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Claims for Patent: 5,767,082

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Claims for Patent: 5,767,082

Title: Nonapeptide and decapeptide analogs of LHRH useful as LHRH antagonists
Abstract:Synthetic nona- and decapeptide LHRH antagonist analogs are disclosed, having a sterically hindered guanidino-substituted arginyl or homoarginyl residue at position 8, with no arginyl substituent at position 6.
Inventor(s): Nestor, Jr.; John J. (San Jose, CA), Vickery; Brian H. (Saratoga, CA)
Assignee: Syntex (U.S.A.) Inc. (Palo Alto, CA)
Application Number:08/526,940
Patent Claims: 1. A method of: inhibiting ovulation in a female mammalian subject; preventing ovarian hyperstimulation in response to exogenous gonadotropins in a female human subject; treating premenstrual syndrome in a female human subject; treating endometriosis in a female human subject; treating prostatic hypertrophy in a male mammalian subject; inhibiting spermatogenesis in a male mammalian subject; treating precocious puberty in a human subject; interrupting heat in a female animal subject; or terminating pregnancy in a female mammalian subject; which method comprises administering to said subject an effective amount of at least one member of the group consisting of:

(a) a compound of the formula ##STR6## wherein: A is an amino acyl residue selected from the group consisting of either the D- or the L- isomer of:

N-Ac-D,L-.DELTA..sup.3,4 -prolyl, N-Ac-D,L-prolyl, N-Ac-D,L-phenylalanyl,

N-Ac-D,L-p-chlorophenylalanyl, N-Ac-D,L,-p-fluorophenylalanyl,

N-Ac-3-(1-naphthyl)-D,L-alanyl, N-Ac-3-(2-naphthyl)-D,L-alanyl,

and N-Ac-3-(2,4,6-trimethylphenyl)-D,L-alanyl;

B is an amino acyl residue selected from the group consisting of D-phenylalanyl, D-p-chlorophenylalanyl, D-p-fluorophenylalanyl, D-p-nitrophenylalanyl, 2,2-diphenylglycyl, D-.alpha.-methyl-p-chlorophenylalanyl and 3-(2-naphthyl)-D-alanyl;

C is an amino acyl residue selected from the group consisting of D-tryptophanyl, D-phenylalanyl, 3-(3-pyridyl)-D-alanyl, and 3-(2-naphthyl)-D-alanyl;

D is an amino acyl residue selected from the group consisting of L-phenylalanyl, L-tyrosyl, and 3-(3-pyridyl)-alanyl, arginyl, or G;

E is 3-(2-naphthyl)-D-alanyl, 3-(3-pyridyl)-D-alanyl, D-tyrosyl, D-tryptophanyl, D-nicotinyl-lysyl, pyridylacetyl-lysyl, D-Glu(AA) or G;

F is an amino acyl residue selected from the group consisting of L-leucyl, L-norleucyl, L-phenylalanyl, L-tryptophanyl, and 3-(2-naphthyl)-L-alanyl;

G is an amino acyl residue selected from the group consisting of the radicals represented by the following structural formulae: ##STR7## wherein n is 1 to 5;

R.sup.1 is alkyl of 1 to 6 carbon atoms or fluoroalkyl;

R.sup.2 is hydrogen or R.sup.1 ; or R.sup.1 --HN--C.dbd.NR.sup.2 is a ring represented by the following structural formulas: ##STR8## wherein m is 1 to 4; A is hydrogen or alkyl of 1 to 6 carbon atoms; and X is halo or A; and ##STR9## wherein R.sup.3 is hydrogen, alkyl of 1 to 6 carbon atoms, phenyl or phenylloweralkyl; and

J is D-alaninamide; D-leucinamide; glycinamide; or --NHR.sup.4 wherein R.sup.4 is lower alkyl or NHCONH.sub.2 ;

(b) a pharmaceutically acceptable salt of said compound (a) above; or

(c) a pharmaceutical composition containing at least one compound of (a) above or one salt of (b) above, in admixture with a pharmaceutically acceptable excipient.

2. A method of: inhibiting ovulation in a female mammalian subject; preventing ovarian hyperstimulation in response to exogenous gonadotropins in a female subject; treating premenstrual syndrome in a female human subject; treating endometriosis in a female human subject; treating prostatic hypertrophy in a male mammalian subject; inhibiting spermatogenesis in a male mammalian subject; treating precocious puberty in a human subject; interrupting heat in a female animal subject; or terminating pregnancy in a female mammalian subject; which method comprises administering to said subject an effective amount of at least one member of the group consisting of:

(a) a compound of the formula: ##STR10## wherein A is N-Ac-D-Nal(2);

B is D-pCl-Phe;

C is D-Pal(3);

D is Pal(3), Tyr, Arg, Deh, Mbh, or Bth;

E is D-Pal(3), D-Tyr or D-Deh;

F is Leu;

G is Deh, Bth, or Mbh; and

J is D-AlaNH.sub.2 ;

(b) a pharmaceutically acceptable salt of said compound (a) above; or

(c) a pharmaceutical composition containing at least one compound of (a) above or one salt of (b) above, in admixture with a pharmaceutically acceptable excipient.

3. A method of: inhibiting ovulation in a mammalian female subject; preventing ovarian hyperstimulation in response to exogenous gonadotropins in a female human subject; treating premenstrual syndrome in a female human subject; treating endometriosis in a female human subject; treating prostatic hypertrophy in a male mammalian subject, inhibiting spermatogenesis in a male mammalian subject; treating precocious puberty in a human subject; interrupting heat in a female animal subject; or terminating pregnancy in a female mammalian subject; which method comprises administering to said subject an effective amount of the compound:

N-Ac-D-Nal(2)-D-pCl-Phe-D-Pal(3)-Ser-Tyr-D-Deh-Leu-Deh-Pro-D-AlaNH.sub.2 ;

an optical isomer thereof or a pharmaceutically acceptable salt thereof, in admixture with at least one pharmaceutically acceptable excipient.
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