申请人:Sterling Winthrop Inc.
公开号:US05292736A1
公开(公告)日:1994-03-08
Compounds of the formula ##STR1## wherein Alk is lower-alkylene; R.sub.1 is hydrogen, lower-alkyl, Ar or ArCOO; R.sub.2 is hydrogen or lower-alkyl; R.sub.3 and R.sub.4 are the same or different hydrogen, fluoro, chloro, bromo, hydroxy, lower-alkoxy, lower-alkyl, or trifluoromethyl; Ar is phenyl, naphthyl, anthryl, 2-phenylethenyl or a 5- or 6-membered monocyclic or 9- or 10-membered bicyclic fused aromatic heterocyclic ring containing carbon and one or two heteroatoms independently selected from oxygen, nitrogen and sulfur, or such carbocyclic or heterocyclic rings substituted with from 1 to about 3 of lower-alkoxy, lower-alkyl, lower-alkylthio, lower-alkyl sulfinyl, lower-alkyl sulfonyl, hydroxy, cyano, amino, lower-alkylamino, dilower-alkylamino or halo; or pharmaceutically acceptable acid addition salts thereof are useful as analgesics and in the treatment of glaucoma.
式为##STR1##的化合物,其中Alk是较低的烷基;R.sub.1是氢、较低的烷基、Ar或ArCOO;R.sub.2是氢或较低的烷基;R.sub.3和R.sub.4相同或不同,是氢、氟、氯、溴、羟基、较低烷氧基、较低烷基或三氟甲基;Ar是苯基、萘基、蒽基、2-苯乙烯基或含有碳和一个或两个独立选择的氧、氮和硫杂原子的5-或6-成员单环或9-或10-成员双环螺环芳香杂环,或带有1至约3个较低的烷氧基、较低的烷基、较低的烷基硫、较低的烷基亚砜基、较低的烷基磺酰基、羟基、氰基、氨基、较低烷基氨基、二较低烷基氨基或卤素的这种碳环或杂环取代物;或其药学上可接受的酸盐在镇痛和青光眼治疗中有用。