2, 5, 6, 7-TETRAHYDRO-[1, 4]OXAZEPIN-3-YLAMINES OR 2, 3, 6, 7-TETRAHYDRO-[1, 4]OXAZEPIN-5-YLAMINES Russian patent published in 2015 - IPC C07D413/12 C07D417/12 A61K31/553 A61P25/28 

Abstract RU 2570796 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to formula

compounds, possessing properties of BACE1 (enzyme 1, cleaving β-site of protein-precursor of β-amyloid) and/or BACE2 inhibitors, and their pharmaceutically acceptable salts, as well as to based on them pharmaceutical composition, their application and method of therapeutic and/or preventive impact on such diseases as Alzheimer's disease, type 2 diabetes. In general formula (I) A represents O, and B represents -CR8R9-; or B represents O and A represents -CR8R9-; R1 is selected from hydrogen and C1-7-alkyl; R2 is selected from hydrogen and C1-7-alkyl; R3 is selected from hydrogen and halogen; R4 is selected from hydrogen and halogen; R5 represents C1-7-alkyl; or R3 and R5 together with C atom, which they are bound to, form cyclopropyl ring; R6a, R6b, R6c and R6d are selected from hydrogen and halogen; R7 represents -(CO)-R10 or R11, where R10 is selected from the group, consisting of 5-6-membered heteroaryl with 1-3 heteroatoms, selected from N, O and S, with said heteroaryl being non-substituted or substituted with one-two groups, selected from the group, consisting of C1-7-alkyl, halogen, halogen-C1-7-alkyl, C1-7-alkoxy, halogen-C1-7-alkoxy, cyano, -COO-CH2-CH3, halogen-C1-7-alkyl, C3-7-cycloalkyl, with said cycloalkyl being non-substituted or substituted with one-four groups, selected from C1-7-alkyl, halogen or halogen-C1-7-alkyl, and C1-7-alkoxy-C1-7-alkyl, R11 is selected from C1-7-alkyl and C3-7-cycloalkyl; R8 and R9 independently on each other are selected from hydrogen, C1-7-alkyl and phenyl.

EFFECT: obtaining medication for therapeutic and/or preventive impact on such diseases as Alzheimer's disease, type 2 diabetes.

25 cl, 7 tbl, 118 ex

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RU 2 570 796 C2

Authors

Behnner Dehvid

Guba Vol'Fgang

Khil'Pert Khans

Khumm Roland

Mauzer Kharal'D

Majveg Aleksander F.

Narkizan Rober

Pover Ehojn

Rodzhers-Ehvans Mark

Rombakh Did'E

Voltering Tomas

Vostl' Vol'Fgang

Dates

2015-12-10Published

2011-05-03Filed