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1. 发明申请

US20090286759A1 ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS OF SYNTHESIS AND USE 失效
标题翻译：丙烯酰基碳酸酯产品，合成和使用方法
公开(公告)号：US20090286759A1
公开(公告)日：2009-11-19
申请号：US12506961
申请日：2009-07-21
申请人： Mark A Gallop , Feng Xu , Thu Phan , Usha Dilip , Ge Peng
发明人： Mark A Gallop , Feng Xu , Thu Phan , Usha Dilip , Ge Peng
IPC分类号： A61K31/662 , C07C271/06
CPC分类号： C07F9/301
摘要： Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of making acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of using acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, and pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs 3-aminopropylphosphinic acid and analogs thereof for treating diseases or disorders such as mild cognitive impairment, cognitive impairment associated with Alzheimer's disease Alzheimer's disease, depression, anxiety, and epilepsy are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, which are suitable for oral administration and sustained release oral dosage forms are also disclosed.
摘要翻译： 3-氨基丙基次膦酸的氨基甲酸烷基酯氨基甲酸酯前药及其类似物，3-氨基丙基次膦酸及其类似物的制备酰氨基烷基氨基甲酸酯前药的方法及其类似物，使用3-氨基丙基次膦酸及其类似物的酰氨基烷基氨基甲酸酯前药的方法和包含酰氨基烷基氨基甲酸酯前药3 - 氨基丙基次膦酸及其类似物用于治疗疾病或病症如轻度认知障碍，与阿尔茨海默氏病相关的认知障碍阿尔茨海默氏病，抑郁症，焦虑和癫痫。还公开了适用于口服给药和缓释口服剂型的3-氨基丙基次膦酸的氨基氧基烷基氨基甲酸酯前药及其类似物。

2. 发明授权

US07569576B2 Cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, compositions and uses thereof 失效
标题翻译： GABA类似物的环状1-（酰氧基） - 烷基前体药物，其组合物和用途
公开(公告)号：US07569576B2
公开(公告)日：2009-08-04
申请号：US11332607
申请日：2006-01-12
申请人： Mark A Gallop , Jia-Ning Xiang , Fenmei Yao , Laxminarayan Bhat
发明人： Mark A Gallop , Jia-Ning Xiang , Fenmei Yao , Laxminarayan Bhat
IPC分类号： A61K31/515 , A61K31/44 , C07D317/00 , C07D407/00 , C07D313/16
CPC分类号： C07D307/89 , C07D309/30 , C07D313/04
摘要： The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.
摘要翻译：本发明提供GABA类似物的环状1-（酰氧基） - 烷基前体药物，制备GABA类似物的环状1-（酰氧基） - 烷基前体药物的方法和GABA类似物的环状1-（酰氧基）烷基前体药物的组合物。本发明还提供了使用GABA类似物的环状1-（酰氧基） - 烷基前体药物和GABA类似物的环状1-（酰氧基） - 烷基前体药物组合物的方法。

3. 发明授权

US07026351B2 Cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, compositions and uses thereof 失效
公开(公告)号：US07026351B2
公开(公告)日：2006-04-11
申请号：US10393806
申请日：2003-03-20
申请人： Mark A Gallop , Jia-Ning Xiang , Fenmei Yao , Laxminarayan Bhat
发明人： Mark A Gallop , Jia-Ning Xiang , Fenmei Yao , Laxminarayan Bhat
IPC分类号： A61K31/35 , A61K31/335 , C07D307/00 , C07D313/00 , C07D307/78
CPC分类号： C07D307/89 , C07D309/30 , C07D313/04
摘要： The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.

4. 发明授权

US07799829B2 Acyloxyalkyl carbamate prodrugs of α-amino acids, methods of synthesis and use 失效
标题翻译： α-氨基酸氨基氧烷基氨基甲酸酯前药，合成和使用方法
公开(公告)号：US07799829B2
公开(公告)日：2010-09-21
申请号：US12416823
申请日：2009-04-01
申请人： Xuedong Dai , Archana Gangakhedkar , Jia-Ning Xiang , Mark A Gallop
发明人： Xuedong Dai , Archana Gangakhedkar , Jia-Ning Xiang , Mark A Gallop
IPC分类号： A61K31/27 , C07C69/74
CPC分类号： C07C271/16 , C07C271/24 , C07C271/34 , C07C271/36 , C07C2601/02 , C07C2601/14
摘要： Acyloxyalkyl carbamate prodrugs of α-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of α-amino acids and methods of using acyloxyalkyl carbamate prodrugs of α-amino acids, and pharmaceutical compositions thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of α-amino acids suitable for oral administration using sustained release dosage forms are also disclosed.
摘要翻译：公开了α-氨基酸的氰氧基烷基氨基甲酸酯前药，其药物组合物，制备α-氨基酸的酰氨基烷基氨基甲酸酯前药的方法和使用α-氨基酸的酰氨基烷基氨基甲酸酯前药的方法及其药物组合物来治疗疾病。还公开了适用于使用持续释放剂型的口服给药的α-氨基酸的氨基氧基烷基氨基甲酸酯前药。

5. 发明申请

US20090124582A1 Acyloxyalkyl Carbamate Prodrugs, Methods of Synthesis, and Use 有权
标题翻译：氨苄青霉素前体药物，合成方法和用途
公开(公告)号：US20090124582A1
公开(公告)日：2009-05-14
申请号：US12353703
申请日：2009-01-14
申请人： Mark A Gallop
发明人： Mark A Gallop
IPC分类号： A61K31/662 , A61P1/00
CPC分类号： C07F9/301 , C07F9/4816
摘要： Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of making prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of using prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and pharmaceutical compositions thereof for treating or preventing diseases or disorders such as spasticity or gastroesophageal reflux disease are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and sustained release oral dosage forms thereof, which are suitable for oral administration, are also disclosed.
摘要翻译： 3-氨基丙基亚膦酸，3-氨基丙基次膦酸及其类似物的氨基氧烷基氨基甲酸酯前药，包含3-氨丙基亚磷酸，3-氨基丙基次膦酸及其类似物的酰氨基烷基氨基甲酸酯前药的药物组合物，制备3-氨基丙基亚磷酸前体药物的方法 - 氨基丙基次膦酸及其类似物，公开了使用3-氨基丙基亚膦酸，3-氨基丙基次膦酸及其类似物的前药的方法及其药物组合物，用于治疗或预防诸如痉挛或胃食管反流病等疾病或病症。还公开了适用于口服给药的3-氨基丙基亚膦酸，3-氨基丙基次膦酸及其类似物的氨基甲酸烷基酯氨基甲酸酯前药和缓释口服剂型。

6. 发明授权

US07531572B2 Acyloxyalkyl carbamate prodrugs of α-amino acids, methods of synthesis and use 失效
标题翻译： α-氨基酸的氨基甲酸氨基甲酸酯前体药物，合成和使用方法
公开(公告)号：US07531572B2
公开(公告)日：2009-05-12
申请号：US11878661
申请日：2007-07-26
申请人： Xuedong Dai , Archana Gangakhedkar , Jia-Ning Xiang , Mark A Gallop
发明人： Xuedong Dai , Archana Gangakhedkar , Jia-Ning Xiang , Mark A Gallop
IPC分类号： A61K31/27 , C07C269/00
CPC分类号： C07C271/16 , C07C271/24 , C07C271/34 , C07C271/36 , C07C2601/02 , C07C2601/14
摘要： Acyloxyalkyl carbamate prodrugs of α-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of α-amino acids and methods of using acyloxyalkyl carbamate prodrugs of α-amino acids, and pharmaceutical compositions thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of α-amino acids suitable for oral administration using sustained release dosage forms are also disclosed.
摘要翻译：公开了α-氨基酸的氰氧基烷基氨基甲酸酯前药，其药物组合物，制备α-氨基酸的酰氨基烷基氨基甲酸酯前药的方法和使用α-氨基酸的氨基甲酸酰氨基甲酸酯前药的方法及其药物组合物来治疗疾病。还公开了适用于使用持续释放剂型的口服给药的α-氨基酸的氨基氧基烷基氨基甲酸酯前药。

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