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公开(公告)号：EP1610776A2
公开(公告)日：2006-01-04
申请号：EP04758273.9
申请日：2004-03-24
Applicant: Merck & Co. Inc. , Evotec OAI
Inventor： FISHER, Michael, H. , GARCIA, Maria, L. , KACZOROWSKI, Gregory, J. , MEINKE, Peter, T. , PARSONS, William, H. , BOYD, Edward Andrew , PRICE, Stephen , STIBBARD, John
IPC: A61K31/404 , C07D209/04
CPC classification number: C07D405/12 , C07D209/28 , C07D401/12 , C07D413/12 , C07D417/12 , C07D417/14
Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
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公开(公告)号：EP1709014B1
公开(公告)日：2007-05-30
申请号：EP05722436.2
申请日：2005-01-18
Applicant: Merck & Co., Inc.
Inventor： SHI, Guo, Q. , MEINKE, Peter, T. , DROPINSKI, James, F. , ZHANG, Yong
IPC: C07D263/44 , C07D277/34 , A61K31/421 , A61K31/426 , A61P3/10
CPC classification number: C07D263/44 , A61K38/26 , A61K38/28 , C07D263/64 , C07D277/34 , A61K2300/00
Abstract: Phenoxyphenyl and phenoxybenzyl oxazolidine-2,4-diones and thiazolidine-2,4-diones of formula (I) are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
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公开(公告)号：EP1546142A2
公开(公告)日：2005-06-29
申请号：EP03791782.0
申请日：2003-08-28
Applicant: Merck & Co., Inc.
Inventor： ACTON, John, J., III , MEINKE, Peter, T. , WOOD, Harold, B. , BLACK, Regina, M.
IPC: C07D413/04 , A61K31/42
CPC classification number: C07D413/14 , C07D413/04
Abstract: Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
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公开(公告)号：EP1204411A1
公开(公告)日：2002-05-15
申请号：EP00947507.0
申请日：2000-07-19
Applicant: MERCK & CO., INC.
Inventor： MEINKE, Peter, T. , SCHMATZ, Dennis , FISHER, Michael, H. , RATTRAY, Sandra, J. , COLLETTI, Steven, L. , WYVRATT, Matthew, J. , MYERS, Robert, W. , GURNETT, Anne, M.
IPC: A61K31/395 , A61K38/12 , C07D257/10 , C07K5/12
CPC classification number: C07K5/126 , A61K38/00 , Y02A50/402 , Y02A50/411 , Y02A50/475
Abstract: Cyclic tetrapeptide compounds derived from apicidin therapeutically inhibit histone deacetylase activity and are represented by Formula (I).
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公开(公告)号：EP1909789A2
公开(公告)日：2008-04-16
申请号：EP06787175.6
申请日：2006-07-14
Applicant: Merck & Co., Inc.
Inventor： MEINKE, Peter, T. , SHI, Guo, Q. , WOOD, Harold, B.
IPC: A61K31/44 , A61K31/433 , A61K31/4245 , C07D401/02
CPC classification number: C07D417/14
Abstract: Pyridinyloxyphenyl and pyridinyloxybenzyl oxazolidine-2,4-diones and thiazolidine-2,4-diones are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
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公开(公告)号：EP1765329A2
公开(公告)日：2007-03-28
申请号：EP05763714.2
申请日：2005-06-28
Applicant: Merck & Co., Inc.
Inventor： LIU, Kun , MEINKE, Peter, T. , WOOD, Harold, B.
IPC: A61K31/404 , C07D209/04
CPC classification number: C07D413/14 , C07D413/10
Abstract: Indoles of Formula (I) having -X-aryl-(CH2)x#191-oxazolidinedione and -X-heteroaryl-(CH2)X-oxazolidinedione substituents on the N atom of the indole ring, where x is 0 or 1, and -X-is a bond or -CH2-, and their thiazolidinedione analogs, are PPAR gamma agonists or partial agonists and are useful in the treatment and control of type II diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
Abstract translation: 在吲哚环的N原子上具有-X-芳基 - （CH 2）x＃191-恶唑烷二酮和-X-杂芳基 - （CH 2）x - 恶唑烷二酮取代基的式（I）的吲哚，其中x为0或1， -X-是键或-CH 2 - ，它们的噻唑烷二酮类似物是PPARγ激动剂或部分激动剂，并且可用于治疗和控制II型糖尿病，包括高血糖症，血脂异常，高脂血症，高胆固醇血症，高甘油三酯血症和肥胖症 通常与2型糖尿病有关。
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公开(公告)号：EP1537078A1
公开(公告)日：2005-06-08
申请号：EP03791952.9
申请日：2003-08-27
Applicant: Merck & Co., Inc.
Inventor： ACTON, John, J., III , DEBENHAM, Sheryl, D. , LIU, Kun , MEINKE, Peter, T. , WOOD, Harold, B. , BLACK, Regina, M.
IPC: C07D209/12 , A61K31/404 , A61P3/10 , C07D401/04 , C07D209/36 , C07D413/04 , C07D209/30 , C07D401/06 , C07D405/06 , C07D403/12 , C07D209/10
CPC classification number: C07D209/10 , C07D209/12 , C07D209/14 , C07D209/30 , C07D209/36 , C07D401/04 , C07D401/06 , C07D403/12 , C07D405/06 , C07D413/04
Abstract: Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
Abstract translation: 具有芳氧基链烷酸取代基或芳基链烷酸取代基的吲哚是PPARγ的激动剂或部分激动剂，并且可用于治疗和控制II型糖尿病症状的高血糖症，以及血脂异常，高脂血症，高胆固醇血症，高甘油三酯血症和肥胖症， 通常与2型糖尿病有关。
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8.发明公开METHOD OF TREATMENT USING FUSED AROMATIC COMPOUNDS HAVING ANTI-DIABETIC ACTIVITY 有权治疗的方法，使用稠合芳族化合物与抗糖尿病作用
公开(公告)号：EP2155187A1
公开(公告)日：2010-02-24
申请号：EP08767538.5
申请日：2008-05-02
Applicant: Merck & Co., Inc.
Inventor： MEINKE, Peter, T. , DENKER, Andrew , MEININGER, Gary, E. , UEMURA, Naoto , WAGNER, John, A. , CHARNICK, Steven
Abstract: Fused aromatic compounds of Formula I are PPAR gamma agonists or partial agonists and are useful for weekly dosing in the treatment or control of type II diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
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公开(公告)号：EP1907381A1
公开(公告)日：2008-04-09
申请号：EP06786261.5
申请日：2006-06-30
Applicant: Merck & Co., Inc.
Inventor： DROPINSKI, James, F. , MEINKE, Peter, T. , SHI, Guo, Q. , ZHANG, Yong
IPC: C07D413/00 , C07D307/44 , C07D417/00 , C07D401/00 , A61K31/44 , A61K31/42 , A61K31/415
CPC classification number: C07D263/44 , C07D413/12 , C07D417/12
Abstract: Phenoxyphenyl and phenoxybenzyl oxazolidine-2,4-diones and thiazolidine-2,4-diones are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
Abstract translation: 苯氧基苯基和苯氧基苄基恶唑烷-2,4-二酮和噻唑烷-2,4-二酮是PPARγ的激动剂或部分激动剂，并且可用于治疗和控制II型糖尿病症状的高血糖以及血脂异常，高脂血症 ，高胆固醇血症，高甘油三酯血症和通常与2型糖尿病有关的肥胖症。
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公开(公告)号：EP1789381A2
公开(公告)日：2007-05-30
申请号：EP05770022.1
申请日：2005-07-08
Applicant: Merck & Co., Inc.
Inventor： CHAKRAVARTY, Prasun, K. , KUO, Howard , MATTHEWS, Jay, M. , MEINKE, Peter, T.
IPC: C07C259/10 , C07C311/21 , C07D271/12 , A61K31/16
CPC classification number: 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
Abstract: 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.
Abstract translation: 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。
