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1. 发明申请

WO1994027966A1 PROCESS FOR PREPARING AND RESOLVING 2-PHENYL-3-AMINOPIPERIDINE 审中-公开
标题翻译：制备和分解2-苯基-3-氨基哌啶的方法
公开(公告)号：WO1994027966A1
公开(公告)日：1994-12-08
申请号：PCT/IB1994000059
申请日：1994-04-06
申请人： PFIZER INC. , SNYDER, William, M. , WATSON, Harry, A., Jr. , WILCOX, Glenn, E.
发明人： PFIZER INC.
IPC分类号： C07D211/56
CPC分类号： C07D211/56 , Y10S514/872
摘要： The present invention relates to a novel process for preparing and resolving 3-amino-2-phenylpiperidine and for synthesizing from the enantiomers of such compound certain pharmaceutically active substituted 2-phenyl-3-benzylaminopiperidines. The substituted 2-phenyl-3-benzylaminopiperidines that can be prepared by the processes of this invention are substance P receptor antagonists and are useful in the treatment and prevention of inflammatory and central nervous system disorders, as well as several other disorders.
摘要翻译：本发明涉及一种用于制备和分解3-氨基-2-苯基哌啶的新方法，并用于从该化合物的对映异构体合成某些药学活性的取代的2-苯基-3-苄基氨基哌啶。可以通过本发明的方法制备的取代的2-苯基-3-苄基氨基哌啶是物质P受体拮抗剂，可用于治疗和预防炎性和中枢神经系统疾病以及其它几种疾病。

2. 发明申请

WO1997000268A1 PROCESS FOR PREPARING DERIVATIVES OF AZABICYCLO NAPHTHYRIDINE CARBOXYLIC ACID COMPRISING A DIPEPTIDE 审中-公开
标题翻译：制备包含哌啶酮的亚硫酰基萘甲酸羧酸衍生物的方法
公开(公告)号：WO1997000268A1
公开(公告)日：1997-01-03
申请号：PCT/IB1996000257
申请日：1996-03-27
申请人： PFIZER INC. , BRAISH, Tamim, F. , CASTALDI, Michael, J. , WATSON, Harry, A., Jr.
发明人： PFIZER INC.
IPC分类号： C07K01/06
CPC分类号： C07K5/06191 , Y02P20/55
摘要： A novel process for preparing a prodrug acid, viz., 7-[(1 alpha , 6 alpha , 7 alpha )-6-(L-Ala-L-Ala-amino)-3-azabicyclo[3.1.0]hex-3-yl]-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, in the form of a pharmaceutically acceptable acid addition salt, is disclosed, which involves (1) treating an N-protected 7-[(1 alpha , 5 alpha , 6 alpha )-6-amino-3-azabicyclo[3.1.0]hex-3-yl]-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid C1-C4 alkyl ester, wherein the nitrogen-protecting group is benzyloxycarbonyl, C1-C4 alkoxycarbonyl or C1-C4 alkanoyl, with a strongly-protic acid to selectively remove the N-protecting group; (2) then condensing the resulting free amino ester compound with an N-protected L-alanyl-L-alanine dipeptide compound, wherein the N-protecting group is as previously defined, in the presence of a standard dehydrating agent to form the corresponding N-protected prodrug ester compound as the desired condensation product; and (3) thereafter hydrolyzing the intermediate N-protected prodrug ester in the presence of a pharmaceutically-acceptable strong acid to convert said N-protected prodrug ester to the desired naphthyridinone L-Ala-L-Ala prodrug acid final product, in the form of the corresponding pharmaceutically acceptable acid addition salt, indicated above. The latter prodrug acid final product is especially useful in the form of the corresponding methanesulfonic acid addition salt, which serves as a water-soluble prodrug companion to a known antibacterial agent, viz., 7-[(1 alpha , 5 alpha , 6 alpha )-6-amino-3-azabicyclo[3.1.0]hex-3-yl]-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1-naphthyridine-3-carboxylic acid.
摘要翻译：制备前体药物酸，即7 - [（1α，6α，7α）-6-（L-Ala-L-Ala-氨基）-3-氮杂双环[3.1.0] 吡啶-3-基] -6-氟-1-（2,4-二氟苯基）-1,4-二氢-4-氧代-1,8-二氮杂萘-3-羧酸，其为药学上可接受的酸加成盐，其涉及（1）处理N-保护的7 - [（1α，5α，6α）-6-氨基-3-氮杂双环[3.1.0]己-3-基] -6-氟 -1-（2,4-二氟苯基）-1,4-二氢-4-氧代-1,8-二氮杂萘-3-羧酸C1-C4烷基酯，其中氮保护基是苄氧羰基，C1-C4烷氧基羰基或C 1 -C 4烷酰基，用强质子酸选择性除去N-保护基; （2）然后将所得游离氨基酯化合物与N-保护的L-丙氨酰-L-丙氨酸二肽化合物缩合，其中N-保护基团如前所定义，在标准脱水剂存在下形成相应的N 保护的前药酯化合物作为所需的缩合产物; 和（3）然后在药学上可接受的强酸存在下水解中间体N-保护的前药酯，以将所述N-保护的前药酯转化为所需的萘啶酮L-Ala-L-Ala前药酸最终产物，形式的上述相应的药学上可接受的酸加成盐。后一种前药酸最终产物特别可用于相应的甲磺酸加成盐的形式，其用作已知抗菌剂的水溶性前体药物，即7 - [（1α，5α，6α 基）-6-氨基-3-氮杂双环[3.1.0]己-3-基] -6-氟-1-（2,4-二氟苯基）-1,4-二氢-4-氧代-1-萘-3- -羧酸。

3. 发明申请

WO1996006854A1 SPIROSTANYL GLYCOSIDAL CRYSTALS 审中-公开
公开(公告)号：WO1996006854A1
公开(公告)日：1996-03-07
申请号：PCT/IB1995000317
申请日：1995-05-04
申请人： PFIZER INC. , ALLEN, Douglas, J. , BUZON, Richard, A. , DENNINO, Michael, P. , WATSON, Harry, A., Jr. , ZUNG, Jonathan, B.
发明人： PFIZER INC.
IPC分类号： C07J71/00
CPC分类号： C07J71/0005 , Y10S514/824
摘要： Highly crystalline forms of (3 beta ,5 alpha ,25R)-3-[( beta -D-4",6"-bis-[2-fluorophenylcarbamoyl]cellobiosyl)oxy]-spirostan-12-one that are useful as hypocholesterolemic or antiatherosclerosis agents.
摘要翻译：可用作低胆固醇血症的（3β，5α，25R）-3 - [（β-D-4“，6” - 双 - [2-氟苯基氨基甲酰基]纤维素二糖基）氧基] - 螺甾烷-8-酮的高度结晶形式或抗动脉粥样硬化剂。

4. 发明申请

WO1994025479A1 SPIROSTANYL GLYCOSIDAL CRYSTALLINE MONOHYDRATE 审中-公开
标题翻译： SPIROSTANYL GLYCOSIDAL晶体单糖
公开(公告)号：WO1994025479A1
公开(公告)日：1994-11-10
申请号：PCT/US1994000446
申请日：1994-01-19
申请人： PFIZER INC. , ALLEN, Douglas, J., M. , WATSON, Harry, A., Jr , ZUNG, Jonathan, B.
发明人： PFIZER INC.
IPC分类号： C07J71/00
CPC分类号： C07J71/0005
摘要： A crystalline monohydrate of (3 beta , 5 alpha , 25R)-3-[( beta -D-cellobiosyl)oxy] spirostan-11-one that is useful as a hypocholesterolemic or antiatherosclerosis agent.
摘要翻译：可用作低胆固醇血症或抗动脉粥样硬化剂的（3β，5α，25R）-3 - [（β-D-纤维二糖基）氧]螺甾烷-11-酮的结晶一水合物。

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