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1. 发明申请

WO2007136607A3 SUBSTITUTED ESTERS AS CANNABINOID-1 RECEPTOR MODULATORS 审中-公开
标题翻译：作为CANNABINOID-1受体调节剂的替代品
公开(公告)号：WO2007136607A3
公开(公告)日：2008-05-08
申请号：PCT/US2007011548
申请日：2007-05-14
申请人： MERCK & CO INC , COLANDREA VINCENT J , HAGMANN WILLIAM K , HALE JEFFREY J , WHITNEY IRENE E
发明人： COLANDREA VINCENT J , HAGMANN WILLIAM K , HALE JEFFREY J , WHITNEY IRENE E
IPC分类号： C07D221/00 , C07C229/00 , C07D231/00 , C07D263/02 , C07D277/04
CPC分类号： C07C255/60 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D213/79 , C07D213/80 , C07D231/14 , C07D233/90 , C07D239/28 , C07D241/28 , C07D249/06 , C07D257/04 , C07D261/18 , C07D263/34 , C07D271/06 , C07D271/08 , C07D285/06 , C07D307/24 , C07D307/33 , C07D417/04 , C07D471/04 , C07D487/04 , C07D513/04
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，阿尔茨海默病，偏头痛，神经病，包括多发性硬化症和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症的中枢作用药物脑血管意外，头部创伤，焦虑障碍，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻，肝硬化，非酒精性脂肪性肝病（NAFLD ），非酒精性脂肪性肝炎（NASH），以及促进觉醒。

2. 发明申请

WO2004029204A3 SUBSTITUTED PYRIMIDINES 审中-公开
标题翻译：取代的嘧啶
公开(公告)号：WO2004029204A3
公开(公告)日：2004-06-17
申请号：PCT/US0330161
申请日：2003-09-23
申请人： MERCK & CO INC , KOPKA IHOR E , LI BING , HAGMANN WILLIAM K
发明人： KOPKA IHOR E , LI BING , HAGMANN WILLIAM K
IPC分类号： A61K31/505 , A61K31/513 , A61P25/18 , A61P25/28 , C07D239/28 , C07D239/34 , C07D239/38 , C07D239/42 , C07D239/46 , C07D239/52 , C07D239/54 , C07D239/56 , C07D401/12 , C07D487/08 , A61K31/506 , C07D239/36 , C07D239/47 , C07D239/48 , C07D239/58
CPC分类号： C07D239/28 , C07D239/34 , C07D239/38 , C07D239/42 , C07D239/47 , C07D239/52 , C07D239/54 , C07D239/56 , C07D401/12 , C07D487/08
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，并且可用于治疗，预防和抑制由CB1受体介导的疾病。本发明化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化症和格林 - 巴利综合征的神经炎症和病毒性脑炎的炎性后遗症，脑血管障碍事故和头部创伤，焦虑症，压力，癫痫，帕金森病，运动障碍和精神分裂症。该化合物还可用于治疗物质滥用障碍，肥胖或饮食失调的治疗，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

3. 发明申请

WO03063781A2 SUBSTITUTED IMIDAZOLES AS CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译：取代的咪唑烷作为CANNABINOID受体调节剂
公开(公告)号：WO03063781A2
公开(公告)日：2003-08-07
申请号：PCT/US0302351
申请日：2003-01-24
申请人： MERCK & CO INC , HAGMANN WILLIAM K , QI HONGBO , SHAH SHRENIK K
发明人： HAGMANN WILLIAM K , QI HONGBO , SHAH SHRENIK K
IPC分类号： A61K31/4164 , A61K31/4178 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/55 , C07D233/90 , A61K
CPC分类号： A61K31/454 , A61K31/4164 , A61K31/4178 , A61K31/496 , A61K31/5377 , A61K31/55 , C07D233/90
摘要： Compounds of the present invention are antagonists and/or inverse agonists of the Cannabinoid−1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the Cannabinoid−1 (CB1) receptor. The compounds of the present invention are useful as psychotropic drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro−inflammatory disorders including multiple sclerosis and Guillain−Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as, the treatment of asthma, constipation, chronic intestinal pseudo−obstruction, and cirrhosis of the liver. Particular novel compounds of structural formula (I) are also claimed.
摘要翻译：本发明化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制大麻素-1（CB1）受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管意外的精神药物，头部创伤，焦虑障碍，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物也可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。还要求具体结构式（I）的新颖化合物。

4. 发明申请

WO2008024284A3 SULFONYLATED PIPERAZINES AS CANNABINOID-1 RECEPTOR MODULATORS 审中-公开
标题翻译：磺酰化哌嗪作为大麻素-1受体调节剂
公开(公告)号：WO2008024284A3
公开(公告)日：2008-11-20
申请号：PCT/US2007018287
申请日：2007-08-17
申请人： MERCK & CO INC , FLETCHER JOAN M , FONG TUNG M , HAGMANN WILLIAM K , VACHAL PETR
发明人： FLETCHER JOAN M , FONG TUNG M , HAGMANN WILLIAM K , VACHAL PETR
IPC分类号： A61K31/4965 , A61K31/497
CPC分类号： A61K31/496
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，并且可用于治疗，预防和抑制由CB1受体介导的疾病。本发明化合物可用作治疗精神病，记忆缺陷，认知障碍，阿尔茨海默氏病，偏头痛，神经病，包括多发性硬化症和格林 - 巴利综合征的神经炎症和病毒性脑炎的炎症性后遗症的中枢作用药物，脑血管意外，头部外伤，焦虑症，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物还可用于治疗药物滥用障碍，肥胖或饮食失调的治疗，以及治疗哮喘，便秘，慢性肠假性梗阻，肝硬化，非酒精性脂肪肝疾病（NAFLD）），非酒精性脂肪性肝炎（NASH）和促进觉醒。

5. 发明申请

WO2004058145A3 SUBSTITUTED AMIDES 审中-公开
标题翻译：取代的酰胺
公开(公告)号：WO2004058145A3
公开(公告)日：2004-09-02
申请号：PCT/US0340040
申请日：2003-12-15
申请人： MERCK & CO INC , LIN LINUS S , HAGMANN WILLIAM K , KUMAR SANJEEV , YIN WENJI , DOSS GEORGE
发明人： LIN LINUS S , HAGMANN WILLIAM K , KUMAR SANJEEV , YIN WENJI , DOSS GEORGE
IPC分类号： C07C255/60 , C07C275/24 , C07D213/64 , C07C233/05 , A61K31/44 , C07D213/02
CPC分类号： C07D213/64 , C07C255/60 , C07C275/24 , C07C2601/04
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，并且可用于治疗，预防和抑制由CB1受体介导的疾病。本发明化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化症和格林 - 巴利综合征的神经炎症和病毒性脑炎的炎性后遗症，脑血管障碍事故和头部创伤，焦虑症，压力，癫痫，帕金森病，运动障碍和精神分裂症。该化合物还可用于治疗物质滥用障碍，肥胖或饮食失调的治疗，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

6. 发明申请

WO2005027837A3 SUBSTITUTED SULFONAMIDES 审中-公开
标题翻译：取代的磺酰胺
公开(公告)号：WO2005027837A3
公开(公告)日：2006-10-05
申请号：PCT/US2004030122
申请日：2004-09-14
申请人： MERCK & CO INC , ARMSTRONG HELEN M , CHANG LINDA L , GUTHIKONDA RAVINDRA N , HAGMANN WILLIAM K , LIN LINUS S , SHAH SHRENIK K
发明人： ARMSTRONG HELEN M , CHANG LINDA L , GUTHIKONDA RAVINDRA N , HAGMANN WILLIAM K , LIN LINUS S , SHAH SHRENIK K
IPC分类号： C07C311/10 , A61K20060101 , A61K31/18 , C07C311/03 , C07C311/06 , C07C311/13 , C07C311/16 , C07C311/17 , C07C311/19 , C07C311/29 , C07D209/08
CPC分类号： C07C311/06 , A61K31/18 , A61K31/277 , A61K31/44 , C07C311/03 , C07C311/13 , C07C311/16 , C07C311/17 , C07C311/19 , C07C311/29 , C07D209/08
摘要： The substituted sulfonamides of the invention are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译：本发明的取代磺酰胺是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管事故和头部创伤，焦虑症，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

7. 发明申请

WO0114328A3 SUBSTITUTED UREAS AS CELL ADHESION INHIBITORS 审中-公开
标题翻译：作为细胞粘附抑制剂的替代性URAAS
公开(公告)号：WO0114328A3
公开(公告)日：2002-01-31
申请号：PCT/US0022437
申请日：2000-08-16
申请人： MERCK & CO INC , DELASZLO STEPHEN E , HAGMANN WILLIAM K , KAMENECKA THEODORE M
发明人： DELASZLO STEPHEN E , HAGMANN WILLIAM K , KAMENECKA THEODORE M
IPC分类号： C07C275/24 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/42 , C07D207/08 , C07D207/09 , C07D207/16 , C07D209/02 , C07D211/16 , C07D211/32 , C07D211/34 , C07D211/58 , C07D211/60 , C07D211/64 , C07D215/08 , C07D215/18 , C07D217/06 , C07D221/20 , C07D223/16 , C07D295/215 , C07D307/14 , C07D307/68 , C07D317/58 , C07D471/10 , C07C205/00 , C07C229/00 , C07C241/00 , C07C243/00
CPC分类号： C07D207/08 , A61K9/0019 , A61K9/008 , A61K9/2054 , A61K9/4858 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/42 , C07C2601/14 , C07D207/09 , C07D207/16 , C07D209/02 , C07D211/16 , C07D211/32 , C07D211/34 , C07D211/58 , C07D211/60 , C07D211/64 , C07D215/08 , C07D215/18 , C07D217/06 , C07D221/20 , C07D223/16 , C07D295/215 , C07D307/14 , C07D307/68 , C07D317/58 , C07D471/10
摘要： Compounds of Formula (I) are antagonists of VLA-4 and/or alpha 4 beta 7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
摘要翻译：式（I）化合物是VLA-4和/或α4β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理。这些化合物可以配制成药物组合物，适用于治疗AIDS相关的痴呆，过敏性结膜炎，过敏性鼻炎，阿尔茨海默病，哮喘，动脉粥样硬化，自体骨髓移植，某些类型的毒性和免疫性肾炎，接触皮肤过敏，包括溃疡性结肠炎和克罗恩病的炎性肠病，炎症性肺病，病毒感染的炎症后遗症，脑膜炎，多发性硬化，多发性骨髓瘤，心肌炎，器官移植，牛皮癣，肺纤维化，再狭窄，视网膜炎，类风湿性关节炎，败血症关节炎，中风，肿瘤转移，葡萄膜炎和I型糖尿病。

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