Claims
- 1. 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 .paren open-st.CH.sub.2 .paren close-st..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 -.sub.4 alkyl;
- R" is independently selected, at each occurrence, from H and .paren open-st.CH.sub.2 .paren close-st..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, .paren open-st.CHR'.paren close-st..sub.n, .paren open-st.O[CHR'].sub.n .paren close-st..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, 1, 2, 4- triozol-1-yl, cyano, halo, --N.sub.3, --NR'R'", --CO.sub.2 R', or 5-tetrazolyl optionally substituted with a C.sub.1 -C.sub.4 alkyl group; and
- 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.
- 2. The compounds of claim 1, or their pharmaceutically acceptable salts, wherein:
- X and Y are the same or different and are selected individually, at each occurrence, from --CH.sub.2 -- or --O--;
- A is a linear or branched C.sub.2 -C.sub.6 alkylidene;
- G is ##STR39## and, R.sub.4 is selected from: ##STR40## wherein R.sub.5 is --CO.sub.2 H.sub.3 and m ranges from 0-2 and n ranges from 1-6.
- 3. The compounds of claim 1 and their pharmaceutically acceptable salts, wherein:
- X and Y are the same or different and are individually selected, at each occurrence, from: --CH.sub.2 --, and --O--;
- A is a linear or branched C.sub.2 -C.sub.6 alkylidene;
- G is ##STR41## and R.sub.2 is --OH;
- W is a bond, ##STR42## R.sub.5 is: --CO.sub.2 R' or 5-tetrazolyl; and R.sub.6 is independently selected, at each occurrence, from --WR.sub.5, --H, C.sub.1 -C.sub.4 alkyl, halo, hydroxy, methoxy, benzyl, or phenyl; and
- R4 is: ##STR43## and n, at each occurrence is from 1-4 and m, at each occurrence, ranges from 0-2.
- 4. The compounds of claim 2 wherein:
- W is a bond, .paren open-st.CH.sub.2 .paren close-st..sub.n or --O.paren open-st.CH.sub.2 .paren close-st..sub.n ;
- R.sub.5 is --CO.sub.2 H;
- R', R", and R'" are all --H;
- R.sub.6 is, at each occurrence, selected individually from H, halo, or C.sub.1 -C.sub.4 alkyl; and
- R.sub.4 is: ##STR44## wherein m ranges from 0-1, n ranges from 1-4; and R.sub.7 and R.sub.8 are both either H or --CH.sub.3.
- 5. A pharmaceutical formulation comprising:
- ______________________________________Compound Wt. %______________________________________a) A compound of Claim 1 0.1%-99.9 wt %b) Fillers, inerts, carriers, Remainder excipients, solvents, lubricants, or mixtures thereof______________________________________
- 6. A pharmaceutical formulation comprising:
- ______________________________________a) A compound of Claim 2 0.1%-99.9 wt %b) Fillers, inerts, carriers, Remainder excipients, solvents, lubricants, or mixtures thereof______________________________________
- 7. A pharmaceutical formulation comprising:
- ______________________________________a) A compound of Claim 3 0.1%-99.9 wt %b) Fillers, inerts, carriers, Remainder excipients, solvents, lubricants, or mixtures thereof______________________________________
- 8. A pharmaceutical formulation comprising:
- ______________________________________a) A compound of Claim 4 0.1%-99.9 wt %b) Fillers, inerts, carriers, Remainder excipients, solvents, lubricants, or mixtures thereof______________________________________
- 9. A compound of claim 1, or its pharmaceutically acceptable salts, having the formula; ##STR45##
- 10. A compound of claim 1, or its pharmaceutically acceptable salts, having the formula: ##STR46##
- 11. A compound of claim 1 having the formula: ##STR47##
- 12. A compound of claim 1, or its pharmaceutically acceptable salts, having the formula: ##STR48##
- 13. A method of treating a mammal suffering from a disease state characterized by the presence of an excess of leukotriene, LTB.sub.4, which method comprises administering to said mammal an effective amount of one or more compounds of claim 1.
- 14. The method of claim 13 wherein the effective amount of compound(s) ranges from about 0.1 mg/Kg body weight to about 200 mg/Kg body weight of the mammal.
Parent Case Info
This application is a division of prior application Ser. No. 07/988,615, filed Dec. 10, 1992, now U.S. Pat. No. 5,324,743.
US Referenced Citations (3)
| Number |
Name |
Date |
Kind |
| 4200577 |
Buckle et al. |
Apr 1980 |
|
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Buckle et al. |
Jul 1980 |
|
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Non-Patent Literature Citations (1)
| Entry |
| Buckle et al., J. Med. Chem 22 (2) 158-68 (1979). |
Divisions (1)
|
Number |
Date |
Country |
| Parent |
988615 |
Dec 1992 |
|
Patent Grant
5552441
