Claims
- 1. A compound of the formula: ##STR23## wherein: R.sup.1 is H or loweralkyl;
- R.sup.2 is H or loweralkyl, or two R.sup.2 's may be joined to form a ring of 3-6 atoms;
- R.sup.3 is --(CH.sub.2).sub.m --Het;
- R.sup.4, R.sup.5 and R.sup.6 is each independently H, lower-alkyl, C.sub.2 -C.sub.6 alkenyl, or --(CR.sup.2 R.sup.2).sub.p M;
- R.sup.7 and R.sup.8 are independently H, C.sub.1 -C.sub.3 alkyl, halogen, OH, CN, CF.sub.3, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkylthio, CO.sub.2 H, C.sub.1 -C.sub.3 alkoxycarbonyl, C.sub.1 -C.sub.3 alkylcarbonyl, or azide;
- R.sup.9 is CF.sub.3, loweralkyl, substituted or unsubstituted benzyl, or substituted or unsubstituted phenyl;
- R.sup.10 is H, loweralkyl, unsubstituted phenyl, unsubstituted benzyl, or two R.sup.10 's attached to a nitrogen may form a ring of 5 to 7 members;
- R.sup.11 is H or --(CH.sub.2).sub.q R.sup.9 ;
- R.sup.12 is loweralkyl, substituted or unsubstituted benzyl, or substituted or unsubstituted phenyl;
- R.sup.13 is H, loweralkyl, substituted or unsubstituted phenyl, or substituted or unsubstituted benzyl;
- R.sup.14 is --CH.sub.2 CH.sub.2 N(R.sup.10).sub.2, CH.sub.2 CH(OH)CH.sub.2 OH, --CH.sub.2 O.sub.2 CC(CH.sub.3).sub.3, --CH(CH.sub.3)O.sub.2 CC(CH.sub.3).sub.3, ##STR24## E is CH.sub.2 OH, CO.sub.2 R.sup.13, CO.sub.2 R.sup.14, tetrazol-5-yl, CHO, C(O)NR.sup.2 R.sup.2, C(O)NHS(O).sub.2 R.sup.9, or C(O)N(OR.sup.2)R.sup.2 ;
- M is a) OR.sup.10 ;
- b) halogen;
- c) CF.sub.3 ;
- d) SR.sup.9 ;
- e) substituted or unsubstituted phenyl;
- f) COOR.sup.10 ; ##STR25## h) tetrazole; ##STR26## j) --NR.sup.10 R.sup.10 ; k) --NHSO.sub.2 R.sup.9 ; ##STR27## m) --S(O)R.sup.9 ; n) --CONR.sup.10 R.sup.10 ;
- o) --S(O).sub.2 NR.sup.10 R.sup.10 ;
- p) --S(O).sub.2 R.sup.9 ;
- q) NO.sub.2 ; ##STR28## u) CN; v) N.sub.3 ; or
- w) H;
- X is O, S, S(O), or S(O).sub.2 ;
- m is 0-2;
- n is 0-5;
- p is 0-3;
- q is 0-4;
- substituted phenyl and substituted benzyl mean 1 or 2 substituents on the benzene ring selected from C.sub.1 -C.sub.3 alkyl, halogen, CN, CF.sub.3, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkylthio, CO.sub.2 H, C.sub.1 -C.sub.3 alkoxycarbonyl, C.sub.1 -C.sub.3 alkylcarbonyl, and azide;
- Het is 2-, 3-, or 4-pyridyl; or 2-, 3- or 4-quinolinyl, each optionally substituted with 1 or 2 substituents selected from C.sub.1 -C.sub.3 alkyl, halogen, CN, CF.sub.3, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkylthio, CO.sub.2 H, C.sub.1 -C.sub.3 alkoxycarbonyl, C.sub.1 -C.sub.3 alkylcarbonyl, and azide;
- and the pharmaceutically acceptable salts thereof.
- 2. A compound of claim 1 of the formula: ##STR29## wherein the substituents are as follows:
- ______________________________________Ex. R.sup.3 X______________________________________64. 4-pyridyl S65. 2-pyridyl S68. CH.sub.2 -2-pyridyl S69. CH.sub.2 -4-pyridyl S121. 2-quinolinyl S______________________________________
- 3. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.
- 4. A method of preventing the synthesis of leukotrienes in a mammal which comprises administering to said mammal an effective amount of a compound of claim 1.
- 5. The method of claim 4 wherein the mammal is man.
- 6. A method of inducing cytoprotecting in a mammal comprising administering to a mammal in need of such treatment a cytoprotective amount of a compound of claim 1.
- 7. A method of treating inflammatory diseases of the eye in a mammal which comprises administering to a mammal in need of such treatment a therapeutically effective amount of a compound of claim 1.
- 8. The method of claim 7 wherein the mammal is man.
CROSS-REFERENCE
This is a division of Ser. No. 130,771 filed Dec. 9, 1987, now 5,081,138, which is a C-I-P of U.S. Ser. No. 942,900, filed Dec. 17, 1986, abandoned.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
5081138 |
Gillard et al. |
Jan 1992 |
|
Non-Patent Literature Citations (3)
Entry |
Tetra. Lett. 24(33), 3531-2 (1983). |
C.A. 84(5): 30798t (1976). |
C.A. 90(19): 15920j (1979). |
Divisions (1)
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Number |
Date |
Country |
Parent |
130771 |
Dec 1987 |
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Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
942900 |
Dec 1986 |
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