公开(公告)号：EP2140864A3

公开(公告)日：2010-01-27

申请号：EP09010003.3

申请日：2002-01-31

申请人： H. Lundbeck A/S

发明人： Blackburn, Thomas P. ,  Konkel, Michael ,  Boteju, Lakmal W. ,  Talisman, Ian Jamie ,  Wetzel, John M. ,  Packiarajan, Mathivanaan ,  Chen, Heidi ,  Jimenez, Hermo ,  Lagu, Bharat ,  Lim, Kitae ,  Noble, Stewart

IPC分类号： A61K31/407 ,  A61K31/506 ,  C07D209/40 ,  C07D239/50 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D417/12 ,  A61P25/24

CPC分类号： A61K31/407 ,  A61K31/00 ,  A61K31/506 ,  C07D209/40 ,  C07D239/47 ,  C07D239/48 ,  C07D239/50 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D413/04 ,  C07D413/06 ,  C07D417/12

摘要： This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist.

公开(公告)号：EP2140862A3

公开(公告)日：2010-02-17

申请号：EP09010004.1

申请日：2002-01-31

申请人： H. Lundbeck A/S

发明人： Blackburn, Thomas P. ,  Konkel, Michael ,  Boteju, Lakmal W. ,  Talisman, Ian Jamie ,  Wetzel, John M. ,  Packiarajan, Mathivanaan ,  Chen, Heidi ,  Jimenez, Hermo ,  Lagu, Bharat ,  Lim, Kitae ,  Noble, Stewart

IPC分类号： A61K31/00 ,  A61K31/407 ,  A61K31/506 ,  C07D209/40 ,  C07D239/50 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D417/12 ,  A61P25/24 ,  A61P25/22

CPC分类号： A61K31/407 ,  A61K31/00 ,  A61K31/506 ,  C07D209/40 ,  C07D239/47 ,  C07D239/48 ,  C07D239/50 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D413/04 ,  C07D413/06 ,  C07D417/12

摘要： This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist.

摘要翻译： 本发明涉及作为GAL3受体的选择性拮抗剂的嘧啶和吲哚酮衍生物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供了通过组合治疗有效量的本发明化合物和药学上可接受的载体制成的药物组合物。 本发明进一步提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。 本发明还提供治疗患有抑郁症和/或焦虑症的受试者的方法，其包括向受试者施用有效治疗受试者的抑郁症和/或焦虑的量的本发明化合物。 本发明还提供了治疗受试者中的抑郁症和/或焦虑症的方法，其包括给受试者施用包含药学上可接受的载体和治疗有效量的GAL3受体拮抗剂的组合物。

公开(公告)号：EP2140864A2

公开(公告)日：2010-01-06

申请号：EP09010003.3

申请日：2002-01-31

申请人： H. Lundbeck A/S

发明人： Blackburn, Thomas P. ,  Konkel, Michael ,  Boteju, Lakmal W. ,  Talisman, Ian Jamie ,  Wetzel, John M. ,  Packiarajan, Mathivanaan ,  Chen, Heidi ,  Jimenez, Hermo ,  Lagu, Bharat ,  Lim, Kitae ,  Noble, Stewart

IPC分类号： A61K31/407 ,  A61K31/506 ,  C07D209/40 ,  C07D239/50 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D417/12 ,  A61P25/24

CPC分类号： A61K31/407 ,  A61K31/00 ,  A61K31/506 ,  C07D209/40 ,  C07D239/47 ,  C07D239/48 ,  C07D239/50 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D413/04 ,  C07D413/06 ,  C07D417/12

摘要： This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist.

摘要翻译： 本发明涉及嘧啶衍生物和吲哚酮其对于GAL3受体选择性拮抗剂。 本发明提供一种药物组合物，其包含治疗有效量的本发明和药学上可接受的载体的化合物。 所以本发明提供了通过组合治疗有效量的本发明和药学上可接受的载体的化合物制备的药物组合物。 本发明还提供制备包含将治疗有效量的本发明和药学上可接受的载体的化合物的药物组合物的方法。 本发明因此提供了治疗抑郁症和/或焦虑，包括给予受试者发明有效治疗其抑郁症和/或焦虑的化合物的量的受试者的方法。 本发明因此提供了在该方法包括施用给所述受试者的组合物，其包含药学上可接受的载体和GAL3受体拮抗剂的治疗有效量的受试者中治疗抑郁症和/或焦虑的方法。

公开(公告)号：EP2140862A2

公开(公告)日：2010-01-06

申请号：EP09010004.1

申请日：2002-01-31

申请人： H. Lundbeck A/S

发明人： Blackburn, Thomas P. ,  Konkel, Michael ,  Boteju, Lakmal W. ,  Talisman, Ian Jamie ,  Wetzel, John M. ,  Packiarajan, Mathivanaan ,  Chen, Heidi ,  Jimenez, Hermo ,  Lagu, Bharat ,  Lim, Kitae ,  Noble, Stewart

IPC分类号： A61K31/00 ,  A61K31/407 ,  A61K31/506 ,  C07D209/40 ,  C07D239/50 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D417/12 ,  A61P25/24 ,  A61P25/22

CPC分类号： A61K31/407 ,  A61K31/00 ,  A61K31/506 ,  C07D209/40 ,  C07D239/47 ,  C07D239/48 ,  C07D239/50 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D413/04 ,  C07D413/06 ,  C07D417/12

摘要： This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist.

摘要翻译： 本发明涉及嘧啶衍生物和吲哚酮其对于GAL3受体选择性拮抗剂。 本发明提供一种药物组合物，其包含治疗有效量的本发明和药学上可接受的载体的化合物。 所以本发明提供了通过组合治疗有效量的本发明和药学上可接受的载体的化合物制备的药物组合物。 本发明还提供制备包含将治疗有效量的本发明和药学上可接受的载体的化合物的药物组合物的方法。 本发明因此提供了治疗抑郁症和/或焦虑，包括给予受试者发明有效治疗其抑郁症和/或焦虑的化合物的量的受试者的方法。 本发明因此提供了在该方法包括施用给所述受试者的组合物，其包含药学上可接受的载体和GAL3受体拮抗剂的治疗有效量的受试者中治疗抑郁症和/或焦虑的方法。