P 2003

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

GUZI, Timothy, Kamil PARUCH, Alan MALLAMS, Jocelyn RIVERA, Ronald DOLL et. al.

Basic information

Original name

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

Name in Czech

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

Authors

GUZI, Timothy (840 United States of America), Kamil PARUCH (203 Czech Republic, guarantor), Alan MALLAMS (840 United States of America), Jocelyn RIVERA (840 United States of America), Ronald DOLL (840 United States of America), Viyyoor GIRIJAVALLABHAN (840 United States of America), Jonathan PACHTER (840 United States of America), Yi-Tsung LIU (840 United States of America) and Anil SAKSENA (840 United States of America)

Edition

Number: WO 2003/22835 A1, Publisher: World Intellectual Property Organization, Place of publication: USA, Owner's name: Schering-Plough, 2003

Other information

Language

English

Type of outcome

Patent

Field of Study

10401 Organic chemistry

Country of publisher

United States of America

Confidentiality degree

není předmětem státního či obchodního tajemství

RIV identification code

RIV/00216224:14310/03:00036034

Organization unit

Faculty of Science

Keywords (in Czech)

hydroxysteroid dehydrogenase; inhibitor; prostate cancer

Keywords in English

hydroxysteroid dehydrogenase; inhibitor; prostate cancer

Tags

Změněno: 25/6/2009 14:58, doc. Mgr. Kamil Paruch, Ph.D.

Abstract

ORIG CZ

V originále

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.

In Czech

viz Anotace