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公开(公告)号：US07718682B2
公开(公告)日：2010-05-18
申请号：US12078662
申请日：2008-04-02
IPC分类号： A61K31/426
CPC分类号： C07D277/20 , C07D277/24 , C07D277/34
摘要： Novel diphenylethylene compounds and derivatives thereof containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.
摘要翻译： 提供了含有噻唑烷二酮或恶唑烷二酮部分的新型二苯基乙烯化合物及其衍生物，其有效降低II型糖尿病动物模型中的血糖水平，血清胰岛素，甘油三酯和游离脂肪酸水平。 所述化合物被公开用于各种治疗，包括治疗炎症，炎症和免疫疾病，胰岛素抵抗，高脂血症，冠状动脉疾病，癌症和多发性硬化。
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公开(公告)号：US20080293949A1
公开(公告)日：2008-11-27
申请号：US12078662
申请日：2008-04-02
IPC分类号： C07D277/14
CPC分类号： C07D277/20 , C07D277/24 , C07D277/34
摘要： Novel diphenylethylene compounds and derivatives thereof containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.
摘要翻译： 提供了含有噻唑烷二酮或恶唑烷二酮部分的新型二苯基乙烯化合物及其衍生物，其有效降低II型糖尿病动物模型中的血糖水平，血清胰岛素，甘油三酯和游离脂肪酸水平。 所述化合物被公开用于各种治疗，包括治疗炎症，炎症和免疫疾病，胰岛素抵抗，高脂血症，冠状动脉疾病，癌症和多发性硬化。
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公开(公告)号：US07202366B2
公开(公告)日：2007-04-10
申请号：US10808519
申请日：2004-03-25
IPC分类号： A61K31/41 , C07D277/60
CPC分类号： C07D277/20 , C07D277/24 , C07D277/34
摘要： Novel diphenylethylene compounds and derivatives thereof containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. In contrast to previously reported thiazolidinedione compounds, known to lower leptin levels, the present compounds increase leptin levels and have no known liver toxicity. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.
摘要翻译： 提供了含有噻唑烷二酮或恶唑烷二酮部分的新型二苯基乙烯化合物及其衍生物，其有效降低II型糖尿病动物模型中的血糖水平，血清胰岛素，甘油三酯和游离脂肪酸水平。 与之前报道的已知降低瘦蛋白水平的噻唑烷二酮化合物相比，本发明化合物增加瘦素水平并且没有已知的肝脏毒性。 所述化合物被公开用于各种治疗，包括治疗炎症，炎症和免疫疾病，胰岛素抵抗，高脂血症，冠状动脉疾病，癌症和多发性硬化。
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公开(公告)号：US07105552B2
公开(公告)日：2006-09-12
申请号：US09843167
申请日：2001-04-27
IPC分类号： A61K31/41
CPC分类号： C07D277/20 , C07D277/24 , C07D277/34
摘要： Novel diphenylethylene compounds and derivatives thereof containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. In contrast to previously reported thiazolidinedione compounds, known to lower leptin levels, the present compounds increase leptin levels and have no known liver toxicity. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.
摘要翻译： 提供了含有噻唑烷二酮或恶唑烷二酮部分的新型二苯基乙烯化合物及其衍生物，其有效降低II型糖尿病动物模型中的血糖水平，血清胰岛素，甘油三酯和游离脂肪酸水平。 与之前报道的已知降低瘦蛋白水平的噻唑烷二酮化合物相比，本发明化合物增加瘦素水平并且没有已知的肝脏毒性。 所述化合物被公开用于各种治疗，包括治疗炎症，炎症和免疫疾病，胰岛素抵抗，高脂血症，冠状动脉疾病，癌症和多发性硬化。
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公开(公告)号：US06525093B1
公开(公告)日：2003-02-25
申请号：US09436047
申请日：1999-11-08
申请人： Partha Neogi , Bishwajit Nag , Frederick J. Lakner , Debendranath Dey , Satyanarayana Medicherla
发明人： Partha Neogi , Bishwajit Nag , Frederick J. Lakner , Debendranath Dey , Satyanarayana Medicherla
IPC分类号： A01N3710
CPC分类号： C07C69/736
摘要： Compounds are provided that lower blood glucose concentrations, lower serum triglyceride concentrations, lower systolic blood pressure, and increase glucose uptake by adipose tissue, but do not affect the expression of PPAR-&ggr; by adipose tissue.
摘要翻译： 提供化合物，其降低血糖浓度，降低血清甘油三酯浓度，降低收缩压，并增加脂肪组织的葡萄糖摄取，但不影响脂肪组织中PPAR-γ的表达。
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公开(公告)号：US06331633B1
公开(公告)日：2001-12-18
申请号：US09287237
申请日：1999-04-06
IPC分类号： H61K31425
CPC分类号： C07D277/34
摘要： Novel diphenylethylene compounds containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. In contrast to previously reported thiazolidine compounds, known to lower leptin levels, the present compound increase leptin levels and have no known liver toxicity.
摘要翻译： 提供了含有噻唑烷二酮或恶唑烷二酮部分的新型二苯基乙烯化合物，其有效降低II型糖尿病动物模型中的血糖水平，血清胰岛素，甘油三酯和游离脂肪酸水平。 与以前报道的已知降低瘦蛋白水平的噻唑烷化合物相比，本发明化合物增加瘦素水平并且没有已知的肝毒性。
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公开(公告)号：US07407978B2
公开(公告)日：2008-08-05
申请号：US10265902
申请日：2002-10-08
IPC分类号： A61K31/425
CPC分类号： C07D277/20 , C07D277/24 , C07D277/34
摘要： Novel diphenylethylene compounds and derivatives thereof containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.
摘要翻译： 提供了含有噻唑烷二酮或恶唑烷二酮部分的新型二苯基乙烯化合物及其衍生物，其有效降低II型糖尿病动物模型中的血糖水平，血清胰岛素，甘油三酯和游离脂肪酸水平。 所述化合物被公开用于各种治疗，包括治疗炎症，炎症和免疫疾病，胰岛素抵抗，高脂血症，冠状动脉疾病，癌症和多发性硬化。
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公开(公告)号：US06245814B1
公开(公告)日：2001-06-12
申请号：US09074925
申请日：1998-05-08
IPC分类号： A61K3119
CPC分类号： C07D277/34
摘要： Novel diphenylethylene and styrenes are provided which are administered orally to decrease blood glucose levels in rats. The glucose tolerance in insulin resistant rats is also shown, as well as lowering of triglyceride levels in serum insulin resistant, hyperinsulinemic and hypertriglycedemic rats. The compounds are orally effective anti-diabetic agents that potentially may reduce abnormality of glucose and lipid metabolism in diabetes.
摘要翻译： 提供新的二苯乙烯和苯乙烯，其口服给药以降低大鼠的血糖水平。 还显示胰岛素抵抗大鼠的葡萄糖耐量，以及降低血清胰岛素抵抗，高胰岛素血症和高胰岛素血症大鼠的甘油三酯水平。 这些化合物是口服有效的抗糖尿病药物，其可能降低糖尿病中葡萄糖和脂质代谢的异常。
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公开(公告)号：US06624197B1
公开(公告)日：2003-09-23
申请号：US09642618
申请日：2000-08-17
IPC分类号： A61K3119
CPC分类号： C07D277/34
摘要： Novel diphenylethylene and styrenes are provided which are administered orally to decrease blood glucose levels in rats. The glucose tolerance in insulin resistant rats is also shown, as well as lowering of triglyceride levels in serum insulin resistant, hyperinsulinemic and hypertriglycedemic rats. The compounds are orally effective anti-diabetic agents that potentially may reduce abnormality of glucose and lipid metabolism in diabetes.
摘要翻译： 提供新的二苯乙烯和苯乙烯，其口服给药以降低大鼠的血糖水平。 还显示胰岛素抵抗大鼠的葡萄糖耐量，以及降低血清胰岛素抵抗，高胰岛素血症和高胰岛素血症大鼠的甘油三酯水平。 这些化合物是口服有效的抗糖尿病药物，其可能降低糖尿病中葡萄糖和脂质代谢的异常。
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公开(公告)号：US20090069313A1
公开(公告)日：2009-03-12
申请号：US11896902
申请日：2007-09-06
IPC分类号： A61K31/5377 , C07D277/16 , A61K31/426 , C07D209/34 , A61P25/24 , A61P25/32 , A61P25/08 , A61P25/00 , A61P25/34 , A61P25/28 , A61K31/404 , C07D413/12 , A61K31/422
CPC分类号： C07D277/36 , C07D209/34 , C07D277/34 , C07D413/12 , C07D417/12
摘要： The present invention provides a new medical use for the compounds of the formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof, as MAO-A inhibitors. Also included is a method for prophylaxis and treatment of mental disorders such as depression, in a mammal, comprising administering an effective amount of a compound of formula (I). These compounds are also effective in treating a disease, condition or disorder such as weight loss, obesity, bulimia, depression, bipolar disorders, psychoses, schizophrenia, behaviors, alcoholism, tobacco abuse, memory loss, Alzheimer's disease, dementia of aging, seizure disorders, epilepsy, attention deficit disorder, and Parkinson's disease, which is modulated by a cannabinoid receptor antagonist.
摘要翻译： 本发明提供了作为MAO-A抑制剂的式（I）化合物，其衍生物，类似物，互变异构形式，立体异构体，多晶型物，水合物，溶剂合物，药学上可接受的盐和组合物，其代谢物和前药的新医学用途 。 还包括在哺乳动物中预防和治疗精神障碍如抑郁症的方法，包括施用有效量的式（I）化合物。 这些化合物在治疗疾病，病症或病症如体重减轻，肥胖，贪食症，抑郁症，双相性精神障碍，精神病，精神分裂症，行为，酒精中毒，吸烟，记忆丧失，阿尔茨海默病，老年痴呆，癫痫发作障碍 ，癫痫，注意力缺陷障碍和由大麻素受体拮抗剂调节的帕金森病。
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