C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/242.5
C07D 487/04 (2006.01) C07D 209/08 (2006.01) C07D 209/30 (2006.01) C07D 209/34 (2006.01) C07D 209/88 (2006.01) C07D 295/185 (2006.01)
Patent
CA 1093555
ABSTRACT OF THE DISCLOSURE The present invention provides a compound if the general formula: Image or a non-toxic acid addition salt thereof, wherein: (a) X is hydrogen and Y is -CH2R or -R1 wherein: R is hydrogen; methyl; ethyl; n-propyl; i-propyl; n-butyl; i-butyl; n-pentyl; n-hexyl; 2-methyl-1-propenyl; cyclo- butyl; cyclopentyl; cyclohexyl; 2-phenylethyl; 2-phenylvinyl; phenyl; phenyl monosubstituted in the 2-, 3-, or 4-position by chlorine, bromine, iodine, fluorine, trifluoromethyl, methyl, ethyl, n-propyl, i-prophyl, n-butyl, i-butyl, t-butyl, methoxy, ethoxy, n-propoxy, trifluoromethoxy, cyano, methylsulfonyl, acetyl, propionyl, methlthio, ethylthio, carbethoxy, carbonyl, sodium carboxy, or potassium carboxy; phenyl monsubstituted in the 3-position by amino or nitro; phenyl disubstituted in the 2,3-, 2,4-, 2,5-, 2,6-, 3,4-, or 3,5-positions by methyl, ethyl, n-propyl, methoxy, ethoxy, n-propoxy, chlorine, bromine, iodine, or fluorine; phenyl trisubstituted in the 2,4,6- or 3,4,5-positions by methyl, ethyl, methoxy, or ethoxy; 2,3,5,6- tetramethylphenyl; 3,4-(methylene dioxy)phenyl; 1-naphthalenyl; 2-naphthalenyl; 2-methyl-1-naphthalenyl; 1-bromo-2-naphthalenyl; 2-pyridinyl; 3-pyridinyl; 4-pyridinyl; 2-quinolinyl; 8-quinolinyl; 2-thienyl; 3-thienyl; 4-thiazolyl; 3,5-dimethyl-4-isoxazolyl; tetrahydro-2-furanyl; or benzo(B)thein-3-yl; and R1 is hydrogen; phenyl monosubstituted in the 2- or 4- position by amino, nitro, cyano, acetyl, propionyl, methylsulfonyl, trifluoromethyl or carbethoxy: 2,4-dinitrophenyl; 2,4-diamino- phenyl; 2-cyano-4-nitrophenyl; 2-cyano-4-aminophenyl; 3-methyl-4- nitrophenyl; 3-methyl-4-aminophenyl; 2-trifluoromethyl-4-nitro- phenyl; 2-trifluoromethyl-4-aminophenyl; 2-thiazolyl; 2-pyridinyl; 5-nitro-2-pyridinyl; 2-pyrimidinyl; 2-pyrazinyl; 2-quinolinyl; 4-quinolinyl, 4-methyl-2-quinolinyl; 7-chloro-4-quinolinyl; 7-trifluoromethyl-4-quinolinyl; 2-methyl-4-quinolinyl; 3- methyl-2-quinoxalinyl; 2-phenyl-4-quinolinyl; or 2-benzothiazolyl; and (b) X is methyl, phenyl, or chlorine: and Y is hydrogen, methyl, benzyl, 3-cyanobenzyl, 4-cyanobenzyl, or 2,5-dimethylbenzyl; provided that when X is phenyl, Y may only be hydrogen or methyl, and when X is chlorine, Y may only be benzyl. The compounds inhibit the growth of bacteria in vitro as demonstrated in a standard tube dilution test employing seed agar or Wellcotest Sensitivity. In addition the compounds exhibit in vitro antifolic acid activity, as demonstrated by the inhibition of Streptoccus faecalis ATCC 8043 grown in a folic acid medium.
281981
American Home Products Corporation
Marks & Clerk
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