PENTACYCLIC COMPOUND SALT AND CRYSTAL THEREOF Russian patent published in 2024 - IPC C07D495/22 A61K31/551 A61P25/28 A61P43/00 

Abstract RU 2820938 C2

FIELD: chemistry.

SUBSTANCE: invention relates to monohydrochloride 5,10-dimethyl-5,6,9,10,11,12-hexahydropyrido[4",3":4',5']thieno[2',3':4,5]pyrimido[1,2-a]thieno[3,2-f][1,4]diazepine-4,13-dione of formula (I), as well as type A, B, C, D, E, F crystals with diffraction peaks at diffraction angles (2θ ± 0.2°), given in the claim, in powder X-ray diffraction obtained using CuKα as an X-ray source. Invention relates to monohydrobromide 5,10-dimethyl-5,6,9,10,11,12-hexahydropyrido[4",3":4',5']thieno[2',3':4,5]pyrimido[1,2-a]thieno[3,2-f][1,4]diazepine-4,13-dione of formula (I), as well as its crystal with diffraction peaks at diffraction angles (2θ ± 0.2°), given in the claim, in powder X-ray diffraction obtained using CuKα as an X-ray source. Invention relates to crystal of 5,10-dimethyl-5,6,9,10,11,12-hexahydropyrido[4",3":4',5']thieno[2',3':4,5]pyrimido[1,2-a]thieno[3,2-f][1,4]diazepine-4,13-dione, represented by formula (I), with diffraction peaks at diffraction angles (2θ ± 0.2°) 9.0°, 11.1°, 14.5°, 18.1°, 20.0°, 21.9°, 23.6°, 24.4°, 24.9° and 28.5° in powder X-ray diffraction obtained using CuKα as an X-ray source. Invention also relates to a pharmaceutical composition having an activating effect on cholinergic neurons, containing a monohydrochloride salt or a monohydrobromide of a compound of formula (I) or a crystal of a compound of formula (I) as an active ingredient and pharmaceutically acceptable additives.

EFFECT: compound 5,10-dimethyl-5,6,9,10,11,12-hexahydropyrido[4",3":4',5']thieno[2',3':4,5]pyrimido[1],2-a]thieno[3,2-f][1,4]diazepine-4,13-dione in the form of its monohydrochloride or monohydrobromide salt, also in crystalline form, capable of activating cholinergic neurons and/or has neuroprotective action.

12 cl, 19 dwg, 3 tbl, 9 ex

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RU 2 820 938 C2

Authors

Yoshida Kenshi

Ohashi Yoshiaki

Hoshikawa Tamaki

Sato Nobuaki

Kushida Ikuo

Dates

2024-06-13Published

2020-03-03Filed