EP 0550444 A4 19930303 - SUBSTITUTED NAPHTHOXAZINES USEFUL AS DOPAMINERGICS.
Title (en)
SUBSTITUTED NAPHTHOXAZINES USEFUL AS DOPAMINERGICS.
Title (de)
SUBSTITUIERTE NAPHTHOXAZINE ALS DOPAMINERGE MITTEL.
Title (fr)
NAPHTOXAZINES SUBSTITUEES UTILES COMME DOPAMINERGIQUES.
Publication
Application
Priority
US 53884790 A 19900615
Abstract (en)
[origin: WO9119719A1] The present invention comprises the compounds selected from the group of compounds represented by formula (1), wherein R1 and R2 are selected from the group consisting of H and OA, wherein A is H or is selected from the group consisting of hydrocarbyl radicals having from 1 to about 12 carbon atoms, or A is -COR5, -CONHR5, or -COOR5, wherein R5 is selected from the group consisting of hydrocarbyl radicals having between 1 and about 12 carbon atoms and wherein R1, R2 and R5 are optionally substituted with one or more halogen atoms; X is selected from the group consisting of CH2, oxygen, sulfur, NH or NR3, wherein R3 is a lower alkyl radical having from 1 to about 4 carbon atoms; R4 is selected from the group consisting of H, R3, COOR6, and -(CH2)n2-CH(R7)-Ar, wherein R6 is H or R3, n is 0 or an integer of from 1 to about 4, R7 is selected from the group consisting of R3, OR3, OCOR3 and H, and Ar is selected from the group consisting of radicals represented by general formulae: (a), (b), (c), (d), (e), (f), (g), wherein Y is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and heteroatom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur, and phosphorous and said hydrocarbyl radicals comprise from 1 to about 12 carbon atoms, a is 0 or an integer of from 1 to 2, W is oxygen, sulfur or nitrogen and Z represents two hydrogen radicals, oxygen or sulfur; with the proviso that when Z represents 2 hydrogen radicals, then R4 cannot be H, and pharmaceutical compositions comprising said compounds and a pharmaceutically-acceptable vehicle. Said compounds and compositions are effective for inducing a dopaminergic response in a subject, e.g., a mammal, and are useful for alleviating glaucoma, parkinsonism, etc., and inducing weight loss.
IPC 1-7
IPC 8 full level
A61K 31/47 (2006.01); A61K 31/473 (2006.01); A61K 31/495 (2006.01); A61K 31/535 (2006.01); A61K 31/538 (2006.01); A61K 31/54 (2006.01); A61K 31/5415 (2006.01); A61P 3/04 (2006.01); A61P 25/00 (2006.01); A61P 25/18 (2006.01); A61P 27/02 (2006.01); C07D 221/10 (2006.01); C07D 241/36 (2006.01); C07D 241/38 (2006.01); C07D 265/34 (2006.01); C07D 279/14 (2006.01); C07D 401/04 (2006.01); C07D 405/04 (2006.01); C07D 409/04 (2006.01); C07D 413/04 (2006.01); C07D 413/06 (2006.01); C07D 417/04 (2006.01)
CPC (source: EP)
A61P 3/04 (2017.12); A61P 25/00 (2017.12); A61P 25/18 (2017.12); A61P 27/02 (2017.12); C07D 265/34 (2013.01); C07D 413/06 (2013.01)
Citation (search report)
- [XD] US 4540691 A 19850910 - HORN ALAN S [NL]
- See references of WO 9119719A1
Designated contracting state (EPC)
DE FR GB IT
DOCDB simple family (publication)
WO 9119719 A1 19911226; AU 651608 B2 19940728; AU 8224991 A 19920107; CA 2083146 A1 19911216; EP 0550444 A1 19930714; EP 0550444 A4 19930303; JP H05508408 A 19931125
DOCDB simple family (application)
US 9104112 W 19910611; AU 8224991 A 19910611; CA 2083146 A 19910611; EP 91913320 A 19910611; JP 51241391 A 19910611