Preparation of imidazopyridine compounds and their use as 5-​HT6 receptor ligands

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15110%2F17%3A73584515" target="_blank" >RIV/61989592:15110/17:73584515 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/61989592:15310/17:73584515

Výsledek na webu

<a href="https://worldwide.espacenet.com/publicationDetails/originalDocument?CC=WO&NR=2017052394A1&KC=A1&FT=D&ND=3&date=20170330&DB=&locale=en_EP#" target="_blank" >https://worldwide.espacenet.com/publicationDetails/originalDocument?CC=WO&NR=2017052394A1&KC=A1&FT=D&ND=3&date=20170330&DB=&locale=en_EP#</a>

DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

Preparation of imidazopyridine compounds and their use as 5-​HT6 receptor ligands

Popis výsledku v původním jazyce

The invention relates to novel imidazo​pyridine and imidazo​pyridine derivs. of formula I as antagonists of 5-​HT6 receptors; their prepn. and use in the prevention or treatment of schizophrenia, anxiety, depression and other diseases. Compds. of formula I wherein A1 and A2 are different and are N and C; R1 is H and C1-​3 alkyl; R2 is H, (un)​substituted alkyl, (un)​substituted 5- to 6-​membered aryl, etc.; T is CH2, SO2, substituted C1-​2 alkyl; R3 is 5- to 6-​membered unsubstituted aryl, 8- to 10-​membered biaryl, 8- to 10 -​membered heteroaryl, etc.; and tautomers, stereoisomers, enantiomers, N-​oxide, a pharmaceutically acceptable salts, hydrates and solvates thereof, are claimed. Example compd. II was prepd. by a general procedure using solid-​phase synthesis. The invention compds. were evaluated for their 5-​HT6 antagonistic activity. From the assay, it was detd. that compd. II exhibited Ki value of 120 nM.

Název v anglickém jazyce

Preparation of imidazopyridine compounds and their use as 5-​HT6 receptor ligands

Popis výsledku anglicky

The invention relates to novel imidazo​pyridine and imidazo​pyridine derivs. of formula I as antagonists of 5-​HT6 receptors; their prepn. and use in the prevention or treatment of schizophrenia, anxiety, depression and other diseases. Compds. of formula I wherein A1 and A2 are different and are N and C; R1 is H and C1-​3 alkyl; R2 is H, (un)​substituted alkyl, (un)​substituted 5- to 6-​membered aryl, etc.; T is CH2, SO2, substituted C1-​2 alkyl; R3 is 5- to 6-​membered unsubstituted aryl, 8- to 10-​membered biaryl, 8- to 10 -​membered heteroaryl, etc.; and tautomers, stereoisomers, enantiomers, N-​oxide, a pharmaceutically acceptable salts, hydrates and solvates thereof, are claimed. Example compd. II was prepd. by a general procedure using solid-​phase synthesis. The invention compds. were evaluated for their 5-​HT6 antagonistic activity. From the assay, it was detd. that compd. II exhibited Ki value of 120 nM.

Druh

P - Patent

CEP obor

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OECD FORD obor

10401 - Organic chemistry

Projekt

<a href="/cs/project/LO1304" target="_blank" >LO1304: Podpora udržitelnosti Ústavu molekulární a translační medicíny</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2017

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Číslo patentu nebo vzoru

WO 2017052394

Vydavatel

EPO_1 -

Název vydavatele

European Patent Office

Místo vydání

Munich, The Hague, Berlin, Vienna, Brussels

Stát vydání

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Datum přijetí

30. 3. 2017

Název vlastníka

Uniwersytet Jagiellonski; Palacky University Olomouc; Instytut Farmakologii Polskej Akademii Nauk

Způsob využití

A - Výsledek využívá pouze poskytovatel

Druh možnosti využití

A - K využití výsledku jiným subjektem je vždy nutné nabytí licence