THIOPHENE AND THIAZOLE SUBSTITUTED TRIFLUOROETHANONE DERIVATIVES AS HISTONE DEACETYLASE (HDAC) INHIBITORS

PROBLEM TO BE SOLVED: To provide thiophene and thiazole substituted trifluoroethanone derivatives that are inhibitors of histone deacetylase (HDAC), particularly class II HDAC.SOLUTION: The present invention relates to compounds represented by formula (I), and pharmaceutically acceptable salts and t...

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Main Authors ONTORIA ONTORIA JESUS MARIA, CARSTEN SCHULTZ-FADEMRECHT, JONES PHILIP, ESTER MURAGLIA, FEDERICA FERRIGNO, RITA SCARPELLI
Format Patent
LanguageEnglish
Japanese
Published 18.06.2015
Subjects
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
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Summary:PROBLEM TO BE SOLVED: To provide thiophene and thiazole substituted trifluoroethanone derivatives that are inhibitors of histone deacetylase (HDAC), particularly class II HDAC.SOLUTION: The present invention relates to compounds represented by formula (I), and pharmaceutically acceptable salts and tautomers thereof. The compounds are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. They are also useful for treating neurodegenerative diseases, mental retardation, 10 schizophrenia, inflammatory diseases, restenosis, immune disorders, diabetes, cardiovascular disorders and asthma. 【課題】ヒストン脱アセチル化酵素（ＨＤＡＣ）、特に、クラスＩＩ ＨＤＡＣの阻害剤であるチオフェン及びチアゾール置換トリフルオロエタノン誘導体の提供。【解決手段】式（Ｉ）で示される化合物及びその医薬上許容され得る塩及び互変異性体。前記化合物は、ヒストン脱アセチル化酵素（ＨＤＡＣ）の阻害剤であり、細胞増殖性疾患、例えば、がんを治療するのに有用である。それらはまた、神経変性疾患、精神遅滞、１０統合失調症、炎症性疾患、再狭窄、免疫障害、糖尿病、心血管障害及び喘息を治療するのにも有用である。【選択図】なし
Bibliography:Application Number: JP20140262112