公开(公告)号：EP1243576A4

公开(公告)日：2004-05-06

申请号：EP00905281

申请日：2000-02-23

申请人： DAINIPPON PHARMACEUTICAL CO

发明人： SATO FUMINORI ,  OMODANI TOMOKI ,  SHIRATAKE RYOTARO ,  INOUE YASUNAO ,  DEGUCHI TAKASHI

IPC分类号： C07C213/02 ,  C07C215/08 ,  C07C269/06 ,  C07C271/16

CPC分类号： C07C213/02 ,  C07C269/06 ,  Y02P20/55 ,  C07C215/08 ,  C07C271/16

摘要： Processes for industrially producing (aminomethyl)trifluoromethylcarbinol derivatives (I), in particular, optically active compounds, which are useful as materials for producing drugs such as proteases. A process for producing the compound (I) characterized by starting with a 1,3-oxazolidin-5-one derivative (III), which is easily derived from an α-amino acid, and effecting the reaction either stepwise or in one spot; and another process for producing compound (I) characterized by reducing a 5-hydroxy compound (II): a: trialkyl; b: reduction wherein R1 represents a group corresponding to a side chain moiety of a natural or unnatural α-amino acid; and R2 represents hydrogen or R21 (wherein R21 represents an amino-protective group having carbonyl at the binding site to the nitrogen atom).

公开(公告)号：EP1157998A4

公开(公告)日：2003-01-29

申请号：EP00905282

申请日：2000-02-23

申请人： DAINIPPON PHARMACEUTICAL CO

发明人： SATO FUMINORI ,  INOUE YASUNAO ,  OMODANI TOMOKI ,  SHIRATAKE RYOTARO ,  HONDA SEIJI ,  KOMIYA MASANOBU ,  TAKEMURA TADASHI

IPC分类号： A61K38/00 ,  A61K31/00 ,  A61K31/495 ,  A61K31/506 ,  A61P11/00 ,  A61P11/06 ,  A61P29/00 ,  A61P43/00 ,  C07D403/12 ,  C07D413/14 ,  C07K5/02 ,  C07K5/083 ,  C07K5/097 ,  C07K5/103 ,  C07K5/117 ,  A61K38/55 ,  C07D233/34 ,  C07D239/54

CPC分类号： C07D403/12 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/0222 ,  C07K5/0806 ,  C07K5/0821 ,  C07K5/1008

摘要： Heterocyclic compounds represented by general formula (I-a), its esters or salts thereof; and human neutrophilic elastase inhibitors, etc. containing the same as the active ingredient wherein A and B are the same of different and each represents lower alkylene optionally substituted by oxo; D represents a monocyclic or dicyclic heterocyclic group optionally substituted by oxo; R?1 and R2¿ are the same or different and each represents lower alkyl; R?3 and R4¿ are different from each other and each represents hydrogen or hydroxy, or R?3 and R4¿ form together oxo; and R5 represents 2-benzoxasolyl, trifluoromethyl, benzylaminocarbonyle, etc.