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    3-(PHENYLSULFONYL)-[1,2,3]TRIAZOLO[1,5A]QUINAZOLIN-5(4H)-ONE DERIVATIVES
    10.
    发明申请
    3-(PHENYLSULFONYL)-[1,2,3]TRIAZOLO[1,5A]QUINAZOLIN-5(4H)-ONE DERIVATIVES 审中-公开

    公开(公告)号：WO2020109350A1

    公开(公告)日：2020-06-04

    申请号：PCT/EP2019/082663

    申请日：2019-11-27

    申请人： BIOVERSYS AG

    发明人： BOUROTTE, Marilyne ,  PIEREN, Michel ,  LOCIURO, Sergio ,  GITZINGER, Marc ,  KEMMER, Christian ,  SCHELLHORN, Birgit ,  SCHILL, Julian ,  SCHNEIDER, Peter

    IPC分类号： C07D487/02 ,  C07D487/04 ,  A61P31/04 ,  A61K31/40

    摘要： The present invention relates to a compound according to formula (I), wherein R1 and R5 are independently selected from H, halogen, hydroxyl, NO 2 , CN, C 1 -C 6 -alkyl optionally substituted by one or more R11, C 1 -C 6 -alkoxy optionally substituted by one or more R11, C 3 -C 6 -cycloalkyl optionally substituted by one or more R11, -C n -alkyl-N(R12)(R13) with n=0-3, -C n -alkyl-C(O)N(R12)(R13) with n=0-3, -SO 2 -N(R14)-C(O)-R15; -C n -alkyl-N(R14)-C(O)-R15 with n=0-3, -C n -alkyl-C(O)-OR16 with n=0-3, -O(C 1 -C 3 -alkyl-O) m -C 1 -C 3 -alkyl-OR10 with m=0-3, -C n -alkyl-OR16 with n=0-3, -NH-C n -alkyl-R18 with n=0-3; -O-C n -alkyl-R18 with n=0-3; -OPO(OR10) 2 , -PO(OR10) 2 , and a heterocycle optionally substituted by one or more R17; R3 is selected from halogen, hydroxyl, NO 2 , CN, C 1 -C 6 -alkyl optionally substituted by one or more R11, C 1 -C 6 -alkoxy optionally substituted by one or more R11, C 3 -C 6 -cycloalkyl optionally substituted by one or more R11, -C n -alkyl-N(R12)(R13) with n=0-3, -C n -alkyl-C(O)N(R12)(R13) with n=0-3, -SO 2 -N(R14)-C(O)-R15; -C n -alkyl-N(R14)-C(O)-R15 with n=0-3, -C n -alkyl-C(O)-OR16 with n=0-3, -O(C 1 -C 3 -alkyl-O) m -C 1 -C 3 -alkyl-OR10 with m=0-3, -C n -alkyl-OR16 with n=0-3, -NH-C n -alkyl-R18 with n=0-3; -O-C n -alkyl-R18 with n=0-3; -OPO(OR10) 2 , -PO(OR10) 2 , and a heterocycle optionally substituted by one or more R17; R2 and R4 are independently selected from H, halogen, C 1 -C 6 -alkyl optionally substituted by one or more R11; R6, R7, R8 and R9 are independently selected from H, halogen, hydroxyl, NO 2 , CN, C 1 -C 6 -alkyl optionally substituted by one or more R11, C 1 -C6-alkoxy optionally substituted by one or more R11, C 3 -C 6 -cycloalkyl optionally substituted by one or more R11, -C n -alkyl-N(R12)(R13) with n=0-3, -C n -alkyl-C(O)N(R12)(R13) with n=0-3, -SO 2 -N(R12)(R13), -SO 2 -N(R14)-C(O)-R15; -C n -alkyl-N(R14)-C(O)-R15 with n=0-3, -C n -alkyl-C(O)-OR16 with n=0-3, -O(C 1 -C 3 -alkyl-O) m -C 1 -C 3 -alkyl-OR10 with m=0-3, -C n -alkyl-OR16 with n=0-3, -NH-C n -alkyl-R18 with n=0-3; -O-C n -alkyl-R18 with n=0-3; -OPO(OR10) 2 , -PO(OR10) 2 , and a heterocycle optionally substituted by one or more R17; R10 is selected from H and C 1 -C 6 -alkyl optionally substituted by one or more R11; said one or more R11 is independently selected from Cl, F and hydroxy; R12, R13, R14, R15 and R16 are independently selected from H, C 1 -C 6 -alkyl optionally substituted by one or more R11, C 3 -C 6 -cycloalkyl optionally substituted by one or more R11, -SO 2 -C 1 -C 6 -alkyl optionally substituted by one or more R11, or wherein said R12 and R13 together with the nitrogen to which they are attached form a heterocycle optionally substituted by one or more R17; said one or more R17 is independently selected from halogen, hydroxy, NO 2 , CN, -N(R12)(R13), -C(O)-R16, -C(O)-OR16, -C n -alkyl-OR16 with n=0-3, C 1 -C 6 -alkyl optionally substituted by one or more R11, and C 1 -C 6 -alkoxy optionally substituted by one or more R11; R18 is selected from -N(R12)(R13), -OR10, -C(O)-R16, -C(O)-OR16, -C(O)- N(R12)(R13), CN, and a heterocycle optionally substituted by one or more R17; and wherein at least one of R1, R2, R4, R5, R6, R7, R8 or R9 is not H; and pharmaceutically acceptable salts, stereoisomers, enantiomers, tautomers of the compounds of formula (I) as well as pharmaceutical compositions thereof and their uses in methods of reducing the virulence of bacteria that express AgrA, in methods for preventing or treating diseases caused or exacerbated by bacteria, preferably by Staphylococcus aureus, such as skin or lung infections or atopic dermatitis.