COMPOUNDS Russian patent published in 2020 - IPC C07D401/14 C07D403/04 C07D403/14 C07D405/14 C07D413/14 C07D471/04 C07D487/04 C07D491/107 A61K31/4545 A61K31/496 A61K31/506 A61K31/519 A61K31/5377 A61P25/16 

Abstract RU 2725616 C2

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts thereof

,

where X is selected from CH or N; Y CR3, and R3 is methyl; R1 is selected from a group, consisting of 5- or 6-member heterocyclyl optionally substituted with one, two or three substitutes independently selected from a group consisting of C1-3 alkyl, optionally further substituted with one C1-3 alkoxy, C1-3 alkoxy, halogen, hydroxyl, -SO2CH3, -COCH3, oxo groups, and oxetanyl, -O-4-6-member heterocyclyl, optionally substituted with one or two substituents C1-3 alkyl, which may be identical or different, and C1-6 alkoxy; and R2 is

,

where Z1 and Z2 independently represent N or CR7, and where R7 is H or C1-3 alkoxy, but Z1 and Z2 can not both be CR7, Ra is selected from a group consisting of CN, C1-3 alkyl, C1-3 alkoxy, -OC1-3 haloalkyl, and C3-6 cycloalkyl; and Rb is selected from a group, consisting of 2-oxa-6-azaspiro[3.4]octanyl, C3-6 cycloalkyl optionally substituted with one hydroxyl, -CONHCH3, -NHCOCH3, 4–6-member heterocyclyl, optionally substituted with one or two substituents, independently selected from a group consisting of hydroxyl, CN, -CONHCH3, oxetanyl, C1-3 alkyl optionally substituted with one hydroxyl, and C1-3 alkoxy, optionally substituted with one hydroxyl, which inhibit LRRK2 kinase activity, methods for preparing them, compositions containing them, and their use in treating or preventing diseases, characterized by LRRK2 kinase activity, e.g. Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis (ALS).

EFFECT: compounds can be used in treating or preventing diseases characterized by LRRK2 kinase activity.

15 cl, 273 ex

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RU 2 725 616 C2

Authors

Ding Xiao

Jin Yun

Liu Qian

Ren Feng

Sang Yingxia

Stasi Luigi Piero

Wan Zehong

Wang Hailong

Xing Weiqiang

Zhan Yang

Zhao Baowei

Dates

2020-07-03Published

2016-07-22Filed