OXAZOLIDINE-BASED COMPOUND AND ANDROGEN RECEPTOR SELECTIVE AGONIST

FIELD: chemistry.SUBSTANCE: invention relates to a compound of the following chemical formula 1, an enantiomer, a diastereomer or a pharmaceutically acceptable salt thereof, where Ris a substitute of the following chemical formula 2 or chemical formula 3; Ris hydrogen, oxo or C-Calkyl; Rand Reach in...

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Hauptverfasser: SUN Dzhi Khen, SON Ben Khva, KAN Ken Gu, CHOJ Sol Min, KIM Khen Dzhun, CHOJ Sun Pil, KIM Yndzhin, KIM Dzhu Mi, LI Dzhi Khe, DZHAN Ben Dzhun, KIM Soon-Khoe
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: chemistry.SUBSTANCE: invention relates to a compound of the following chemical formula 1, an enantiomer, a diastereomer or a pharmaceutically acceptable salt thereof, where Ris a substitute of the following chemical formula 2 or chemical formula 3; Ris hydrogen, oxo or C-Calkyl; Rand Reach independently represents a substitute selected from a group consisting of hydrogen and C-Calkyl; Rand Reach independently represents a substitute selected from the group consisting of hydrogen, halogen and C-Calkyl; Ris cyano or nitro, and when Ris cyano and Ris H, then Ris X(CH)Rprovided that if n is 0 and X is O, then Rdoes not represent H; C-Calkyl as Rvalue and Rcontains one or more substitutes selected from a group consisting of hydrogen, hydroxy and halogen; chemical formula 2 is -X(CH)R, where X is O, N(H), S or S(O), Ris hydrogen, piperidine, phenyl or pyridine, which can be substituted (substitutes are given in the claim), n is 0 or 1; chemical formula 3 represents structure (a), where Y is CH or N, m is integer 0, 1 or 2, Rrepresents a substitute selected from a group consisting of hydrogen, oxo, C-Calkyl, cyano, C(O)R, C(O)OR, C(O)NRR, S(O)R, NHC(O)R, NRRand NHC(O)OR, Rand Rare given in the claim, and C-Calkyl contains one or more substitutes selected from a group consisting of hydrogen, hydroxy, halogen and cyano. Invention also relates to specific compounds: oxime (E)-4-(((2R,5S)-3-(3-methyl-4-nitrophenyl)-2-(trifluoromethyl)oxazolidin-5-yl)methoxy)benzaldehyde, 2-chloro-4-((2R,5S)-5-((4-((E)-(hydroxyimino)methyl)phenoxy)methyl)-2-(trifluoromethyl)oxazolidin-3-yl)benzonitrile, 2-chloro-4-((2R,5S)-5-((4-((E)-(hydroxyimino)methyl)phenoxy)methyl)-2-(trifluoromethyl)oxazolidin-3-yl)-3-methylbenzonitrile, 4-((2R,5S)-5-((4-((E)-(methoxyimino)methyl)phenoxy)methyl)-2-(trifluoromethyl)oxazolidin-3-yl)-2-(trifluoromethyl)benzonitrile, 4-((2R,5S)-5-((4-((E)-(hydroxyimino)methyl)phenoxy)methyl)-2-(trifluoromethyl)oxazolidin-3-yl)-2-(trifluoromethyl)benzonitrile, oxime(E)-4-(((2R,5S)-3-(4-nitro-3-(trifluoromethyl)phenyl)-2-(trifluoromethyl)oxazolidin-5-yl)methoxy)benzaldehyde, 4-((2R,5S)-5-((4-((E)-(hydroxyimino)methyl)-2-nitrophenoxy)methyl)-2-(trifluoromethyl)oxazolidin-3-yl)-2-(trifluoromethyl)benzonitrile, (2R,5S)-5-(1-acetylpiperidin-4-yl)-3-(4-cyano-3-(trifluoromethyl)phenyl)-2-(trifluoromethyl)oxazolidine-5-carboxamide or 4-((2R,5S)-5-(1-hydroxy-2-phenylethyl)-2-(trifluoromethyl)oxazolidin-3-yl)-2-(trifluoromethyl)benzonitrile. Invention relates to methods