COMPOUNDS 6,7-DIHYDRO-5H-PYRAZOLO[5,1-B][1,3]OXAZINE-2-CARBOXAMIDE Russian patent published in 2020 - IPC C07D498/04 A61K31/5365 A61P25/00 

Abstract RU 2719599 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula I or a pharmaceutically acceptable salt thereof, wherein R1 represents a substituent selected from the group consisting of phenyl, pyridyl, triazolopyridine, pyrazolopyridine and imidazopyridine, where phenyl and pyridyl substituted with one to three R5; each of R2 and R3 are independently selected from the group consisting of hydrogen, (C1-C6) alkyl and (C3-C8) cycloalkyl; or R2 and R3 together with the nitrogen atom to which they are attached, form azetidinyl, pyrrolidinyl or piperidinyl; R4, when present, in each case is halogen or (C1-C6) alkyl; R5 when present is in each case independently selected from a group consisting of halogen, cyano, optionally substituted (C1-C6) alkyl, optionally substituted (C1-C6) alkylthio and optionally substituted (C1-C6) alkoxy, where (C1-C6) alkyl, (C1-C6) alkylthio, (C1-C6) alkoxy optionally substituted with one to three halogen atoms; and a is an integer selected from 0, 1 or 2. Invention also relates to a pharmaceutical composition for inhibiting PDE4 isozymes containing these compounds, and a method of treating using said compounds.

EFFECT: technical result is obtaining novel compounds and pharmaceutical compositions based thereon, which can be used in medicine for treating diseases such as schizophrenia, depression, anxiety, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotrophic lateral sclerosis, chronic obstructive pulmonary disease, inflammation, stroke, asthma and allergic rhinitis.

30 cl, 9 tbl, 64 dwg

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RU 2 719 599 C2

Authors

Chappie Thomas Allen

Patel Nandini Chaturbhai

Verhoest Patrick Robert

Helal Christopher John

Sciabola Simone

Lachapelle Erik Alphie

Wager Travis T.

Hayward Matthew Merrill

Dates

2020-04-21Published

2017-02-15Filed