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    Condensed n-heterocyclic compounds and their use as crf receptor antagonists
    8.
    发明申请
    Condensed n-heterocyclic compounds and their use as crf receptor antagonists 有权
    缩合的N-杂环化合物及其作为crf受体拮抗剂的用途

    公开(公告)号：US20070004708A1

    公开(公告)日：2007-01-04

    申请号：US10552493

    申请日：2004-04-07

    申请人： Daniele Andreotti ,  Giovannie Bernasconi ,  Emiliano Castiglioni ,  Stefania Contini ,  Romano Di Fabio ,  Elettra Fazzolari ,  Aldo Feriani ,  Gabriella Gentile ,  Mario Mattioli ,  Anna Mingardi ,  Fabio Sabbatini ,  Yves St-Denis

    发明人： Daniele Andreotti ,  Giovannie Bernasconi ,  Emiliano Castiglioni ,  Stefania Contini ,  Romano Di Fabio ,  Elettra Fazzolari ,  Aldo Feriani ,  Gabriella Gentile ,  Mario Mattioli ,  Anna Mingardi ,  Fabio Sabbatini ,  Yves St-Denis

    IPC分类号： A61K31/549 ,  A61K31/519 ,  A61K31/496 ,  A61K31/501 ,  A61K31/4745 ,  C07D487/02 ,  C07D471/02

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof (Formula (I)) wherein the dashed line may represent a double bond; R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups J selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 lkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —C(O)R2, nitro, hydroxy, —NR3R4, cyano and or a group Z; R1 is hydrogen, C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR3R4 or cyano; D, G is —C— optionally substituted; X is carbon or nitrogen; Y is nitrogen or —C— optionally substituted; W is a 4-8 membered ring, which may be saturated or may contain one to three double bonds, and in which:—one carbon atom is replaced by a carbonyl or S(O)m; and—one to four carbon atoms may optionally be replaced by oxygen, nitrogen or NR12, S(O)m, carbonyl, and such ring may be further substituted by 1 to 8 substituents; Z is a 5-6 membered heterocycle, which may be substituted by 1 to 8 R5 groups or a phenyl ring, which may be substituted by 1 to 4 substituents; m is an integer from 0 to 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).

    摘要翻译： 本发明提供了包含立体异构体，前体药物和药学上可接受的盐或溶剂合物（式（I））的式（I）化合物，其中虚线可以表示双键; R是芳基或杂芳基，其各自可以被1-4个选自以下的基团取代：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤素 C 1 -C 6烷氧基，-C（O）R 2，硝基，羟基，-NR 3 R 4，氰基和/或Z ; R 1是氢，C 3 -C 7环烷基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6硫代烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 3 R 4或氰基; D，G是-C-任选取代的; X是碳或氮; Y是氮或-C-任选取代的; W是4-8元环，其可以是饱和的或可以含有一至三个双键，并且其中： - 一个碳原子被羰基或S（O）m取代; 一至四个碳原子可以任选地被氧，氮或NR 12，S（O）m H，羰基取代，并且这种环可进一步被1 至8个取代基; Z是5-6元杂环，其可被1至8个R 5取代基或可被1至4个取代基取代的苯环; m为0至2的整数。其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症的用途。

    Spiro (piperidine-4,2′-pyrrolidine)-1-(3,5-trifluoromethyl phenyl) methylcarboxamides as NK1 tachikynin receptor antagonists
    9.
    发明授权
    Spiro (piperidine-4,2′-pyrrolidine)-1-(3,5-trifluoromethyl phenyl) methylcarboxamides as NK1 tachikynin receptor antagonists 有权
    螺（哌啶-4,2'-吡咯烷）-1-（3,5-三氟甲基苯基）甲基甲酰胺作为N​​K1振动子受体拮抗剂

    公开(公告)号：US08367692B2

    公开(公告)日：2013-02-05

    申请号：US12989699

    申请日：2009-04-29

    申请人： Giuseppe Alvaro ,  Emiliano Castiglioni ,  Agostino Marasco

    发明人： Giuseppe Alvaro ,  Emiliano Castiglioni ,  Agostino Marasco

    IPC分类号： A61K31/438 ,  C07D401/04 ,  C07D471/10

    CPC分类号： C07D471/10 ,  C07D498/20

    摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof. wherein R is hydrogen or C1-4 alkyl; R1 is hydrogen, C1-4 alkyl, C(O)OH, C(O)NH2 or (C1-4 alkylene)R10; R2 and R3 are independently hydrogen, C1-4 alkyl or R2 together with R3 and together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R4 is C1-4 alkyl, C1-4 alkoxy or halogen; R5 and R7 are independently hydrogen, hydroxy, halogen, C(O)NH2, C(O)OH or (C1-4 alkylene)R10; R6 and R8 are independently hydrogen or halogen; R9 is hydrogen, (C1-4 alkylene)R10, C(O)NH2, C(O)OH or R9 together with R form a 6 membered heterocyclic ring optionally containing a further heteroatom selected from oxygen, sulphur or nitrogen; R10 is hydrogen, halogen, hydroxy, C(O)NH2, C(O)NH(C1-4 alkyl), C(O)N(C1-4 alkyl)2 or C(O)OH; n is 0, 1 or 2. processes for their preparation, to compositions containing them and to their use in the treatment of diseases and conditions for which antagonism of NK1 is beneficial.

    摘要翻译： 式（I）化合物或其药学上可接受的盐。 其中R是氢或C 1-4烷基; R 1是氢，C 1-4烷基，C（O）OH，C（O）NH 2或（C 1-4亚烷基）R 10; R2和R3独立地为氢，C1-4烷基或R2与R3一起并与它们所连接的碳原子一起形成C 3-8环烷基; R4是C1-4烷基，C1-4烷氧基或卤素; R 5和R 7独立地是氢，羟基，卤素，C（O）NH 2，C（O）OH或（C 1-4亚烷基）R 10; R6和R8独立地是氢或卤素; R9是氢，（C1-4亚烷基）R10，C（O）NH2，C（O）OH或R9与R一起形成任选地含有另外选自氧，硫或氮的杂原子的6元杂环; R 10是氢，卤素，羟基，C（O）NH 2，C（O）NH（C 1-4烷基），C（O）N（C 1-4烷基）2或C（O） n为0,1或2.其制备方法，含有它们的组合物及其在治疗NK1拮抗作用有益的疾病和病症中的用途。

    Spiro (Piperidine-4,2'-Pyrrolidine)-1-(3,5-Trifluoromethyl Phenyl) Methylcarboxamides As NK1 Tachikynin Receptor Antagonists
    10.
    发明申请
    Spiro (Piperidine-4,2'-Pyrrolidine)-1-(3,5-Trifluoromethyl Phenyl) Methylcarboxamides As NK1 Tachikynin Receptor Antagonists 有权
    螺（哌啶-4,2'-吡咯烷）-1-（3,5-三氟甲基苯基）甲基甲酰胺作为N​​K1激动素受体拮抗剂

    公开(公告)号：US20110053922A1

    公开(公告)日：2011-03-03

    申请号：US12989699

    申请日：2009-04-29

    申请人： Giuseppe Alvaro ,  Emiliano Castiglioni ,  Agostino Marasco

    发明人： Giuseppe Alvaro ,  Emiliano Castiglioni ,  Agostino Marasco

    IPC分类号： A61K31/5386 ,  C07D471/10 ,  A61K31/438 ,  C07D491/20 ,  A61P25/24 ,  A61P25/22

    CPC分类号： C07D471/10 ,  C07D498/20

    摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein R is hydrogen or C1-4 alkyl; R1 is hydrogen, C1-4 alkyl, C(O)OH, C(O)NH2 or (C1-4 alkylene)R10; R2 and R3 are independently hydrogen, C1-4 alkyl or R2 together with R3 and together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R4 is C1-4 alkyl, C1-4 alkoxy or halogen; R5 and R7 are independently hydrogen, hydroxy, halogen, C(O)NH2, C(O)OH or (C1-4 alkylene) R10; R6 and R8 are independently hydrogen or halogen; R9 is hydrogen, (C1-4 alkylene)R10, C(O)NH2, C(O)OH or R9 together with R form a 6 membered heterocyclic ring optionally containing a further heteroatom selected from oxygen, sulphur or nitrogen; R10 is hydrogen, halogen, hydroxy, C(O)NH2, C(O)NH(C1-4 alkyl), C(O)N(C1-4 alkyl)2 or C(O)OH; n is 0, 1 or 2. processes for their preparation, to compositions containing them and to their use in the treatment of diseases and conditions for which antagonism of NK1 is beneficial.

    摘要翻译： 式（I）化合物或其药学上可接受的盐，其中R是氢或C 1-4烷基; R 1是氢，C 1-4烷基，C（O）OH，C（O）NH 2或（C 1-4亚烷基）R 10; R2和R3独立地为氢，C1-4烷基或R2与R3一起并与它们所连接的碳原子一起形成C 3-8环烷基; R4是C1-4烷基，C1-4烷氧基或卤素; R 5和R 7独立地是氢，羟基，卤素，C（O）NH 2，C（O）OH或（C 1-4亚烷基）R 10; R6和R8独立地是氢或卤素; R9是氢，（C1-4亚烷基）R10，C（O）NH2，C（O）OH或R9与R一起形成任选地含有另外选自氧，硫或氮的杂原子的6元杂环; R 10是氢，卤素，羟基，C（O）NH 2，C（O）NH（C 1-4烷基），C（O）N（C 1-4烷基）2或C（O） n为0,1或2.其制备方法，含有它们的组合物及其在治疗NK1拮抗作用有益的疾病和病症中的用途。