SALT FORM OF ISOQUINOLINONE TYPE COMPOUND AS ROCK INHIBITOR AND METHOD FOR ITS PREPARATION Russian patent published in 2024 - IPC C07D401/12 A61K31/551 A61P9/10 A61P9/12 A61P27/06 

Abstract RU 2821792 C1

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (II) and its crystalline form A, in which the X-ray powder diffraction pattern contains characteristic diffraction peaks at following angles 2θ: 3.30±0.20°, 6.33±0.20°, 6.55±0.20°, 10.62±0.20°, 12.57±0.20° and 13.11±0.20°, and crystalline form B, in which the X-ray powder diffraction pattern contains characteristic diffraction peaks at following angles 2θ: 12.12±0.20°, 16.48±0.20°, 16.95±0.20°, 17.94±0.20° and 21.87±0.20°. Invention also relates to a method of producing crystalline form B of a compound of formula (II), comprising (a) adding crystalline form A of the compound of formula (II) to a solvent to form a suspension; and (b) stirring suspension at 50 °C for 3 hours, filtering and drying, wherein the solvent is selected from a group consisting of isopropanol, tetrahydrofuran, acetonitrile, 2-butanone and ethyl acetate. According to the invention, the compound of formula (II) is used in preparing a drug for treating glaucoma or ocular hypertension.

EFFECT: invention discloses a salt form of an isoquinolinone type compound as an ROCK inhibitor and a method for preparing said compound.

17 cl, 7 dwg, 11 tbl, 9 ex

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RU 2 821 792 C1

Authors

Ge, Jian

Wang, Yandong

Liu, Yizhi

Wu, Lingyun

You, Xu

Xiao, Zheming

Chen, Shuhui

Dates

2024-06-26Published

2021-12-21Filed