| 摘要 |
<p>Compounds having the formula:
<Chemistry id="chema01" num="0001"><Image id="ia01" he="38" wi="128" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>
and their pharmaceutically acceptable salts or acid-addition salts are antagonists of leukotrienes of C<Sub>4</Sub>, D<Sub>4</Sub> and E<Sub>4</Sub>, the slow-reacting substance of anaphylaxis, and are useful in anti-asthmatic, anti-allergic and anti-inflammatory agents.
<UnorderedLists id="ula01" listStyle="none"><ListItem>In the formula</ListItem><ListItem>Y is Cr or N, but at least one Y must be N;</ListItem><ListItem>n is 0 to 6;</ListItem><ListItem>R is H, OH, alkyl, CF<Sub>3</Sub>, alkenyl alkoxy SH, thioalkyl, possibly substituted phenyl, benzyl, phenetyl, halogen, amino, N(R<Sub>4</Sub>)<Sub>2</Sub>, COOR<Sub>4</Sub> CH<Sub>2</Sub>OR<Sub>4</Sub>, CHO, CN, SCF<Sub>3</Sub>, or NO<Sub>2</Sub>;</ListItem><ListItem>R<Sub>1</Sub> is H, alkyl or alkoxy;</ListItem><!-- EPO <DP n="2"> --><ListItem>R<Sub>2</Sub> is H, alkyl, R<Sub>4</Sub>CO, or R<Sub>4</Sub>0CH<Sub>2</Sub>;</ListItem><ListItem>R<Sub>3</Sub> is alkyl, alkenyl possibly substituted phenyl;</ListItem><ListItem>R<Sub>4</Sub> is H or alkyl;</ListItem><ListItem>R<Sub>5</Sub> is H, OH, alkyl, alkenyl or both R<Sub>5</Sub>'s may be combined to create a doubly bonded oxygen (=0) or doubly bonded =C(R<Sub>4</Sub>)<Sub>2</Sub> group;</ListItem><ListItem>X<Sub>1</Sub> and X<Sub>2</Sub> are oxygen, S(O)<Sub>m</Sub> with m is 0-2;
<Chemistry id="chema02" num="0002"><Image id="ia02" he="14" wi="70" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry></ListItem></UnorderedLists></p><p>Z is O, S, H and OH, CH<Sub>2</Sub>, alkenyl; N-R<Sub>e</Sub> wherein R<Sub>e</Sub> is OH, N(R<Sub>4</Sub>)<Sub>2</Sub>, alkyl, alkoxy, possibly substituted phenyl;
<UnorderedLists id="ula02" listStyle="none"><ListItem>R<Sub>a</Sub> is H, OH or alkyl;</ListItem><ListItem>p is 0 to 2; and</ListItem><ListItem>r is 0 - 4;</ListItem><ListItem>R<Sup>7</Sup> is COOR<Sub>4</Sub>; CH<Sub>2</Sub>OH; CHO; tetrazole; CONHSO<Sub>2</Sub>R<Sub>9</Sub>; NHSO<Sub>2</Sub>R<Sub>9</Sub>; hydroxymethylketone; acetoxymethylketone; CN; CON(R<Sub>4</Sub>)<Sub>2</Sub>; a monocyclic or bicyclic heterocyclic ring containing an acidic hydroxyl group; or
<Chemistry id="chema03" num="0003"><Image id="ia03" he="22" wi="48" file="IMGA0003.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>
wherein s is independently 0 to 3; R<Sub>10</Sub> is</ListItem><ListItem>A) a monocyclic or bicyclic heterocyclic radical, or</ListItem><ListItem>B) the radical W-R<Sub>11</Sub> wherein W is 0, S or</ListItem><ListItem>NH and R<Sub>11</Sub> is (1) a hydrocarbon radical or (2) an acyl radical of an organic acyclic or monocyclic carboxylic acid containing not more than 1 heteroatom in the ring;</ListItem><ListItem>R<Sub>8</Sub> is H, or alkyl, and is absent when a triple bond is present.</ListItem></UnorderedLists></p> |
