INHIBITION OF CYCLIC AMP-SENSITIVE ELEMENT-BINDING PROTEIN (CREB) Russian patent published in 2024 - IPC C07D471/04 A61K31/444 A61K31/4545 A61K31/4745 A61P35/00 

Abstract RU 2831142 C2

FIELD: chemistry.

SUBSTANCE: invention relates to an additive salt of hydrochloric acid (1R,3R)-3-((S)-2-((R)-(5-fluoro-2-methoxyphenyl)(hydroxy)methyl)-6-(methoxycarbonyl)-7-methyl-6,7,8,9-tetrahydro-3H-imidazo[4,5-f]quinolin-3-yl)cyclohexane-1-carboxylic acid of formula (II). Invention also relates to a solid form of an additive salt of hydrochloric acid of a compound of formula (II), characterized by a powder X-ray diffraction pattern containing the following peaks (angles 2 θ ± 0.2) when measuring using radiation Cu Kα: 7.27, 8.98, 10.60, 15.60 and 23.93. Solid form according to the invention is an anhydrate. Invention relates to a method of producing a hydrochloric acid addition salt of a compound of formula (II), comprising dissolving the compound in ethyl acetate to form a solution and adding hydrochloric acid to the solution; heating the solution to temperature of 50 °C and subsequent cooling of the solution to temperature of 20 °C to 25 °C.

EFFECT: additive salt of hydrochloric acid (1R,3R)-3-((S)-2-((R)-(5-fluoro-2-methoxyphenyl)(hydroxy)methyl)-6-(methoxycarbonyl)-7-methyl-6,7,8,9-tetrahydro-3H-imidazo[4,5-f]quinolin-3-yl)cyclohexane-1-carboxylic acid of formula (II) is used to inhibit bromodomain CBP and/or bromodomain p300.

11 cl, 10 dwg, 1 tbl, 4 ex

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RU 2 831 142 C2

Authors

Luke, George

Dates

2024-12-02Published

2020-03-13Filed