Publication details

17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases

Authors

GUZI Timothy PARUCH Kamil MALLAMS Alan RIVERA Jocelyn DOLL Ronald GIRIJAVALLABHAN Viyyoor PACHTER Jonathan LIU Yi-Tsung SAKSENA Anil

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 2003/22835 A1
Description The title compds. [I; R1, R2 = (un)substituted (hetero)aryl, (hetero)arylakyl; R3 = H, OH, alkoxy, alkyl, provided that when X = N, R3 is not OH or alkoxy; R4, R5, R7, R8 = H, OH, alkyl, etc.; R6 = COR15, SO2R15; R9, R10 = H, F, CF3, etc.; R15 = alkyl, cycloalkyl, aryl, etc.; X, Z = C, N] which are useful as inhibitors of Type 3 17.beta.-hydroxysteroid dehydrogenase, were prepd. Thus, treating the amine II.2HCl [X = H] (multi-step synthesis given) with TMSNCO in the presence of TEA in CH2Cl2 afforded 61% II [X = CONH2]. Compds. I have a range of 17.beta.-hydrosteroid dehydrogenase type 3 binding activity from about 0.005 nM to about > 100 nM.

You are running an old browser version. We recommend updating your browser to its latest version.

More info