Lhrh antagonists

Details Lhrh antagonists Lhrh antagonists

C - Chemistry, Metallurgy

07

K

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

Patent

CA 2079461

2079461 9213883 PCTABS00014 Disclosed herein are analogues of the luteinizing hormone-releasing hormone (LH-RH), which are potent antagonists of LH-RH. These peptides inhibit the release of gonadrotropins from the pituitary in mammals, including humans and possess antitumor activity. Formula (I): X-R1-R2-R3-Ser-R5-R6(AY2)-Leu-Arg-Pro-D-Ala-NH2 represents peptides which are within the scope of this invention and the pharmaceutically acceptable salts thereof, wherein R1 is D-Phe, D-Phe(4Cl), D-Nal(1) or D-Nal(2), R2 is D-Phe or D-Phe(4Hl), R3 is D-Trp, D-Phe, D-Phe(4Hl), D-Nal(1), D-Nal(2) or D-Pal(3), R5 is Tyr or Arg, R6 is D-Lys or D-Orn, Hl is fluoro, chloro or bromo, X is a lower alkanoyl group of 2-5 carbon atoms, A is a diaminoacyl residue having formula (II), where m is 0 or 1, n is 0 or 1, Y is hydrogen or Y1 or Y2, wherein Y1 is an acyl group derived from straight or branched chain aliphatic, alicyclic carboxylic acids having from 3 to 12 carbon atoms or aromatic carboxylic acid of 6 or 10 ring carbon atoms, Y2 is carbamoyl or alkyl-substituted carbamoyl group having formula (III): H-(CH2)n-NH-CO-, where n is 0-3.

Affiliated with

Also associated with

Rating

Lhrh antagonists does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Lhrh antagonists, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Lhrh antagonists will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFCA-PAI-O-1525375