SMYD INHIBITORS

• Main Authors: LORNA HELEN MITCHELL, JAMES EDWARD JOHN MILLS, MEGAN ALENE CLOONAN FOLEY, DARREN MARTIN HARVEY, MICHAEL JOHN MUNCHHOF, KEVIN WAYNE KUNTZ
• Format: Patent
• Language: English; Japanese
• Published: 11.06.2020
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

To provide compounds that are SMYD protein inhibitors, such as SMYD3 and SMYD2 inhibitors, as drugs for treating cancer in a mammal.SOLUTION: For example, the compounds are N-(1-(1-((S)-2-aminopropanoyl)piperidin-4-yl)ethyl)-6-chloro-2-oxoindolin-5-carboxamide, N-(1-(4-aminobutanoyl)piperidin-4-yl)-1H-1,2,4-triazol-5-carboxamide, N-((1r,4r)-4-aminocyclohexyl)-1-benzyl-3-methyl-1H-pyrazol-5-carboxamide hydrochloride, and 2-oxo-N-(piperidin-4-ylmethyl)indolin-5-carboxamide hydrochloride.SELECTED DRAWING: None 【課題】哺乳動物の癌を治療するための薬剤としてのＳＭＹＤ３およびＳＭＹＤ２阻害剤などのＳＭＹＤタンパク質阻害剤となる化合物の提供。【解決手段】例えば、Ｎ−（１−（１−（（Ｓ）−２−アミノプロパノイル）ピペリジン−４−イル）エチル）−６−クロロ−２−オキソインドリン−５−カルボキサミド、Ｎ−（１−（４−アミノブタノイル）ピペリジン−４−イル）−１Ｈ−１，２，４−トリアゾール−５−カルボキサミド、Ｎ−（（１ｒ，４ｒ）−４−アミノシクロヘキシル）−１−ベンジル−３−メチル−１Ｈ−ピラゾール−５−カルボキサミド塩酸塩、２−オキソ−Ｎ−（ピペリジン−４−イルメチル）インドリン−５−カルボキサミド塩酸塩。【選択図】なし