TRK-INHIBITING COMPOUND Russian patent published in 2018 - IPC C07D401/12 C07D403/12 C07D401/14 C07D403/14 C07D471/04 C07D487/04 A61K31/444 A61K31/506 A61K31/519 A61K31/4439 A61P29/00 

Abstract RU 2667907 C9

FIELD: medicine.

SUBSTANCE: invention relates to a compound of general formula (I) wherein the Cy1 cycle is phenyl, cyclohexyl, pyridinyl, pyrazolyl, triazolyl, thienyl, tetrahydrofuranyl; Cy2 cycle is a pyridine ring, a pyrimidine ring, a pyrazolopyrimidine ring, an imidazopyridazine ring, an imidazopyridine ring, a pyrrolopyridine ring, an imidazopyrazine ring or a pyrazolopyridine ring; R1 represents a halogen; C1-6-alkyl group optionally substituted with 1 to 3 substituents selected from the group consisting of (i) halogen and (ii) hydroxy or C2-6-alkynyl group; phenyl optionally substituted with one or two R5 groups or indanyl; A 5-6 membered monocyclic heterocycle optionally substituted with one or two R5 groups or dihydrobenzofuran; -S(O)m1-R6; -SO2NR7R8; -OR14; R5 represents a halogen; cyano group; or C1-3-alkyl group optionally substituted with 1 to 3 substituents selected from the group consisting of (i) halogen, (ii) hydroxy groups and (iii) oxo groups; when there are two groups R5, the group R5 independently may be the same or different; R6, R7, R8, R14 or R20 respectively and independently represent (1) a hydrogen atom or (2) C1-6-alkyl group optionally substituted by (ii) a hydroxy group; R2 represents a halogen; C1-6-alkyl group optionally substituted with (i) a halogen or (ii) a hydroxy group; C3-6-cycloalkyl group; C1-6-alkoxy group; -NR28R29; pyrrolidinyl, azetidinyl; or -O-(oxetanyl); R28 and R29 respectively and independently represent a hydrogen atom or C1-6-alkyl group optionally substituted by (ii) a hydroxy group; A1 and A2 respectively and are independently =CR3- or =N-; A3, A4, A5 and A6 respectively and are independently =CR4-; R3 and R4 respectively and independently represent a hydrogen atom; m1 is an integer from 0 to 2; p is an integer from 0 to 4; q is an integer from 0 to 2; r represents 0; provided that when p, q and r are respectively an integer of 2 or more, group R1, R2 and R3 respectively, and independently may be the same or different, or a pharmaceutically acceptable salt thereof. Invention also relates to a pharmaceutical composition having an inhibitory activity against Trk based on a compound of formula (I).

(I).

EFFECT: technical result consists in that new compounds have been obtained that can be used in medicine for the treatment of pain or cancer.

18 cl, 8 tbl, 23 ex

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RU 2 667 907 C9

Authors

Takeuti Dzun

Itadani Satosi

Khasimura Kazuya

Ikura Masakhiro

Khigasino Masato

Yasukhiro Tetsuya

Nagaura Takesi

Dates

2018-09-25Published

2014-02-18Filed