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1. 发明申请

WO2008077138A1 3-BENZOFURANYL-4-INDOLYL MALEIMIDES AS POTENT GSK3 INHIBITORS FOR NEUROGENERATIVE DISORDERS 审中-公开
标题翻译： 3-BENZOFURANYL-4-INDOLYL maleimides as POTENT GSK3 INHIBITORS FOR NEUROGENERATIVE DISORDERS
公开(公告)号：WO2008077138A1
公开(公告)日：2008-06-26
申请号：PCT/US2007/088248
申请日：2007-12-19
申请人： THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS , KOZIKOWSKI, Alan, P. , GAYSINA, Irina
发明人： KOZIKOWSKI, Alan, P. , GAYSINA, Irina
IPC分类号： C07C49/00 , C07D249/00 , C07D285/00
CPC分类号： C07D405/14
摘要： Compounds of formula (I): and pharmaceutically acceptable salts, esters and solvates thereof, where variables are defined in the specification, useful generally as inhibitors of protein kinases and particularly useful for inhibition of GSK-3. Pharmaceutically compositions and medicaments containing a compound of the invention are provided. The invention provides methods of treatment of protein kinase-related disease, disorders or conditions. The invention provides methods of treatment of GSK-3-related diseases, disorders or conditions. More specifically, methods of treatment of bipolar disorder, including mania, schizophrenia, stroke, epilepsy, motor neuron disease, cranial or spinal trauma, neurodegenerative disorders, including multiple sclerosis (MS), Alzheimer's disease, Fragile X syndrome, autism, Huntington's disease, Parkinson's
摘要翻译：式（I）化合物及其药学上可接受的盐，酯和溶剂合物，其中变量在说明书中定义，其通常用作蛋白激酶的抑制剂，特别可用于抑制GSK-3。提供含有本发明化合物的药物组合物和药物。本发明提供了治疗蛋白激酶相关疾病，病症或病症的方法。本发明提供治疗GSK-3相关疾病，病症或病症的方法。更具体地，治疗双相情感障碍的方法，包括躁狂症，精神分裂症，中风，癫痫，运动神经元疾病，颅脑损伤或脊髓损伤，包括多发性硬化症（MS），阿尔茨海默氏病，脆性X综合征，自闭症，亨廷顿舞蹈病在内的神经变性疾病，帕金森氏

2. 发明申请

WO2010045212A2 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS AND THE USES THEREOF 审中-公开
标题翻译： NICOTINIC乙酰胆碱受体配体及其用途
公开(公告)号：WO2010045212A2
公开(公告)日：2010-04-22
申请号：PCT/US2009/060473
申请日：2009-10-13
申请人： PSYCHOGENICS, INCstatuts , CHANDRASEKHAR, Jayaraman , KOZIKOWSKI, Alan, P. , LIU, Jianhua , TUECKMANTEL, Werner , WALKER, Joel, R. , YUEN, Po-wai , THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
发明人： CHANDRASEKHAR, Jayaraman , KOZIKOWSKI, Alan, P. , LIU, Jianhua , TUECKMANTEL, Werner , WALKER, Joel, R. , YUEN, Po-wai
IPC分类号： C07D401/12 , C07D401/04 , C07D401/02 , A61K31/44 , A61K31/4427 , A61P25/18 , A61P25/26
CPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , C07D471/18
摘要： The invention relates to pyridinyl nicotinic acetylcholine receptor ligands, compositions comprising an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand and methods to treat or prevent a condition, such as depression and nicotine dependence, comprising administering to an animal in need thereof an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand.
摘要翻译：本发明涉及吡啶基烟碱乙酰胆碱受体配体，包含有效量的吡啶基烟碱乙酰胆碱受体配体的组合物和治疗或预防诸如抑郁症和尼古丁依赖之类的病症的方法，包括向有需要的动物施用有效量的吡啶基烟碱乙酰胆碱受体配体。

3. 发明申请

WO2007008514A2 INHIBITORS OF GLYCOGEN SYNTHASE KINASE 3 审中-公开
标题翻译： GLYCOGEN SYNTHASE KINASE的抑制剂3
公开(公告)号：WO2007008514A2
公开(公告)日：2007-01-18
申请号：PCT/US2006/026137
申请日：2006-07-06
申请人： GEORGETOWN UNIVERSITY , KOZIKOWSKI, Alan, P. , GAYSINA, Irina , PETUKHOV, Pavel , SRIDHAR, Jayalakshmi , TUECKMANTEL, Werner
发明人： KOZIKOWSKI, Alan, P. , GAYSINA, Irina , PETUKHOV, Pavel , SRIDHAR, Jayalakshmi , TUECKMANTEL, Werner
IPC分类号： A61K31/426
CPC分类号： C07D403/14 , C07D403/04
摘要： One aspect of the present invention relates to heterocyclic compounds that inhibit mammalian or human glycogen synthase kinase 3. Another aspect of the invention relates to pharmaceutical compositions comprising such a heterocyclic compound. The present invention also relates to methods of treating a mammal or human suffering from a malady that is based at least in part on abnormal activity of glycogen synthase kinase 3. The present invention also relates to methods of treating a mammal or human suffering from diabetes, Alzheimer's disease, Huntington's disease, Parkinson's disease, AIDS-associated dementia, ALS, MS, or schizophrenia.
摘要翻译：本发明的一个方面涉及抑制哺乳动物或人糖原合成酶激酶3的杂环化合物。本发明的另一方面涉及包含这种杂环化合物的药物组合物。本发明还涉及治疗至少部分基于糖原合成酶激酶3的异常活性的患有疾病的哺乳动物或人的方法。本发明还涉及治疗患有糖尿病的哺乳动物或人的方法，阿尔茨海默病，亨廷顿氏病，帕金森病，AIDS相关性痴呆，ALS，MS或精神分裂症。

4. 发明公开

EP2342192A2 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS AND THE USES THEREOF 审中-公开
标题翻译：尼古丁乙酰胆碱受体配体和用途
公开(公告)号：EP2342192A2
公开(公告)日：2011-07-13
申请号：EP09821104.8
申请日：2009-10-13
申请人： Psychogenics Inc. , The Board Of Trustees Of The University Of Illinois
发明人： CHANDRASEKHAR, Jayaraman , KOZIKOWSKI, Alan, P. , LIU, Jianhua , TUECKMANTEL, Werner , WALKER, Joel, R. , YUEN, Po-wai
IPC分类号： C07D401/12 , C07D401/04 , C07D401/02 , A61K31/44 , A61K31/4427 , A61P25/18 , A61P25/26
CPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , C07D471/18
摘要： The invention relates to pyridinyl nicotinic acetylcholine receptor ligands, compositions comprising an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand and methods to treat or prevent a condition, such as depression and nicotine dependence, comprising administering to an animal in need thereof an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand.

5. 发明公开

EP0975595A1 ANALOGS OF COCAINE 失效
标题翻译：模拟可卡因
公开(公告)号：EP0975595A1
公开(公告)日：2000-02-02
申请号：EP98915409.1
申请日：1998-04-07
申请人： GEORGETOWN UNIVERSITY , Kozikowski, Alan, P. , Araldi, Gian, Luca
发明人： KOZIKOWSKI, Alan, P. , ARALDI, Gian, Luca
IPC分类号： C07D211/60 , C07D211/22 , A61K31/445 , C07D211/20 , C07D211/14 , C07D211/12
CPC分类号： C07D211/60 , C07B59/002 , C07B2200/07 , C07D211/12 , C07D211/14 , C07D211/20 , C07D211/22
摘要： The invention provides a compound of formula (I), wherein R?1, R2, R3¿, and Y have any of the meanings defined in the specification; as well as a pharmaceutical composition comprising a compound of formula (I); intermediates and methods useful for preparing a compound of formula (I); and therapeutic methods for treating drug addiction, Parkinson's disease or depression comprising administering a compound of formula (I), to a mammal in need of such treatment.

6. 发明公开

EP0944626A1 TROPANE DERIVATIVES AND METHOD FOR THEIR SYNTHESIS 失效
标题翻译：托烷衍生物的合成及方法
公开(公告)号：EP0944626A1
公开(公告)日：1999-09-29
申请号：EP97954023.0
申请日：1997-12-02
申请人： GEORGETOWN UNIVERSITY , Kozikowski, Alan, P. , Araldi, Gian, Luca
发明人： KOZIKOWSKI, Alan, P. , ARALDI, Gian, Luca
IPC分类号： A61K31 , A61K51 , A61P3 , A61P25 , A61P43 , C07D451
CPC分类号： C07D451/02
摘要： A compound of formula (I) wherein R1 - R6 have any of the values defined in the specification, as well as pharmaceutical compositions comprising a compound of formula (I), and methods for preparing and using compounds of formula (I) are described.

7. 发明授权

EP0975595B9 ANALOGS OF COCAINE 失效
标题翻译：模拟可卡因
公开(公告)号：EP0975595B9
公开(公告)日：2009-09-16
申请号：EP98915409.1
申请日：1998-04-07
申请人： GEORGETOWN UNIVERSITY , Kozikowski, Alan, P. , Araldi, Gian, Luca
发明人： KOZIKOWSKI, Alan, P. , ARALDI, Gian, Luca
IPC分类号： C07D211/60 , C07D211/22 , A61K31/445 , C07D211/20 , C07D211/14 , C07D211/12
CPC分类号： C07D211/60 , C07B59/002 , C07B2200/07 , C07D211/12 , C07D211/14 , C07D211/20 , C07D211/22
摘要： The invention provides a compound of formula (I), wherein R?1, R2, R3¿, and Y have any of the meanings defined in the specification; as well as a pharmaceutical composition comprising a compound of formula (I); intermediates and methods useful for preparing a compound of formula (I); and therapeutic methods for treating drug addiction, Parkinson's disease or depression comprising administering a compound of formula (I), to a mammal in need of such treatment.

8. 发明公开

EP1000015A1 BICYCLIC METABOTROPIC GLUTAMATE RECEPTOR LIGANDS 失效
标题翻译： BIZYCLISCHE LIGANDE DES代谢物谷氨酸受体
公开(公告)号：EP1000015A1
公开(公告)日：2000-05-17
申请号：EP98936911.1
申请日：1998-07-17
申请人： GEORGETOWN UNIVERSITY , Kozikowski, Alan, P. , Steensma, Darryl Hugh , Tueckmantel, Werner , Araldi, Gian, Luca
发明人： KOZIKOWSKI, Alan, P. , STEENSMA, Darryl, Hugh , TUECKMANTEL, Werner , ARALDI, Gian, Luca
IPC分类号： C07C229/50 , C07F9/117 , A61K31/195
CPC分类号： C07F9/117 , C07C229/50 , C07C2602/40
摘要： The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and methods for their use.
摘要翻译：本发明提供双环代谢型谷氨酸受体配体，以及包含这种配体的组合物及其使用方法。

9. 发明授权

EP0975595B1 ANALOGS OF COCAINE 失效
标题翻译：可卡因的类似物
公开(公告)号：EP0975595B1
公开(公告)日：2009-06-17
申请号：EP98915409.1
申请日：1998-04-07
申请人： GEORGETOWN UNIVERSITY , Kozikowski, Alan, P. , Araldi, Gian, Luca
发明人： KOZIKOWSKI, Alan, P. , ARALDI, Gian, Luca
IPC分类号： C07D211/60 , C07D211/22 , A61K31/445 , C07D211/20 , C07D211/14 , C07D211/12
CPC分类号： C07D211/60 , C07B59/002 , C07B2200/07 , C07D211/12 , C07D211/14 , C07D211/20 , C07D211/22
摘要： The invention provides a compound of formula (I), wherein R?1, R2, R3¿, and Y have any of the meanings defined in the specification; as well as a pharmaceutical composition comprising a compound of formula (I); intermediates and methods useful for preparing a compound of formula (I); and therapeutic methods for treating drug addiction, Parkinson's disease or depression comprising administering a compound of formula (I), to a mammal in need of such treatment.
摘要翻译：本发明提供了式（I）化合物，其中R 1，R 2，R 3和Y具有说明书中定义的任何含义; 以及包含式（I）化合物的药物组合物; 用于制备式（I）化合物的中间体和方法; 和用于治疗药物成瘾，帕金森病或抑郁症的治疗方法，包括给需要这种治疗的哺乳动物施用式（I）化合物。

10. 发明公开

EP1015427A1 SUBSTITUTED 2-PYRROLIDINONE ACTIVATORS OF PKC 审中-公开
标题翻译：取代的2- PYRROLIDONONE AS的PKC激活剂
公开(公告)号：EP1015427A1
公开(公告)日：2000-07-05
申请号：EP98945967.2
申请日：1998-09-08
申请人： GEORGETOWN UNIVERSITY , Kozikowski, Alan, P. , Wang, Shaomeng , Qiao, Lixin
发明人： KOZIKOWSKI, Alan, P. , WANG, Shaomeng , QIAO, Lixin
IPC分类号： C07D207/26 , A61K31/40
CPC分类号： C07D207/26
摘要： Compounds of formula (I) wherein R1 and R2 are each independently (C1-C15)alkyl, (C2-C15)alkenyl, (C2-C15)alkynyl, (C3-C8)cycloalkyl, (C3-C8)cycloalkyl(C1-C10)alkyl, (C3-C8)cycloalkyl(C1-C15)alkenyl, (C3-C8)cycloalkyl(C1-C15)alkynyl, (C1-C15)alkoxy, (C1-C15)alkanoyl, (C1-C15)alkanoyloxy, aryl, heteroaryl, aryl(C1-C6)alkyl, heteroaryl(C1-C6)alkyl, aryl(C2-C15)alkenyl, heteroaryl(C2-C15)alkenyl, aryl(C2-C15)alkynyl, heteroaryl(C2-C15)alkynyl, aryl(C1-C15)alkoxy, heteroaryl(C1-C15)alkoxy, aryl(C1-C15)alkanoyl, heteroaryl(C1-C15)alkanoyl, aryl(C1-C15)alkanoyloxy, or heteroaryl(C1-C15)alkanoyloxy; wherein any R1 or R2 is optionally substituted with one or more substituents and their pharmaceutically acceptable salts, are PKC activators and are useful for treating diseases, such as, for example, cancer. Also disclosed are pharmaceutical compositions comprising compounds of formula (I), processes for preparing compounds of formula (I), and intermediates useful for preparing compounds of formula (I).

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