COMPOUND HAVING THROMBOCYTE AGGREGATION INHIBITION ACTION, AND A SALT THEREOF, AND A COMPOSITION COMPRISING SUCH COMPOUNDS FOR PREVENTING OR TREATING THROMBOTIC DISEASES Russian patent published in 2020 - IPC C07C235/46 C07C235/48 C07C235/56 C07D209/18 C07D213/56 C07D213/66 C07D213/81 C07D231/40 C07D261/20 C07D295/73 C07D295/192 C07D309/38 C07D333/24 C07D333/36 C07D413/04 C07D495/04 A61K31/423 A61K31/4365 A61K31/5375 A61P7/02 

Abstract RU 2739915 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound represented by formulas (I) or (II), or a pharmaceutically acceptable salt or stereoisomer thereof, which have property of thrombocyte aggregation inhibition. In formulas (I) and (II), R1 is hydroxy or C1-C10-alkoxy, X is N or O, R2 is -(CH2)p-(5–12-member heterocycle)-(CH2)p-C6-C12-aryl, 5–12-member heterocycle, -(CH2)p-NHC(=O)-C6-C12-aryl, -CHR4R5, 5–12-member heteroaryl, C6-C12-aryl, -C6-C12-aryl-O-(5–12-member heteroaryl) or -(CH2)p-(5–12-member heteroaryl), wherein p is integer from 1 to 10, R4 and R5 represent, each independently, C1-C6-alkoxycarbonyl or -CH2-(5–12-member heteroaryl), said heterocycle and heteroaryl can contain from 1 to 3 heteroatoms selected from N, O and S, said aryl is substituted with 1–4 substitutes selected from a group consisting of nitro, nitrile and hydroxy-C1-C6-alkyl, said heterocycle is substituted with 1–4 substitutes selected from a group consisting of halogen and oxo, said heteroaryl is substituted with 1–4 substitutes selected from a group, consisting of oxo, aminocarbonyl, C1-C6-alkyl, C1-C6-alkylaminocarbonyl, hydroxy and hydroxy-C1-C6-alkyl, provided that when R2 is -(CH2)p-(5–12-member heteroaryl), heteroaryl is not pyrazine, indole or pyridine, and when R2 is 5–12-membered heteroaryl, the heteroaryl is not benzothiazole, R3 represents hydrogen, when X is O, R3 does not exist when X is N, X, taken together with R2 and R3, can form 6-member heterocycle containing 1–3 heteroatoms selected from N, wherein said heterocycle can be substituted with C6-C12-aryl or -O-CHR6R7, where R6 and R7 are each independently C6-C12-aryl or 6–10-member heteroaryl containing 1–3 heteroatoms, selected from O, N and S, which are both unsubstituted or substituted with halogen. Invention also relates to specific compounds and a pharmaceutical composition for preventing or treating thrombotic diseases containing said compounds.

EFFECT: disclosed is a compound having thrombocyte aggregation inhibition action, and a salt thereof, and a composition comprising such compounds for preventing or treating thrombotic diseases.

4 cl, 16 tbl, 35 ex

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RU 2 739 915 C2

Authors

Ryu, Jei Man

Lee, Dong Won

Lee, Kang Hyeok

Park, Jin Hun

Cho, Geum Sil

Lee, Ki Sung

Chung, Jin Ho

Park, Woo Ile

Lee, Jae Young

Dates

2020-12-29Published

2016-09-02Filed