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    Beta-Lactams for Treatment of Cns Disorders
    1.
    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

    Chemical compounds
    2.
    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
    5.
    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。

    Chemical compounds
    8.
    发明申请
    Chemical compounds 审中-公开

    公开(公告)号：US20060128752A1

    公开(公告)日：2006-06-15

    申请号：US10520143

    申请日：2003-07-02

    申请人： Giuseppe Alvaro ,  Francesca Cardullo ,  Romano Di Fabio ,  Riccardo Giovannini ,  Elisabeth Piga ,  Maria Tranquillini

    发明人： Giuseppe Alvaro ,  Francesca Cardullo ,  Romano Di Fabio ,  Riccardo Giovannini ,  Elisabeth Piga ,  Maria Tranquillini

    IPC分类号： A61K31/445 ,  C07D211/06

    CPC分类号： C07D211/34 ,  C07D211/64 ,  C07D223/04 ,  C07D223/06

    摘要： The present invention relates to cyclic amine derivatives of formula(l) wherein R represents halogen, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy; R1 represents hydrogen, halogen, C3-7cycloalkyl, hydroxy, nitro, cyano or C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy; R2 represents hydrogen or C1-4 alkyl; R3 and R4 independently represent hydrogen, cyano, C1-4 alkyl or R3 together with R4 represents C3-7 cycloalkyl; R5 represents trifluoromethyl, S(O)t C1-4 alkyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy, halogen or cyano; R6 represents hydrogen or (CH2)rR7; R7 represents hydrogen, C37 cycloalkyl, NH(C1-4alkylOC1-4alkoxy), NH(C1-4alkyl), N(C1-4alkyl)2, OC(O)NR9R8, NR8C(O)R9 or C(O)NR9R8; R9 and R8 independently represent hydrogen, C1-4 alkyl or C3-7 cycloalkyl; m represents zero or an integer from 1 to 4; n represents 1 or 2; p is zero or an integer from 1 to 3; q is an integer from 1 to 3; r is an integer from 1 to 4; t is 0, 1 or 2; provided that when m is 0, p is 2, q , r and n represent 1, R1, R2,R3, R4, R5 and R7 are hydrogen and R is chlorine, R5 is not iodine; and pharmaceutically acceptable salts and solvates thereof; process for their preparation and their use in the treatment of conditions mediated by tackykinins and/or by selective inhibition of serotonin reuptake transporter protein.