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...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: ACHAB Abdelgkhani Abe, DENG Jongki, KATTAR Solomon, MU Chanvej, CHZHOU Khua, GYUZI Timoti, KATTS Dzhejson D, LEN Syanshen, ENTONI Nevill Dzhon, CHZHAN Zhun, MAKGOVAN Meredet, ALTMAN Majkl D, FRADERA LINAS Fransesk Ksaver, FONG Kin Chiu, METOT Dzhon L, CHZHAN Sisin, KRISTOFER Mettyu P, GARSIYA Yudit
Format: Patent
Sprache:eng ; rus
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
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