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1. 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。

2. 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).

3. 发明申请

WO2005007655A1 NICOTINE ADDICTION REDUCING HETEROARYL FUSED AZAPOLYCYCLIC COMPOUNDS 审中-公开
标题翻译：尼古丁加入减少异氟醚融合的化合物
公开(公告)号：WO2005007655A1
公开(公告)日：2005-01-27
申请号：PCT/IB2004/002261
申请日：2004-07-08
申请人： PFIZER PRODUCTS INC. , ALLEN, Martin, Patrick , COE, Jotham, Wadsworth , LIRAS, Spiros , O'DONNELL, Christopher, John , O'NEILL, Brian, Thomas
发明人： ALLEN, Martin, Patrick , COE, Jotham, Wadsworth , LIRAS, Spiros , O'DONNELL, Christopher, John , O'NEILL, Brian, Thomas
IPC分类号： C07D471/08
CPC分类号： C07D471/08
摘要： The present invention provides a compound having the structure of formula (I): wherein R 1 is hydrogen, (C 1 -C 6 ) alkyl, unconjugated (C 3 -C 6 ) alkenyl, benzyl, YC(=O)(C 1 -C 6 ) alkyl or -CH 2 CH 2 -O-(C 1 -C 4 ) alkyl; X is CH 2 or CH 2 CH 2 ; Y is (C 2 -C 6 ) alkylene; Z is (CH 2 ) m , CF 2 , or C(=O), where m is 0, 1 or 2; R 2 and R 3 are selected independently from hydrogen, halogen, - (C 1 -C 6 ) alkyl optionally substituted with from 1 to 7 halogen atoms, and -O(C 1 -C 6 ) alkyl optionally substituted with from 1 to 7 halogen atoms, or R 2 and R 3 each together with the atom to which it is connected independently form C(=O), S→O , S(=O) 2 , or N→O; and Het is a 5- to 7- membered monocyclic heteroaryl group selected from pyridinyl, pyridone, pyridazinyl, imidazolyl, pyrimidinyl, pyrazolyl, triazolyl, pyrazinyl, furyl, thienyl, isoxazolyl, thiazolyl, oxazolyl, isothiazolyl, pyrrolyl, cinnolinyl, triazinyl, oxadiazolyl, thiadiazolyl and furazanyl groups. The compounds can be used to treat disease states mediated by neuronal nicotinic acetylcholine specific receptor sites.
摘要翻译：本发明提供具有式（I）结构的化合物：其中R 1是氢，（C 1 -C 6）烷基，未结合的（C 3 -C 6）烯基，苄基，YC（= O）（C 1 -C 6）烷基或-CH 2 CH 2 -O-（C 1 -C 4）烷基; X是CH 2或CH 2 CH 2; Y是（C 2 -C 6）亚烷基; Z是（CH 2）m，CF 2或C（= O），其中m是0,1或2; R 2和R 3独立地选自氢，卤素，任选被1至7个卤素原子取代的 - （C 1 -C 6）烷基和任选被1至7个取代的-O（C 1 -C 6）烷基卤素原子或R 2和R 3各自与其连接的原子一起独立地形成C（= O），S-> O，S（= O）2或N-> O; 吡啶基，咪唑基，嘧啶基，吡唑基，三唑基，吡嗪基，呋喃基，噻唑基，异恶唑基，噻唑基，恶唑基，异噻唑基，吡咯基，噌啉基，三嗪基，恶二唑基，噻二唑基和呋咱基。该化合物可用于治疗由神经元烟碱乙酰胆碱特异性受体位点介导的疾病状态。

4. 发明申请

WO2007060526A1 SUBSTITUTED AZACYCLOALKANES USEFUL FOR TREATING CNS CONDITIONS 审中-公开
标题翻译：用于治疗CNS病症的替代AZACYCLOALKANES有用
公开(公告)号：WO2007060526A1
公开(公告)日：2007-05-31
申请号：PCT/IB2006/003318
申请日：2006-11-10
申请人： PFIZER PRODUCTS INC. , BOYD, James, Gorham , BUTLER, Todd, William , O'NEILL, Brian, Thomas
发明人： BOYD, James, Gorham , BUTLER, Todd, William , O'NEILL, Brian, Thomas
IPC分类号： C07D205/04 , C07D207/14 , C07D207/48 , C07D211/58 , C07D211/64 , C07D211/76 , A61K31/4439 , A61K31/4468 , A61K31/45 , A61P25/00 , C07D213/38 , C07D239/42 , C07D277/42 , C07D263/58 , A61K31/506
CPC分类号： C07D211/58 , C07D205/04 , C07D207/14 , C07D211/76 , C07D239/42 , C07D263/58 , C07D401/04 , C07D417/04
摘要： The invention relates to substituted azacycloalkaπe compounds useful in treating conditions of the Central Nervous System (CNS); a pharmaceutical composition comprising same; a method of treating such conditions and of treating conditions in which inhibition of beta-secretase is indicated.
摘要翻译：本发明涉及可用于治疗中枢神经系统（CNS）的病症的取代的氮杂环烷基化合物; 包含该组合物的药物组合物; 治疗这些病症的方法以及治疗其中表达β-分泌酶抑制的病症。

5. 发明申请

WO2005110987A1 PIPERIDINE DERIVATIVES AS NK1 AND NK3 ANTAGONISTS 审中-公开
标题翻译：哌啶衍生物作为NK1和NK3拮抗剂
公开(公告)号：WO2005110987A1
公开(公告)日：2005-11-24
申请号：PCT/IB2005/001198
申请日：2005-04-29
申请人： PFIZER PRODUCTS INC. , O'NEILL, Brian, Thomas , PARIKH, Vinod, Dipak , WELCH, Willard, McKowan, Jr.
发明人： O'NEILL, Brian, Thomas , PARIKH, Vinod, Dipak , WELCH, Willard, McKowan, Jr.
IPC分类号： C07D211/46
CPC分类号： C07D211/46 , C07D211/58 , C07D211/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/06
摘要： The invention relates to compounds according to formula I exhibiting neurokinin inhibitory properties, a pharmaceutical composition comprising, same and a method of treatment for neurokinin-mediated conditions. Formula (I) or a pharmaceutically acceptable salt or solvate thereof wherein: m , =0 or 1; n =0 or 1; s=0 or 1; L is -O- or -N(R 4 )-; R 1 and R 2 are each independently H, aryl, heteroaryl, -(C 1 -C 6 )atkylheterocyloalkyl, -(C 1 -C 6 )alkylheterocycloalkyl, -(C 1- C 6 )alkylheteroaryl, -(C 1- C 6 )alkyl-O-aryl, -(C 1- C 6 )alkylaryl, and -CH 2 N(R 4 )(R 5 ), wherein each of said heterocyloalkyl, -(C 1- C 6 )alkylheterocycloalkyl, -(C 1- C 6 )alkylheteroaryl, -(C 1- C 6 )alkyl-0-aryl, aryl, -(C 1- C 6 )alkylaryl, heteroaryl, and -CH 2 N(R 4 )(R 5 ), is optionally substituted with 1-3 moieties independently selected from X', Y' or Z'; R 3 is H, CF 3 , OH, or-(C 1- C 6 )alkyl; R 4 , and R 5 , are each independently selected from H, -(C 1- C 6 )alkyl, or -(C 1- C 6 )(C=0)R 7 ; R 7 is (C 1- C 6 )alkyl, OH, -N(R 4 )(R), or -OR 4 ; R 8 and R 9 are each independently (C 1- C 6 )alkyl; X, Y, X', Y' and Z' are each independently selected from H, -(C 1- C 6 )alkyl, -(C 1- C 6 )alkyl-NR 4 R 5 , CF 3 , OH, -O-(C 1- C 6 )alkyl, -(C 1- C 6 )alkyl-C(=0)R 7 , aryl, heteroaryl, cycloalkyl, -N0 2 , -(C 1- C 6 )alkylaryl, -0-aryl, halogen, CN, -CH 3 N(R 4 )(R5), -C(=O)R 7 , -C(=O)R 7 , -R 6 C(=0)R 7 or -R 6 C(=O)NR 4 R 5 ; and R 6 is a bond, -CH 2 -, -0-, or -NR 4 .
摘要翻译：本发明涉及具有神经激肽抑制特性的式I化合物，包含与神经激肽介导的病症相同的治疗方法的药物组合物。式（I）或其药学上可接受的盐或溶剂合物，其中：m = 0或1; n = 0或1; s = 0或1; L是-O-或-N（R 4） - ; R 1和R 2各自独立地为H，芳基，杂芳基， - （C 1 -C 6）烷基杂烷基烷基， - （C 1 -C 6）烷基杂环烷基， - （C 1 -C 6）烷基杂芳基 - （（C 1 -C 6）烷基芳基和-CH 2 N（R 4）（R 5），其中每个所述杂烷基烷基， - （C1-C6）烷基杂环烷基， - （C 1 -C 6）烷基杂芳基， - （C 1 -C 6）烷基-O-芳基，芳基， - （C 1 -C 6）烷基芳基，杂芳基和-CH 2 N（R 4）（R 5）任选被1-3个独立地选自X'，Y'或Z'的部分取代; R 3是H，CF 3，OH或 - （C 1 -C 6）烷基; R 4和R 5各自独立地选自H， - （C 1 -C 6）烷基或 - （C 1 -C 6）（C = O）R 7; R 7是（C 1 -C 6）烷基，OH，-N（R 4）（R）或-OR 4; R 8和R 9各自独立地为（C 1 -C 6）烷基; X，Y，X'，Y'和Z'各自独立地选自H， - （C 1 -C 6）烷基， - （C 1 -C 6）烷基-NR 4 R 5， -O-（C 1 -C 6）烷基， - （C 1 -C 6）烷基-C（= O）R 7，芳基，杂芳基，环烷基，-NO 2， - （C 1 -C 6）烷基芳基，卤素，CN，-CH 3 N（R 4）（R 5），-C（= O）R 7，-C（= O）R 7，-R 6 C（= O）或R 6 C（= O）NR 4 R 5; 并且R 6是键，-CH 2 - ， - O-或-NR 4。

6. 发明申请

WO2004024729A1 DIAZABICYCLIC COMPOUNDS USEFUL IN THE TREATMENT OF CNS AND OTHER DISORDERS 审中-公开
标题翻译：用于治疗CNS和其他疾病的双胍化合物
公开(公告)号：WO2004024729A1
公开(公告)日：2004-03-25
申请号：PCT/IB2003/003795
申请日：2003-08-29
申请人： PFIZER PRODUCTS INC. , O'DONELL, Christopher, John , VINCENT, Lawrence, Albert , O'NEILL, Brian, Thomas , COE, Jotham, Wadsworth
发明人： O'DONELL, Christopher, John , VINCENT, Lawrence, Albert , O'NEILL, Brian, Thomas , COE, Jotham, Wadsworth
IPC分类号： C07D487/08
CPC分类号： C07D487/08
摘要： The present invention relates to a compounds of formula (I): wherein A, B, D, E and F are defined herein; that are useful in treating central nervous system (CNS) diseases, disorders and conditions, such as but not limited to nicotine addiction, schizophrenia, depression, Alzheimer's disease, Parkinson's disease and ADHD. The present invention further comprises pharmaceutical compositions containing such compounds and methods of treatment comprising the use of such compounds.
摘要翻译：本发明涉及式（I）化合物：其中A，B，D，E和F如本文所定义; 可用于治疗中枢神经系统（CNS）疾病，疾病和病症，例如但不限于尼古丁成瘾，精神分裂症，抑郁症，阿尔茨海默病，帕金森病和ADHD。本发明还包含含有这些化合物的药物组合物和包括使用这些化合物的治疗方法。

7. 发明申请

WO2006061711A1 1, 2, 3, 3A, 8, 8A-HEXAHYDRO-2, 7A-DIADA-CYCLOPENTA [A] INDEN-7-ONE DERIVATIVES WHICH BIND TO NEURONAL NICOTINIC ACETYLCHOLINE SPECIFIC RECEPTOR SITES AND ARE USEFUL IN MODULATING CHOLINERGIC FUNCTION AND IN THE TREATMENT OF ADDICTIVE DISORDERS 审中-公开
标题翻译： 1,2,3,4,8-8A-HEXAHYDRO-2,7A-DIADA-CYCLOPENTA [A]茚-7-酮衍生物，其与神经酰胺基乙酰基特异性受体位点结合，并且有助于调节胆碱功能和治疗接触性疾病
公开(公告)号：WO2006061711A1
公开(公告)日：2006-06-15
申请号：PCT/IB2005/003730
申请日：2005-11-30
申请人： PFIZER PRODUCTS INC. , O'NEILL, Brian, Thomas , PROCKO, Kristen , YOHANNES, Daniel
发明人： O'NEILL, Brian, Thomas , PROCKO, Kristen , YOHANNES, Daniel
IPC分类号： C07D471/14 , A61P25/34
CPC分类号： C07D471/14
摘要： The present invention relates to novel fused bicyclicpyrrolidine pyridone compounds of the formula (I) wherein R, R P and n are as defined herein, their pharmaceutically acceptable salts, pharmaceutical compositions and their use in treating addictive disorders such as the use of tobacco or other nicotine containing products and in the treatment of neurological and mental disorders related to a decrease in cholinergic function.
摘要翻译：本发明涉及式（I）的新型稠合双环吡咯烷吡啶酮化合物，其中R，R p和n如本文所定义，其药学上可接受的盐，药物组合物及其在治疗成瘾性疾病中的用途作为使用烟草或其他含尼古丁的产品和用于治疗与胆碱能功能降低相关的神经和精神障碍。

8. 发明申请

WO2005018622A1 A PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF OBESITY OR TO FACILITATE OR PROMOTE WEIGHT LOSS 审中-公开
标题翻译：用于治疗肥胖或促进重量损失的药物组合物
公开(公告)号：WO2005018622A1
公开(公告)日：2005-03-03
申请号：PCT/IB2004/002604
申请日：2004-08-09
申请人： PFIZER PRODUCTS INC. , COE, Jotham, Wadsworth , O'NEILL, Brian, Thomas , SANDS, Steven, Bradley
发明人： COE, Jotham, Wadsworth , O'NEILL, Brian, Thomas , SANDS, Steven, Bradley
IPC分类号： A61K31/00
CPC分类号： A61K45/06 , A61K31/195 , A61K2300/00
摘要： Pharmaceutical compositions are disclosed for the treatment of obesity, an overweight condition and compulsive overeating. The pharmaceutical compositions are comprised of a therapeutically effective combination of a nicotinic receptor partial agonist and an alpha2dela ligand and a pharmaceutically acceptable carrier. The method of using these compounds is also disclosed.
摘要翻译：公开了用于治疗肥胖，超重状况和强迫性暴饮暴食的药物组合物。药物组合物由烟碱受体部分激动剂和α2dela配体和药学上可接受的载体的治疗有效组合组成。还公开了使用这些化合物的方法。

9. 发明申请

WO2004110996A1 NK1 ANTAGONIST 审中-公开
公开(公告)号：WO2004110996A1
公开(公告)日：2004-12-23
申请号：PCT/IB2004/001910
申请日：2004-06-07
申请人： PFIZER PRODUCTS INC. , WAGER, Travis, T. , WELCH, Willard, McKowan, Jr. , O'NEILL, Brian, Thomas
发明人： WAGER, Travis, T. , WELCH, Willard, McKowan, Jr. , O'NEILL, Brian, Thomas
IPC分类号： C07D207/16
CPC分类号： C07D207/08 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/56 , C07D211/60 , C07D401/06 , C07D403/06 , C07D471/08 , C07D487/04
摘要： The invention is to a compound exhibiting neurokinin inhibitory properties, a pharmaceutical composition comprising same and a method of treatment for neurokinin-meditated conditions.Formula (I)
摘要翻译：本发明涉及显示神经激肽抑制性质的化合物，包含其的药物组合物和治疗神经激肽抑制状态的方法。（I）

10. 发明公开

EP2300484A1 NOVEL CLASS OF SPIRO PIPERIDINES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES 有权
标题翻译：用于治疗神经变性疾病螺哌啶类新
公开(公告)号：EP2300484A1
公开(公告)日：2011-03-30
申请号：EP09742523.5
申请日：2009-05-04
申请人： Pfizer Inc.
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.

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