Novel 1,4-diazabicycloalkane derivatives, their preparation and use
    54.
    发明申请
    Novel 1,4-diazabicycloalkane derivatives, their preparation and use 有权
    新型1,4-二氮杂双环链烷烃衍生物,其制备和应用

    公开(公告)号:US20060122172A1

    公开(公告)日:2006-06-08

    申请号:US10528361

    申请日:2003-09-29

    IPC分类号: C07D487/04 A61K31/551

    CPC分类号: C07D471/08 C07D487/04

    摘要: This invention relates to novel 1,4-diazabicycloalkane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention 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1,4-二氮杂双环链烷烃衍生物及其在制备药物组合物中的用途。 发现本发明的化合物是烟碱乙酰胆碱受体的胆碱能配体和单胺受体和转运蛋白的调节剂。 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。

    Heteroaryl diazacycloalkanes, their preparation and use
    55.
    发明申请
    Heteroaryl diazacycloalkanes, their preparation and use 失效
    杂芳基二氮杂环烷烃,其制备和用途

    公开(公告)号:US20060100192A1

    公开(公告)日:2006-05-11

    申请号:US11312574

    申请日:2005-12-21

    IPC分类号: A61K31/551 C07D403/02

    摘要: The present invention relates to novel heteroaryl diazacycloalkane derivatives, which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. 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), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

    摘要翻译: 本发明涉及新颖的杂芳基二氮杂环烷烃衍生物,其在烟碱乙酰胆碱受体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)的胆碱能系统有关的疾病或病症,与平滑肌收缩相关的疾病或病症,内分泌疾病或 与神经变性相关的疾病,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。

    Novel aryl ureido benzoic acid derivatives and their use
    56.
    发明申请
    Novel aryl ureido benzoic acid derivatives and their use 失效
    新型芳基脲基苯甲酸衍生物及其用途

    公开(公告)号:US20060069255A1

    公开(公告)日:2006-03-30

    申请号:US10535683

    申请日:2003-11-10

    IPC分类号: C07D271/06 C07D211/82

    摘要: This invention relates to novel aryl ureido benzoic acid derivatives useful as selective and non-competitive antagonists of the ionotropic GluR5 receptor. Due to their biological activity, the aryl ureido derivatives of the invention are considered useful for treating diseases that are responsive to modulation of an aspartate or a glutamate receptor. Moreover the invention provides chemical compounds for use according to the invention, as well as pharmaceutical compositions comprising the chemical compounds, and methods of treating diseases or disorders or conditions responsive to modulation of an aspartate or a glutamate receptor.

    摘要翻译: 本发明涉及可用作离子型GluR5受体的选择性和非竞争性拮抗剂的新型芳基脲基苯甲酸衍生物。 由于其生物学活性,本发明的芳基脲基衍生物被认为可用于治疗对天冬氨酸或谷氨酸受体的调节有反应的疾病。 此外,本发明提供了根据本发明使用的化合物,以及包含化合物的药物组合物,以及治疗对天冬氨酸或谷氨酸受体的调节作用的疾病或病症或病症的方法。

    Disubstituted morpholine, oxazepine or thiazepine derivatives, their preparation and their use as dopamine d4 receptor antagonists
    60.
    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。