SOLID FORMS OF PLADIENOLIDE PYRIDINE COMPOUNDS AND METHODS FOR USE THEREOF Russian patent published in 2021 - IPC C07D405/06 A61K31/4427 A61P35/00 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to crystalline form 1 (2S,3S,6S,7R,10R,E)-7,10-dihydroxy-3,7-dimethyl-12-oxo-2-((R,2E,4E)-6-(pyridin-2-yl)hepta-2,4-dien-2-yl)oxacyclododec-4-en-6-yl 4-methylpiperazine-1-carboxylate ("compound 1"), having XRPD-diffractogram, in which there are at least three peaks selected from peaks at 5.9±0.2, 7.7±0.2, 12.8±0.2, 15.3±0.2, 18.2±0.2, 19.3±0.2, 21.2±0.2, 23.6±0.2 and 25.8±0.2 two-theta degree. Invention also relates to a pharmaceutical composition for treating cancer, which is positive for one or more mutations in the splicingosome gene or protein, based on said compound.

EFFECT: technical result is obtaining a novel crystalline form of (2S,3S,6S,7R,10R,E)-7,10-dihydroxy-3,7-dimethyl-12-oxo-2-((R,2E,4E)-6-(pyridin-2-yl)hepta-2,4-dien-2-yl)oxacyclododec-4-en-6-yl 4-methylpiperazine-1-carboxylate and a pharmaceutical composition based thereon, which can be used in medicine for cancer treatment, where cancer is selected from the following: myelodysplastic syndrome, chronic lymphocytic leukemia, acute lymphoblastic leukemia, chronic myelomonocytic leukemia, acute myeloid leukemia, colon cancer, pancreatic cancer, endometrial cancer, ovarian cancer, breast cancer, uveal melanoma, stomach cancer, cholangiocarcinoma and lung cancer.

23 cl, 5 tbl, 7 dwg