2-arylthiazole derivatives and pharmaceutical composition thereof

  • US 5,614,520 A
  • Filed: 01/30/1995
  • Issued: 03/25/1997
  • Est. Priority Date: 11/30/1990
  • Status: Expired due to Term
First Claim
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1. A 2-arylthiazole derivative having the following formula (I), and a pharmaceutically acceptable salt thereof:

  • ##STR71## wherein Ar is an unsubstituted or substituted furyl group;

    or a group represented by the following formula (II);

    ##STR72## wherein R1, R2, and R3 are hydrogen, a halogen atom, or a nitro, cyano or formyl group;

    or a group of OR, S(O)n R and NRR1 (wherein n is an integer of from 1 to 2, R represents an unsubstituted or substituted C1-10 alkyl, aryl, aralkyl, alkylcarbonyl, arylcarbonyl or aralkylcarbonyl group, R1 represents a hydrogen atom, or an unsubstituted or substituted C1-10 alkyl, aryl, aralkyl, alkylcarbonyl, arylcarbonyl or aralkylcarbonyl group;

    or R and R1, taken together with the nitrogen atom bonded thereto, represent atoms forming an unsubstituted or substituted 5- or 7-membered heterocyclic ring), or a group of COR" wherein R" represents an unsubstituted or substituted C1-10 alkyl, aryl or aralkyl group;

    a hydroxyl group;

    an unsubstituted or substituted C1-10 alkoxy, aryloxy or aralkyloxy group;

    an amino group;

    or an unsubstituted or substituted C1-10 alkyl (mono- or di-substituted, independently) amino, aryl (mono- or di-substituted, independently) amino or aralkyl (mono- or di-substituted, independently) amino group, or a 5- to 7-membered cyclic amino group, and at least one of R1, R2 or R3 is other than hydrogen;

    X is a hydrogen atom, or a C1-14 alkyl, carboxyl, C1-5 alkoxycarbonyl, carbamoyl or C1-4 alkyl (mono- or di-substituted) aminocarbonyl group; and

    Y represents a hydrogen atom or a C1-4 alkyl, carboxyl, C1-5 alkoxycarbonyl, carbamoyl or C1-4 alkyl (mono- or di-substituted) aminocarbonyl group, with the proviso that when at least one group of R1, R2 and R3 represents a halogen atom, or an alkoxy, alkylamino or nitro group, at least one group of the two other groups represents a group other than a hydrogen atom;

    when at least one group of R1, R2 and R3 is a halogen atom and another group is a hydrogen atom, a remaining group is a group other than a halogen atom, or an alkoxy, alkylamino or acylamino group, with the additional proviso that when any one of R1, R2 or R3 is OR, one of the remaining groups cannot represent hydrogen while the other group represents OR, or the remaining two groups cannot both represent OR at the same time, nor do all of R1 -R3 represent halogen;

    with the further proviso that both X and Y do not represent carboxyl, C1-5 alkoxycarbonyl, carbamoyl or C1-4 alkyl (a mono- or di-substituted) aminocarbonyl group at the same time.

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