Neocarzinostatin derivatives and method of producing the same
AssigneesKuraray Co., Ltd., Yamanouchi Pharmaceutical Co., Ltd., Kayaku Antibiotics Research Co., Ltd., Hiroshi Maeda
InventorsHiroshi Maeda, Ryunosuke Kanamaru, Nakao Ishida, Toshihiko Yoshitake, Minoru Ueda
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Abstract
Substantially pure neocarzinostatin anticancer agents have the formula (A): (SMA)--(NCS)--(SMA) (A) wherein (NCS) is a divalent neocarzinostatin residue and (SMA) comprises the monovalent residue of a partially half-esterified styrene-maleic acid copolymer having a weight-average molecular weight of from 800 to 2,500, said (NCS) residue being bonded to said (SMA) residues via amide linkages formed between primary amino groups of the neocarzinostatin molecule and carbonyl groups of the partially half-esterified styrene-maleic acid copolymer.
Claims24
A substantially pure neocarzinostatin derivative having the formula (A):
- (SMA)--(NCS)--(SMA) (A)
- wherein (NCS) is a divalent neocarzinostatin residue and (SMA) comprises the monovalent residue of a partially half-esterified styrene-maleic acid copolymer having a weight-average molecular weight of from 800 to 2,500, said (NCS) residue being bonded to said (SMA) residues via amide linkages formed between primary amino groups of the neocarzinostatin molecule and carbonyl groups of the partially half-esterified styrene-maleic acid copolymer.
A process for the preparation of a neocarzinostatin derivative, comprising reacting neocarzinostatin, in an aqueous reaction medium, with a molar excess of a partially half-esterified styrene-maleic anhydride copolymer, said copolymer satisfying the formulae (B) and (C):
- 800.ltoreq.Mw.ltoreq.2,500 (B)
- Mw/Mn.ltoreq.1.5-1.1.times.10.sup.-4 Mw (C)
- wherein Mw is the weight-average and Mn the number-average molecular weight thereof.
Dependencies are inferred from the claim text.