INDOLIZINE DERIVATIVES, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF INHIBITION OF ACTIVITY OF TESTOSTERONE-5α-REDUCTASE Russian patent published in 1998 - IPC

Abstract RU 2120942 C1

FIELD: organic chemistry. SUBSTANCE: invention relates to derivatives of indolizine of the formula (I) where R1 - carboxyl, esterified carboxyl; R2 - hydrogen, lower alkyl, halogen; R3 - aryl or ar(lower)- -alkyl, (lower)alkylcarbamoyl, (lower)alkyl, (lower)alkyl- -arylcarbamoyl-(lower)alkyl; R11 - hydrogen, lower alkyl; A - lower alkylene possibly substituted with oxo-group, lower alkylene; Q - carbonyl, lower alkylene; R4, R5 - hydrogen, lower alkyl; y - bond, lower alkylene; Z - lower alkylene, lower alkenylene, -O-, ; R6 - hydrogen, lower alkyl, ar(lower)alkyl that can has a suitable substitute, and their pharmacologically acceptable salts. Compounds are synthesized by interaction of compounds of the formula (II) and (III) where W10 - acid residue. Compounds of the formula (I) can be used as inhibitors of testosterone-5α-reductase for prophylaxis and treatment of diseases mediated with this enzyme (alopecia, acne, prostatitis). EFFECT: improved method of synthesis. 13 cl, 6 dwg, 112 ex

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RU 2 120 942 C1

Authors

Satosi Okada

Kozo Savada

Akio Kuroda

Sinija Vatanabe

Khirokazu Tanaka

Dates

1998-10-27Published

1992-06-16Filed