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81. 发明申请

US20110009483A1 ACYLOXYALKYL CARBAMATE PRODRUGS OF TRANEXAMIC ACID, METHODS OF SYNTHESIS AND USE 有权
标题翻译： ACYLOXYALKYL CARBAMATE PRACRUGS OF TRANEXAMIC ACID，METHODS OF SYNTHESIS AND USE
公开(公告)号：US20110009483A1
公开(公告)日：2011-01-13
申请号：US12835663
申请日：2010-07-13
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： A61K31/27 , C07C271/22 , A61K8/44 , A61P17/02 , A61P17/16 , A61P17/00 , A61Q19/00 , A61P35/04 , A61P15/00 , A61P7/04
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。

82. 发明授权

US07727976B2 Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs 失效
标题翻译：用于增强口服吸收和药物全身生物利用度的胆汁酸衍生化合物
公开(公告)号：US07727976B2
公开(公告)日：2010-06-01
申请号：US11234310
申请日：2005-09-26
申请人： Laxminarayan Bhat , Mark A. Gallop , Bernd Jandeleit
发明人： Laxminarayan Bhat , Mark A. Gallop , Bernd Jandeleit
IPC分类号： A61K31/58 , C07J71/00
CPC分类号： C07J31/006 , C07J9/005 , C07J41/0055 , C07J53/002 , C07J71/0005 , C07J71/0047 , C07J71/0063
摘要： Disclosed are compounds that exhibit high transport across the intestinal wall of an animal. The compounds may optionally be linked to drugs that are poorly absorbed or poorly transported across the intestinal wall after oral administration to provide for enhanced therapeutic, and optionally prolonged therapeutic, systemic blood concentrations of the drugs upon oral administration of the drug-compound conjugate. Also disclosed are pharmaceutical compositions containing and methods of using such compounds.
摘要翻译：公开了表现出高度运输通过动物肠壁的化合物。所述化合物可任选地与口服给药后通过肠壁不良吸收或运输不良的药物连接，以提供药物 - 化合物缀合物口服后药物的增强的治疗和任选地延长的治疗性全身血液浓度。还公开了含有药物组合物和使用这些化合物的方法。

83. 发明授权

US07671089B2 Levodopa prodrugs, and compositions and uses thereof 失效
标题翻译：左旋多巴前药及其组合物和用途
公开(公告)号：US07671089B2
公开(公告)日：2010-03-02
申请号：US12001618
申请日：2007-12-11
申请人： Jia-Ning Xiang , Mark A. Gallop , Cindy X. Zhou , Mark Nguyen , Xuedong Dai , Jianhua Li , Kenneth C. Cundy , Nelson L. Jumbe
发明人： Jia-Ning Xiang , Mark A. Gallop , Cindy X. Zhou , Mark Nguyen , Xuedong Dai , Jianhua Li , Kenneth C. Cundy , Nelson L. Jumbe
IPC分类号： A61K31/24
CPC分类号： C07C229/36
摘要： Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.
摘要翻译：公开了左旋多巴的前药，制备左旋多巴的前药的方法，使用左旋多巴的前药的方法和左旋多巴的前药组合物。

84. 发明授权

US07662987B2 Methods for synthesis of acyloxyalkyl compounds 失效
标题翻译：酰氧基烷基化合物的合成方法
公开(公告)号：US07662987B2
公开(公告)日：2010-02-16
申请号：US10893130
申请日：2004-07-15
申请人： Laxminarayan Bhat , Mark A. Gallop
发明人： Laxminarayan Bhat , Mark A. Gallop
IPC分类号： C07C261/00 , C07C269/00 , C07C271/00
CPC分类号： C07C269/06 , C07C67/42 , C07C68/06 , C07C303/30 , C07C2601/14 , C07F9/091 , C07F9/094 , C07F9/4006 , C07F9/6552 , C07C69/76 , C07C69/612 , C07C69/732 , C07C69/92 , C07C69/738 , C07C69/72 , C07C309/75 , C07C271/22 , C07C69/96
摘要： Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
摘要翻译：本文公开了通过在无水反应条件下氧化药物的1-酰基 - 烷基衍生物来合成药物的1-（酰氧基） - 烷基前药衍生物的方法。所述方法通常以高产率立体特异地进行，不需要使用活化的中间体和/或有毒化合物，并且易于放大。

85. 发明授权

US07601706B2 Bile-acid conjugates providing for sustained systemic concentration of drugs 失效
标题翻译：提供药物持续全身浓缩的胆汁酸共轭物
公开(公告)号：US07601706B2
公开(公告)日：2009-10-13
申请号：US11388021
申请日：2006-03-24
申请人： Kenneth C. Cundy , Mark A. Gallop , Cindy X. Zhou
发明人： Kenneth C. Cundy , Mark A. Gallop , Cindy X. Zhou
IPC分类号： A61K31/56 , A61K31/58 , C07J17/00 , C07J43/00 , C07J9/00
CPC分类号： C07D233/64 , A61K38/00 , A61K47/554 , A61K47/64 , A61K47/65 , C07C237/12 , C07C237/20 , C07C323/60 , C07C2601/14 , C07D207/16 , C07K5/0205 , C07K5/06 , C07K5/08
摘要： This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.
摘要翻译：本发明涉及在给予动物后提供治疗性或预防性药物的持续全身浓度的化合物。本发明还涉及药物组合物，包括使用这些化合物的方法。

86. 发明授权

US07534813B2 Levodopa prodrugs, and compositions and uses thereof 有权
标题翻译：左旋多巴前药及其组合物和用途
公开(公告)号：US07534813B2
公开(公告)日：2009-05-19
申请号：US12008473
申请日：2008-01-10
申请人： Jia-Ning Xiang , Mark A. Gallop , Cindy X. Zhou , Mark Nguyen , Xuedong Dai , Jianhua Li , Kenneth C. Cundy , Nelson L. Jumbe
发明人： Jia-Ning Xiang , Mark A. Gallop , Cindy X. Zhou , Mark Nguyen , Xuedong Dai , Jianhua Li , Kenneth C. Cundy , Nelson L. Jumbe
IPC分类号： A01N47/10 , A61K31/27
CPC分类号： C07C235/60 , C07C229/34 , C07C229/36 , C07C235/48 , C07C2601/14 , C07D213/79 , C07D213/80 , C07D213/803
摘要： Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.
摘要翻译：公开了左旋多巴的前药，制备左旋多巴的前药的方法，使用左旋多巴的前药的方法和左旋多巴的前药组合物。

87. 发明授权

US07494985B2 Acyloxyalkyl carbamate prodrugs, methods of synthesis, and use 有权
标题翻译：甲氧基烷基氨基甲酸酯前药，合成方法和用途
公开(公告)号：US07494985B2
公开(公告)日：2009-02-24
申请号：US11265203
申请日：2005-11-03
申请人： Mark A. Gallop
发明人： Mark A. Gallop
IPC分类号： A61K31/66 , C07F9/02
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。

88. 发明申请

US20080132570A1 Levodopa prodrugs, and compositions and uses thereof 有权
标题翻译：左旋多巴前药及其组合物和用途
公开(公告)号：US20080132570A1
公开(公告)日：2008-06-05
申请号：US12008473
申请日：2008-01-10
申请人： Jia-Ning Xiang , Mark A. Gallop , Cindy X. Zhou
发明人： Jia-Ning Xiang , Mark A. Gallop , Cindy X. Zhou
IPC分类号： A61K31/216 , A61P25/00
CPC分类号： C07C235/60 , C07C229/34 , C07C229/36 , C07C235/48 , C07C2601/14 , C07D213/79 , C07D213/80 , C07D213/803
摘要： Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.
摘要翻译：公开了左旋多巴的前药，制备左旋多巴的前药的方法，使用左旋多巴的前药的方法和左旋多巴的前药组合物。

89. 发明授权

US07183259B2 Amino acid conjugates providing for sustained systemic concentrations of GABA analogues 失效
公开(公告)号：US07183259B2
公开(公告)日：2007-02-27
申请号：US10436100
申请日：2003-05-13
申请人： Randall A. Scheuerman , Mark A. Gallop , Kenneth C. Cundy , Ronald W. Barrett
发明人： Randall A. Scheuerman , Mark A. Gallop , Kenneth C. Cundy , Ronald W. Barrett
IPC分类号： A61K38/00
CPC分类号： C07K5/06 , A61K38/00 , A61K47/64 , C07C237/12 , C07C271/22 , C07C271/54 , C07K5/0215 , C07K5/06113
摘要： This invention is directed to compounds that provide for sustained systemic concentrations of GABA analogs following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

90. 发明授权

US06984634B2 Bile-acid conjugates for providing sustained systemic concentrations of drugs 失效
公开(公告)号：US06984634B2
公开(公告)日：2006-01-10
申请号：US09974768
申请日：2001-10-09
申请人： Kenneth C. Cundy , Mark A. Gallop
发明人： Kenneth C. Cundy , Mark A. Gallop
IPC分类号： A61K31/58 , A61K31/56 , C07J9/00 , C07J43/00
CPC分类号： C07D233/64 , A61K38/00 , A61K47/554 , A61K47/64 , A61K47/65 , C07C237/12 , C07C237/20 , C07C323/60 , C07C2601/14 , C07D207/16 , C07K5/0205 , C07K5/06 , C07K5/08
摘要： This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

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