sub.1 -C.sub.6) alkyl optionally substituted by a phenyl itself optionally substituted, a (C.sub.3 -C.sub.6) cycloalkyl, optionally substituted phenyl, furyl, thienyl or acyl;R.sub.2 is hydrogen, a halogen or a (C.sub.1 -C.sub.6) alkyl optionally substituted by amino or dialkylamino;R.sub.3 is hydrogen, (C.sub.1 -C.sub.6) alkyl optionally substituted by an aryl, or R--CO--(CH.sub.2).sub.n -- [n being 1, 2 or 3, and R being (C.sub.1 -C.sub.6) alkoxy, amino, (alkyl or dialkyl)amino, morpholino or methylpiperazinyl]; andX is hydrogen or a halogen.These compounds and their physiologically tolerated salts can be used in medical treatment of coronary smooth-muscle dysfunctions.

    摘要翻译： 新的咪唑并[1,2-c]喹唑啉化合物，可用作冠状平滑肌松弛剂，对应于下式：其中：Y为氧或硫; R 1是任选被苯基本身任选取代的（C 1 -C 6）烷基，（C 3 -C 6）环烷基，任选取代的苯基，呋喃基，噻吩基或酰基; R 2是氢，卤素或任选被氨基或二烷基氨基取代的（C 1 -C 6）烷基; R 3是氢，任选被芳基取代的（C 1 -C 6）烷基，或R-CO-（CH 2）n - [n是1,2或3，并且R是（C 1 -C 6）烷氧基，氨基，（烷基或 二烷基）氨基，吗啉代或甲基哌嗪基]; X是氢或卤素。 这些化合物及其生理耐受盐可用于治疗冠状动脉平滑肌功能障碍。