Publication details

Piperidine- and Piperazineacetamides as 17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases

Authors

GUZI Timothy PARUCH Kamil

Year of publication 2003
Type Patent
MU Faculty or unit

Faculty of Science

Publisher World Intellectual Property Organization
State United States of America
Patent's number WO 2003/33487 A1
Description Compds. of formula I [R1 = aryl, heteroaryl, arylalkyl, heteroarylalkyl, diphenylalkyl, etc.; R2, R3 = H, OH, alkoxy, alkyl, cycloalkyl, etc.; R4, R5, R7, R8 = H, substituted OH, substituted amino, alkyl, aryl, cycloalkyl, etc.; R6 = acyl, substituted sulfonyl; R9, R10 = H, F, CF3, alkyl, cycloalkyl, arylalkyl, etc.; X, Z = C, N] are prepd. which are useful as inhibitors of Type 3 17.beta.-Hydroxysteroid Dehydrogenase. Also disclosed are pharmaceutical compns. contg. said compds. and their use for the treatment or prevention of androgen dependent diseases. Thus, II was prepd. in several steps. The prepd. compds. had type 3 17.beta.-hydroxysteroid dehydrogenase binding activity of 0.010 to 100 nM.

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