BICYCLIC COMPOUNDS FOR DIAGNOSTICS AND TREATMENT Russian patent published in 2022 - IPC C07D417/14 C07D495/04 C07D513/04 C07B59/00 A61K31/4365 A61K31/4439 A61K31/4427 A61K51/04 A61P25/16 A61P25/28 

Abstract RU 2766139 C2

FIELD: medicine.

SUBSTANCE: invention relates to a compound of the formula (IIa), its definably labeled derivatives, stereoisomers, racemic mixtures and pharmaceutically acceptable salts, a pharmaceutical composition based on them for the treatment, relief or prevention of a disorder or anomaly related to alpha-synuclein aggregates, a diagnostical composition based on them for use for visualizing alpha-synuclein aggregates, a method for data collection for the diagnostics or for the determination of predisposition to a disorder or anomaly related to alpha-synuclein aggregates, a method for data collection for tracking a residual disorder or predicting a reaction of a patient suffering from a disorder or anomaly related to alpha-synuclein aggregates, and to a method for the determination of a number of alpha-synuclein aggregates, where alpha-synuclein aggregates are Levi’s corpuscles and/or Levi’s neurites. In the general formula (IIa), is selected from a group consisting of , hydrogen and alkyl, where and alkyl can be attached in any available position, and where can be optionally substituted with one or more substituents RD; where is selected from where can be attached in any available position, and where can be optionally substituted with one or more substituents RE; in each case, RD is independently selected from a group consisting of halogen; in each case, RE is independently selected from a group consisting of heterocyclyl, where heterocyclyl can be optionally substituted with halogen.

EFFECT: development of new compounds of the formula (IIa) that can be used for the diagnostics, tracking of disease development or tracking of activity of drugs, group of disorders or anomalies related to alpha-synuclein aggregates, such as Parkinson’s disease, dementia with Levi’s corpuscles, Alzheimer’s disease, as well as for the treatment, relief or prevention of such disorders or anomalies.

(IIa)

18 cl, 10 tbl, 132 ex

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RU 2 766 139 C2

Authors

Molette, Jerome

Gabellieri, Emanuele

Darmency, Vincent

Dates

2022-02-08Published

2017-03-10Filed