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1. 发明申请

US20110172274A1 FLUORO-SUBSTITUTED 3,4-DIARYL-4,5-DIHYDRO-1H-PYRAZOLE-1-CARBOXAMIDINE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有CB1拮抗活性的氟取代的3,4-二基-4,5-二氢-1H-吡唑-1-羧酰胺衍生物
公开(公告)号：US20110172274A1
公开(公告)日：2011-07-14
申请号：US12999494
申请日：2009-06-15
申请人： Josephus H.M. Lange , Bernard J. Vliet, Van
发明人： Josephus H.M. Lange , Bernard J. Vliet, Van
IPC分类号： A61K31/454 , C07D401/12 , A61P3/04 , A61P9/00 , A61P25/30 , A61P1/16 , A61P31/00
CPC分类号： C07D401/12
摘要： This invention concerns fluorinated 3,4-diaryl-4,5-dihydro-1H-pyrazole-1-carboxamidine derivatives as cannabinoid-CB1 receptor antagonists, methods for preparing these compounds, novel intermediates useful for the synthesis of said compounds, methods for the preparation of these intermediates, pharmaceutical compositions containing one or more of these dihydropyrazole derivatives as active ingredient, as well as the use of these pharmaceutical compositions for the treatment of obesity and obesity-related cardiovascular disorders, drug addiction, cognition deficits, liver fibrosis and inflammatory disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及作为大麻素-CB1受体拮抗剂的氟化3,4-二芳基-4,5-二氢-1H-吡唑-1-甲脒衍生物，制备这些化合物的方法，可用于合成所述化合物的新中间体，这些中间体的制备，含有一种或多种这些二氢吡唑衍生物作为活性成分的药物组合物，以及这些药物组合物用于治疗肥胖和肥胖相关心血管疾病，药物成瘾，认知缺陷，肝纤维化和炎症的用途疾病化合物具有通式（I），其中符号具有说明书中给出的含义。

2. 发明申请

US20080312276A1 4,5 Dihydro-(1H)-Pyrazole Derivatives as Cannabinoid CB1 Receptor Modulators 有权
标题翻译： 4,5二氢 - （1H） - 吡唑衍生物作为大麻素CB1受体调节剂
公开(公告)号：US20080312276A1
公开(公告)日：2008-12-18
申请号：US12136986
申请日：2008-06-11
申请人： Josephus H.M. Lange , Hendrik C. Wals , Bernard J. Vliet Van , Mahmut Yildirim
发明人： Josephus H.M. Lange , Hendrik C. Wals , Bernard J. Vliet Van , Mahmut Yildirim
IPC分类号： A61K31/4709 , C07D231/06 , C07D401/12 , A61P25/28 , A61K31/415
CPC分类号： C07D231/06 , C07D401/12 , C07D409/04
摘要： The invention is directed to 4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor modulators, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, to methods for preparing novel intermediates useful for their syntheses, and to methods for preparing compositions. The invention also relates to the uses of compounds and compositions administered to patients to achieve a therapeutic effect in multiple sclerosis, traumatic brain injury, pain including chronic pain, neuropathic pain, acute pain and inflammatory pain, osteoporosis, appetite disorders, epilepsy, Alzheimer's disease, Tourette's syndrome, cerebral ischaemia, emesis, nausea, and gastrointestinal disorders.Compounds of the present disclosure are directed to formula (I): wherein the substituents have the definitions given in the specification.
摘要翻译：本发明涉及作为大麻素CB1受体调节剂的4,5-二氢 - （1H） - 吡唑（吡唑啉）衍生物，包含这些化合物的药物组合物，其合成方法，制备用于其合成的新中间体的方法，以及制备组合物的方法。本发明还涉及施用于患者的化合物和组合物在多发性硬化，创伤性脑损伤，疼痛，包括慢性疼痛，神经性疼痛，急性疼痛和炎性疼痛，骨质疏松症，食欲障碍，癫痫，阿尔茨海默病中的治疗效果的用途，Tourette综合征，脑缺血，呕吐，恶心和胃肠道疾病。本公开的化合物涉及式（I）：其中取代基具有说明书中给出的定义。

3. 发明申请

US20100292204A1 SULPHUR CONTAINING PYRAZOLE DERIVATIVES AS SELECTIVE CANNABINOID CB1 RECEPTOR ANTAGONISTS 有权
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：US20100292204A1
公开(公告)日：2010-11-18
申请号：US12844156
申请日：2010-07-27
申请人： Josephus H.M. Lange , Cornelis G. Kruse , Bernard J. Vliet Van
发明人： Josephus H.M. Lange , Cornelis G. Kruse , Bernard J. Vliet Van
IPC分类号： A61K31/397 , A61K31/454 , A61K31/4155 , A61K31/55 , A61P29/00 , A61P25/00 , A61P27/06 , A61P35/00 , A61P15/00 , A61P11/00 , A61P11/06 , A61P9/00 , A61P3/10 , A61P3/06 , A61P1/00
CPC分类号： C07D401/12 , C07D403/12
摘要： The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these 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CB1 / CB2受体亚型选择性的选择性大麻素CB1受体拮抗剂，用于制备这些化合物的方法，可用于合成的新中间体这些吡唑衍生物，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，以及这些药物组合物用于治疗精神和神经障碍的用途。化合物具有通式（I），其中符号具有说明书中给出的含义。

4. 发明申请

US20080214559A1 COMPOUNDS WITH A COMBINATION OF CANNABINOID CB1 ANTAGONISM AND SEROTONIN REUPTAKE INHIBITION 有权
标题翻译：具有CANNABINOID CB1拮抗剂和丝氨酸蛋白酶重排抑制组合的化合物
公开(公告)号：US20080214559A1
公开(公告)日：2008-09-04
申请号：US11970229
申请日：2008-01-07
申请人： Josephus H.M. Lange , Cornelis G. Kruse
发明人： Josephus H.M. Lange , Cornelis G. Kruse
IPC分类号： A61K31/497 , C07D231/38 , C07D233/54 , C07D403/02 , A61P3/04 , A61K31/415 , A61K31/4164
CPC分类号： C07D403/12 , C07D231/06 , C07D233/90
摘要： Compounds with a combination of cannabinoid CB1 antagonism and serotonin re-uptake inhibition, pharmaceutical compositions containing these compounds, methods for preparing these compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing these compositions are disclosed. Uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders are disclosed.In at least one embodiment, the invention relates to compounds of the general formula (1); wherein the substitutents have the definitions given in the specification.
摘要翻译：具有大麻素CB 1拮抗剂和5-羟色胺再吸收抑制的组合的化合物，含有这些化合物的药物组合物，制备这些化合物的方法，制备用于其合成的新中间体的方法及其制备方法公开了组合物。这些化合物和组合物的用途，特别是它们在给予患者以在精神病，焦虑症，抑郁症，注意力缺陷，认知障碍，肥胖症，药物依赖，帕金森病，阿尔茨海默病，疼痛障碍，神经性疼痛障碍中治疗效果方面的用途并且公开了性障碍。在至少一个实施方案中，本发明涉及通式（1）的化合物; 其中取代基具有说明书中给出的定义。

5. 发明申请

US20080153867A1 COMPOUNDS WITH A COMBINATION OF CANNABINOID-CB1 ANTAGONISM AND ACETYLCHOLINESTERASE INHIBITION 有权
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：US20080153867A1
公开(公告)日：2008-06-26
申请号：US11957948
申请日：2007-12-17
申请人： Josephus H.M. Lange , Cornelis G. Kruse , Belal Shadid
发明人： Josephus H.M. Lange , Cornelis G. Kruse , Belal Shadid
IPC分类号： A61K31/4439 , C07D219/12 , A61P35/00 , A61P25/00 , A61P25/28
CPC分类号： C07D401/12
摘要： Embodiments of this invention relate to compounds having a combination of cannabinoid-CB1 antagonism and cholinesterase inhibition, to pharmaceutical compositions comprising these compounds, to methods for preparing these compounds, methods for preparing novel intermediates useful for the synthesis of these compounds, and methods for preparing compositions comprising these compounds. The invention also relates to methods of treating Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficit disorder, traumatic brain injury, drug dependence, addiction or substance abuse by administering a pharmaceutical composition comprising these compounds to a patient in need thereof. A compound with a combination of cannabinoid-CB1 antagonism and cholinesterase inhibition is a compound of formula (1) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明的实施方案涉及具有大麻素-CB 1拮抗作用和胆碱酯酶抑制的组合的化合物，包含这些化合物的药物组合物，制备这些化合物的方法，制备用于合成的新中间体的方法的这些化合物，以及制备包含这些化合物的组合物的方法。本发明还涉及通过向有需要的患者施用包含这些化合物的药物组合物来治疗阿尔茨海默病，认知障碍，记忆障碍，痴呆，注意力缺陷障碍，创伤性脑损伤，药物依赖，成瘾或药物滥用的方法。具有大麻素-CB 1拮抗剂和胆碱酯酶抑制剂的组合的化合物是式（1）的化合物，其中符号具有说明书中给出的含义。

6. 发明申请

US20070281973A1 SULPHUR CONTAINING PYRAZOLE DERIVATIVES AS SELECTIVE CANNABINOID CB1 RECEPTOR ANTAGONISTS 有权
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：US20070281973A1
公开(公告)日：2007-12-06
申请号：US11754544
申请日：2007-05-29
申请人： Josephus H.M. Lange , Cornelis G. Kruse , Bernard J. Van Vliet
发明人： Josephus H.M. Lange , Cornelis G. Kruse , Bernard J. Van Vliet
IPC分类号： A61K31/454 , A61K31/416 , C07D403/02
CPC分类号： C07D401/12 , C07D403/12
摘要： The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these 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，可用于合成这些吡唑衍生物的新中间体，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。

7. 发明申请

US20110237569A1 SPIRO AZEPANE-OXAZOLIDINONES AS Kv1.3 POTASSIUM CHANNEL BLOCKERS 有权
标题翻译： SPIRO AZEPANE-OXAZOLIDINONES作为Kv1.3钾通道阻断剂
公开(公告)号：US20110237569A1
公开(公告)日：2011-09-29
申请号：US13133042
申请日：2009-12-10
申请人： Pieter Smid , Michael Mlinaric , Konrad F. Koehler , Sara Nunez Garcia , Elmar Wegener , Josephus H.M. Lange
发明人： Pieter Smid , Michael Mlinaric , Konrad F. Koehler , Sara Nunez Garcia , Elmar Wegener , Josephus H.M. Lange
IPC分类号： A61K31/55 , C07D498/10 , A61P3/10 , A61P37/02 , A61P3/04
CPC分类号： C07D498/10
摘要： This invention concerns Spiro azepane-ox-azolidinones as voltage gated Kv1.3 potassium channel blockers, pharmaceutical compositions containing these compounds, 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 their use in administering them to patients to achieve a therapeutic effect in the treatment of diabetes, psoriasis, obesity, transplant rejection and inflammatory neuropathies, including T-cell mediated autoimmune diseases such as rheumatoid arthritis and multiple sclerosis. The compounds have formula (1): wherein R1, R2, (R3)n, and (R4)m have the meanings given in the specification.
摘要翻译：本发明涉及作为电压门控的Kv1.3钾通道阻滞剂的螺氮氮杂环庚烷 - 恶唑烷酮，含有这些化合物的药物组合物，制备化合物的方法，制备用于其合成的新中间体的方法和制备组合物的方法。本发明还涉及这些化合物和组合物的用途，特别是它们在将它们施用于患者以在治疗糖尿病，银屑病，肥胖症，移植排斥和炎性神经病中的治疗效果方面的用途，包括T细胞介导的自身免疫性疾病作为类风湿性关节炎和多发性硬化。化合物具有式（1）：其中R1，R2，（R3）n和（R4）m具有本说明书中给出的含义。

8. 发明申请

US20110137040A1 SYNTHESIS OF 3,4-DIARYL-4,5-DIHYDRO-(H)-PYRAZOLE-1-CARBOXAMIDINE DERIVATIVES 审中-公开
标题翻译： 3,4-二基-4,5-二氢 - （（H） - 吡咯-1-羧酰胺衍生物的合成）
公开(公告)号：US20110137040A1
公开(公告)日：2011-06-09
申请号：US13056861
申请日：2009-07-30
申请人： Josephus H.M. Lange , Hans J. Sanders , Jeroen Van Rheenen
发明人： Josephus H.M. Lange , Hans J. Sanders , Jeroen Van Rheenen
IPC分类号： C07D231/06 , C07D401/12
CPC分类号： C07D231/06 , C07D401/12
摘要： The invention relates to a novel chemical route to 3,4-diaryl-4,5-dihydro-(1H)-pyrazole-1-carbox-amidine derivatives, known as potent cannabinoid-CB1 receptor antagonists, and to novel intermediates of these compounds. The synthetic route produced considerably higher yields than those reported, without the use of corrosive reagents. The process concerns the preparation of a compound of formula (I): wherein the symbols have the meanings given in the description.
摘要翻译：本发明涉及一种已知为有效的大麻素-CB1受体拮抗剂的3,4-二芳基-4,5-二氢 - （1H） - 吡唑-1-羧酸 - 脒衍生物的新化学途径，以及这些化合物的新型中间体。合成路线产生的产量高于报道的产量，而不使用腐蚀性试剂。该方法涉及式（I）化合物的制备：其中符号具有说明书中给出的含义。

9. 发明申请

US20130060041A1 SYNTHESIS OF SUBSTITUTED PYRAZOLINE CARBOXAMIDINE DERIVATIVES 有权
标题翻译：取代的吡唑啉羧酰胺衍生物的合成
公开(公告)号：US20130060041A1
公开(公告)日：2013-03-07
申请号：US13574176
申请日：2011-01-27
申请人： Arnold van Loevezijn , Josephus H.M. Lange , Gerrit A. Barf , Arnold P. den Hartog
发明人： Arnold van Loevezijn , Josephus H.M. Lange , Gerrit A. Barf , Arnold P. den Hartog
IPC分类号： C07D231/06 , C07D401/12 , C07D409/04 , C07D491/10 , C07D231/54 , C07D403/12
CPC分类号： C07D231/06 , C07D231/54 , C07D409/04 , C07D409/12 , C07D491/107 , C07D513/10
摘要： This invention relates to organic chemistry, in particular to processes for the preparation of pyrazoline carboxamidine derivatives of formula (I), known as potent 5-HT6 antagonists. The invention also relates to novel intermediates of these compounds. wherein the symbols have the meanings given in the description.
摘要翻译：本发明涉及有机化学，特别涉及称为有效的5-HT 6拮抗剂的式（I）的吡唑啉甲脒衍生物的制备方法。本发明还涉及这些化合物的新型中间体。其中符号具有在说明书中给出的含义。

10. 发明申请

US20110053983A1 (5R)-1,5-DIARYL-4,5-DIHYDRO-1H-PYRAZOLE-3-CARBOXAMIDINE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：（5R）具有CB1拮抗活性的-1,5-二基-4,5-二氢-1H-吡唑-3-羧酰胺衍生物
公开(公告)号：US20110053983A1
公开(公告)日：2011-03-03
申请号：US12988654
申请日：2009-04-22
申请人： Josephus H.M. Lange , Arnold P. Den Hartog , Bernard J. Van Vliet
发明人： Josephus H.M. Lange , Arnold P. Den Hartog , Bernard J. Van Vliet
IPC分类号： A61K31/454 , C07D401/12 , A61P25/00 , A61P3/04 , A61P1/00 , A61P3/10 , A61P11/06 , A61P19/02 , A61P9/00 , A61P35/00
CPC分类号： C07D231/06 , C07D401/12 , C07D403/12
摘要： Embodiments of the invention relate to (5R)-1,5-diaryl-4,5-dihydro-1H-pyrazole-3-carboxamidine derivatives as cannabinoid-CB1 receptor antagonists, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said dihydropyrazole derivatives, to methods for the preparation of these intermediates, pharmaceutical compositions containing one or more of these dihydropyrazole derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders involving cannabinoid receptors. The compounds of embodiments of the invention are compounds of formula (I) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明的实施方案涉及作为大麻素-CB1受体拮抗剂的（5R）-1,5-二芳基-4,5-二氢-1H-吡唑-3-甲脒衍生物，制备这些化合物的方法，可用于新型中间体用于合成所述二氢吡唑衍生物的方法，制备这些中间体的方法，含有一种或多种这些二氢吡唑衍生物作为活性成分的药物组合物，以及这些药物组合物用于治疗精神和神经障碍的用途涉及大麻素受体。本发明实施方案的化合物是式（I）化合物，其中符号具有说明书中给出的含义。

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