1,4-benzodiazepine-2,5-diones and related compounds with therapeutic properties

1,4-benzodiazepine-2,5-diones and related compounds with therapeutic properties

  • CN 102,753,544 A
  • Filed: 11/03/2010
  • Published: 10/24/2012
  • Est. Priority Date: 11/17/2009
  • Status: Active Application
First Claim
Patent Images

1. be designed to suppress the compound of Rho kinase activity in the cell;

  • Said compound is described by being selected from following chemical formula;

    it is substituted and unsubstituted, comprises R and S enantiomeric form and racemic mixture;

    Wherein R1 is the chemical group that contains at least two carbon molecules, and the said chemical group that wherein contains at least two carbon molecules is not a pyridine;

    Wherein R1 '"'"'is selected from;

    R wherein 2Be selected from H, alkyl, substituted alkyl and R 1R wherein 3Be selected from H, alkyl (for example, methyl, ethyl, hexyl, sec.-propyl) and substituted alkyl;

    H;

    CH 3Ethyl;

    Hexyl;

    Sec.-propyl;

    Halogen (for example, fluorine, chlorine, bromine, iodine, astatine);

    OH;

    The chemical part that contains the secondary group of aryl;

    The chemical part that contains the secondary group of substituted aryl;

    The chemical part that contains the secondary group of cyclic aliphatic;

    The chemical part that contains the secondary group of substituted cyclic aliphatic;

    The chemical part that contains the secondary group of heterocycle;

    The chemical part that contains the secondary group of substituted heterocycle;

    The chemical part that contains the secondary group of at least one ester;

    The chemical part that contains the secondary group of at least one ether;

    Have the straight or branched of at least 2 carbon, saturated or unsaturated, replacement or non-substituted aliphatic chain;

    The chemical part that contains sulphur;

    The chemical part that contains nitrogen;

    -OR-, wherein R is selected from;

    the chemical part that comprises the secondary group of aryl;

    The chemical part that comprises the secondary group of substituted aryl;

    The chemical part that comprises the secondary group of cyclic aliphatic;

    The chemical part that comprises the secondary group of substituted cyclic aliphatic;

    The chemical part that comprises the secondary group of heterocycle;

    The chemical part that comprises the secondary group of substituted heterocycle;

    Have the straight or branched of at least 2 carbon, saturated or unsaturated, replacement or non-substituted aliphatic chain;

    The chemical part that comprises the secondary group of at least one ester;

    The chemical part that comprises the secondary group of at least one ether;

    The chemical part that comprises sulphur;

    With the chemical part that comprises nitrogen;

    Wherein R4 is selected from C, N, S and O;

    Wherein R5 is selected from H, alkyl, substituted alkyl, mono-substituted aryl, dibasic aryl and trisubstituted aryl;

    Wherein R6 is selected from C, N, S and O;

    Wherein R7, R8, R9 and R10 are independently selected from;

    do not exist, and H, halogen, CF3, (for example, substituted alkyl) (for example, unsubstituted alkyl), (for example, substituted alkyl) (for example, unsubstituted alkyl), OH, fluoroalkyl, sulphonamide, sulfone, OCH 3, CH 3, SO 2R 28, SO 2N (R 7 '"'"') 2, OR 7 '"'"', N (R 7 '"'"') 2, CON (R 7 '"'"') 2, NHCOR 7 '"'"', NHSO 2R 7 '"'"', alkyl, mono-substituted alkyl, dibasic alkyl, trisubstituted alkyl;

    R wherein 7 '"'"'Be selected from halogen, H, alkyl, mono-substituted alkyl, dibasic alkyl;

    Trisubstituted alkyl, aryl, mono-substituted aryl, dibasic aryl;

    Trisubstituted aryl, cycloaliphatic, mono-substituted cycloaliphatic, dibasic cycloaliphatic and trisubstituted cycloaliphatic;

    Wherein R11, R12, R13 and R14 are independently selected from;

    H;

    Alkyl (for example;

    Substituted alkyl) (for example;

    Unsubstituted alkyl);

    Fluoroalkyl;

    (for example;

    Substituted alkyl) (for example;

    Unsubstituted alkyl);

    Aminoalkyl group;

    (for example, substituted alkyl) (for example, unsubstituted alkyl);

    and its substituted and unsubstituted and its verivate;

    Wherein R15, R16, R17 and R18 are independently selected from;

    C, N, O and S;

    Wherein R19 is selected from;

    H, alkyl (for example, substituted alkyl) (unsubstituted alkyl);

    Ketone;

    Comprise the chemical part (for example, substituted alkyl) (unsubstituted alkyl) of nitrogen, (for example wrap oxygen containing chemical part;

    Substituted alkyl) (unsubstituted alkyl) and comprise the chemical part (for example, substituted alkyl) (unsubstituted alkyl) of sulphur;

    Wherein R20 is selected from;

    H, alkyl (for example, substituted alkyl) (unsubstituted alkyl);

    Ketone;

    Comprise the chemical part (for example, substituted alkyl) (unsubstituted alkyl) of nitrogen, (for example wrap oxygen containing chemical part;

    Substituted alkyl) (unsubstituted alkyl) and comprise the chemical part (for example, substituted alkyl) (unsubstituted alkyl) of sulphur;

    Wherein R21, R22, R23 and R24 are independently selected from;

    do not exist, and H, halogen, CF3, (for example, substituted alkyl) (for example, unsubstituted alkyl), (for example, substituted alkyl) (for example, unsubstituted alkyl), OH, fluoroalkyl, sulphonamide, sulfone, OCH 3, CH 3, SO 2R 7 '"'"', SO 2N (R 7 '"'"') 2, OR 7 '"'"', N (R 7 '"'"') 2, CON (R 7 '"'"') 2, NHCOR 7 '"'"', NHSO 2R 7 '"'"', alkyl, mono-substituted alkyl, dibasic alkyl, trisubstituted alkyl;

    R wherein 7 '"'"'Be selected from halogen, H, alkyl, mono-substituted alkyl, dibasic alkyl;

    Trisubstituted alkyl, aryl, mono-substituted aryl, dibasic aryl;

    Trisubstituted aryl, cycloaliphatic, mono-substituted cycloaliphatic, dibasic cycloaliphatic and trisubstituted cycloaliphatic;

    Wherein among R21, R22, R23 and the R24 at the most two can be hydrogen;

    With Wherein R25, R26, R27 and R28 are independently selected from;

    hydrogen;

    Alkyl (for example;

    Substituted alkyl) (for example;

    Unsubstituted alkyl);

    Fluoroalkyl;

    (for example;

    Substituted alkyl) (for example;

    Unsubstituted alkyl);

    Aminoalkyl group;

    (for example, substituted alkyl) (for example, unsubstituted alkyl);

    and substituted and unsubstituted and its verivate;

    Wherein among R25, R26, R27 and the R28 at the most three can be hydrogen.

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