Title:
PROCESS FOR PREPARING BENZOXAZIN-4-ONE POLYMER CONJUGATES
Document Type and Number:
WIPO Patent Application WO2002004531
Kind Code:
A3
Abstract:
The present invention relates to a process for forming polymer conjugates which are useful as enzyme inhibitors. The process of the present invention comprises the steps of:a) reacting a polymer or copolymer having the formula (1) wherein R is a hydrocarbyl moiety, a polyalkyleneoxy moiety, or a heteroatom comprising hydrocarbyl moiety, said polymer or copolymer having a molecular weight of from about 500 daltons, with phosgene to form a chloroformate having the formula (2); b) combining a substituted or unsubstituted anthranilic acid having the formula (3) wherein each R1 unit is an enzyme interaction attenuating unit; and a base catalyst wherein said base catalyst is a supported base catalyst, to form a substrate reactive admixture; and c) adding to said chloroformate formed in step (a) said substrate reactive admixture formed in step (b) to form a benzoxazin-4-one conjugate having the formula (4).
Inventors:
FOSSUM RENAI DIANNA
UNDERINER TODD LAURENCE
UNDERINER TODD LAURENCE
Application Number:
PCT/US2001/021816
Publication Date:
April 11, 2002
Filing Date:
July 11, 2001
Export Citation:
Assignee:
PROCTER & GAMBLE (US)
International Classes:
A61P17/00; A61P29/00; A61K31/787; A61P43/00; C07B61/00; C08F8/18; C08F8/30; C08G65/333; (IPC1-7): C08F8/30; C08G85/00
Domestic Patent References:
| WO2001023439A1 | 2001-04-05 |
Foreign References:
| US3669928A | 1972-06-13 | |||
| EP0467167A2 | 1992-01-22 | |||
| DE3000284A1 | 1981-07-09 | |||
| EP0336762A2 | 1989-10-11 |
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