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83 条记录 (耗时 0.049 秒)

    Piperidine Derivatives
    6.
    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。

    Pyridine Derivatives and Their Use in The Treatment of Psychotic Disorders
    7.
    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.

    Novel Compounds
    8.
    发明申请
    Novel Compounds 审中-公开
    新型化合物

    公开(公告)号：US20090286836A1

    公开(公告)日：2009-11-19

    申请号：US12464171

    申请日：2009-05-12

    申请人： Giuseppe Alvaro ,  Agostino Marasco

    发明人： Giuseppe Alvaro ,  Agostino Marasco

    IPC分类号： A61K31/4439 ,  C07D401/04

    CPC分类号： C07D401/04

    摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C1-4 alkyl useful in the treatment of diseases and conditions for which antagonism of NK1 receptor is beneficial.

    摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐，其中R是可用于治疗NK1受体拮抗作用有益的疾病和病症的C 1-4烷基。

    Cyclic Amine Derivatives, Processes For Their Preparation, And Pharmaceutical Compositions Containing Them
    9.
    发明申请
    Cyclic Amine Derivatives, Processes For Their Preparation, And Pharmaceutical Compositions Containing Them 审中-公开
    环胺衍生物，其制备方法以及含有它们的药物组合物

    公开(公告)号：US20090192194A1

    公开(公告)日：2009-07-30

    申请号：US11869945

    申请日：2007-10-10

    申请人： Giuseppe Alvaro ,  Luca Arista ,  Francesca Cardullo ,  Lucilla D'Adamo ,  Aldo Feriani ,  Riccardo Giovannini ,  Catia Seri

    发明人： Giuseppe Alvaro ,  Luca Arista ,  Francesca Cardullo ,  Lucilla D'Adamo ,  Aldo Feriani ,  Riccardo Giovannini ,  Catia Seri

    IPC分类号： A61K31/445 ,  C07D401/02 ,  C07D211/22 ,  A61P25/22

    CPC分类号： C07D405/04 ,  C07D211/34 ,  C07D405/12

    摘要： A compound of formula (I) wherein R is a radical selected from in which R7 is halogen, cyano, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy; p is an integer from 0 to 3; R1 is hydrogen, halogen, cyano, C2-4 alkenyl, C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy; R2 is hydrogen or C1-4 alkyl; R3 and R4 independently are hydrogen, C1-4 alkyl or R3 together with R4 is C3-7 cycloalkyl; R5 is phenyl substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl, naphthyl substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl, a 9 to 10 membered fused bicyclic heterocyclic group substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl or R5 is a 5 or 6 membered heteroaryl group substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl; R6 is hydrogen or (CH2)qR8; R8 is hydrogen, C3-7 cycloalkyl, C1-4 alkoxy, amine, C1-4 alkylamine, (C1-4 alkyl)2amine, OC(O)NR9R10 or C(O)NR9R10; R9 and R10 independently are hydrogen, C1-4 alkyl or C3-7 cycloalkyl; m is zero or 1; n is 1 or 2; q is an integer from 1 to 4; r is 1 or 2; or pharmaceutically acceptable salts and solvates thereof; processes for their preparation to pharmaceutical compositions containing them and their use in the treatment of conditions mediated by tachykinins and/or by selective inhibition of serotonin reuptake transporter protein.

    摘要翻译： 式（I）化合物，其中R为选自其中R 7为卤素，氰基，C 1-4烷基，C 1-4烷氧基，三氟甲基或三氟甲氧基的基团; p是0至3的整数; R 1是氢，卤素，氰基，C 2-4链烯基，任选地被卤素，氰基或C 1-4烷氧基取代的C 1-4烷基; R2是氢或C1-4烷基; R3和R4独立地是氢，C1-4烷基或R3与R4一起是C3-7环烷基; R5是被1-3个独立地选自三氟甲基，C1-4烷基，氰基，C1-4烷氧基，三氟甲氧基，卤素或（SO）rC1-4烷基取代的苯基，被1至3个独立地选自三氟甲基， C 1-4烷基，氰基，C 1-4烷氧基，三氟甲氧基，卤素或（SO）r C 1-4烷基，被1至3个独立地选自三氟甲基，C 1-4烷基，氰基的1-3元基团取代的9至10元稠合双环杂环基 ，C 1-4烷氧基，三氟甲氧基，卤素或（SO）rC 1-4烷基或R 5是被1-3个独立地选自三氟甲基，C 1-4烷基，氰基，C 1-4烷氧基， 三氟甲氧基，卤素或（SO）rC 1-4烷基; R6是氢或（CH2）qR8; R 8为氢，C 3-7环烷基，C 1-4烷氧基，胺，C 1-4烷基胺，（C 1-4烷基）2胺，OC（O）NR 9 R 10或C（O）NR 9 R 10; R9和R10独立地是氢，C1-4烷基或C3-7环烷基; m为零或1; n为1或2; q是1至4的整数; r为1或2; 或其药学上可接受的盐和溶剂化物; 其制备方法用于含有它们的药物组合物及其用于治疗由速激肽介导的病症和/或通过选择性抑制5-羟色胺再摄取转运蛋白。