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15 条记录 (耗时 0.061 秒)

    Pyrazole derivatives, method for preparing same, and pharmaceutical compositions containing said derivatives
    3.
    发明授权
    Pyrazole derivatives, method for preparing same, and pharmaceutical compositions containing said derivatives 失效
    吡唑衍生物，其制备方法和含有所述衍生物的药物组合物

    公开(公告)号：US6028084A

    公开(公告)日：2000-02-22

    申请号：US068869

    申请日：1998-05-19

    申请人： Francis Barth ,  Christian Congy ,  Serge Martinez ,  Murielle Rinaldi

    发明人： Francis Barth ,  Christian Congy ,  Serge Martinez ,  Murielle Rinaldi

    IPC分类号： A61K31/00 ,  A61K31/415 ,  A61K31/445 ,  A61K31/4453 ,  A61P25/00 ,  A61P43/00 ,  C07D231/14 ,  C07D401/12

    CPC分类号： C07D231/14

    摘要： Compounds of formula (I), wherein R.sub.1 is fluorine, hydroxy, (C.sub.1-5) alkoxy, (C.sub.1-5) alkylthio, hydroxy(C.sub.1-5)alkoxy, a -NR.sub.10 R.sub.11, group, cyano, (C.sub.1-5) alkyl-sulphonyl or (C.sub.1-5) alkylsulphinyl; R.sub.2 and R.sub.3 are each (C,.sub.4) alkyl or, taken together with the nitrogen atom to which they are attached, form a saturated or unsaturated 5- to 10-membered heterocyclic radical optionally substituted one or more times by (C.sub.1-3) alkyl or (C.sub.1-3) alkoxy; each of R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 is independently hydrogen, halogen or trifluoromethyl, and when R.sub.1 is fluorine, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and/or R.sub.9 may also be fluoromethyl; with the proviso that at least one of substituents R.sub.4 or R.sub.7. is other than hydrogen; each of R.sub.10 and R.sub.11 is independently hydrogen or (C.sub.1-5) alkyl, or R.sub.10 and R.sub.11, taken together with the nitrogen atom to which they are attached, form a heterocyclic radical selected from pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or piperazin-1-yl optionally substituted by (C.sub.1-4) alkyl; a method for preparing same, and pharmaceutical compositions containing said compounds, are disclosed. Said compounds have very high affinity for central cannabinoid receptors. ##STR1##

    摘要翻译： PCT No.PCT / FR96 / 01847 Sec。 371日期1998年5月19日 102（e）日期1998年5月19日PCT 1996年11月21日PCT PCT。 第WO97 / 19063号公报 日期：1997年5月29日，式（I）的化合物，其中R 1为氟，羟基，（C 1-5）烷氧基，（C 1-5）烷硫基，羟基（C 1-5）烷氧基，-NR 10 R 11基，氰基，（C 1 -5）烷基磺酰基或（C 1-5）烷基亚磺酰基; R 2和R 3各自为（C 1-4）烷基，或与它们所连接的氮原子一起形成任选被（C 1-3）取代一次或多次的饱和或不饱和的5至10元杂环基， 烷基或（C 1-3）烷氧基; R4，R5，R6，R7，R8和R9各自独立地是氢，卤素或三氟甲基，当R1是氟时，R4，R5，R6，R7，R8和/或R9也可以是氟甲基; 条件是至少一个取代基R4或R7。 不是氢; R 10和R 11各自独立地为氢或（C 1-5）烷基，或者R 10和R 11与它们所连接的氮原子一起形成选自吡咯烷-1-基，哌啶-1-基 ，任选被（C 1-4）烷基取代的吗啉-4-基或哌嗪-1-基; 公开了其制备方法和含有所述化合物的药物组合物。 所述化合物对中枢大麻素受体具有非常高的亲和力。

    CB.sub.2 Receptor agonist compounds
    4.
    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.