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1. 发明申请

WO0232412A3 COMBINATION USE OF ACETYLCHOLINESTERASE INHIBITORS AND GABAA INVERSE AGONISTS FOR THE TREATMENT OF COGNITIVE DISORDERS 审中-公开
标题翻译：乙酰胆碱酯酶抑制剂和GABAA反转激素治疗认知障碍的联合使用
公开(公告)号：WO0232412A3
公开(公告)日：2003-03-20
申请号：PCT/IB0101934
申请日：2001-10-15
申请人： PFIZER PROD INC , VILLALOBOS ANABELLA , CASSELLA JAMES VINCENT , RAJACHANDRAN LAVANYA , NEUROGEN CORP
发明人： VILLALOBOS ANABELLA , CASSELLA JAMES VINCENT , RAJACHANDRAN LAVANYA
IPC分类号： A61K31/13 , A61K31/195 , A61K31/4375 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/55 , A61K31/66 , A61K45/06 , A61P9/10 , A61P17/02 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28
CPC分类号： A61K31/55 , A61K31/00 , A61K31/13 , A61K31/195 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/66 , A61K45/06 , A61K31/435 , A61K31/40 , A61K31/27 , A61K31/125 , A61K2300/00
摘要： This invention provides a composition for treating a cognitive disorder, which comprises an acetylcholinesterase, and a GABAA inverse agonist selected from a compound of the formula (I) where X and Y are defined herein.
摘要翻译：本发明提供了一种用于治疗认知障碍的组合物，其包含乙酰胆碱酯酶和选自本文定义X和Y的式（I）化合物的GABA A反向激动剂。

2. 发明申请

WO2002069948A1 USE OF GABAA INVERSE AGONISTS IN COMBINATION WITH NICOTINE RECEPTOR PARTIAL AGONISTS, ESTROGEN, SELECTIVE ESTROGEN MODULATORS, OR VITAMIN E FOR THE TREATMENT OF COGNITIVE DISORDERS 审中-公开
标题翻译：使用GABAA反转激动剂联合非依诺贝因受体部分激素，雌激素，选择性雌激素调节剂或维生素E治疗认知障碍
公开(公告)号：WO2002069948A1
公开(公告)日：2002-09-12
申请号：PCT/IB2002/000515
申请日：2002-02-20
申请人： PFIZER PRODUCTS INC. , VILLALOBOS, Anabella
发明人： VILLALOBOS, Anabella
IPC分类号： A61K31/00
CPC分类号： A61K45/06 , A61K31/195 , A61K31/355 , A61K31/56 , A61K2300/00
摘要： A pharmaceutical composition and method of treatment of diseases of cognitive dysfunction in a mammal comprising administration of a GABA A inverse agonist or a pharmaceutically acceptable salt thereof; and a nicotine receptor partial agonist, an estrogenic agent, selective estrogen receptor modulator or vitamin E or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier. The GABA A inverse agonist, and nicotine receptor partial agonist, estrogen, selective estrogen receptor modulator or vitamin E are present in amounts that render the composition effective enhancing cognition or in the treatment of diseases of cognitive dysfunction including but not limited to Alzheimer's Disease (AD), mild cognitive impairment, age-related cognitive decline, vascular dementia, Parkinson's disease, Huntington's disease, memory impairment associated with depression or anxiety, schizophrenia, Down's syndrome, stroke, traumatic brain injury (TBI), AIDS associated dementia and attention deficit disorder. The method of using these compositions is also disclosed.
摘要翻译：一种治疗哺乳动物认知功能障碍疾病的药物组合物和方法，包括给予GABAA反向激动剂或其药学上可接受的盐; 尼古丁受体部分激动剂，雌激素剂，选择性雌激素受体调节剂或维生素E或其药学上可接受的盐; 和药学上可接受的载体。 GABAA反向激动剂和尼古丁受体部分激动剂，雌激素，选择性雌激素受体调节剂或维生素E以使组合物有效增强认知或治疗认知功能障碍疾病的量存在，包括但不限于阿尔茨海默病（AD），轻度认知障碍，年龄相关认知衰退，血管性痴呆，帕金森病，亨廷顿病，与抑郁或焦虑相关的记忆障碍，精神分裂症，唐氏综合征，中风，创伤性脑损伤（TBI），AIDS相关性痴呆和注意力缺陷障碍。还公开了使用这些组合物的方法。

3. 发明申请

WO1995029909A1 NOVEL ACYCLIC AND CYCLIC AMIDES AS NEUROTRANSMITTER RELEASE ENHANCERS 审中-公开
标题翻译：新型ACYCLIC和循环辅助剂作为神经递质释放增强剂
公开(公告)号：WO1995029909A1
公开(公告)日：1995-11-09
申请号：PCT/IB1995000189
申请日：1995-03-20
申请人： PFIZER INC. , VOLKMANN, Robert, A. , JASYS, Vytautas, J. , BRIGHT, Gene, M. , VILLALOBOS, Anabella , SEYMOUR, Patricia, A.
发明人： PFIZER INC.
IPC分类号： C07D401/06
CPC分类号： C07D213/20 , C07C233/06 , C07C2602/42 , C07D239/26 , C07D401/06 , C07D401/14 , C07D405/06 , C07D405/14 , C07D413/06
摘要： This invention relates to compounds of formula (IA), (IB), (IC) or (ID), wherein m, X, Z, R , R , R , R , R , R and the dotted lines are as defined below, their pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of using them to treat Alzheimer's disease, age-associated memory impairment, Parkinson's disease and other central nervous system disorders. The claimed compounds have the ability to enhance the release of neurotransmitters such as acetylcholine, dopamine and serotonin.
摘要翻译：本发明涉及式（IA），（IB），（IC）或（ID）的化合物，其中m，X，Z，R 2，R 3，R 4，R 5， R 6，R 14和虚线如下所定义，其药学上可接受的盐，含有它们的药物组合物和使用它们治疗阿尔茨海默氏病，年龄相关记忆障碍，帕金森病和其他中枢神经系统的方法障碍。所要求保护的化合物具有增强神经递质如乙酰胆碱，多巴胺和5-羟色胺的释放的能力。

4. 发明申请

WO1992017475A1 HETEROCYCLIC-CYCLIC AMINE DERIVATIVES 审中-公开
标题翻译：杂环化合物氨衍生物
公开(公告)号：WO1992017475A1
公开(公告)日：1992-10-15
申请号：PCT/US1992001605
申请日：1992-03-09
申请人： PFIZER INC. , VILLALOBOS, Anabella , NAGEL, Arthur, Adam , CHEN, Yuhpyng, Liang
发明人： PFIZER INC.
IPC分类号： C07D413/06
CPC分类号： C07D401/06 , C07D211/32 , C07D261/20 , C07D413/06 , C07D413/14 , C07D417/06 , Y02P20/55
摘要： Compounds of formula (I) wherein R , R , R , R , X, Y, M and L are defined as below. The compounds of formula (I) are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.
摘要翻译：其中R 1，R 2，R 7，R 8，X，Y，M和L的式（I）化合物定义如下。式（I）化合物是胆碱酯酶抑制剂，可用于增强患有痴呆和阿尔茨海默病的患者的记忆。

5. 发明申请

WO1996013505A1 PROCESSES AND INTERMEDIATES FOR PREPARING 5,7-DIHYDRO-3-[2-{1-BENZYLPIPERIDIN-4-YL}ETHYL]-6H-PYRROLO-[4,5-f]-1,2-BENZISOXAZOL-6-ONE 审中-公开
标题翻译：制备5,7-二氢-3- [2- {1-苄基哌啶-4-基]乙基] -6H-吡咯并[4,5-f] -1,2-苯并咪唑-6-酮的方法和中间体
公开(公告)号：WO1996013505A1
公开(公告)日：1996-05-09
申请号：PCT/IB1995000755
申请日：1995-09-13
申请人： PFIZER INC. , DEVRIES, Keith, M. , VILLALOBOS, Anabella
发明人： PFIZER INC.
IPC分类号： C07D498/04
CPC分类号： C07D498/04
摘要： This invention relates to a process for preparing the compound having formula (I) which comprises i) heating the compound of formula (VII) wherein R is R or benzyl and R is R C(=O), R OC(=O) or R SO2 wherein R is (C1-C6)alkyl or (C6-C10)aryl(C1-C6)alkyl; at an elevated temperature in the presence of a base with the proviso that when R in the resultant product is R said product is ii) further treated with an aqueous mineral acid at an elevated temperature followed by iii) treatment of the product of ii) with a) a benzylating agent in the presence of a base or b) benzaldehyde in the presence of a reducing agent and an acid.
摘要翻译：本发明涉及制备具有式（I）的化合物的方法，该方法包括：i）加热其中R 3为R 4或苄基且R 4为R 5 C的式（Ⅶ）化合物（= O），R 5 OC（= O）或R 5 SO 2，其中R 5为（C 1 -C 6）烷基或（C 6 -C 10）芳基（C 1 -C 6）烷基; 在碱的存在下在高温下，条件是当所得产物中的R 3为R 4时，所述产物是ii）在升高的温度下用无机酸水溶液进一步处理，随后iii）处理 ii）与a）苄基化试剂在碱存在下或b）苯甲醛的存在下，在还原剂和酸存在下反应。

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