- pyrazolo pyrimidine Derivatives of pyrazolo - pirimidinona, pyrazolo - pyridine and pyrazolo - pyrazine FUSED, Pharmaceutical compositions containing them and their use in the preparation of drugs for the treatment of diseases mediated by the p38 kinase

摘要

Formula group compound (1),Used in the treatment of p38 moderate disorder in one subject ILO Convention No. 1: a compound consisting of formula group (1),or a pharmaceutically acceptable salt thereof, wherein: R1 is aryl, heteroaryl, aralkyl or cycloalkyl; R2 is aryl, heteroaryl, cycloalkyl, branched alkyl or heterocyclyl; R3 is hydrogen or alkyl; R4 is hydrogen, alkyl, hydroxy, amino, heteroalkyl, heterocyclyl, heterocyclylalkyl, hydroxycycloalkyl, cycloalkylalkyl, alkylsulfonyl, alkylsulfonamido, aryl, heteroaryl, aralkyl, heteroaralkyl, - (CHRa) rC (= O) -Rb, r (CH) = O) -Rb, - (CHRa) r-NH-C (= O) -Rb or -SO2-Rb, wherein Ra is hydrogen, alkyl or heteroalkyl; Rb is alkyl, hydroxy, amino, heteroalkyl, aryl, aralkyl, heteroaryl, or heterocyclyl; r is a number from 0 to 4; R5 is hydrogen,Tar, isopar, aralquilo, isopropyl, isopropyl, isopropyl, hydroxypropyl-c (= O) - rc-o-so2-rc, wherein RC is tar, isopar, arilo, aralquilo, isopropene or isopropene; X and y are nitro, or X and y are nitro, the other is CRD; Z is n or CRD, wherein RD is hydrogeno, hydrocarbon, hydroxy, ALKO, amino or amino, Halo tar, cyanogen, halogenation, ISO tar, C (= O) - re-so2-re, where re is hydrogen or tar; W is O, s (o) m, CH2 or NRF, where m is 0-2, RF is hydrogen, tar, ISO tar, ISO cyclohexane, hydrocyclohexane, - C (= O) - RG or so2-rg, where RG is tar, arilo, aralquilo, ISO propene, ISO propene, ISO propene or propene;Or R4 and RF, together with the atoms to which they are linked, can form a heterocyclic ring; a is O, CH2, s (o) n, C (= O),NRh o CH (ORb)N is a number from 0 to 2, RH is hydrogen or tar, or R1 and Rh can form an isomerization; K is 0 or 1; B is O, s (o) J, CH (ORI),This is life. This is life.J is 0, 1 or 2; R is hydrogen or tar, RJ is hydrogeno, tar, C (= O) - rk, o-so2rm, rk is tar, arilo or aralquilo; RM is tar.