| 摘要 |
Nonapeptide and decapeptide analogs of LHRH which have the formula <CHEM> 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-pentafluorophenyl)-L-alanyl; C is an amino acyl residue selected from the radicals represented by the following structural formulas: <CHEM> 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: <CHEM> 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 <CHEM> 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 <CHEM> 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 E is glycinamide or -NH-R<1>, wherein R<1> is lower alkyl, cycloalkyl, fluoro lower alkyl or -NH-CO-NH-R<2> wherein R<2> is hydrogen or lower alkyl. |
