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N-oxides of amino containing pyrido ›2,3-D! pyrimidines

  • US 5,945,422 A
  • Filed: 01/29/1998
  • Issued: 08/31/1999
  • Est. Priority Date: 02/05/1997
  • Status: Expired due to Fees
First Claim
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1. A compound of the formula ##STR42## wherein A and B are linkers which independently are C1 -C6 - alkylene, C1 -C6 - alkylenoxy, C1 -C6 - alkylenethio, or phenylene;

  • X is NH, N--C1 -C6 alkanoyl, O, or S;

    R2 is hydrogen, (CH2)n Ph, where Ph is phenyl or phenyl substituted by one, two or three groups selected from halo, C1 -C6 alkyl, C1 -C6 alkoxy, SH, C1 -C6 alkylthio, hydroxy, C1 -C6 alkanoyl, --CN, --NO2, C1 -C6 alkanoyloxy, --CF3 or NR5 R6, and n is 0, 1, 2, or 3,C3 -C6 -cycloalkyl, C1 -C6 alkanoyl, C2 -C6 alkenyl, and C2 -C6 alkynyl, where the alkyl, alkenyl, and alkynyl groups may be substituted by NR5 R6, phenyl, C1 -C6 alkylthio, C1 -C6 -alkyloxy, hydroxy, carboxy, halogen, C3 -C6 - cycloalkyl, or phenyl substituted by one, two or three groups selected from halo, C1 -C6 alkyl, C1 -C6 alkoxy, SH, C1 -C6 alkylthio, hydroxy, C1 -C6 alkanoyl, --CN, --NO2, C1 -C6 alkanoyloxy, --CF3 or NR5 R6, and where R5 and 6 are independently hydrogen, C1 -C6 alkyl, C2 -C6 alkenyl, C2 -C6 alkynyl, (CH2)n Ph where Ph is phenyl or phenyl substituted by one, two or three groups selected from halo, C1 -C6 alkyl, C1 -C6 alkoxy, SH, C1 -C6 alkylthio, hydroxy, C1 -C6 alkanoyl, --CN, --NO2, C1 -C6 alkanoyloxy, --CF3 or NR5 R6, and n is 0, 1, 2, or 3, C3 -C6 - cycloalkyl, or R5 and R6 taken together nitrogen to which they are attached can complete a ring selected from piperazine;

    Ar is phenyl, phenyl substituted by one, two or three groups selected from halo, C1 C6 alkyl, C1 C6 alkoxy, SH, C1 C6 alkylthio, hydroxy, C1 C6 alkanoyl, --CN, --NO2, C1 -C6 alkanoyloxy, --CF3 or NR56, or the pharmaceutically acceptable salts thereof.

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