Patent number: 6355653
Abstract: The invention relates to compounds of formula
wherein
R1 is a 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally substituted by one or two substituents, which are lower alkyl, —(CH2)nOH, halogen or lower alkoxy, and wherein the heteroaryl groups may be optionally linked to the pyrazole ring via an alkylene or alkenyl group, or is
phenyl, optionally substituted by one or two substituents being lower alkyl, hydroxy-lower alkyl, halogen, hydroxy or lower alkoxy or is
—O(CH2)n,phenyl, benzofuryl, indolyl or benzothiophenyl, or is
—S-lower alkyl;
R2 and R4 are independently from each other hydrogen, cyano or —S(O)2-phenyl;
R3 is hydrogen, halogen or is
a 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally substituted by one or two substituents, which are lower alkyl, —(CH2)n-aryl, hydroxy, halogen, lower alkoxy, morpholin
Type:
Grant
Filed:
August 24, 2000
Date of Patent:
March 12, 2002
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Gerda Huber Trottmann, Walter Hunkeler, Roland Jakob-Roetne, Gavin John Kilpatrick, Matthias Heinrich Nettekoven, Claus Riemer
Patent number: 6294668
Abstract: The present invention relates to cephalosporin derivatives of the general formula
where
R1 is halogen, lower alkyl, phenyl, benzyl, styryl, naphthyl or heterocyclyl; the lower alkyl, phenyl, benzyl, styryl, naphthyl and heterocyclyl being optionally substituted by at least one of halogen, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkoxy, optionally substituted phenyl, amino, lower alkylamino, di-lower alkylamino, carboxy, lower alkylcarboxy, carbamoyl or lower alkylcarbamoyl;
R4, R5 independently are hydrogen, lower alkyl or phenyl;
X is S, O, NH or CH2;
n is 0,1 or 2;
m is 0 or 1;
s is 0 or 1;
R2 is hydrogen, hydroxy, —CH2—CONHR6, lower alkyl-Qr, cycloalkyl-Qr, lower alkoxy, lower alkenyl, cycloalkenyl-Qr, lower alkynyl, aralkyl-Qr, aryl-Qr, aryloxy, aralkoxy, a heterocyclic ring or a heterocyclyl-Qr, the lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl, aryl, aryloxy, aralkoxy and the heterocyclic
Type:
Grant
Filed:
November 5, 1997
Date of Patent:
September 25, 2001
Assignee:
Hoffman-La Roche Inc.
Inventors:
Peter Angehrn, Ingrid Heinze-Krauss, Hans G. F. Richter