| 摘要 |
<p>Novel dibenz[b,flthiepin derivatives have the formula</p><p><Chemistry id="chema01" num="0001"><Image id="ia01" he="27" wi="82" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry><Chemistry id="chema02" num="0002"><Image id="ia02" he="21" wi="82" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry><Chemistry id="chema03" num="0003"><Image id="ia03" he="27" wi="83" file="IMGA0003.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein n is 1 or 2;
<UnorderedLists id="ula01" listStyle="none"><ListItem>the broken lines represent optional double bonds;</ListItem><ListItem>Z is thio, sulfinyl or sulfonyl;</ListItem><ListItem>each of R<Sup>2</Sup>, R<Sup>3</Sup> and R<Sup>9</Sup>, independently of the others, is a hydrogen or halogen atom or a nitro, lower alkyl, amino, N-(lower alkyl)amino, N,N-di(lower alkyl)amino, lower alkanoyl, hydroxy, lower alkoxy, lower acyloxy, lower alkylthio, trifluoromethylthio, lower alkylsulfinyl, lower alkylsulfonyl ortri- fluoromethyl radical, or R<Sup>2</Sup> and R<Sup>3</Sup> together represent a doubly bonded oxygen; and</ListItem><ListItem>R<Sup>1</Sup> is</ListItem><ListItem>(a) 5-tetrazoyl, 5-tetrazoylmethyl, 3-hydroxy-1,2,5-thia- diazol-4-yl, 4-hydroxy-Δ<Sup>3</Sup>-pyrrolin-3-yl-2,5-dione or
<Chemistry id="chema04" num="0004"><Image id="ia04" he="14" wi="29" file="IMGA0004.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>where m is 0, 1,2,3 or 4 and R<Sub>4 </Sub>is hydroxy, lower alkoxy, N,N-di(lower alkyl)aminolower alkoxy), lower hydroxyalkyl, lower carboxylalkoxy, amino, N-(lower alkyl)amino, N,N-di(lower alkyl)amino, lower alkylsulfonylamino, carboxy(lower alkyl)-amino, carboxamido(lower alkyl)amino, 2-imino-3-methylthia zolidine, (lower acyloxy)-(lower alkoxy) or (5-methyl-2-oxo-1,3-dioxolen-4-yl)methoxy</ListItem><!-- EPO <DP n="2"> --><ListItem>(b) -CHO or a prodrug derivative of an aldehyde having the formulae:
<Chemistry id="chema05" num="0005"><Image id="ia05" he="13" wi="52" file="IMGA0005.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>where R<Sub>5</Sub> is hydrogen, lower alkyl, aryl, hydroxy, lower alkoxy, lower acyloxy, amino or lower alkylamino; each of Y and Z, independently of the other, is oxygen, sulfur or NR<Sub>6</Sub>; and each of R<Sub>6</Sub> and R<Sub>7</Sub>, independently of the other, is hydrogen lower alkyl or R<Sub>6</Sub> and R<Sub>7</Sub> are joined to form a ring of 5-8 members; or</ListItem><ListItem>(c) -(CH<Sub>2</Sub>)<Sub>n</Sub>-OR<Sub>8</Sub> where n is 0, 1, 2, 3 or 4 and R<Sub>8</Sub> is hydrogen, lower acyl, lower alkylaminoacyl, lower alkylcarboxy, lower alkylcarboxamido, lower alkylcarboxamidoacyl or (lower acyloxy)-(lower alkyl);
and compounds that are pharmaceutically acceptable salts of such dibenzothiepins. They are useful in the treatment and control of allergic conditions such as allergic asthma and of other prostaglandin-related and TXA<Sub>2</Sub>-related diseases and are made into pharmaceutical compositions suitable for treating such conditions.</ListItem></UnorderedLists></p> |
