PARUCH, Kamil and Timothy GUZI. 17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors. 2004.
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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.
Other information
Original language English
Type of outcome Patent
Field of Study 10401 Organic chemistry
Country of publisher United States of America
Confidentiality degree is not subject to a state or trade secret
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
Changed by Changed by: doc. Mgr. Kamil Paruch, Ph.D., učo 108413. Changed: 25/6/2009 14:45.
Abstract
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).
Abstract (in Czech)
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