Peptide compound and its preparation

Details Peptide compound and its preparation Peptide compound and its preparation

C - Chemistry, Metallurgy

07

K

C07K 5/02 (2006.01) A61K 38/05 (2006.01) A61K 38/06 (2006.01) C07K 5/06 (2006.01) C07K 5/078 (2006.01) C07K 5/08 (2006.01) C07K 5/083 (2006.01) C07K 5/103 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2042442

ABSTRACT Peptide compounds of the formula (I): Image (I) in which R1 is hydrogen or acyl, R2 is lower alkyl, optionally substituted ar(lower)alkyl, cyclo(lower)alkyl(lower)alkyl or optionally substituted heterocyclic(lower) alkyl, R3 is optionally substituted heterocyclic(lower)alkyl or optionally substituted ar(lower)alkyl, R4 is hydrogen or optionally substituted lower alkyl, R5 is carboxy, protected carboxy, carboxy(lower)alkyl or protected carboxy(lower)alkyl, R6 is hydrogen or optionally substituted lower alkyl, R7 is hydrogen or lower alkyl, and A is -O-, -NH-, lower alkylimino or lower alkylene, provided that when R2 is (S)-isobutyl, R3 is N-(dichlorobenzyloxycarbonyl)indol-3-yl- methyl, R4 is methyl, R5 is methoxycarbonyl, R6 is hydrogen, R7 is hydrogen and A is -NH-, then the partial formula : Image has the absolute configuration of Image or a pharmaceutically acceptable salt thereof. The preparation of these compounds, pharmaceutical compositions containing same, the preparation of these compositions, and the treatment of endothelin mediated diseases using the above compositions are also dis- closed. The invention is particularly useful for treating hypertension, and the like.

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