17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors

PARUCH, Kamil and Timothy GUZI. 17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors. 2004.

Basic information

Original name

17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors

Name in Czech

17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors

Authors

PARUCH, Kamil (203 Czech Republic, guarantor) and Timothy GUZI (840 United States of America)

Edition

Number: WO 2004/046111 A1, Publisher: World Intellectual Property Organization, Place of publication: USA, Owner's name: Schering-Plough, 2004

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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/00216224:14310/04:00036032

Organization unit

Faculty of Science

Keywords (in Czech)

hydroxysteroid dehydrogenase; inhibitor; prostate cancer

Keywords in English

hydroxysteroid dehydrogenase; inhibitor; prostate cancer

Tags

hydroxysteroid dehydrogenase, inhibitor, prostate cancer

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Abstract

V originále

The invention relates to a prepn. of piperazine derivs. of formula I [wherein: X is CH or N; Z is O or NH, N-alkyl, or N-aryl, etc.; R1 and R2 are independently selected from (un)substituted (hetero)aryl, (hetero)arylalkyl; R3 is H, OH, alkoxy, aryloxy, etc.; R4 is H, (cyclo)alkyl, (hetero)aryl, etc.; R5 is C(O)R6 or SO2R6; R6 is alkyl, (hetero)aryl, (hetero)arylalkyl, (un)substituted amine], useful as inhibitors of type 3 17.beta.-hydroxysteroid dehydrogenase. The invention compds. are claimed to be useful for the treatment, prevention, inhibition, or amelioration of diseases such as prostate cancer, acne, and androgenic alopecia, etc. The invention compds. exhibited a range of 17.beta.-hydroxysteroid dehydrogenase type 3 binding activity from about 0.005 nM to 10 nM. For instance, piperazine deriv. II was prepd. via amination of phenyl(trifluoromethylphenyl)methanol by (S)-2-tert-butylpiperazine (example 7) and subsequent reaction of the obtained piperazine deriv. III and piperidine deriv. IV (example 15).

In Czech

viz Anotace