Pharmacologically active peptides
AssigneeEli Lilly and Company
InventorPaul D. Gesellchen
Life of this patent
Estimating the term…
Abstract
Compounds of the formula [R-Tyr-A-Gly-(N-R.sub.1)Phe(p-Y)-X].sub.2 -(CH.sub.2).sub.n in which R is hydrogen or methyl; A is the residue of a D-amino acid selected from the group consisting of Ala, Abu, Ser, Thr, and Met; R.sub.1 is hydrogen, C.sub.1 -C.sub.3 primary alkyl, cyclopropylmethyl, or allyl; Y is hydrogen or fluoro; n is an integer from 1 to 10; and X is --NH-- or a group of the formula ##STR1## in which R.sub.2 is hydrogen or C.sub.1 -C.sub.3 primary alkyl; R.sub.3 is phenyl, 2-methylthioethyl, or isobutyl; or R.sub.2 and R.sub.3 taken together are --CH.sub.2 --CH.sub.2 --CH.sub.2 --; subject to the limitation that, when R.sub.2 is other than hydrogen, R.sub.1 is hydrogen; are useful analgesic agents.
Claims41
A compound of the formula
- [R-Tyr-A-Gly-(N-R.sub.1)Phe(p-Y)-X].sub.2 -(CH.sub.2).sub.n
- in which
- R is hydrogen or methyl;
- A is the residue of a D-amino acid selected from the group consisting of Ala, Abu, Ser, Thr, and Met;
- R.sub.1 is hydrogen, C.sub.1 -C.sub.3 primary alkyl, cyclopropylmethyl, or allyl;
- Y is hydrogen or fluoro;
- n is an integer from 1 to 10;
- and
- X is --NH-- or a group of the formula ##STR9## in which R.sub.2 is hydrogen or C.sub.1 -C.sub.3 primary alkyl;
- R.sub.3 is phenyl, 2-methylthioethyl, or isobutyl;
- or R.sub.2 and R.sub.3 taken together are --CH.sub.2 --CH.sub.2 --CH.sub.2 --;
- subject to the limitation that, when R.sub.2 is other than hydrogen, R.sub.1 is hydrogen.
Dependencies are inferred from the claim text.