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1. 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。

2. 发明申请

WO0134632A3 ALIPHATIC HYDROXY SUBSTITUTED PIPERIDYL DIARYL PYRROLE DERIVATIVES AS ANTIPROTOZOAL AGENTS 审中-公开
标题翻译：作为抗真菌剂的二氢羟基替代哌啶衍生物衍生物
公开(公告)号：WO0134632A3
公开(公告)日：2001-09-27
申请号：PCT/US0030748
申请日：2000-11-09
申请人： MERCK & CO INC , BIFTU TESFAYE , FENG DANQING D , LIANG GUI BAI , PONPIPOM MITREE M , QIAN XIAOXIA , FISHER MICHAEL H , WYVRATT MATTHEW J , BUGIANESI ROBERT L
发明人： BIFTU TESFAYE , FENG DANQING D , LIANG GUI-BAI , PONPIPOM MITREE M , QIAN XIAOXIA , FISHER MICHAEL H , WYVRATT MATTHEW J , BUGIANESI ROBERT L
IPC分类号： C07D401/14 , C07D405/14 , A61K31/4545
CPC分类号： C07D401/14 , C07D405/14
摘要： Trisubstituted pyrroles are antiprotozal agents useful in the treatment and prevention of protozoal diseases in human an animals, including the control of coccidiosis in poultry.
摘要翻译：三取代吡咯是可用于治疗和预防人类动物体内原生动物疾病的抗替罗尔剂，包括控制家禽中的球虫病。

3. 发明申请

WO1997046556A1 OXADIAZOLE BENZENESULFONAMIDES AS SELECTIVE 'beta'3 AGONISTS FOR THE TREATMENT OF DIABETES AND OBESITY 审中-公开
标题翻译：作为选择性β3治疗糖尿病和肥胖症的氧化亚苯基亚砜
公开(公告)号：WO1997046556A1
公开(公告)日：1997-12-11
申请号：PCT/US1997009536
申请日：1997-06-03
申请人： MERCK & CO., INC. , BIFTU, Tesfaye , FENG, Danqing, Dennis , FISHER, Michael, H. , KUO, Chan-Hwa , LIANG, Gui-Bai , WEBER, Ann, E. , NAYLOR, Elizabeth, M.
发明人： MERCK & CO., INC.
IPC分类号： C07D413/10
CPC分类号： C07D213/40 , C07D409/14 , C07D413/12 , C07D413/14
摘要： Oxadiazole substituted benzenesulfonamides 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：恶二唑取代的苯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

WO2005060571A3 ANTIPROTOZOAL IMIDAZOPYRIDINE COMPOUNDS 审中-公开
标题翻译：抗真菌药咪唑吡啶化合物
公开(公告)号：WO2005060571A3
公开(公告)日：2005-12-15
申请号：PCT/US2004040617
申请日：2004-12-06
申请人： MERCK & CO INC , BIFTU TESFAYE , FISHER MICHAEL H , WYVRATT MATTHEW J
发明人： BIFTU TESFAYE , FISHER MICHAEL H , WYVRATT MATTHEW J
IPC分类号： A61K31/4188 , C07D401/04 , C07D403/04 , C07D417/04 , C07D471/04
CPC分类号： C07D471/04
摘要： Compounds described by the Formula (I) or (II): or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and birds. A method for controlling coccidiosis in poultry comprises administering an effective amount of the compound alone, or in combination with one or more anticoccidieal agent(s). A composition for controlling coccidiosis in poultry comprises the compound alone, or in combination with one or more anticoccidial agent(s). Methods for the treatment and prevention of mammalian protozoal diseases, such as, for example, toxoplasmosis, malaria. African typanosomiasis, Chagas disease, and opportunistic infections comprise administering the compound alone, or in combination with one or more antiprotozoal agent(s).
摘要翻译：由式（I）或（II）表示的化合物：或其药学上可接受的盐或N-氧化物。该化合物可用于治疗和预防哺乳动物和鸟类中的原生动物疾病。用于控制家禽中球虫病的方法包括单独施用有效量的化合物，或与一种或多种抗球虫剂组合施用。用于控制家禽中球虫病的组合物包含单独的化合物，或与一种或多种抗球虫剂组合。用于治疗和预防哺乳动物原生动物疾病的方法，例如弓形体病，疟疾。非洲typanosomias，恰加斯病和机会性感染包括单独施用化合物，或与一种或多种抗原虫剂组合施用。

5. 发明申请

WO2005047270A3 SUBSTITUTED TRIAZOLES AS SODIUM CHANNEL BLOCKERS 审中-公开
公开(公告)号：WO2005047270A3
公开(公告)日：2005-05-26
申请号：PCT/US2004/037280
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
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 (I), (II), (III).

6. 发明申请

WO2004094395A3 BIARYL SUBSTITUTED THIAZOLES, OXAZOLES AND IMIDAZOLES AS SODIUM CHANNEL BLOCKERS 审中-公开
公开(公告)号：WO2004094395A3
公开(公告)日：2004-11-04
申请号：PCT/US2004/011271
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： C07D277/42
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.

7. 发明申请

WO2004083189A1 BIARYL SUBSTITUTED TRIAZOLES AS SODIUM CHANNEL BLOCKERS 审中-公开
标题翻译： BIARYL取代三唑作为钠通道阻塞剂
公开(公告)号：WO2004083189A1
公开(公告)日：2004-09-30
申请号：PCT/US2004/007597
申请日：2004-03-12
申请人： MERCK & CO., INC. , CHAKRAVARTY, Prasun, K. , FISHER, Michael, H. , PALUCKI, Brenda , PARK, Min, K. , PARSONS, William, H. , ZHOU, Bishan , CAREY, James, P. , FRANTZ, Douglas, E. , KRESS, Michael, H. , WEAVER, Damian
发明人： CHAKRAVARTY, Prasun, K. , FISHER, Michael, H. , PALUCKI, Brenda , PARK, Min, K. , PARSONS, William, H. , ZHOU, Bishan , CAREY, James, P. , FRANTZ, Douglas, E. , KRESS, Michael, H. , WEAVER, Damian
IPC分类号： C07D249/08
CPC分类号： C07D249/08 , C07D249/10
摘要： Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and 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, 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，II或III表示的二芳基取代的三唑化合物或其药学上可接受的盐，以及制备这些化合物及其盐的方法。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。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

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。

9. 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。

10. 发明申请

WO1994018161A1 SUBSTITUTED PHENYL SULFONAMIDES AS SELECTIVE beta3 AGONISTS FOR THE TREATMENT OF DIABETES AND OBESITY 审中-公开
标题翻译：取代的苯基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：WO1994018161A1
公开(公告)日：1994-08-18
申请号：PCT/US1994000766
申请日：1994-01-19
申请人： MERCK & CO., INC. , FISHER, Michael, H. , MATHVINK, Robert, J. , OK, Hyun, O. , PARMEE, Emma, R. , WEBER, Ann, E.
发明人： MERCK & CO., INC.
IPC分类号： C07C311/21
CPC分类号： C07D213/73 , C07C311/13 , C07C311/14 , C07C311/21 , C07C311/29 , C07C311/44 , C07C311/46 , C07C311/47 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D209/12 , C07D209/34 , C07D213/65 , C07D213/71 , C07D215/36 , C07D261/20 , C07D277/74 , C07D285/14 , C07D307/79 , C07D307/82 , C07D311/08 , C07D317/62 , C07D319/18 , C07D333/34 , C07D333/54 , C07D333/62 , C07D401/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Substituted phenylsulphonamides having formula (I) where the variables are as defined in Claim 1; are selective beta-3 adrenergic receptor agonists with very little beta-1 and beta-2 adregenic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have very potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to reduce triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to reduce gut motility. In addition, the compounds can be used to reduce neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenylsulphonamide with an appropriately substituted alkyl epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for the reduction of 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）的取代的苯基磺酰胺，其中变量如权利要求1所定义; 是具有非常少的β-1和β-2 adregenic受体活性的选择性β-3肾上腺素能受体激动剂，因此这些化合物能够增加细胞中的脂肪分解和能量消耗。因此，化合物在治疗II型糖尿病和肥胖中具有非常有效的活性。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减少肠道运动性。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烷基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。

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