Preparation of biogically active substances bearing -NH.sub.2 groups in a form releasable by enzymatic cleavage
US4097470A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Jun 9, 1975 |
| Grant date | Jun 27, 1978 |
| Priority date | — |
| Expiry date | Jun 9, 1995 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY10S260/47
- WIPO fieldMacromolecular chemistry, polymers
- WIPO sectorChemistry
Abstract
Polymeric form of a biologically active compound containing at least one -NH.sub.2 group in its molecule, adapted for the protracted release of said biologically active compound by enzymatic cleavage of the polymer in vivo in the organism. The active compound is bonded by its -NH.sub.2 group to the carboxylic group of an L-amino acid as for instance, .beta.-phenylalanine, tyrosine, tryptophane, lysine, arginine, glycine, alanine, leucine, citruline or ornithine, which latter is in twin bonded by its amino group to the terminal carboxylic group of the side chain of a substituted amide or ester of acrylic or methacrylic acid, said side chain constituting a linear moiety containing at least 3 carbon atoms. The latter compound or monomer is copolymerized with a hydrophilic monomer such as, N-alkylmethacrylamide, N-alkylacrylamide, N,N-dialkylacrylamide, wherein alkyl has 1-6 carbon atoms and may contain 1 to 3 OH groups, or glycol acrylate or methacrylate alone or in admixture, and which copolymer may contain further monomeric components, for example, cross-linking agents. It is the copolymer which constitutes the subject matter of the invention, i.e., the biologically active substance…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.