Abstract: The invention relates to benzylketone phospholipase A.sub.2 inhibitors, pharmaceutical compositions containing them, and methods of treating phospholipase A.sub.2 -mediated conditions in mammals by administration of a therapeutically effective amount of such a benzylketone phospholipase A.sub.2 inhibitor. These compounds are also intermediates in the synthesis of other PLA.sub.2 inhibitors.
Abstract: Phenylhydrazines of the formula I ##STR1## wherein R.sub.1 is --A--R--Z,A is oxygen, sulfur, ##STR2## R is C.sub.1 -C.sub.6 -alkylene, C.sub.1 -C.sub.6 -haloalkyl-C.sub.1 -C.sub.6 -alkylene, C.sub.1 -C.sub.6 -alkoxy-C.sub.1 -C.sub.6 -alkylene or C.sub.1 -C.sub.6 -alkylthio-C.sub.1 -C.sub.6 -alkylene,Z is halogen, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulfinyl or C.sub.1 -C.sub.6 -alkylsulfonyl, orR and Z together are ##STR3## R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio or (C.sub.1 -C.sub.6 -alkyl).sub.2 amino,n is a number from 1-4, and R.sub.2 can be different when n is one of the numbers 2-4,R.sub.3 is halogen,R.sub.4 is hydrogen,R.sub.5 is --COOR.sub.6, orR.sub.3, R.sub.4 and R.sub.5 together form a bridge member of the formula ##STR4## and R.sub.6 is C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl.
Abstract: This invention relates to new isoprenylamine derivatives and acid addition salts thereof, which are useful for controlling virus infection of vertebrate animals.
Abstract: A 5,10-dihydroimidazo[2,1-b]quinazoline in which at least one ring carbon atom, other than the carbon atom in the 2-position, bears a substituent, or a pharmaceutically acceptable acid addition salt thereof is a useful cardiotonic agent and vasodilator in heart insufficiency and a blood platelet aggregation inhibitor.
Abstract: Novel halophenyl and loweralkyl substituted halophenyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful because of their low toxicity, and as such are advantageously included as the active agent in surgical scrubs, antibacterial soaps, as preservatives in cosmetic preparations, and the like.
Type:
Grant
Filed:
February 4, 1981
Date of Patent:
July 20, 1982
Assignee:
Merck & Co., Inc.
Inventors:
Richard A. Dybas, Nathaniel Grier, Bruce E. Witzel
Abstract: Certain phenyl amines have been prepared wherein the "methyl" carbon is substituted with a polyfluoroalkyl radical. The compounds form acid addition salts, exist in resolvable stereoisomeric forms, and are useful for treating hypertension. Formulations for human and veterinary medicine are described, as well as methods of use.
Type:
Grant
Filed:
October 15, 1980
Date of Patent:
February 9, 1982
Assignee:
Science Union et Cie
Inventors:
Charles E. Malen, Pierre Roger, Michel Laubie
Abstract: A method for racemization of optically active amines which comprises contacting an optically active amine of the formula: ##STR1## wherein C* is an asymmetric carbon atom, R.sub.1 is alkyl, aralkyl or aryl and R.sub.2 is aryl or alkoxycarbonyl, the aryl or aralkyl moiety bearing optionally one or more alkyl or alkoxy groups on the aromatic ring, provided that R.sub.1 and R.sub.2 are always different from each other, with a catalyst comprising an alkali metal and a polycyclic aromatic hydrocarbon until a sufficient amount of the optically active amine is racemized.