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公开(公告)号:EP1921065B1
公开(公告)日:2010-10-20
申请号:EP06797001.2
申请日:2006-08-23
发明人: NAYA, Akira , SAKAMOTO, Toshihiro , HAGA, Yuji , OTAKE, Norikazu
IPC分类号: C07D213/64 , A61K31/4412 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/5377 , A61P1/00 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P7/08 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/12 , A61P15/06
CPC分类号: C07D213/69 , C07D213/64 , C07D401/10 , C07D413/10
摘要: A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents -CH2-O-, -CH=CH- or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.
摘要翻译: 含有由式(I)表示的化合物作为活性成分:其中R 1和R 2独立地表示氢原子,低级烷基等,或R 1与连接有L,Z 2和R 1的氮原子一起 可以形成脂肪族含氮杂环基,并且R 1和R 2与它们所连接的氮原子一起可以形成脂肪族含氮杂环基; X代表次甲基或氮原子; Y表示-CH 2 -O - , - CH = CH-等; Z1表示单键,C1-4亚烷基等; Z2表示单键或C1-4亚烷基; L表示亚甲基,C 3-8亚环烷基等; Ar表示芳族碳环基团等。 该化合物可用作中枢神经系统疾病,心血管疾病或代谢疾病的药物。
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公开(公告)号:EP1921065A1
公开(公告)日:2008-05-14
申请号:EP06797001.2
申请日:2006-08-23
发明人: NAYA, Akira , SAKAMOTO, Toshihiro , HAGA, Yuji , OTAKE, Norikazu
IPC分类号: C07D213/64 , A61K31/4412 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/5377 , A61P1/00 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P7/08 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/12 , A61P15/06
CPC分类号: C07D213/69 , C07D213/64 , C07D401/10 , C07D413/10
摘要: A compound represented by the formula (I) is contained as an active ingredient:
wherein R 1 and R 2 independently represent a hydrogen atom, a lower alkyl group or the like, or R 1 together with a nitrogen atom to which L, Z 2 and R 1 are attached may form an aliphatic nitrogenated heterocyclic group and R 1 and R 2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents -CH 2 -O-, -CH=CH- or the like; Z 1 represents a single bond, a C 1-4 alkylene group or the like; Z 2 represents a single bond or a C 1-4 alkylene group; L represents a methylene group, a C 3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.摘要翻译: 作为活性成分,含有式(I)表示的化合物:其中,R 1和R 2分别独立地表示氢原子,低级烷基等,或者R 1与氮原子一起,L,Z 2 R 1可以形成脂族氮杂环基,R 1和R 2与它们所连接的氮原子一起形成脂族氮杂环基; X表示次甲基或氮原子; Y表示-CH 2 -O-,-CH = CH-等; Z 1表示单键,C 1-4亚烷基等; Z 2表示单键或C 1-4亚烷基; L表示亚甲基,C 3-8亚环烷基等; Ar表示芳香族碳环基等。 该化合物可用作中枢神经系统疾病,心血管疾病或代谢疾病的药物。
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公开(公告)号:EP2303269A1
公开(公告)日:2011-04-06
申请号:EP09759077.2
申请日:2009-05-28
发明人: FURUYAMA, Hidetomo , GOTO, Yasuhiro , KAWANISHI, Nobuhiko , LAYTON, Mark, E. , MITA, Takashi , NAYA, Akira , OGINO, Yoshio , ONOZAKI, Yu , RODZINAK, Kevin, J. , SAKAMOTO, Toshihiro , SANDERSON, Philip, E. , WANG, Jiabing
CPC分类号: C07D471/14
摘要: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity especially Akt1 by administering the compound to a patient in need of treatment of cancer.
摘要翻译: 本发明提供了抑制Akt活性的取代的萘啶化合物。 具体而言,所公开的化合物选择性地抑制一种或两种Akt同种型,优选Akt1。 本发明还提供了包含此类抑制性化合物的组合物以及通过将该化合物给予需要治疗癌症的患者来抑制Akt活性,尤其是Akt1的方法。
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