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US 5,296,486 AGranted
Leukotriene biosynthesis inhibitors
AssigneeBoehringer Ingelheim Pharmaceuticals, Inc.
InventorsEdward S. Lazer, Julian Adams, Clara K. Miao, Peter Farina
Life of this patent
Estimating the term…
Abstract
Various substituted benzoxazoles, benzothiazoles, oxazolopyridines and thiazolopyridines are described and disclosed, compounds that are potent inhibitors of leukotriene synthesis in warm-blooded animals.
Claims10
A compound having the following formula:
- ##STR22## wherein X is O or S
- R.sub.1 and R.sub.2 are each, independent of one another, hydrogen;
- C.sub.1 -C.sub.6 alkyl;
- halo ;
- CF.sub.3 ;
- nitrile;
- C.sub.1 -C.sub.6 alkoxy;
- --CO.sub.2 R.sub.7 wherein R.sub.7 is hydrogen or C.sub.1 -C.sub.6 alkyl;
- NO.sub.2 ;
- --C(O)NR.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 are hydrogen, C.sub.1 -C.sub.3 allyl or methoxy;
- --NR.sub.10 R.sub.11 wherein R.sub.10 and R.sub.11 are hydrogen or C.sub.1 -C.sub.6 alkyl;
- --C(O)R.sub.12 wherein R.sub.12 is C.sub.1 -C.sub.6 alkyl;
- 'SO.sub.2 R.sub.12, --NHC(O)R.sub.12 ;
- --NHSO.sub.2 R.sub.12 ;
- or --SO.sub.2 NR.sub.13 R.sub.14 wherein R.sub.13 and R.sub.14 are hydrogen or C.sub.1 -C.sub.6 alkyl;
- R.sub.3 is cyclohexyl or an optionally substituted phenyl ring wherein the substituents are selected from halo, CF.sub.3, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy;
- --SO.sub.2 R.sub.12 ;
- --NHC(O)R.sub.12 ;
- --NHSO.sub.2 R.sub.12 ;
- SO.sub.2 NR.sub.13 R.sub.14 ;
- or NO.sub.2 ;
- or R.sub.3 may be a 2-, 3- or 4-pyridine ring;
- or R.sub.3 may be a dialkylamine (C.sub.1 -C.sub.4);
- or may be an alkyl ether, (C.sub.1 -C.sub.4)
- R.sub.4 is 2-, 3-, or 4-pyridyl.
- R.sub.5 and R.sub.6 are each, independent of one another, hydrogen or methyl and
- n is an integer of b 0, 1 or 2, in racemic form, or the pure or substantially pure enantiomers thereof.
24 more elements
Dependencies are inferred from the claim text.