Derivatives of benzofuro 3,2-d pyrimidines proteinquinasas Inhibitors, Pharmaceutical compositions containing same and Uses Thereof in the treatment of cancer.

摘要

Item 1: a compound according to formula (1),Or a pharmaceutically acceptable salt with the following characteristics: R1 is hydrogen or tar; R2 is from amino acid tar, amino acid kiokio kiokio kiokio kiokio kiokio kiokio kiokio kiokio kiokio Using 1-3 groups of selected halogens and - NH2, substituting isocyclic propylene, substituting noncyclic propylene, substituting noncyclic propylene, substituting amino group, substituting 1, 2 or 3-OH, substituting tar, substituting optional tar, substituting 1, 2 or 3-OH, substituting tar, substituting 1, 2 or 3-OH,Instead of 1,2 or 3-OH, alcoxicoquiloaminoqui, isocyclopropyl loamino, non cyclopropene can be replaced by tar at any cancellation position of 1,2 or 3-halogen Replace with 1-2 tar, ariloalquiloamino alternative in any cancellation position with diacquiloamino, halo, Alcoy, heterosexual or heterosexual, alternative with 1, 2 or 3-OH in arilo position.Use 1, 2 or 3 selected groups of halogen, isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl Ariloal quilo amino, cicloal quilo C4-7 alternatives are - NH2, NHC (o) - O - (CH3) 3, O - (CH3) amino quilo, - n (H) C (o) - o-asphalt, alkylpyridine, isocyano propyl dioxy, isopropylidene isopropylideneoxy, optional alternatives, 1, 2 or 3 selected amino alternatives at any cancellation location, SomeoneBitumen, halogen, o-isopropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropylpropyl Group 2 or 3 R5 is in any cancellation position, - NHC (o) R7, aminoalquiloamino, - cr11r12, selective isopropylidene propylene substitute is group 1, 2 or 3 R10, isopropylidene propylene, halogen replaced by 1, 2 or 3 tar in any cancellation position; arilo or ariloal quilo, isoacrylonitrile, isopropylidene glycol, isopropylidene glycol, isopropylidene propylene acrylonitrile propylene HeterosexualsThe optional ariloal quiloamino is replaced by isocyclopropylene or isocyclopropylene and isocyclopropylene; or R1 and R2 are combined with the added carbon atom to form a 5-person isocyclopropylene ring; R3a is selected from halogen, tar, NO2, alcoxi and optional tar. In this paper, the author analyzes the characteristics of,-OH, alkoxy, and halo; or R3a and R3d, together with the carbons to which they bind, bind to form a 5-membered heteroaryl optionally substituted by methyl or -NH2, or a 5-6-membered heterocycloalkyl; R4 is selected from -OH, amino, aminoalkyl, halo, alkyl optionally substituted by -OH, alkoxy, alkylaminoalkyl, heteroaryloalkyl, -C (O) OH, -C (O) -O-alkyl, -C (O) -alkyl , oxo, aryl optionally substituted by alkyl, arylalkyl or halo, heteroaryl, -OH, dialkyloamino, dialkyloaminoalkyl, alkylamino, spiro-heterocycloalkyl, -NHC (O) R8, -C (O) NHR9, arylalkyloaminocarbonyl optionally substituted by halo at any position aryl ringheterocycloalkylalkylamino dialkylaminoalkylcarbonyl, dialkylaminocarbonylalkyl, heterocycloalkylalkyl optionally substituted by -CF3, heterocycloalkyl optionally substituted by alkyl, arylalkyl optionally substituted by -CF3, alkoxyalkyl and heterocycloalkyl optionally substituted by; R5 is selected from alkyl, -OH, amino, aminoalkyl, -C (O) N (H) -heteroarylalkyl, halo, -NO2, -C (O) -N (H) -heterocycloalkylalkyl, alkylaminoalkyl, heteroaryl, cycloalkylaminoalkyl, alkylamino , dialkyloamino, -C (O) Oalkyl, -C (O) OH, heterocycloalkyl, -N (H) -alkylheterocycloalkylC (O) -O-alkyl,-O-asphalt-c (o) - n (H) - asphalt-c (o) - n (H) - asphalt-c (o) n (H) - asphalt-cyclopropyl-cyclopropyl-ordovician tar-o-isopropyl-isopropyl-ordovicianTar, - NHC (o) R6, alcoxicarbolinicoyclohexacloalquiloaminoqui, an alternative to isocycloacryloxyl, in the isocycloacrylonitrile part, alcoxio NiO, dialquiloaminoquiloamino, y alcoxi; R6 was selected as dialquiloaminoqui, heteromorphic, isocycloprene, isopropyl, Substitution substitution of non allyl allyl allyl allyl isopropyl, allyl allyl, allyl allyl, allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl allyl Alternative arilo replacement 1,2 or 3 halo, n (H) C (o) C H 3, tar or alcoxi; R7 is selected from heterogeneous epoxy compounds and replaced with 1, 2 or 3 halogens, diacycloheaminoqui, isocyclopropylamino, optional heteromorph in any ring position and 1, 2 or 3 selected halogenation and coordination groups, And alcoxie; R8 is selected from ariloalquilo, isopropyl propyl ester and aspha R9 is selected from alternative h, tar, ariloalquilo, and any ring position of ariloalquiloamino carbonio is replaced by halogen and diaquiloaminoqui aspha R10 is selected from asphalt, oxo, Heterosexualsdialquiloaminoalquilocarbonilo, dialquiloaminocarboniloalquilo, aminoalkyl, -OH, halo, heteroarilocarbonilo, dialkylaminoalkyl, heterocycloalkyl (piperidinyl) optionally substituted by alkyl, -C (O) -O-alkyl, ariloalquilocarbonilo, arylcarbonyl, alkylcarbonyl, alcoxialquilocarbonilo, heterocicloalquilocarbonilo, heteroarylalkyl, -O-heterocycloalkyl and aryloalkyl; R11 is selected from aryl optionally substituted by halo, heteroarylalkyl, cycloalkyl, spirocycloalkyl and arylalkyl optionally substituted by alkoxy or phenylmethylmethoxy; R12 is selected from -NH2 and heterocycloalkyl optionally substituted by alkyl;R13 is selected from ariloan quilo with the following characteristics: ariloan quilo's ariloan share can be replaced by 1, 2 or 3 alcoxi, halo, methyl, methoxi, - CF3, cycloquilo and isoariloan; R14 is selected from hydroxyl, h and TMS.