| 摘要 |
<p>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.</p> |
