公开(公告)号：EP1448509A4

公开(公告)日：2006-02-08

申请号：EP02776011

申请日：2002-09-26

申请人： EMISPHERE TECH INC

发明人： BERNADINO JOSEPH N

IPC分类号： C07C51/09 ,  C07C51/38 ,  C07C51/41 ,  C07C59/68 ,  C07C69/76

CPC分类号： C07C51/38 ,  C07C51/09 ,  C07C51/412 ,  C07C59/68

摘要： The present invention relates to a method of preparing a phenoxy alkanoic, alkenoic, or alkynoic acid or a salt thereof from a phenoxy containing compound via a dicarboxylate intermediate. The phenoxy alkanoic, alkenoic, and alkynoic acids and salts thereof prepared by this method are suitable for use in composition for delivering active agents via oral or other routes of administration to animals. Furthermore, the present invention relates to phenoxy dicarboxylic acids and their salts for delivering active agents, such as biologically or chemically active agents, to a target.

公开(公告)号：EP1284724A4

公开(公告)日：2007-10-17

申请号：EP01959913

申请日：2001-03-21

申请人： EMISPHERE TECH INC

发明人： BERNADINO JOSEPH N ,  O'TOOLE DORIS C ,  BAY WILLIAM E

IPC分类号： C07C231/12 ,  C07D265/36 ,  A61K45/00 ,  A61K47/16 ,  A61P1/04 ,  A61P3/00 ,  A61P3/02 ,  A61P5/06 ,  A61P7/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/12 ,  A61P11/06 ,  A61P13/00 ,  A61P15/00 ,  A61P19/08 ,  A61P19/10 ,  A61P31/00 ,  A61P35/00 ,  A61P37/02 ,  A61P37/08 ,  A61P43/00 ,  C07C235/60 ,  C07C269/00 ,  C07C271/64 ,  C07D265/22 ,  C07D265/26

CPC分类号： C07D265/22 ,  C07C231/12 ,  C07C235/60 ,  C07D265/26 ,  Y02P20/55

摘要： The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide via a dicarboxylated salicylamide intermediate. The present invention also relates to dicarboxylic salicylamide delivery agent compounds for the delivery of active agents. Methods of administration are provided as well.

公开(公告)号：EP1149066A4

公开(公告)日：2002-09-04

申请号：EP00911725

申请日：2000-02-04

申请人： EMISPHERE TECH INC

发明人： GSCHNEIDNER DAVID ,  BERNADINO JOSEPH N ,  BAY WILLIAM E

IPC分类号： A61K9/00 ,  A61K9/20 ,  A61K47/18 ,  C07C231/00 ,  C07C233/51 ,  C07C235/24 ,  C07C235/34 ,  C07C235/58 ,  C07C235/64 ,  C07C235/74 ,  C07C271/28 ,  C07C271/54 ,  C07C271/58 ,  C07C275/42 ,  C07C309/59 ,  C07C317/44 ,  C07D239/91 ,  C07D239/94 ,  C07D239/96 ,  C07D265/26 ,  C07D311/18 ,  C07D317/68 ,  C07C229/14

CPC分类号： A61K9/0014 ,  A61K9/0031 ,  A61K9/2013 ,  A61K47/18 ,  A61K47/183 ,  C07C231/00 ,  C07C233/51 ,  C07C235/24 ,  C07C235/34 ,  C07C235/64 ,  C07C235/74 ,  C07C271/28 ,  C07C271/54 ,  C07C271/58 ,  C07C275/42 ,  C07C309/59 ,  C07C317/44 ,  C07D239/91 ,  C07D239/94 ,  C07D239/96 ,  C07D265/26 ,  C07D311/18 ,  C07D317/68 ,  C07C235/58

摘要： The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide (hereinafter referred to as a 'protected/activated salicylamide'). The method comprises the steps of (a) alkylating the protected/activated salicylamide with an alkylating agent to form a protected/activated alkylated salicylamide, and (b) deprotecting and deactivating the protected/activated alkylated salicylamide, simultaneously or in any order, to form the alkylated salicylamide. The alkylated salicylamides prepared by this method are suitable for use in compositions for delivering active agents via oral or other routes of administration to animals.