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公开(公告)号：US06610685B2
公开(公告)日：2003-08-26
申请号：US10017978
申请日：2001-12-14
申请人： Jonathan Mark Bentley , Michael John Bickerdike , Paul Hebeisen , Guy Anthony Kennett , Sean Lightowler , Patrizio Mattei , Jacques Mizrahi , Timothy James Morley , Jean-Marc Plancher , Hans Richter , Stephan Roever , Sven Taylor , Steven Paul Vickers
发明人： Jonathan Mark Bentley , Michael John Bickerdike , Paul Hebeisen , Guy Anthony Kennett , Sean Lightowler , Patrizio Mattei , Jacques Mizrahi , Timothy James Morley , Jean-Marc Plancher , Hans Richter , Stephan Roever , Sven Taylor , Steven Paul Vickers
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： The present invention is a chemical compound of formula (I) or a pharmaceutically acceptable salt, solvate and ester thereof, wherein R1 to R4 and n are as defined in the specification. A compound of formula 1 is useful as a pharmaceutical composition for the treatment or prevention of disorders of the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.
摘要翻译： 本发明是式（I）化合物或其药学上可接受的盐，溶剂化物和酯，其中R1至R4和n如说明书中所定义。 式1的化合物可用作治疗或预防中枢神经系统疾病，心血管疾病，胃肠道疾病，糖尿病，肥胖症和睡眠呼吸暂停的药物组合物。
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2.发明授权公开(公告)号：US06433175B1
公开(公告)日：2002-08-13
申请号：US09763889
申请日：2001-02-28
申请人： David Reginald Adams , Jonathan Mark Bentley , Jonathan Richard Anthony Roffey , Richard John Hamlyn , Suneel Gaur , Matthew Alexander James Duncton , James Edward Paul Davidson , Michael John Bickerdike , Ian Anthony Cliffe , Howard Langham Mansell
发明人： David Reginald Adams , Jonathan Mark Bentley , Jonathan Richard Anthony Roffey , Richard John Hamlyn , Suneel Gaur , Matthew Alexander James Duncton , James Edward Paul Davidson , Michael John Bickerdike , Ian Anthony Cliffe , Howard Langham Mansell
IPC分类号： C07D48704
CPC分类号： C07D471/04 , C07D487/04 , C07D491/14
摘要： A chemical compound of formula (I), wherein n is 1, 2 or 3; R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, or R5 and R6 together form a carbocyclic or heterocyclic ring, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders, diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity
摘要翻译： 式（I）的化合物，其中n为1,2或3; R1和R2独立地选自氢和烷基; R3是烷基; R4至R7独立地选自氢，卤素，羟基，烷基，芳基，烷氧基，芳氧基，烷硫基，芳硫基，烷基磺酰基，烷基磺酰基，芳基亚砜基，芳基磺酰基，氨基，单烷基氨基，二烷基氨基，硝基，氰基，甲醛，烷基羰基，芳基羰基，氨基羰基 ，单烷基氨基羰基，二烷基氨基羰基，烷氧基羰基氨基，氨基羰基氧基，单烷基氨基羰基氧基，二烷基氨基羰基氧基，单烷基氨基羰基氨基和二烷基氨基羰基氨基，或R5和R6一起形成碳环或杂环，以及其药学上可接受的盐和前药，以及其用于治疗，特别是治疗疾病 的中枢神经系统; 损害中枢神经系统; 心血管疾病; 胃肠道疾病，尿崩症和睡眠呼吸暂停，特别是用于治疗肥胖症
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3.发明授权Cyclic glycyl-2-allyl proline improves cognitive performance in impaired animals 有权环状甘氨酰-2-烯丙基脯氨酸改善受损动物的认知功能公开(公告)号：US08791117B2
公开(公告)日：2014-07-29
申请号：US13043215
申请日：2011-03-08
申请人： Michael John Bickerdike , Jian Guan
发明人： Michael John Bickerdike , Jian Guan
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D241/36 , C07D471/00 , C07D487/00 , A61K31/4985 , A61K31/498
CPC分类号： A61K31/4985 , A61K31/498 , C07D487/04 , C07D487/10
摘要： Embodiments of this invention provide methods for therapeutic use of cyclic G-2-Allyl Proline to treat cognitive disorders as well as manufacture of medicaments including tablets, capsules, injectable solutions that are useful for treatment of such conditions.
摘要翻译： 本发明的实施方案提供了用于治疗性使用环状G-2-烯丙基脯氨酸治疗认知障碍以及制备药物的方法，所述药物包括片剂，胶囊，可用于治疗这些病症的可注射溶液。
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公开(公告)号：US09708366B2
公开(公告)日：2017-07-18
申请号：US13699087
申请日：2012-01-27
IPC分类号： A61K9/00 , C07K5/062 , A61K31/401 , A61K45/06 , A61K38/06 , A61K9/127 , A61K38/05 , A61K9/06 , A61K9/107
CPC分类号： C07K5/06026 , A61K9/0019 , A61K9/0085 , A61K9/06 , A61K9/107 , A61K9/127 , A61K31/401 , A61K38/05 , A61K38/06 , A61K45/06
摘要： This invention provides compounds, compositions and methods for treating Autism Spectrum Disorders (ASD) using glycyl-2-methylprolyl-glutamic acid (G-2-MePE) and analogs thereof. Autism Spectrum Disorders include Autism, Autistic Disorder Asperger Syndrome, Childhood Disintegrative Disorder, Pervasive Developmental Disorder—Not Otherwise Specified (PDD-NOS), Fragile X Syndrome, and Rett Syndrome. Compositions containing compounds include water-soluble formulations, water-in-oil micro-emulsions, water-in-oil coarse emulsions, water-in-oil liquid crystals, nanocapsules, tablets, and orally administered gels. The compounds and compositions of this invention can be administered intravenously, intraventricularly, parenterally, or orally, and can be effective in treating neurodegeneration, promoting neurological function, treating seizure activity and other symptoms of ASD, and can prolong life in animals including human beings having Autism Spectrum Disorders.
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5.发明申请CYCLIC GLYCYL-2-ALLYL PROLINE IMPROVES COGNITIVE PERFORMANCE IN IMPAIRED ANIMALS 有权周期性GLYCYL-2-ALLYL PROLINE改善了有害动物的认知性能公开(公告)号：US20110201614A1
公开(公告)日：2011-08-18
申请号：US13043215
申请日：2011-03-08
IPC分类号： A61K31/4985 , A61K31/499 , A61P25/28
CPC分类号： A61K31/4985 , A61K31/498 , C07D487/04 , C07D487/10
摘要： Embodiments of this invention provide methods for therapeutic use of cyclic G-2-Allyl Proline to treat cognitive disorders as well as manufacture of medicaments including tablets, capsules, injectable solutions that are useful for treatment of such conditions.
摘要翻译： 本发明的实施方案提供了用于治疗性使用环状G-2-烯丙基脯氨酸治疗认知障碍以及制备药物的方法，所述药物包括片剂，胶囊，可用于治疗这些病症的可注射溶液。
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6.发明申请TREATMENT OF AUTISM SPECTRUM DISORDERS USING GLYCYL-L-2-METHYLPROLYL-L-GLUTAMIC ACID 有权使用GLYCYL-L-2-甲基丙氨酸-L-谷氨酸处理脂质光谱异常公开(公告)号：US20140147491A1
公开(公告)日：2014-05-29
申请号：US13699087
申请日：2012-01-27
CPC分类号： C07K5/06026 , A61K9/0019 , A61K9/0085 , A61K9/06 , A61K9/107 , A61K9/127 , A61K31/401 , A61K38/05 , A61K38/06 , A61K45/06
摘要： This invention provides compounds, compositions and methods for treating Autism Spectrum Disorders (ASD) using glycyl-2-methylprolyl-glutamic acid (G-2-MePE) and analogs thereof. Autism Spectrum Disorders include Autism, Autistic Disorder Asperger Syndrome, Childhood Disintegrative Disorder, Pervasive Developmental Disorder—Not Otherwise Specified (PDD-NOS), Fragile X Syndrome, and Rett Syndrome. Compositions containing compounds include water-soluble formulations, water-in-oil micro-emulsions, water-in-oil coarse emulsions, water-in-oil liquid crystals, nanocapsules, tablets, and orally administered gels. The compounds and compositions of this invention can be administered intravenously, intraventricularly, parenterally, or orally, and can be effective in treating neurodegeneration, promoting neurological function, treating seizure activity and other symptoms of ASD, and can prolong life in animals including human beings having Autism Spectrum Disorders.
摘要翻译： 本发明提供使用甘氨酰-2-甲基脯氨酰 - 谷氨酸（G-2-MePE）及其类似物治疗自闭症谱系障碍（ASD）的化合物，组合物和方法。 自闭症谱系障碍包括自闭症，孤独症，阿斯伯格综合征，儿童解体障碍，普遍性发育障碍（PDD-NOS），脆性X综合征和Rett综合征。 含有化合物的组合物包括水溶性制剂，油包水微乳液，油包水粗乳液，油包水液晶，纳米胶囊，片剂和口服凝胶。 本发明的化合物和组合物可以静脉内，心室内，胃肠外或口服施用，并且可以有效治疗神经变性，促进神经功能，治疗癫痫发作活动和ASD的其他症状，并且可以延长动物的寿命，包括具有 自闭症谱系障碍
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