Endothelin analogues with alpha-amine substitution at...

C - Chemistry – Metallurgy – 07 – K

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C07K 14/575 (2006.01) A61K 38/22 (2006.01)

Patent

CA 2072390

HA575 Abstract ENDOTHELIN ANALOGUES WITH ALPHA- AMINE SUBSTITUTION AT RESIDUE 20 Endothelin receptor antagonism is exhibited by novel compounds of the formula Image wherein: Image ; R9 is alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, or aralkyl; R10 is alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, or cycloalkenylalkyl; or R9 and R10 together are an alkylene chain of three to five carbons (e.g., such that A20 is prolyl), optionally substituted with one or two alkyl, alkoxy, aryl, aralkyl, cycloalkyl, or hydroxy groups; and the remaining symbols are as defined in the specification.

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