Derivatives of lh-rh

Details Derivatives of lh-rh Derivatives of lh-rh

C - Chemistry, Metallurgy

07

K

530/7.2

C07K 7/23 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1082173

ABSTRACT OF THE DISCLOSURE A peptide amide derivative of general formula (I) pGlu-His-Trp-Ser-Tyr-X-Y-Arg-Pro-Z (I) wherein when X is Gly, Y is Leu and Z is .beta.-Ala-NH2 or Sar-NH2; when X is D-Ala, Y is Leu, Ile, Nle, Val, Nval, or Met and Z is Gly-NH2; .beta.-Ala-NH2 or Sar-NH2, provided that when X is D-Ala and Y is Leu Z is not Gly-NH2, and when X is .beta.-Ala, Y is Leu, Ile, Nle, Val, Nval or Met and Z is Gly-NH2, .beta.-Ala-NH2, Sar-NH2 or -NRR' wherein R and R', which may be the same or different, are H, lower alkyl containing from 1 to 6 carbon atoms, substituted lower alkyl containing from 1 to 6 carbon atoms, or together may form a ring; or a pharma- ceutically acceptable acid-addition salt or metal-ion complex thereof; and an inert carrier therefor The derivative shows high activity in releasing pituitary luteinizing hormone (LH) and follicle stimulating hormone (FSH) and as a conse- quence shows high ovulation inducing actlvity.

250589

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