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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
    4.
    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.

    Pyridine Derivatives and Their Use in The Treatment of Psychotic Disorders
    10.
    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.