Patent ID: 6268383
Filing Date: 2001-07-31
Classification: A61K,C07C,C07D

Abstract:
A method of treating or preventing infection caused by bacteria, mycobactera or fungi by administration of a composition containing as an active agent a bacteria, mycobacteria or yeast growth-inhibiting effective amount of a compound of the formula: ##STR16##wherein A is a phenanthrene ring system, R.sub.1 is bound directly to an oxygen and is also bound to a nitrogen through a saturated carbon or carbon chain, and R.sub.1 is CHOZX wherein Z may be hydrogen, a second bond to the oxygen, or may be ether or ester moiety wherein the ether or ester moiety may be alkyl of 1-8 carbons, phenyl, phenylalkyl, wherein the alkyl moiety consists of 1-4 carbons and wherein any said alkyl or phenyl group may, additionally, be substituted with hydroxy, alkyl of 1-2 carbons, alkenyl of 2-3 carbons, halo, amino, or alkyl amino group and X is (CH.sub.2)N((CH2).sub.n (CH.sub.3)).sub.m wherein is 1 to 3, n is .ltoreq.6, m is 1 or 2 with the proviso that when m is 2, at least one of n is <3, or X may be (CH.sub.2).sub.o J wherein o is 0-4 and J is a saturated nitrogen-containing ring system with up to 10 carbon atoms in the ring system and may have up to 4 bridge carbons, and wherein any saturated ring system may be substituted with alkyl, alkenyl, halo, alkoxy or haloalkyl moieties of 1-5 carbons or with phenyl, phenoxy, phenylalkyl, phenylalkoxy, carboxy or carbonyl groups, wherein the carboxy or carbonyl groups, including keto or ester moieties, with alkyl groups having 1-4 carbons, alkenyl groups of 2-5 carbons or phenylalkyl wherein the alkyl is of 1-3 carbons or phenylalkoxy wherein the alkyl is of 1-3 carbons and, further, wherein X and Z may be linked to form a heterocyclic ring system and (a) is 0-4 with the proviso that at least one of (a) is not 0, R.sub.2, R.sub.3 and R.sub.4 may be alkyl (including cycloalkyl), a saturated, nitrogen-containing ring of 4-10 atoms, alkoxy, aryl, aryloxy, aryloxyalkyl, amino, amino-alkyl, alkyl-aminoalkyl, arylamino, alkenyl, arylalkenyl, arylalkyl-aminoalkyl, carboxyalkyl, hydroxy, halo, alkenyl, or alkenyloxy, halo-substituted alkyl, wherein any alkyl has 1-8 carbons, alkenyl has 2-8 carbons, wherein halo is chloro, fluoro or bromo and aryl is a ring system of 1-3 rings and wherein any alkyl or aryl at R.sub.2, R.sub.3 and R.sub.4 may be further substituted with halo (including multiple halo subtitutions), aryl of 1-2 rings, alkyl, haloalkyl or alkoxy, with the proviso that at least one of R.sub.2, R.sub.3 and R.sub.4 is an electron-rich substituent.