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(19)

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2 692 102

(13)

(51)

IPC

C07D417/14(2006-01-01)

C07D417/04(2006-01-01)

A61K31/444(2006-01-01)

A61K31/505(2006-01-01)

A61K31/541(2006-01-01)

A61P25/28(2006-01-01)

(21) (22)

Application

2017107495, 2015-08-12

(24)

Start date

2015-08-12

(22)

Actual filing date

2015-08-12

(45)

Published

2019-06-21

(72)

Inventor

Anzelm LilliBartels BernDolente KozimoGuba VolfgangKhaap VolfgangPeters Jens-UveVoltering TomasObst Zander UlrikeRodzhers-Evans Mark

(73)

Holder

F. Hoffmann-La Roche Ag

2,2,2-TRIFLUOROETHYL-THIADIAZINES Russian patent published in 2019 - IPC C07D417/14 C07D417/04 A61K31/444 A61K31/505 A61K31/541 A61P25/28

Abstract RU 2692102 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula Ia', where R¹ is pyridyl or pyrazinyl substituted with 1–2 substitutes, individually selected from cyano, methyl, methoxy, fluoromethoxy, trifluoroethoxy, but-2-inoxy and prop-2-inoxy; R² is 2,2,2-trifluoroethyl or methyl; R³ is methyl; R⁴ is methyl or -CH₂CF₃; k or a pharmaceutically acceptable salt thereof, as well as to an intermediate compound of formula I'. Also described is a pharmaceutical composition which inhibits BACE1 based on the compound of formula Ia'.

EFFECT: technical result is obtaining novel compounds and pharmaceutical compositions based thereon, which can be used in medicine for therapeutic and/or preventive treatment of Alzheimer's disease.

10 cl, 8 tbl, 18 ex

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RU 2 692 102 C2

Authors

Anzelm Lilli

Bartels Bern

Dolente Kozimo

Guba Volfgang

Khaap Volfgang

Peters Jens-Uve

Voltering Tomas

Obst Zander Ulrike

Rodzhers-Evans Mark

Dates

2019-06-21—Published

2015-08-12—Filed