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    CB.sub.2 Receptor agonist compounds
    3.
    发明授权
    CB.sub.2 Receptor agonist compounds 失效

    公开(公告)号：US6013648A

    公开(公告)日：2000-01-11

    申请号：US995902

    申请日：1997-12-22

    申请人： Murielle Rinaldi ,  Francis Barth ,  Pierre Casellas ,  Christian Congy ,  Didier Oustric ,  Malcolm R. Bell ,  Thomas E. D'Ambra ,  Richard E. Philion

    发明人： Murielle Rinaldi ,  Francis Barth ,  Pierre Casellas ,  Christian Congy ,  Didier Oustric ,  Malcolm R. Bell ,  Thomas E. D'Ambra ,  Richard E. Philion

    IPC分类号： C07D295/08 ,  A61K31/135 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/435 ,  A61K31/47 ,  A61K31/535 ,  A61K31/5355 ,  A61K31/5375 ,  A61K31/538 ,  A61K45/00 ,  A61P29/00 ,  A61P37/00 ,  A61P37/02 ,  A61P37/08 ,  A61P43/00 ,  C07D209/08 ,  C07D209/12 ,  C07D209/14 ,  C07D209/16 ,  C07D413/06 ,  C07D471/04 ,  C07D471/06 ,  C07D487/06 ,  C07D491/06 ,  C07D498/06 ,  A61K31/405

    CPC分类号： A61K31/404 ,  A61K31/5355 ,  A61K31/538

    摘要： The use of human CB.sub.2 receptor-specific agonists of formula (I) or (I') for preparing immunomodulating drugs is disclosed. In formulae (I) and (I'), R.sub.1 is a group selected from --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11, --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11, --CHR.sub.9 CH.sub.2 NR'.sub.6 R'.sub.11, --(CH.sub.2).sub.n Z and --COR.sub.8 ; R'.sub.1 is a --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11 or --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11 group; R.sub.2 and R'.sub.2 are hydrogen, halogen or C.sub.1-4 alkyl; R.sub.3 is hydrogen, C.sub.1-4 alkyl or a group selected from --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11, --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11 and --COR.sub.8 ; R'.sub.3 is a .dbd.CR.sub.6 R.sub.8 group; R.sub.4 has one of the meanings given for R.sub.5 or is a --COR.sub.8 group; R.sub.5 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, a halogen atom, a CF.sub.3 group, an OCF.sub.3 group or C.sub.1-4 alkylthio; R'.sub.5 has one of the meanings given for R.sub.5 and is in the 5 or 6 position of the indene ring; R.sub.6 is hydrogen or C.sub.1-4 alkyl; R'.sub.6 is C.sub.1-4 alkyl; R.sub.7 has one of the meanings given for R.sub.5 or R.sub.7 and R.sub.9 together form a --Y--CH.sub.2 -- group attached to the indole ring in the 7 position by a group Y; R.sub.8 is phenyl substituted one to four times by a substituent selected from halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy; a polycyclic ring selected from naphth-1-yl, naphth-2-yl, 1,2,3,4-tetrahydronaphth-1-yl, 1,2,3,4-tetrahydronaphth-5-yl, anthryl, benzofuryl, benzothien-2-yl, benzothien-3-yl, 2-, 3-, 4- or 8-quinolyl, said polycyclic rings optionally being substituted once or twice by a substituent selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen, cyano, hydroxyl, trifluoromethyl and imidazol-1-yl; R.sub.10 and R.sub.11 together are a group selected from --CH.sub.2 --O--CH.sub.2 --CR.sub.12 R.sub.13 -- and --(CH.sub.2).sub.p --CR.sub.12 R.sub.13 --, wherein the carbon atom substituted by R.sub.12 and R.sub.13 is attached to the nitrogen atom; R'.sub.11 is C.sub.1-4 alkyl; or R'.sub.11 and R'.sub.6, taken together with the nitrogen atom to which they are attached, form a group selected from morpholin-4-yl, thiomorpholin-4-yl, piperidin-1-yl and pyrrolidin-1-yl; each of R.sub.12 and R.sub.13 is independently hydrogen or C.sub.1-4 alkyl; n is 2, 3, 4 or 5; p is 2 or 3; Z is a methyl group or a halogen atom; and Y is a methylene group or an oxygen atom.

    3-pyrazolecarboxamide derivatives having cannabinoid receptor affinity
    4.
    发明授权
    3-pyrazolecarboxamide derivatives having cannabinoid receptor affinity 失效
    具有大麻素受体亲和力的3-吡唑酰胺衍生物

    公开(公告)号：US5925768A

    公开(公告)日：1999-07-20

    申请号：US77767

    申请日：1998-06-03

    申请人： Francis Barth ,  Pierre Casellas ,  Joseph Millan ,  Didier Oustric ,  Murielle Rinaldi ,  Martine Sarran

    发明人： Francis Barth ,  Pierre Casellas ,  Joseph Millan ,  Didier Oustric ,  Murielle Rinaldi ,  Martine Sarran

    IPC分类号： A61K31/00 ,  A61K31/415 ,  A61P37/00 ,  A61P37/02 ,  A61P43/00 ,  C07D231/14

    CPC分类号： C07D231/14

    摘要： The present invention relates to compounds of the formula ##STR1## in which: X.sub.1 is a group --NR.sub.1 R.sub.2 or a group --OR.sub.2 ;g.sub.2, g.sub.3, g.sub.4, g.sub.5, g.sub.6 and w.sub.2, w.sub.3, w.sub.4, w.sub.5, w.sub.6 are identical or different and are each independently hydrogen, a halogen atom, a (C.sub.1 -C.sub.4)alkyl, a (C.sub.1 -C.sub.4)alkoxy, a trifluoromethyl, a nitro or a (C.sub.1 -C.sub.4)alkylthio, with the proviso that at least one of the substituents g.sub.2, g.sub.3, g.sub.4, g.sub.5, g.sub.6 and at least one of the substituents w.sub.2, w.sub.3, w.sub.4, w.sub.5, w.sub.6 are other than hydrogen;R.sub.1 is hydrogen or a (C.sub.1 -C.sub.4)alkyl;R.sub.2 is a non-aromatic (C.sub.3 -C.sub.15)carbocyclic radical which is unsubstituted or monosubstituted or polysubstituted by a substituent selected from a halogen atom, a (C.sub.1 -C.sub.4)alkyl and a (C.sub.1 -C.sub.4)alkoxy;R.sub.3 is hydrogen or a group --CH.sub.2 R.sub.6 ; andR.sub.4 and R.sub.5 are each independently a hydrogen, a (C.sub.1 -C.sub.4)alkyl or a trifluoromethyl;or else R.sub.4 is hydrogen and R.sub.5 and w.sub.6 together constitute an ethylene or trimethylene radical; andR.sub.6 is hydrogen, a (C.sub.1 -C.sub.4)alkyl, a fluorine, a hydroxyl, a (C.sub.1 -C.sub.5)alkoxy, a (C.sub.1 -C.sub.5)alkylthio, a hydroxy(C.sub.1 -C.sub.5)alkoxy, a cyano, a (C.sub.1 -C.sub.5)alkylsulfinyl or a (C.sub.1 -C.sub.5)alkylsulfonyl with the proviso that when the substituents g.sub.2, g.sub.3, g.sub.4, g.sub.5 and/or g.sub.6 are a (C.sub.1 -C.sub.4)alkyl R.sub.6 is only hydrogen;to a process for their preparation and to the pharmaceutical compositions in which they are present.These compounds have a good affinity for the peripheral cannabinoid receptors.

    摘要翻译： PCT No.PCT / FR96 / 01953 Sec。 371日期1998年6月3日第 102（e）1998年6月3日PCT PCT 1996年12月6日PCT公布。 公开号WO97 / 21682 日期：1997年6月19日本发明涉及下式的化合物，其中：X 1为基团-NR 1 R 2或基团-OR 2; g2，g3，g4，g5，g6和w2，w3，w4，w5，w6相同或不同，各自独立地为氢，卤素原子，（C1-C4）烷基，（C1-C4）烷氧基， 三氟甲基，硝基或（C 1 -C 4）烷硫基，条件是至少一个取代基g2，g3，g4，g5，g6和至少一个取代基w2，w3，w4，w5，w6是其他 比氢; R1是氢或（C1-C4）烷基; R 2是未被取代或被选自卤素原子，（C 1 -C 4）烷基和（C 1 -C 4）烷氧基的取代基单取代或多取代的非芳族（C 3 -C 15）碳环基团; R3是氢或基团-CH2R6; 和R 4和R 5各自独立地为氢，（C 1 -C 4）烷基或三氟甲基; 或者R4是氢，R5和w6一起构成乙烯或三亚甲基; （C 1 -C 5）烷氧基，（C 1 -C 5）烷硫基，羟基（C 1 -C 5）烷氧基，氰基，（C 1 -C 5）烷氧基， -C 5）烷基亚磺酰基或（C 1 -C 5）烷基磺酰基，条件是当取代基g2，g3，g4，g5和/或g6为（C1-C4）烷基时，R6仅为氢; 涉及其制备方法及其存在的药物组合物。 这些化合物对外周大麻素受体具有良好的亲和力。

    Pyridopyrimidone derivatives, preparation thereof, therapeutic use thereof
    5.
    发明授权
    Pyridopyrimidone derivatives, preparation thereof, therapeutic use thereof 失效
    吡啶并嘧啶衍生物，其制备方法，治疗用途

    公开(公告)号：US07842806B2

    公开(公告)日：2010-11-30

    申请号：US12166431

    申请日：2008-07-02

    申请人： Pierre Perreaut ,  Samir Jegham ,  Bernard Bourrie ,  Pierre Casellas ,  Jean-Robert Labrosse ,  Florence Durand

    发明人： Pierre Perreaut ,  Samir Jegham ,  Bernard Bourrie ,  Pierre Casellas ,  Jean-Robert Labrosse ,  Florence Durand

    IPC分类号： C07D471/00

    CPC分类号： C07D471/04

    摘要： The disclosure relates to pyrido[2,3-d]pyrimidone compounds, to the preparation thereof and to the therapeutic use thereof, wherein said compounds are of general formula (I): in the form of a base or of an addition salt with an acid which is pharmaceutically acceptable, in the form of hydrates or of solvates, and also in the form of enantiomers, diastereoisomers and a mixture thereof. The disclosure also relates to processes for preparing said compounds, to pharmaceutical compositions containing a compound of general formula (I), and to the therapeutic use of said compounds and compositions.

    摘要翻译： 本公开涉及吡啶并[2,3-d]嘧啶酮化合物，其制备方法及其治疗用途，其中所述化合物为通式（I）：以碱的形式或加成盐与 其为药学上可接受的，为水合物或溶剂化物形式，也为对映异构体，非对映异构体及其混合物的形式。 本公开还涉及制备所述化合物的方法，含有通式（I）化合物的药物组合物以及所述化合物和组合物的治疗用途。

    PYRIDO-PYRIMIDINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
    7.
    发明申请
    PYRIDO-PYRIMIDINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF 有权
    吡啶二吡啶衍生物，其制备方法及其治疗方法

    公开(公告)号：US20090233923A1

    公开(公告)日：2009-09-17

    申请号：US12415256

    申请日：2009-03-31

    申请人： Bernard Bourrie ,  Pierre Casellas ,  Samir Jegham ,  Pierre Perreaut

    发明人： Bernard Bourrie ,  Pierre Casellas ,  Samir Jegham ,  Pierre Perreaut

    IPC分类号： A61K31/5377 ,  C07D471/04 ,  A61K31/519 ,  A61P35/00

    CPC分类号： C07D471/04

    摘要： The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I): and acid addition salts, hydrates and solvates thereof, as well as in the form of enantiomers, diastereoisomers and mixtures thereof. The disclosure also concerns methods for preparing said derivatives, pharmaceutical compositions containing a compound of general formula (I), and their therapeutic use.

    摘要翻译： 本公开涉及通式（I）的吡啶并[2,3-d]嘧啶衍生物及其制备方法及其治疗应用：及其酸加成盐，水合物和溶剂化物，以及对映异构体，非对映异构体和混合物的形式 其中。 本公开还涉及制备所述衍生物的方法，含有通式（I）的化合物的药物组合物及其治疗用途。

    Pyridoindolone derivatives substituted in the 3-position by a heterocyclic group, their preparation and their application in therapeutics
    8.
    发明授权
    Pyridoindolone derivatives substituted in the 3-position by a heterocyclic group, their preparation and their application in therapeutics 失效
    吡啶并吲哚酮衍生物在3位被杂环基取代，其制备及其在治疗中的应用

    公开(公告)号：US07456193B2

    公开(公告)日：2008-11-25

    申请号：US11109121

    申请日：2005-04-19

    申请人： Bernard Bourrie ,  Pierre Casellas ,  Jean-Marie Derocq ,  Samir Jegham ,  Yvette Muneaux

    发明人： Bernard Bourrie ,  Pierre Casellas ,  Jean-Marie Derocq ,  Samir Jegham ,  Yvette Muneaux

    IPC分类号： A61K31/437 ,  C07D487/04 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： The present invention relates to pyridoindolone derivatives substituted in the 3-position by a heterocyclic group of general formula (I): in which: R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 represents a hydrogen atom or a (C1-C4)alkyl group; R3 represents a thienyl mono- or polysubstituted by a methyl group; or a monocyclic or bicyclic heterocyclic radical chosen from: a pyridyl, an N-oxidopyridinio, a pyrazolyl, an (N-phenyl)pyrazolyl, an (N-halophenyl)pyrazolyl, a furyl, an indolyl, an (N-benzyl)indolyl, an (N-halobenzyl)indolyl, a benzothienyl or a benzofuryl, the said radicals being unsubstituted or substituted one or more times by a halogen atom or a methyl or methoxy group; R4 and R5 are identical or different and each independently represent a hydrogen or halogen atom or a hydroxyl, hydroxymethyl, (C1-C4)alkyl, trifluoromethyl, C1-C4)alkoxy, (C1-C4)alkoxycarbonyl or cyano group. Preparation process and application in therapeutics.

    摘要翻译： 本发明涉及通式（I）的杂环基在3-位上取代的吡啶并吲哚酮衍生物：其中：R 1表示氢原子或（C 1〜 （C 1 -C 4）烷基; R 2表示氢原子或（C 1 -C 4 -C 4）烷基; R 3表示被甲基单取代或多取代的噻吩基; 或选自以下的单环或双环杂环基：吡啶基，N-氧化吡啶基，吡唑基，（N-苯基）吡唑基，（N-卤代苯基）吡唑基，呋喃基，吲哚基，（N-苄基）吲哚基 ，（N-卤代苄基）吲哚基，苯并噻吩基或苯并呋喃基，所述基团是未取代的或被卤素原子或甲基或甲氧基取代一次或多次; R 4和R 5相同或不同，并且各自独立地表示氢或卤素原子或羟基，羟甲基，（C 1 -C 3 - （C 1 -C 4）烷基，三氟甲基，C 1 -C 4烷氧基，（C 1 -C 4 - 4）烷氧基羰基或氰基。 制剂工艺及其在治疗中的应用

    Tetrahydropyridines, preparation method and pharmaceutical compositions containing same
    10.
    发明授权
    Tetrahydropyridines, preparation method and pharmaceutical compositions containing same 失效
    四氢吡啶类，制备方法和含有它们的药物组合物

    公开(公告)号：US06689797B2

    公开(公告)日：2004-02-10

    申请号：US10169528

    申请日：2002-10-15

    申请人： Marco Baroni ,  Bernard Bourrie ,  Rosanna Cardamone ,  Pierre Casellas

    发明人： Marco Baroni ,  Bernard Bourrie ,  Rosanna Cardamone ,  Pierre Casellas

    IPC分类号： A61K3144

    CPC分类号： C07D405/06 ,  C07D409/06

    摘要： The present invention relates to compounds of formula (I): in which R1 represents a hydrogen or halogen atom, or a group CF3; R2 and R3 represent, independently, a hydrogen atom or a methyl group; n and n′ each represent, independently, 0 or 1; * represents the positions of attachment; A represents N or CH; X represents a sulfur or oxygen atom; R4 and R5 represent, independently, a hydrogen atom or a (C1-C6) alkyl group; and also their salts or solvates, to a method for the preparation thereof and to the pharmaceutical compositions containing them.

    摘要翻译： 本发明涉及式（I）化合物：其中R 1表示氢或卤素原子或基团CF 3; R 2和R 3独立地表示氢原子或甲基; n和n'各自独立地表示， 0或1; *表示连接位置; A表示N或CH; X表示硫或氧原子; R4和R5独立地表示氢原子或（C1-C6）烷基;以及它们的盐或 溶剂合物，其制备方法和含有它们的药物组合物。