公开(公告)号：US06841624B2

公开(公告)日：2005-01-11

申请号：US10406982

申请日：2003-04-03

申请人： Dominique Charmot ,  Han Ting Chang ,  Yunxiao Li ,  Peter Huefner

发明人： Dominique Charmot ,  Han Ting Chang ,  Yunxiao Li ,  Peter Huefner

IPC分类号： C07D231/10 ,  C07C337/02 ,  C07C337/04 ,  C07D285/125 ,  C08F2/00 ,  C08F2/38 ,  C08F4/00 ,  C08F4/04 ,  C08F8/00

CPC分类号： C08F2/38

摘要： Control agents that have a nitrogen-nitrogen bond covalently bonded to a thiocarbonyl moiety are provided for living-type free radical polymerization of a wide variety of monomers. These control agents provide superior properties for control of the polymerization and/or the properties of the polymers obtained and/or the monomers that may be polymerized. In some embodiments, a bulky group is pendant off the activated thiocarbonyl portion of the control agents. Multifunctional control agents provide the opportunity for a variety of structurally unique polymers, including block copolymers, stars and hyper-branched polymers.

摘要翻译： 提供了与硫代羰基部分共价连接的氮 - 氮键的对照试剂，用于各种单体的活性自由基聚合。 这些控制剂提供了用于控制聚合的优异性质和/或所获得的聚合物和/或可被聚合的单体的性质。 在一些实施方案中，大体积基团从控制剂的活化的硫代羰基部分脱落。 多功能控制剂为各种结构独特的聚合物，包括嵌段共聚物，恒星和超支化聚合物提供了机会。

公开(公告)号：US06518364B2

公开(公告)日：2003-02-11

申请号：US09963235

申请日：2001-09-25

申请人： Dominique Charmot ,  Han Ting Chang ,  Peter Huefner ,  Yunxiao Li

发明人： Dominique Charmot ,  Han Ting Chang ,  Peter Huefner ,  Yunxiao Li

IPC分类号： C08F238

CPC分类号： C08F2/38

摘要： Heterogeneous (e.g., emulsion) polymerization systems include a control agent that has a nitrogen-nitrogen bond covalently bonded to a thiocarbonyl moiety for living-type free radical polymerization of a wide variety of monomers. These control agents provide superior properties for control of the polymerization and/or the properties of the polymers obtained and/or the monomers that may be polymerized. Multifunctional control agents provide the opportunity for a variety of structurally unique polymers, including block copolymers, stars and hyper-branched polymers.

公开(公告)号：US06518448B2

公开(公告)日：2003-02-11

申请号：US09963174

申请日：2001-09-25

申请人： Han Ting Chang ,  Dominique Charmot ,  Yunxiao Li

发明人： Han Ting Chang ,  Dominique Charmot ,  Yunxiao Li

IPC分类号： C07C33300

CPC分类号： C08F2/38

摘要： Control agents that have a nitrogen-nitrogen bond covalently bonded to a thiocarbonyl moiety are provided for living-type free radical polymerization of a wide variety of monomers. These control agents provide superior properties for control of the polymerization and/or the properties of the polymers obtained and/or the monomers that may be polymerized. In some embodiments, a bulky group is pendant off the activated thiocarbonyl portion of the control agents. Multifunctional control agents provide the opportunity for a variety of structurally unique polymers, including block copolymers, stars and hyper-branched polymers.

公开(公告)号：US06482909B2

公开(公告)日：2002-11-19

申请号：US09963870

申请日：2001-09-25

申请人： Dominique Charmot ,  Han Ting Chang ,  Yunxiao Li

发明人： Dominique Charmot ,  Han Ting Chang ,  Yunxiao Li

IPC分类号： C08F400

CPC分类号： C08F2/38

摘要： Control agents that have a nitrogen-nitrogen bond covalently bonded to a thiocarbonyl moiety are provided for living-type free radical polymerization of a wide variety of monomers. These control agents provide superior properties for control of the polymerization and/or the properties of the polymers obtained and/or the monomers that may be polymerized. In some embodiments, a bulky group is pendant off the activated thiocarbonyl portion of the control agents. Multifunctional control agents provide the opportunity for a variety of structurally unique polymers, including block copolymers, stars and hyper-branched polymers.

摘要翻译： 提供了与硫代羰基部分共价连接的氮 - 氮键的对照试剂，用于各种单体的活性自由基聚合。 这些控制剂提供了用于控制聚合的优异性质和/或所获得的聚合物和/或可被聚合的单体的性质。 在一些实施方案中，大体积基团从控制剂的活化的硫代羰基部分脱落。 多功能控制剂为各种结构独特的聚合物，包括嵌段共聚物，恒星和超支化聚合物提供了机会。

公开(公告)号：US06559255B2

公开(公告)日：2003-05-06

申请号：US09520583

申请日：2000-03-08

申请人： Gerrit Klaerner ,  Adam Safir ,  Ralph B. Nielsen ,  Bernd Jandeleit ,  Peter Huefner ,  Yunxiao Li

发明人： Gerrit Klaerner ,  Adam Safir ,  Ralph B. Nielsen ,  Bernd Jandeleit ,  Peter Huefner ,  Yunxiao Li

IPC分类号： C08F222

CPC分类号： C08F220/58 ,  C08F4/00 ,  G01N33/54353

摘要： Nitroxides having an alpha-carbon atom with a destabilizing moiety are effective control agents for emulsion and water-based polymerizations, including the formation of block copolymers from a wide range of monomers. The nitroxide radicals may be used as a free radical or as an adduct with a residue from the initiator. The emulsions have living characteristics, including the re-initiation of polymer chains. Also, a seeded process for emulsions, which includes the step-wise addition of monomer is disclosed, providing access to a wide range of initiator types.

公开(公告)号：US07777070B2

公开(公告)日：2010-08-17

申请号：US12541861

申请日：2009-08-14

申请人： Noa Zerangue ,  Bernd Jandeleit ,  Yunxiao Li ,  Mark A. Gallop

发明人： Noa Zerangue ,  Bernd Jandeleit ,  Yunxiao Li ,  Mark A. Gallop

IPC分类号： C07C269/00

CPC分类号： C07C271/22 ,  C07B2200/07 ,  C07C2601/14

摘要： Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid, pharmaceutical compositions thereof, methods of making prodrugs of trans-4-(aminomethyl)-cyclohexane-carboxylic acid, and methods of using prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof to treat or prevent various diseases or disorders are disclosed. Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof suitable for oral and topical administration and for administration using sustained release dosage forms are also disclosed.

摘要翻译： 反式-4-（氨基甲基） - 环己烷甲酸的氨基甲酸烷基酯氨基甲酸酯前药，其药物组合物，制备反式-4-（氨基甲基） - 环己烷羧酸的前药的方法，以及使用反式-4-（氨基甲基） - 环己烷羧酸及其药物组合物，用于治疗或预防各种疾病或病症。 还公开了反式-4-（氨基甲基） - 环己烷羧酸的氨基甲酸烷氧基烷基酯前药及其适用于口服和局部给药以及使用持续释放剂型给药的药物组合物。

公开(公告)号：US20100036148A1

公开(公告)日：2010-02-11

申请号：US12541861

申请日：2009-08-14

申请人： Noa Zerangue ,  Bernd Jandeleit ,  Yunxiao Li ,  Mark A. Gallop

发明人： Noa Zerangue ,  Bernd Jandeleit ,  Yunxiao Li ,  Mark A. Gallop

IPC分类号： C07C269/00

CPC分类号： C07C271/22 ,  C07B2200/07 ,  C07C2601/14

摘要： Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid, pharmaceutical compositions thereof, methods of making prodrugs of trans-4-(aminomethyl)-cyclohexane-carboxylic acid, and methods of using prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof to treat or prevent various diseases or disorders are disclosed. Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof suitable for oral and topical administration and for administration using sustained release dosage forms are also disclosed.

摘要翻译： 反式-4-（氨基甲基） - 环己烷甲酸的氨基甲酸烷基酯氨基甲酸酯前药，其药物组合物，制备反式-4-（氨基甲基） - 环己烷羧酸的前药的方法，以及使用反式-4-（氨基甲基） - 环己烷羧酸及其药物组合物，用于治疗或预防各种疾病或病症。 还公开了反式-4-（氨基甲基） - 环己烷羧酸的氨基甲酸烷氧基烷基酯前药及其适用于口服和局部给药以及使用持续释放剂型给药的药物组合物。

公开(公告)号：US20090082440A1

公开(公告)日：2009-03-26

申请号：US12205080

申请日：2008-09-05

申请人： Bernd Jandeleit ,  Yunxiao Li ,  Mark A. Gallop ,  Noa Zerangue ,  Peter A. Virsik ,  Wolf-Nicolas Fischer

发明人： Bernd Jandeleit ,  Yunxiao Li ,  Mark A. Gallop ,  Noa Zerangue ,  Peter A. Virsik ,  Wolf-Nicolas Fischer

IPC分类号： A61K31/255 ,  C07C305/10 ,  A61P25/22 ,  A61P25/02 ,  A61P25/28

CPC分类号： C07C309/15

摘要： Pantoic acid ester neopentyl sulfonyl ester prodrugs of acamprosate, pharmaceutical compositions comprising such prodrugs, and methods of using such prodrugs and compositions thereof for treating diseases are disclosed. In particular, acamprosate prodrugs exhibiting enhanced oral bioavailability and methods of using acamprosate prodrugs to treat neurodegenerative disorders, psychotic disorders, mood disorders, anxiety disorders, somatoform disorders, movement disorders, substance abuse disorders, binge eating disorder, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis, and pain are disclosed.

摘要翻译： 公开了阿卡波酸的泛酸酯新戊基磺酰酯前药，包含这些前药的药物组合物，以及使用这些前药及其组合物治疗疾病的方法。 特别地，表现出增强的口服生物利用度的阿坎酸酯前药和使用阿坎酸类前药治疗神经变性疾病，精神病性障碍，情绪障碍，焦虑症，躯体形式障碍，运动障碍，物质滥用障碍，暴饮暴食症，皮质扩张抑郁症相关疾病，耳鸣的方法 ，睡眠障碍，多发性硬化和疼痛。

公开(公告)号：US20090069419A1

公开(公告)日：2009-03-12

申请号：US12204961

申请日：2008-09-05

申请人： Bernd Jandeleit ,  Yunxiao Li ,  Mark A. Gallop ,  Noa Zerangue ,  Peter A. Virsik ,  Wolf-Nicolas Fischer

发明人： Bernd Jandeleit ,  Yunxiao Li ,  Mark A. Gallop ,  Noa Zerangue ,  Peter A. Virsik ,  Wolf-Nicolas Fischer

IPC分类号： A61K31/255 ,  C07C233/01 ,  A61K31/164 ,  A61P25/28 ,  A61P25/22 ,  A61P25/18 ,  C07C303/02

CPC分类号： C07C309/15

摘要： Masked carboxylate neopentyl sulfonyl ester prodrugs of acamprosate, pharmaceutical compositions comprising such prodrugs, and methods of using such prodrugs and compositions thereof for treating diseases are disclosed. In particular, acamprosate prodrugs exhibiting enhanced oral bioavailability and methods of using acamprosate prodrugs to treat neurodegenerative disorders, psychotic disorders, mood disorders, anxiety disorders, somatoform disorders, movement disorders, substance abuse disorders, binge eating disorder, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis, and pain are disclosed.

摘要翻译： 本发明公开了阿卡波酸的掩蔽性羧酸新戊酰磺酰酯前药，包含这些前药的药物组合物，以及使用这些前药及其组合物治疗疾病的方法。 特别地，表现出增强的口服生物利用度的阿坎酸酯前药和使用阿坎酸类前药治疗神经变性疾病，精神病性障碍，情绪障碍，焦虑症，躯体形式障碍，运动障碍，物质滥用障碍，暴饮暴食症，皮质扩张抑郁症相关疾病，耳鸣的方法 ，睡眠障碍，多发性硬化和疼痛。

公开(公告)号：US20090076147A1

公开(公告)日：2009-03-19

申请号：US12205031

申请日：2008-09-05

申请人： Bernd Jandeleit ,  Yunxiao Li ,  Mark A. Gallop ,  Noa Zerangue ,  Peter A. Virsik ,  Wolf-Nicolas Fischer

发明人： Bernd Jandeleit ,  Yunxiao Li ,  Mark A. Gallop ,  Noa Zerangue ,  Peter A. Virsik ,  Wolf-Nicolas Fischer

IPC分类号： A61K31/225 ,  C07C69/00 ,  A61P25/00 ,  A61P29/00

CPC分类号： C07C309/15

摘要： Pantoic acid ester neopentyl sulfonyl ester prodrugs of acamprosate, pharmaceutical compositions comprising such prodrugs, and methods of using such prodrugs and compositions thereof for treating diseases are disclosed. In particular, acamprosate prodrugs exhibiting enhanced oral bioavailability and methods of using acamprosate prodrugs to treat neurodegenerative disorders, psychotic disorders, mood disorders, anxiety disorders, somatoform disorders, movement disorders, substance abuse disorders, binge eating disorder, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis, and pain are disclosed.

摘要翻译： 公开了阿卡波酸的泛酸酯新戊基磺酰酯前药，包含这些前药的药物组合物，以及使用这些前药及其组合物治疗疾病的方法。 特别地，表现出增强的口服生物利用度的阿坎酸酯前药和使用阿坎酸类前药治疗神经变性疾病，精神病性障碍，情绪障碍，焦虑症，躯体形式障碍，运动障碍，物质滥用障碍，暴饮暴食症，皮质扩张抑郁症相关疾病，耳鸣的方法 ，睡眠障碍，多发性硬化和疼痛。