PURINE INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA
FIELD: medicine; pharmaceuticals.SUBSTANCE: present invention relates to a novel compound of formula I, or a pharmaceutically acceptable salt or stereoisomer thereof, having properties of a PI3K-alpha inhibitor and relative selectivity for PI3K-delta. In formula II Ris selected from hydrogen, Calkyl...
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Zusammenfassung: | FIELD: medicine; pharmaceuticals.SUBSTANCE: present invention relates to a novel compound of formula I, or a pharmaceutically acceptable salt or stereoisomer thereof, having properties of a PI3K-alpha inhibitor and relative selectivity for PI3K-delta. In formula II Ris selected from hydrogen, Calkyl or Ccycloalkyl, where Ris optionally substituted with 0, 1 or 2 groups independently selected from hydrogen, fluorine and chlorine; Ris selected from cyclopropyl, isobutyl, 2-methylpropyl, methyl, ethyl, iodine, pyridazinyl, pyrimidinyl, pyrazinyl, pyridinyl, pyrrolidinyl, piperidinyl, ethoxycarbonyl, cyclohexyl, phenyl, quinazolinyl, isoquinolinyl, pyrazolyl, imidazolyl, indolyl, indazolyl, thiazolyl, pyrazolo[1,5-a]pyrimidinyl, 3,6-dihydro-2H-pyranyl, 1H-pyrrolo[2,3-b]pyridinyl, cyclobutyl, 1H-pyrazolo[3,4-b]pyridinyl, pyrrolo[2,3-b]pyridinyl, benzimidazolyl, morpholinyl, 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridinyl, 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazolyl, where Ris substituted with 0, 1 or 2 independently selected R; n is 0, 1, 2, or 3; A is Ccycloalkyl, mono- or bicyclic Cheterocycloalkyl, containing a nitrogen atom as a heteroatom, and Cspirocyclyl containing a nitrogen atom in the ring; L is selected from O, S, SOand -CH; K is selected from a bond, O, N((C)alkyl)and -C(O)N(R)-(CH); Ris H or Calkyl; m has the value 0; Ris independently selected from a fluorine atom, chlorine atom, methyl, ethyl, propyl, methoxy, pyrazolyl, thiazolyl, benzisoxazolyl, pyrazinyl, cyclopropyl, pyridinyl, cyclopropylmethyl, hydroxy, oxo, dimethylamino, morpholinyl, imidazolyl, pyrrolidinyl, piperidinyl, tert-butyl, trifluoromethyl, methoxymethyl, isoxybutylcarboxy, tert-butylcarboxy, phenylcarboxy, hydrogen, methylpropylcarboxy, ethoxycarbonyl and others indicated in the claims, where each Ris substituted with 0, 1, 2 or 3 substituents Rand each Ris independently selected from methyl, trifluoromethyl, methoxy, amino, dimethylamino, fluorine atom, cyano, oxo, piperazinyl, butenoyl, methylethyl, ethyl, t-butyl, 1,1,3,3-tetramethylbutyl(Calkyl), chlorine atom, cyclopropyl, difluoromethyl, hydroxymethyl, fluoromethyl, phenyl, tert-butoxycarbonyl, tert-butylcarboxy, ethylcarboxy, pyrazolyl, ethylcarbonyl, thiazolyl and furanyl; Ris substituted with 0, 1 or 2 substituents Rand each substituent Ris independently selected from methyl, hydroxy and fluorine atom.EFFECT: compounds can be used for the treatment of arthritis, asthma and obstructive airway diseases, autoimmune diseases or diso |
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