17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216224%3A14310%2F04%3A00036032" target="_blank" >RIV/00216224:14310/04:00036032 - isvavai.cz</a>
Result on the web
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DOI - Digital Object Identifier
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Alternative languages
Result language
angličtina
Original language name
17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors
Original language description
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
Czech name
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Czech description
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Classification
Type
P - Patent
CEP classification
CC - Organic chemistry
OECD FORD branch
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Result continuities
Project
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Continuities
N - Vyzkumna aktivita podporovana z neverejnych zdroju
Others
Publication year
2004
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Patent/design ID
WO 2004/046111 A1
Publisher
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Publisher name
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Place of publication
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Publication country
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Date of acceptance
Jun 3, 2004
Owner name
Schering-Plough
Method of use
A - Výsledek využívá pouze poskytovatel
Usage type
A - K využití výsledku jiným subjektem je vždy nutné nabytí licence