17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the
Treatment of Androgen Dependent Diseases

P 2003

17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases

GUZI, Timothy, Kamil PARUCH, Alan MALLAMS, Jocelyn RIVERA, Ronald DOLL et. al.

Základní údaje

Originální název

17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases

Název česky

17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases

Autoři

GUZI, Timothy (840 Spojené státy), Kamil PARUCH (203 Česká republika, garant), Alan MALLAMS (840 Spojené státy), Jocelyn RIVERA (840 Spojené státy), Ronald DOLL (840 Spojené státy), Viyyoor GIRIJAVALLABHAN (840 Spojené státy), Jonathan PACHTER (840 Spojené státy), Yi-Tsung LIU (840 Spojené státy) a Anil SAKSENA (840 Spojené státy)

Vydání

Číslo: WO 2003/22835 A1, Vydavatel: World Intellectual Property Organization, Místo vydání: USA, Název vlastníka: Schering-Plough, 2003

Další údaje

Jazyk

angličtina

Typ výsledku

Patent

Obor

10401 Organic chemistry

Stát vydavatele

Spojené státy

Utajení

není předmětem státního či obchodního tajemství

Kód RIV

RIV/00216224:14310/03:00036034

Organizační jednotka

Přírodovědecká fakulta

Klíčová slova česky

hydroxysteroid dehydrogenase; inhibitor; prostate cancer

Klíčová slova anglicky

hydroxysteroid dehydrogenase; inhibitor; prostate cancer

Štítky

hydroxysteroid dehydrogenase, inhibitor, prostate cancer

Změněno: 25. 6. 2009 14:58, doc. Mgr. Kamil Paruch, Ph.D.

Anotace

ORIG CZ

V originále

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.

Česky

viz Anotace

Citovat

GUZI, Timothy, Kamil PARUCH, Alan MALLAMS, Jocelyn RIVERA, Ronald DOLL, Viyyoor GIRIJAVALLABHAN, Jonathan PACHTER, Yi-Tsung LIU a Anil SAKSENA. 17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases. 2003. Patent. Číslo: WO 2003/22835 A1. Vydavatel: World Intellectual Property Organization. Místo vydání: USA. Název vlastníka: Schering-Plough. Datum registrace: 5. 9. 2002. Datum přijetí: 20. 3. 2003.

@misc{838523,
   author = {Guzi, Timothy and Paruch, Kamil and Mallams, Alan and Rivera, Jocelyn and Doll, Ronald and Girijavallabhan, Viyyoor and Pachter, Jonathan and Liu, YiandTsung and Saksena, Anil},
   keywords = {hydroxysteroid dehydrogenase; inhibitor; prostate cancer},
   language = {eng},
   title = {17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases},
   year = {2003}
}

TY  - PAT
ID  - 838523
AU  - Guzi, Timothy - Paruch, Kamil - Mallams, Alan - Rivera, Jocelyn - Doll, Ronald - Girijavallabhan, Viyyoor - Pachter, Jonathan - Liu, Yi-Tsung - Saksena, Anil
PY  - 2003
TI  - 17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases
KW  - hydroxysteroid dehydrogenase
KW  - inhibitor
KW  - prostate cancer
N2  - 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.
ER  -

GUZI, Timothy, Kamil PARUCH, Alan MALLAMS, Jocelyn RIVERA, Ronald DOLL, Viyyoor GIRIJAVALLABHAN, Jonathan PACHTER, Yi-Tsung LIU a Anil SAKSENA. \textit{17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases}. 2003. Patent. Číslo: WO 2003/22835 A1. Vydavatel: World Intellectual Property Organization. Místo vydání: USA. Název vlastníka: Schering-Plough. Datum registrace: 5. 9. 2002. Datum přijetí: 20. 3. 2003.

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