Therapeutic decapeptides

Details Therapeutic decapeptides Therapeutic decapeptides

1989-05-15

1991-12-17

Nutter, Nathan M.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Lutenizing hormone releasing factor ; related peptides

530328, 514800, C07C10352, A61K 3702

Patent

active

050736248

ABSTRACT:
A decapeptide of the formula: N-AC-A.sup.1 -A.sup.2 -A.sup.3 -Ser-A-.sup.4 -A.sup.5 -A.sup.6 -A.sup.7 -A.sup.8 -A.sup.9, wherein each A.sup.1, A.sup.2, and A.sup.3, independently, is D-.beta.-Nal, D-p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, OH, or C.sub.1-3 alkyl), D-benzothienyl (2)-Ala, or D-benzothienyl (1)-Ala; A.sup.4 is p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, or C.sub.1-3 alkyl), Tyr, Lys, Arg, Leu, Trp, or Nal; A.sup.5 is D-Lys, D-Tyr, D-Arg, D-Phe, D-.beta.-Nal, D-Trp, D-homo-Arg, D-diethyl-homo-Arg, D-p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, or C.sub.1-3 alkyl), or D-Lys-.epsilon.-NH-R (where R is H, a branched or straight chain C.sub.1 -C.sub.10 alkyl group, or an aryl group); A.sub.6 is Leu, .beta.-Nal, p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, OH, C.sub.2 F.sub.5, C.sub.1-3 alkyl), or Trp; A.sup.7 is Arg, Lys, or Lys .epsilon.-NH-R (where R is H, a branched or straight chain C.sub.1 -C.sub.6 alkyl group, or an aryl group); A.sub.8 is Pro; and A.sup.9 is D-Ala, D-Ala-NH.sub.2, Ala-NH.sub.2, aminoisobutyric acid amide, or Gly-NH.sub.2 ; provided that at least one of A.sup.2 or A.sup.3 must be D-Phe or D-Tyr, and provided further that when A.sup.4 is Lys or Arg, A.sup.5 must not be D-Arg, D-Lys, D-homo-Arg, D-diethyl-homo-Arg, or D-Lys-.epsilon.-NH-R, or a pharmaceutically acceptable salt thereof.
The invention also features a method of treating T-cell-deficient patients, e.g., those suffering from Acquired Immune Dificiency Syndrome, by administering a therapeutically effective amount of an LH-RH antagonist.

REFERENCES:
patent: 4569967 (1986-02-01), Kornreich et al.
patent: 4642332 (1987-02-01), Folkers et al.
patent: 4866160 (1989-09-01), Coy et al.
Folkers et al. (Abstract No. 84-30988, Naturforsch, B (39, No. 4, 528-32 (1984)).
Nestor et al. (Abstract No. 4-55672 of J. Med. Chem. 27, 1170 (1984)).
Folkers et al., (BBRC 123:1221 (1984)).

Affiliated with

Also associated with

Rating

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

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

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-836285