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1. 发明申请

WO2007138050A1 SULPHUR CONTAINING PYRAZOLE DERIVATIVES AS SELECTIVE CANNABINOID CB1 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：含硫胺衍生物作为选择性CANNABINOID CB1受体拮抗剂
公开(公告)号：WO2007138050A1
公开(公告)日：2007-12-06
申请号：PCT/EP2007/055192
申请日：2007-05-29
申请人： SOLVAY PHARMACEUTICALS B.V. , LANGE, Josephus H.M. , KRUSE, Cornelis G. , VAN VLIET, Bernard J.
发明人： LANGE, Josephus H.M. , KRUSE, Cornelis G. , VAN VLIET, Bernard J.
IPC分类号： C07D231/18 , A61K31/4155 , A61P25/30
CPC分类号： C07D231/18
摘要： The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB 1 receptor antagonists having a high CB 1 /CB 2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及含硫吡唑衍生物及其S-氧化的活性代谢物，作为具有高CB 1 / CB 2的选择性大麻素CB 1受体拮抗剂受体亚型选择性，制备这些化合物的方法，可用于合成所述吡唑衍生物的新型中间体，包含一种或多种这些吡唑衍生物作为活性成分的药物组合物，以及使用的这些用于治疗精神和神经障碍的药物组合物。化合物具有通式（I），其中符号具有说明书中给出的含义。

2. 发明申请

WO2005074920A1 1,3,5-TRISUBSTITUTED 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有CB1拮抗活性的1,3,5-三唑并[4,5-d]二氢-1H-吡唑衍生物
公开(公告)号：WO2005074920A1
公开(公告)日：2005-08-18
申请号：PCT/EP2005/050339
申请日：2005-01-27
申请人： SOLVAY PHARMACEUTICALS B.V. , LANGE, Josephus H.M. , KRUSE, Cornelis G. , VAN STUIVENBERG, Herman H.
发明人： LANGE, Josephus H.M. , KRUSE, Cornelis G. , VAN STUIVENBERG, Herman H.
IPC分类号： A61K31/4155
CPC分类号： C07D231/06
摘要： The present invention relates to 1,3,5-trisubstituted 4,5-dihydro-1 H-pyrazole derivatives as CB 1 antagonists, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said pyrazole derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及作为CB1拮抗剂的1,3,5-三取代的4,5-二氢-1H-吡唑衍生物，用于制备这些化合物的方法和用于合成所述吡唑衍生物的新型中间体。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。化合物具有通式（I），其中符号具有说明书中给出的含义。

3. 发明申请

WO2008074816A1 COMPOUNDS WITH A COMBINATION OF CANNABINOID-CB1 ANTAGONISM AND ACETYLCHOLINESTERASE INHIBITION 审中-公开
标题翻译：具有CANNABINOID-CB1拮抗剂和乙酰胆碱酯酶抑制剂的组合的化合物
公开(公告)号：WO2008074816A1
公开(公告)日：2008-06-26
申请号：PCT/EP2007/064169
申请日：2007-12-19
申请人： SOLVAY PHARMACEUTICALS B.V. , LANGE, Josephus H.M. , KRUSE, Cornelis G. , SHADID, Belal
发明人： LANGE, Josephus H.M. , KRUSE, Cornelis G. , SHADID, Belal
IPC分类号： C07D401/12 , A61K31/473 , A61P25/28 , A61P25/30 , A61P25/24
CPC分类号： C07D401/12
摘要： Thisinvention concerns compounds with a combination of cannabinoid-CB 1 antagonism and cholinesterase inhibition, to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly for treating Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficits, traumatic brain injury, drug dependence, addiction and substance abuse. In particular the invention relates to compounds of the general Formula (1) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及具有大麻素-CB 1拮抗剂和胆碱酯酶抑制的组合的化合物，含有这些化合物的药物组合物，制备该化合物的方法，制备用于其合成的新中间体的方法和制备组合物。本发明还涉及这些化合物和组合物，特别是用于治疗阿尔茨海默病，认知障碍，记忆障碍，痴呆，注意力缺陷，创伤性脑损伤，药物依赖，成瘾和药物滥用的用途。具体而言，本发明涉及通式（1）的化合物，其中符号具有说明书中给出的含义。

4. 发明申请

WO2005118553A1 TETRASUBSTITUTED IMIDAZOLE DERIVATIVES AS CANNABINOID CB1 RECEPTOR MODULATORS WITH A HIGH CB1/CB2 RECEPTOR SUBTYPE SELECTIVITY 审中-公开
标题翻译：作为具有高CB1 / CB2受体亚型选择性的CANNABINOID CB1受体调节剂的四唑基咪唑衍生物
公开(公告)号：WO2005118553A1
公开(公告)日：2005-12-15
申请号：PCT/EP2005/052405
申请日：2005-05-26
申请人： SOLVAY PHARMACEUTICALS B.V. , LANGE, JOSEPHUS H.M. , WALS, Henderik C. , KRUSE, Cornelis G.
发明人： LANGE, JOSEPHUS H.M. , WALS, Henderik C. , KRUSE, Cornelis G.
IPC分类号： C07D233/90
CPC分类号： C07D233/90
摘要： The present invention relates to 1,2,4,5-tetrasubstituted imidazole derivatives as selective cannabinoid CB 1 receptor modulators, in particular CB 1 receptor antagonists or inverse agonists having a high CB 1 /CB 2 receptor subtype selectivity, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said imidazole derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. A beneficial effect is disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. The invention also relates to the use of a compound of the invention for the manufacture of a medicament for treating or preventing a disease or condition. More particularly, the invention relates to a new use for the treatment of a disease or condition disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. In embodiments of the invention specific compounds disclosed herein are used for the manufacture of a medicament useful in the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及作为选择性大麻素CB1受体调节剂的1,2,4,5-四取代咪唑衍生物，特别是具有高CB1 / CB2受体亚型选择性的CB1受体拮抗剂或反向激动剂，用于制备这些化合物的方法和涉及可用于合成所述咪唑衍生物的新型中间体。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。本领域技术人员从本领域的说明书和一般知识中可以公开有益效果或显而易见的。本发明还涉及本发明化合物在制备用于治疗或预防疾病或病症的药物中的用途。更具体地，本发明涉及本领域技术人员从本领域技术人员的说明书和一般知识中治疗本文公开的疾病或病症的新用途。在本发明的实施方案中，本文公开的具体化合物用于制备用于治疗精神病和神经障碍的药物。化合物具有通式（I），其中符号具有说明书中给出的含义。

5. 发明申请

WO2005040130A1 1H-IMIDAZOLE DERIVATIVES AS CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译： 1H-咪唑衍生物作为CANNABINOID受体调节剂
公开(公告)号：WO2005040130A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/052575
申请日：2004-10-19
申请人： SOLVAY PHARMACEUTICALS B.V. , LANGE, Josephus H.M. , KRUSE, Cornelis G. , VAN STUIVENBERG, Herman H. , KEIZER, Hiskias G.
发明人： LANGE, Josephus H.M. , KRUSE, Cornelis G. , VAN STUIVENBERG, Herman H. , KEIZER, Hiskias G.
IPC分类号： C07D233/90
CPC分类号： C07D233/90
摘要： The invention relates to a group of 1H -imidazole derivatives which are modulators of cannabinoid receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders in which cannabinoid receptors are involved. The compounds have the general formula (I) wherein R, R 1 -R 4 and X have the meanings given in the specification.
摘要翻译：本发明涉及一组1H-咪唑衍生物，其是大麻素受体的调节剂，制备这些化合物的方法，可用于合成所述咪唑衍生物的新中间体，制备这些中间体的方法，药物含有这些1H-咪唑衍生物中的一种或多种作为活性成分的组合物，以及这些药物组合物用于治疗涉及大麻素受体的精神病和神经障碍的用途。所述化合物具有通式（I），其中R，R 1 -R 4和X具有说明书中给出的含义。

6. 发明申请

WO2005028456A1 THIAZOLE DERIVATIVES AS CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译：作为CANNABINOID受体调节剂的噻唑衍生物
公开(公告)号：WO2005028456A1
公开(公告)日：2005-03-31
申请号：PCT/EP2004/052239
申请日：2004-09-20
申请人： SOLVAY PHARMACEUTICALS B.V. , LANGE, Josephus H.M. , KRUSE, Cornelis G. , VAN STUIVENBERG, Herman H. , SLIEDREGT, Leonardus A.J.M.
发明人： LANGE, Josephus H.M. , KRUSE, Cornelis G. , VAN STUIVENBERG, Herman H. , SLIEDREGT, Leonardus A.J.M.
IPC分类号： C07D277/24
CPC分类号： A61K31/427 , A61K31/4439 , C07D277/24 , C07D277/56 , C07D417/12
摘要： The present invention relates to a group of thiazole derivatives, to methods for the preparation of these compounds, to pharmaceutical compositions containing at least one these compounds as active ingredient, as well to the use of these compositions for the treatment of psychiatric and neurological disorders and other diseases involving cannabinoid CB neurotransmission. 'The thiazole derivatives of the invention are either cannabinoid (CB) receptor antagonists, CB receptor antagonists, CB receptor inverse agonists or CB receptor partial agonists.The compounds have the general formula (l) wherein R, R 1 and X have the meanings given in the specification.
摘要翻译：本发明涉及一组噻唑衍生物，制备这些化合物的方法，含有至少一种这些化合物作为活性成分的药物组合物，以及这些组合物用于治疗精神和神经障碍的用途，以及其他涉及大麻素CB神经传递的疾病。本发明的噻唑衍生物是大麻素（CB）受体拮抗剂，CB受体拮抗剂，CB受体反向激动剂或CB受体部分激动剂。化合物具有通式（1），其中R，R 1和X具有规格。

7. 发明申请

WO2004026301A1 1H-1,2,4-TRIAZOLE-3-CARBOXAMIDE DERIVATIVES AS CANNABINOID-CB1 RECEPTOR LIGANDS 审中-公开
标题翻译：作为CANNABINOID-CB1受体配体的1H-1,2,4-三唑-3-羧酰胺衍生物
公开(公告)号：WO2004026301A1
公开(公告)日：2004-04-01
申请号：PCT/EP2003/050628
申请日：2003-09-17
申请人： SOLVAY PHARMACEUTICALS B.V. , LANGE, Josephus H.M. , KRUSE, Cornelis G. , McCREARY, Andrew C. , VAN STUIVENBERG, Herman H.
发明人： LANGE, Josephus H.M. , KRUSE, Cornelis G. , McCREARY, Andrew C. , VAN STUIVENBERG, Herman H.
IPC分类号： A61K31/41
CPC分类号： A61K31/41 , C07D249/10
摘要： The present invention relates to a group of 1H-1,2,4-triazole-3-carboxamide derivatives, to methods for the preparation of these compounds, and to pharmaceutical compositions containing at least one of these compounds as an active ingredient. These 1H-1,2,4-triazole-3-carboxamide derivatives are potent cannabinoid-CB 1 receptor agonists, partial agonists, inverse agonists or antagonists, useful for the treatment of disorders involving cannabinoid neurotransmission. The compounds have the general formula (I), wherein R and R 1 -R 3 have the meanings given in the specification.
摘要翻译：本发明涉及一组1H-1,2,4-三唑-3-甲酰胺衍生物，制备这些化合物的方法，以及含有至少一种这些化合物作为活性成分的药物组合物。这些1H-1,2,4-三唑-3-甲酰胺衍生物是可用于治疗涉及大麻素神经传递的病症的有效的大麻素-CB1受体激动剂，部分激动剂，反向激动剂或拮抗剂。化合物具有通式（I），其中R和R 1 -R 3具有说明书中给出的含义。

8. 发明申请

WO2006061376A1 ARYLOXYETHYLAMINE DERIVATIVES WITH A COMBINATION OF PARTIAL D0PAMINE-D2 RECEPTOR AGONISM AND SEROTONIN REUPTAKE INHIBITION 审中-公开
标题翻译：具有部分D0PAMINE-D2受体激动剂和丝氨酸蛋白酶重复抑制组合的芳基乙酰胺衍生物
公开(公告)号：WO2006061376A1
公开(公告)日：2006-06-15
申请号：PCT/EP2005/056505
申请日：2005-12-06
申请人： SOLVAY PHARMACEUTICALS B.V. , FEENSTRA, Roelof W. , STOIT, Axel , TERPSTRA, Jan-willem , PRAS-RAVES, Maria L. , MCCREARY, Andrew C. , VAN VLIET, Bernard J. , HESSELINK, Mayke B. , KRUSE, Cornelis G. , VAN SCHARRENBURG, Gustaaf J.m.
发明人： FEENSTRA, Roelof W. , STOIT, Axel , TERPSTRA, Jan-willem , PRAS-RAVES, Maria L. , MCCREARY, Andrew C. , VAN VLIET, Bernard J. , HESSELINK, Mayke B. , KRUSE, Cornelis G. , VAN SCHARRENBURG, Gustaaf J.m.
IPC分类号： A61K31/423 , C07D263/58 , C07D413/12 , A61P25/00
CPC分类号： C07D263/58 , C07D413/12
摘要： The invention relates to a group of novel aryloxyethylamine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine -D 2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): Z-T-Ar wherein: Z is a fragment of the general formula (2): and wherein the other symbols have the meanings given in the specification, and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.
摘要翻译：本发明涉及一组具有双重作用模式的新型芳氧基乙胺衍生物：5-羟色胺再摄取抑制和对多巴胺-D2受体的部分激动作用。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。所述化合物具有通式（1）：ZT-Ar其中：Z是通式（2）的片段：其中，其它符号具有本说明书中给出的含义及其互变异构体，立体异构体和N-氧化物，以及所述式（1）化合物及其互变异构体，立体异构体和N-氧化物的药理学上可接受的盐，水合物和溶剂化物。

9. 发明申请

WO2006061379A1 PHENYLPIPERAZINE DERIVATIVES WITH A COMBINATION OF PARTIAL DOPAMINE-D2 RECEPTOR AGONISM AND SEROTONIN REUPTAKE INHIBITION 审中-公开
标题翻译：具有部分多巴胺-D2受体激动剂和丝氨酸蛋白酶重复抑制的组合的苯基哌嗪衍生物
公开(公告)号：WO2006061379A1
公开(公告)日：2006-06-15
申请号：PCT/EP2005/056508
申请日：2005-12-06
申请人： SOLVAY PHARMACEUTICALS B.V. , FEENSTRA, Roelof W. , STOIT, Axel , TERPSTRA, Jan-Willem , PRAS-RAVES, Maria L. , MCCREARY, Andrew C. , VAN VLIET, Bernard J. , HESSELINK, Mayke B. , KRUSE, Cornelis G. , VAN SCHARRENBURG, Gustaaf J.M.
发明人： FEENSTRA, Roelof W. , STOIT, Axel , TERPSTRA, Jan-Willem , PRAS-RAVES, Maria L. , MCCREARY, Andrew C. , VAN VLIET, Bernard J. , HESSELINK, Mayke B. , KRUSE, Cornelis G. , VAN SCHARRENBURG, Gustaaf J.M.
IPC分类号： A61K31/423 , C07D413/12 , A61P25/00
CPC分类号： C07D263/58 , C07D413/12
摘要： The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine -D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及一组具有双重作用方式的新型苯基哌嗪衍生物：5-羟色胺再摄取抑制和对多巴胺-D2受体的部分激动作用。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。化合物具有通式（1），其中符号具有说明书中给出的含义。

10. 发明申请

WO2008034863A2 SULFONYLPYRAZOLE AND SULFONYLPYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS 审中-公开
标题翻译：作为5-HT6拮抗剂的磺酰基吡唑和磺酰基吡唑烷酮衍生物
公开(公告)号：WO2008034863A2
公开(公告)日：2008-03-27
申请号：PCT/EP2007/059944
申请日：2007-09-20
申请人： SOLVAY PHARMACEUTICALS B.V. , IWEMA BAKKER, Wouter I. , KEIZER, Hiskias G. , NEUT, VAN DER, Martina A.W. , KRUSE, Cornelis G. , LOEVEZIJN, VAN, Arnold , ZORGDRAGER, Jan
发明人： IWEMA BAKKER, Wouter I. , KEIZER, Hiskias G. , NEUT, VAN DER, Martina A.W. , KRUSE, Cornelis G. , LOEVEZIJN, VAN, Arnold , ZORGDRAGER, Jan
IPC分类号： C07D231/06 , C07D401/12 , C07D409/12 , C07D513/04 , C07D417/12 , C07D403/12 , C07D231/12 , A61K31/415 , A61K31/4155 , A61P25/00 , C07D401/04 , C07D407/04
CPC分类号： C07D513/04 , A61K9/0019 , A61K9/0031 , A61K9/1652 , A61K9/2054 , C07D231/06 , C07D231/12 , C07D231/54 , C07D231/56 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/10 , C07D491/10 , C07D491/107 , C07D519/00
摘要： This invention concerns sulfonylpyrazoline carboxamidine derivatives as antagonists of 5-HT 6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes. The compounds have the general formula (1), wherein the symbols have the meanings given in the description.
摘要翻译：本发明涉及作为5-HT 6受体拮抗剂的磺酰吡唑啉甲脒衍生物，涉及制备这些化合物的方法和用于它们合成的新型中间体。本发明还涉及这些化合物和组合物的用途，特别是它们在给予患者以在帕金森病，亨廷顿氏舞蹈症，精神分裂症，焦虑症，抑郁症，躁狂抑郁症，精神病，癫痫，强迫症中的治疗效果方面的用途，情绪障碍，偏头痛，阿尔茨海默病，年龄相关认知衰退，轻度认知障碍，睡眠障碍，进食障碍，厌食症，贪食症，暴饮暴食症，惊恐发作，静坐不动，注意力缺陷多动障碍，注意力缺陷障碍，可卡因滥用，乙醇，尼古丁或苯并二氮杂，疼痛，与脊髓损伤或头部损伤相关的疾病，脑积水，功能性肠病，肠易激综合征，肥胖症和2型糖尿病。化合物具有通式（1），其中符号具有说明书中给出的含义。

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