C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/314, 260/517
C07D 233/88 (2006.01) C07K 7/23 (2006.01) A61K 38/00 (2006.01)
Patent
CA 1264760
23620-FF ABSTRACT OF THE DISCLOSURE Nonapeptide and decapeptide analogs of LHRH which have the formula A-B-C-D-E-F-G-Arg-Pro-H (I) 1 2 3 4 5 6 7 8 9 10 and the pharmaceutically acceptable salts thereof, wherein: A is an amino acyl residue selected from the group consisting of L-pyroglutamyl, D-pyroglutamyl, N-acyl-D,L-tryptophanyl, N-acyl-glycyl, N-Ac-D,L-.DELTA.3,4-prolyl, N-Ac-D,L-prolyl, N-Ac-L-alkylprolyl, N-Ac-D,L-phenylalanyl, N-Ac-D,L-p-chlorophenylalanyl, N-Ac-D,L-seryl, N-Ac-D,L-threonyl, N-Ac-D,L-alanyl, 3-(1-naphtnyl)-D,L-alanyl, 3-(2-naphthyl)-D,L-alanyl, 3-(2,4,6-trimethylphenyl)-D,L-alanyl, 3-(4-trifluoromethylphenyl)-D,L-alanyl, 3-(9-anthryl)-D,L-alanyl, 3-(2-fluorenyl)-D,L-alanyl, and 3-(Het)-D,L-alanyl wherein Het is a heterocyclic aryl containing radical selected from Image wherein A" and A' are independently selected from the group consisting of hydrogen, lower alkyl, chlorine and bromine, and G is selected from the group consisting of oxygen, nitrogen and sulfur; B is an amino acyl residue selected from the group consisting of D-phenylalanyl, D-p-Cl-phenylalanyl, D-p-F-phenylalanyl, D-p-nitrophenylalanyl, 3-(3,4,5-trimethoxyphenyl)-D-alanyl, 2,2-diphenylglycine, D-.alpha.-methyl-p-Cl-phenylalanine and 3-(2,4,6-trimethylphenyl)-D-alanyl; C is an amino acyl residue selected from the group consisting of L-tryptophanyl, D-tryptophanyl, D-phenylalanyl, D-Me5phenylalanyl, 3-(3-pyridyl)-D-alanyl, 3-(1-naphthyl)-D-alanyl, and 3-(2-naphthyl)-D-alanyl;3-(2-pyridyl)-D-alanyl and 3-(4-pyridyl)-D-alanyl; D is an amino acyl residue selected from the group consisting of L-seryl, and D-alanyl; E is an amino acyl residue selected from the group consisting of L-phenylalanyl and L-tyrosyl; F is an amino acyl selected from the group consisting of the radicals represented by the following structural formulas: a) (II) Image wherein n is 1 to 5; R1 is alkyl of 1 to 12 carbon atoms, -NRR3 wherein R is hydrogen or alkyl of 1 to 4 carbon atoms, R3 is alkyl of 1 to 12 carbon atoms, cycloalkyl, phenyl, benzyl, -(CH2)n-morpholino or -(CH2)nN(R4)2 wherein n is 1 to 5 and R4 is lower alkyl; R2 is hydrogen or R3; or R1 and R2 comprise a ring represented by the following structural formulas: Image wherein n is 1 to 7; A is hydrogen, alkyl of 1 to 6 carbon atoms or cycloalkyl; and X is halo or A or b) Image (III) wherein R5 is alkyl of 1 to 6 carbon atoms, benzyl, phenylethyl, cyclohexyl, cyclopentyl; and R6, R7 and R8 are hydrogen or alkyl of 1 to 4 carbon atoms; and n is the integer 2-5; or c) a substituent of the formula Image (IV) Image (V) wherein R9 is hydrogen, alkyl of 1 to 12 carbon atoms, phenyl or phenylloweralkyl; G is an amino acyl residue selected from the group consisting of L-leucyl, L-norleucyl and L-norvalyl; H is D-alaninamide, D-leucinamide, glycinamide or -NHR5 wherein R5 is lower alkyl, cycloalkyl, fluoro lower alkyl, or NHCONH-R10 wherein R10 is hydrogen or lower alkyl; and the pharmaceutically acceptable salts thereof.
566251
Nestor John J.
Vickery Brian H.
Johnson Douglas S. Q.c.
Syntex (u.s.a.) Inc.
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