About: 17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
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 deriv. 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. (en)
Title	17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors 17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors (en)
skos:prefLabel	17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors 17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors (en)
skos:notation	RIV/00216224:14310/04:00036032!RIV10-MSM-14310___
http://linked.open...tracePatentuVzoru	2003-11-14 (xsd:date)
http://linked.open...avai/riv/aktivita	N
http://linked.open...avai/riv/aktivity	N
http://linked.open...cisloPatentuVzoru	WO 2004/046111 A1
http://linked.open...eleniPatentuVzoru	2004-06-03 (xsd:date)
http://linked.open...vai/riv/dodaniDat	2010
http://linked.open...aciTvurceVysledku	Paruch, Kamil
http://linked.open.../riv/druhVysledku	P - Patent
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Masarykova univerzita / Přírodovědecká fakulta
http://linked.open...dnocenehoVysledku	596544
http://linked.open...ai/riv/idVysledku	RIV/00216224:14310/04:00036032
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	hydroxysteroid dehydrogenase; inhibitor; prostate cancer (en)
http://linked.open.../riv/klicoveSlovo	prostate cancer hydroxysteroid dehydrogenase inhibitor
http://linked.open...ontrolniKodProRIV	[AA7034C53A0B]
http://linked.open.../licencniPoplatek	A - Poskytovatel licence na výsledek požaduje licenční poplatek
http://linked.open...ydaniPatentuVzoru	USA
http://linked.open...atelePatentuVzoru	World Intellectual Property Organization
http://linked.open...in/vavai/riv/obor	CC
http://linked.open...ichTvurcuVysledku	1 (xsd:int)
http://linked.open...cetTvurcuVysledku	2 (xsd:int)
http://linked.open...UplatneniVysledku	2004
http://linked.open...ydaniPatentuVzoru	US - Spojené státy americké
http://linked.open...iv/tvurceVysledku	Guzi, Timothy Paruch, Kamil
http://linked.open...mniOchranaPatentu	B - USTPO (Úřad pro patenty a ochranné známky USA)
http://linked.open...avai/riv/vlastnik	Schering-Plough
http://linked.open...itiJinymSubjektem	A - Nabytí licence je nutné vždy
http://linked.open...uzitiPatentuVzoru	A - Pouze udělený nebo využívaný pouze vlastníkem
http://linked.open...stnikPatentuVzoru	Schering-Plough
http://localhost/t...ganizacniJednotka	14310

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