PURINE INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA
FIELD: chemistry.SUBSTANCE: in the general formula IRare selected from methyl, ethyl, propyl, cyclopropyl, cyclopropylmethyl, difluoroethyl and 2,2,2-trifluoroethyl; Ris selected from hydrogen, Calkyl, Calkyloxy, CalkylaminoCalkyl, Ccycloalkyl, saturated 4-6-membered heterocycloalkyl containing 1-2...
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Hauptverfasser: | , , , , , , , , , , , , , , , , , , , , , |
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Format: | Patent |
Sprache: | eng ; rus |
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Zusammenfassung: | FIELD: chemistry.SUBSTANCE: in the general formula IRare selected from methyl, ethyl, propyl, cyclopropyl, cyclopropylmethyl, difluoroethyl and 2,2,2-trifluoroethyl; Ris selected from hydrogen, Calkyl, Calkyloxy, CalkylaminoCalkyl, Ccycloalkyl, saturated 4-6-membered heterocycloalkyl containing 1-2 heteroatoms selected from nitrogen, oxygen or nitrogen and oxygen, phenyl and mono- or bicyclic Cheteroaryl containing in the ring 1 to 2 nitrogen atoms or a nitrogen atom and a sulphur atom, where Ris substituted with 0, 1, 2 or 3 Rsubstitutes; n is 1, 2, 3; A is selected from pyrrolidinyl, piperidinyl, azetidinyl, azaspiro[2.4]hept-7-yl and azepanyl; L is selected from NH and N(Calkyl); K is selected from a chemical bond, C(O), CH, -C(O)N(R)-(CH)- and Calkynylene; Ris H or Calkyl, m is 0, 1, 2, or 3; Rare independently selected from: halogen, Calkyl, Calkenyl, Calkyl(oxy), Calkyl(oxy)(carbonyl), Calkyl(carbonyl), phenyl(oxy), phenyl(oxy)(carbonyl), phenylCalkyl(oxy)(carbonyl), phenylCalkyl(carbonyl), Ccycloalkyl(carbonyl), CcycloalkylCalkyl, Cbicycloalkyl(carbonyl), Cspirocycloalkyl(carbonyl), 5-10 membered mono- or bicyclic heteroaryl containing 1 to 3 heteroatoms in a ring selected from nitrogen or nitrogen and sulphur, 5-10 membered mono- or bicyclic heteroaryl(carbonyl), wherein the heteroaryl contains 1 to 3 ring heteroatoms selected from nitrogen or nitrogen and / or sulphur, (C)heterocycloalkyl containing 1-2 heteroatoms selected from nitrogen and oxygen, (C)heterocycloalkyl (carbonyl), wherein heterocycloalkyl contains 1-2 heteroatoms selected from nitrogen and oxygen, Calkylamino(carbonyl), Ccycloalkylamino(carbonyl), -C(O)(Calkyl), -(Calkyl)COH, oxo(=O); CalkylS(O), amino, (Calkyl)amino, Cacylamino, hydroxyl, (Calkyl)OH, cyano; where Reach is substituted with 0, 1, 2 Rsubstitutes, and each Rare independently selected from halogen, Calkyl, Calkyl(oxy), phenyl, 5-6 membered heteroaryl containing an oxygen or nitrogen ring atom, (C) of heterocycloalkyl containing a nitrogen, oxygen or sulphur atom, or S(O)group in the ring, (C) heterocycloalkyl (carbonyl), wherein the heterocycloalkyl contains a nitrogen, oxygen or sulphur atom, or S(O)group in the ring, oxo(=O), amino, (Calkyl)amino, (Calkyl)OH, Calkoxy, cyano and Chaloalkyl. Invention also includes specific compounds as defined in claim 2.EFFECT: invention relates to a novel compound of formula I or a pharmaceutically acceptable salt or stereoisomer thereof, which have the properties of a PI3K-alpha i |
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