DIAZABENZOFLUORANTHRENE COMPOUNDS Russian patent published in 2019 - IPC C07D461/00 C07D519/00 A61K31/4745 A61P9/10 A61P25/08 

Abstract RU 2697513 C2

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula (I), to its pharmaceutically acceptable salts or tautomers, where R1 is independently selected from H or optionally substituted R01 S(=O)2NH2; R3 is independently selected from C1-10alkyl; R2 selected from , , , , , , , , , , or ; where from zero to two T21-23 are N, and the rest are C(Rt); D21 is selected from -C(Rd1)(Rd2)-, -N(Rd4)-, -O-, -S- or -C(=O)-; T24 is selected from N or C(Rt); each of D22-24 is independently selected from -C(Rd1)(Rd2)-, -O-, -S- or -C(=O)-; up to two T25-29 are N, and the rest are C (Rt); optionally any two of Rt and Rd1-d4 are bonded together with common atom or group of atoms to form one 5-6-member ring; each of Rt, Rd1 and Rd2 is independently selected from H, CN, NH2, C(=O)NH2, C(=O)N(CH3)2; or Rt is independently selected from a group consisting of optionally substituted R01 C1-10alkyl, C1-10heteroalkyl, tetrahydropyranyl, tetrahydropyridinyl, morpholinyl, pyridinyl, , , , CF3, CH2CF3, CH2CHF2 or phenyl; R01 is selected from OH or R02; R02 is selected from C1-10alkyl, C1-10heteroalkyl, C3-10cycloalkyl, heterocyclic C6alkyl, which contains carbon atoms and 1 heteroatom, selected from O; wherein "hetero-" denotes a heteroatom or heteroatom-containing group selected from a group consisting of -C(=O)N(Rd3)- or -C(=O)O-; each of Rd3-d4 is independently selected from H or CH3; R02 optionally substituted with R001; R001 is selected from F, Cl, Br, I, OH or methyl, wherein the number of each of R01, R001, heteroatoms or heteroatom-containing groups independently is selected from 0, 1, 2, 3 or 4.

EFFECT: obtaining novel compounds which can be used in medicine in preparing a medicinal preparation for treating apoplexy of brain or epilepsy by inhibiting PDE1 activity.

10 cl, 2 tbl, 84 ex

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Authors

Yuan Shujie

Yang Xinchun

Zhao Jinlong

Zhang Daoxu

Sun Mingda

Liu Jiaji

Wei Tao

Zhao Huanan

Luo Yunfu

Yang Chundao

Dates

2019-08-15Published

2016-02-02Filed