MACROCYCLIC KRAS INHIBITORS AND METHODS OF USE

To provide macrocyclic KRAS inhibitors and methods of use.SOLUTION: The present disclosure provides compounds useful for the inhibition of KRAS G12D, G12V, G12A, G12S, G13D, Q61H, Q61L or G12C. The compounds have the general Formula I' in the figure, where the variables in the Formula I' a...

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Hauptverfasser:	BRIAN ALAN LANMAN, RRIMALI VASUNDERA NAVARATNE, QUENTIN TERCENIO, LIPING H PETTUS, RYAN PAUL WURZ, ADRIANO BAUER, RENE RAHIMOFF, BENJAMIN WIGMAN, ALBERT AMEGADZIE, LI XIAOFEN, CHRISTOPHER MOHR, JOSE M MEDINA, JOHN CHARLES STELLWAGEN, FABIEN EMMETIERE, LI YUNXIAO, AARON C SIEGMUND, LIU QINGYIAN, SHON BOOKER, ZHAO WEI, CHEN NING, ANDREW SMALIGO, KEXUE LI, MICHAEL MASAHARU YAMANO, WU ZHICHEN
Format:	Patent
Sprache:	eng ; jpn
Schlagworte:	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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Beschreibung
Zusammenfassung:	To provide macrocyclic KRAS inhibitors and methods of use.SOLUTION: The present disclosure provides compounds useful for the inhibition of KRAS G12D, G12V, G12A, G12S, G13D, Q61H, Q61L or G12C. The compounds have the general Formula I' in the figure, where the variables in the Formula I' are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, e.g., cancer.SELECTED DRAWING: None 【課題】大環状ＫＲＡＳ阻害剤及び使用方法を提供する。【解決手段】本開示は、ＫＲＡＳＧ１２Ｄ、Ｇ１２Ｖ、Ｇ１２Ａ、Ｇ１２Ｓ、Ｇ１３Ｄ、Ｑ６１Ｈ、Ｑ６１Ｌ又はＧ１２Ｃの阻害に有用な化合物を提供する。化合物は、一般式Ｉ'：TIFF2024071370000848.tif45170（式中、式Ｉ'の変数は、本明細書で定義される）を有する。本開示は、その化合物を含む医薬組成物、その化合物の使用及び例えば癌の治療のための組成物も提供する。【選択図】なし