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US 4,904,672 AGranted
Derivatives of 3-hydroxyazabenzo[b]thiophene useful as 5-lipoxygenase inhibitors
AssigneeMerck & Co., Inc.
InventorsRobert K. Baker, Kathleen M. Rupprecht, Arsenio A. Pessolano, Philippe L. Durette
Life of this patent
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Abstract
3-Hydroxyazabenzo[b]thiophene derivatives having optionally 2-aryl, 2-aralkyl, 2-alkyl or 2-alkenyl substituents were prepared by, among other methods, ring closure of an appropriately substituted benzylthioalkoxycarbonyl-pyridine. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases such as psoriasis and atopic eczema, cardiovascular disorders, inflammatory disease and other leukotriene mediated diseases.
Claims8
A compound of formula:
- ##STR26## or a pharmaceutically acceptable salt thereof wherein X.sub.1 is selected from the group consisting of
- (a) H,
- (b) C.sub.1-6 alkyl,
- (c) halo,
- (d) halo-C.sub.1-6 alkyl,
- (e) CN,
- (f) --(CO)OR.sup.3, wherein R.sup.3 is C.sub.1-6 alkyl, and
- (g) --OC.sub.1-6 alkyl;
- R is selected from the group consisting of
- (a) H,
- (b) --(CO)R.sup.3,
- (c) --(CO)OR.sup.3,
- (d) --(CO)NR.sup.3 R.sup.4 wherein R.sup.4 is C.sub.1-6 alkyl,
- (e) --(CO)SR.sup.3, and
- (f) --(CO)(CH.sub.2).sub.m OR.sup.3, wherein m is an integer from 1 to 6;
- R.sup.1 is selected from the group consisting of
- (a) pyridyl, and
- (b) substituted phenyl, wherein the substituent is
- (1) H,
- (2) -methylenedioxy,
- (3) haloC.sub.1-6 alkyl,
- (4) halo,
- (5) CN,
- (6) --OC.sub.1-6 alkyl,
- (7) --(CO)OR.sup.3.
- (8) C.sub.1-6 alkyl, or
- (9) NO.sub.2.
24 more elements
Dependencies are inferred from the claim text.