4-Phenyl-1-piperazinyl, -piperidinyl and-tetrahydropyridyl derivatives
    42.
    发明申请
    4-Phenyl-1-piperazinyl, -piperidinyl and-tetrahydropyridyl derivatives 失效
    4-苯基-1-哌嗪基,哌啶基和四氢吡啶基衍生物

    公开(公告)号:US20060148815A1

    公开(公告)日:2006-07-06

    申请号:US11377772

    申请日:2006-03-15

    摘要: The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W is N or CH; X is CH2, O, S, CO, CS, SO or SO2; and Q is a group of formula wherein Z is a chain of 3 to 4 chain members; wherein the chain members are selected from C, CH, CH2, CO, N and NH, provided that only one of the chain members may be N or NH, and said chain optionally containing one or two double bonds; provided that X is not O or S when the group Q is attached via an N atom; and any of its enantiomers and acid addition salts thereof. These compounds have high affinity for D4 receptors.

    摘要翻译: 本发明涉及具有式I的取代的4-苯基-1-哌嗪基衍生物,其中W是C,CH或N,当W是C时,由W发出的虚线表示键,当W是N或CH时,没有键 ; X是CH 2,O,S,CO,CS,SO或SO 2; Q为下式的基团,其中Z为3至4个链成员的链; 其中链成员选自C,CH,CH 2,CO,N和NH,条件是链中只有一个可以是N或NH,并且所述链任选地含有一个或两个双 债券 条件是当基团Q经由N原子连接时,X不为O或S; 及其任何对映异构体及其酸加成盐。 这些化合物对D 4 S受体具有高亲和力。

    4-, 5-, 6- And 7-indole derivatives useful for the treatment of CNS disorders

    公开(公告)号:US20060004022A1

    公开(公告)日:2006-01-05

    申请号:US11219544

    申请日:2005-09-01

    摘要: The present invention relates to 4-, 5-, 6- or 7-methylene substituted indolyl derivatives of formula I wherein R is aryl or heteroaryl, where said aryl or heteroaryl groups may be substituted one or more times with a substituent seleceted from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, C1-6-alkoxy, C1-6-alkylthio, hydroxy, hydroxy-C1-6-alkyl trifluoromethyl, trifluoromethylsulfonyl, C1-6-alkylsulfonyl, amino, C1-6-alkylamino, di-(C1-6-alkyl)amino, acyl, aminocarbonyl and a methylene dioxy group; X is N, C or CH; provided that the dotted line indicates a bond when X is C and no bond when X is N or CH; R1 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, aryl, aryl-C1-6-alkyl, acyl, thioacyl, C1-6-alkylsulfonyl, trifluoromethylsulfonyl or arylsulfonyl; and R2 and R3 are independently selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, C1-6-alkoxy, C1-6-alkylthio, hydroxy, hydroxy-C1-6-alkyl trifluoromethyl, trifluoromethylsulfonyl, C1-6-alkylsulfonyl, amino, C1-6-alkylamino, di-(C1-6-alkyl)amino, acyl and aminocarbonyl. The compounds of the invention are selective dopamine D4 ligands.

    4-,5-,6-and 7-indole derivatives useful for the treatment of CNS disorders

    公开(公告)号:US06958338B2

    公开(公告)日:2005-10-25

    申请号:US10359052

    申请日:2003-02-04

    摘要: The present invention relates to 4-, 5-, 6- or 7-methylene substituted indolyl derivatives of formula I wherein R is aryl or heteroaryl, where said aryl or heteroaryl groups may be substituted one or more times with a substituent selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, C1-6-alkoxy, C1-6-alkylthio, hydroxy, hydroxy-C1-6-alkyl trifluoromethyl, trifluoromethylsulfonyl, C1-6-alkylsulfonyl, amino, C1-6-alkylamino, di-(C1-6-alkyl)amino, acyl, aminocarbonyl and a methylene dioxy group; X is N, C or CH; provided that the dotted line indicates a bond when X is C and no bond when X is N or CH; R1 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, aryl, aryl-C1-6-alkyl, acyl, thioacyl, C1-6-alkylsulfonyl, trifluoromethylsulfonyl or arylsulfonyl; and R2 and R3 are independently selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, C1-6-alkoxy, C1-6-alkylthio, hydroxy, hydroxy-C1-6-alkyl trifluoromethyl, trifluoromethylsulfonyl, C1-6-alkylsulfonyl, amino, C1-6-alkylamino, di-(C1-6-alkyl)amino, acyl and aminocarbonyl. The compounds of the invention are selective dopamine D4 ligands.

    Crystalline base of trans-1-((1R,3S)-6-chloro-3-phenylindan-1-yl)-3,3-dimethylpiperazine
    46.
    发明授权
    Crystalline base of trans-1-((1R,3S)-6-chloro-3-phenylindan-1-yl)-3,3-dimethylpiperazine 有权
    反式-1 - ((1R,3S)-6-氯-3-苯基茚满-1-基)-3,3-二甲基哌嗪的结晶基

    公开(公告)号:US08450324B2

    公开(公告)日:2013-05-28

    申请号:US12628613

    申请日:2009-12-01

    IPC分类号: A61K31/4965

    CPC分类号: C07D295/073

    摘要: Crystalline base of compound trans-1-((1R,3S)-6-chloro-3-phenylindan-1-yl)-3,3-dimethylpiperazine, processes for the preparation of purified free base or salts of this compound, pharmaceutical compositions comprising the base and medical use thereof, including for treatment of schizophrenia and other psychotic disorders.

    摘要翻译: 化合物反式-1 - ((1R,3S)-6-氯-3-苯基茚-1-基)-3,3-二甲基哌嗪的结晶碱,该化合物的纯化游离碱或盐的制备方法,药物组合物 包括其基础和医疗用途,包括用于治疗精神分裂症和其他精神病。