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公开(公告)号：US09481646B2
公开(公告)日：2016-11-01
申请号：US12596252
申请日：2008-04-18
IPC分类号： C07C401/00 , C07D307/02 , C07D307/42
CPC分类号： C07C401/00 , C07C2601/14 , C07C2601/16 , C07C2602/24 , C07D307/42
摘要： The disclosure provides compounds, compositions and methods using these compounds and compositions to stimulate the differentiation of cells and inhibit excessive cell proliferation of certain cells, including cancer cells and skin cells, which may be useful in the treatment of diseases characterized by abnormal cell proliferation and/or cell differentiation such as leukemia, myelofibrosis and psoriasis without the well known effect on calcium metabolism, which gives rise to hypercalcemia.
摘要翻译： 本公开提供使用这些化合物和组合物刺激细胞分化并抑制某些细胞（包括癌细胞和皮肤细胞）的过度细胞增殖的化合物，组合物和方法，其可用于治疗以异常细胞增殖为特征的疾病， /或细胞分化例如白血病，骨髓纤维化和牛皮癣，而没有众所周知的对钙代谢的作用，其引起高钙血症。
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公开(公告)号：US20100137262A1
公开(公告)日：2010-06-03
申请号：US12596252
申请日：2008-04-18
IPC分类号： A61K31/59 , C07C401/00 , C07D307/02
CPC分类号： C07C401/00 , C07C2601/14 , C07C2601/16 , C07C2602/24 , C07D307/42
摘要： The disclosure provides compounds, compositions and methods using these compounds and compositions to stimulate the differentiation of cells and inhibit excessive cell proliferation of certain cells, including cancer cells and skin cells, which may be useful in the treatment of diseases characterized by abnormal cell proliferation and/or cell differentiation such as leukemia, myelofibrosis and psoriasis without the well known effect on calcium metabolism, which gives rise to hypercalcemia.
摘要翻译： 本公开提供使用这些化合物和组合物刺激细胞分化并抑制某些细胞（包括癌细胞和皮肤细胞）的过度细胞增殖的化合物，组合物和方法，其可用于治疗以异常细胞增殖为特征的疾病， /或细胞分化例如白血病，骨髓纤维化和牛皮癣，而没有众所周知的对钙代谢的作用，其引起高钙血症。
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公开(公告)号：US09775903B2
公开(公告)日：2017-10-03
申请号：US13521980
申请日：2011-01-13
申请人： Gary H. Posner , Lindsey C. Hess , Alvin S. Kalinda , Rachel D. Slack , Uttam Saha , P. Martin Petkovich
发明人： Gary H. Posner , Lindsey C. Hess , Alvin S. Kalinda , Rachel D. Slack , Uttam Saha , P. Martin Petkovich
IPC分类号： A61K45/06 , C07C401/00 , A61K31/593
CPC分类号： A61K45/06 , A61K31/593 , C07C401/00 , C07C2601/14 , C07C2602/24
摘要： This present disclosure is directed to novel prodrugs of activated vitamin D3 compounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases.
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公开(公告)号：US20130157987A1
公开(公告)日：2013-06-20
申请号：US13521980
申请日：2011-01-13
申请人： Gary H. Posner , Lindsey C. Hess , Alvin S. Kalinda , Rachel D. Slack , Uttam Saha , P. Martin Petkovich
发明人： Gary H. Posner , Lindsey C. Hess , Alvin S. Kalinda , Rachel D. Slack , Uttam Saha , P. Martin Petkovich
IPC分类号： A61K45/06 , A61K31/593 , C07C401/00
CPC分类号： A61K45/06 , A61K31/593 , C07C401/00 , C07C2601/14 , C07C2602/24
摘要： This present disclosure is directed to novel prodrugs of activated vitamin D3 compounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases.
摘要翻译： 本公开内容涉及活化的维生素D3化合物的新型前药。 前药可以被设计为具有一种或多种有益的性质，例如CYP24酶的选择性抑制，低钙血症活性和抗增殖活性。 具体来说，这些前药是活性维生素D类似物的1-脱氧激素。 骨化三醇的类似物。 本公开还涉及含有本发明前药的药物和诊断组合物及其医疗用途，特别是作为前药治疗和/或预防疾病。
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