EP 0374218 A4 19910911 - NOVEL TRANSDERMAL PENETRATION ENHANCERS
Title (en)
NOVEL TRANSDERMAL PENETRATION ENHANCERS
Publication
Application
Priority
US 17914488 A 19880408
Abstract (en)
[origin: WO8909800A1] This invention relates to compounds and a method for their use in carrying physiologically active agents through body membranes such as skin and for retaining these agents in body tissues. More specifically, the invention relates to carboxylic acid derivatives and salts thereof, which compounds are useful in topically administering a physiologically active agent to a human or animal via a composition comprising the agent and an effective amount of a compound represented in one embodiment by general formula (I), wherein W represents oxygen, sulfur, or two hydrogen radicals; wherein Z represents oxygen, sulfur, or -CH2-; wherein R represents alkyl optionally substituted with one to three double or triple bonds, -SR''', -OR''', -NHR''', -CH3, or COOR1, and wherein R1 represents hydrogen or lower alkyl; wherein R''' represents alkyl, alkylthioalkyl, alkoxyalkyl, substituted aminoalkyl, optionally substituted with a phenyl, benzoyl or heterocyclic group; wherein R' represents hydrogen, alkyl, alkoxy, acyloxy, alkylthio, hydroxy, -(CH2)yCOOR1 and with y being between zero and 3, inclusive; and wherein R'' represents hydrogen or -(CH2)yCOOR1 such that when R'' is hydrogen, then W is two hydrogen radicals and R' is not hydrogen; and when R' is hydrogen, then R'' is not hydrogen; and wherein m is between 1 and 5, preferably 2, 3, or 4, while n is between 1 and 24, preferably between 5 and 12, and x is zero or 1, inclusive. It has been found that physiologically active agents are carried through body membranes by the above penetration-enhancing agents and are retained in body tissue. The invention further relates to the penetration-enhancing agents themselves and the method of making such penetration-enhancing agents.
IPC 1-7
IPC 8 full level
C07D 295/14 (2006.01); A01N 25/00 (2006.01); A01N 25/30 (2006.01); A01N 37/44 (2006.01); A01N 43/36 (2006.01); A01N 43/40 (2006.01); A01N 43/46 (2006.01); A01N 43/62 (2006.01); A01N 43/84 (2006.01); A61K 8/00 (2006.01); A61K 8/44 (2006.01); A61K 8/49 (2006.01); A61K 31/40 (2006.01); A61K 31/401 (2006.01); A61K 31/4015 (2006.01); A61K 31/445 (2006.01); A61K 31/4465 (2006.01); A61K 31/45 (2006.01); A61K 31/55 (2006.01); A61K 45/00 (2006.01); A61K 47/22 (2006.01); A61P 43/00 (2006.01); A61Q 17/04 (2006.01); C05G 3/00 (2006.01); C07C 233/47 (2006.01); C07D 207/16 (2006.01); C07D 207/27 (2006.01); C07D 207/28 (2006.01); C07D 211/60 (2006.01); C07D 211/76 (2006.01); C07D 223/10 (2006.01); C07D 263/22 (2006.01); C07D 295/15 (2006.01); D06M 13/02 (2006.01); D06M 13/322 (2006.01); D06M 13/342 (2006.01); D06M 13/345 (2006.01); D06M 13/35 (2006.01); D06M 13/352 (2006.01); D06M 13/355 (2006.01); D06M 13/402 (2006.01); D06M 13/418 (2006.01); D06P 1/642 (2006.01); C07D 207/26 (2006.01)
CPC (source: EP KR)
A01N 37/44 (2013.01 - EP); A01N 43/36 (2013.01 - EP); A01N 43/40 (2013.01 - EP); A01N 43/46 (2013.01 - EP); A61K 9/0014 (2013.01 - EP); A61K 31/70 (2013.01 - KR); A61K 47/22 (2013.01 - EP); A61P 43/00 (2017.12 - EP); C05G 3/00 (2013.01 - EP); C07C 233/47 (2013.01 - EP); C07D 207/16 (2013.01 - EP); C07D 207/27 (2013.01 - EP); C07D 207/28 (2013.01 - EP); C07D 223/10 (2013.01 - EP); C07D 263/22 (2013.01 - EP); C07D 295/15 (2013.01 - EP); C09B 67/00 (2013.01 - KR); D06P 1/6426 (2013.01 - EP)
Citation (search report)
- [E] WO 8902735 A1 19890406 - NELSON RES & DEV [US], et al
- [XP] WO 8802626 A1 19880421 - NELSON RES & DEV [US]
- [X] WO 8704706 A1 19870813 - NELSON RES & DEV [US]
- [X] EP 0309624 A1 19890405 - NITTO DENKO CORP [JP]
- [X] GB 2192539 A 19880120 - CIBA GEIGY AG
- [X] DE 3536669 A1 19860430 - NITTO ELECTRIC IND CO [JP]
- [X] GB 2141025 A 19841212 - NITTO ELECTRIC IND CO
- [X] WO 8704346 A1 19870730 - JAVITT NORMAN B, et al
- [X] EP 0164998 A2 19851218 - ALLERGAN PHARMA [US]
- [X] CHEMICAL ABSTRACTS, vol. 104, no. 2, January 1986, page 311, abstract no. 10508b, Columbus, Ohio, US; J. HADGRAFT et al.. "Facilitated transport of sodium salicylate across an artificial lipid membrane by Azone", & J. PHARM. PHARMACOL. 1985, 37(10), 725-7
- See references of WO 8909800A1
Designated contracting state (EPC)
AT BE CH DE FR GB IT LI LU NL SE
DOCDB simple family (publication)
WO 8909800 A1 19891019; AU 3561689 A 19891103; AU 628344 B2 19920917; CA 1334646 C 19950307; EP 0374218 A1 19900627; EP 0374218 A4 19910911; JP 2965303 B2 19991018; JP H03500543 A 19910207; JP H11171795 A 19990629; KR 900700112 A 19900811
DOCDB simple family (application)
US 8901381 W 19890405; AU 3561689 A 19890405; CA 595603 A 19890404; EP 89905539 A 19890405; JP 26305998 A 19980917; JP 50521389 A 19890405; KR 890702292 A 19891207