High molecular weight polymer-based prodrugs
US5965566A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Aug 20, 1997 |
| Grant date | Oct 12, 1999 |
| Priority date | — |
| Expiry date | Aug 20, 2017 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D305/14
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The present invention is directed compositions of the formula: ##STR1## wherein: D is a residue of biologically active moiety; PA1 X is an electron withdrawing group; PA1 Y and Y' are independently O or S; PA1 (n) is zero (0) or a positive integer, preferably from 1 to about 12; wherein: R.sub.1 and R.sub.2 are independently selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls and substituted C.sub.1-6 alkyls; PA1 wherein: R.sub.3 is a substantially non-antigenic polymer, C.sub.1-12 straight or branched alkyl or substituted allyl, C.sub.5-8 cycloalkyl or substituted cycloalkyl, carboxyalkyl, carboalkoxy alkyl, dialkylaminoalkyl, phenylalkyl, phenylaryl or ##STR2## wherein: R.sub.4 and R.sub.5 are independently selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls, and substituted C.sub.1-6 alkyls or jointly form a cyclic C.sub.5 -C.sub.7 ring. In preferred embodiments, the prodrugs contain a polyethylene glycol having a molecular weight of at least about 20,000.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.