GAMMA-AMINOBUTYRIC ACID (GABA) ANALOGUES FOR TREATMENT OF PAIN AND OTHER DISORDERS Russian patent published in 2019 - IPC C07D257/04 C07D261/12 A61K31/42 A61K31/41 A61P29/00 A61P25/28 A61P25/02 A61P25/08 A61P25/16 A61P9/10 A61P25/22 

Abstract RU 2679407 C1

FIELD: chemistry.

SUBSTANCE: invention relates to the novel compound of formula (1) and its enantiomer. Above compound has affinity binding properties for subunits α2δ of potentially dependent calcium channels and can be used in treatment of neuropathic pain, in particular headache and migraine, in treatment of diseases of the central nervous system and/or peripheral nervous system, for example, selected from epilepsy, ischemic cerebrovascular disease, stroke, cerebral neoplasms, Alzheimer's disease, Peak's disease, Huntington's disease, dementia, Parkinson's disease and others. In formula (1) Formula 1 R1 represents C1-4 alkyl group, R2 is or , and R3 is hydrogen or C1-4 alkyl group. Also, the invention relates to methods for producing the compound of formula 1 by reducing the compound of formula 12. Formula 12 Formula 2a. Above enantiomer of formula 2a can be obtained by separating a mixture of the enantiomers of formula 1. In the indicated compounds of the group, R1, R2, R3 have the above meaning. In addition, the invention relates to new intermediate compounds Formula 16 and Formula 14, where R1 has the above values, R2a represents -R2, -CN, -CONH2, -COOH, -(C=NH)NHOH.

EFFECT: proposed analogues of gamma-aminobutyric acid (gaba) for treatment of pain and other disorders.

19 cl, 1 tbl, 5 ex

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RU 2 679 407 C1

Authors

Megkhani Premzhi

Kritsek Frants

Dates

2019-02-08Published

2014-12-16Filed