公开(公告)号：EP0038541B1

公开(公告)日：1986-08-13

申请号：EP81102940.4

申请日：1981-04-16

申请人： Merck & Co., Inc.

发明人： Bodor, Nicholas S. ,  Sloan, Kenneth B. ,  Pogany, Stefano A.

IPC分类号： C07D207/16 ,  C07D213/89 ,  C07D473/38 ,  C07D239/60 ,  C07D233/84 ,  C07D239/26 ,  C07D295/20 ,  C07C149/22 ,  C07C149/20 ,  C07C149/24

CPC分类号： C07D239/42 ,  C07D207/16 ,  C07D233/84 ,  C07D239/38 ,  C07D307/88 ,  C07D473/38 ,  C07H19/16 ,  Y02P20/55 ,  Y10S514/863

公开(公告)号：EP0038541A1

公开(公告)日：1981-10-28

申请号：EP81102940.4

申请日：1981-04-16

申请人： Merck & Co., Inc.

发明人： Bodor, Nicholas S. ,  Sloan, Kenneth B. ,  Pogany, Stefano A.

IPC分类号： C07D207/16 ,  C07D213/89 ,  C07D473/38 ,  C07D239/60 ,  C07D233/84 ,  C07D239/26 ,  C07D295/20 ,  C07C149/22 ,  C07C149/20 ,  C07C149/24

CPC分类号： C07D239/42 ,  C07D207/16 ,  C07D233/84 ,  C07D239/38 ,  C07D307/88 ,  C07D473/38 ,  C07H19/16 ,  Y02P20/55 ,  Y10S514/863

摘要： Novel, transient prodrug forms of biologically active agents containing mercapto groups have (i) the structural formula:
wherein X is O, S or NR 5 ; R 1 S is the residue of any biologically active agent R'SH; R 2 is alkyl; aryl; cycloalkyl; alkenyl; cycloalkenyl; alkynynl; aralkyl, alkyryl, aralkenyl, aralkynyl, alkenylaryl, alkynylaryl, loweracyloxyalkyl, and caraboxyal- kyl, heterocyclic, either directly bonded to the carbonyl function or linked thereto via an alkylene bridge, and subsituted derivatives of the above; R 3 is hydrogen, R 2 , lower acyl, cyano, haloloweralkyl, carbamyl, -CH 2 ONO 2 and -CH 2 OCOR 2 ; R 5 is hydrogen or lower alkyl; and further wherein R 2 and R 3 may be taken together to form a cyclizing moiety with the provizo that when R'S is the residue of a sulfur containing amino acid, the X cannot be NR 5 ; (ii) the structural formula (I) wherein
is the residue of an amino acid, and (iii) the non-toxic, pharmaceutically acceptable salt thereof; process for preparing and therapeutically effective composition containing the same.