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69 条记录 (耗时 0.051 秒)

    Pyridine Derivatives and Their Use in The Treatment of Psychotic Disorders
    61.
    发明申请
    Pyridine Derivatives and Their Use in The Treatment of Psychotic Disorders 有权

    公开(公告)号：US20100152175A1

    公开(公告)日：2010-06-17

    申请号：US12636849

    申请日：2009-12-14

    申请人： Giuseppe Alvaro ,  Daniele Andreotti ,  Sandro Belvedere ,  Romano Di Fabio ,  Alessandro Falchi ,  Riccardo Giovannini

    发明人： Giuseppe Alvaro ,  Daniele Andreotti ,  Sandro Belvedere ,  Romano Di Fabio ,  Alessandro Falchi ,  Riccardo Giovannini

    IPC分类号： A61K31/5383 ,  A61P25/30

    CPC分类号： C07D487/04 ,  C07D513/04

    摘要： There are provided according to the invention novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein: X represents a nitrogen atom; Y represents —C(H2)—, (—C(H2)—)2, —S(O2)— or —C(═O)—; Z represents —C(H2)—, —S(O2)—, —N(Rz)—, or an oxygen or sulphur atom; A represents hydrogen or —CH2OH; Rz represents hydrogen, C1-6 alkyl, C1-6 alkoxy, —COR7 or —SO2R7; R1 represents halogen, C1-6 alkyl, C1-6 alkoxy, ═O, haloC1-6 alkyl, haloC1-6 alkoxy, hydroxyl or —CH2OH; m represents an integer from 0 to 3; R2 represents halogen, ═O, C1-6 alkyl (optionally substituted by one or more hydroxyl groups), —COOR7, —CONR7R8, C1-6 alkoxy, haloC1-6 alkyl, haloC1-6 alkoxy or C1-6alkylOC1-6alkyl; n represents an integer from 0 to 3; p and q independently represent an integer from 0 to 2; R3 represents an -aryl, -heteroaryl, -heterocyclyl, -aryl-aryl, -aryl-heteroaryl, -aryl-heterocyclyl, -heteroaryl-aryl, -heteroaryl-heteroaryl, -heteroaryl-heterocyclyl, -heterocyclyl-aryl, -heterocyclyl-heteroaryl or -heterocyclyl-heterocyclyl group, all of which may be optionally substituted by one or more (e.g. 1, 2 or 3) halogen, C1-6 alkyl (optionally substituted by one or more hydroxyl groups), C3-8 cycloalkyl, C1-6 alkoxy, hydroxyl, haloC1-6 alkyl, haloC1-6 alkoxy, cyano, —S—C1-6 alkyl, —SO—C1-6 alkyl, —SO2—C1-6 alkyl, —COR7, —CONR7R8, —NR7R8, —NR7COC1-6 alkyl, —NR7SO2—C1-6 alkyl, C1-6 alkyl-NR7R8, —OCONR7R8, —NR7CO2R8 or —SO2NR7R8 groups; R4 and R5 independently represent C1-6 alkyl, or R4 and R5 together with the carbon atom to which they are attached may together form a C3-8 cycloalkyl group; R6 represents halogen, C1-6 alkyl, C3-8 cycloalkyl, C1-6 alkoxy, haloC1-6 alkyl or haloC1-6 alkoxy; s represents an integer from 0 to 4; R7 and R8 independently represent hydrogen, C1-6 alkyl or C3-8 cycloalkyl; or solvates thereof.

    Chemical compounds
    62.
    发明授权
    Chemical compounds 失效
    化合物

    公开(公告)号：US07691893B2

    公开(公告)日：2010-04-06

    申请号：US11851459

    申请日：2007-09-07

    申请人： Romano Di Fabio

    发明人： Romano Di Fabio

    IPC分类号： A61K31/403 ,  C07D209/52

    CPC分类号： C07D221/04

    摘要： The present invention relates to (1S,6R)-6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane, pharmaceutically acceptable salts, prodrugs or solvates thereof; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.

    摘要翻译： 本发明涉及（1S，6R）-6-（3,4-二氯苯基）-1 - [（甲氧基）甲基] -3-氮杂双环[4.1.0]庚烷，其药学上可接受的盐，前药或溶剂合物; 再摄入抑制剂，作为5-羟色胺（5-HT），多巴胺（DA）和去甲肾上腺素（NE），再摄取抑制剂，它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的应用。

    Chemical compounds
    64.
    发明授权
    Chemical compounds 有权
    化合物

    公开(公告)号：US07060702B2

    公开(公告)日：2006-06-13

    申请号：US10994605

    申请日：2004-11-22

    申请人： Giuseppe Alvaro ,  Romano Di Fabio ,  Paolo Maragni ,  Marsia Tampieri ,  Maria Elvira Tranquillini

    发明人： Giuseppe Alvaro ,  Romano Di Fabio ,  Paolo Maragni ,  Marsia Tampieri ,  Maria Elvira Tranquillini

    IPC分类号： A61K31/496 ,  C07D401/04

    CPC分类号： A61K31/496 ,  C07D211/58

    摘要： The present invention provides compounds of formula (I): wherein each R independently represents a halogen atom or a C1-4 alkyl group; R1 represents a C1-4 alkyl group; R2 represents hydrogen or a C1-4 alkyl group; R3 represents hydrogen or C1-4 alkyl group; R4 represents a trifluoromethyl group; R5 represents hydrogen, a C1-4 alkyl group or C(O)R6; R6 represents C1-4 alkyl, C3-7 cycloalkyl, NH(C1-4 alkyl) or N(C1-4alkyl)2; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; or a pharmaceutically acceptable salt or solvate thereof; compositions containing the same, processes for their preparation and methods for their use in the treatment of conditions mediated by tachykinins.

    摘要翻译： 本发明提供式（I）化合物：其中每个R独立地表示卤素原子或C 1-4烷基; R 1表示C 1-4烷基; R 2表示氢或C 1-4烷基; R 3表示氢或C 1-4烷基; R 4表示三氟甲基; R 5表示氢，C 1-4烷基或C（O）R 6; R 6表示C 1-4烷基，C 3-7环烷基，NH（C 1-4烷基） ）或N（C 1-4烷基）2。 m为0或1〜3的整数; n为1〜3的整数， 或其药学上可接受的盐或溶剂化物; 含有它们的组合物，其制备方法和用于治疗由速激肽介导的病症使用的方法。

    Piperidine derivatives
    67.
    发明申请
    Piperidine derivatives 有权
    哌啶衍生物

    公开(公告)号：US20050176715A1

    公开(公告)日：2005-08-11

    申请号：US10502255

    申请日：2003-02-10

    申请人： Giuseppe Alvaro ,  Romano Di Fabio ,  Maria Tranquillini ,  Simone Spada

    发明人： Giuseppe Alvaro ,  Romano Di Fabio ,  Maria Tranquillini ,  Simone Spada

    IPC分类号： A61K31/4985 ,  A61P1/08 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D487/04 ,  A61K31/498

    CPC分类号： C07D487/04 ,  A61K31/445

    摘要： The present invention relates to piperidine derivatives of formula (I): R represents halogen or C1-4 alkyl R1 represents C1-4 alkyl; R2 or R3 independently represent hydrogen or C1-4 alkyl; R4 represents trifluoromethyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy or halogen; R5 represents hydrogen, C1-4 alkyl or C3-7 cycloalkyl; R6 is hydrogen and R7 is a radical of formula (W): or R6 is a radical of formula (W) and R7 is hydrogen; X represents CH2, NR5 or O; Y represents Nitrogen and Z is CH or Y represents CH and Z is Nitrogen; A represents C(O) or S(O)q, provided that when Y is nitrogen and Z is CH, A is not S(O)q; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; p and q are independently an integer from 1 to 2; and pharmaceutically acceptable salts and solvates thereof. The process for their preparation and their use in the treatment of a condition mediated by tachykinins.

    摘要翻译： 本发明涉及式（I）的哌啶衍生物：R表示卤素或C 1-4烷基R 1表示C 1-4烷基， 烷基; R 2或R 3独立地表示氢或C 1-4烷基; R 4表示三氟甲基，C 1-4烷基，C 1-4烷氧基，三氟甲氧基或卤素; R 5表示氢，C 1-4烷基或C 3-7环烷基; R 6是氢，R 7是式（W）的基团：或R 6是式（W）的基团，R 7是氢; X表示CH 2，NR 5或O; Y表示氮，Z表示CH或Y表示CH，Z表示氮; A表示C（O）或S（O）q，条件是当Y为氮且Z为CH时，A不为S（O）q。 m为0或1〜3的整数; n为1〜3的整数， p和q独立地为1至2的整数; 及其药学上可接受的盐和溶剂化物。 其制备方法及其用于治疗由速激肽介导的病症。