3-Amidino ansamycins

US4327096A · kind A · utility

Assignee

• Farmitalia Carlo Erba S.p.A. · IT

Inventors

• Leonardo Marsili · Milano, IT
• Giovanni Franceschi · Milano, IT
• Aurora Sanfilippo · Milano, IT

Key dates

• Filing date: Feb 9, 1981
• Grant date: Apr 27, 1982
• Expiry date: Feb 9, 2001

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P31/06
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Novel 3-amidino rifamycins having the formula: ##STR1## wherein Y is --H or --COCH.sub.3 ; R.sub.1 and R.sub.2 may be linear or branched alkyl having from 1 to 7 carbon atoms and alkenyl having 3 or 4 atoms and R.sub.2 may be also chloroalkyl having from 2 to 4 carbon atoms, cycloalkyl having from 3 to 7 carbon atoms in the ring, cycloalkylalkyl having from 3 to 6 carbon atoms in the ring, phenyl, bornyl, arylalkyl hydrocarbon having 7 or 8 carbon atoms which may be substituted with one halogen atom in the aryl group; and R.sub.1 and R.sub.2 along with the N atom to which they are bonded form an unsubstituted cyclic moiety having from 5 to 8 carbon atoms, a cyclic moiety having from 5 to 8 carbon atoms substituted with 1 or 2 methyl radicals, 4-alkylpiperazine, morpholine, 1,2,3,4-tetrahydroisoquinoline. These novel compounds are from grey to dark solids having high antibacterial activity which are obtained by reacting 3-amino rifamycin S or SV with a chloroformiminio chloride.