SUBSTITUTED PYRROLO [2,3-D] PYRIDAZIN-4-ONES AND PYRAZOLO [3,4-D] PYRIDAZIN-4-ONES AS PROTEINKINASE INHIBITORS

FIELD: pharmaceutical compounds.SUBSTANCE: invention relates to a compound of Formula (II) or a pharmaceutically acceptable salt thereof, which can find use as inhibitors of Bruton's tyrosine kinase (BTK). In Formula (II), ring Q1 is selected from aryl and heteroaryl, where aryl and heteroaryl...

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Hauptverfasser: YAN, Litszyun, SUN, Tszin, CHZHAN, Vejpen, LI, Chzhifu, TAN, Khaokhan, LYU, Bin, CHEN, Lin, LIN, Min, VAN, Syanlun, CHEN, Chzhifan, VAN, Vejbo, CHZHAO, Sindun, TAN, Zhuj, RAN, Kaj, TSZOU, Tszunyao
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: pharmaceutical compounds.SUBSTANCE: invention relates to a compound of Formula (II) or a pharmaceutically acceptable salt thereof, which can find use as inhibitors of Bruton's tyrosine kinase (BTK). In Formula (II), ring Q1 is selected from aryl and heteroaryl, where aryl and heteroaryl are each unsubstituted or substituted with at least one substituent independently selected from RX, where aryl is phenyl or naphthyl, where heteroaryl is a 5-6 membered aromatic, monocyclic ring containing from 1 to 2 heteroatoms selected from N, with the remaining ring atoms being carbon; ring Q2 is selected from heterocyclyl, where heterocyclyl is a single aliphatic ring with 4-6 ring atoms containing 1 to 2 heteroatoms selected from N; L is selected from -O-, -N(RA1)C(O)- and -C(O)N(RA1)-; W is -C(O)-; Y is selected from N and CR6; R1is hydrogen; each R2is hydrogen; R3is hydrogen; R5is selected from hydrogen and C1-10alkyl; R4is selected from hydrogen, C1-10alkyl, heterocyclyl or heterocyclyl-C1-4alkyl, where heterocyclyl is unsubstituted or substituted by at least one substituent independently selected from RX, where heterocyclyl is a single aliphatic ring with 4-5 ring atoms containing 1 heteroatom selected from N; or R3and R4, taken together, form a bond; R6is hydrogen; each RA1is hydrogen; each RXis independently selected from hydrogen, C1-10alkyl, halogen, CN and NO2; n is 0; p is 0. The invention also relates to a pharmaceutical composition for inhibiting the kinase activity of Bruton's tyrosine kinase (BTK), containing an effective amount of the said compound and at least one pharmaceutically acceptable carrier, and to a method of treating, ameliorating or preventing a condition that responds to BTK inhibition, comprising administering to a subject in need of such treatment, an effective amount of the said compound.EFFECT: invention can be used for treatment of an inflammatory and/or autoimmune condition.34 cl, 2 tbl, 117 ex(II) Изобретение относится к соединению формулы (II) или его фармацевтически приемлемой соли, которые могут найти применение в качестве ингибиторов тирозинкиназы Брутона (BTK). В формуле (II) кольцо Q1 выбрано из арила и гетероарила, где арил и гетероарил каждый является незамещенным или замещен по меньшей мере одним заместителем, независимо выбранными из RX, где арил представляет собой фенил или нафтил, где гетероарил представляет собой 5-6-членное ароматическое, моноциклическое кольцо, содержащее от 1 до 2 гетероатомов, выбранных из N,