Smithkline Beckman Corporation

Charles M Kinzig

John G Gleason

Deborah Lynne Bryan

Henry M Sarau

Seymour Mong

Sylvia T Hoffstein

A method for inhibiting the effects of LTB.sub.4 comprises administration of an effective amount of a compound represented by the following structural formula (I) ##STR1## wherein m is 1 or 2; n is 1, 2 or 3; p is 0, 1, or 2; R' is hydrogen or methyl; R is phenyl substituted with A, R.sub.1 and R.sub.2 wherein R.sub.1 and R.sub.2 are independently selected from either (1) (S).sub.a --(CH.sub.2).sub.b --(T).sub.c --B wherein a is 0 or 1; b is 5 to 12; c is 0 or 1; S and T are independently sulfur, oxygen, or CH.sub.2 with the proviso that S or T are not sulfur when p is 1 or 2; and B is C.sub.1-4 alkyl, ethynyl, trifluoromethyl, or phenyl optionally monosubstituted with Br, Cl, CF.sub.3, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, methylthio, or trifluoromethylthio; or (2) hydrogen bromo, chloro, methyl, trifluoromethyl, methoxy or nitro; and A is selected from (2) as defined above or a pharmaceutically acceptable salt thereof. Such methods are useful in the treatment of diseases in which LTB.sub.4 is a factor.

Leukotriene antagonists

Esters of leukotriene A are conveniently prepared by reacting 9-oxo-5,6-trans-epoxynon-7(E)-enoates with 11-triphenylphosphoranylidene undec-6(Z),9(Z)-diene. Esters of leukotriene-A are useful intermediates in the synthesis of naturally occurring leukotrienes, which have been shown to be potent broncho-constricting substances. Novel intermediates to the esters of leukotriene A, 9-oxo-5,6-transepoxynon-7(E)-enoates and 7-oxo-5,6-trans-epoxyheptanoates, are disclosed.

Process for the preparation of esters of leukotriene A

Esters of leukotriene A are conveniently prepared by reacting 9-oxo-5,6-trans-epoxynon-7(E)-enoates with 11-triphenylphosphoranylidene undec-6(Z),9(Z)-diene. Esters of leukotriene-A are useful intermediates in the synthesis of naturally occurring leukotrienes, which have been shown to be potent broncho-constricting substances. Novel intermediates to the esters of leukotriene A. 9-oxo-5,6-trans-epoxynon-7(E)-enoates and 7-oxo-5,6-trans-epoxyheptanoates, are disclosed.

Esters of leukotriene A are conveniently prepared by reacting 9-oxo-5,6-trans-epoxynon-7(E)-enoates with 11-triphenylphosphoranylidene undec-6(Z),9(Z)-diene. Esters of leukotriene-A are useful intermediates in the synthesis of naturally occurring leukotrienes, which have been shown to be potent broncho-constricting substances. Novel intermediates to the esters of leukotriene A, 9-oxo-5,6-transepoxynon-7(E)-enoates and 7-oxo-5,6-transepoxyheptanoates, are disclosed.

Growing community of inventors

Merion Station, PA, United States of America

Charles M Kinzig