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1. 发明申请

WO2009094569A3 METHOD FOR THE ENZYMATIC KINETIC RESOLUTION OF ACYLOXYALKYL THIOCARBONATES USED FOR THE SYNTHESIS OF ACYLOXYALKYL CARBAMATES 审中-公开
标题翻译：用于合成氰乙酰氨基甲酸酯的乙酰氧基甲基丙烯酸酯的动力学分解方法
公开(公告)号：WO2009094569A3
公开(公告)日：2009-10-08
申请号：PCT/US2009031873
申请日：2009-01-23
申请人： XENOPORT INC , GALLOP MARK A , YAO FENMEI , LUDWIKOW MARIA J , PENG GE , RAILLARD STEVEN P
发明人： GALLOP MARK A , YAO FENMEI , LUDWIKOW MARIA J , PENG GE , RAILLARD STEVEN P
IPC分类号： C07B57/00 , C07C269/04 , C07C271/22 , C07C329/06 , C07D207/46 , C12P41/00
CPC分类号： C07C329/06 , A61K31/325 , C07B2200/07 , C07B2200/13 , C07C271/22 , C12P11/00 , C12P41/005
摘要： Methods of enzymatically resolving acyloxyalkyl thiocarbonates useful in the synthesis of acyloxyalkyl carbamates are disclosed. These carbamates can be coupled to drugs containing amines such as R-baclofen or S-pregabalin.
摘要翻译：公开了用于合成酰氧基烷基氨基甲酸酯的酶解分解酰氧基烷基硫代碳酸酯的方法。这些氨基甲酸酯可以与含有胺的药物例如R-巴氯芬或S-普瑞巴林结合。

2. 发明申请

WO2009094569A2 ENANTIOMERICALLY RESOLVING ACYLOXYALKYL THIOCARBONATES USED IN SYNTHESIZING ACYLOXYALKYL CARBAMATE PRODRUGS 审中-公开
标题翻译：用于合成炔丙基碳酸酯原料的全氟聚合甲基丙烯酸
公开(公告)号：WO2009094569A2
公开(公告)日：2009-07-30
申请号：PCT/US2009/031873
申请日：2009-01-23
申请人： XENOPORT, INC. , GALLOP, Mark A. , YAO, Fenmei , LUDWIKOW, Maria J. , PENG, Ge , RAILLARD, Steven P.
发明人： GALLOP, Mark A. , YAO, Fenmei , LUDWIKOW, Maria J. , PENG, Ge , RAILLARD, Steven P.
IPC分类号： C07B57/00 , C07C269/04 , C07C329/06 , C07D207/46 , C12P41/00 , C07C271/22
CPC分类号： C07C329/06 , A61K31/325 , C07B2200/07 , C07B2200/13 , C07C271/22 , C12P11/00 , C12P41/005
摘要： Methods of enzymatically resolving acyloxyalkyl thiocarbonates useful in the synthesis of acyloxyalkyl carbamate prodrugs are disclosed.
摘要翻译：公开了用于合成酰氨基烷基氨基甲酸酯前药的酶解分解酰氧基烷基硫代碳酸酯的方法。

3. 发明申请

WO2005019163A3 ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS OF SYNTHESIS AND USE 审中-公开
公开(公告)号：WO2005019163A3
公开(公告)日：2005-03-03
申请号：PCT/US2004/027330
申请日：2004-08-20
申请人： XENOPORT, INC. , GALLOP, Mark, A. , YAO, Fenmei , LUDWIKOW, Maria, J. , PHAN, Thu , PENG, Ge
发明人： GALLOP, Mark, A. , YAO, Fenmei , LUDWIKOW, Maria, J. , PHAN, Thu , PENG, Ge
IPC分类号： C07C271/22
摘要： The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±) 4 amino 3 (4 chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof , methods of making prodrugs of (±) 4 amino 3 (4 chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±) 4 amino 3 (4 chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±) 4 amino 3 (4 chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.

4. 发明申请

WO2010120370A2 GAMMA-AMINO-BUTYRIC ACID DERIVATIVES AS GABAB RECEPTOR LIGANDS 审中-公开
标题翻译： γ-氨基丁酸衍生物作为GABAB受体配体
公开(公告)号：WO2010120370A2
公开(公告)日：2010-10-21
申请号：PCT/US2010/001128
申请日：2010-04-16
申请人： XENOPORT, INC. , XU, Feng , GALLOP, Mark A. , PENG, Ge , PHAN, Thu , DILIP, Usha , WUSTROW, David J.
发明人： XU, Feng , GALLOP, Mark A. , PENG, Ge , PHAN, Thu , DILIP, Usha , WUSTROW, David J.
IPC分类号： C07C229/34
CPC分类号： C07C255/59 , C07C229/34 , C07C229/38 , C07C229/42 , C07C229/58 , C07C229/60 , C07C233/81 , C07C237/30 , C07C255/58 , C07C311/21 , C07C317/48 , C07D213/30 , C07D213/74 , C07D333/24 , C07D333/70 , C07F9/301 , C07F9/306 , C07F9/582
摘要： Gamma-amino-butyric acid derivatives that are GABA B receptor ligands, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives and pharmaceutical compositions thereof for treating diseases are disclosed.
摘要翻译：公开了作为GABA B受体配体的γ-氨基丁酸衍生物，包含该衍生物的药物组合物，以及使用这些衍生物的方法及其药物组合物治疗疾病。

5. 发明申请

WO2005066122A3 SYNTHESIS OF ACYLOXYALKYL CARBAMATE PRODRUGS AND INTERMEDIATES THEREOF 审中-公开
标题翻译：乙酰基亚氨基碳酸酯原料的合成及其中间体
公开(公告)号：WO2005066122A3
公开(公告)日：2005-10-13
申请号：PCT/US2004043823
申请日：2004-12-30
申请人： XENOPORT INC , GALLOP MARK A , DAI XUEDONG , SCHEUERMAN RANDALL A , RAILLARD STEPHEN P , MANTHATI SURESH K , YAO FENMEI , PHAN THU , LUDWIKOW MARIA , PENG GE , BHAT SEEMA
发明人： GALLOP MARK A , DAI XUEDONG , SCHEUERMAN RANDALL A , RAILLARD STEPHEN P , MANTHATI SURESH K , YAO FENMEI , PHAN THU , LUDWIKOW MARIA , PENG GE , BHAT SEEMA
IPC分类号： C07D207/404 , C07D207/416 , C07D207/46 , C07D207/40
CPC分类号： C07D207/46 , C07D207/404 , C07D207/416
摘要： Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
摘要翻译：描述了合成1-（酰氧基） - 烷基氨基甲酸酯的方法，特别是合成含有伯胺或仲胺的药物的1-（酰氧基） - 烷基氨基甲酸酯前药。还描述了合成1-（酰氧基） - 烷基N-羟基琥珀酰亚胺基碳酸酯的方法，其在合成1-（酰氧基） - 烷基氨基甲酸酯中是有用的中间体。

6. 发明申请

WO2005019163A2 ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS OF SYNTHESIS AND USE 审中-公开
标题翻译：酰氧基烷基氨基甲酸酯前体，合成方法和用途
公开(公告)号：WO2005019163A2
公开(公告)日：2005-03-03
申请号：PCT/US2004027330
申请日：2004-08-20
申请人： XENOPORT INC , GALLOP MARK A , YAO FENMEI , LUDWIKOW MARIA J , PHAN THU , PENG GE
发明人： GALLOP MARK A , YAO FENMEI , LUDWIKOW MARIA J , PHAN THU , PENG GE
IPC分类号： A61K31/195 , C07C271/22 , C07D207/40 , C07D207/416 , C07D213/79 , C07D213/80 , C07D307/30 , C07D333/38 , C07D401/04 , C07C271/00
CPC分类号： C07C269/06 , A61K31/27 , C07C271/22 , C07C2101/08 , C07C2101/14 , C07C2601/08 , C07C2601/14 , C07D213/79 , C07D307/30 , C07D307/68 , C07D333/32 , C07D333/38
摘要： The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±) 4 amino 3 (4 chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof , methods of making prodrugs of (±) 4 amino 3 (4 chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±) 4 amino 3 (4 chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±) 4 amino 3 (4 chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.
摘要翻译：本文公开内容一般涉及（±）4氨基-3-（4-氯苯基）丁酸的酰氧基烷基氨基甲酸酯前药及其类似物，其药物组合物，制备（±）4氨基-3-（4-氯苯基）丁酸的前体药物及其类似物的方法，使用（±）4氨基3（4-氯苯基）丁酸的前药和其类似物的方法及其药物组合物用于治疗或预防常见疾病和/或病症如痉挛状态和/或酸逆流疾病。本文的公开内容还涉及适用于口服给药的（±）4氨基-3-（4-氯苯基）丁酸的酰氧基烷基氨基甲酸酯前药及其类似物及其持续释放口服剂型。

7. 发明申请

WO2010120370A3 GAMMA-AMINO-BUTYRIC ACID DERIVATIVES AS GABAB RECEPTOR LIGANDS 审中-公开
标题翻译： γ-氨基丁酸衍生物作为GABAB受体配体
公开(公告)号：WO2010120370A3
公开(公告)日：2011-01-20
申请号：PCT/US2010001128
申请日：2010-04-16
申请人： XENOPORT INC , XU FENG , GALLOP MARK A , PENG GE , PHAN THU , DILIP USHA , WUSTROW DAVID J
发明人： XU FENG , GALLOP MARK A , PENG GE , PHAN THU , DILIP USHA , WUSTROW DAVID J
IPC分类号： C07C229/34 , A61K31/195 , A61K31/341 , A61K31/381 , A61K31/4164 , A61K31/4184 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/505 , A61K31/662 , A61P11/00 , A61P43/00 , C07C229/42 , C07C233/81 , C07C311/21 , C07D213/53 , C07D233/64 , C07D317/48 , C07F9/30
CPC分类号： C07C255/59 , C07C229/34 , C07C229/38 , C07C229/42 , C07C229/58 , C07C229/60 , C07C233/81 , C07C237/30 , C07C255/58 , C07C311/21 , C07C317/48 , C07D213/30 , C07D213/74 , C07D333/24 , C07D333/70 , C07F9/301 , C07F9/306 , C07F9/582
摘要： Gamma-amino-butyric acid derivatives of formula (I) that are GABAB receptor ligands, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives and pharmaceutical compositions thereof for treating diseases are disclosed. R5 is chosen from -COOH, -SOOH, and -P(O)(OH)R8 wherein R8 is chosen from hydrogen and C1-4 alkyl.
摘要翻译：公开了作为GABA B受体配体的式（I）的γ-氨基丁酸衍生物，包含该衍生物的药物组合物，以及使用该衍生物的方法及其药物组合物治疗疾病。 R 5选自-COOH，-SOOH和-P（O）（OH）R 8，其中R 8选自氢和C 1-4烷基。

8. 发明申请

WO2008033572A1 ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS OF SYNTHESIS AND USE 审中-公开
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：WO2008033572A1
公开(公告)日：2008-03-20
申请号：PCT/US2007/020210
申请日：2007-09-13
申请人： XENOPORT, INC. , GALLOP, Mark, A. , XU, Feng , PHAN, Thu , DILIP, Usha , PENG, Ge
发明人： GALLOP, Mark, A. , XU, Feng , PHAN, Thu , DILIP, Usha , PENG, Ge
IPC分类号： C07F9/30 , A61K31/662 , A61P25/00
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 of 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，制备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，使用3-氨基丙基次膦酸的酰氨基烷基氨基甲酸酯前药及其类似物，以及包含酰氨基烷基氨基甲酸酯前药的药物组合物的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，与阿尔茨海默病有关的认知障碍阿尔茨海默氏病，抑郁症，焦虑症和癫痫。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。

9. 发明申请

WO2005066122A2 SYNTHESIS OF ACYLOXYALKYL CARBAMATE PRODRUGS AND INTERMEDIATES THEREOF 审中-公开
标题翻译：氨基甲酸乙酯烷基酯的合成及其中间体的合成
公开(公告)号：WO2005066122A2
公开(公告)日：2005-07-21
申请号：PCT/US2004/043823
申请日：2004-12-30
申请人： XENOPORT, INC. , GALLOP, Mark A. , DAI, Xuedong , SCHEUERMAN, Randall A. , RAILLARD, Stephen P. , MANTHATI, Suresh K. , YAO, Fenmei , PHAN, Thu , LUDWIKOW, Maria , PENG, Ge , BHAT, Seema
发明人： GALLOP, Mark A. , DAI, Xuedong , SCHEUERMAN, Randall A. , RAILLARD, Stephen P. , MANTHATI, Suresh K. , YAO, Fenmei , PHAN, Thu , LUDWIKOW, Maria , PENG, Ge , BHAT, Seema
IPC分类号： C07D207/00
CPC分类号： C07D207/46 , C07D207/404 , C07D207/416
摘要： Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
摘要翻译：描述了合成1-（酰氧基） - 烷基氨基甲酸酯的方法，特别是含有伯胺或仲胺药物的1-（酰氧基） - 烷基氨基甲酸酯前药的合成。还描述了用于合成1-（酰氧基） - 烷基氨基甲酸酯的有用中间体的1-（酰氧基） - 烷基N-羟基琥珀酰亚胺基碳酸酯的合成方法也有描述。

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