Bombesin antagonists with deletion of net-residue at the C-terminus
US5068222A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Nov 1, 1988 |
| Grant date | Nov 26, 1991 |
| Priority date | — |
| Expiry date | Nov 1, 2008 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K38/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The invention relates to a polypeptide of formula I: EQU R.sup.1 -A.sup.1 -A.sup.2 -A.sup.3 -A.sup.3 -A.sup.4 -A.sup.5 -A.sup.6 -A.sup.7 -A.sup.9 -Q wherein each of the generic terms is disclosed in full in the specification and includes: R.sup.1 is (2-6C)alkanoyl or (1-4C)alkoxycarbonyl; A.sup.1 is a direct link to A.sup.2, or is Gly or Arg; A.sup.2 is a direct link to A.sup.3, or is Gly or Pro; A.sup.3 is a direct link to A.sup.4, or is Lys or Lys(Z); A.sup.4 is His or D-His; A.sup.5 is Trp or MeTrp; A.sup.6 is Ala or MeAla; A.sup.7 is Val or MeVal; A.sup.8 is Gly or Sar; A.sup.9 is His or MeHis; and Q is a group of the formula -A.sup.10.R.sup.2 in which A.sup.10 is Leu or D-Leu and R.sup.2 is hydroxy, amino, (1-3C)alkylamino or (1-3C)alkoxy; or Q is (1-6C)alkoxy or (1-10C)alkylamino; provided that when R.sup.1 is acetyl and -A.sup.4 -A.sup.5 -A.sup.6 -A.sup.7 -A.sup.8 -A.sup.9 -Q is -His-Trp-Ala-Val-Gly-His-Leu-NH.sub.2 then -A.sup.1 -A.sup.2 -A.sup.3 - is not a direct link to His. The compounds possess antagonist properties against bombesin-like peptides and are of value in the treatment of malignant disease in warm-blooded animals.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.