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3-Alkoxyisoxazol-4-yl-substituted 2-amino carboxylic acid compounds

  • US 6,200,999 B1
  • Filed: 05/20/1999
  • Issued: 03/13/2001
  • Est. Priority Date: 10/04/1996
  • Status: Expired due to Fees
First Claim
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1. A (3-alkoxyisoxazol-4-yl)-substituted 2-amino carboxylic acid derivative having general Formula I or II wherein R1 is hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, cycloalk(en)yl, cycloalk(en)yl-C1-6alk(en/yn)yl or phenyl-C1-6alk(en/yn)yl, the phenyl group being optionally substituted with CF3, halogen, C1-6 alkyl or C1-6 alkoxy;

  • A is a bond or a spacer group selected from C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene, and cycloalkylene;

    B is a group —

    CRa (NRbRc)—

    COOR5 wherein Ra-Rc are independently hydrogen or C1-6 alkyl, and R5 is defined as R1 or pivaloyloxymethyl, or B is a group of Formula III

    wherein R2, R3 and R4 are independently selected from the group consisting of a) hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, cycloalk(en)yl, cycloalk(en)yl-C1-6 alk(en/yn)yl, phenyl-C1-6 alkyl, thienyl-C1-6-alkyl, and b) C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl in which one or more carbon atoms are replaced by N, O, and/or S, or R3 and R4 are connected, thereby forming a C2-C6 alkylene, C2-C6 alkenylene or C2-C6 alkynylene group, or R4 and R2 are connected in order to form a C1-C3 alkylene, C2-C3 alkenylene or C2-C3 alkynylene group optionally mono- or di-substituted with hydroxy or methyl, or to form CH2

    O—

    CH2;

    E is COOR6, where R6 is defined as R5;

    X is O;

    Y is O or S;

    or a pharmaceutically acceptable salt thereof.

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