1-(4-ISOXAZOLE-5-YL)-1H-PYRAZOLE-1-YL)-2-METHYLPROPANE-2-OL DERIVATIVES AND RELATED COMPOUNDS AS IL-17 AND IFN-GAMMA INHIBITORS FOR TREATMENT OF AUTOIMMUNE DISEASES AND CHRONIC INFLAMMATION Russian patent published in 2022 - IPC C07D413/04 C07D413/14 C07D417/14 A61K31/422 A61K31/427 A61K31/5377 A61K31/541 A61P1/04 A61P5/14 A61P9/10 A61P17/06 A61P19/02 A61P37/06 

Abstract RU 2785342 C2

FIELD: pharmaceutical chemistry.

SUBSTANCE: group of inventions relates to pharmaceutical chemistry and includes a compound of the formula (I) and its use for the manufacture of a drug for the treatment of a disease or a medical condition, in which inhibition of interleukin-17 (hereinafter – IL-17) and/or interferon-γ (hereinafter – IFN-γ) is preferable. In the formula (I), Ar is selected from a group consisting of phenyl and pyridyl, each of which is optionally substituted with one, two, or three independently selected substitutes RAr; RAr is selected from a group consisting of halogen, -OH, -CN, C1-6-alkoxy, di-C1-6-alkylamino-C1-6-alkoxy, -CONHR’, benzyloxy, -CO-azetidinyl, -CO-pyrrolidinyl, -CO-morpholinyl, -CO-C3-6-cycloalkyl, -CONH-C3-6-cycloalkyl, and -O-C1-6-alkyl-heterocycle, where heterocycle is selected from a group consisting of pyrrolidinyl, piperazinyl, morpholinyl, 1,1-dioxothiomorpholinyl, and (2-oxa-6-azaspiro[3.3]hept-6-yl)-C1-4-alkoxy, and where each of the specified heterocycle groups is optionally substituted with C1-6-alkyl, and where R’ is C1-6-alkyl; Z is selected from a group consisting of H, -CO-RZ, -CH2-O-RZ, -CO-CH2-RZ, -CO-CH2-O-RZ, -COORZ, -CO-NHRZ, -C1-6-alkyl-O-C1-6-alkyl-O-RZ, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, 5- or 6-element heteroaryl including one or two heteroatoms independently selected from N, S, and O, and tetrahydrofuranyl, where each of the specified alkyl and heteroaryl groups is optionally substituted with C1-6-alkyl, OH, or C3-6-cycloalkyl; RZ is selected from a group consisting of H, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-6-cycloalkyl, and oxetanyl; Y is C1-4-halogenalkyl or C1-6-alkyl; R1 is such as specified in the claims.

EFFECT: compound of the formula (I), having inhibitory activity relatively to interleukin-17 (IL-17) and/or interferon-γ (IFN-γ).

11 cl, 1 tbl, 167 ex

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RU 2 785 342 C2

Authors

Felding, Yakob

Kolkhof, Khella

Greppel, Manfred

Myuler, Rolf Andreas

Fitt, Daniel

Shevrie, Karin

Zaya, Mirko

Tasler, Shtefan

Dates

2022-12-06Published

2018-09-06Filed