Conjugation reagents
View Patent ↗The invention provides compound of the general formula: in which each X independently represents a polymer chain; n represents an integer greater than 1; Q represents a linker; Y represents an amide group; and Z represents either —CH.(CH 2 L) 2 or —C(CH 2 L)(═CH 2 ), in which each L independently represents a leaving group. The compounds are useful reagents for the conjugation of polymers to proteins, the resulting conjugates being novel and also forming part of the invention.
1. A compound having general formula:
in which Q is:
each X independently represents a polymer chain; and Z represents either —CH.(CH 2 L) 2 or —C(CH 2 L)(═CH 2 ), in which each L independently represents a leaving group.
2. A compound as claimed in claim 1 , in which each X represents a poly(alkylene glycol), polyvinylpyrrolidone, polyacrylate, polymethacrylate, polyoxazoline, polyvinylalcohol, polyacrylamide, polymethacrylamide, HPMA copolymer, polyester, polyacetal, poly(ortho ester), polycarbonate, poly(imino carbonate), polyamide, or polysaccharide.
3. A compound as claimed in claim 1 , in which each L independently represents —SR, —SO 2 R, —OSO 2 R, —N + R 3 , —N + R 2 , —N + H 2 R, halogen, or —OØ, in which R represents a hydrogen atom or an alkyl, aryl or alkyl-aryl group, and Ø represents a substituted aryl group containing at least one electron withdrawing substituent.
4. A compound as claimed in claim 3 , in which each L independently represents phenylsulfonyl or tosyl.
5. A compound, said compound having the formula:
in which each X independently represents a polymer chain.
6. A compound as claimed in claim 5 , in which each X independently represents polyethylene glycol of the formula CH 3 O—(CH 2 CH 2 O) m — in which m is the number of ethylene oxide units in X.