Pyrrolotriazines inhibitors of kinases

Pyrrolotriazines inhibitors of kinases

  • CN 1,351,498 A
  • Filed: 05/16/2000
  • Published: 05/29/2002
  • Est. Priority Date: 05/21/1999
  • Status: Active Grant
First Claim
Patent Images

1. the chemical compound of a formula I Its enantiomer, diastereomer and pharmaceutically acceptable salt, prodrug and its solvate, wherein X and Y independently are selected from O, OCO, S, SO, SO 2, CO, CO 2, NR 10, NR 11CO, NR 12CONR 13, NR 14CO 2, NR 15SO 2, NR 16SO 2NR 17, SO 2NR 18, CONR 19, halogen, nitro, cyano group, perhaps X or Y do not exist;

  • Z is selected from O, S, N or CR 20R 1Be hydrogen, CH 3, OH, OCH 3, SH, SCH 3, OCOR 21, SOR 22, SO 2R 23, SO 2NR 24R 25, CO 2R 26, CONR 27R 28, NH 2, NR 29SO 2NR 30R 31, NR 32SO 2R 33, NR 34COR 35, NR 36CO 2R 37, NR 38CONR 39R 40, halogen, nitro or cyano group;

    R 2And R 3Independently be the Heterocyclylalkyl of aralkyl, Heterocyclylalkyl or replacement of heterocyclic radical, aralkyl, the replacement of aryl, heterocyclic radical, the replacement of alkynyl, aryl, the replacement of alkenyl, alkynyl, the replacement of alkyl, alkenyl, the replacement of hydrogen, alkyl, replacement, or when X is halogen, nitro or cyano group R 2Do not exist, or when Y is halogen, nitro or cyano group, R 3Do not exist;

    R 4And R 5Independently be heterocyclic radical, the aralkyl of aryl, heterocyclic radical, the replacement of alkyl, aryl, the replacement of hydrogen, alkyl, replacement, the aralkyl of replacement, or R 4And R 5Can form optional monocycle 5-7 unit saturated or unsaturated carbocyclic or the heterocycle that replaces together, or optional dicyclo 7-11 saturated or undersaturated carbocyclic ring of unit or the heterocycle that replaces, except when Z is when being O or S, R 5Do not exist, or when Z is nitrogen, R 4And R 5Not all be hydrogen;

    R 6Be alkyl, aryl, the aryl of replacement, heterocyclic radical, the heterocyclic radical of replacement, the NR of hydrogen, alkyl, replacement 7R 8, OR 9Or halogen;

    R 7, R 8, R 9, R 10, R 11, R 12, R 13, R 14, R 15, R 16, R 17, R 18, R 19, R 21, R 24, R 25, R 26, R 27, R 28, R 29, R 30, R 31, R 32, R 34, R 35, R 36, R 38, R 39And R 40Independently be selected from the heterocyclic radical of aryl, heterocyclic radical or replacement of alkyl, aryl, the replacement of hydrogen, alkyl, replacement;

    R 22, R 23, R 33And R 37Independently be selected from the heterocyclic radical of aryl, heterocyclic radical or replacement of alkyl, aryl, the replacement of alkyl, replacement;

    And R 20Be selected from the alkyl of hydrogen, low alkyl group or replacement, if or the carbon atom that it connected when being the aryl of insatiable hunger or heteroaryl ring a part of, then R 20Do not exist;

    Condition is;

    If a. X is SO, SO 2, NR 13CO 2Or NR 14SO 2, R 2Cannot be hydrogen. If b. Y is SO, SO 2, NR 13CO 2Or NR 14SO 2, R 3Cannot be hydrogen.

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