Lh-rh analogues

Details Lh-rh analogues Lh-rh analogues

C - Chemistry, Metallurgy

07

K

530/7.2

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

Patent

CA 1057743

ABSTRACT Novel peptide compounds of the formula X1-X2-X3-X4-X5-X6-X7-X8-Pro-W are provided together with their acid addition salts and their complexes with pharmaceutically acceptable metals. The compounds are LH-RH analogues and together with their salts and complexes exhibit LH-RH antagonist activity. In the formula X1 is selected from pyroglutamyl, a group V1-Pro- where V1 is acyl, alkyloxycarbonyl or aralkyloxycarbonyl, and a group V2-CO- where V2 is cycloalkyl; X2 is selected from histidyl and a direct bond; X3 is selected from phenylalanyl optionally substi- tuted in the benzene ring and tryptophyl; X4 is selected from glycyl, seryl, alanyl (D- or L), D-leucyl and D-valyl; X5 is phenylalanyl optionally substituted in the benzene ring; X6 is selected from glycyl, alanyl (D- or L-), D-leucyl and D-valyl; X7 is selected from phenylalanyl optionally substi- tuted in the benzene ring and leucyl; X8 is a direct bond when X2 is histidyl and is otherwise arginyl or homoarginyl; and W is selected from glycine amide and a group -NR1R2 where R1, R2 and the nitrogen atom together comprise a group selected from amino, N-alkylamino, N,N-dialkylamino, pyrrolidino, morpholino and 1-methyl-5- aminomethyltetrazolyl, the 'alkyl' having from 1 to 4 carbon atoms and being optionally substituted by an hydroxyl group, provided that, when X1, X3, X4, X5, X7 and X8 are respectively pyroglutamyl, tryptophyl, seryl, tyrosyl, leucyl and arginyl, W is other than glycine amide or N-ethylamino when X6 is glycyl and is other than glycine amide when X6 is D-alanyl. All references are to the L-amino acids and their radicals except in the case of glycine and unless otherwise stated. Also provided are methods for the preparation of the peptides, salts and complexes, pharmaceutical formula- tions containing them and methods for the preparation of such formulations, and methods for the use of the peptides, salts and complexes in human and in veterinary medicine.

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