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1. 发明申请

WO1995007908A1 HETEROARYLAMINO AND HETEROARYLSULFONAMIDO SUBSTITUTED 3-BENZYLAMINOMETHYL PIPERIDINES AND RELATED COMPOUNDS 审中-公开
标题翻译：取代的三苯甲酰氨基哌啶及其相关化合物
公开(公告)号：WO1995007908A1
公开(公告)日：1995-03-23
申请号：PCT/IB1994000221
申请日：1994-07-18
申请人： PFIZER INC. , HOWARD, Harry, R., Jr.
发明人： PFIZER INC.
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： The present invention relates to novel heteroarylamino and heteroarylsulfonamido substituted 3-benzylaminomethylpiperidines and, specifically, to compounds of formula (I), wherein W, R , R , P and A are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formula (I) are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.
摘要翻译：本发明涉及新的杂芳基氨基和杂芳基磺酰氨基取代的3-苄基氨基甲基哌啶，具体地，涉及式（I）的化合物，其中W，R 1，R 3，P和A如说明书中所定义，用于合成这些化合物的中间体。式（I）的新型化合物可用于治疗炎性和中枢神经系统疾病以及其它疾病。

2. 发明申请

WO1994004496A1 SUBSTITUTED BENZYLAMINO NITROGEN CONTAINING NON-AROMATIC HETEROCYCLES 审中-公开
标题翻译：取代的苯甲酰胺含有非芳香杂环的氮
公开(公告)号：WO1994004496A1
公开(公告)日：1994-03-03
申请号：PCT/US1993004063
申请日：1993-05-05
申请人： PFIZER INC. , HOWARD, Harry, R., Jr. , IKUNAKA, Masaya , ITO, Fumitaka , LOWE, John, A., III , NAKANE, Masami , O'NEILL, Brian, T. , ROSEN, Terry, R. , SATAKE, Kunio
发明人： PFIZER INC.
IPC分类号： C07D211/56
CPC分类号： C07D401/12 , C07D211/56 , C07D417/12 , C07D453/02 , C07D487/08
摘要： The present invention relates to novel substituted benzylamino nitrogen containing non-aromatic heterocycles and, specifically, to compounds of formula (I) wherein W, R1, R2, R3 and A are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formula (I) are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.
摘要翻译：本发明涉及新的取代的苄基氨基氮的非芳族杂环，具体地说，涉及式（I）的化合物，其中W，R 1，R 2，R 3和A如说明书中所定义，以及用于合成这样的化合物。式（I）的新型化合物可用于治疗炎性和中枢神经系统疾病以及其它疾病。

3. 发明申请

WO1996000720A1 ARYL AND HETEROARYL ALKOXYNAPHTHALENE DERIVATIVES 审中-公开
标题翻译： ARYL和HETEROARYL ALKOXYNPHTHALENE DERIVATIVES
公开(公告)号：WO1996000720A1
公开(公告)日：1996-01-11
申请号：PCT/IB1995000381
申请日：1995-05-18
申请人： PFIZER INC. , CHENARD, Bertrand, L. , DESAI, Kishor, A. , HOWARD, Harry, R., Jr. , MACOR, John, E. , SHENK, Kevin, D.
发明人： PFIZER INC.
IPC分类号： C07C271/06
CPC分类号： C07D213/30 , C07D209/34 , C07D213/64 , C07D213/85 , C07D215/14 , C07D237/14 , C07D239/34 , C07D239/42 , C07D257/04 , C07D263/56 , C07D271/06 , C07D271/107 , C07D277/24 , C07D277/64 , C07D295/155 , C07D333/28 , C07D401/12 , C07D413/12 , C07D417/12
摘要： Compounds of formula (I) wherein R , R , R , R , R , R and R are defined as in the specification. These compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and antagonists.
摘要翻译：其中R 1，R 2，R 4，R 23，R 24，R 25和R 26的式（I）化合物如说明书中所定义。这些化合物是有用的精神治疗药物，是有效的5-羟色胺（5-HT1）激动剂和拮抗剂。

4. 发明申请

WO1995018129A1 DIAZABICYCLIC NEUROKININ ANTAGONISTS 审中-公开
公开(公告)号：WO1995018129A1
公开(公告)日：1995-07-06
申请号：PCT/IB1994000352
申请日：1994-11-14
申请人： PFIZER INC. , HOWARD, Harry, R., Jr. , SHENK, Kevin, D.
发明人： PFIZER INC.
IPC分类号： C07D471/08
CPC分类号： C07D471/08
摘要： The present invention relates to diazabicyclic compounds and, specifically, to compounds of formula (I), wherein A, G, R , R , R , R , R , R , and R are as defined in the specification. The compounds of formula (I) are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.
摘要翻译：本发明涉及二氮杂双环化合物，具体地涉及式（I）化合物，其中A，G，R 1，R 2，R 3，R 4，R 5，R 5， <6>和R 7如说明书中所定义。式（I）的化合物可用于治疗炎性和中枢神经系统疾病以及其它疾病。

5. 发明公开

EP1373231A1 3-HETEROCYCLYLPROPANOHYDROXAMIC ACID PCP INHIBITORS 有权
标题翻译： 3-杂环PROPANOHYDROXAMSÄURE衍生物作为抑制剂PCP
公开(公告)号：EP1373231A1
公开(公告)日：2004-01-02
申请号：EP02707045.7
申请日：2002-03-18
申请人： Pfizer Limited , PFIZER INC.
发明人： FISH, Paul Vincent , KENDALL, Jackie Diane , WHITLOCK, Gavin Alistair , PFIZER INC.
IPC分类号： C07D271/06 , A61K31/4245 , C07D413/12 , A61P17/02
CPC分类号： C07D263/34 , C07D271/06 , C07D271/07 , C07D413/12
摘要： Compounds of formula (I): (I), and their salts, solvates, prodrugs, etc., wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by PCP.

6. 发明授权

EP1373231B1 3-HETEROCYCLYL-PROPANO-HYDROXAMIC ACID AS PCP INHIBITORS 有权
标题翻译： 3-杂环PROPANOHYDROXAMSÄURE衍生物作为抑制剂PCP
公开(公告)号：EP1373231B1
公开(公告)日：2005-06-08
申请号：EP02707045.7
申请日：2002-03-18
申请人： Pfizer Limited , PFIZER INC.
发明人： FISH, Paul Vincent , KENDALL, Jackie Diane , WHITLOCK, Gavin Alistair , PFIZER INC.
IPC分类号： C07D271/06 , A61K31/4245 , C07D413/12 , A61P17/02
CPC分类号： C07D263/34 , C07D271/06 , C07D271/07 , C07D413/12
摘要： Compounds of formula (I): (I), and their salts, solvates, prodrugs, etc., wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by PCP.

7. 发明申请

WO1998030209A1 RAPIDLY RELEASING AND TASTE-MASKING PHARMACEUTICAL DOSAGE FORM 审中-公开
标题翻译：快速释放和吸收药物药物剂型
公开(公告)号：WO1998030209A1
公开(公告)日：1998-07-16
申请号：PCT/IB1997001471
申请日：1997-11-20
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC. , ITOH, Akinori , NIWA, Toshiyuki
发明人： PFIZER PHARMACEUTICALS INC. , PFIZER INC.
IPC分类号： A61K09/54
CPC分类号： A61K9/5078 , A61K9/1623 , A61K9/1652 , A61K9/5015 , A61K9/5026 , A61K9/5073
摘要： The present invention provides a rapidly releasing and taste-masking pharmaceutical dosage form comprising a core containing a pharmaceutically active ingredient, low-substituted hydroxypropyl cellulose and microcrystalline cellulose, the amount of the microcrystalline cellulose being at least 26.0 weight percent based on the total weight of the core; an inner coating layer formed on the core and containing a water-soluble polymer; and an outer coating layer formed on the inner coating layer and containing a saliva-insoluble polymer. A process for preparing such oral dosage form is also disclosed.
摘要翻译：本发明提供了一种快速释放和掩味的药物剂型，其包含含有药物活性成分，低取代羟丙基纤维素和微晶纤维素的核心，微晶纤维素的量基于总重量的至少26.0重量％核心; 形成在芯上并含有水溶性聚合物的内涂层; 以及形成在内涂层上并含有唾液不溶性聚合物的外涂层。还公开了制备这种口服剂型的方法。

8. 发明申请

WO1998023613A1 FUSED BICYCLIC PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：熔化的双相吡啶衍生物
公开(公告)号：WO1998023613A1
公开(公告)日：1998-06-04
申请号：PCT/IB1997001393
申请日：1997-11-05
申请人： PFIZER INC. , ARNOLD, Lee, Daniel , MOYER, Mikel, Paul , SOBOLOV-JAYNES, Susan, Beth
发明人： PFIZER INC.
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to compounds of formula (I) and to pharmaceutically acceptable salts thereof, wherein R , R and Z are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula (I) and to methods of using said compounds in the treatment of hyperproliferative diseases such as cancer.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，其中R 1，R 2和Z如本文所定义。本发明还涉及含有式（I）化合物的药物组合物以及使用所述化合物治疗过度增殖性疾病如癌症的方法。

9. 发明申请

WO1998023593A1 APO B-SECRETION/MTP INHIBITORY AMIDES 审中-公开
标题翻译： APO B分泌/ MTP抑制剂
公开(公告)号：WO1998023593A1
公开(公告)日：1998-06-04
申请号：PCT/IB1997001368
申请日：1997-11-03
申请人： PFIZER INC. , CHANG, George , QUALLICH, George, Joseph
发明人： PFIZER INC.
IPC分类号： C07D217/04
CPC分类号： C07D401/04 , C07D217/04 , C07D401/06 , C07D405/04 , C07D405/06 , C07D409/06 , C07D417/06
摘要： This invention is directed to compounds of formula (I) or the stereoisomers, pharmaceutically acceptable salts and hydrates thereof. The compounds are Apo B/MTP inhibitors and are useful in the treatment of various disorders and conditions such as atherosclerosis, pancreatitis, obesity, hypercholesteremia, hypertriglyceridemia, hyperlipidemia, and diabetes. The compounds of this invention are also useful in combination with other pharmaceutical agents including cholesterol biosynthesis inhibitors and cholesterol absorption inhibitors, especially HMG-CoA reductase inhibitors and HMG-CoA synthase inhibitors; HMG-CoA reductase gene expression inhibitors; CETP inhibitors; bile acid sequestrants; fibrates; cholesterol absorption inhibitors; ACAT inhibitors, squalene synthetase inhibitors, ion-exchange resins, anti-oxidants and niacin. This invention is also directed to intermediates and processes useful in the preparation of compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物或其立体异构体，其药学上可接受的盐和水合物。这些化合物是Apo B / MTP抑制剂，可用于治疗各种疾病和病症如动脉粥样硬化，胰腺炎，肥胖症，高胆固醇血症，高甘油三酯血症，高脂血症和糖尿病。本发明的化合物还可与其它药剂组合使用，包括胆固醇生物合成抑制剂和胆固醇吸收抑制剂，特别是HMG-CoA还原酶抑制剂和HMG-CoA合成酶抑制剂; HMG-CoA还原酶基因表达抑制剂; CETP抑制剂; 胆汁酸螯合剂贝特类药物; 胆固醇吸收抑制剂; ACAT抑制剂，角鲨烯合成酶抑制剂，离子交换树脂，抗氧化剂和烟酸。本发明还涉及可用于制备式（I）化合物的中间体和方法。

10. 发明申请

WO1998012177A1 PYRROLIDINYL AND PYRROLINYL ETHYLAMINE COMPOUNDS AS KAPPA AGONISTS 审中-公开
标题翻译：吡咯烷酮和吡咯烷酮化合物作为KAPPA激动剂
公开(公告)号：WO1998012177A1
公开(公告)日：1998-03-26
申请号：PCT/IB1997001021
申请日：1997-08-21
申请人： PFIZER INC. , PFIZER PHARMACEUTICALS INC. , ITO, Fumitaka , KONDO, Hiroshi
发明人： PFIZER INC. , PFIZER PHARMACEUTICALS INC.
IPC分类号： C07D207/12
CPC分类号： C07D213/82 , C07D207/10 , C07D207/12 , C07D207/20 , C07D207/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , Y02P20/55
摘要： A compound of formula (I) and the salts thereof, wherein A is halo, hydroxy or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar is optionally substituted phenyl or the like; Ar is aryl or heteroaryl selected from phenyl, naphthyl, pyridyl and the like, the aryl or heteroaryl being optionally substituted; R is hydrogen, hydroxy, C1-C4 alkyl or the like; and R and R are independently selected from optionally substituted C1-C7 alkyl C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl and the like or R and R , together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.
摘要翻译：式（I）化合物及其盐，其中A为卤素，羟基等; 虚线表示任选的双键，条件是如果虚线是双键，则A不存在; Ar 1是任选取代的苯基等; Ar 2是选自苯基，萘基，吡啶基等的芳基或杂芳基，芳基或杂芳基任选被取代; R 1是氢，羟基，C 1 -C 4烷基等; R 2和R 3独立地选自任选取代的C 1 -C 7烷基C 3 -C 6环烷基，C 2 -C 6烯基，C 2 -C 6炔基等或R 2和R 3连同它们所连接的氮原子形成任选取代的吡咯烷，哌啶或吗啉环。这些化合物可用作κ激动剂。

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