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1. 发明授权

US5925768A 3-pyrazolecarboxamide derivatives having cannabinoid receptor affinity 失效
标题翻译：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。

2. 发明授权

US6013648A 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. 发明授权

US06916838B1 1-benzylpyrazole-3-carboxylic acid tricyclic derivatives as cannabinoid receptor antagonists 有权
标题翻译： 1-苄基吡唑-3-羧酸三环衍生物作为大麻素受体拮抗剂
公开(公告)号：US06916838B1
公开(公告)日：2005-07-12
申请号：US10111916
申请日：2000-11-02
申请人： Francis Barth , Joseph Millan , Didier Oustric , Murielle Rinaldi , Martine Vernhet
发明人： Francis Barth , Joseph Millan , Didier Oustric , Murielle Rinaldi , Martine Vernhet
IPC分类号： A61K31/416 , A61P1/00 , A61P1/04 , A61P1/06 , A61P1/08 , A61P3/10 , A61P7/00 , A61P7/06 , A61P9/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P19/08 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/28 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P33/00 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D231/54
CPC分类号： C07D231/54
摘要： Tricyclic derivatives of 1-benzylpyrazole-3-carboxylic acid which are antagonists of the cannabinoid CB2 receptors; their method of preparation and pharmaceutical compositions containing them.
摘要翻译： 1-苄基吡唑-3-羧酸的三环衍生物<？img id =“CUSTOM-CHARACTER-00001”he =“279.40mm”wi =“215.90mm”file =“US06916838-20050712-P00900.TIF”alt =“custom 作为大麻素CB 2受体的拮抗剂的字符“img-content =”character“img-format =”tif“？其制备方法和含有它们的药物组合物。

4. 发明授权

US5462960A Pyrazole-3-carboxamide derivatives, process for their preparation and pharmaceutical compositions in which they are present 失效
标题翻译：吡唑-3-甲酰胺衍生物，其制备方法及其存在的药物组合物
公开(公告)号：US5462960A
公开(公告)日：1995-10-31
申请号：US357880
申请日：1994-12-16
申请人： Francis Barth , Pierre Casellas , Christian Congy , Serge Martinez , Murielle Rinaldi
发明人： Francis Barth , Pierre Casellas , Christian Congy , Serge Martinez , Murielle Rinaldi
IPC分类号： A61K31/415 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/55 , A61P25/00 , A61P25/18 , A61P43/00 , C07D231/14 , C07D401/12 , C07D471/08
CPC分类号： C07D231/14
摘要： The present invention relates to novel pyrazole-3-carboxamide derivatives of the formula ##STR1## in which the substituents are as defined in the specification. The present invention further relates to a process for the preparation of these novel derivatives and to the pharmaceutical compositions in which they are present.
摘要翻译：本发明涉及式（I）的新的吡唑-3-甲酰胺衍生物，其中取代基如说明书中所定义。本发明还涉及制备这些新型衍生物的方法及其存在的药物组合物。

5. 发明授权

US5624941A Pyrazole derivatives, method of preparing them and pharmaceutical compositions in which they are present 失效
标题翻译：吡唑衍生物，其制备方法和它们存在的药物组合物
公开(公告)号：US5624941A
公开(公告)日：1997-04-29
申请号：US348881
申请日：1994-11-29
申请人： Francis Barth , Pierre Casellas , Christian Congy , Serge Martinez , Murielle Rinaldi , Gilles Anne-Archard
发明人： Francis Barth , Pierre Casellas , Christian Congy , Serge Martinez , Murielle Rinaldi , Gilles Anne-Archard
IPC分类号： A61K31/415 , A61K31/4155 , A61K31/4402 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/5375 , A61K31/553 , A61P1/08 , A61P9/00 , A61P9/10 , A61P11/06 , A61P11/08 , A61P21/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/28 , A61P27/02 , A61P27/06 , A61P37/00 , A61P37/02 , A61P37/06 , A61P43/00 , C07D20060101 , C07D231/12 , C07D231/14 , C07D231/38 , C07D231/40 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D453/02 , C07D493/08
CPC分类号： C07D231/12 , C07D231/14 , C07D231/40 , C07D401/12 , C07D403/12 , C07D405/12 , C07D493/08
摘要： The present invention relates to compounds of the formula: ##STR1## These compounds are useful in pharmaceuticals in which cannabis is known to be involved.
摘要翻译：本发明涉及下式的化合物：（I）这些化合物可用于已知涉及大麻的药物中。

6. 发明申请

US20050192332A1 Pyrazolecarboxylic acid tricyclic derivatives, preparation and pharmaceutical compositions containing same 有权
公开(公告)号：US20050192332A1
公开(公告)日：2005-09-01
申请号：US11119074
申请日：2005-04-29
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： A61K31/4162 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/55 , A61P1/00 , A61P1/12 , A61P3/04 , A61P3/10 , A61P13/00 , A61P15/00 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P29/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07D231/54 , C07D231/56 , C07D401/12 , C07D495/04 , C07D498/02
CPC分类号： C07D231/56 , C07D231/54 , C07D495/04
摘要： The subject of the invention is tricyclic derivatives of pyrazolecarboxylic acid of formula: in which R1 represents a C3-C15 carboxyl radical or an NR2R3 group. The invention also relates to the method for preparing the compounds of formula (I), pharmaceutical compositions containing them. The compounds of formula (I) are active on cannabinoid CB1 receptors.

7. 发明授权

US06995184B2 3-arylindole derivatives and their use as CB2 receptor agonists 失效
标题翻译： 3-芳基吲哚衍生物及其作为CB2受体激动剂的用途
公开(公告)号：US06995184B2
公开(公告)日：2006-02-07
申请号：US10416617
申请日：2001-11-21
申请人： Francis Barth , Christian Congy , Carole Guillaumont , Murielle Rinaldi , Fabienne Vasse , Claude Vernhet
发明人： Francis Barth , Christian Congy , Carole Guillaumont , Murielle Rinaldi , Fabienne Vasse , Claude Vernhet
IPC分类号： A61K31/404 , A61K31/405 , C07D209/08
CPC分类号： C07D209/12
摘要： A subject-matter of the present invention is compounds of formula: and their preparation and the pharmaceutical compositions comprising them. These compounds are agonists for CB2 cannabinoid receptors.
摘要翻译：本发明的主题是下式的化合物：化学式id =“CHEM-US-00001”num =“000

8. 发明授权

US06906080B1 Pyrazolecarboxylic acid tricyclic derivatives, preparation and pharmaceutical compositions containing same 有权
标题翻译：吡唑羧酸三环衍生物，制剂和含有它们的药物组合物
公开(公告)号：US06906080B1
公开(公告)日：2005-06-14
申请号：US10111765
申请日：2000-11-02
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： A61K31/4162 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/55 , A61P1/00 , A61P1/12 , A61P3/04 , A61P3/10 , A61P13/00 , A61P15/00 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P29/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07D231/54 , C07D231/56 , C07D401/12 , C07D495/04
CPC分类号： C07D231/56 , C07D231/54 , C07D495/04
摘要： The subject of the invention is tricyclic derivatives of pyrazolecarboxylic acid of formula: in which R1 represents a C3-C15 carboxyl radical or an NR2R3 group. The invention also relates to the method for preparing the compounds of formula (I), pharmaceutical compositions containing them. The compounds of formula (I) are active on cannabinoid CB1 receptors.
摘要翻译：本发明的主题是下式的吡唑羧酸的三环衍生物：其中R 1代表C 3 -C 15羧基或 NR 2 R 3 N 3基团。本发明还涉及制备式（I）化合物的方法，含有它们的药物组合物。式（I）化合物在大麻素CB 1受体上是有活性的。

9. 发明授权

US06645985B2 Pyrazolecarboxylic acid derivatives, their preparation and pharmaceutical compositions containing them, and method of treating 有权
标题翻译：吡唑羧酸衍生物，其制备方法和含有它们的药物组合物，以及治疗方法
公开(公告)号：US06645985B2
公开(公告)日：2003-11-11
申请号：US10165140
申请日：2002-06-07
申请人： Francis Barth , Philippe Camus , Serge Martinez , Murielle Rinaldi
发明人： Francis Barth , Philippe Camus , Serge Martinez , Murielle Rinaldi
IPC分类号： A61K314427
CPC分类号： C07D231/14 , C07C251/80
摘要： N-Piperidino-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole -3-carboxamide and its salts and solvates are powerful antagonists of the CB1 cannabinoid receptors. They are prepared by reacting a functional derivative of 5-(4-bromophenyl)-1-(2,4-dichlorophenyl) -4-ethylpyrazole-3-carboxylic acid with 1-aminopiperidine, optionally followed by salification.
摘要翻译： N-哌啶子基-5-（4-溴苯基）-1-（2,4-二氯苯基）-4-乙基吡唑-3-甲酰胺及其盐和溶剂合物是CB1大麻素受体的强力拮抗剂。它们通过使5-（4-溴苯基）-1-（2,4-二氯苯基）-4-乙基吡唑-3-羧酸的官能衍生物与1-氨基哌啶反应制备，任选地随后进行成盐。

10. 发明授权

US06432984B1 Pyrazolecarboxylic acid derivatives, their preparation, pharmaceutical compositions containing them 有权
标题翻译：吡唑羧酸衍生物，其制备方法，含有它们的药物组合物
公开(公告)号：US06432984B1
公开(公告)日：2002-08-13
申请号：US09890242
申请日：2001-07-27
申请人： Francis Barth , Philippe Camus , Serge Martinez , Murielle Rinaldi
发明人： Francis Barth , Philippe Camus , Serge Martinez , Murielle Rinaldi
IPC分类号： A61K31454
CPC分类号： C07D231/14 , C07C251/80
摘要： N-Piperidino-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxamide and its salts and solvates are powerful antagonists of the CB1 cannabinoid receptors. They are prepared by reacting a functional derivative of 5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxylic acid with 1-aminopiperidine, optionally followed by salification.
摘要翻译： N-哌啶子基-5-（4-溴苯基）-1-（2,4-二氯苯基）-4-乙基吡唑-3-甲酰胺及其盐和溶剂合物是CB1大麻素受体的强力拮抗剂。它们通过使5-（4-溴苯基）-1-（2,4-二氯苯基）-4-乙基吡唑-3-羧酸的官能衍生物与1-氨基哌啶反应制备，任选地随后进行成盐

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