ETHYNYL DERIVATIVES Russian patent published in 2020 - IPC C07D471/04 A61K31/519 A61P25/16 

Abstract RU 2722014 C2

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula I applicable in medicine and pharmaceutical compositions based thereon:

I,

where R1 is hydrogen, F or Cl; L is a bond or lower alkylene; R2 represents -(CH2)nO-lower alkyl, lower alkyl substituted by halogen, -(CH2)nC(O)O-lower alkyl, phenyl, substituted with lower alkyl or halogen, or represents 5- or 6-member heteroaryl group selected from pyridinyl, pyrimidinyl, pyridazinyl, thiazolyl, imidazolyl, pyrazolyl or triazolyl, which are optionally substituted with lower alkyl, halogen, lower alkoxy, =O, benzyloxy, cycloalkyloxy, hydroxy, cyano, lower alkyl, substituted halogen, or -(CH2)nO-lower alkyl; is 1, 2 or 3; R3 represents hydrogen, lower alkyl or -(CH2)nO-lower alkyl; R4 is phenyl, optionally substituted with F; Y is CF or CCl; or a pharmaceutically acceptable salt thereof, or an acid addition salt, a racemic mixture or a corresponding enantiomer.

EFFECT: disclosed is a novel compound and a pharmaceutical composition based thereon, effective for treating Parkinson's disease, anxiety, emesis, obsessive-compulsive disorder, autism, cancer, depression, type 2 diabetes associated with metabotropic receptor glutamate 4 activity disorder, and for neuroprotection.

11 cl, 1 tbl, 112 ex

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RU 2 722 014 C2

Authors

Eshke, Georg

O Khara, Fionn

Plansher, Zhan-Mark

Richchi, Antonio

Ryukher, Daniel

Viejra, Erik

Dates

2020-05-26Published

2016-08-02Filed