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1. 发明申请

WO2005021024A1 AMINO ACID DERIVED PRODRUGS OF PROPOFOL, COMPOSITIONS AND USES THEREOF 审中-公开
标题翻译：丙氨酸氨基酸衍生物，其组合物及其用途
公开(公告)号：WO2005021024A1
公开(公告)日：2005-03-10
申请号：PCT/US2004/002537
申请日：2004-01-28
申请人： XENOPORT, INC. , GALLOP, Mark, A. , XU, Feng , CUNDY, Kenneth, C. , SASIKUMAR, Vivek , WOIWODE, Thomas, W.
发明人： GALLOP, Mark, A. , XU, Feng , CUNDY, Kenneth, C. , SASIKUMAR, Vivek , WOIWODE, Thomas, W.
IPC分类号： A61K38/00
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，制备丙泊酚前药的方法，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障碍，例如偏头痛头痛和化疗后或术后手术恶心和呕吐。

2. 发明申请

WO2004052841A1 CARBIDOPA PRODRUGS AND USES THEREOF 审中-公开
标题翻译： CARBIDOPA PRODRUGS及其用途
公开(公告)号：WO2004052841A1
公开(公告)日：2004-06-24
申请号：PCT/US2003/038742
申请日：2003-12-08
申请人： XENOPORT, INC. , XIANG, Jia-Ning , GALLOP, Mark, A. , CUNDY, Kenneth, C. , LI, Jianhua , XU, Feng , ZHOU, Cindy, X. , BHAT, Laxminarayan
发明人： XIANG, Jia-Ning , GALLOP, Mark, A. , CUNDY, Kenneth, C. , LI, Jianhua , XU, Feng , ZHOU, Cindy, X. , BHAT, Laxminarayan
IPC分类号： C07C243/18
CPC分类号： C07D213/30 , C07C243/18 , C07C281/02 , C07D295/088 , C07D307/89
摘要： Prodrugs of carbidopa, derivatives of carbidopa prodrugs, methods of making prodrugs of carbidopa and derivatives thereof, methods of using prodrugs of carbidopa and derivatives thereof, and compositions of prodrugs of carbidopa and derivatives thereof are disclosed.
摘要翻译：卡比多巴的前药，卡比多前药的衍生物，卡比多巴的前药及其衍生物的制备方法，使用卡比多巴的前药及其衍生物的方法，以及卡比多巴及其衍生物的前药组合物。

3. 发明申请

WO2005023204A2 AROMATIC PRODRUGS OF PROPOFOL, COMPOSITIONS AND USES THEREOF 审中-公开
标题翻译：丙泊酚的组合物及其用途
公开(公告)号：WO2005023204A2
公开(公告)日：2005-03-17
申请号：PCT/US2004/030999
申请日：2004-09-09
申请人： XENOPORT, INC. , GALLOP, Mark, A. , XU, Feng
发明人： GALLOP, Mark, A. , XU, Feng
IPC分类号： A61K
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障碍，如偏头痛头痛和化疗后或术后手术恶心和呕吐。

4. 发明申请

WO2006017351A1 PRODRUGS OF PROPOFOL, COMPOSITIONS AND USES THEREOF 审中-公开
标题翻译：丙泊酚的原料，组合物及其用途
公开(公告)号：WO2006017351A1
公开(公告)日：2006-02-16
申请号：PCT/US2005/024907
申请日：2005-07-12
申请人： XENOPORT, INC. , XU, Feng , GALLOP, Mark, A.
发明人： XU, Feng , GALLOP, Mark, A.
IPC分类号： C07C237/02
CPC分类号： C07C229/22 , C07C237/02 , C07C237/06 , C07C237/08 , C07C237/12 , C07C237/20 , C07C271/52 , C07C2601/14 , C07D207/16 , C07D209/20
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，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，用于治疗或预防疾病或障碍，如偏头痛头痛和化疗后或术后手术恶心呕吐。

5. 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。

6. 发明申请

WO2006091790A1 PLATINUM-CONTAINING COMPOUNDS EXHIBITING CYTOSTATIC ACTIVITY, SYNTHESIS AND METHODS OF USE 审中-公开
标题翻译：含铂化合物展示细胞活性，合成和使用方法
公开(公告)号：WO2006091790A1
公开(公告)日：2006-08-31
申请号：PCT/US2006/006551
申请日：2006-02-23
申请人： XENOPORT, INC. , GAO, Qingzhi , GALLOP, Mark, A. , XIANG, Jia-ning
发明人： GAO, Qingzhi , GALLOP, Mark, A. , XIANG, Jia-ning
IPC分类号： A61K31/282
CPC分类号： C07H23/00 , C07F15/0093
摘要： Platinum containing compounds exhibiting cytostatic activity, methods of synthesizing platinum-containing compounds exhibiting cytostatic activity pharmaceutical compositions comprising platinum containing compounds, and methods of using such compounds and compositions for treating cancer are disclosed.
摘要翻译：公开了含有显示细胞抑制活性的含铂化合物，显示出细胞抑制活性的含铂化合物的方法，包含含铂化合物的药物组合物，以及使用这些化合物和组合物治疗癌症的方法。

7. 发明申请

WO2003099338A3 AMINO ACID CONJUGATES PROVIDING FOR SUSTAINED SYSTEMIC CONCENTRATIONS OF GABA ANALOGUES 审中-公开
公开(公告)号：WO2003099338A3
公开(公告)日：2003-12-04
申请号：PCT/US2003/013404
申请日：2003-05-13
申请人： XENOPORT, INC. , SCHEUERMAN, Randall, A. , GALLOP, Mark, A. , CUNDY, Kenneth, C. , BARRETT, Ronald, W.
发明人： SCHEUERMAN, Randall, A. , GALLOP, Mark, A. , CUNDY, Kenneth, C. , BARRETT, Ronald, W.
IPC分类号： A61K47/48
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.

8. 发明申请

WO2011150380A1 METHODS OF TREATMENT OF FRAGILE X SYNDROME, DOWN'S SYNDROME, AUTISM AND RELATED DISORDERS 审中-公开
标题翻译：治疗脆性X综合征，下行综合征，异常及相关疾病的方法
公开(公告)号：WO2011150380A1
公开(公告)日：2011-12-01
申请号：PCT/US2011/038422
申请日：2011-05-27
申请人： XENOPORT, INC. , JANDELEIT, Bernd , GALLOP, Mark, A. , VIRSIK, Peter, A. , WUSTROW, David, J.
发明人： JANDELEIT, Bernd , GALLOP, Mark, A. , VIRSIK, Peter, A. , WUSTROW, David, J.
IPC分类号： A61K31/00 , A61K31/255 , A61K31/661
CPC分类号： A61K31/255 , A61K45/06 , A61K2300/00
摘要： Disclosed herein are methods of treating fragile X syndrome, fragile X-associated tremor/ataxia syndrome, Down's syndrome and/or autism, comprising administering a prodrug of acamprosate to a subject suffering therefrom, wherein, in certain embodiments, the acamprosate prodrugs comprise compounds of Formula (I).
摘要翻译：本文公开了治疗脆性X综合征，脆性X相关性震颤/共济失调综合征，唐氏综合征和/或自闭症的方法，包括向患有其的受试者施用阿坎酸的前药，其中在某些实施方案中，阿坎酸酯前药包含式（I）。

9. 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.

10. 发明申请

WO2003020214A3 BILE-ACID DERIVED COMPOUNDS FOR ENHANCING ORAL ABSORPTION AND SYSTEMIC BIOAVAILABILITY OF DRUGS 审中-公开
公开(公告)号：WO2003020214A3
公开(公告)日：2003-03-13
申请号：PCT/US2002/027458
申请日：2002-08-29
申请人： XENOPORT, INC. , BHAT, Laxminarayan , GALLOP, Mark, A. , JANDELEIT, Bernd
发明人： BHAT, Laxminarayan , GALLOP, Mark, A. , JANDELEIT, Bernd
IPC分类号： C07J9/00
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.

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