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Publication details
Piperidine- and Piperazineacetamides as 17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases
Authors | |
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Year of publication | 2003 |
Type | Patent |
MU Faculty or unit | |
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. |