Tyk Medicines Inc.

Tyk Medicines (Zhengzhou), Inc.

Yusheng Wu

Jun Li

Apeng Liang

Chengshan Niu

Yang Geng

Zhongwei Guo

Maolin Zheng

A kinase inhibitor compound of formula I or a pharmaceutically acceptable salt, solvate, or prodrug thereof. The compound has good inhibitory activity on EGFR and Her2 exon 20 insertion mutation, EGFR exon 19 deletion and L858R point mutation of exon 21.

Compounds used as kinase inhibitors and application thereof

Provided is the compound represented by formula I, or tautomer thereof, or meso thereof, racemate thereof, and mixture of meso and racemate thereof, or enantiomer thereof, diastereomer, and mixture of enantiomer and diastereomer, or pharmaceutically acceptable salt thereof, or deuterate thereof. The compound of formula I can be used as a kinase inhibitor, as a drug for the treatment of ROS1, NTRK, ALK, and other kinase-mediated diseases.

3-oxadiazolyl substituted pyrazolo[1,5,a]pyrimidines for ROS1, NTRK, and ALK mediated diseases

A crystal form of a deuterated AZD9291 has an X-ray powder diffraction measured using Cu-K&#x3b1; rays with diffraction peaks at 7.1&#xb1;0.2, 8.5&#xb1;0.2, 9.4&#xb1;0.2, 10.3&#xb1;0.2, 15.1&#xb1;0.2, 16.3&#xb1;0.2, 18.7&#xb1;0.2, 22.0&#xb1;0.2, 25.6&#xb1;0.2, and 26.0&#xb1;0.2. The crystal form of the deuterated AZD9291 is used in the preparation of medicaments for the treatment of cancer. The crystal form of the deuterated AZD9291 provided by the present invention has stable physical and chemical properties and good metabolic stability, and blood concentrations in vivo and concentrations in the brain thereof are significantly improved, achieving an improved therapeutic effect.

Crystal form of deuterated AZD9291, preparation method therefor, and use thereof

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Zhejiang, China

Yusheng Wu