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    Chemical compounds
    22.
    发明申请
    Chemical compounds 有权
    化合物

    公开(公告)号：US20050137208A1

    公开(公告)日：2005-06-23

    申请号：US10994605

    申请日：2004-11-22

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

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

    IPC分类号： A61K31/445 ,  A61K31/496 ,  A61P25/00 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/32 ,  A61P25/36 ,  C07D211/58 ,  C07D43/02

    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
    24.
    发明申请
    Piperidine Derivatives 审中-公开
    哌啶衍生物

    公开(公告)号：US20100152446A1

    公开(公告)日：2010-06-17

    申请号：US12633265

    申请日：2009-12-08

    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： C07D487/04

    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 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; R1表示C1-4烷基; R2或R3独立地表示氢或C1-4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; R5代表氢，C1-4烷基或C3-7环烷基; R6是氢，R7是式（W）的基团：或R6是式（W）的基团，R7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。

    Piperidine derivatives
    25.
    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。

    Tri-and tetraaza-acenaphthylen derivatives as CRF receptor antagonists
    27.
    发明授权
    Tri-and tetraaza-acenaphthylen derivatives as CRF receptor antagonists 失效
    三 - 和四氮杂苊烯衍生物作为CRF受体拮抗剂

    公开(公告)号：US07446108B2

    公开(公告)日：2008-11-04

    申请号：US10477886

    申请日：2002-05-21

    申请人： Romano Di Fabio ,  Gabriella Gentile ,  Yves St Denis

    发明人： Romano Di Fabio ,  Gabriella Gentile ,  Yves St Denis

    IPC分类号： A01N43/54 ,  C07D239/00

    CPC分类号： C07D471/16

    摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, R1, R2, R4, R5, R6, A, X, and Y are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.

    摘要翻译： 公开了CRF受体拮抗剂，其可用于治疗各种疾病，包括治疗在温血动物（例如中风）中表现出CRF过度分泌的病症。 本发明的CRF受体拮抗剂具有以下结构：包括立体异构体，其前药和药学上可接受的盐，R 1，R 2，R 4， R 5，R 6，A，X和Y如本文所定义。 还公开了含有CRF受体拮抗剂与药学上可接受的载体的组合物，以及其用途的方法。

    Chemical Compounds
    30.
    发明申请
    Chemical Compounds 审中-公开

    公开(公告)号：US20070219232A1

    公开(公告)日：2007-09-20

    申请号：US11749433

    申请日：2007-05-16

    申请人： Romano Di Fabio ,  Fabrizio Micheli ,  Yves St-Denis

    发明人： Romano Di Fabio ,  Fabrizio Micheli ,  Yves St-Denis

    IPC分类号： A61K31/44 ,  C07D211/00 ,  C07D471/00

    CPC分类号： C07D471/04

    摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —C(O)R5, nitro, —NR6R7, cyano, and a group R8; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR6R7 or cyano; R2 is hydrogen, C3-C7 cycloalkyl, or a group R9; R3 is C3-C7 cycloalkyl, or a group R9; or R2 and R3 together with N form a 5-14 membered heterocycle, which may be substituted by 1 to 3 R10 groups; R4 is hydrogen, C1-C6 alkyl, halogen or halo C1-C6 alkyl; R5 is a C1-C4 alkyl, —OR6 or —NR6R7; R6 is hydrogen or C1-C6 alkyl; R7 is hydrogen or C1-C6 alkyl; R8 is a 5-6 membered heterocycle, which may be saturated or may contain one to three double bonds, and which may be substituted by 1 or more R11 groups; R9 is a C1-C6 alkyl that may be substituted by one or more groups selected from: C3-C7 cycloalkyl, C1-C6 alkoxy, haloC1-C6 alkoxy, hydroxy, haloC1-C6 alkyl; R10 is a group R8, C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, C(O)NR6R7, phenyl which may be substituted by 1 to 4 R11 groups; R11 is C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, or C(O)NR6R7; X is carbon or nitrogen; n is 1 or 2; to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).