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US 5,324,743 AGranted
Leukotriene B.sub.4 antagonists
AssigneeEli Lilly and Company
InventorsRobert D. Dillard, J. Scott Sawyer, Michael J. Sofia
Life of this patent
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Abstract
This invention provides certain 1,2,4,5 substituted benzene derivatives containing "acid" substituents derived from cyclic or heterocyclic moieties. These unique compounds are leukotriene B.sub.4 antagonists and formulations of these derivatives, and a method of using these derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
Claims14
A compound represented by the formula:
- ##STR35## and salts thereof, wherein:
- R.sub.1 is hydrogen;
- R.sub.2 is halo, or --OR"
- R.sub.3 is C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.6 alkanoyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.1 -C.sub.4 alkoxy, hydroxy substituted C.sub.1 -C.sub.3 alkyl, or C.sub.1 -C.sub.4 thioalkyl;
- X and Y are the same or different and are selected individually at each occurrence from:
- --CR'.sub.2 --, --O--, --S--, or --NR'--;
- Z is --CH.sub.2).sub.n, --NR'"-- or phenylene;
- A is a bond or a linear or branched chain C.sub.1 -C.sub.10 alkylidene;
- G is --CH.sub.2 --, ##STR36## and wherein:
- R' is independently selected, at each occurrence, from H and C.sub.1-4 alkyl;
- R" is independently selected, at each occurrence, from H and --CH.sub.2).sub.n --H;
- R'" is independently selected, at each occurrence, from H or C.sub.1 -C.sub.4 alkyl;
- n is selected independently,at each occurrence, and ranges from 1-8;
- m is selected independently, at each occurrence, and ranges from 0-4;
- and
- wherein:
- R.sub.4 is selected from the groups;
- ##STR37## wherein W is a bond, 13 CHR).sub.n, --O[CHR'].sub.n).sub.n, --O--, --S--, or ##STR38## and R.sub.5 is H, C.sub.1 -C.sub.6, linear or branched alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, hydroxy, or, cyano, halo, --N.sub.3, --NR'R'", --CO.sub.2 R'
- R.sub.6 is individually selected, at each occurrence, from H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, phenyl, benzyl, --WR.sub.5, halo, thio (C.sub.1 -C.sub.4 alkyl), hydroxy, or --O-- (C.sub.1 -C.sub.10 alkoxy);
- and
- R.sub.7 and R.sub.8 are both individually selected from H or C.sub.1 -C.sub.3 alkyl;
- and
- halo is --F, --Cl, --Br, or --I;
- and pharmaceutically acceptable salts thereof.
21 more elements
Dependencies are inferred from the claim text.