公开(公告)号：US08546440B2

公开(公告)日：2013-10-01

申请号：US13133027

申请日：2009-12-16

申请人： Henricus Jacobus Maria Gijsen ,  Gregor James MacDonald ,  François Paul Bischoff ,  Gary John Tresadern ,  Andrés Avelino Trabanco-Suárez ,  Sven Franciscus Anna Van Brandt ,  Didier Jean-Claude Berthelot

发明人： Henricus Jacobus Maria Gijsen ,  Gregor James MacDonald ,  François Paul Bischoff ,  Gary John Tresadern ,  Andrés Avelino Trabanco-Suárez ,  Sven Franciscus Anna Van Brandt ,  Didier Jean-Claude Berthelot

IPC分类号： A61K31/5377 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/4196 ,  A61K31/4188 ,  C07D487/04

CPC分类号： C07D471/04

摘要： The present invention is concerned with novel substituted bicyclic imidazole derivatives of Formula (I) wherein R0, R1, R3, R4, X, A1, A2, A3, A4, Y1, Y2 and Y3 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said novel compound as an active ingredient as well as the use of said compounds as a medicament.

摘要翻译： 本发明涉及式（I）的新型取代双环咪唑衍生物，其中R 0，R 1，R 3，R 4，X，A 1，A 2，A 3，A 4，Y 1，Y 2和Y 3具有权利要求中定义的含义。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述新化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：US20110237580A1

公开(公告)日：2011-09-29

申请号：US13133027

申请日：2009-12-16

申请人： Henricus Jacobus Maria Gijsen ,  Gregor James MacDonald ,  François Paul Bischoff ,  Gary John Tresadern ,  Andrés Avelino Trabanco-Suárez ,  Sven Franciscus Anna Van Brandt ,  Didier Jean-Claude Berthelot

发明人： Henricus Jacobus Maria Gijsen ,  Gregor James MacDonald ,  François Paul Bischoff ,  Gary John Tresadern ,  Andrés Avelino Trabanco-Suárez ,  Sven Franciscus Anna Van Brandt ,  Didier Jean-Claude Berthelot

IPC分类号： A61K31/5377 ,  C07D471/04 ,  C07D487/04 ,  C07D413/14 ,  A61K31/437 ,  A61K31/5025 ,  A61K31/4985 ,  A61P25/28

CPC分类号： C07D471/04

摘要： The present invention is concerned with novel substituted bicyclic imidazole derivatives of Formula (I) wherein R0, R1, R3, R4, X, A1, A2, A3, A4, Y1, Y2 and Y3 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said novel compound as an active ingredient as well as the use of said compounds as a medicament.

摘要翻译： 本发明涉及式（I）的新型取代双环咪唑衍生物，其中R 0，R 1，R 3，R 4，X，A 1，A 2，A 3，A 4，Y 1，Y 2和Y 3具有权利要求中定义的含义。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述新化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：US08772504B2

公开(公告)日：2014-07-08

申请号：US13144557

申请日：2010-02-15

申请人： Henricus Jacobus Maria Gijsen ,  François Paul Bischoff ,  Wei Zhuang ,  Sven Franciscus Anna Van Brandt ,  Michel Surkyn ,  Mirko Zaja ,  Didier Jean-Claude Berthelot ,  Michel Anna Jozef De Cleyn ,  Gregor James MacDonald ,  Daniel Oehlrich

发明人： Henricus Jacobus Maria Gijsen ,  François Paul Bischoff ,  Wei Zhuang ,  Sven Franciscus Anna Van Brandt ,  Michel Surkyn ,  Mirko Zaja ,  Didier Jean-Claude Berthelot ,  Michel Anna Jozef De Cleyn ,  Gregor James MacDonald ,  Daniel Oehlrich

IPC分类号： C07D235/00 ,  C07D403/02

CPC分类号： C07D413/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

摘要： The present invention is concerned with novel substituted benzoxazole, benzimidazole, oxazolopyridine and imidazopyridine derivatives of Formula (I) wherein R1, R2, R3, R4, X, A1, A2, A3, A4, Y1, Y2, Y3 and Z have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

摘要翻译： 本发明涉及式（I）的新的取代苯并恶唑，苯并咪唑，恶唑并吡啶和咪唑并吡啶衍生物，其中R1，R2，R3，R4，X，A1，A2，A3，A4，Y1，Y2，Y3和Z具有含义 在权利要求中限定。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：US08946426B2

公开(公告)日：2015-02-03

申请号：US13144554

申请日：2010-02-02

申请人： Henricus Jacobus Maria Gijsen ,  Adriana Ingrid Velter ,  Gregor James MacDonald ,  François Paul Bischoff ,  Tongfei Wu ,  Sven Franciscus Anna Van Brandt ,  Michel Surkyn ,  Mirko Zaja ,  Serge Maria Aloysius Pieters ,  Didier Jean-Claude Berthelot ,  Michel Anna Jozef De Cleyn ,  Daniel Oehlrich

发明人： Henricus Jacobus Maria Gijsen ,  Adriana Ingrid Velter ,  Gregor James MacDonald ,  François Paul Bischoff ,  Tongfei Wu ,  Sven Franciscus Anna Van Brandt ,  Michel Surkyn ,  Mirko Zaja ,  Serge Maria Aloysius Pieters ,  Didier Jean-Claude Berthelot ,  Michel Anna Jozef De Cleyn ,  Daniel Oehlrich

IPC分类号： A61K31/437 ,  C07D471/04 ,  C07D487/04 ,  C07D403/10 ,  C07D413/10

CPC分类号： C07D487/04 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04

摘要： The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

摘要翻译： 本发明涉及其中Het1，Het2，A1，A2，A3和A4具有权利要求中限定的含义的式（I）的取代双环杂环化合物。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：US08946266B2

公开(公告)日：2015-02-03

申请号：US13382659

申请日：2010-07-13

申请人： Tongfei Wu ,  Henricus Jacobus Maria Gijsen ,  Frederik Jan Rita Rombouts ,  François Paul Bischoff ,  Didier Jean-Claude Berthelot ,  Daniel Oehlrich ,  Michel Anna Jozef De Cleyn ,  Serge Maria Aloysius Pieters ,  Garrett Berlond Minne ,  Adriana Ingrid Velter′ ,  Sven Franciscus Anna Van Brandt ,  Michel Surkyn

发明人： Tongfei Wu ,  Henricus Jacobus Maria Gijsen ,  Frederik Jan Rita Rombouts ,  François Paul Bischoff ,  Didier Jean-Claude Berthelot ,  Daniel Oehlrich ,  Michel Anna Jozef De Cleyn ,  Serge Maria Aloysius Pieters ,  Garrett Berlond Minne ,  Adriana Ingrid Velter′ ,  Sven Franciscus Anna Van Brandt ,  Michel Surkyn

IPC分类号： A61K31/4439 ,  C07D401/14 ,  C07D233/60 ,  C07D403/10 ,  C07D405/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

CPC分类号： C07D233/60 ,  C07D401/14 ,  C07D403/10 ,  C07D405/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

摘要： The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

摘要翻译： 本发明涉及式（I）的新型取代三唑和咪唑衍生物，其中R1，R2，A1，A2，A3，A4，X和Het1具有权利要求中限定的含义。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：US20120135981A1

公开(公告)日：2012-05-31

申请号：US13382659

申请日：2010-07-13

申请人： Tongfei Wu ,  Henricus Jacobus Maria Gijsen ,  Frederik Jan Rita Rombouts ,  François Paul Bischoff ,  Didier Jean-Claude Berthelot ,  Daniel Oehlrich ,  Michel Anna Jozef De Cleyn ,  Serge Maria Aloysius Pieters ,  Garrett Berlond Minne ,  Adriana Ingrid Velter' ,  Sven Franciscus Anna Van Brandt ,  Michel Surkyn

发明人： Tongfei Wu ,  Henricus Jacobus Maria Gijsen ,  Frederik Jan Rita Rombouts ,  François Paul Bischoff ,  Didier Jean-Claude Berthelot ,  Daniel Oehlrich ,  Michel Anna Jozef De Cleyn ,  Serge Maria Aloysius Pieters ,  Garrett Berlond Minne ,  Adriana Ingrid Velter' ,  Sven Franciscus Anna Van Brandt ,  Michel Surkyn

IPC分类号： A61K31/553 ,  C07D403/10 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/4439 ,  A61K31/4196 ,  A61P25/28 ,  A61P25/00 ,  A61P25/16 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D405/14 ,  A61K31/437 ,  A61K31/55 ,  A61K31/519 ,  A61K31/4985 ,  A61K31/5383 ,  C07D401/14

CPC分类号： C07D233/60 ,  C07D401/14 ,  C07D403/10 ,  C07D405/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

摘要： The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

摘要翻译： 本发明涉及式（I）的新型取代三唑和咪唑衍生物，其中R1，R2，A1，A2，A3，A4，X和Het1具有权利要求中限定的含义。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：US20120295901A1

公开(公告)日：2012-11-22

申请号：US13522430

申请日：2011-01-12

申请人： Michel Anna Jozef De Cleyn ,  Sven Franciscus Anna Van Brandt ,  Henricus Jacobus Maria Gijsen ,  Didier Jean-Claude Berthelot ,  Daniel Oehlrich

发明人： Michel Anna Jozef De Cleyn ,  Sven Franciscus Anna Van Brandt ,  Henricus Jacobus Maria Gijsen ,  Didier Jean-Claude Berthelot ,  Daniel Oehlrich

IPC分类号： A61K31/444 ,  A61K31/437 ,  C07D487/04 ,  A61P25/16 ,  C07D498/04 ,  A61K31/5383 ,  A61P25/00 ,  A61P25/28 ,  C07D471/04 ,  A61K31/4985

CPC分类号： C07D403/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D413/04

摘要： The present invention is concerned with novel substituted bicyclic triazole derivatives of Formula (I) wherein Het1, R1, R2, A1, A2, A3, A4, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

摘要翻译： 本发明涉及式（I）的新型取代双环三唑衍生物，其中Het1，R1，R2，A1，A2，A3，A4，L1和L2具有权利要求中限定的含义。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：US20120295891A1

公开(公告)日：2012-11-22

申请号：US13522409

申请日：2011-01-12

申请人： Sven Franciscus Anna Van Brandt ,  Michel Anna Jozef De Cleyn ,  Henricus Jacobus Maria Gijsen ,  Didier Jean-Claude Berthelot ,  Michel Surkyn

发明人： Sven Franciscus Anna Van Brandt ,  Michel Anna Jozef De Cleyn ,  Henricus Jacobus Maria Gijsen ,  Didier Jean-Claude Berthelot ,  Michel Surkyn

IPC分类号： A61K31/4196 ,  C07D401/14 ,  A61K31/454 ,  A61P25/28 ,  A61K31/496 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/551 ,  C07D403/12 ,  C07D403/14

CPC分类号： C07D403/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D413/04

摘要： The present invention is concerned with novel substituted triazole derivatives of Formula (I) wherein Het1, R1, R2, A1, A2, A3, A4, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

摘要翻译： 本发明涉及式（I）的新型取代的三唑衍生物，其中Het1，R1，R2，A1，A2，A3，A4，L1和L2具有权利要求中限定的含义。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：US09145399B2

公开(公告)日：2015-09-29

申请号：US13522430

申请日：2011-01-12

申请人： Michel Anna Jozef De Cleyn ,  Sven Franciscus Anna Van Brandt ,  Henricus Jacobus Maria Gijsen ,  Didier Jean-Claude Berthelot ,  Daniel Oehlrich

发明人： Michel Anna Jozef De Cleyn ,  Sven Franciscus Anna Van Brandt ,  Henricus Jacobus Maria Gijsen ,  Didier Jean-Claude Berthelot ,  Daniel Oehlrich

IPC分类号： C07D498/04 ,  A61K31/5365 ,  C07D403/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D413/04

CPC分类号： C07D403/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D413/04

摘要： The present invention is concerned with novel substituted bicyclic triazole derivatives of Formula (I) wherein Het1, R1, R2, A1, A2, A3, A4, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

摘要翻译： 本发明涉及式（I）的新型取代双环三唑衍生物，其中Het1，R1，R2，A1，A2，A3，A4，L1和L2具有权利要求中限定的含义。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：US09079886B2

公开(公告)日：2015-07-14

申请号：US13522409

申请日：2011-01-12

申请人： Sven Franciscus Anna Van Brandt ,  Michel Anna Jozef De Cleyn ,  Henricus Jacobus Maria Gijsen ,  Didier Jean-Claude Berthelot ,  Michel Surkyn

发明人： Sven Franciscus Anna Van Brandt ,  Michel Anna Jozef De Cleyn ,  Henricus Jacobus Maria Gijsen ,  Didier Jean-Claude Berthelot ,  Michel Surkyn

IPC分类号： C07D401/10 ,  C07D401/14 ,  C07D401/12 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D403/14 ,  C07D403/10 ,  C07D403/12 ,  C07D413/04

CPC分类号： C07D403/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D413/04

摘要： The present invention is concerned with novel substituted triazole derivatives of Formula (I) wherein Het1, R1, R2, A1, A2, A3, A4, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

摘要翻译： 本发明涉及式（I）的新型取代的三唑衍生物，其中Het1，R1，R2，A1，A2，A3，A4，L1和L2具有权利要求中限定的含义。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。