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Statements

Subject Item
n2:RIV%2F00216224%3A14310%2F03%3A00036034%21RIV10-MSM-14310___
rdf:type
skos:Concept n17:Vysledek
dcterms:description
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. 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.
dcterms:title
17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases 17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases
skos:prefLabel
17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases 17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases
skos:notation
RIV/00216224:14310/03:00036034!RIV10-MSM-14310___
n3:datumRegistracePatentuVzoru
2002-09-05+02:00
n3:aktivita
n16:N
n3:aktivity
N
n3:cisloPatentuVzoru
WO 2003/22835 A1
n3:datumUdeleniPatentuVzoru
2003-03-20+01:00
n3:dodaniDat
n10:2010
n3:domaciTvurceVysledku
n14:1390333
n3:druhVysledku
n8:P
n3:duvernostUdaju
n4:S
n3:entitaPredkladatele
n6:predkladatel
n3:idSjednocenehoVysledku
636755
n3:idVysledku
RIV/00216224:14310/03:00036034
n3:jazykVysledku
n12:eng
n3:klicovaSlova
hydroxysteroid dehydrogenase; inhibitor; prostate cancer
n3:klicoveSlovo
n13:inhibitor n13:hydroxysteroid%20dehydrogenase n13:prostate%20cancer
n3:kontrolniKodProRIV
[4E7B4AB95B52]
n3:licencniPoplatek
n11:A
n3:mistoVydaniPatentuVzoru
USA
n3:nazevVydavatelePatentuVzoru
World Intellectual Property Organization
n3:obor
n9:CC
n3:pocetDomacichTvurcuVysledku
1
n3:pocetTvurcuVysledku
9
n3:rokUplatneniVysledku
n10:2003
n3:statVydaniPatentuVzoru
n18:US
n3:tvurceVysledku
Saksena, Anil Mallams, Alan Doll, Ronald Liu, Yi-Tsung Pachter, Jonathan Girijavallabhan, Viyyoor Guzi, Timothy Rivera, Jocelyn Paruch, Kamil
n3:uzemniOchranaPatentu
n21:B
n3:vlastnik
n6:vlastnikVysledku
n3:vyuzitiJinymSubjektem
n15:A
n3:vyuzitiPatentuVzoru
n20:A
n3:vlastnikPatentuVzoru
Schering-Plough
n19:organizacniJednotka
14310