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91. 发明申请

US20100041882A1 METHODS FOR SYNTHESIS OF ACYLOXYALKYL COMPOUNDS 有权
标题翻译：合成聚乙烯醇化合物的方法
公开(公告)号：US20100041882A1
公开(公告)日：2010-02-18
申请号：US12538480
申请日：2009-08-10
申请人： Laxminarayan Bhat , Mark A. Gallop
发明人： Laxminarayan Bhat , Mark A. Gallop
IPC分类号： C07D265/30 , 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。

92. 发明申请

US20100016254A1 GEMCITABINE PRODRUGS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF 失效
标题翻译：化学药物制剂，药物组合物及其用途
公开(公告)号：US20100016254A1
公开(公告)日：2010-01-21
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： A61K31/7068 , C07H19/06 , A61P35/00
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和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。

93. 发明申请

US20090286763A1 AMINO ACID DERIVED PRODRUGS OF PROPOFOL, COMPOSITIONS AND USES THEREOF 审中-公开
标题翻译：丙烯酸的氨基酸衍生物，组合物及其用途
公开(公告)号：US20090286763A1
公开(公告)日：2009-11-19
申请号：US12467758
申请日：2009-05-18
申请人： Feng Xu , Mark A. Gallop , Vivek Sasikumar
发明人： Feng Xu , Mark A. Gallop , Vivek Sasikumar
IPC分类号： A61K31/56 , A61K31/265 , C07C69/96
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.
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。

94. 发明授权

US07598235B2 Bile-acid conjugates for providing sustained systemic concentrations of drugs 失效
公开(公告)号：US07598235B2
公开(公告)日：2009-10-06
申请号：US11218468
申请日：2005-09-06
申请人： Kenneth C. Cundy , Mark A. Gallop
发明人： Kenneth C. Cundy , Mark A. Gallop
IPC分类号： A61K31/56 , 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.

95. 发明申请

US20090234138A1 ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS 审中-公开
标题翻译： ACYLOXYALKYL CARBAMATE PRODRUGS，方法
公开(公告)号：US20090234138A1
公开(公告)日：2009-09-17
申请号：US12473112
申请日：2009-05-27
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： C07D207/12 , C07C271/22
CPC分类号： C07C269/06 , A61K31/27 , C07C271/22 , 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。

96. 发明申请

US20090215809A1 CRYSTALLINE FORM OF A (3S)-AMINOMETHYL-5-METHYL-HEXANOIC ACID PRODRUG AND METHODS OF USE 有权
标题翻译：（3S） - 氨基甲酰基-5-甲基 - 十六烷酸的制备方法及其使用方法
公开(公告)号：US20090215809A1
公开(公告)日：2009-08-27
申请号：US12358454
申请日：2009-01-23
申请人： Fenmei Yao , Mark A. Gallop , Ronald W. Barrett , Peter A. Virsik
发明人： Fenmei Yao , Mark A. Gallop , Ronald W. Barrett , Peter A. Virsik
IPC分类号： A61K31/197 , C07C229/04 , A61P29/00 , A61K31/439 , A61P1/00 , A61P25/28 , A61P25/22 , A61P25/18 , A61P9/00 , A61P13/00 , A61P19/00 , A61P15/12 , A61P25/06 , A61P25/32 , A61P37/00
CPC分类号： C07C271/22 , A61K31/325 , C07B2200/07 , C07B2200/13 , C07C329/06 , C12P11/00 , C12P41/005
摘要： A crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug and methods of preparing a crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug, and methods of using a crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug are provided.
摘要翻译：（3S） - 氨基甲基-5-己酸前药的结晶形式和（3S） - 氨基甲基-5-己酸前药的结晶形式的制备方法，以及使用（3S） - 提供氨基甲基-5-己酸前药。

97. 发明授权

US07576127B2 Aromatic prodrugs of propofol, compositions and uses thereof 失效
标题翻译：丙泊酚的芳族前药，其组合物和用途
公开(公告)号：US07576127B2
公开(公告)日：2009-08-18
申请号：US11507968
申请日：2006-08-21
申请人： Mark A. Gallop , Feng Xu
发明人： Mark A. Gallop , Feng Xu
IPC分类号： A61K31/265 , A61K31/235
CPC分类号： C07C271/28
摘要： Prodrugs of propofol, methods of making prodrugs of propofol, pharmaceutical compositions of prodrugs of propofol and methods of using prodrugs of propofol 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 are disclosed herein.
摘要翻译：丙泊酚的前药，制备丙泊酚前药的方法，丙泊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。

98. 发明授权

US07566738B2 Acyloxyalkyl carbamate prodrugs of sulfinic acids, methods of synthesis, and use 失效
标题翻译：亚磺酸氨基甲酸氨基甲酸酯前药，合成和使用方法
公开(公告)号：US07566738B2
公开(公告)日：2009-07-28
申请号：US11265204
申请日：2005-11-03
申请人： Mark A. Gallop
发明人： Mark A. Gallop
IPC分类号： A61K31/325 , C07C313/10
CPC分类号： C07C313/04 , C07C2601/14
摘要： Acyloxyalkyl carbamate prodrugs of 3-aminopropylsulfinic acid and analogs thereof, pharmaceutical compositions of 3-aminopropylsulfinic acid and analogs thereof, methods of making prodrugs of 3-aminopropylsulfinic acid and analogs thereof, methods of using prodrugs of 3-aminopropylsulfinic 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-aminopropylsulfinic 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-氨基丙基亚磺酸的氨基甲酸烷基酯氨基甲酸酯前药及其类似物，3-氨基丙基亚磺酸及其类似物的药物组合物，制备3-氨基丙基亚磺酸的前药的方法及其类似物，使用3-氨基丙基亚磺酸的前药及其类似物的方法和公开了用于治疗或预防诸如痉挛或胃食管反流病等疾病或病症的药物组合物。还公开了适用于口服给药的3-氨基丙基亚磺酸及其类似物的氨基氧基烷基氨基甲酸酯前药和缓释口服剂型。

99. 发明授权

US07550506B2 Amino acid derived prodrugs of propofol, compositions and uses thereof 失效
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：US07550506B2
公开(公告)日：2009-06-23
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： A61K31/24 , C07C229/36
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.
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。

100. 发明申请

US20090099253A1 Internally Masked Neopentyl Sulfonyl Ester Cyclization Release Prodrugs of Acamprosate, Compositions Thereof, and Methods of Use 审中-公开
标题翻译：内在掩蔽的新戊基磺酰酯环化释放Acamprosate，其组成及其使用方法
公开(公告)号：US20090099253A1
公开(公告)日：2009-04-16
申请号：US12252167
申请日：2008-10-15
申请人： Yunxiao Li , Bernd Jandeleit , Mark A. Gallop , Noa Zerangue , Peter A. Virsik , Wolf-Nicolas Fischer
发明人： Yunxiao Li , Bernd Jandeleit , Mark A. Gallop , Noa Zerangue , Peter A. Virsik , Wolf-Nicolas Fischer
IPC分类号： A61K31/35 , C07C233/00 , A61K31/16 , C07D309/00
CPC分类号： C07D311/76 , C07D307/33 , C07D307/88 , C07D309/30 , C07D317/32 , C07D317/36 , C07D333/64
摘要： Internally masked neopentyl sulfonyl ester prodrugs of acamprosate, pharmaceutical compositions comprising such prodrugs, and methods of using such prodrugs and compositions thereof for treating diseases are disclosed. In particular, acamprosate prodrugs exhibiting enhanced oral bioavailability and methods of using acamprosate prodrugs to treat neurodegenerative disorders, psychotic disorders, mood disorders, anxiety disorders, somatoform disorders, movement disorders, substance abuse disorders, binge eating disorder, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis, and pain are disclosed.
摘要翻译：本发明公开了含有阿坎酸盐的内部掩蔽的新戊基磺酰基酯前体药物，包含这些前药的药物组合物，以及使用这些前药及其组合物治疗疾病的方法。特别地，表现出增强的口服生物利用度的阿坎酸酯前药和使用阿坎酸类前药治疗神经变性疾病，精神病性障碍，情绪障碍，焦虑症，躯体形式障碍，运动障碍，物质滥用障碍，暴饮暴食症，皮质扩张抑郁症相关疾病，耳鸣的方法，睡眠障碍，多发性硬化和疼痛。

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