发明名称 Benzisoxazoles
摘要 The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents an integer from 1 to 3; X represents amino, hydroxy, -oxo or -Z-R<SUP>1</SUP>; Y is absent when X represents -Z-R<SUP>1 </SUP>and -(C-O)-R<SUP>6 </SUP>when X represents oxo; Z represents carbonyl, -oxy-carbonyl- or -NR<SUP>5</SUP>-carbonyl-; R<SUP>1 </SUP>represents C<SUB>1-4</SUB>alkyl, Ar<SUP>1</SUP>, Ar<SUP>1</SUP>-C<SUB>1-4</SUB>alkyl-, -NR<SUP>3</SUP>R<SUP>4 </SUP>or -Het<SUP>1</SUP>; R<SUP>2 </SUP>represents hydrogen, halo, nitro, hydroxycarbonyl-, C<SUB>1-4</SUB>alkyloxy or C<SUB>1-4</SUB>alkyl; R<SUP>3 </SUP>and R<SUP>4 </SUP>are each independently selected from hydrogen, Ar<SUP>3 </SUP>or C<SUB>1-4</SUB>alkyl; R<SUP>5 </SUP>represents hydrogen, C<SUB>1-4</SUB>alkylcarbonyl- or Ar<SUP>4</SUP>-carbonyl-; R<SUP>6 </SUP>represents a substituent selected from the group consisting of C<SUB>1-4</SUB>alkyl, Ar<SUP>5</SUP>, Ar<SUP>6</SUP>-C<SUB>1-4</SUB>alkyl- or NR<SUP>7</SUP>R<SUP>8</SUP>; R<SUP>7 </SUP>and R<SUP>8 </SUP>are each independently selected from hydrogen, Het<SUP>4 </SUP>or C<SUB>1-4</SUB>alkyl; Het<SUP>1 </SUP>represents a heterocycle selected from oxazolyl, isoxazolyl, imidazolyl or pyrazolyl wherein said heterocycle is optionally substituted with one, two or three substitutents selected from the group consisting of amino, C<SUB>1-4</SUB>alkyl, hydroxy-C<SUB>1-4</SUB>alkyl, phenyl, phenyl-C<SUB>1-4</SUB>alkyl- and phenyl substituted with one or more halo substitutents; Het<SUP>4 </SUP>represents a heterocycle selected from oxazolyl or isoxazolyl, wherein said heterocycle is optionally substituted with one or more substitutents selected from the group consisting of amino, C<SUB>1-4</SUB>alkyl, hydroxy-C<SUB>1-4</SUB>alkyl-, phenyl, phenyl-C<SUB>1-4</SUB>alkyl and phenyl substituted with one or more halo substitutents; and Ar<SUP>1</SUP>, Ar<SUP>2</SUP>, Ar<SUP>3</SUP>, Ar<SUP>4</SUP>, Ar<SUP>5 </SUP>or Ar<SUP>6 </SUP>each independently represents phenyl optionally substituted one or where possible two or more substitutents selected from halo, nitro, C<SUB>1-4</SUB>alkyl, hydroxy or C<SUB>1-4</SUB>alkyloxy-.
申请公布号 US2007197610(A1) 申请公布日期 2007.08.23
申请号 US20050598957 申请日期 2005.03.11
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 KENNIS LUDO E.J.;VANHOOF GRETA C.P.;BONGARTZ JEAN-PIERRE A.M.;LUYCKX MARCEL G.M.;MINKE WENDA E.
分类号 A61K31/426;A61K31/42;A61K31/423;A61K31/425;A61K31/428;C07D261/20;C07D413/02;C07D413/12;C07D417/02 主分类号 A61K31/426
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