Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-02-25
2000-09-05
Berch, Mark L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
5142345, 544119, 544237, C07D24702, C07D40514, A61P 3104, A61K 31506
Patent
active
061143308
ABSTRACT:
The invention is concerned with compounds of formula ##STR1## wherein R.sup.1 is lower-alkoxy, R.sup.2 is hydroxy or lower-alkoxy, R.sup.3 is hydrogen, cyano, alkyl, alkenyl, cycloalkyl, aryl, heterocycyl, aryl-Q-alkyl, or a group of the formula --CR.sup.4 R.sup.4 'COR.sup.5 --, Q is --SO-- or --SO.sub.2 --; R.sup.4, R.sup.4 ' are each independently hydrogen, alkyl, aryl or heterocyclyl, R.sup.5 is hydrogen, alkyl, alkoxy, hydroxy, aryl or heterocycyl, or R.sup.4 and R.sup.5 together form --(CH.sub.2).sub.n --, and n is a whole number between 2 to 5 inclusive and the enantiomers, epimers, and diastereomers thereof, as well as pharmaceutically acceptable salts thereof. These compounds have valuable antibacterial activity.
REFERENCES:
patent: 5866583 (1999-02-01), Guerry
Roth, et al.; 2,4-Diamino-5-benzylpyrimidines as Antibacterial Agents; J. Med. Chem.; 32; (8), 1949 (1989).
Baccanari, D.P. and S.S. Joyner, Biochemistry, 20:1710-1716 (1981).
Hartman, P.G., et al., FEBS Letters, 242:175-160 (1988).
"Academic Press Dictionary of Science and Technology" p. 93, 1992.
Guerry Philippe
Hubschwerlen Christian
Jolidon Synese
Specklin Jean-Luc
Wyss Pierre-Charles
Berch Mark L.
Ebel Eileen M.
Hoffmann-La Roche Inc.
Johnston George W.
Rocha-Tramaloni Patricia S.
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