42 results about "VEGFR Inhibitor" patented technology

The invention relates to a pharmaceutical composition containing crenolanib and application of the pharmaceutical composition. The present invention relates to the use of a combination comprising crenolanib or a salt thereof and a VEGF / VEGFR inhibitor of non-axitinib for the preparation of a medicament for the treatment of proliferative diseases, wherein the crenolanib and the VEGF / VEGFR inhibitorof non-axitinib are provided for a subject in at least one of a sequential or simultaneous manner for treating proliferative diseases, and the subject is a human subject.

The invention discloses a synthesis method of VEGFR inhibitor fruquintinib and its benzofuran intermediate. The synthesis method of VEGFR inhibitor fruquintinib in the invention comprises the following steps: S1: halogenation; S2: acyl S3: coupling; S4: ring closure; S5: hydrolysis; S6: amination; S7: substitution. The present invention has few synthetic steps, and the process is simple and easy to operate; no expensive and dangerous compounds are used in the synthetic process, and there is no safety risk; the method uses commercially available starting materials, and the cost is low, which ensures good reproducibility of the synthetic route and is A process suitable for large-scale industrial production.

The present invention provides diagnostic methods, therapeutic methods, and compositions for the treatment of cancer (e.g., kidney cancer (e.g., renal cell carcinoma (RCC)), lung cancer (e.g., non-small cell lung cancer (NSCLC)), bladder cancer (e.g., urothelial bladder cancer (UBC)), liver cancer (e.g., hepatocellular carcinoma (HCC)), ovarian cancer, or breast cancer (e.g., triple-negative breast cancer (TNBC))). The invention is based, at least in part, on the discovery that expression levels of one or more biomarkers described herein in a sample from an individual having cancer can be used in methods of predicting the therapeutic efficacy of treatment with a VEGF antagonist (e.g., an anti-VEGF antibody, (e.g., bevacizumab) or a VEGFR inhibitor (e.g., a multi-targeted tyrosine kinase inhibitor (e.g., sunitinib, axitinib, pazopanib, or cabozantinib))) and a PD-L1 axis binding antagonist (e.g., a PD-L1 binding antagonist (e.g., anti-PD-L1 antibody, e.g., atezolizumab (MPDL3280A)) or a PD-1 binding antagonist (e.g., anti-PD-1 antibody)), or with an angiogenesis inhibitor (e.g., a VEGF antagonist (e.g., a VEGFR inhibitor, (e.g., a multi-targeted tyrosine kinase inhibitor (e.g., sunitinib, axitinib, pazopanib, or cabozantinib)))).