Preparation of phenylalanine derivatives bearing a 1,2,4-triazole moiety and their use in peptides
US5565574A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Aug 11, 1994 |
| Grant date | Oct 15, 1996 |
| Priority date | — |
| Expiry date | Aug 11, 2014 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02P20/55
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Methods of making unnatural amino acids are provided which unnatural amino acids can be incorporated into peptides which either inhibit or promote the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. These unnatural amino acids are useful in the synthesis of peptides and have the formula (a): ##STR1## where W is (CH.sub.2).sub.n or ##STR2## n is an integer from 1 to 6; j=1, 2 or 3, and preferably, Y is N--CN, X is NH and R.sub.2 is alkyl, modified alkyl, alkenyl, alkynyl, aryl or methyl pyridyl. Disclosed are peptides that are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.