Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
208 words
A compound of the formula and the pharmaceutically acceptable salts thereof, wherein: . X is a D-alanyl residue wherein one hydrogen on C-3 is replaced by: a) a carbocyclic aryl-containing radical selected from phenyl substituted with three or more straight chain Cl-4 alkyl groups, naphthyl, anthryl, fluorenyl, phenanthryl, biphenylyl and benzhydryl; or b) a saturated carbocyclic radical selected from cyclohexyl substituted with three or more straight chain Cl-4 alkyl groups, perhydronaphthyl, perhydrobiphenylyl, perhydro-2,2-diphenylmethyl, and adamantyl; or c) a heterocyclic aryl containing radical selected from radicals represented by the following structural formulas: wherein A" and A' are independently selected from hydrogen, C 1-4 alkyl, chlorine, and bromine, and G is selected from oxygen, nitrogen, and sulfur; A is an aminoacyl residue selected from L-pyroglutamyl, D-pyroglutamyl, N-acyl-L-prolyl, N-acyl-D-prolyl, N-acyl-D-tryptophanyl, N-acyl-D-phenylalanyl, N-acyl-D-p-halophenylalanyl, and N-acyl-X, wherein X is as defined previously; B is an amino acyl residue selected from D -phenylalanyl, D-p-halophenylalanyl, 2,2-diphenylglycyl, and X wherein X is as defined previously; C is an amino acyl residue selected from L -tryptophanyl, D-tryptophanyl, D-phenylalanyl and X wherein X is as defined above; E is glycinamide or -NH-R 1 , wherein R 1 is C 1-4 alkyl, C 3-6 cycloalkyl, fluoro C 1-4 alkyl or wherein R 2 is hydrogen or C 1-4 alkyl.
Claim 2
Dependent Claim
208 words
A compound of the formula and the pharmaceutically acceptable salts thereof, wherein: . X is a D-alanyl residue wherein one hydrogen on C-3 is replaced by: a) a carbocyclic aryl-containing radical selected from phenyl substituted with three or more straight chain Cl-4 alkyl groups, naphthyl, anthryl, fluorenyl, phenanthryl, biphenylyl and benzhydryl; or b) a saturated carbocyclic radical selected from cyclohexyl substituted with three or more straight chain Cl-4 alkyl groups, perhydronaphthyl, perhydrobiphenylyl, perhydro-2,2-diphenylmethyl, and adamantyl; or c) a heterocyclic aryl containing radical selected from radicals represented by the following structural formulas: wherein A" and A' are independently selected from hydrogen, C 1-4 alkyl, chlorine, and bromine, and G is selected from oxygen, nitrogen, and sulfur; A is an aminoacyl residue selected from L-pyroglutamyl, D-pyroglutamyl, N-acyl-L-prolyl, N-acyl-D-prolyl, N-acyl-D-tryptophanyl, N-acyl-D-phenylalanyl, N-acyl-D-p-halophenylalanyl, and N-acyl-X, wherein X is as defined previously; B is an amino acyl residue selected from D -phenylalanyl, D-p-halophenylalanyl, 2,2-diphenylglycyl, and X wherein X is as defined previously; C is an amino acyl residue selected from L -tryptophanyl, D-tryptophanyl, D-phenylalanyl and X wherein X is as defined above; E is glycinamide or -NH-R 1 , wherein R 1 is C 1-4 alkyl, C 3-6 cycloalkyl, fluoro C 1-4 alkyl or wherein R 2 is hydrogen or C 1-4 alkyl.
Claim 3
Dependent Claim
55 words
The compounds of Claim 1, including the pharmaceutically acceptable salts thereof, wherein A is selected from L-(pyro)Glu, D-(pyro)Glu, NAc-D-Phe and NAc-L-Pro; B is selected from D-Phe, D-p-halo-Phe and DPG; C is selected from L-Trp, D-Trp, D-Nal(l) and D-Nal(2); X is selected from D-Nal(2), D-TMP, D-BIA, and D-TBA; E is selected from GlyNH 2 and AzaGlyNHR.
Claim 4
Dependent Claim
15 words
The compounds of Claim 2, including the pharmaceutically acceptable salts thereof, wherein X is D-Nal(2).
Claim 5
Dependent Claim
20 words
The compounds of Claim 3 including the pharmaceutically acceptable salts thereof, wherein E is GlyNH 2 or AzaGlyNH 2 .
Claim 6
Dependent Claim
35 words
A compound of Claim 4 which is selected from: (pyro)Glu-DPG-Trp-Ser-Tyr-D-Nal(2)-Leu-Arg-Pro-GlyNH 2 , (pyrolGlu-D-Phe-D-Trp-Ser-Tyr-D-Nal(2)-Leu-Arg-Pro-GlyNH 2 , (pyro)Glu-D-Phe-D-Nal(2)-Ser-Tyr-D-Nal(2)-Leu-Arg-Pro-GlyNH 2 , NAc-L-Pro-D-Phe-D-Trp-Ser-Tyr-D-Nal(2)-Leu-Arg-Pro-GlyNH 2 , NAc-D-Phe-D-p-Cl-Phe-D-Trp-Ser-Tyr-D-Nal(2)-Leu-Arg-Pro-GlyNH2; NAc-L-Pro-D-p-C1-Phe-D-Nal(2)-Ser-Tyr-D-Nal(2)-Leu-Arg-Pro-GlyNH 2 ; and NAc-L-Pro-D-p-F-Phe-D-Nal(2)-Ser-Tyr-D-Nal(2)-Leu-Arg-Pro-GlyNH 2 ; and the pharmaceutically acceptable salts thereof.
Claim 7
Dependent Claim
22 words
A compound of any of Claims 1 to 5 for use in treating disorders affecting the reproductive system of a human subject.
Claim 8
Dependent Claim
17 words
A compound of any of Claims 1 to 5 for use in effecting contraception in human beings.
Claim 9
Independent Claim
38 words
A method of effecting contraception in human beings which method comprises administering to a subject an effective amount of, or a pharmaceutical composition containing an effective amount of a compound of any one of Claims 1 to 5.
Claim 10
Dependent Claim
22 words
A pharmaceutical composition which comprises a compound of any one of Claims 1 to 5 in admixture with a pharmaceutically acceptable excipient.
Claim 11
Dependent Claim
89 words
A process for the preparation of a compound of Claim 1 which process comprises: removing protecting groups and, optionally, covalently bound solid support from a protected polypeptide to afford a compound of the Formula (I) or a salt thereof, or optionally (a) converting a compound of the Formula (I) to a pharmaceutically acceptable salt, (b) converting a salt of a compound of the Formula (I) to a pharmaceutically acceptable salt, or (c) decomposing a salt of a compound of Formula (1) to a free polypeptide of the Formula (I).