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1. 发明授权

US08344028B2 Gamma-amino-butyric acid derivatives as GABAB receptor ligands 有权
标题翻译： γ-氨基丁酸衍生物作为GABA B受体配体
公开(公告)号：US08344028B2
公开(公告)日：2013-01-01
申请号：US12762152
申请日：2010-04-16
申请人： Feng Xu , Mark A. Gallop , Ge Peng , Thu Phan , Usha Dilip , David J. Wustrow
发明人： Feng Xu , Mark A. Gallop , Ge Peng , Thu Phan , Usha Dilip , David J. Wustrow
IPC分类号： A61K31/19 , A61K31/135 , A61K31/03 , C07C211/00 , C07C22/00
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 , C07F9/58
摘要： Gamma-amino-butyric acid derivatives 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.
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。

2. 发明申请

US20100267676A1 GAMMA-AMINO-BUTYRIC ACID DERIVATIVES AS GABAB RECEPTOR LIGANDS 有权
标题翻译： γ-氨基丁酸衍生物作为GABAB受体配体
公开(公告)号：US20100267676A1
公开(公告)日：2010-10-21
申请号：US12762152
申请日：2010-04-16
申请人： Feng Xu , Mark A. Gallop , Ge Peng , Thu Phan , Usha Dilip , David J. Wustrow
发明人： Feng Xu , Mark A. Gallop , Ge Peng , Thu Phan , Usha Dilip , David J. Wustrow
IPC分类号： A61K31/66 , C07C53/23 , A61K31/196 , A61K31/195 , C07D213/04 , A61K31/44 , C07D235/04 , A61K31/4184 , C07D333/40 , A61K31/381 , C07D239/24 , A61K31/505 , C07C255/60 , A61K31/277 , C07C63/70 , C07D307/38 , A61K31/341 , C07D277/02 , A61K31/426 , C07D263/02 , A61K31/421 , A61P1/04 , A61P11/00 , A61P13/10 , A61P25/00
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 , C07F9/58
摘要： Gamma-amino-butyric acid derivatives 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.
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。

3. 发明授权

US07803785B2 Gemcitabine prodrugs, pharmaceutical compositions and uses thereof 失效
标题翻译：吉西他滨前药，药物组合物及其用途
公开(公告)号：US07803785B2
公开(公告)日：2010-09-28
申请号：US12556458
申请日：2009-09-09
申请人： Mark A. Gallop , Ge Peng , Thomas F. Woiwode , Kenneth C. Cundy
发明人： Mark A. Gallop , Ge Peng , Thomas F. Woiwode , Kenneth C. Cundy
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： C07H19/06
摘要： The present invention provides gemcitabine prodrugs, methods of making gemcitabine prodrugs, pharmaceutical compositions of gemcitabine prodrugs and methods of using gemcitabine prodrugs and pharmaceutical compositions of using gemcitabine prodrugs to treat or prevent diseases or disorders such as cancer or viral infections.
摘要翻译：本发明提供吉西他滨前药，制备吉西他滨前药的方法，吉西他滨前药的药物组合物和使用吉西他滨前药的方法以及使用吉西他滨前药治疗或预防疾病或病症如癌症或病毒感染的药物组合物。

4. 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。

5. 发明申请

US20090216037A1 Synthesis of Acyloxyalkyl Carbamate Prodrugs and Intermediates Thereof 有权
标题翻译：氨基甲酰氨基磺酸前体药物及其中间体的合成
公开(公告)号：US20090216037A1
公开(公告)日：2009-08-27
申请号：US12390000
申请日：2009-02-20
申请人： Mark A. Gallop , Xuedong Dai , Randall A. Scheuerman , Stephen P. Raillard , Suresh K. Manthati , Fenmei Yao , Thu Phan , Maria J. Ludwikow , Ge Peng , Seema Bhat
发明人： Mark A. Gallop , Xuedong Dai , Randall A. Scheuerman , Stephen P. Raillard , Suresh K. Manthati , Fenmei Yao , Thu Phan , Maria J. Ludwikow , Ge Peng , Seema Bhat
IPC分类号： C07C329/06 , C07C271/22
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

US20080146526A1 Acyloxyalkyl carbamate prodrugs, methods of synthesis and use 失效
标题翻译：氨基甲酸氨基甲酸烷基酯前药，合成和使用方法
公开(公告)号：US20080146526A1
公开(公告)日：2008-06-19
申请号：US11901194
申请日：2007-09-13
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 , 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 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。

7. 发明授权

US07300956B2 Acyloxyalkyl carbamate prodrugs, methods of synthesis and use 有权
标题翻译：氨基甲酸氨基甲酸烷基酯前药，合成和使用方法
公开(公告)号：US07300956B2
公开(公告)日：2007-11-27
申请号：US11508131
申请日：2006-08-21
申请人： Mark A. Gallop , Fenmei Yao , Maria J. Ludwikow , Thu Phan , Ge Peng
发明人： Mark A. Gallop , Fenmei Yao , Maria J. Ludwikow , Thu Phan , Ge Peng
IPC分类号： A61K31/24 , C07D401/04 , C07D207/00 , C07D333/36 , C07D307/02 , C07D271/00
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：本文的公开内容通常涉及（±）-4-氨基-3-（4-氯苯基）丁酸及其类似物的氨基氧基烷基氨基甲酸酯前药，其药物组合物，制备（±）-4-氨基-3- （4-氯苯基）丁酸及其类似物，使用（±）-4-氨基-3-（4-氯苯基）丁酸及其类似物的前药的方法及其药物组合物，用于治疗或预防常见疾病和/或疾病如痉挛和/或酸反流疾病。本文的公开内容还涉及适于口服给药的（±）-4-氨基-3-（4-氯苯基）丁酸及其类似物的氨氧基烷基氨基甲酸酯前药及其缓释口服剂型。

8. 发明申请

US20070037988A9 Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 有权
标题翻译：酰氨基烷基氨基甲酸酯前药及其中间体的合成
公开(公告)号：US20070037988A9
公开(公告)日：2007-02-15
申请号：US11026491
申请日：2004-12-30
申请人： Mark Gallop , Xuedong Dai , Randall Scheuerman , Stephen Raillard , Suresh Manthati , Fenmei Yao , Thu Phan , Maria Ludwikow , Ge Peng , Seema Bhat
发明人： Mark Gallop , Xuedong Dai , Randall Scheuerman , Stephen Raillard , Suresh Manthati , Fenmei Yao , Thu Phan , Maria Ludwikow , Ge Peng , Seema Bhat
IPC分类号： 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。还描述了合成合成1-（酰氧基） - 烷基氨基甲酸酯的有用的中间体的1-（酰氧基） - 烷基N-羟基琥珀酰亚胺基碳酸酯的合成方法。

9. 发明授权

US07109239B2 Acyloxyalkyl carbamate prodrugs, methods of synthesis and use 有权
公开(公告)号：US07109239B2
公开(公告)日：2006-09-19
申请号：US10932374
申请日：2004-08-20
申请人： Mark A. Gallop , Fenmei Yao , Maria J. Ludwikow , Thu Phan , Ge Peng
发明人： Mark A. Gallop , Fenmei Yao , Maria J. Ludwikow , Thu Phan , Ge Peng
IPC分类号： A61K31/235 , 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.

10. 发明授权

US08378137B2 Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 有权
公开(公告)号：US08378137B2
公开(公告)日：2013-02-19
申请号：US13208176
申请日：2011-08-11
申请人： Mark A. Gallop , Xuedong Dai , Randall A. Scheuerman , Stephen P. Raillard , Suresh K. Manthati , Fenmei Yao , Thu Phan , Maria Ludwikow , Ge Peng , Seema Bhat
发明人： Mark A. Gallop , Xuedong Dai , Randall A. Scheuerman , Stephen P. Raillard , Suresh K. Manthati , Fenmei Yao , Thu Phan , Maria Ludwikow , Ge Peng , Seema Bhat
IPC分类号： C07C271/22 , C07C269/00 , C07D207/46
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.

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