FIELD: pharmacology.
SUBSTANCE: group of inventions is a Ras antagonist represented by the formula R1-R2-R3-R4, where: R3 is S; R4 is farnesyl or geranyl-geranyl, wherein geranyl-geranyl has the structure
:
R2 is a 5-membered heterocyclic ring containing one S heteroatom; R1 is C(=O)R5, CO2M; R5 is hydroxyl; M is a salt forming an organic or inorganic counterion; and R8is hydrogen or C1-C4 alkyl; and pharmaceutically acceptable salts thereof; or R1 is a 5-membered heterocyclic ring containing 2-4 N heteroatoms and R2 is a phenyl ring; or R2 is a 5-membered heterocyclic ring containing three heteroatoms selected from N and S, and R1 is C(=O)R10, and R10 is hydrogen, hydroxyl or C1-C4 alkyloxy. The invention also relates to a method for inhibition of Ras-induced cell proliferation associated with a malignant or non-malignant disease, comprising Ras antagonist administration to a patient.
EFFECT: increased efficiency of treatment.
20 cl, 9 ex, 7 dwg
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Authors
Dates
2017-10-02—Published
2012-10-05—Filed