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Naphthyridines as inhibitors of hpk1
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A heteroaryl and heterocyclyl technology, applied in the field of compounds that regulate the function of HPK1, can solve the problems that surgical resection is not feasible and damages cells
Active Publication Date: 2020-01-10
F HOFFMANN LA ROCHE & CO AG
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Unfortunately, for many tumors or forms of cancer, surgical removal is not a viable option
In addition, radiation therapy and chemotherapy drugs do not target only diseased cells, thus ultimately damaging healthy cells
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[0798] At -78°C, N 2 , to a solution of 2,6-dichloro-3-iodo-pyridine (13.69 g, 50 mmol) in anhydrous THF (150 mL) was added LDA (2.0 M in THF, 27.5 mL, 55 mmol) dropwise. After the addition was complete, the reaction solution was stirred at -78°C for 2 hours. in CO 2 After bubbling for 5 minutes, the reaction mixture was stirred at room temperature for 2 hours. The reaction solution was quenched with concentrated HCl, and extracted with dichloromethane. The combined organic layers were in Na 2 SO 4 Drying on , filtered and concentrated gave 2,6-dichloro-4-iodo-pyridine-3-carboxylic acid (8.1 g, 51% yield) as a light yellow solid. LCMS(ESI)[M+H] + = 317.8.
[0826] To the vial add tert-butyl N-(6,8-dichloro-2,7-naphthyridine-3-yl)carbamate (1.05 g, 3.34 mmol), HCl / 1,4-dioxane (10 mL, 4N, 40 mmol) and dichloromethane (5 mL). The mixture was stirred at 40°C for 4 hours. The mixture was concentrated and dried in vacuo to give 6,8-dichloro-2,7-naphthyridine hydrochloride (823 mg, 96% yield) as a yellow solid. LCMS(ESI)[M+H] + = 214.1.
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Abstract
Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods ofinhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.
Description
[0001] Cross References to Related Applications [0002] This application claims priority to International Patent Application No. PCT / CN2017 / 078792, filed March 30, 2017, and International Patent Application No. PCT / CN2018 / 076909, filed February 15, 2018, the contents of which are incorporated by reference in their entirety Incorporated into this article. [0003] sequence listing [0004] This application contains a Sequence Listing, which has been filed electronically in ASCII format, and is hereby incorporated by reference in its entirety. Said ASCII copy, created on March 26, 2018, is named P34139_WO_2_SL.TXT and is 21KB in size. technical field [0005] The present invention relates to compounds that modulate the function of HPK1, which are useful in the treatment of diseases and conditions mediated by HPK1, such as cancer. Background technique [0006] The main treatments that oncologists use to treat cancer are surgical resection, radiation therapy, and classic che...
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