Hoffmann-la Roche Inc.

Klaus Gubernator

Jean Ackermann

Kurt Hilpert

David Banner

Gerard Schmid

Beat Wirz

Hans Peter Wessel

Paul Hadvary

Thomas B Tschopp

Ludvik Labler

Christian N Hubschwerlen

Klaus Muller

Robert Charnas

G Erard Schmid

Ingrid Heinze

Klaus M Uller

Bicyclic and tricyclic &bgr;-lactams

Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.

Guanidine derivatives

Sulfonamidocarboxamides of the formula ##STR1## wherein A, M, Q, X and Y have the significance given in the description, as well as hydrates, solvates and salts thereof, which inhibit thrombin-induced blood platelet aggregation and clotting of fibrinogen in plasma, as described. The compounds of formula I can be prepared by amidination of a cyclic amino group standing for grouping X or by C(O)N(Q) amide formation.

Sulfonamidocarboxamides

There are described pharmaceutical compositions comprising

Compositions of tricyclic .beta.-lactams and uses thereof

Compositions of bicyclic .beta.-lactams and uses thereof

The novel carboxamides of the formula ##STR1## wherein A, E, G, L, M, R and Q have the significance given in the description, as well as hydrates or solvates thereof inhibit thrombin-induced platelet aggregation and fibrinogen coagulation in plasma. They can be manufactured starting from the corresponding acid and the corresponding amine H.sub.2 NCH.sub.2 Q.

Carboxamides

There are described compounds of the formula ##STR1## in which R signifies lower alkoxycarbonyl, lower alkoxycarbonylamino, the acyl residue of an .alpha.- or .beta.-amino acid or a residue of the general formula

Bicyclic and tricyclic .beta.-lactams

Guanidine derivatives compositions and use

Growing community of inventors

Freiburg, Germany

Klaus Gubernator