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11.发明授权Pyrazolecarboxylic acid derivatives, their preparation and pharmaceutical compositions containing them, and method of treating 有权吡唑羧酸衍生物，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
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。
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12.发明授权Pyrazolecarboxylic acid derivatives, their preparation, pharmaceutical compositions containing them 有权吡唑羧酸衍生物，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
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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13.发明授权1-benzylpyrazole-3-carboxylic acid tricyclic derivatives as cannabinoid receptor antagonists 有权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
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。
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14.发明授权
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。
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15.发明申请Derivative of 5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidine-1-yl)-1H-pyrazole-3-carboxamide, the preparation and therapeutic use thereof 审中-公开5-（4-溴苯基）-1-（2,4-二氯苯基）-4-乙基-N-（哌啶-1-基）-1H-吡唑-3-甲酰胺的衍生物，其制备和治疗用途公开(公告)号：US20060004055A1
公开(公告)日：2006-01-05
申请号：US11159779
申请日：2005-06-23
IPC分类号： A61K31/454 , C07D43/02
CPC分类号： C07D401/12
摘要： The invention relates to a derivative of 5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide of general formula (I): Preparation process and therapeutic use.
摘要翻译： 本发明涉及通式（5）的5-（4-溴苯基）-1-（2,4-二氯苯基）-4-乙基-N-（哌啶-1-基）-1H-吡唑-3-甲酰胺的衍生物 I）：制备过程和治疗用途。
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