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53 条记录 (耗时 0.047 秒)

    N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
    41.
    发明授权
    N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists 失效
    N-（3-（4-取代-1-哌啶基）-1-苯基丙基）取代的磺酰胺作为N​​K-3受体拮抗剂

    公开(公告)号：US07153868B2

    公开(公告)日：2006-12-26

    申请号：US10417360

    申请日：2003-04-16

    申请人： Mark Stuart Chambers ,  Philip Jones ,  Helen Jane Szekeres

    发明人： Mark Stuart Chambers ,  Philip Jones ,  Helen Jane Szekeres

    IPC分类号： A61K31/445 ,  C07D401/06

    CPC分类号： C07D401/04 ,  A61K31/454 ,  A61K31/497 ,  C07D211/58 ,  C07D401/14 ,  C07D409/14

    摘要： The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明提供治疗患有诸如精神分裂症的受试者的方法，所述疾病包括施用NK-3拮抗剂，其包括向该受试者施用治疗有效量的式I化合物：其中 通常，Q是R 1是苄基，苯基，噻吩或任选被C 1-4烷基或卤素取代的咪唑基，例如甲基，氟或溴; R 2是氢或C 1-4烷基，例如甲基; R 3是苯基; R 4是氢; R 5是氢或C 1-6烷基羰基，例如甲基羰基; X是-SO 2 - 或-C（O）N（R 2）SO 2 - ，其中R 2 O / >优选为氢; Y是键，CH 2或Z 1，其中Z 1是-N（R f）， - 其中R 1是C 1-6烷基羰基，例如乙基羰基; R 6是苯基，吡唑基，吡啶基，嘧啶基或苯并咪唑烷基，任选地被一个或两个选自C 1-6烷基和苄基的基团取代，例如甲基，乙基和 苄基; 或其药学上可接受的盐。

    Substituted 1,2,3-triazolo[1,5-a]quinazolines for enhancing cognition
    47.
    发明授权
    Substituted 1,2,3-triazolo[1,5-a]quinazolines for enhancing cognition 失效
    取代的1,2,3-三唑并[1,5-a]喹唑啉用于增强认知

    公开(公告)号：US07144887B2

    公开(公告)日：2006-12-05

    申请号：US10149852

    申请日：2000-12-11

    申请人： Helen Jane Bryant ,  Mark Stuart Chambers ,  Philip Jones ,  Angus Murray MacLeod ,  Robert James Maxey

    发明人： Helen Jane Bryant ,  Mark Stuart Chambers ,  Philip Jones ,  Angus Murray MacLeod ,  Robert James Maxey

    IPC分类号： A61K471/04 ,  A61K31/505 ,  C07D239/00 ,  C07D471/00 ,  C07D487/00

    CPC分类号： C07D487/04

    摘要： The present invention provides a compound of formula (I) in which R1 is generally hydrogen or CF3, R2 is generally hydrogen, W is a cyclic amine, a heterocycle or a group L-Y—X where L-Y is a linking portion and X is generally an aromatic or non-aromatic heterocycle, alkyl or alkylcarbonyl and Z is generally a heterocycle such as 5-methylisoxazol-3-yl, and pharmaceutically acceptable salts thereof for enhancing cognition in conditions such as Alzheimer's Disease, pharmaceutical compositions comprising them, their use for manufacturing medicaments and methods of treatment using them

    摘要翻译： 本发明提供式（I）化合物，其中R 1通常是氢或CF 3，R 2通常是氢，W 是环状胺，杂环或LYX基团，其中LY是连接部分，X通常是芳族或非芳族杂环，烷基或烷基羰基，Z通常是杂环，例如5-甲基异恶唑-3-基和药学上 用于增强诸如阿尔茨海默氏病等疾病的认知的可接受的盐，包含它们的药物组合物，其用于制备药物的用途和使用它们的治疗方法