C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/300, 260/356
C07D 307/79 (2006.01) C07D 311/58 (2006.01) C07D 409/12 (2006.01)
Patent
CA 1261333
Abstract of the disclosure The present invention relates to substituted 5-hydroxy-2,3-dihydrobenzofuran and analogs represented by the following formula: Image or a pharmaceutically acceptable salt thereof, wherein: m is an integer ranging from 1 to 4; A is (a) phenyl substituted with (R1)q wherein when there are more than one R1 (q>1) R1 can be the same or different from each other and is (1) hydrogen; (2) halo; (3) loweralkoxy; (4) lower alkylthio; (5) lower alkyl sulfinyl; (6) lower alkyl sulfonyl; (7) unsubstituted or substituted phenyl substituted with 1 or 2 radicals selected from a group consisting of loweralkoxy; halo; lowerhaloalkyl; loweralkanoyl; hydroxyloweralkyl and CN;(8) loweralkyl; (9) loweralkenyl; (10) lower alkanoyl; (11) haloloweralkyl; (12) -COOH or -COOC1-6 alkyl; (13) aryl having from 1 to 10 carbon atoms; (14) aryloxy having from 1 to 10 carbon atoms; (15) cyano; (16) hydroxyloweralkyl: (17) halo loweralkanoyl; (18) heteroaryl as defined below; or (19) loweralkanoyloxy; q is an integer ranging from 0 to 5; (b) unsubstituted or substituted heteroaryl selected from a group consisting of: (1) thienyl; (2) benzothienyl; (3) furyl; (4) benzofuryl; (5) pyrryl; (6) indolyl; (7) thiazolyl; (8) benzothiazolyl; (9) thiadiazolyl; (10) benzothiadiazolyl; (11) quinolyl; (12) isoquinolyl; (13) pyridyl; (14) pyrazinyl; (15) tetrazolyl; or (16) triazolyl, the heteroaryl above being substituted with one or more of R1. These compounds were found to be potent topical anti-inflammatory agents.
468172
Chang Michael N.
Hammond Milton L.
Jensen Norman P.
Zambias Robert A.
Goudreau Gage Dubuc
Merck & Co. Inc.
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