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PTERIDINES AS FGFR INHIBITORS
专利权人:
ASTEKS TERAPYUTIKS LIMITED
发明人:
SAKSTI Gordon (GB),САКСТИ Гордон (GB),KHAMLETT Kristofer Charlz Frederik (GB),ХАМЛЕТТ Кристофер Чарльз Фредерик (GB),BERDINI Valerio (GB),БЕРДИНИ Валерио (GB),MYURREJ Kristofer Uillyam (GB),МЮРРЕЙ Кри
申请号:
RU2014153050
公开号:
RU0002702906C2
申请日:
2013.05.30
申请国别(地区):
RU
年份:
2019
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to a novel pteridine derivative of formula (I), including any stereochemically isomeric form thereof and a pharmaceutically acceptable salt thereof. In particular, the compounds can be used in treating or preventing cancer selected from prostate cancer, bladder cancer, lung cancer, such as non-small cell lung carcinoma, breast cancer, stomach cancer and liver cancer, multiple myeloma, myeloproliferative disorders, endometrial cancer, ovarian cancer, colorectal cancer and squamous cell carcinoma of the oral cavity. Compounds can be used, for example, in treating bladder cancer, with translocation of FGFR3 chromosomes and with a point mutation FGFR3. Cancer can be a tumour with mutations FGFR1, FGFR2, FGFR3 or FGFR4, in particular mutant FGFR2 or FGFR3 with the acquisition of a new function or with overexpression of FGFR1. In formula (I)W is -N(R3) -; each R2 is independently selected from halogen and C1-4alkoxy; D is phenyl or 5-member aromatic monocyclic heterocyclyl containing two heteroatoms of nitrogen, where each said phenyl and heterocyclyl can optionally be substituted with one group R1; R1 is hydrogen or C1-6alkyl; R3 is halo C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyl substituted with R9, C1-6alkyl substituted with -NR10R11; R9 is C3-8cycloalkyl or 5-member monocyclic unsaturated or saturated heterocyclyl containing one or two heteroatoms of nitrogen, where each said C3-8cycloalkyl or 5-member monocyclic heterocyclyl, and each is independently substituted with 1 substituent selected from = O, C1-4alkyl and -S(=O)2-NR14R15; each R10 and R11 independently represents hydrogen or C1-6alkyl; each R14 and R15 independently represent hydrogen or C1-4alkyl; n independently represents an integer equal to 0, 1, 2, 3 or 4.EFFECT: compounds have the properties of a FGFR kinase inhibitor and can be used to treat a disease or condition mediated by FGFR kinase, particularly cancer.27 cl, 1 tbl, 4 exИзобретение относится к новому про
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