TREATMENT OF NEUROLOGICAL DISORDERS Russian patent published in 2022 - IPC C07D403/14 C07D498/08 C07D491/153 C07D417/14 C07D413/14 A61K31/5377 A61K31/5386 A61K31/541 A61P25/08 A61P25/28 

Abstract RU 2765868 C2

FIELD: medicine.

SUBSTANCE: present invention relates to an application of a compound by the formula (I)

wherein X1, X2, and X3 independently represent N or CH, provided that at least two from X1, X2, and X3 represent N; Y represents N or CH; R1 and R2 independently represent (i) morpholinyl by the formula (II)

wherein the arrow indicates the bond in the formula (I); and wherein R3 and R4 independently represent H, a C1-C3alkyl, optionally substituted with one or two OH, C1fluoroalkyl, a C1-C2alkoxy, a C1-C2alcoxyC1-C3alkyl or CN; or R3 and R4 together form a divalent residue of -R5R6-, selected from a C1-C3alkylene optionally substituted with 1-2 F, -CH2-O-CH2-, -CH2-NH-CH2-, or any of the structures:

wherein the arrows indicate bonds in the formula (II); or (ii) a saturated 6-membered heterocyclic ring Z, selected from thiomorpholinyl, and piperazinyl, optionally substituted with 1-3 R7, wherein R7 in each case independently represents a C1-C3alkyl optionally substituted with one or two HE, a C1-C2fluoroalkyl, a C1-C2alcoxyC1-C3alkyl, a C3-C6cycloalkyl; or the two substituents of R7 together form a divalent residue of -R8R9-, selected from a C1-C3alkylene optionally substituted with 1-4 F, -CH2-O-CH2- or -O-CH2CH2-O-; provided that at least one from R1 and R2 represents morpholinyl by the formula II, or a prodrug, solvate, or a pharmaceutically acceptable salt of said compound, for preventing or treating a neurological disorder in a subject, wherein the neurological disorder is selected from epilepsy and a neurodegenerative disease. Also proposed is a method for preventing or treating a neurological disorder in a subject, wherein the neurological disorder is selected from epilepsy and a neurodegenerative disease.

EFFECT: compound by the formula (I) is an inhibitor of protein kinase mTOR and can be applied for preventing or treating a neurological disorder.

30 cl, 29 dwg, 15 tbl, 14 ex

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RU 2 765 868 C2

Authors

Razho, Denis

Khebajzen, Paul

Bofil, Floran

Fabbro, Doriano

Khillman-Vyullner, Petra

Ngujen, Khoa Khu Fuk

Lesher, Volfgang

Brandt, Klaudiya

Zele, Aleksandr Markus

Dates

2022-02-04Published

2017-05-17Filed