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公开(公告)号：US20110257074A1
公开(公告)日：2011-10-20
申请号：US12634877
申请日：2009-12-10
CPC分类号： C07C45/80 , C07C2601/10 , C07C49/743
摘要： Methods of purifying individual congeners of substituted cyclohexa-2,4-dienones, substituted cyclohexane-1,3,5-triones, substituted cyclopent-2-en-1-ones, and substituted 1,3-cyclopentadiones and compositions using the same are disclosed. The purification method includes the steps of: (a) selecting a congener to be isolated; (b) dissolving the mixture of congeners in a bi-phasic solvent system specific to the selected congener to be isolated, wherein said bi-phasic system has a partition coefficient from about 0.5 to 5.0; (c) subjecting the mixture dissolved in the bi-phasic solvent system to a counter current chromatography; and (d) isolating the selected congener in substantially pure form.
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2.发明申请METHOD FOR THE PURIFICATION OF SUBSTITUTED CYCLOPENT-2-EN-1-ONE CONGENERS AND SUBSTITUTED 1,3-CYCLOPENTADIONE CONGENERS FROM A COMPLEX MIXTURE USING COUNTERCURRENT SEPARATION 审中-公开使用反电势分离从复合混合物中纯化取代的环戊二烯-1-酮-1-一元素和取代的1,3-环戊二烯化合物的方法公开(公告)号：US20110275721A1
公开(公告)日：2011-11-10
申请号：US13132492
申请日：2009-12-10
IPC分类号： A61K31/122 , C07C45/80
CPC分类号： C07C45/80 , C07C2601/10 , C07C49/743
摘要： Methods of purifying individual congeners of substituted cyclohexa-2,4-dienones, substituted cyclohexane-1,3,5-triones, substituted cyclopent-2-en-1-ones, and substituted 1,3-cyclopentadiones and compositions using the same are disclosed. The purification method includes the steps of: (a) selecting a congener to be isolated; (b) dissolving the mixture of congeners in a bi-phasic solvent system specific to the selected congener to be isolated, wherein said bi-phasic system has a partition coefficient from about 0.5 to 5.0; (c) subjecting the mixture dissolved in the bi-phasic solvent system to a counter current chromatography; and (d) isolating the selected congener in substantially pure form.
摘要翻译： 取代的环己烷-2,4-二烯酮，取代的环己烷-1,3,5-三酮，取代的环戊-2-烯-1-酮和取代的1,3-环戊二氢和其组合物的纯化方法 披露 净化方法包括以下步骤：（a）选择要分离的同源物; （b）将同系物的混合物溶解在所选择的同源物特异性的双相溶剂系统中，其中所述双相系统具有约0.5-5.0的分配系数; （c）使溶解在双相溶剂体系中的混合物进行逆流色谱; 和（d）以基本上纯的形式分离所选择的同类物。
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3.发明申请SUBSTITUTED 1,3-CYCLOPENTADIONE MULTI-TARGET PROTEIN KINASE MODULATORS OF CANCER, ANGIOGENESIS AND THE INFLAMMATORY PATHWAYS ASSOCIATED THEREWITH 审中-公开取代的1,3-CYCLOPENTADIONE多靶点蛋白激酶调节因子与癌细胞，血管生成以及与之相关的炎症途径公开(公告)号：US20100137449A1
公开(公告)日：2010-06-03
申请号：US12331887
申请日：2008-12-10
申请人： Matthew L. Tripp , John G. Babish , Jeffrey S. Bland , Veera Konda , Anu Desai , Gary Darland , Brian J. Carroll , James S. Traub , Linda M. Pacioretty , Dennis Emma
发明人： Matthew L. Tripp , John G. Babish , Jeffrey S. Bland , Veera Konda , Anu Desai , Gary Darland , Brian J. Carroll , James S. Traub , Linda M. Pacioretty , Dennis Emma
IPC分类号： A61K31/122 , A61P35/00 , A61P9/10
CPC分类号： A61K31/12 , A61K45/06 , A61K2300/00
摘要： Compounds and methods for multi-targeted protein kinase modulation for angiogenesis, cancer treatment or the inflammatory pathways associated with those conditions are disclosed. The compounds and methods disclosed are based on substituted 1,3-cyclopentadione compounds.
摘要翻译： 公开了用于血管生成，癌症治疗或与这些病症相关的炎症途径的多靶向蛋白激酶调节的化合物和方法。 所公开的化合物和方法是基于取代的1,3-环戊二酮化合物。
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4.发明授权Cis, 3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-derivatives, substantially enantiomerically pure compositions and methods 有权顺式，3,4-二羟基-2-（3-甲基丁酰基）-5-（3-甲基丁基）-4-（4-甲基戊酰基）环戊-2-烯-1-酮衍生物，基本上对映体纯的组合物和方法公开(公告)号：US08410179B2
公开(公告)日：2013-04-02
申请号：US13420062
申请日：2012-03-14
申请人： Brian J. Carroll , Gary Darland , Anuradha Desai , Veera Konda , Clinton J. Dahlberg , Jan Urban
发明人： Brian J. Carroll , Gary Darland , Anuradha Desai , Veera Konda , Clinton J. Dahlberg , Jan Urban
CPC分类号： A61K31/122 , C07B2200/13 , C07C49/707
摘要： The present application provides cis 3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one derivatives and substantially enantiomerically pure compositions thereof. These derivatives include (+)-(4S,5R)-3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one, (−)-(4R,5S)-3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one, and salts and crystals thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPARγ, activate GPR120, inhibit inflammation, and treat conditions responsive to PPARγ modulation, conditions responsive to GPR120 modulation, and metabolic disturbances such as diabetes.
摘要翻译： 本申请提供了顺式3,4-二羟基-2-（3-甲基丁酰基）-5-（3-甲基丁基）-4-（4-甲基戊酰基）环戊-2-烯-1-酮衍生物及其基本上对映体纯的组合物 。 这些衍生物包括（+） - （4S，5R）-3,4-二羟基-2-（3-甲基丁酰基）-5-（3-甲基丁基）-4-（4-甲基戊酰基）环戊-2-烯-1-酮 （ - ） - （4R，5S）-3,4-二羟基-2-（3-甲基丁酰基）-5-（3-甲基丁基）-4-（4-甲基戊酰基）环戊-2-烯-1-酮 ，及其盐和晶体。 本申请还提供了使用所公开的化合物和组合物来激活PPARγ，激活GPR120，抑制炎症和治疗对PPARγ调节有响应的病症，对GPR120调节作用的病症和代谢紊乱如糖尿病的方法。
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5.发明授权CIS 3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-derivatives, substantially enantiomerically pure compositions and methods 有权CIS 3,4-二羟基-2-（3-甲基丁酰基）-5-（3-甲基丁基）-4-（4-甲基戊酰基）环戊-2-烯-1-酮衍生物，基本上对映体纯的组合物和方法公开(公告)号：US08410178B2
公开(公告)日：2013-04-02
申请号：US13284852
申请日：2011-10-28
申请人： Brian J. Carroll , Gary Darland , Anuradha Desai , Veera Konda , Clinton J. Dahlberg , Jan Urban
发明人： Brian J. Carroll , Gary Darland , Anuradha Desai , Veera Konda , Clinton J. Dahlberg , Jan Urban
CPC分类号： A61K31/122 , C07B2200/13 , C07C49/707
摘要： The present application provides cis 3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one derivatives and substantially enantiomerically pure compositions thereof. These derivatives include (+)-(4S,5R)-3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one, (−)-(4R,5S)-3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one, and salts and crystals thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPARγ, activate GPR120, inhibit inflammation, and treat conditions responsive to PPARγ modulation, conditions responsive to GPR120 modulation, and metabolic disturbances such as diabetes.
摘要翻译： 本申请提供了顺式3,4-二羟基-2-（3-甲基丁酰基）-5-（3-甲基丁基）-4-（4-甲基戊酰基）环戊-2-烯-1-酮衍生物及其基本上对映体纯的组合物 。 这些衍生物包括（+） - （4S，5R）-3,4-二羟基-2-（3-甲基丁酰基）-5-（3-甲基丁基）-4-（4-甲基戊酰基）环戊-2-烯-1-酮 （ - ） - （4R，5S）-3,4-二羟基-2-（3-甲基丁酰基）-5-（3-甲基丁基）-4-（4-甲基戊酰基）环戊-2-烯-1-酮 ，及其盐和晶体。 本申请还提供了使用所公开的化合物和组合物来激活PPARγ，激活GPR120，抑制炎症和治疗对PPARγ调节有响应的病症，对GPR120调节作用的病症和代谢紊乱如糖尿病的方法。
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6.发明申请CIS, 3,4-DIHYDROXY-2-(3-METHYLBUTANOYL)-5-(3-METHYLBUTYL)-4-(4-METHYLPENTANOYL)CYCLOPENT-2-EN-1-ONE DERIVATIVES, SUBSTANTIALLY ENANTIOMERICALLY PURE COMPOSITIONS AND METHODS 有权CIS，3,4-二羟基-2-（3-甲基丁基）-5-（3-甲基丁基）-4-（4-甲基戊基）环丙-2-烯-1-酮衍生物，基本上纯的组合物和方法公开(公告)号：US20130018105A1
公开(公告)日：2013-01-17
申请号：US13420062
申请日：2012-03-14
申请人： Brian J. CARROLL , Gary Darland , Anuradha Desai , Veera Konda , Clinton J. Dahlberg , Jan Urban
发明人： Brian J. CARROLL , Gary Darland , Anuradha Desai , Veera Konda , Clinton J. Dahlberg , Jan Urban
IPC分类号： A61K31/122 , A61P29/00 , A61P3/10 , C07C49/597
CPC分类号： A61K31/122 , C07B2200/13 , C07C49/707
摘要： The present application provides cis 3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one derivatives and substantially enantiomerically pure compositions thereof. These derivatives include (+)-(4S,5R)—3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one, (−)-(4R,5S)-3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one, and salts and crystals thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPARγ, activate GPR120, inhibit inflammation, and treat conditions responsive to PPARγ modulation, conditions responsive to GPR120 modulation, and metabolic disturbances such as diabetes.
摘要翻译： 本申请提供了顺式3,4-二羟基-2-（3-甲基丁酰基）-5-（3-甲基丁基）-4-（4-甲基戊酰基）环戊-2-烯-1-酮衍生物及其基本上对映体纯的组合物 。 这些衍生物包括（+） - （4S，5R）-3,4-二羟基-2-（3-甲基丁酰基）-5-（3-甲基丁基）-4-（4-甲基戊酰基）环戊-2-烯-1-酮 （ - ） - （4R，5S）-3,4-二羟基-2-（3-甲基丁酰基）-5-（3-甲基丁基）-4-（4-甲基戊酰基）环戊-2-烯-1-酮 ，及其盐和晶体。 本申请还提供了使用所公开的化合物和组合物来激活PPARγ，激活GPR120，抑制炎症和治疗对PPARγ调节有响应的病症，对GPR120调节作用的病症和代谢紊乱如糖尿病的方法。
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7.发明申请CIS 3,4-DIHYDROXY-2-(3-METHYLBUTANOYL)-5-(3-METHYLBUTYL)-4-(4-METHYLPENTANOYL)CYCLOPENT-2-EN-1-ONE DERIVATIVES, SUBSTANTIALLY ENANTIOMERICALLY PURE COMPOSITIONS AND METHODS 有权（3,4-二羟基-2-（3-甲基丁基）-5-（3-甲基丁基）-4-（4-甲基戊基）环戊-2-烯-1-酮衍生物，主要是纯的组合物和方法公开(公告)号：US20120108671A1
公开(公告)日：2012-05-03
申请号：US13284852
申请日：2011-10-28
申请人： Brian J. Carroll , Gary Darland , Anuradha Desai , Veera Konda , Clinton J. Dahlberg , Jan Urban
发明人： Brian J. Carroll , Gary Darland , Anuradha Desai , Veera Konda , Clinton J. Dahlberg , Jan Urban
IPC分类号： A61K31/122 , A61P29/00 , A61P3/04 , C07C49/707 , A61P3/10
CPC分类号： A61K31/122 , C07B2200/13 , C07C49/707
摘要： The present application provides cis 3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one derivatives and substantially enantiomerically pure compositions thereof. These derivatives include (+)-(4S,5R)-3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one, (−)-(4R,5S)-3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one, and salts and crystals thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPARγ, activate GPR120, inhibit inflammation, and treat conditions responsive to PPARγ modulation, conditions responsive to GPR120 modulation, and metabolic disturbances such as diabetes.
摘要翻译： 本申请提供了顺式3,4-二羟基-2-（3-甲基丁酰基）-5-（3-甲基丁基）-4-（4-甲基戊酰基）环戊-2-烯-1-酮衍生物及其基本上对映体纯的组合物 。 这些衍生物包括（+） - （4S，5R）-3,4-二羟基-2-（3-甲基丁酰基）-5-（3-甲基丁基）-4-（4-甲基戊酰基）环戊-2-烯-1-酮 （ - ） - （4R，5S）-3,4-二羟基-2-（3-甲基丁酰基）-5-（3-甲基丁基）-4-（4-甲基戊酰基）环戊-2-烯-1-酮 ，及其盐和晶体。 本申请还提供了使用所公开的化合物和组合物来激活PPARγ，激活GPR120，抑制炎症和治疗对PPARγ调节有响应的病症，对GPR120调节作用的病症和代谢紊乱如糖尿病的方法。
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