POLYCYCLIC PHTHALAZIN DERIVATIVES, PARTICULARLY SUBSTITUTED MADURAPHTHALAZINES AND THEIR USE THEREOF

摘要

PCT No. PCT/FI96/03632 Sec. 371 Date Jan. 28, 2000 Sec. 102(e) Date Jan. 28, 2000 PCT Filed Jul. 9, 1997 PCT Pub. No. WO98/07706 PCT Pub. Date Feb. 26, 1998Polycyclic phthalazines, in particular 2-substituted maduraphthalazines (10,12,15,16-tetrahydroxy-8-methoxy-11-methyl-1,9,14-trioxo-1,2,6,7,9,14-hexahydronaphthaceno-1,2-g-phthalazines), of formula I and their use against gram-positive bacterial strains, particularly against multi-resistant staphylococci (MRSA) and against glycopeptide-resistant, for example vancomycin-resistant, enterococci. The polycyclic phthalazines are thus suitable for preparing anti-bacterially effective pharmaceutical compositions. In formula I, R1 is carboxyalkyl or carboxyaryl, and R2 and R3 represent H or acyl (for example CO-alkyl or COO-alkyl), with R1 being different from optionally substituted carboxyphenyl when R3 represents C1-8 alkanoyl. The invention also relates to salts, amides and esters of compounds of formula I.