Lhrh antagonists

Details Lhrh antagonists Lhrh antagonists

C - Chemistry, Metallurgy

07

K

530/17.08, 530/7

C07K 14/59 (2006.01) A61K 38/24 (2006.01) C07K 1/06 (2006.01) C07K 7/23 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1339623

The present invention provides LHRH antagonists which possess improved water solubility and, while having the high antagonist potency of the basic peptides, are free of the edematogenic effects. These compounds are highly potent in inhibiting the release of gonadotropins from the pituitary gland in mammals, including humans. The compounds of this invention are represented by the formula X-R1-R2-R3-Ser-Tyr-R6-Leu-Arg-Pro-R10-NH2 wherein X is an acyl group derived from straight or branched chain aliphatic or alicyclic carboxylic acids having from 1 to 7 carbon atoms or H2N-CO, R1 is D- or L-Pro, D- or L-.DELTA. 3-Pro, D-Phe, D-Phe(4-Hl), D-Ser, D-Thr, D-Ala, D-Nal(l) or D-Nal(2), R2 is D-Phe or D-Phe(4-Hl), R3 is D-Trp, D-Phe, D-Pal(3), D-Nal(l) or D-Nal(2), R6 is D-Cit, D-Hci, D-Cit(Q) or D-Hci(Q), and R10 is Gly or D-Ala; in which Q is lower alkyl of 1-3 carbon atoms and Hl is fluoro, chloro or bromo; the pharmaceutically-acceptable acid addition salts thereof, and methods of use pertaining to these compounds.

572236

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