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1.发明申请METHODS OF TREATMENT OF FRAGILE X SYNDROME, DOWN'S SYNDROME, AUTISM AND RELATED DISORDERS 审中-公开治疗脆性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
Applicant: XENOPORT, INC. , JANDELEIT, Bernd , GALLOP, Mark, A. , VIRSIK, Peter, A. , WUSTROW, David, J.
Inventor： JANDELEIT, Bernd , GALLOP, Mark, A. , VIRSIK, Peter, A. , WUSTROW, David, J.
IPC: A61K31/00 , A61K31/255 , A61K31/661
CPC classification number: A61K31/255 , A61K45/06 , A61K2300/00
Abstract: 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).
Abstract translation: 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）。
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2.发明申请
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
Applicant: XENOPORT, INC. , BHAT, Laxminarayan , GALLOP, Mark, A. , JANDELEIT, Bernd
Inventor： BHAT, Laxminarayan , GALLOP, Mark, A. , JANDELEIT, Bernd
IPC: C07J9/00
Abstract: 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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3.发明申请SIMPLE PANTOIC ACID ESTER NEOPENTYL SULFONYL ESTER CYCLIZATION RELEASE PRODRUGS OF ACAMPROSATE, COMPOSITIONS THEREOF, AND METHODS OF USE 审中-公开简单的苹果酸酯NEOPYYL SULFONYL ESTER循环释放ACAMPROSATE的产品，其组合物及其使用方法
公开(公告)号：WO2009033069A1
公开(公告)日：2009-03-12
申请号：PCT/US2008/075462
申请日：2008-09-05
Applicant: XENOPORT, INC. , JANDELEIT, Bernd , LI, Yunxiao , GALLOP, Mark A. , ZERANGUE, Noa , VIRSIK, Peter A. , FISCHER, Wolf-nicolas
Inventor： JANDELEIT, Bernd , LI, Yunxiao , GALLOP, Mark A. , ZERANGUE, Noa , VIRSIK, Peter A. , FISCHER, Wolf-nicolas
IPC: C07C309/15 , C07D295/088 , C07D213/30 , A61K31/255 , A61K31/4406 , A61K31/5377 , A61P25/00
CPC classification number: C07C309/15
Abstract: Pantoic acid ester neopentyl sulfonyl ester prodrugs of acamprosate of formula (I), 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 disorders, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis and pain are disclosed.
Abstract translation: 公开了式（I）的阿卡波酸，包含这些前药的药物组合物的泛酸酯新戊基磺酰酯前药，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酯前药治疗神经变性疾病，精神障碍，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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4.发明申请ACYLOXYALKYL CARBAMATE PRODRUGS OF TRANEXAMIC ACID, METHODS OF SYNTHESIS AND USE 审中-公开ACYLOXYALKYL CARBAMATE PRACRUGS OF TRANEXAMIC ACID，METHODS OF SYNTHESIS AND USE
公开(公告)号：WO2007002013A2
公开(公告)日：2007-01-04
申请号：PCT/US2006/023873
申请日：2006-06-20
Applicant: XENOPORT, INC. , JANDELEIT, Bernd , LI, Yunxiao , ZERANGUE, Noa , GALLOP, Mark, A.
Inventor： JANDELEIT, Bernd , LI, Yunxiao , ZERANGUE, Noa , GALLOP, Mark, A.
IPC: C07C271/22
CPC classification number: C07C271/22 , C07B2200/07 , C07C2601/14
Abstract: 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.
Abstract translation: 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，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） - 环己烷羧酸的氨基氧基烷基氨基甲酸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的给药的药物组合物。
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5.发明申请INTERNALLY MASKED NEOPENTYL SULFONYL ESTER CYCLIZATION RELEASE PRODRUGS OF ACAMPROSATE, COMPOSITIONS THEREOF, AND METHODS OF USE 审中-公开内部封闭的NEOPYYL SULFONYL ESTER循环释放ACAMPROSATE的产品，其组合物及其使用方法
公开(公告)号：WO2009052191A1
公开(公告)日：2009-04-23
申请号：PCT/US2008/080009
申请日：2008-10-15
Applicant: XENOPORT, INC. , LI, Yunxiao , JANDELEIT, Bernd , GALLOP, Mark A. , ZERANGUE, Noa , VIRSIK, Peter A. , FISCHER, Wolf-nicolas
Inventor： LI, Yunxiao , JANDELEIT, Bernd , GALLOP, Mark A. , ZERANGUE, Noa , VIRSIK, Peter A. , FISCHER, Wolf-nicolas
IPC: C07D307/33 , C07D307/88 , C07D309/30 , C07D311/76 , C07D317/32 , C07D317/36 , C07D333/64 , A61P25/00 , A61K31/335 , A61K31/381
CPC classification number: C07D311/76 , C07D307/33 , C07D307/88 , C07D309/30 , C07D317/32 , C07D317/36 , C07D333/64
Abstract: 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.
Abstract translation: 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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Patent Agency Ranking6.发明申请EXTERNALLY MASKED NEOPENTYL SULFONYL ESTER CYCLIZATION RELEASE PRODRUGS OF ACAMPROSATE, COMPOSITIONS THEREOF, AND METHODS OF USE 审中-公开外用苯丙醇磺酸酯环化酶释放丙酸钠，其组合物及其使用方法
公开(公告)号：WO2009033079A1
公开(公告)日：2009-03-12
申请号：PCT/US2008/075472
申请日：2008-09-05
Applicant: XENOPORT, INC. , JANDELEIT, Bernd , LI, Yunxiao , GALLOP, Mark A. , ZERANGUE, Noa , VIRSIK, Peter A. , FISCHER, Wolf-nicolas
Inventor： JANDELEIT, Bernd , LI, Yunxiao , GALLOP, Mark A. , ZERANGUE, Noa , VIRSIK, Peter A. , FISCHER, Wolf-nicolas
IPC: C07C309/15 , A61K31/255 , A61P25/00
CPC classification number: C07C309/15
Abstract: Masked nitrogen-substituted and oxygen-substituted neopentyl sulfonyl ester prodrugs of acamprosate of formulae (I) and (III), 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 disorders, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis and pain are disclosed.
Abstract translation: 公开了式（I）和（III）的阿卡波酸的掩蔽的氮取代和氧取代的新戊基磺酰酯前药，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酯前药治疗神经变性疾病，精神障碍，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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7.发明申请MASKED CARBOXYLATE NEOPENTYL SULFONYL ESTER CYCLIZATION RELEASE PRODRUGS OF ACAMPROSATE, COMPOSITIONS THEREOF, AND METHODS OF USE 审中-公开掩蔽的羧酸酯类抗坏血酸酯环氧化合物释放丙酸钠，其组合物及其使用方法
公开(公告)号：WO2009033061A1
公开(公告)日：2009-03-12
申请号：PCT/US2008/075453
申请日：2008-09-05
Applicant: XENOPORT, INC. , JANDELEIT, Bernd , LI, Yunxiao , GALLOP, Mark, A. , ZERANGUE, Noa , VIRSIK, Peter, A. , FISCHER, Wolf-Nicolas
Inventor： JANDELEIT, Bernd , LI, Yunxiao , GALLOP, Mark, A. , ZERANGUE, Noa , VIRSIK, Peter, A. , FISCHER, Wolf-Nicolas
IPC: C07C309/15 , C07D213/30 , C07D295/088 , A61K31/255 , A61K31/5377 , A61K31/4406 , A61P25/00
CPC classification number: C07C309/15
Abstract: Masked carboxylate neopentyl sulfonyl ester prodrugs of acamprosate of formula (I), 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 disorders, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis and pain are disclosed.
Abstract translation: 公开了式（I）的阿坎酸盐，包含这些前药的掩蔽的羧酸新戊酰磺酰酯前体药物，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酯前药治疗神经变性疾病，精神障碍，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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8.发明申请COMPLEX PANTOIC ACID ESTER NEOPENTYL SULFONYL ESTER CYCLIZATION RELEASE PRODRUGS OF ACAMPROSATE, COMPOSITIONS THEREOF, AND METHODS OF USE 审中-公开复方苯甲酸酯类NEOPYYL SULFONYL ESTER CYCLATIONATION RELEASE PROPRUGS OF ACAMPROSATE，COMPOSITIONS WITHER AND AND METHODS OF USE
公开(公告)号：WO2009033054A1
公开(公告)日：2009-03-12
申请号：PCT/US2008/075444
申请日：2008-09-05
Applicant: XENOPORT, INC. , JANDELEIT, Bernd , LI, Yunxiao , GALLOP, Mark A. , ZERANGUE, Noa , VIRSIK, Peter A. , FISCHER, Wolf-Nicolas
Inventor： JANDELEIT, Bernd , LI, Yunxiao , GALLOP, Mark A. , ZERANGUE, Noa , VIRSIK, Peter A. , FISCHER, Wolf-Nicolas
IPC: C07C309/15 , C07F9/09 , A61K31/255 , A61K31/661 , A61P25/00
CPC classification number: C07C309/15
Abstract: Pantoic acid ester neopentyl sulfonyl ester prodrugs of acamprosate of formula (I), 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 disorders, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis and pain are disclosed.
Abstract translation: 公开了式（I）的阿卡波酸，包含这些前药的药物组合物的泛酸酯新戊基磺酰酯前药，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酯前药治疗神经变性疾病，精神障碍，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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9.发明申请ACYLOXYALKYL CARBAMATE PRODRUGS OF TRANEXAMIC ACID, METHODS OF SYNTHESIS AND USE 审中-公开鬼臼酰胺的酰氧基烷基氨基甲酸酯前体，合成和使用方法
公开(公告)号：WO2007002013A3
公开(公告)日：2007-03-22
申请号：PCT/US2006023873
申请日：2006-06-20
Applicant: XENOPORT INC , JANDELEIT BERND , LI YUNXIAO , ZERANGUE NOA , GALLOP MARK A
Inventor： JANDELEIT BERND , LI YUNXIAO , ZERANGUE NOA , GALLOP MARK A
IPC: C07C271/22
CPC classification number: C07C271/22 , C07B2200/07 , C07C2601/14
Abstract: 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.
Abstract translation: 反式-4-（氨基甲基） - 环己烷羧酸的酰基氧基烷基氨基甲酸酯前药及其药物组合物，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以治疗或预防各种疾病或病症。 还公开了反式-4-（氨基甲基） - 环己烷羧酸的酰基氧基烷基氨基甲酸酯前药及其药物组合物，其适用于口服和局部给药以及使用持续释放剂型给药。
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10.发明申请BILE-ACID DERIVED COMPOUNDS FOR ENHANCING ORAL ABSORPTION AND SYSTEMIC BIOAVAILABILITY OF DRUGS 审中-公开用于增强口服吸收和系统生物利用度的胆汁酸衍生化合物
公开(公告)号：WO03020214A2
公开(公告)日：2003-03-13
申请号：PCT/US0227458
申请日：2002-08-29
Applicant: XENOPORT INC , BHAT LAXMINARAYAN , GALLOP MARK A , JANDELEIT BERND
Inventor： BHAT LAXMINARAYAN , GALLOP MARK A , JANDELEIT BERND
CPC classification number: C07J31/006 , C07J9/005 , C07J41/0055 , C07J53/002 , C07J71/0005 , C07J71/0047 , C07J71/0063
Abstract: 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.
Abstract translation: 公开了表现出穿过动物肠壁的高运输的化合物。 所述化合物可以任选地与口服给药后吸收不良或穿过肠壁不良转运的药物连接，以提供口服给药药物 - 化合物缀合物后药物的增强的治疗性和任选延长的治疗性全身血药浓度。 还公开了含有和使用这些化合物的方法的药物组合物。
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