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1. 发明申请

WO2010100606A1 NOVEL PHENYL IMIDAZOLES AND PHENYL TRIAZOLES AS GAMMA-SECRETASE MODULATORS 审中-公开
标题翻译：新型苯并咪唑和苯乙酮作为胶体分泌调节剂
公开(公告)号：WO2010100606A1
公开(公告)日：2010-09-10
申请号：PCT/IB2010/050896
申请日：2010-03-02
申请人： PFIZER INC. , ALLEN, Martin, Patrick , AM ENDE, Christopher, William , BRODNEY, Michael, Aaron , DOUNAY, Amy, Beth , JOHNSON, Douglas, Scott , PETTERSSON, Martin, Youngjin , SCHWARZ, Jacob, Bradley , TRAN, Tuan, Phong
发明人： ALLEN, Martin, Patrick , AM ENDE, Christopher, William , BRODNEY, Michael, Aaron , DOUNAY, Amy, Beth , JOHNSON, Douglas, Scott , PETTERSSON, Martin, Youngjin , SCHWARZ, Jacob, Bradley , TRAN, Tuan, Phong
IPC分类号： C07D233/54 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , A61K31/41 , A61P25/00
CPC分类号： C07D413/12 , C07D233/54 , C07D401/12 , C07D403/12 , C07D417/12
摘要： Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
摘要翻译：公开了化合物的化合物和药学上可接受的盐，其中所述化合物具有如说明书中定义的式（I）的结构。还公开了相应的药物组合物，治疗方法，合成方法和中间体。

2. 发明申请

WO2009136350A1 NOVEL CLASS OF SPIRO PIPERIDINES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES 审中-公开
标题翻译：治疗神经病变疾病的新一代螺旋管
公开(公告)号：WO2009136350A1
公开(公告)日：2009-11-12
申请号：PCT/IB2009/051815
申请日：2009-05-04
申请人： PFIZER INC. , BRODNEY, Michael, Aaron , HELAL, Christopher, John , O'NEILL, Brian, Thomas
发明人： BRODNEY, Michael, Aaron , HELAL, Christopher, John , O'NEILL, Brian, Thomas
IPC分类号： C07D513/10 , A61K31/4436 , A61P25/28
CPC分类号： C07D513/10
摘要： Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
摘要翻译：公开了化合物的化合物和药学上可接受的盐，其中所述化合物具有如说明书中定义的式（I）的结构。还公开了相应的药物组合物，治疗方法，合成方法和中间体。

3. 发明申请

WO2007034326A3 IMIDAZOLE COMPOUNDS FOR THE TREATMENT OF NEUROLOGICAL DISORDERS 审中-公开
公开(公告)号：WO2007034326A3
公开(公告)日：2007-03-29
申请号：PCT/IB2006/002753
申请日：2006-09-11
申请人： PFIZER PRODUCTS INC. , BRODNEY, Michael, Aaron , CHEN, Yuhpyng, Liang , COFFMAN, Karen, Jean , KLEINMAN, Edward, Fox , O'NEILL, Brian, Thomas
发明人： BRODNEY, Michael, Aaron , CHEN, Yuhpyng, Liang , COFFMAN, Karen, Jean , KLEINMAN, Edward, Fox , O'NEILL, Brian, Thomas
IPC分类号： C07D233/54 , C07D401/04 , C07D403/04 , C07D403/10 , C07D403/12 , C07D401/12 , C07D405/12 , C07D405/06 , C07D401/06 , C07D409/12 , C07D413/12 , C07D487/04 , C07D487/08 , A61K31/4178
摘要： The present invention relates to compounds of Formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 6 , R 7 and A are as defined. Compounds of Formula (I) have activity inhibiting production of Aβ-peptide. The invention also relates to pharmaceutical compositions and methods for treating diseases and disorders, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of Formula (I).

4. 发明申请

WO2006000912A2 PYRIDYL PIPERAZINES FOR THE TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：用于治疗CNS病症的吡啶哌啶
公开(公告)号：WO2006000912A2
公开(公告)日：2006-01-05
申请号：PCT/IB2005/002074
申请日：2005-06-13
申请人： PFIZER PRODUCTS INC. , BRODNEY, Michael, Aaron
发明人： BRODNEY, Michael, Aaron
IPC分类号： A61K31/00
CPC分类号： C07D413/14 , C07D401/06 , C07D405/14 , C07D413/06
摘要： This invention is directed to compounds of Formula (I) and to pharmaceutical compositions comprising the compound of Formula (I) or a prodrug thereof and a pharmaceutically effective carrier. where G is G 1 or G2; where the dashed line represents an optional double bond; and where n is 1 or 2, and Ar 1 , Ar 2 , ... and Z are as defined in the specification. The invention is also directed to a method of treating or preventing in mammals, including humans, a disorder or condition that can be treated by altering serotonin-mediated neurotransmission, including a disorder selected from the group consisting of migraine, headache, cluster headache, anxiety, depression, dysthymia, major depressive disorder, migraine, post-traumatic stress disorder, avoidant personality disorder, borderline personality disorder and phobias This invention is also directed to intermediates useful in the synthesis of compounds of Formula (I).
摘要翻译：本发明涉及式（I）的化合物和包含式（I）化合物或其前药和药学上有效载体的药物组合物。其中G是G 1或G2; 其中虚线表示可选的双键; 并且其中n为1或2，Ar 1，Ar 2，...和Z如说明书中所定义。本发明还涉及一种治疗或预防哺乳动物（包括人）的疾病或病症的方法，所述疾病或病症可以通过改变血清素介导的神经传递来治疗，包括选自偏头痛，头痛，丛集性头痛，焦虑症抑郁症，精神抑郁症，重度抑郁症，偏头痛，创伤后应激障碍，避孕人格障碍，边缘人格障碍和恐惧症本发明还涉及可用于合成式（I）化合物的中间体。

5. 发明申请

WO2008023239A1 PYRIMIDONE COMPOUNDS AS GSK-3 INHIBITORS 审中-公开
标题翻译： PYRIMIDONE化合物作为GSK-3抑制剂
公开(公告)号：WO2008023239A1
公开(公告)日：2008-02-28
申请号：PCT/IB2007/002390
申请日：2007-08-13
申请人： PFIZER PRODUCTS INC. , LEFKER, Bruce, Allen , BRODNEY, Michael, Aaron , SAKYA, Subas, Man , HAY, Bruce, Allan , WESSEL, Matthew, David , CONN, Edward, Lee
发明人： LEFKER, Bruce, Allen , BRODNEY, Michael, Aaron , SAKYA, Subas, Man , HAY, Bruce, Allan , WESSEL, Matthew, David , CONN, Edward, Lee
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/14 , C07D413/14 , C07D417/14 , C07D487/04 , A61K31/435 , A61K31/505 , A61K31/55
CPC分类号： C07D401/14 , C07D401/04 , C07D403/04 , C07D403/12 , C07D405/14 , C07D413/14 , C07D417/14 , C07D487/04
摘要： The invention relates to pyrimidone derivatives I having activity as GSK-3 inhibitors. The invention further relates to pharmaceutical compositions comprising such derivatives and uses thereof in treating certain disorders. Formula (I):
摘要翻译：本发明涉及作为GSK-3抑制剂具有活性的嘧啶酮衍生物I。本发明还涉及包含这些衍生物的药物组合物及其在治疗某些疾病中的用途。式（I）：

6. 发明申请

WO2006106416A1 PYRIDIL-LACTAMS AND THEIR USE 5 -HTl RECEPTORS LIGAN 审中-公开
标题翻译：吡嗪类药物及其使用5-HT受体配体
公开(公告)号：WO2006106416A1
公开(公告)日：2006-10-12
申请号：PCT/IB2006/000799
申请日：2006-03-27
申请人： PFIZER PRODUCTS INC. , BRODNEY, Michael, Aaron
发明人： BRODNEY, Michael, Aaron
IPC分类号： C07D413/14 , C07D413/06 , C07D401/06 , C07D401/14 , C07D405/14 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61P25/00
CPC分类号： C07D413/06 , C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14
摘要： The present invention relates to novel pyridyl-lactams, compounds of the formula (I), wherein R 1 is a group of the formula G 1 , G 2 , G 3 or G 4 depicted below, and R 3 , Y, R 6 , R 7 , R 8 , R 13 , a, n and m are as defined herein, their pharmaceutically acceptable salts, pharmaceutical compositions, their preparation and intermediates therefrom, and their use in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT 1B antagonist is indicated.
摘要翻译：本发明涉及新的吡啶基内酰胺，式（I）的化合物，其中R 1是式G 1，G 2， / SUP>，G 3或G 4，以及R 3，Y，R 6，R R 7，R 8，R 13，a，n和m如本文所定义，其药学上可接受的盐，药物组合物，其制备和其中间体及其在治疗或预防抑郁，焦虑，强迫症（OCD）以及其中指示5-HT 1B拮抗剂的其它病症中的用途。

7. 发明申请

WO2005107808A2 COMBINATION OF ATYPICAL ANTIPSYCHOTICS AND 5-HT1B RECEPTOR ANTAGONISTS 审中-公开
标题翻译：原位抗原与5-HT1B受体拮抗剂的组合
公开(公告)号：WO2005107808A2
公开(公告)日：2005-11-17
申请号：PCT/IB2005/001195
申请日：2005-04-29
申请人： PFIZER PRODUCTS INC. , BRODNEY, Michael, Aaron , HELAL, Christopher, John , BRONK, Brian, Scott , LIRAS, Spiros
发明人： BRODNEY, Michael, Aaron , HELAL, Christopher, John , BRONK, Brian, Scott , LIRAS, Spiros
IPC分类号： A61K45/06
CPC分类号： A61K31/541 , A61K45/06
摘要： The present invention relates to a pharmaceutical composition for treating, for example, a disorder or condition selected from the group consisting of hypertension, depression, generalized anxiety disorder, phobias, posttraumatic stress disorder, avoidant personality disorder, sexual dysfunction, eating disorders, obesity, chemical dependencies, cluster headache, migraine, pain, Alzheimer’s disease, obsessive-compulsive disorder, panic disorder, memory disorders, Parkinson’s diseases, endocrine disorders, cerebellar ataxia, gastrointestinal tract disorders, negative symptoms of schizophrenia, premenstrual syndrome, Fibromyalgia Syndrome, stress incontinence, Tourette syndrome, trichotillomania, kleptomania, male impotence, cancer, chronic paroxysmal hemicrania and headache in a mammal, preferably a human, comprising (i) an atypical antipsychotic or a pharmaceutically acceptable salt thereof, (ii) a 5-HT 1B receptor antagonist or a pharmaceutically acceptable salt thereof, wherein the 5-HT 1B receptor antagonist is selected from the group consisting of (A) a compound of the formula I as described in the specification and (B) a compound of the formula II as described in the specification, and optionally (iii) a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及一种用于治疗例如选自高血压，抑郁症，广泛性焦虑症，恐惧症，创伤后应激障碍，避孕人格障碍，性功能障碍，进食障碍，肥胖症，化学依赖性，丛集性头痛，偏头痛，疼痛，阿尔茨海默病，强迫症，恐慌症，记忆障碍，帕金森病，内分泌紊乱，小脑共济失调，胃肠道疾病，精神分裂症阴性症状，经前综合征，纤维肌痛综合征，压力性尿失禁，尤其是哺乳动物（优选人）中的Tourette综合征，头发性短鞭毛虫，kleptomania，男性阳ence症，癌症，慢性阵发性高血压和头痛，包括（i）非典型抗精神病药或其药学上可接受的盐，（ii）5-HT1B受体拮抗剂或其药学上可接受的盐，其中5- HT1B受体拮抗剂选自（A）如说明书中所述的式I化合物和（B）如说明书中所述的式II化合物，和任选地（iii）药学上可接受的载体。

8. 发明申请

WO2005082370A1 COMBINATIONS OF AN ATYPICAL ANTIPSYCHOTIC AND AN AMINOMETHYLPYRIDYLOXYMETHYL/BENZISOXAZOLE AZABICYCLIC DERIVATIVES FOR TREATING CNS DISORDERS 审中-公开
标题翻译：复方抗惊厥药与用于治疗中枢神经系统疾病的氨基甲基吡咯烷基甲基苯甲酸唑烷偶联衍生物的组合
公开(公告)号：WO2005082370A1
公开(公告)日：2005-09-09
申请号：PCT/IB2005/000106
申请日：2005-01-17
申请人： PFIZER PRODUCTS INC. , BRODNEY, Michael, Aaron , HOWARD, Harry, Ralph, Jr.
发明人： BRODNEY, Michael, Aaron , HOWARD, Harry, Ralph, Jr.
IPC分类号： A61K31/498
CPC分类号： A61K31/496 , A61K31/498 , A61K31/551 , A61K31/5513 , A61K2300/00
摘要： An aminomethylpyridyloxymethyl/benzisoxazole substituted azabicyclic compound, a pharmaceutical composition same, and a method of treating one or more CNS or other disorders, including concurrent treatment of disorders such as a schizophrenia and depression.
摘要翻译：氨基甲基吡啶氧基甲基/苯并异恶唑取代的氮杂双环化合物，其药物组合物，以及治疗一种或多种CNS或其它病症的方法，包括同时治疗诸如精神分裂症和抑郁症等疾病。

9. 发明申请

WO2005113527A1 TETRAHYDRONAPHTHYL- PIPERAZINES AS 5-HT1B ANTAGONISTS, INVERSE AGONISTS AND PARTIAL AGONISTS 审中-公开
标题翻译：四氢叶酸作为5-HT1B拮抗剂，反相激动剂和部分促红细胞生成素
公开(公告)号：WO2005113527A1
公开(公告)日：2005-12-01
申请号：PCT/IB2005/001299
申请日：2005-05-09
申请人： PFIZER PRODUCTS INC. , BRODNEY, Michael, Aaron , COFFMAN, Karen, Jean
发明人： BRODNEY, Michael, Aaron , COFFMAN, Karen, Jean
IPC分类号： C07D295/04
CPC分类号： C07D213/40 , C07D211/26 , C07D213/38 , C07D213/64 , C07D213/74 , C07D213/75 , C07D213/79 , C07D213/80 , C07D213/82 , C07D217/24 , C07D231/40 , C07D239/42 , C07D285/135 , C07D295/03 , C07D295/033 , C07D295/073 , C07D295/096 , C07D295/135 , C07D295/155 , C07D295/192 , C07D307/52 , C07D317/60 , C07D319/18 , C07D405/04 , C07D471/04
摘要： The present invention relates to novel tetrahydronaphthylpiperazines derivatives, that are compounds of the formula (I) wherein R 1 , R 2 and R 6 are as defined herein, X is CH 2 or O, A is a group of the formula (G 1 , G 2 , G 2a , G 3 , G 4 , G 5 or G 6 ) depicted below, and D is a group of the formula (D), wherein Y, W and Z are C or N and wherein R 7 is as defined herein and their salts and compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT 1 ) receptors. Compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT 1 agonist or antagonist is indicated.
摘要翻译：本发明涉及新的四氢萘基哌嗪衍生物，其是式（I）的化合物，其中R 1，R 2和R 6如本文所定义，X是CH 2或O，A是式（G 1，G 2，G 2a，G 3，G 4，G 5或G 6）），D是式（D），其中Y，W和Z是C或N，并且其中R 7如本文所定义，以及它们的盐和组合物，其包括5-羟色胺1（5-HT1）受体的选择性拮抗剂，反向激动剂和部分激动剂。本发明的化合物可用于治疗或预防抑郁，焦虑，强迫症（OCD）以及其中指示5-HT1激动剂或拮抗剂的其它病症。

10. 发明申请

WO2005092864A1 IMIDAZOLE COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS 审中-公开
标题翻译：用于治疗神经损伤性疾病的咪唑化合物
公开(公告)号：WO2005092864A1
公开(公告)日：2005-10-06
申请号：PCT/IB2005/000659
申请日：2005-03-11
申请人： PFIZER PRODUCTS INC. , BRODNEY, Michael, Aaron , COFFMAN, Karen, Jean
发明人： BRODNEY, Michael, Aaron , COFFMAN, Karen, Jean
IPC分类号： C07D233/88
CPC分类号： C07D233/88 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds of the Formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and A are as defined. Compounds of the Formula (I) have activity inhibiting production of Aβ-peptide. The invention also relates to pharmaceutical compositions and methods for treating diseases and disorders, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer’s disease, in a mammal comprising compounds of the Formula (I).
摘要翻译：本发明涉及式（I）的化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和A是如定义。式（I）的化合物具有抑制Abeta肽生产的活性。本发明还涉及用于治疗疾病和障碍的药物组合物和方法，例如包含式（I）化合物的哺乳动物的神经变性和/或神经障碍，例如阿尔茨海默氏病。

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