Nonapeptide and decapeptide analogs of lhrh, useful as lhrh...

Details Nonapeptide and decapeptide analogs of lhrh, useful as lhrh... Nonapeptide and decapeptide analogs of lhrh, useful as lhrh...

C - Chemistry, Metallurgy

07

K

530/7.2, 167/103

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

Patent

CA 1267999

24160-FF ABSTRACT OF THE DISCLOSURE Nonapeptide and decapeptide analogs of LHRH which are useful as LHRH agonists and have the formula pyro)Glu-His-A-Ser-B-C-D-E-Pro-F (I) 1 2 3 4 5 6 7 8 9 10 and the pharmaceutically acceptable salts thereof, wherein: A is tryptophyl, phenylalanyl, 3-(1-naphthyl)-L- alanyl or 3-(2-napthyl)-L-alanyl; B is tyrosyl, phenylalanyl, histidyl or 3-(1-pentafluoro-phenyl)-L-alanyl; C is an amino acyl residue selected from the group consisting of the radicals represented by the following structural formulas: a) Image (II) 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 hydrogen, alkyl of 1 to 12 carbon atoms, cycloalkyl, fluoroalkyl, 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 IIA IIB IIC IID 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) (III) Image wherein R5 is alkyl of 1 to 12 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 (IV) (Y) Image Image wherein R9 is hydrogen, alkyl of 1 to 12 carbon atoms, phenyl or phenylloweralkyl; D is leucyl, isoleucyl, nor-leucyl, N-methyl-leucyl or tryptophanyl; E is arginyl, glutaminyl, tyrosyl or leucyl; and F is glycinamide or -NH-R1, wherein R1 is lower alkyl, cycloalkyl, fluro lower alkyl or -NH-CO-NH-R2 wherein R2 is hydrogen or lower alkyl.

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