Disubstituted morpholine, oxazepine or thiazepine derivatives, their preparation and their use as dopamine d4 receptor antagonists
    8.
    发明授权
    Disubstituted morpholine, oxazepine or thiazepine derivatives, their preparation and their use as dopamine d4 receptor antagonists 失效
    二取代的吗啉,氧氮杂或硫氮衍生物,其制备及其作为多巴胺d4受体拮抗剂的用途

    公开(公告)号:US06479491B1

    公开(公告)日:2002-11-12

    申请号:US09709297

    申请日:2000-11-13

    IPC分类号: A61K31535

    摘要: The present invention relates to compounds of formula (I), any of it enantiomers, or any mixture thereof, or a pharmaceutically acceptable acid addition salt thereof, wherein R1, R2, R3, R4, R11, R12, R13, R14 and R15 each independently are hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, nitro, cyano, amino, acyl, alkylamino, dialkylamino, aminocarbonyl, or acylamino; R5 is hydrogen, alkyl, alkoxyalkyl, or phenylalkyl; X is —CH2—Z—, Z—CH2—, NH—CO—, —CO—NH—, or —CH═CH—; wherein Z is O, S, CH2, or NH; Y is O, —CH2—W—, —W—CH2—; wherein W is O, or S; and n is 0, 1 or 2. The compounds are useful in the treatment of psychotic disorders.

    摘要翻译: 本发明涉及式(I)化合物,其任何对映异构体或其任何混合物或其药学上可接受的酸加成盐,其中R 1,R 2,R 3,R 4,R 11,R 12,R 13,R 14和R 15各自 氰基,氨基,酰基,烷基氨基,二烷基氨基,氨基羰基或酰氨基; R5是氢,烷基,烷氧基烷基或苯基烷基; X是-CH 2 -Z-,Z-CH 2 - ,NH-CO - , - CO-NH-或-CH = CH-; 其中Z是O,S,CH 2或NH; Y是O,-CH 2 -W-,-W-CH 2 - ; 其中W是O或S; 并且n为0,1或2.该化合物可用于治疗精神病。

    Disubstituted morpholine, oxazepine or thiazepine derivatives, their preparation and their use as dopamine D4 receptor antagonists
    9.
    发明授权
    Disubstituted morpholine, oxazepine or thiazepine derivatives, their preparation and their use as dopamine D4 receptor antagonists 失效
    二取代的吗啉,氧氮杂或硫氮衍生物,其制备及其作为多巴胺D4受体拮抗剂的用途

    公开(公告)号:US06207662B1

    公开(公告)日:2001-03-27

    申请号:US09242693

    申请日:1999-02-23

    IPC分类号: A61K3155

    摘要: The present invention relates to compounds of formula (I), any of it enantiomers, or any mixture thereof, or a pharmaceutically acceptable acid addition salt thereof, wherein R1, R2, R3, R4, R11, R12, R13, R14 and R15 each independently are hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, nitro, cyano, amino, acyl, alkylamino, dialkylamino, aminocarbonyl, or acylamino; R5 is hydrogen, alkyl, alkoxyalkyl, or phenylalkyl; X is —CH2—Z—, Z—CH2—, NH—CO—, —CO—NH—, or —CH═CH—; wherein Z is O, S, CH2, or NH; Y is O, —CH2—W—, —W—CH2—; wherein W is O, or S; and n is 0, 1 or 2. The compounds are useful in the treatment of psychotic disorders.

    摘要翻译: 本发明涉及式(I)化合物,其任何对映异构体或其任何混合物或其药学上可接受的酸加成盐,其中R 1,R 2,R 3,R 4,R 11,R 12,R 13,R 14和R 15各自 氰基,氨基,酰基,烷基氨基,二烷基氨基,氨基羰基或酰氨基; R5是氢,烷基,烷氧基烷基或苯基烷基; X是-CH 2 -Z-,Z-CH 2 - ,NH-CO - , - CO-NH-或-CH = CH-; 其中Z是O,S,CH 2或NH; Y是O,-CH 2 -W-,-W-CH 2 - ; 其中W是O或S; 并且n为0,1或2.该化合物可用于治疗精神病。

    3, 9-diazabicyclo(3.3.1)non-3-yl-aryl methanone derivatives as nicotinic acetylcholine receptor agonists
    10.
    发明授权
    3, 9-diazabicyclo(3.3.1)non-3-yl-aryl methanone derivatives as nicotinic acetylcholine receptor agonists 失效
    3,9-二氮杂双环(3.3.1)壬-3-基 - 芳基甲酮衍生物作为烟碱乙酰胆碱受体激动剂

    公开(公告)号:US07855208B2

    公开(公告)日:2010-12-21

    申请号:US12160567

    申请日:2007-02-13

    CPC分类号: C07D471/08

    摘要: This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

    摘要翻译: 本发明涉及新的二氮杂双环芳基衍生物,其在烟碱乙酰胆碱受体和单胺受体和转运蛋白的调节剂中被发现是胆碱能配体。 由于其药理学特征,本发明的化合物可用于治疗与中枢神经系统(CNS),周围神经系统(PNS),疾病或病症相关的胆碱能系统相关的疾病或障碍 平滑肌肉收缩,内分泌疾病或病症,与神经变性相关的疾病或病症,与由化学物质的滥用终止引起的炎症,疼痛和戒断症状相关的疾病或病症。