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1. 发明专利

CA2573378A1 AMIDE DERIVATIVES AS INHIBITORS OF HISTONE DEACETYLASE 未知
公开(公告)号：CA2573378A1
公开(公告)日：2006-01-19
申请号：CA2573378
申请日：2005-07-11
申请人： ANGELETTI P IST RICHERCHE BIO , MERCK & CO INC
发明人： JONES PHILIP , STEINKUHLER CHRISTIAN , SCARPELLI RITA , INGENITO RAFFAELE , CHAKRAVARTY PRASUN K , COLLETTI STEVEN L , MEINKE PETER T , ROWLEY MICHAEL , MURAGLIA ESTER , PETROCCHI ALESSIA
IPC分类号： C07C237/22 , A61K31/16 , C07D241/02
摘要： The present invention relates to ketone derivatives that are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.

2. 发明专利

CA2573380A1 AMIDE DERIVATIVES AS INHIBITORS OF HISTONE DEACETYLASE 未知
公开(公告)号：CA2573380A1
公开(公告)日：2006-01-19
申请号：CA2573380
申请日：2005-07-11
申请人： MERCK & CO INC , ANGELETTI P IST RICHERCHE BIO
发明人： CHAKRAVARTY PRASUN K , COLLETTI STEVEN L , INGENITO RAFFAELE , JONES PHILIP , PETROCCHI ALESSIA , MEINKE PETER T , STEINKUHLER CHRISTIAN
IPC分类号： C07D209/18 , A61K31/405 , A61P35/00 , C07D401/12 , C07D409/12
摘要： The present invention relates to carboxylic acid derivatives that are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.

3. 发明申请

WO2004084824A3 BIARYL SUBSTITUTED 6-MEMBERED HETEROCYLES AS SODIUM CHANNEL BLOCKERS 审中-公开
标题翻译： BIARYL取代的6位杂交体作为钠通道阻断剂
公开(公告)号：WO2004084824A3
公开(公告)日：2005-03-31
申请号：PCT/US2004008532
申请日：2004-03-19
申请人： MERCK & CO INC , CHAKRAVARTY PRASUN K , FISHER MICHAEL H , PARSONS WILLIAM H , LIANG JUN , ZHOU BISHAN
发明人： CHAKRAVARTY PRASUN K , FISHER MICHAEL H , PARSONS WILLIAM H , LIANG JUN , ZHOU BISHAN
IPC分类号： A61K20060101 , A61K31/4418 , A61K31/4436 , A61K31/505 , A61K31/506 , C07D213/26 , C07D213/55 , C07D213/56 , C07D239/26 , C07D401/04 , C07D403/04
CPC分类号： C07D213/26 , C07D213/55 , C07D213/56 , C07D239/26 , C07D401/04 , C07D403/04
摘要： Biaryl substituted pyridine, pyrimidine and pyrazine compounds are sodium channel blockers useful for the treatment of pain. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more 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, 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.
摘要翻译：双芳基取代的吡啶，嘧啶和吡嗪化合物是可用于治疗疼痛的钠通道阻滞剂。药物组合物包含单独的或与一种或多种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病症的方法，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，抑郁症，焦虑症，多发性硬化症和双相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。

4. 发明申请

WO2007084394A3 2,5 DIAZA-BICYCLO[2.2.1]HEPTANE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS 审中-公开
标题翻译： 2,5 DIAZA-BICYCLO [2.2.1] HEPTANE衍生物作为钙通道阻断剂
公开(公告)号：WO2007084394A3
公开(公告)日：2008-01-24
申请号：PCT/US2007000883
申请日：2007-01-12
申请人： MERCK & CO INC , CHAKRAVARTY PRASUN K
发明人： CHAKRAVARTY PRASUN K
IPC分类号： A61K31/497 , A61K31/43 , A61K31/58
CPC分类号： C07D487/08
摘要： 2,5-diaza-bicyclo[2.2.1]heptane derivatives 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, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
摘要翻译：由式（I）表示的2,5-二氮杂双环[2.2.1]庚烷衍生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疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，尿失禁，瘙痒，过敏性皮炎，癫痫，肠易激综合征，抑郁症，焦虑，多发性硬化，双相性精神障碍和中风，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。

5. 发明申请

WO2004024061A3 ARYL-LINK-ARYL SUBSTITUTED THIAZOLIDINE-DIONE AND OXAZOLIDINE-DIONE AS SODIUM CHANNEL BLOCKERS 审中-公开
标题翻译：作为钠通道阻断剂的ARYL-LINK-ARYL取代噻唑烷二酮和氧杂环丁酮
公开(公告)号：WO2004024061A3
公开(公告)日：2004-06-10
申请号：PCT/US0312910
申请日：2003-04-25
申请人： MERCK & CO INC , KUO HOWARD C H , AYER MICHELLE B , CHAKRAVARTY PRASUN K , MEINKE PETER T , PARSONS WILLIAM H , TYAGARAJAN SRIRAM
发明人： KUO HOWARD C H , AYER MICHELLE B , CHAKRAVARTY PRASUN K , MEINKE PETER T , PARSONS WILLIAM H , TYAGARAJAN SRIRAM
IPC分类号： A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , C07D263/44 , C07D277/20 , C07D277/34 , C07D417/06 , C07D417/10 , C07D417/12 , C07D417/14 , A61K31/44 , A61K31/42 , A61K31/425 , C07D263/04 , C07D277/04 , C07D401/00
CPC分类号： A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , C07D263/44 , C07D277/20 , C07D277/34 , C07D417/06 , C07D417/10 , C07D417/12 , C07D417/14
摘要： Aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-dione compounds are sodium channel blockers; pharmaceutical compositions that include an effective amount of the aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-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 depression, and tachy-arrhythmias by the administration of an effective amount of aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-dione compounds are described.
摘要翻译：芳基 - 链接 - 芳基噻唑烷二酮和芳基 - 芳基恶唑烷二酮化合物是钠通道阻断剂; 包括有效量的芳基 - 链烷基 - 噻唑烷二酮和芳基 - 芳基恶唑烷二酮化合物和药学上可接受的载体的药物组合物; 以及治疗急性疼痛，慢性疼痛，内脏痛，炎症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，双相抑郁和快速性心律失常的方法通过施用有效量的芳基链接 - 芳基噻唑烷二酮和芳基 - 链烯基 - 恶唑烷二酮化合物。

6. 发明申请

WO2006017214A3 INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译： HISTONE DEACETYLASE的抑制剂
公开(公告)号：WO2006017214A3
公开(公告)日：2006-06-01
申请号：PCT/US2005024512
申请日：2005-07-08
申请人： MERCK & CO INC , CHAKRAVARTY PRASUN K , KUO HOWARD , MATTHEWS JAY M , MEINKE PETER T
发明人： CHAKRAVARTY PRASUN K , KUO HOWARD , MATTHEWS JAY M , MEINKE PETER T
IPC分类号： C07C259/10 , A61K31/16 , C07C311/21 , C07D271/12
CPC分类号： C07C259/10 , C07C307/10 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/44 , C07C2602/08 , C07C2602/42 , C07C2603/24 , C07D215/36 , C07D215/38 , C07D235/28 , C07D261/10 , C07D263/56 , C07D277/46 , C07D277/74 , C07D295/108 , C07D333/38 , C07D409/04 , C07D413/04
摘要： The present invention relates to hydroxamic acid derivatives that are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases. Further, the compounds of the present invention have antiprotozoal properties.
摘要翻译：本发明涉及作为组蛋白脱乙酰酶（HDAC）抑制剂的异羟肟酸衍生物。本发明的化合物可用于治疗细胞增殖性疾病，包括癌症。此外，本发明化合物可用于治疗神经退行性疾病，精神分裂症和其他疾病中的中风。此外，本发明的化合物具有抗原虫特性。

7. 发明申请

WO2005047270A2 SUBSTITUTED TRIAZOLES AS SODIUM CHANNEL BLOCKERS 审中-公开
标题翻译：取代三唑作为钠通道阻断剂
公开(公告)号：WO2005047270A2
公开(公告)日：2005-05-26
申请号：PCT/US2004037280
申请日：2004-11-05
申请人： MERCK & CO INC , PARK MIN K , CHAKRAVARTY PRASUN K , ZHOU BISHAN , GONZALEZ EDWARD , OK HYUN , PALUCKI BRENDA , PARSONS WILLIAM H , SISCO ROSEMARY , FISHER MICHAEL H
发明人： PARK MIN K , CHAKRAVARTY PRASUN K , ZHOU BISHAN , GONZALEZ EDWARD , OK HYUN , PALUCKI BRENDA , PARSONS WILLIAM H , SISCO ROSEMARY , FISHER MICHAEL H
IPC分类号： C07D249/10 , C07D403/10 , A61K31/4196 , A61P25/00
CPC分类号： C07D249/10 , C07D403/10
摘要： Substituted triazole compounds represented by Formula I, II or III, 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, migraine, headache pain, migraine headache, epilepsy, irritable bowel syndrome, diabetic neuropathy, multiple sclerosis, manic depression 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，II或III表示的取代的三唑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疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，偏头痛，头痛，偏头痛，癫痫，肠易激综合征，糖尿病神经病，多发性硬化症，躁狂抑郁症和双相性精神障碍，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。

8. 发明申请

WO2008066803A3 SUBSTITUTED PIPERIZINES FOR THE TREATMENT OF PAIN 审中-公开
标题翻译：用于治疗疼痛的替代管
公开(公告)号：WO2008066803A3
公开(公告)日：2009-05-22
申请号：PCT/US2007024430
申请日：2007-11-26
申请人： MERCK & CO INC , ABBADIE CATHERINE , CHAKRAVARTY PRASUN K , DUFFY JOSEPH L
发明人： ABBADIE CATHERINE , CHAKRAVARTY PRASUN K , DUFFY JOSEPH L
IPC分类号： A61K31/495 , A61P29/00
CPC分类号： A61K31/495
摘要： The present invention is directed to the use of substituted piperizine compounds represented by Formula (I), for the treatment of pain, including acute pain, chronic pain, cancer pain, visceral pain, inflammatory pain, neuropathic pain, post-herpetic neuralgia, diabetic neuropathy, trigeminal neuralgia, migraine, and fibromyalgia.
摘要翻译：本发明涉及式（I）表示的取代哌嗪化合物在治疗疼痛方面的应用，包括急性疼痛，慢性疼痛，癌症疼痛，内脏痛，炎性疼痛，神经性疼痛，疱疹后神经痛，糖尿病神经病，三叉神经痛，偏头痛和纤维肌痛。

9. 发明申请

WO2007075524A2 SUBSTITUTED PIPERIDINES AS CALCIUM CHANNEL BLOCKERS 审中-公开
标题翻译：取代的管道作为钙通道阻塞剂
公开(公告)号：WO2007075524A2
公开(公告)日：2007-07-05
申请号：PCT/US2006048162
申请日：2006-12-18
申请人： MERCK & CO INC , CHAKRAVARTY PRASUN K , SHAO PENGCHENG PATRICK , YE FENG
发明人： CHAKRAVARTY PRASUN K , SHAO PENGCHENG PATRICK , YE FENG
IPC分类号： A61K31/445
CPC分类号： C07D211/58 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/04 , C07D413/06 , C07D413/10 , C07D471/04 , C07D513/04
摘要： Substituted piperidine 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, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, 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.
摘要翻译：由式I表示的取代的哌啶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和药学上可接受的载体组合的有效量的本发明化合物。治疗与钠通道活性相关或由其引起的病症的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，尿失禁，瘙痒，过敏性皮炎，癫痫，肠易激综合征，抑郁症，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。

10. 发明申请

WO2004094395A2 BIARYL SUBSTITUTED THIAZOLES, OXAZOLES AND IMIDAZOLES AS SODIUM CHANNEL BLOCKERS 审中-公开
标题翻译： BIARYL取代的THIAZOLES，OXAZOLES和IMIDAZOLES作为钠通道阻断剂
公开(公告)号：WO2004094395A2
公开(公告)日：2004-11-04
申请号：PCT/US2004011271
申请日：2004-04-14
申请人： MERCK & CO INC , CHAKRAVARTY PRASUN K , FISHER MICHAEL H , PARSONS WILLIAM H , TYAGARAJAN SRIRAM , ZHOU BISHAN
发明人： CHAKRAVARTY PRASUN K , FISHER MICHAEL H , PARSONS WILLIAM H , TYAGARAJAN SRIRAM , ZHOU BISHAN
IPC分类号： C07D233/54 , C07D233/68 , C07D233/90 , C07D263/32 , C07D263/34 , C07D263/48 , C07D277/22 , C07D277/24 , C07D277/30 , C07D277/40 , C07D277/42 , C07D277/46 , C07D277/48 , C07D277/52 , C07D277/56 , C07D403/04 , C07D417/04 , C07D417/12 , C07D417/14
CPC分类号： C07D233/64 , C07D233/68 , C07D233/90 , C07D233/96 , C07D263/32 , C07D263/34 , C07D263/48 , C07D277/22 , C07D277/24 , C07D277/30 , C07D277/40 , C07D277/46 , C07D277/48 , C07D277/52 , C07D277/56 , C07D403/04 , C07D417/04 , C07D417/12 , C07D417/14
摘要： Biaryl substituted thiazole, oxazole and imidazole compounds are sodium channel blockers useful for the treatment of pain. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treatment or prevention of conditions, including acute pain, chronic pain, visceral pain, inflammatory pain, and neuropathic pain comprise administering an effective amount of the present compounds, either alone, or in combination with one or more therapeutically active compounds.
摘要翻译：双芳基取代的噻唑，恶唑和咪唑化合物是可用于治疗疼痛的钠通道阻滞剂。药物组合物包含单独的或与一种或多种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。治疗或预防包括急性疼痛，慢性疼痛，内脏痛，炎性疼痛和神经性疼痛的病症的方法包括单独施用有效量的本发明化合物或与一种或多种治疗活性化合物组合施用。

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