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71. 发明授权

US07511158B2 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：US07511158B2
公开(公告)日：2009-03-31
申请号：US11754232
申请日：2007-05-25
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： 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.
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。

72. 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。

73. 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。

74. 发明授权

US07220875B2 Amino acid derived prodrugs of propofol, compositions and uses thereof 有权
标题翻译：丙泊酚的氨基酸衍生前药，其组合物和用途
公开(公告)号：US07220875B2
公开(公告)日：2007-05-22
申请号：US10766990
申请日：2004-01-28
申请人： Mark A. Gallop , Feng Xu , Kenneth C. Cundy , Vivek Susikumar , Thomas W. Woiwode
发明人： Mark A. Gallop , Feng Xu , Kenneth C. Cundy , Vivek Susikumar , Thomas W. Woiwode
IPC分类号： C07C229/00 , A61K31/385
CPC分类号： C07C229/24 , A61K47/64 , C07C229/08 , C07C237/12 , C07C329/06
摘要： The present invention provides propofol prodrugs, methods of making propofol prodrugs, pharmaceutical compositions of propofol prodrugs and methods of using propofol prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting.
摘要翻译：本发明提供丙泊酚前药，制备异丙酚前药的方法，异丙酚前药的药物组合物和使用异丙酚前药的方法及其药物组合物，用于治疗或预防疾病或病症如偏头痛头痛和化疗后或术后手术恶心和呕吐。

75. 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.

76. 发明申请

US20060100160A1 Amino acid derived prodrugs of propofol, compositions and uses thereof 失效
公开(公告)号：US20060100160A1
公开(公告)日：2006-05-11
申请号：US11180064
申请日：2005-07-12
申请人： Feng Xu , Mark A. Gallop , Vivek Sasikumar
发明人： Feng Xu , Mark A. Gallop , Vivek Sasikumar
IPC分类号： A61K38/04 , C07K5/04
CPC分类号： C07C323/60 , A61K38/00 , C07C229/22 , C07C237/12 , C07C237/20 , C07D233/64 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06069 , C07K5/06086 , C07K5/06095 , C07K5/06113 , C07K5/06147 , C07K5/06165
摘要： The present invention provides propofol prodrugs, methods of making propofol prodrugs, pharmaceutical compositions of propofol prodrugs and methods of using propofol prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting.

77. 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.

78. 发明授权

US5846839A Methods for hard-tagging an encoded synthetic library 失效
公开(公告)号：US5846839A
公开(公告)日：1998-12-08
申请号：US577203
申请日：1995-12-22
申请人： Mark A. Gallop , Eric Gordon , Zhi-Jie Ni , Derek MacLean , Christopher Holmes , William Fitch , Nikhil Shah
发明人： Mark A. Gallop , Eric Gordon , Zhi-Jie Ni , Derek MacLean , Christopher Holmes , William Fitch , Nikhil Shah
IPC分类号： C40B70/00 , G01N33/543 , G01N33/545 , G01N33/68 , G01N33/44 , G01N33/53
CPC分类号： G01N33/545 , G01N33/54306 , G01N33/68 , B01J2219/00572 , C40B70/00
摘要： Disclosed are chemical encryption methods for determining the structure of compounds formed in situ on solid supports by the use of specific amines tags which, after compound synthesis, can be deencrypted to provide the structure of the compound found on the support.

79. 发明授权

US5708153A Method of synthesizing diverse collections of tagged compounds 失效
标题翻译：合成多种标签化合物集合的方法
公开(公告)号：US5708153A
公开(公告)日：1998-01-13
申请号：US488470
申请日：1995-06-07
申请人： William J. Dower , Ronald W. Barrett , Mark A. Gallop
发明人： William J. Dower , Ronald W. Barrett , Mark A. Gallop
IPC分类号： C12N15/09 , B01J19/00 , C07B61/00 , C07H19/10 , C07H19/14 , C07H21/00 , C07H21/02 , C07H21/04 , C07K1/04 , C07K1/06 , C07K5/00 , C07K7/00 , C08F8/00 , C08G85/00 , C40B40/06 , C40B40/10 , C40B40/12 , C40B60/14 , C40B70/00 , C12Q1/00 , C07H19/00 , C07K1/00 , C12M1/34
CPC分类号： C07K1/047 , B01J19/0046 , B01J19/0093 , C07H19/10 , C07H19/14 , C07H21/00 , B01J2219/00306 , B01J2219/00313 , B01J2219/00459 , B01J2219/00466 , B01J2219/005 , B01J2219/00502 , B01J2219/00536 , B01J2219/00542 , B01J2219/00545 , B01J2219/00547 , B01J2219/00554 , B01J2219/00563 , B01J2219/00565 , B01J2219/00572 , B01J2219/00574 , B01J2219/00576 , B01J2219/00585 , B01J2219/0059 , B01J2219/00592 , B01J2219/00596 , B01J2219/00689 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , B01J2219/00731 , C07B2200/11 , C40B40/06 , C40B40/10 , C40B40/12 , C40B60/14 , C40B70/00 , Y10S435/81 , Y10T436/143333
摘要： A general stochastic method for synthesizing random oligomers on particles is disclosed. A further aspect of the invention relates to the use of identification tags on the particles to facilitate identification of the sequence of the monomers in the oligomer.
摘要翻译：公开了用于在颗粒上合成无规低聚物的通用随机方法。本发明的另一方面涉及在颗粒上使用识别标签以便于鉴定寡聚体中单体的序列。

80. 发明授权

US5525735A Methods for synthesizing diverse collections of pyrrolidine compounds 失效
标题翻译：合成各种吡咯烷化合物的方法
公开(公告)号：US5525735A
公开(公告)日：1996-06-11
申请号：US354309
申请日：1994-12-12
申请人： Mark A. Gallop , Martin A. Murphy
发明人： Mark A. Gallop , Martin A. Murphy
IPC分类号： C07D207/16 , C07D207/00 , C07D209/00
CPC分类号： C07D207/16 , B01J2219/00592 , B01J2219/0072
摘要： Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds and derivatives thereof on solid supports and synthetic compound libraries comprising pyrrolidine groups and derivatives thereof prepared by such methods.
摘要翻译：公开了用于在固体支持物上合成非常大量的各种吡咯烷化合物及其衍生物的方法，其包含通过这些方法制备的吡咯烷基团及其衍生物的合成化合物文库。

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