AMINOPYRIMIDINE DERIVATIVES AS LEUCINE-RICH REPEAT KINASE 2 (LRRK2) MODULATORS Russian patent published in 2018 - IPC C07D401/12 C07D413/12 C07D405/12 C07D403/12 C07D405/14 C07D413/14 C07D403/14 A61K31/506 A61K31/5377 A61K31/553 A61K31/538 A61P25/16 

Abstract RU 2651544 C2

FIELD: chemistry.

SUBSTANCE: in the general formula I I, A is a five-, six- or seven-membered saturated or unsaturated ring, that includes one or two heteroatoms selected from O and N, which is substituted once with R5 and which is optionally substituted one, two or three times with R6 groups; X is -NRa-, wherein Ra is hydrogen; R1 is C1-6alkyl; R2 is halogen, C1-6alkoxy, cyano or halo-C1-6alkyl; one of the groups R3 and R4 is halogen, C1-6alkyl or C1-6alkoxy, and the other group is hydrogen; R5 is oxo, C1-6alkyl, C3-6cycloalkyl or -C (O) -NRbRc, where each of the Rb and Rc is independently hydrogen or C1-6alkyl, or Rb and Rc together with atoms, to which they are attached, can form a 4-6-membered saturated heterocyclyl, which optionally comprises an additional heteroatom selected from O and N, and which is optionally substituted once with R6; or Rb and Rc together with the atoms to which they are attached, can form 2-oxa-5-azabicyclo [2.2.1] heptanyl; and each group R6 is independently C1-6alkyl, C3-6cycloalkyl, halogen, hydroxy-C1-6alkyl, C1-6alkoxy-C1-6alkyl or 4-6-membered saturated heterocyclyl with oxygen as a heteroatom. Preferable compound is a compound corresponding the formula IIa or IIb

where m is 0; 1 or 2; Z is -C (R7)2-; -NR8- or -O-; each group R7 is independently hydrogen or C1-6alkyl; and each group R8 is independently hydrogen, C1-6alkyl, C3-6cycloalkyl, halogen, hydroxy-C1-6alkyl, C1-6alkoxy-C1-6alkyl or 4-6-membered saturated heterocyclyl with oxygen as a heteroatom.

EFFECT: invention relates to a novel compound of formula I or a pharmaceutically acceptable salt thereof, which possess the properties of the LRRK2 inhibitor and can be used to prevent or treat Parkinson's disease.

22 cl, 3 tbl, 13 ex

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RU 2 651 544 C2

Authors

Bejker-Glenn Charlz

Chembers Mark

Chan Brajan K.

Estrada Entoni

Svini Zakari Kevin

Dates

2018-04-20Published

2012-11-28Filed