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    Cyclic Amine Derivatives, Processes For Their Preparation, And Pharmaceutical Compositions Containing Them
    3.
    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。

    N-benzyl-3-phenyl-3-heterocyclyl-propionamide compounds as tachykinin and/or serotonin reuptake inhibitors
    4.
    发明申请
    N-benzyl-3-phenyl-3-heterocyclyl-propionamide compounds as tachykinin and/or serotonin reuptake inhibitors 审中-公开
    N-苄基-3-苯基-3-杂环基 - 丙酰胺化合物作为速激肽和/或5-羟色胺再摄取抑制剂

    公开(公告)号：US20060058348A1

    公开(公告)日：2006-03-16

    申请号：US10521159

    申请日：2003-07-02

    申请人： Giuseppe Alvaro ,  Francesca Cardullo ,  Lucilla D'Adamo ,  Elisabeth Piga ,  Catia Seri

    发明人： Giuseppe Alvaro ,  Francesca Cardullo ,  Lucilla D'Adamo ,  Elisabeth Piga ,  Catia Seri

    IPC分类号： C07D211/26 ,  A61K31/445

    CPC分类号： C07D207/08 ,  A61K31/40 ,  A61K31/44 ,  A61K31/445 ,  A61K31/535 ,  C07D207/20 ,  C07D211/34 ,  C07D211/38 ,  C07D211/70 ,  C07D213/56 ,  C07D265/30

    摘要： The present invention relates to heterocyclic derivatives of formula (I) wherein R represents halogen, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy; R1 represents a 5 or 6 membered heteroaryl group, in which the 5-membered heteroaryl group contains at least one heteroatom selected from oxygen, sulphur or nitrogen and the 6-membered heteroaryl group contains from 1 to 3 nitrogen atoms, or R1 represents a 4, 5 or 6 membered heterocyclic group, wherein saids 5 or 6 membered heteroaryl or the 4, 5 or 6 membered heterocyclic group may optionally be substituted by one to three substituents, which may be the same or different, selected from (CH2)pR6, wherein p is zero or an integer from 1 to 4 and R6 is selected from: halogen, C1-4alkoxy, C1-4alkyl, C3-7cycloalkyl, C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy, hydroxy, cyano, nitro, trifluoromethyl, carboxy, NH(C1-4 alkyl), N(C1-4 alkyl)2 NH(C3-7 cycloalkyl), N(C1-4 alkyl)(C3-7 cycloalkyl); NH(C1-4alkylOC1-4alkoxy), OC(O)NR7R8, NR8C(O)R7 or C(O)NR7R8; R2 represents hydrogen, or C1-4 alkyl; R3 and R4 independently represent hydrogen, C1-4 alkyl or R3 together with R4 represents C3-7 cycloalkyl; R5 represents trifluoromethyl, S(O)qC1-4 alkyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy, halogen or cyano; R7 and R8 independently represent hydrogen, C1-4 alkyl or C3-7 cycloalkyl; L is a single or a double bond; n is an integer from 1 to 3; m is zero or an integer from 1 to 3; q is zero or an integer from 1 to 2; provided that a) when L is a double bond, R1 is not an optionally substituted 5 or 6 membered heteroaryl group, in which the 5-membered heteroaryl group contains at least one heteroatom selected from oxygen, sulphur or nitrogen and the 6-membered heteroaryl group contains from 1 to 3 nitrogen atoms; b) the group R1 is linked to the carbon atom shown as * via a carbon atom; and c) when the heteroatom contained in the group R1 is substituted, p is not zero; and pharmaceutically acceptable salts and solvates thereof; process for their preparation 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： 本发明涉及式（I）的杂环衍生物，

    Spiro Compounds As NPY Y5 Receptor Antagonists
    7.
    发明申请
    Spiro Compounds As NPY Y5 Receptor Antagonists 审中-公开
    螺环化合物作为NPY Y5受体拮抗剂

    公开(公告)号：US20090203705A1

    公开(公告)日：2009-08-13

    申请号：US12360166

    申请日：2009-01-27

    申请人： Matteo Biagetti ,  Stefania Anna Contini ,  Thorsten Genski ,  Sebastien Guery ,  Colin Philip Leslie ,  Angelica Mazzali ,  Domenica Antonia Pizzi ,  Fabio Maria Sabbatini ,  Catia Seri

    发明人： Matteo Biagetti ,  Stefania Anna Contini ,  Thorsten Genski ,  Sebastien Guery ,  Colin Philip Leslie ,  Angelica Mazzali ,  Domenica Antonia Pizzi ,  Fabio Maria Sabbatini ,  Catia Seri

    IPC分类号： A61K31/501 ,  C07D413/14 ,  A61P3/04

    CPC分类号： C07D413/12 ,  C07D413/14 ,  C07D417/14

    摘要： The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein R is an aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; Z1 is H, C1-C4 alkyl or F; Z is CH2, CH(C1-C4 alkyl), C(C1-C4 alkyl)2 or a bond; A is a 6-10 membered aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or —C(═O)—X; or —O(CH2)0-1R1; B is hydrogen or is a 5-6 membered heteroaryl, or a 4-6 membered heterocycle, or phenyl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, hydroxyl, cyano; A and B being linked via any atom; R1 is —(C1-C4)alkyl(C1-C4)alkoxy; or C3-C8 cycloalkyl; or R1 is an aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or R1 is a 4-6 membered heterocycle, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; X is OR2 or NR3R4; R2 is C1-C4 alkyl; R3 is hydrogen or together with R4 and the nitrogen form a 5-6 saturated membered ring; R4 is C3-C8 cycloalkyl; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.

    摘要翻译： 本发明涉及新的式（I）化合物或其药学上可接受的盐，其中R是可被一个或多个取代的芳基或杂芳基：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C4卤代烷基，C1-C4卤代烷氧基，氰基; Z 1是H，C 1 -C 4烷基或F; Z是CH 2，CH（C 1 -C 4烷基），C（C 1 -C 4烷基）2或键; A是6-10元芳基或杂芳基，其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; 或-C（-O）-X; 或-O（CH 2）0-1R1; B是氢或是5-6元杂芳基或4-6元杂环，或苯基，其可被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C4卤代烷氧基，羟基，氰基; A和B通过任何原子相连; R1是 - （C1-C4）烷基（C1-C4）烷氧基; 或C 3 -C 8环烷基; 或者R 1是可被一个或多个卤素取代的芳基或杂芳基：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; 或R 1是4-6元杂环，其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; X为OR2或NR3R4; R2是C1-C4烷基; R3是氢或与R4一起形成5-6饱和的元环; R4是C3-C8环烷基; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为NPY Y5受体拮抗剂以及用于治疗和/或预防进食障碍如狂饮病症的药剂。

    Novel Compounds
    9.
    发明申请
    Novel Compounds 审中-公开
    新型化合物

    公开(公告)号：US20100227870A1

    公开(公告)日：2010-09-09

    申请号：US12663739

    申请日：2008-06-12

    申请人： Massimo Gianotti ,  Jag Paul Heer ,  Peter John Lovell ,  Catia Seri ,  Ben Gerald Tehan

    发明人： Massimo Gianotti ,  Jag Paul Heer ,  Peter John Lovell ,  Catia Seri ,  Ben Gerald Tehan

    IPC分类号： A61K31/4965 ,  C07D241/04 ,  A61P25/18

    CPC分类号： C07D295/185

    摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof for treating diseases and conditions mediated by positive allosteric modulation of the G-protein coupled metabotropic subtype 5 receptor (mGluR5), such as neurological and psychiatric disorders, for example schizophrenia. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.

    摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐，用于治疗由G-蛋白偶联的代谢型5型受体（mGluR5）的正性变构调节介导的疾病和病症，例如神经和精神疾病，例如精神分裂症 。 此外，本发明涉及含有衍生物的组合物及其制备方法。