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公开(公告)号：US20090312379A1
公开(公告)日：2009-12-17
申请号：US12509190
申请日：2009-07-24
申请人： Patrick G. Harran , Xiaodong Wang , Jef D. De Brabander , Lin Li , Ranny Mathew Thomas , Hidetaka Suzuki
发明人： Patrick G. Harran , Xiaodong Wang , Jef D. De Brabander , Lin Li , Ranny Mathew Thomas , Hidetaka Suzuki
IPC分类号： A61K31/422 , C07D417/14 , C12N5/00 , C07D403/14 , A61K31/41 , A61K31/4192 , A61P35/00
CPC分类号： C07D413/14 , A61K31/41 , A61K31/422 , C07D207/08 , C07D401/10 , C07D403/10 , C07D403/14 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10 , C07D417/14 , C07D495/04 , C07K5/06026 , C07K5/06034
摘要： Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
摘要翻译： 使用通式M1-L-M2的活性二聚体Smac肽模拟物促进胱天蛋白酶活性和凋亡，其中部分M1和M2是单体Smac模拟物，L是共价连接体。 靶向癌性或炎性细胞与有效量的活性二聚体Smac模拟物接触，并且检测到靶细胞凋亡的最终增加。 接触步骤可以通过给予包含治疗有效量的复合模拟物的药物组合物来实现，其中个体可以同时或先前放射或化疗用于治疗新生血管病变。
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公开(公告)号：US07884211B2
公开(公告)日：2011-02-08
申请号：US12509218
申请日：2009-07-24
申请人： Patrick G. Harran , Xiaodong Wang , Jef K. De Brabander , Lin Li , Ranny Mathew Thomas , Hidetaka Suzuki
发明人： Patrick G. Harran , Xiaodong Wang , Jef K. De Brabander , Lin Li , Ranny Mathew Thomas , Hidetaka Suzuki
IPC分类号： C07D249/04 , A61K31/42
CPC分类号： C07D413/14 , A61K31/41 , A61K31/422 , C07D207/08 , C07D401/10 , C07D403/10 , C07D403/14 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10 , C07D417/14 , C07D495/04 , C07K5/06026 , C07K5/06034
摘要： Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
摘要翻译： 使用通式M1-L-M2的活性二聚体Smac肽模拟物促进胱天蛋白酶活性和凋亡，其中部分M1和M2是单体Smac模拟物，L是共价连接体。 靶向癌性或炎性细胞与有效量的活性二聚体Smac模拟物接触，并且检测到靶细胞凋亡的最终增加。 接触步骤可以通过给予包含治疗有效量的复合模拟物的药物组合物来实现，其中个体可以同时或先前放射或化疗用于治疗新生血管病变。
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公开(公告)号：US07638544B2
公开(公告)日：2009-12-29
申请号：US11958365
申请日：2007-12-17
申请人： Patrick G. Harran , Xiaodong Wang , Jef K. De Brabander , Lin Li , Ranny Mathew Thomas , Hidetaka Suzuki
发明人： Patrick G. Harran , Xiaodong Wang , Jef K. De Brabander , Lin Li , Ranny Mathew Thomas , Hidetaka Suzuki
IPC分类号： A61K31/42
CPC分类号： C07D413/14 , A61K31/41 , A61K31/422 , C07D207/08 , C07D401/10 , C07D403/10 , C07D403/14 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10 , C07D417/14 , C07D495/04 , C07K5/06026 , C07K5/06034
摘要： Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of the dimeric mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
摘要翻译： 使用通式M1-L-M2的活性二聚体Smac肽模拟物促进胱天蛋白酶活性和凋亡，其中部分M1和M2是单体Smac模拟物，L是共价连接体。 靶向癌性或炎性细胞与有效量的活性二聚体Smac模拟物接触，并且检测到靶细胞凋亡的最终增加。 接触步骤可以通过给包含治疗有效量的二聚模拟物的药物组合物施用，其中个体可以同时或先前放射或化学治疗用于治疗新生血管病变。
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公开(公告)号：US08143418B2
公开(公告)日：2012-03-27
申请号：US13022033
申请日：2011-02-07
申请人： Patrick G. Harran , Xiaodong Wang , Jef K. De Brabander , Lin Li , Ranny Mathew Thomas , Hidetaka Suzuki
发明人： Patrick G. Harran , Xiaodong Wang , Jef K. De Brabander , Lin Li , Ranny Mathew Thomas , Hidetaka Suzuki
IPC分类号： C07D249/04 , A61K31/42
CPC分类号： C07D413/14 , A61K31/41 , A61K31/422 , C07D207/08 , C07D401/10 , C07D403/10 , C07D403/14 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10 , C07D417/14 , C07D495/04 , C07K5/06026 , C07K5/06034
摘要： Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
摘要翻译： 使用通式M1-L-M2的活性二聚体Smac肽模拟物促进胱天蛋白酶活性和凋亡，其中部分M1和M2是单体Smac模拟物，L是共价连接体。 靶向癌性或炎性细胞与有效量的活性二聚体Smac模拟物接触，并且检测到靶细胞凋亡的最终增加。 接触步骤可以通过给予包含治疗有效量的复合模拟物的药物组合物来实现，其中个体可以同时或先前放射或化疗用于治疗新生血管病变。
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公开(公告)号：US20110124585A1
公开(公告)日：2011-05-26
申请号：US13022033
申请日：2011-02-07
申请人： Patrick G. Harran , Xiaodong Wang , Jef K. De Brabander , Lin Li , Ranny Mathew Thomas , Hidetaka Suzuki
发明人： Patrick G. Harran , Xiaodong Wang , Jef K. De Brabander , Lin Li , Ranny Mathew Thomas , Hidetaka Suzuki
IPC分类号： A61K38/05 , C07D403/14 , C07D413/14 , A61P35/00 , A61P29/00
CPC分类号： C07D413/14 , A61K31/41 , A61K31/422 , C07D207/08 , C07D401/10 , C07D403/10 , C07D403/14 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10 , C07D417/14 , C07D495/04 , C07K5/06026 , C07K5/06034
摘要： Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
摘要翻译： 使用通式M1-L-M2的活性二聚体Smac肽模拟物促进胱天蛋白酶活性和凋亡，其中部分M1和M2是单体Smac模拟物，L是共价连接体。 靶向癌性或炎性细胞与有效量的活性二聚体Smac模拟物接触，并且检测到靶细胞凋亡的最终增加。 接触步骤可以通过给予包含治疗有效量的复合模拟物的药物组合物来实现，其中个体可以同时或先前放射或化疗用于治疗新生血管病变。
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公开(公告)号：US07816538B2
公开(公告)日：2010-10-19
申请号：US12509190
申请日：2009-07-24
申请人： Patrick G. Harran , Xiaodong Wang , Jef K. De Brabander , Lin Li , Ranny Mathew Thomas , Hidetaka Suzuki
发明人： Patrick G. Harran , Xiaodong Wang , Jef K. De Brabander , Lin Li , Ranny Mathew Thomas , Hidetaka Suzuki
IPC分类号： C07D249/04 , C07D257/04 , A61K31/41 , A61K31/42
CPC分类号： C07D413/14 , A61K31/41 , A61K31/422 , C07D207/08 , C07D401/10 , C07D403/10 , C07D403/14 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10 , C07D417/14 , C07D495/04 , C07K5/06026 , C07K5/06034
摘要： Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
摘要翻译： 使用通式M1-L-M2的活性二聚体Smac肽模拟物促进胱天蛋白酶活性和凋亡，其中部分M1和M2是单体Smac模拟物，L是共价连接体。 靶向癌性或炎性细胞与有效量的活性二聚体Smac模拟物接触，并且检测到靶细胞凋亡的最终增加。 接触步骤可以通过给予包含治疗有效量的复合模拟物的药物组合物来实现，其中个体可以同时或先前放射或化疗用于治疗新生血管病变。
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公开(公告)号：US20090281155A1
公开(公告)日：2009-11-12
申请号：US12509218
申请日：2009-07-24
申请人： Patrick G. Harran , Xiaodong Wang , Jef K. De Brabander , Lin Li , Ranny Mathew Thomas , Hidetaka Suzuki
发明人： Patrick G. Harran , Xiaodong Wang , Jef K. De Brabander , Lin Li , Ranny Mathew Thomas , Hidetaka Suzuki
IPC分类号： A61K31/421 , C07D257/04 , A61K31/41 , C07D263/08 , C12Q1/02 , A61P35/00 , A61P37/06
CPC分类号： C07D413/14 , A61K31/41 , A61K31/422 , C07D207/08 , C07D401/10 , C07D403/10 , C07D403/14 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10 , C07D417/14 , C07D495/04 , C07K5/06026 , C07K5/06034
摘要： Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
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公开(公告)号：US07309792B2
公开(公告)日：2007-12-18
申请号：US11070733
申请日：2005-03-01
申请人： Patrick G. Harran , Xiaodong Wang , Jef K. De Brabander , Lin Li , Ranny Mathew Thomas , Hidetaka Suzuki
发明人： Patrick G. Harran , Xiaodong Wang , Jef K. De Brabander , Lin Li , Ranny Mathew Thomas , Hidetaka Suzuki
IPC分类号： C07D249/04 , C07D257/04 , A61K31/41 , A61K31/42
CPC分类号： C07D413/14 , A61K31/41 , A61K31/422 , C07D207/08 , C07D401/10 , C07D403/10 , C07D403/14 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10 , C07D417/14 , C07D495/04 , C07K5/06026 , C07K5/06034
摘要： Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of the dimeric mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
摘要翻译： 使用通式M1-L-M2的活性二聚体Smac肽模拟物促进胱天蛋白酶活性和凋亡，其中部分M1和M2是单体Smac模拟物，L是共价连接体。 靶向癌性或炎性细胞与有效量的活性二聚体Smac模拟物接触，并且检测到靶细胞凋亡的最终增加。 接触步骤可以通过给包含治疗有效量的二聚模拟物的药物组合物施用，其中个体可以同时或先前放射或化学治疗用于治疗新生血管病变。
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