Carboxamidothiazole derivatives, preparation, pharmaceutical compositions containing them
    1.
    发明授权
    Carboxamidothiazole derivatives, preparation, pharmaceutical compositions containing them 失效
    载体酰胺噻唑衍生物,制剂,含有它们的药物组合物

    公开(公告)号:US06380230B1

    公开(公告)日:2002-04-30

    申请号:US09508830

    申请日:2000-06-02

    IPC分类号: C07D41712

    摘要: The present invention relates to cholecystokinin (CCK)-agonist substituted thiazoles of formula: in which R1 is a substituted phenyl group, R2 is a group chosen from CH2—R7, (CH2)2—R7, S—CH2—R7, CH2—S—R7 and (C5-C8)alkyl with R7 being a (C5-C7)cycloalkyl group, and R3 is a group with R8 being a group (CH2)nR15 or and R15 being COOH or COO(C1-C4)alkyl. The invention also relates to a process for the preparation of the pharmaceutical compositions containing them and to their uses for the preparation of medicines.

    摘要翻译: 本发明涉及下列通式的缩胆囊素(CCK) - 拮抗剂取代的噻唑:其中R1是取代的苯基,R2是选自CH2-R7,(CH2)2-R7,S-CH2-R7,CH2- S-R7和(C5-C8)烷基,其中R7是(C5-C7)环烷基,R3是具有R8(CH 2)nR15的基团,R15是COOH或COO(C1-C4)烷基)。 本发明还涉及制备含有它们的药物组合物及其用于制备药物的用途的方法。

    Derivatives of 1,3,4-thiadiazole, a method of obtaining them and
pharmaceutical compositions containing them
    8.
    发明授权
    Derivatives of 1,3,4-thiadiazole, a method of obtaining them and pharmaceutical compositions containing them 失效
    1,3,4-噻二唑的衍生物,获得它们的方法和含有它们的药物组合物

    公开(公告)号:US5086053A

    公开(公告)日:1992-02-04

    申请号:US394321

    申请日:1989-08-16

    摘要: The present invention relates to thiadiazole derivatives having the formula: ##STR1## in which: R.sub.1 represents a phenyl group, non-substituted or substitued 1 to 3 times by a halogen atom, preferably chlorine or fluorine, or by a C.sub.1 -C.sub.4 alkyl group, preferably the methyl group, or by a C.sub.1 -C.sub.4 alkoxy group, preferably the methoxy group, or by a hydroxy group or by a trifluoromethyl group or a phenyl group substituted simultaneously by 1 to 3 halogen atoms and by 1 or 2 methyl groupings;R.sub.2 represents hydrogen or a C.sub.1 -C.sub.4 alkyl group,R.sub.3 represents an alkylamino group or a heterocyclic group,Application: Drugs for treatment of notably senile dementia.

    摘要翻译: 本发明涉及具有下式的噻二唑衍生物:其中:R 1表示苯基,被卤素原子,优选氯或氟或未被取代或取代1至3倍的苯基,或由C1- C4烷基,优选甲基,或通过C1-C4烷氧基,优选甲氧基,或羟基或被同时被1至3个卤素原子取代的三氟甲基或苯基取代,以及1或2个 甲基组; R2表示氢或C1-C4烷基,R3表示烷基氨基或杂环基。应用:用于治疗特别是老年性痴呆的药物。

    Thiadiazole derivatives active on the central nervous system and
pharmaceutical compositions
    9.
    发明授权
    Thiadiazole derivatives active on the central nervous system and pharmaceutical compositions 失效
    对中枢神经系统有活性的噻二唑衍生物和药物组合物

    公开(公告)号:US4596802A

    公开(公告)日:1986-06-24

    申请号:US786465

    申请日:1985-10-11

    CPC分类号: C07D285/12 C07D285/135

    摘要: The invention relates to thiadiazole derivatives corresponding to the formula: ##STR1## in which R represents: a linear or branched alkyl group having from 1 to 5 carbon atoms;a cycloalkyl group having 5 or 6 carbon atoms;a phenyl group optionally substituted by 1 or 2 halogen atoms, preferably chlorine, by 1 or 2 lower alkyl or lower alkoxy groups, by 1 or 2 hydroxyl groups or by a nitro or trifluoromethyl group;a biphenylyl group; oran alpha-naphthyl group;and the pharmaceutically acceptable salts of the said derivatives. It also relates to a process for the preparation of the said derivatives and the pharmaceutical compositions in which they are present. The said derivatives act on the central nervous system.

    摘要翻译: 本发明涉及对应于下式的噻二唑衍生物:其中R表示:具有1至5个碳原子的直链或支链烷基; 具有5或6个碳原子的环烷基; 任选被1或2个卤素原子,优选氯,1或2个低级烷基或低级烷氧基,1或2个羟基或硝基或三氟甲基取代的苯基; 联苯基; 或α-萘基; 和所述衍生物的药学上可接受的盐。 它还涉及制备所述衍生物的方法及其存在的药物组合物。 所述衍生物对中枢神经系统起作用。

    Tricyclic cholinergic receptor agonists
    10.
    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

    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 =< IMAGE> 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。