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1. 发明申请

WO2008106077A1 SUBSTITUTED BENZODIAZEPINONES, BENZOXAZEPINONES AND BENZOTHIAZEPINONES AS SODIUM CHANNEL BLOCKERS 审中-公开
标题翻译：作为钠通道阻断剂的取代苯并恶嗪酮，苯并恶唑酮和苯并噻唑酮
公开(公告)号：WO2008106077A1
公开(公告)日：2008-09-04
申请号：PCT/US2008/002441
申请日：2008-02-25
申请人： MERCK & CO., INC. , HOYT, Scott, B. , OK, Dong , OK, Hyun, O. , LONDON, Clare , DUFFY, Joseph, L.
发明人： HOYT, Scott, B. , OK, Dong , OK, Hyun, O. , LONDON, Clare , DUFFY, Joseph, L.
IPC分类号： A01N43/62 , A61K31/55
CPC分类号： C07D281/10 , C07D245/06 , C07D267/14
摘要： The present invention is directed to substituted benzodiazepinones, benzoxazepinones and benzothiazepinones compounds that are sodium channel blockers useful for the treatment of chronic and neuropathic pain. The compounds of the present invention are also useful for the treatment of other conditions, including disorders of the CNS such as anxiety, depression, epilepsy, manic depression and bipolar disorder. This invention also provides pharmaceutical compositions comprising a compound of the present invention, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. This invention further comprises methods for the treatment of acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain and disorders of the CNS including, but not limited to, epilepsy, manic depression, depression, anxiety and bipolar disorder comprising administering the compounds and pharmaceutical compositions of the present invention.
摘要翻译：本发明涉及用作治疗慢性和神经性疼痛的钠通道阻滞剂的取代苯并二氮杂酮，苯并氧氮杂酮和苯并噻唑酮化合物。本发明的化合物还可用于治疗其他病症，包括CNS的疾病如焦虑症，抑郁症，癫痫症，躁狂抑郁症和双相性精神障碍。本发明还提供包含单独的或与一种或多种治疗活性化合物组合的本发明化合物和药学上可接受的载体的药物组合物。本发明还包括用于治疗急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛和中枢神经系统疾病的方法，包括但不限于癫痫症，躁狂抑郁症，抑郁症，焦虑和双相情感障碍，包括给予化合物和本发明的药物组合物。

2. 发明申请

WO03101381A2 1,2 DIAMIDO CYCLOALKYL SODIUM CHANNEL BLOCKERS 审中-公开
公开(公告)号：WO03101381A2
公开(公告)日：2003-12-11
申请号：PCT/US0316335
申请日：2003-05-23
申请人： MERCK & CO INC , FISHER MICHAEL H , LI CHUNSHI , LIANG JUN , MEINKE PETER T , OK DONG , PARSONS WILLIAM H , SHAO PENGCHENG PATRICK , TYAGARAJAN SRIRAM
发明人： FISHER MICHAEL H , LI CHUNSHI , LIANG JUN , MEINKE PETER T , OK DONG , PARSONS WILLIAM H , SHAO PENGCHENG PATRICK , TYAGARAJAN SRIRAM
IPC分类号： C07C233/59 , C07C233/60 , C07C311/08 , C07C311/46 , C07C317/32 , C07D211/16 , C07D213/40 , C07D239/26 , C07D333/54 , A61K
CPC分类号： C07D213/40 , C07C233/59 , C07C233/60 , C07C311/08 , C07C311/46 , C07C317/32 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/50 , C07D211/16 , C07D239/26 , C07D333/54
摘要： 1,2 Diamido cycloalkyl compounds that are sodium channel blockers; pharmaceutical compositions that include an effective amount of the aryl-link-aryl thiazolidin-dione and aryl-link-aryl oxazolodine-dione compounds and a pharmaceutically acceptable carrier; and a method of treatment of acute pain, chronic pain, visceral pain, inflammatory pain, or neuropathic pain, as well as irritable bowel syndrome, Crohns disease, epilepsy, partial and generalized tonic seizures, multiple sclerosis, bipolar disease, and tachy-arrhythmias by the administration of an effective amount of aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolodine-dione compounds, either alone, or in combination with one or more therapeutically active compounds, are described.
摘要翻译： 1,2二氨基环烷基化合物，其为钠通道阻断剂; 药物组合物，其包含有效量的芳基 - 链烷基 - 噻唑烷二酮和芳基 - 链烷基 - 恶唑并噻吩二酮化合物和药学上可接受的载体; 以及治疗急性疼痛，慢性疼痛，内脏痛，炎性疼痛或神经性疼痛以及肠易激综合征，克罗恩病，癫痫，部分和全身性强直性癫痫发作，多发性硬化症，双相性精神障碍和快速性心律失常的方法通过单独或与一种或多种治疗活性化合物组合施用有效量的芳基 - 链接 - 芳基噻唑烷二酮和芳基链 - 芳基恶唑啉二酮化合物。

3. 发明申请

WO1995029159A1 SUBSTITUTED SULFONAMIDES AS SELECTIVE 'beta'3 AGONISTS FOR THE TREATMENT OF DIABETES AND OBESITY 审中-公开
标题翻译：替代的磺酰胺作为治疗糖尿病和肥胖的选择性β3激动剂
公开(公告)号：WO1995029159A1
公开(公告)日：1995-11-02
申请号：PCT/US1995004956
申请日：1995-04-21
申请人： MERCK & CO., INC. , FISHER, Michael, H. , NAYLOR, Elisabeth, M. , OK, Dong , WEBER, Ann, E. , SHIH, Thomas , OK, Hyun
发明人： MERCK & CO., INC.
IPC分类号： C07D213/30
CPC分类号： C07D213/73 , C07C311/21 , C07C311/47 , C07D209/08 , C07D213/38 , C07D215/36 , C07D233/32 , C07D271/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Substituted sulfonamides having formula (I), are selective beta 3 adrenergic receptor agonists with very little beta 1 and beta 2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduce neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.
摘要翻译：具有式（I）的取代的磺酰胺是具有非常少的β1和β2肾上腺素能受体活性的选择性β3肾上腺素能受体激动剂，因此化合物能够增加细胞中的脂肪分解和能量消耗。因此，这些化合物在治疗II型糖尿病和肥胖中具有有效的活性。该化合物也可用于降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠道运动性。此外，该化合物可用于减少神经源性炎症或作为抗抑郁剂。通过将氨基烷基苯基磺酰胺与适当取代的环氧化物偶合来制备化合物。还公开了用于治疗糖尿病和肥胖以及降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或增加肠蠕动的组合物和方法。

4. 发明申请

WO2003101381A3 1,2 DIAMIDO CYCLOALKYL SODIUM CHANNEL BLOCKERS 审中-公开
公开(公告)号：WO2003101381A3
公开(公告)日：2003-12-11
申请号：PCT/US2003/016335
申请日：2003-05-23
申请人： MERCK & CO., INC. , FISHER, Michael, H. , LI, Chunshi , LIANG, Jun , MEINKE, Peter, T. , OK, Dong , PARSONS, William, H. , SHAO, Pengcheng Patrick , TYAGARAJAN, Sriram
发明人： FISHER, Michael, H. , LI, Chunshi , LIANG, Jun , MEINKE, Peter, T. , OK, Dong , PARSONS, William, H. , SHAO, Pengcheng Patrick , TYAGARAJAN, Sriram
IPC分类号： A61K31/47
摘要： 1,2 Diamido cycloalkyl compounds that are sodium channel blockers; pharmaceutical compositions that include an effective amount of the aryl-link-aryl thiazolidin-dione and aryl-link-aryl oxazolodine-dione compounds and a pharmaceutically acceptable carrier; and a method of treatment of acute pain, chronic pain, visceral pain, inflammatory pain, or neuropathic pain, as well as irritable bowel syndrome, Crohns disease, epilepsy, partial and generalized tonic seizures, multiple sclerosis, bipolar disease, and tachy-arrhythmias by the administration of an effective amount of aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolodine-dione compounds, either alone, or in combination with one or more therapeutically active compounds, are described.

5. 发明申请

WO2007145922A3 BENZAZEPINONES AS SODIUM CHANNEL BLOCKERS 审中-公开
标题翻译：苯并噻吩作为钠通道阻断剂
公开(公告)号：WO2007145922A3
公开(公告)日：2008-08-21
申请号：PCT/US2007013202
申请日：2007-06-05
申请人： MERCK & CO INC , HOYT SCOTT B , LONDON CLARE , OK DONG , PARSONS WILLIAM H
发明人： HOYT SCOTT B , LONDON CLARE , OK DONG , PARSONS WILLIAM H
IPC分类号： C07D223/16 , A61K31/55 , A61P29/00 , A61P29/02
CPC分类号： C07D223/16 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12
摘要： Benzazepinone compounds represented by Formula (I), or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, urinary incontinence, pruritis, itchiness, allergic dermatitis, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.
摘要翻译：由式（I）表示的苯并氮杂酮化合物或其药学上可接受的盐。药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。治疗与钠通道活性相关或由其引起的症状的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，癫痫，肠易激综合征，尿失禁，瘙痒，瘙痒，过敏性皮炎抑郁，焦虑，多发性硬化和双相性精神障碍，包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。施用局部麻醉的方法包括单独或与一种或多种其它治疗活性化合物和药学上可接受的载体一起施用有效量的本发明化合物。

6. 发明申请

WO2007145922A2 BENZAZEPINONES AS SODIUM CHANNEL BLOCKERS 审中-公开
标题翻译：苯并噻吩作为钠通道阻断剂
公开(公告)号：WO2007145922A2
公开(公告)日：2007-12-21
申请号：PCT/US2007/013202
申请日：2007-06-05
申请人： MERCK & CO., INC. , HOYT, Scott, B. , LONDON, Clare , OK, Dong , PARSONS, William, H.
发明人： HOYT, Scott, B. , LONDON, Clare , OK, Dong , PARSONS, William, H.
IPC分类号： A61K31/55
CPC分类号： C07D223/16 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12
摘要： Benzazepinone compounds represented by Formula (I), or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, urinary incontinence, pruritis, itchiness, allergic dermatitis, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.
摘要翻译：由式（I）表示的苯并氮杂酮化合物或其药学上可接受的盐。药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。治疗与钠通道活性相关或由其引起的症状的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，癫痫，肠易激综合征，尿失禁，瘙痒，瘙痒，过敏性皮炎抑郁，焦虑，多发性硬化和双相性精神障碍，包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。施用局部麻醉的方法包括单独或与一种或多种其它治疗活性化合物和药学上可接受的载体一起施用有效量的本发明化合物。

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