Abstract: The compounds of the present invention comprise substituted phenolic thioether derivatives that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
Abstract: This disclosure relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 and R.sup.2 are independently selected from the class consisting of hydrogen, halo, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkoxy;R.sup.3 and R.sup.4 are independently hydrogen or C.sub.1 -C.sub.6 alkyl or R.sup.3 and R.sup.4 together may be a ##STR2## group wherein n is an integer of from 0 to 4; and X, Y and Z are independently--CH-- or --N.dbd. provided that one and only one of X, Y or Z must be --N.dbd..The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions as anti-anaerobic agents.
Type:
Grant
Filed:
August 19, 1986
Date of Patent:
August 2, 1988
Assignee:
G. D. Searle & Co.
Inventors:
George J. Ellames, Roger M. Upton, Albert A. Jaxa-Chamiec, Peter L. Myers
Abstract: The present invention describes allenic prostacyclin derivatives of the formula: ##STR1## wherein: n is 0, 1, or 2;R.sup.1 is hydrogen, lower alkyl, or a pharmaceutically acceptable cation;R.sup.2 is hydrogen, lower alkyl, cycloalkyl, heteroaryl, halogen, phenyl, alkylthio, phenylthio, alkylsulfinyl, phenylsulfinyl or trifluoromethyl;R.sup.3 is lower alkyl, cycloalkyl, phenyl, benzyl, cycloheteroalkyl, lower alkyl having one to eight carbons substituted with one or more fluorines or containing 1 or 2 unsaturated bonds; andcarbon 15 may be in the R or the S configuration, or a mixture of R and S.These compounds are useful for the treatment of platelet dysfunction, atherosclerosis, allergic disorders, gastric ulcers, hypertension and tumor cell metastasis. Also disclosed is the process for preparing them and the appropriate intermediates.
Abstract: This invention relates to 3-alkyl-5-[(substituted amino) methyl]dihydro-3-phenyl-2(3H)-furanones and imino analogs thereof, and to the pharmaceutical compositions containing such compounds, that are useful as inhibitors of cardiac arrhythmias and are therefore useful in the treatment of irregular heartbeat. This invention also relates to the use of such compounds and pharmaceutical compositions in the treatment of irregular heartbeat.
Abstract: This invention relates to 8-chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 2-[(substituted phenylsulfinyl)alkanoyl]hydrazides and 8-chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 2-[(substituted phenylsulfonyl)alkanoyl]hydrazides that are useful as prostaglandin antagonists and analgesic agents. This invention also relates to 8-chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 2-[(substituted phenylthio)alkanoyl]hydrazides that are useful as intermediates in the preparation of the corresponding sulfinyl and sulfonyl compounds.
Abstract: The compounds of this invention are acylaminoalkylpyridines representd by the formula ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk.sub.1 is straight or branched chain lower alkylene of 1 to 6 carbon atoms, R.sub.3 is lower alkyl, Alk.sub.2 is straight or branched chain alkylene of 1 to 4 carbon atoms; R.sub.4 is selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl and lower alkoxy; and the pharmaceutically acceptable salts thereof. The compounds of the present invention are useful in the treatment of inflammation, allergy and hypersensitivity reactions and other disorders of the immune system.
Type:
Grant
Filed:
December 20, 1985
Date of Patent:
May 5, 1987
Assignee:
G. D. Searle & Co.
Inventors:
Richard A. Mueller, Richard A. Partis, James R. Deason
Abstract: This invention relates to substituted aralkoxy and aryloxyalkoxy kojic acid derivatives, which are useful as leukotriene D.sub.4 (LTD.sub.4) inhibitors and therefore useful in the treatment of allergies, inflammatory conditions, and coronary vasoconstriction.