| abstract |
A compound represented by the following structural nformula (I): n nwherein n (a) R₁ is C₈ to C₁₃ alkyl, C₇ to C₁₂ alkoxy, C₇ to C₁₂ nalkylthio, C₁₀ to C₁₂ 1-alkynyl, 10-undecynyloxy, 11-ndodecynyl, phenyl-C₄ to C₁₀ alkyl, phenyl-C₃ to C₉ alkoxy, nphenylthio-C₃ to C₉ alkyl with the phenyl optionally mono nsubstituted with bromo, chloro, trifluoromethyl, nalkoxy, methylthio or trifluoromethylthio, thienyl-C₄ to C₁₀ nalkyl furyl-C₄ to C₁₀ alkyl,trifluoromethyl-C₇ to C₁₂ alkyl or ncycloheyl-C₄ to C₁₀ alkyl; and n R₂ is hydrogen, bromo, chloro, methyl, trifluoromethyl, nhydroxy, alkoxy or nitro; (b) or R₁ is hydrogen and R₂ is C₈ to C₁₃ alkyl, C₇ to C₁₂ nalkoxy, C₇ to C₁₂ alkylthio, C₁₀ to C₁₂ 1-alkynyl, 10-nundecynyloxy, 11-dodecynyl, phenyl-C₄ to C₁₀ alkyl, phenyl-C₃ nto C₉ alkoxy, phenylthio-C₃ to C₉ alkyl with the phenyl noptionally mono substituted with bromo, chloro, trifluoronmethyl, alkoxy, methylthio or trifluoromethylthio, nfuryl-C₄ to C₁₀ alkyl, trifluoromethyl-C₇ to C₁₂ alkyl or ncyclohexyl-C₄ to C₁₀ alkyl; n q is 0, 1, or 2; n Y is COR₃, CH(R₄)(CH₂) m COR₃ or CH(R₄)(CH₂) m -ntetrazol-5-yl the tetrazol-5-yl being nunsubstituted or substituted with A; n n R₁₆ and R₁₇ are independently hydrogen or C₁₋₄ alkyl; n j is 0 to 6; n n n R₁₈ is hydrogen, alkyl, COR₃, SO₃H, SO₂NH₂, COCH₂OH or nCHOHCH₂OH; n R₃ is amino, (CH₂) n CO₂CH₂CONR₁₆R₁₇, or OR₁₄; n R₁₄ is hydrogen, alkyl, cycloalkyl, aryl, arylalkyl, nalkylaryl, alkylarylalkyl, alkyl substituted amino or alkylamino, - nOCH₂CONR₇R₈, indanyl, pivaloyloxymethyl, acetoxymethyl, npropionyloxymethyl, glycyloxymethyl, phenylglycyloxymethyl, or nthienylglycyloxymethyl; n R₄ is hydrogen, methyl, alkoxy, fluoro or hydroxy; n m is 0, or 1; n R is (CH₂) n nCOR₆, CH(CO₂H)CH₂COR₆, n(CH₂) n CO₂CH₂CONR₁₆,R₁₇, or nan imidazole of the formula n n n is 0 to 6; n R₅ is hydrogen, amino, or NHCOCH₂CH₂CH(NH₂)CO₂H; n R₆ is amino, NH(CH₂) n CO₂H, SO₃H, SO₂NH₂, CN, tetrazol-5-yl nunsubstituted or substituted with A as defined above, or OR₁₅; n R₇ is hydrogen, alkyl or alkenyl; n R₈ is hydrogen, alkyl, carboxyl or carboxamido, or, nwhen R₇ and R₉ are hydrogen or alkyl, (CH₂) m COOR₁₅; n R₉ is hydrogen, alkyl or (CH₂) m COOR₁₅; n R₁₅ is hydrogen, alkyl, cycloalkyl, aryl, narylalkyl, alkylaryl, alkylarylalkyl, allayl substituted amino nor alkylamino, -OCH₂CONR₇R₈, indanyl, pivaloyloxymethyl, nacetoxymethyl, propionyloxymethyl, glycyloxymethyl, nphenylglycyloxymethyl, or thienylglycyloxymethyl; n provided that 1) when n is 0, R₅ is hydrogen, 2) R₇, R₈ nand R₉ are not all hydrogen, 3) any of R₁and R₂ above are not nalkylthio or phenylthioalkyl when q is 1 or 2, 4) R₃ and R₆ are nnot both hydroxy, 5) OR₁₄ and OR₁₅ are not simultaneously nhydroxy; 6) if R₄ is hydroxy and m is 0, R₁₄ is hydrogen; or n a pharmaceutically acceptable salt thereof. |