发明名称 Dimeric Piperidine Derivatives
摘要 the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; R<SUP>2 </SUP>represents hydroxy; -X- represents C<SUB>2-4</SUB>alkynyl, C<SUB>1-12</SUB>alkyl optionally substituted with hydroxy or X represents a divalent radical of the formula wherein; -X<SUB>1</SUB>- represents C<SUB>1-12</SUB>alkyl, phenyl or a divalent radical selected from the group consisting of -X<SUB>2</SUB>- represents C<SUB>1-12</SUB>alkyl, C<SUB>1-4</SUB>alkyloxyC<SUB>1-4</SUB>alkyl, phenyl or a divalent radical of formula -X<SUB>3</SUB>- represents phenyl or a divalent radical selected from the group consisting of R<SUP>1 </SUP>independently represents hydrogen, C<SUB>1-4</SUB>alkyl, C<SUB>1-4</SUB>alkyloxy-, Ar<SUP>1</SUP>, Ar<SUP>2</SUP>-carbonyl, Het<SUP>1</SUP>-C<SUB>1-4</SUB>alkyl, Het<SUP>2</SUP>, NR<SUP>3</SUP>R<SUP>4</SUP>-C<SUB>1-4</SUB>alkyl, Ar<SUP>3</SUP>-C<SUB>1-4</SUB>alkyloxy- or Het<SUP>4</SUP>-oxy-; R<SUP>3 </SUP>and R<SUP>4 </SUP>each independently represents hydrogen, C<SUB>1-4</SUB>alkyl, C<SUB>1-4</SUB>alkyloxy-, or Het<SUP>3</SUP>; Het<SUP>1 </SUP>represents a heterocycle selected from pyridinyl, indolinyl, indolyl, benzimidazolyl, benzthiazolyl, benzisoxazolyl, thiazolyl, pyridinyl, or thiadiazolyl wherein said Het<SUP>1 </SUP>is optionally substituted with one or where possible two or more substituents selected from the group consisting of hydroxy, halo, C<SUB>1-4</SUB>alkyloxycarbonyl-, C<SUB>1-4</SUB>alkyl-, C<SUB>1-4</SUB>alkyloxy- and C<SUB>1-4</SUB>alkyloxy-substituted with halo; in particular Het<SUP>1 </SUP>represents a heterocycle selected from indolyl or pyridinyl; Het<SUP>2 </SUP>represents a heterocycle selected from indolyl, benzisoxazolyl or oxodiazolyl wherein said Het<SUP>2 </SUP>is optionally substituted with one or where possible two or more substituents selected from the group consisting of hydroxy, halo, C<SUB>1-6</SUB>alkyl- and C<SUB>1-4</SUB>alkyloxy-; Het<SUP>3 </SUP>represents a heterocycle selected from benzimidazolyl, benzisoxazolyl or benzthiazolyl wherein said Het<SUP>3 </SUP>is optionally substituted with one or where possible two or more substituents selected from the group consisting of hydroxy, halo, C<SUB>1-6</SUB>alkyl- and C<SUB>1-4</SUB>alkyloxy-; in particular Het<SUP>3 </SUP>represents benzthiazolyl substituted with C<SUB>1-4</SUB>alkyloxy-; Het<SUP>4 </SUP>represents a heterocycle selected from benzimidazolyl, benzisoxazolyl or benzthiazolyl wherein said Het<SUP>4 </SUP>is optionally substituted with one or where possible two or more substituents selected from the group consisting of hydroxy, halo, C<SUB>1-6</SUB>alkyl- and C<SUB>1-4</SUB>alkyloxy-; in particular Het<SUP>4 </SUP>represents benzthiazolyl; Ar<SUP>1 </SUP>represents phenyl optionally substituted with halo, C<SUB>1-4</SUB>alkyl or C<SUB>1-4</SUB>alkyl substituted with one, two or three halo substituents; Ar<SUP>2 </SUP>represents phenyl optionally substituted with halo, C<SUB>1-4</SUB>alkyl or C<SUB>1-4</SUB>alkyl substituted with one, two or three halo substituents; in particular Ar<SUP>2 </SUP>represents phenyl substituted with halo or trifluromethyl; Ar<SUP>3 </SUP>represents phenyl optionally substituted with halo, C<SUB>1-4</SUB>alkyl or C<SUB>1-4</SUB>alkyloxy-.
申请公布号 US2008015225(A1) 申请公布日期 2008.01.17
申请号 US20050632479 申请日期 2005.07.13
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 CIK MIROSLAV;DIELS GASTON STANISLAS M.;VAN LOMMEN GUY R.E.
分类号 A61K31/445;A61P25/00;C07D211/16;C07D211/96;C07D401/00;C07D401/04;C07D413/06;C07D417/12 主分类号 A61K31/445
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