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    Tri-and tetraaza-acenaphthylen derivatives as CRF receptor antagonists
    2.
    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。

    Beta-Lactams for Treatment of Cns Disorders
    3.
    发明申请
    Beta-Lactams for Treatment of Cns Disorders 审中-公开
    用于治疗Cns病的β-内酰胺类

    公开(公告)号：US20080262041A1

    公开(公告)日：2008-10-23

    申请号：US10595662

    申请日：2004-11-10

    申请人： Giuseppe Alvaro ,  Romano Di Fabio ,  Riccardo Giovannini ,  Alfredo Paio ,  Maria Elvira Tranquillini ,  Lucia Mattioli

    发明人： Giuseppe Alvaro ,  Romano Di Fabio ,  Riccardo Giovannini ,  Alfredo Paio ,  Maria Elvira Tranquillini ,  Lucia Mattioli

    IPC分类号： A61K31/4439 ,  A61K31/4025 ,  C07D401/04 ,  A61P25/18 ,  A61P25/24 ,  A61P19/02 ,  C07D403/04

    CPC分类号： C07D401/04

    摘要： The present invention relates to novel compounds of formula (I): wherein — represents a single or a double bond; R is a radical selected from: in which R1 is halogen, cyano, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy and p is zero or an integer from 1 to 3; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen, hydroxy or C1-4 alkyl; R4 is hydrogen or R4 together with R3 represents ═O or ═CH2; R5 is phenyl, naphthyl, a 9 to 10 membered fused bicyclic heterocyclic group or a 5 or 6 membered heteroaryl group, wherein said groups are optionally substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, hydroxy, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or S(O)qC1-4 alkyl; R6 and R7 independently are hydrogen, cyano, C1-4 alkyl; R8 is (CH2)rR10; R9 is hydrogen, halogen, C3-7 cycloalkyl, hydroxy, nitro, cyano or C1-4 alkyl optionally substituted by one or two groups selected from halogen, cyano, hydroxy or C1-4 alkoxy; R10 is hydrogen or C3-7 cycloalkyl; n is 1 or 2; q is 0, 1 or 2; r is 0 or an integer from 1 to 4; or a pharmaceutically acceptable salt or a solvate thereof, process for their preparation and their use in the treatment of conditions mediated by tackykinins and/or by selective inhibition of the serotonin reuptake transporter protein

    摘要翻译： 本发明涉及新的式（I）化合物：其中 - 表示单键或双键; R是选自以下的基团：其中R 1是卤素，氰基，C 1-4烷基，C 1-4烷氧基，三氟甲基 或三氟甲氧基，p为0或1至3的整数; R 2是氢或C 1-4烷基; R 3是氢，羟基或C 1-4烷基; R 4是氢或R 4与R 3一起代表-O或-CH 2; R 5是苯基，萘基，9至10元稠合双环杂环基或5或6元杂芳基，其中所述基团任选被1至3个独立地选自三氟甲基， 烷基，羟基，氰基，C 1-4烷氧基，三氟甲氧基，卤素或S（O）q C 1-4烷基; R 6和R 7独立地是氢，氰基，C 1-4烷基; R 8是（CH 2 2）r R 10; R 9是氢，卤素，C 3-7环烷基，羟基，硝基，氰基或C 1-4烷基，任选被一个或多个 两个选自卤素，氰基，羟基或C 1-4烷氧基的基团; R 10是氢或C 3-7环烷基; n为1或2; q是0,1或2; r为0或1至4的整数; 或其药学上可接受的盐或溶剂合物，其制备方法及其用于治疗由粘蛋白介导的病症和/或通过选择性抑制5-羟色胺再摄取转运蛋白

    Piperidine derivatives and their use as antagonists of tachykinins
    6.
    发明授权
    Piperidine derivatives and their use as antagonists of tachykinins 失效
    哌啶衍生物及其作为速激肽拮抗剂的用途

    公开(公告)号：US07276509B2

    公开(公告)日：2007-10-02

    申请号：US10502261

    申请日：2003-02-05

    申请人： Giuseppe Alvaro ,  Romano Di Fabio

    发明人： Giuseppe Alvaro ,  Romano Di Fabio

    IPC分类号： A61K31/496 ,  C07D401/04 ,  C07D211/58

    CPC分类号： C07D401/04

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

    摘要翻译： 本发明涉及式（I）的哌啶衍生物：其中R表示卤素或C 1-4烷基; R 1表示氢或C 1-4烷基; R 2表示氢，C 1-4烷基; R 3表示氢，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，C 3-7环烷基，C（O）R 6 >或S（O）2 R 6 R 6; R 6表示C 1-4烷基或C 3-7环烷基; m为0或1〜3的整数; n为1〜3的整数， p是从1到2的整数; X和Y独立地为C（O）或CH 2 O 2; 条件是i）X和Y不同时为C（O），ii）当X和Y均为CH 2且p为1时，R 5不为氢， C 1-4烷基或C（O）R 6; 及其药学上可接受的盐和溶剂合物，其制备方法及其用于治疗由速激肽介导的病症。

    Chemical Compounds
    8.
    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).

    Piperidine derivatives
    9.
    发明授权
    Piperidine derivatives 有权
    哌啶衍生物

    公开(公告)号：US07189713B2

    公开(公告)日：2007-03-13

    申请号：US10502255

    申请日：2003-02-10

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

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

    IPC分类号： A61K31/535 ,  A01N43/58 ,  C07D498/00 ,  C07D265/12 ,  C07D471/00

    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。