| 摘要 |
<p>This invention relates to 2,2-di-substituted benzopyran compounds which possess leukotriene-D4 (LTD4) antagonistic activity. In particular this invention relates to LTD4 antagonists of the formula: <CHEM> or a pharmaceutically acceptable addition salt thereof, wherein R<1> is methyl, phenyl, <CHEM> wherein X1 and X2 may be the same or different and are members of the group comprising hydrogen, -Cl, -Br, -CF3, -NH2, -NO2, or straight or branched chain alkyl of 1-3 carbon atoms; wherein m is an integer from 1-9; wherein n is an integer from 1-5; wherein V is @C=O, -CH(OH)-, or -CH2-; wherein W is hydrogen or straight or branched chain alkyl of 1-6 carbon atoms; wherein Y is hydrogen or -COCH3; wherein Z is -CHO, -COOR<2>, -COR<3>, <CHEM> or -CH2OR<4>; wherein R<2> is hydrogen, a pharmaceutically acceptable cation, straight or branched chain alkyl having 1-6 carbon atoms, <CHEM> or -CH(CH2OR<5>)2 with the proviso that when Z is -COOR<2>, the R<2> substituent in one -COOR<2> moiety may be the same or different from the R<2> substituent in the other COOR<2> moiety; wherein R<3> is <CHEM> and wherein R<7> and R<8> may be the same or different and are members of the group comprising hydrogen or straight or branched chain alkyl having 1-6 carbon atoms; or wherein N, R<7>, and R<8> may together form a cyclic amine of the formula <CHEM> wherein p is 4 or 5; wherein R<4> is hydrogen, or - @-R<6>; wherein R<5> is hydrogen, benzyl-, or straight or branched chain alkyl having 1-3 carbon atoms; and wherein R<6> is straight or branched chain alkyl of 1-6 carbon atoms.</p> |
