EP 0305496 A4 19890711 - TIMOLOL DERIVATIVES.
Title (en)
TIMOLOL DERIVATIVES.
Title (de)
TIMOLOL-DERIVATE.
Title (fr)
DERIVES DE TIMOLOL.
Publication
Application
Priority
- US 2661887 A 19870317
- US 16727688 A 19880311
Abstract (en)
[origin: WO8807044A1] Lipophilic, transient ester derivatives of timolol represented by general formula (I), wherein R1 represents a substituted or unsubstituted branched chain alkyl, straight or branched chain alkenyl, aryl, aralkyl or cycloalkyl group, a substituted or unsubstituted aromatic 5- or 6-membered heterocyclic ring containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, or a substituted or unsubstituted group of the formula R2-O-, wherein R2 is an alkyl, aryl, aralkyl or cycloalkyl group or of the formula R'2-CONH, wherein R'2 is an alkyl, aryl, aralkyl or cycloalkyl group, and nontoxic pharmaceutically acceptable acid addition salts thereof, are disclosed as prodrug forms of the anti-glaucoma drug timolol which are also useful in the treatment of glaucoma and increased intraocular pressure and which exhibit either improved corneal absorption and/or impeded conjunctival absorption characteristics, thus permitting the use of smaller doses of such derivatives than of timolol, thereby reducing systemic timolol concentration while achieving the same therapeutic effect.
IPC 1-7
IPC 8 full level
A61K 31/41 (2006.01); A61K 31/433 (2006.01); A61K 31/535 (2006.01); A61P 25/02 (2006.01); A61P 27/02 (2006.01); C07D 285/10 (2006.01); C07D 417/00 (2006.01); C07D 417/12 (2006.01)
CPC (source: EP)
A61P 25/02 (2017.12); A61P 27/02 (2017.12); C07D 285/10 (2013.01); C07D 417/12 (2013.01)
Citation (search report)
- No relevant documents have been disclosed.
- See references of WO 8807044A1
Designated contracting state (EPC)
DE FR GB IT SE
DOCDB simple family (publication)
WO 8807044 A1 19880922; EP 0305496 A1 19890308; EP 0305496 A4 19890711
DOCDB simple family (application)
US 8800793 W 19880317; EP 88903090 A 19880317