Patent ID: 8877709
Filing Date: 2014-11-04
Classification: A61K,A61P,C07D

Abstract:
1. A method for preparation of a conjugate of the formula: herein designated (PEG-FMS) n -drug when R 2 is —SO 3 H at position 2 of the fluorene ring or (PEG-Fmoc) n -drug when R 2 is H at position 2 of the fluorene ring, wherein n is an integer from 1 to 3, PEG is a linear or branched PEG moiety of molecular weight in the range of 200 to 200,000, and the drug is a peptide or a protein drug of low or medium molecular weight, said method comprising: (i) reacting a peptide or protein drug of low or medium molecular weight with at least one equivalent of N-[2 maleimido-propionylamino)-7-sulfo-fluoren-9-yl-methoxy-carbonyloxy]succinimide or N-[2 (maleimidopropionylamino)fluoren-9-yl-methoxycarbonyloxy]succinimide, herein identified MAL-FMS-NHS or MAL-Fmoc-NHS, thus obtaining a conjugate (MAL-FMS) (ii) reacting the conjugate (MAL-FMS)