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公开(公告)号:US20090069334A1
公开(公告)日:2009-03-12
申请号:US12228559
申请日:2008-08-13
申请人: Julius Rebek, JR. , Shannon Biros , Lionel Moisan , Alessandro Volonterio , Enrique Mann , Trevor Dale
发明人: Julius Rebek, JR. , Shannon Biros , Lionel Moisan , Alessandro Volonterio , Enrique Mann , Trevor Dale
IPC分类号: A61K31/501 , C07D403/14 , A61P43/00
CPC分类号: C07D401/14 , C07D403/14 , C07D413/04 , C07D413/14
摘要: The synthesis of new α-helix scaffolds mimicking i, i+3 or i+4, i+7 residues, was accomplished. The common pyridazine heterocycle originates from the easily available building block, 6. These scaffolds may be thought of as synthetic counterparts of amphiphilic α-helices having a “wet face” along one side and a hydrophobic face along the other side of the helix.
摘要翻译: 完成了模拟i,i + 3或i + 4,i + 7残基的新的α-螺旋支架的合成。 常见的哒嗪杂环来自容易获得的构建块6.这些支架可以被认为是具有沿着一侧具有“湿面”和沿着螺旋另一侧的疏水面的两亲性α-螺旋的合成对应物。
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公开(公告)号:US20090197895A1
公开(公告)日:2009-08-06
申请号:US12362934
申请日:2009-01-30
IPC分类号: A61K31/496 , C07D413/14 , C40B40/04
CPC分类号: C07D413/04 , C07D413/14
摘要: Amphiphilic α-helix mimetics are provided. These compounds are constructed using an oxazole-pyrrole-piperazine (OPP) scaffold. The amphiphilic α-helix mimetics are also employable for making libraries and for treating diseases or conditions effected by the inhibition or disruption of interactions with the alpha helix of a protein.
摘要翻译: 提供两亲性α-螺旋模拟物。 这些化合物使用恶唑 - 吡咯 - 哌嗪(OPP)支架构建。 两亲性α-螺旋模拟物也可用于制备文库和用于治疗通过抑制或破坏与蛋白质的α螺旋相互作用而产生的疾病或病症。
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公开(公告)号:US20090298835A1
公开(公告)日:2009-12-03
申请号:US12503589
申请日:2009-07-15
申请人: Julius Rebek, JR. , Shen Gu , Shannon Biros
发明人: Julius Rebek, JR. , Shen Gu , Shannon Biros
IPC分类号: A61K31/501 , A61K31/50 , C07K1/107 , C07D237/06 , C07D403/14
CPC分类号: C07D237/24 , C07D237/08 , C07D257/08 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/04
摘要: Functionalized pyridazine derivatives having a low molecular weight and pharmaceutical compositions thereof are useful as alpha-helix mimetics and for treating conditions and/or disorders mediated by alpha-helix-binding receptors and proteins.
摘要翻译: 具有低分子量的官能化哒嗪衍生物及其药物组合物可用作α-螺旋模拟物和用于治疗由α-螺旋结合受体和蛋白质介导的病症和/或病症。
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公开(公告)号:US07579350B2
公开(公告)日:2009-08-25
申请号:US11368302
申请日:2006-03-03
申请人: Julius Rebek, Jr. , Shen Gu , Shannon Biros
发明人: Julius Rebek, Jr. , Shen Gu , Shannon Biros
IPC分类号: C07D403/14 , C07D413/14 , A61K31/501
CPC分类号: C07D237/24 , C07D237/08 , C07D257/08 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/04
摘要: Functionalized pyridazine derivatives having a low molecular weight and pharmaceutical compositions thereof are useful as alpha-helix mimetics and for treating conditions and/or disorders mediated by alpha-helix-binding receptors and proteins.
摘要翻译: 具有低分子量的官能化哒嗪衍生物及其药物组合物可用作α-螺旋模拟物和用于治疗由α-螺旋结合受体和蛋白质介导的病症和/或病症。
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公开(公告)号:US20060205728A1
公开(公告)日:2006-09-14
申请号:US11368302
申请日:2006-03-03
申请人: Julius Rebek , Shen Gu , Shannon Biros
发明人: Julius Rebek , Shen Gu , Shannon Biros
IPC分类号: A61K31/501 , C07D403/14 , C07D413/14
CPC分类号: C07D237/24 , C07D237/08 , C07D257/08 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/04
摘要: Functionalized pyridazine derivatives having a low molecular weight and pharmaceutical compositions thereof are useful as alpha-helix mimetics and for treating conditions and/or disorders mediated by alpha-helix-binding receptors and proteins.
摘要翻译: 具有低分子量的官能化哒嗪衍生物及其药物组合物可用作α-螺旋模拟物和用于治疗由α-螺旋结合受体和蛋白质介导的病症和/或病症。
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