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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