Compositions of bicyclic .beta.-lactams and uses thereof

US5698577A · kind A · utility

Assignee

• Hoffmann-La Roche Inc. · US

Inventors

• Christian Hubschwerlen · Durmenach, FR
• Robert Charnas · Hésingue, FR
• Ingrid Heinze · Freiburg im Breisgau, DE
• Klaus Gubernator · Glückstadt, DE

Key dates

• Filing date: Apr 12, 1995
• Grant date: Dec 16, 1997
• Expiry date: Apr 12, 2015

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D487/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

There are described pharmaceutical compositions comprising PA1 (a) compounds of the formula ##STR1## in which R signifies lower alkoxycarbonyl, lower alkoxy-carbonylamino, the acyl residue of an .alpha.- or .beta.-amino acid or a residue of the general formula EQU Q--X--Y-- (a) PA1 wherein Q signifies a 3- to 6-membered ring which optionally contains nitrogen, sulphur and/or oxygen and which is optionally bonded with a fused ring, X signifies a direct bond or a linear "spacer" with up to 6 atoms consisting of carbon, nitrogen, oxygen and/or sulphur, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulphur, and Y represents one of the groups --CO--, --CS--, --CONH-- and (where X contains neither sulphur nor carbonyl as a terminal component) --SO.sub.2 --; and in which R.sup.1 signifies hydrogen, halogen, carbamoyloxy, lower alkanoyloxy or a group of the formula --S--Het, wherein Het represents a 5- or 6-membered heteroaromatic group containing nitrogen, sulphur and/or oxygen, and R.sup.2 represents the sulpho group --SO.sub.3 H and in which R.sup.3 represents hydrogen or R.sup.1 and R.sup.3 together represent a group of the formula EQU .dbd.CH--R.sup.a (c) PA…