2-ARYL-SUBSTITUTED N-ARYLIMIDAZOLINES, SELECTIVE CYCLOOXYGENASE-2 INHIBITORS, METHODS FOR PRODUCTION AND USE THEREOF Russian patent published in 2015 - IPC C07D233/20 C07D233/24 A61K31/4164 A61P29/00 A61P17/02 A61P19/00 A61P19/02 

Abstract RU 2565667 C1

FIELD: chemistry.

SUBSTANCE: compounds have selective cyclooxygenase-2 inhibitor properties and can be used to treat inflammatory diseases. The diseases can be selected from: articular syndrome with rheumatism and acute gout, rheumatoid arthritis, psoriatic arthritis, osteoarthrosis, radiculitis, in inflammatory processes of ligaments, tendons, ischias, lumbago, menstrual pain or inflammation, associated with inflammations caused by sunburn, skin damage by ultraviolet light, different forms of cancerous diseases of the skin. In formula 1 R is C1-C3 alkyl or an amino group, R' is hydrogen or C1-C3 alkyl, Ar is optionally substituted with a halogen, C1-C3 alkyl, C1-C3 alkoxy group or CF3 aryl; or a 5- or 6-member hetaryl containing one nitrogen, oxygen or sulphur atom in the ring. The invention also relates to a method of producing said compounds. The method includes reaction of a compound of general formula 3 with a substituted ethylenediamine of general formula 4, followed by reaction of the compound of general formula 5: with a compound of general formula 6 to form a compound 1.1, or with a compound of general formula 7 to form a compound 1.2 through an intermediate step of removing the protective group in the compound of general formula 8 according to the scheme where R and R' assume values given above.

EFFECT: high efficiency of using the compounds.

13 cl, 2 tbl, 1 dwg, 40 ex

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RU 2 565 667 C1

Authors

Dorogov Mikhail Vladimirovich

Krasavin Mikhail Jur'Evich

Dates

2015-10-20Published

2014-10-28Filed