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Inhibitors of ATR Kinase for Use in Methods of Treating Hyperproliferative Diseases
专利权人:
바이엘 악티엔게젤샤프트;바이엘 파마 악티엔게젤샤프트
发明人:
벤그너, 안체, 마르그렛,지마이스터, 게르하르트,핸들러, 베르나르트,골피어, 스벤,슐리커, 안드레아스,리우, 리
申请号:
KR1020197024418
公开号:
KR1020190120204A
申请日:
2018.02.22
申请国别(地区):
KR
年份:
2019
代理人:
摘要:
The present invention provides 2-[(3R) -3-methylmorpholin-4-yl] -4- (1-methyl-1H-pyra, an inhibitor of ATR kinase, for use in a method of treating a hyperproliferative disease in a subject. Sol-5-yl) -8- (1H-pyrazol-5-yl) -1,7-naphthyridine (hereinafter referred to as "Compound A"). Preferably the hyperproliferative disease or subject is a) APC, ATG5, ARID1A, ATM, ATR, ATRIP, ATRX, BAP1, BARD1, BLM, BRAF, BRCA1, BRCA2, BRIP1, CCND1, CCNE1, CCNE2, CDC7, CDK12, CHEK1 , CHEK2, DCLRE1A, DCLRE1B, DCLRE1C, DYRK1A, EGFR, ERBB2, ERBB3, ERCC2, ERCC3, ERCC4, ERCC5, FAM175A, FANCA, FANCB, FANCC, FANCD2, FANCE, FANCF, FANCF, FANCG, FANCG18 , FEN1, GEN1, HDAC2, H2AFX, HRAS, KRAS, LIG4, MDC1, MLH1, MLH3, MRE11A, MSH2, MSH3, MSH6, MYC, NBN, NRAS, PALB2, PARP1, PARP2, PARP3, PARP4, PCNA, PIK3CA, PMS2 , POLA1, POLB, POLH, POLL, POLN, POLQ, PRKDC, PTEN, RAD9A, RAD17, RAD18, RAD50, RAD51, RAD52, RAD54B, RAD54L, RB1, REV3L, RPA1, RPA2, SLX4, TDP1, TDP2, TMPRSS2 One or more gene (s) selected from ERG, TOPBP1, TOP2A, TOP2B, TP53, TP53BP1, TRRAP, UBE2N, UIMC1, USP1, WDR48, WRN, XPA, XRCC1, XRCC2, XRCC3, XRCC4 and / or XRCC6 genes / proteins One or more functional mutation (s) in protein (s); And / or b) activation of the ALT pathway; And / or c) one or more biomarker (s) selected from microsatellite instability. The present invention also provides kits comprising Compound A together with means for detecting one or more of the aforementioned biomarker (s) and methods of identifying subjects with hyperproliferative diseases that tend to favorably respond to Compound A. Wherein the method comprises detecting one or more of the aforementioned biomarker (s). Additionally, the present invention includes a method of determining whether a subject with a hyperproliferative disease will respond to treatment with Compound A, wherein the method comprises the detection of one or more of the aforementioned biomarker (s) in a sample of the subject. do.본 발명은 대상체에서 과다증식성 질환을 치료하는 방법에 사용하기 위한, ATR 키나제의 억제제
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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