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公开(公告)号:US09145433B2
公开(公告)日:2015-09-29
申请号:US14046834
申请日:2013-10-04
申请人: Somasekhar Bhamidipati , Marina Gelman , Pingyu Ding , Rajinder Singh , Jeffrey Clough , Todd Kinsella , Donald Payan
发明人: Somasekhar Bhamidipati , Marina Gelman , Pingyu Ding , Rajinder Singh , Jeffrey Clough , Todd Kinsella , Donald Payan
IPC分类号: C07D513/04 , C07D405/04 , C07D487/04 , C07D401/04 , C07F9/6503 , C07D417/04 , C07D471/04 , C07D405/14 , C07D401/14 , C07D213/26 , C07D498/04 , C07D413/04 , C07D417/14 , C07D453/02
CPC分类号: C07D401/04 , C07D213/26 , C07D401/14 , C07D405/04 , C07D405/14 , C07D413/04 , C07D417/04 , C07D417/14 , C07D453/02 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04 , C07F9/65038
摘要: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.
摘要翻译: 描述了式(I)的GCF-8抑制剂及其药学上可接受的盐,其中n,R1,R2,R5,R6,X和Z如本文所定义。 还提供了包含其的药物组合物。 这样的化合物和组合物可用于抑制细胞中的GDF-8的方法和用于治疗患有疾病或病症的患者的方法,其中患者将从肌肉组织的质量或强度的增加中治疗获益。
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公开(公告)号:US20130012501A1
公开(公告)日:2013-01-10
申请号:US13610569
申请日:2012-09-11
申请人: Rajinder Singh , Andy Atuegbu , John Ramphal , Hui Li , Marina Gelman , Jeffrey Clough , Carlos Valdez , Somasekhar Bhamidipati , Sambaiah Thota , Darren McMurtrie
发明人: Rajinder Singh , Andy Atuegbu , John Ramphal , Hui Li , Marina Gelman , Jeffrey Clough , Carlos Valdez , Somasekhar Bhamidipati , Sambaiah Thota , Darren McMurtrie
IPC分类号: A61K31/538 , A61P35/00 , A61K31/5415
CPC分类号: A61K31/5383 , A61K45/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/08 , C07D498/04
摘要: Disclosed embodiments provide pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.
摘要翻译: 公开的实施方案提供了可用于抑制激酶活性的嘧啶二胺化合物,包括polo样激酶1(PLK1)的活性。 还公开了包含这些化合物的药物组合物和治疗与激酶活性相关的疾病的方法,特别是增强的PLK1催化活性,例如与异常细胞增殖相关的疾病,包括肿瘤性疾病。
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公开(公告)号:US20100179134A1
公开(公告)日:2010-07-15
申请号:US12649073
申请日:2009-12-29
申请人: Rajinder Singh , Andy Atuegbu , John Ramphal , Hui Li , Marina Gelman , Jeffrey Clough , Carlos Valdez , Somasekhar Bhamidipati , Sambaiah Thota , Darren McMurtrie
发明人: Rajinder Singh , Andy Atuegbu , John Ramphal , Hui Li , Marina Gelman , Jeffrey Clough , Carlos Valdez , Somasekhar Bhamidipati , Sambaiah Thota , Darren McMurtrie
IPC分类号: A61K31/5415 , C07D413/14 , A61K31/538 , C07D417/14 , A61P35/00
CPC分类号: A61K31/5383 , A61K45/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/08 , C07D498/04
摘要: The present invention provides pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also provided are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.
摘要翻译: 本发明提供了可用于抑制激酶活性的嘧啶二胺化合物,包括polo样激酶1(PLK1)的活性。 还提供了包含这些化合物的药物组合物和治疗与激酶活性相关的疾病的方法,特别是增强的PLK1催化活性,例如与异常细胞增殖相关的疾病,包括肿瘤性疾病。
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公开(公告)号:US08278299B2
公开(公告)日:2012-10-02
申请号:US12649073
申请日:2009-12-29
申请人: Rajinder Singh , Andy Atuegbu , John Ramphal , Hui Li , Marina Gelman , Jeffrey Clough , Carlos Valdez , Somasekhar Bhamidipati , Sambaiah Thota , Darren McMurtrie
发明人: Rajinder Singh , Andy Atuegbu , John Ramphal , Hui Li , Marina Gelman , Jeffrey Clough , Carlos Valdez , Somasekhar Bhamidipati , Sambaiah Thota , Darren McMurtrie
IPC分类号: C07D413/14 , C07D417/14 , A61K31/5415 , A61K31/538
CPC分类号: A61K31/5383 , A61K45/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/08 , C07D498/04
摘要: The present invention provides pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also provided are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.
摘要翻译: 本发明提供了可用于抑制激酶活性的嘧啶二胺化合物,包括polo样激酶1(PLK1)的活性。 还提供了包含这些化合物的药物组合物和治疗与激酶活性相关的疾病的方法,特别是增强的PLK1催化活性,例如与异常细胞增殖相关的疾病,包括肿瘤性疾病。
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公开(公告)号:US08518937B2
公开(公告)日:2013-08-27
申请号:US13610569
申请日:2012-09-11
申请人: Rajinder Singh , Andy Atuegbu , John Ramphal , Hui Li , Marina Gelman , Jeffrey Clough , Carlos Valdez , Somasekhar Bhamidipati , Sambaiah Thota , Darren McMurtrie
发明人: Rajinder Singh , Andy Atuegbu , John Ramphal , Hui Li , Marina Gelman , Jeffrey Clough , Carlos Valdez , Somasekhar Bhamidipati , Sambaiah Thota , Darren McMurtrie
IPC分类号: C07D498/04 , C07D413/04 , C07D413/14 , A61K31/5415 , A61K31/538
CPC分类号: A61K31/5383 , A61K45/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/08 , C07D498/04
摘要: Disclosed embodiments provide pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.
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6.
公开(公告)号:US20050003390A1
公开(公告)日:2005-01-06
申请号:US10789378
申请日:2004-02-26
申请人: Sergey Axenovich , Robert Stull , Marina Gelman , Kitty Chui , Dean Ng
发明人: Sergey Axenovich , Robert Stull , Marina Gelman , Kitty Chui , Dean Ng
IPC分类号: C12Q1/68 , G01N33/574
CPC分类号: G01N33/57419 , C12Q1/6886 , C12Q2600/158 , G01N2510/00
摘要: A method of identifying a compound that induces apoptosis is disclosed. The method includes identifying compounds that inhibit the expression and/or activity of a target. Also disclosed are methods for inducing apoptosis by inhibiting one of the targets. The invention further includes methods for the diagnosis of a tumor that include determining the level of at least one of the targets as a biomarker in a patient sample, the level of the biomarker being indicative of the presence of tumor cells.
摘要翻译: 公开了鉴定诱导细胞凋亡的化合物的方法。 该方法包括鉴定抑制靶标表达和/或活性的化合物。 还公开了通过抑制目标之一诱导细胞凋亡的方法。 本发明还包括用于诊断肿瘤的方法,所述方法包括确定至少一种靶标的水平作为患者样品中的生物标志物,所述生物标志物的水平指示肿瘤细胞的存在。
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