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1. 发明申请

WO1990002123A1 AMINO-SUBSTITUTED BRIDGED AZABICYCLIC QUINOLONE CARBOXYLIC ACIDS AND ESTERS 审中-公开
标题翻译：氨基取代的桥联喹啉酮羧酸和酯
公开(公告)号：WO1990002123A1
公开(公告)日：1990-03-08
申请号：PCT/US1988002908
申请日：1988-08-23
申请人： PFIZER INC. , KLEINMAN, Edward, Fox
发明人： PFIZER INC.
IPC分类号： C07D401/04
CPC分类号： C07D453/06
摘要： Compounds of formula (I), wherein R1 is hydrogen, C¿1?-C6 alkyl, or a pharmaceutically acceptable cation; Y is cyclopropyl, ethyl or p-fluorophenyl, and X is hydrogen or fluoro, or X and Y taken together form a group α or β; and R?2¿ is γ wherein R3 is hydrogen or C¿1?-C4 alkyl; or a pharmaceutically acceptable salt thereof. Also disclosed are antibacterial pharmaceutical compositions comprising the foregoing compounds, methods of using the compounds in treating bacterial infections, and intermediates for the preparation of the compounds.

2. 发明申请

WO1989000158A1 BRIDGED-DIAZABICYCLOALKYL QUINOLONE CARBOXYLIC ACIDS AND ESTERS 审中-公开
标题翻译：桥联二氮杂环戊烯酮羧酸和酯
公开(公告)号：WO1989000158A1
公开(公告)日：1989-01-12
申请号：PCT/US1987001583
申请日：1987-07-02
申请人： PFIZER INC. , KLEINMAN, Edward, Fox
发明人： PFIZER INC.
IPC分类号： C07D215/22
CPC分类号： C07D471/08
摘要： Compounds of formula (I) and pharmaceutically acceptable acid addition salts thereof, wherein R1 is hydrogen, (C1-C6) alkyl, or a pharmaceutically acceptable cation; R2 is ethyl, fluoroethyl, p-fluorophenyl, p-hydroxyphenyl or cyclopropyl; R3 is fluorine or hydrogen; and R4 is (a) or (b), wherein n is 1 or 2 and R5 is hydrogen or (C1-C3)alkyl are disclosed. Also disclosed are antibacterial pharmaceutical compositions comprising the foregoing compounds, methods of using the compounds in treating bacterial infections, and intermediates for the preparation of the compounds.

3. 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.

4. 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.

5. 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。

6. 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。

7. 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。

8. 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。

9. 发明申请

WO1998008846A1 SUBSTITUTED 6,6-HETERO-BICYCLIC DERIVATIVES 审中-公开
标题翻译：取代的6,6-杂双环衍生物
公开(公告)号：WO1998008846A1
公开(公告)日：1998-03-05
申请号：PCT/IB1997000904
申请日：1997-07-21
申请人： PFIZER INC. , CHEN, Yuhpyng, Liang
发明人： PFIZER INC.
IPC分类号： C07D471/04
CPC分类号： C07D215/233 , C07D215/18 , C07D215/42 , C07D405/12 , C07D471/04 , C07D475/02
摘要： This invention relates to compounds of formula (I), wherein A, B, D, E, K, G, R and R are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds. Compounds (I) are corticotropin releasing factor (hormone) CRF (CRH) antagonists.
摘要翻译：本发明涉及式（I）化合物，其中A，B，D，E，K，G，R 3和R 5如说明书中所定义，以及这些化合物的药学上可接受的盐。化合物（I）是促肾上腺皮质激素释放因子（激素）CRF（CRH）拮抗剂。

10. 发明申请

WO1998008835A1 SPIROCYCLIC DOPAMINE RECEPTOR SUBTYPE LIGANDS 审中-公开
标题翻译：螺旋多巴胺受体亚型配体
公开(公告)号：WO1998008835A1
公开(公告)日：1998-03-05
申请号：PCT/IB1997000978
申请日：1997-08-08
申请人： PFIZER INC. , BUTLER, Todd, William , FLIRI, Anton, Franz, Joseph
发明人： PFIZER INC.
IPC分类号： C07D307/94
CPC分类号： C07D295/073 , C07D295/112 , C07D295/155 , C07D307/94 , C07D333/50 , C07D333/58
摘要： This invention relates to novel, pharmaceutically active compounds of formula (I) wherein a, b and R through R are defined as in the specification. These compounds exhibit central dopaminergic activity and are useful in the treatment of CNS disorders.
摘要翻译：本发明涉及式（I）的新的药物活性化合物，其中a，b和R 1至R 6如说明书中所定义。这些化合物表现出中枢多巴胺能活性，可用于治疗CNS疾病。

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