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公开(公告)号：US20120028926A1
公开(公告)日：2012-02-02
申请号：US13146217
申请日：2010-01-26
IPC分类号： A61K31/675 , A61K31/663 , C07F9/58 , C07F9/553 , A61P13/12 , A61P5/18 , A61P19/08 , A61P9/00 , A61P19/10 , C07F9/38 , A61P3/00
CPC分类号： A61K31/66 , A61K31/662 , A61K31/663 , A61K31/675 , A61K45/06 , A61K2300/00
摘要： This invention relates to methods and small molecules having a phosphate group that can be used to inhibit phosphate transport and to treat or prevent diseases that are related to disorders in the maintenance of normal serum phosphate levels.
摘要翻译： 本发明涉及具有磷酸基团的方法和小分子，其可用于抑制磷酸盐转运并且治疗或预防与维持正常血清磷酸盐水平的疾病有关的疾病。
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公开(公告)号：US09198923B2
公开(公告)日：2015-12-01
申请号：US13146217
申请日：2010-01-26
IPC分类号： A61K31/66 , A61K31/662 , A61K31/663 , A61K31/675 , A61K45/06
CPC分类号： A61K31/66 , A61K31/662 , A61K31/663 , A61K31/675 , A61K45/06 , A61K2300/00
摘要： This invention relates to methods and small molecules having a phosphate group that can be used to inhibit phosphate transport and to treat or prevent diseases that are related to disorders in the maintenance of normal serum phosphate levels.
摘要翻译： 本发明涉及具有磷酸基团的方法和小分子，其可用于抑制磷酸盐转运并且治疗或预防与维持正常血清磷酸盐水平的疾病有关的疾病。
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公开(公告)号：US11752158B2
公开(公告)日：2023-09-12
申请号：US12597230
申请日：2008-04-25
IPC分类号： A61K31/592 , A61K31/593
CPC分类号： A61K31/592 , A61K31/593
摘要： The invention relates to methods and compositions for reducing toxicity associated with administration of vitamin D3, its 25-hydroxylated and 1-hydroxylated forms, and analogs thereof.
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公开(公告)号：US08962239B2
公开(公告)日：2015-02-24
申请号：US12935139
申请日：2009-04-02
CPC分类号： G01N33/82 , A61K31/00 , A61K31/59 , A61K31/592 , A61K31/593 , A61K45/06 , C12Q1/6876 , C12Q1/6883 , C12Q2600/106 , C12Q2600/158 , G01N33/6893 , G01N2333/50 , G01N2333/90251 , G01N2800/04 , G01N2800/046 , G01N2800/347
摘要： Methods for diagnosing, treating, and preventing catabolism-related vitamin D deficiency and related disorders, related compositions, apparatus and kits, are disclosed. A method involves measuring CYP24 expression and/or activity, or a proxy thereof such as FGF23 level, in a patient and correlating abnormally elevated CYP24 expression and/or activity with catabolism-related vitamin D deficiency or with susceptibility for catabolism-related vitamin D deficiency. In response to abnormally elevated CYP24 expression and/or activity, the method further includes administering a CYP24 inhibitor to the vitamin D deficient or at-risk patient, and preferably avoiding activation of the vitamin D binding receptor, such as by avoiding administration of active vitamin D compounds to such patients. Optionally, a vitamin D prohormone or prohormone can be administered.
摘要翻译： 公开了用于诊断，治疗和预防分解代谢相关的维生素D缺乏症和相关疾病的方法，相关组合物，装置和试剂盒。 一种方法包括测量患者中的CYP24表达和/或活性或其代谢如FGF23水平，并将与异常升高的CYP24表达和/或活性与分解代谢相关的维生素D缺乏或与分解代谢相关的维生素D缺乏的易感性相关联 。 响应于异常升高的CYP24表达和/或活性，该方法还包括向维生素D缺乏或危险患者施用CYP24抑制剂，并且优选地避免维生素D结合受体的活化，例如通过避免施用活性维生素 D化合物。 任选地，可以施用维生素D激素原或激素原。
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5.发明授权公开(公告)号：US08574862B2
公开(公告)日：2013-11-05
申请号：US13318442
申请日：2010-05-03
IPC分类号： G01N33/53
CPC分类号： C07K14/705 , C07K14/70567 , C07K2319/60 , G01N33/542 , G01N33/82 , G01N2333/70567 , G01N2800/347
摘要： Methods and compositions for measuring the amount of vitamin D derivatives are disclosed. Fluorescence Resonance Energy Transfer (FRET) in combination with a modified ligand-binding domain of the vitamin D receptor (LBD-VDR) to measure vitamin D derivatives are also disclosed.
摘要翻译： 公开了用于测量维生素D衍生物的量的方法和组合物。 还公开了荧光共振能量转移（FRET）与维生素D受体（LBD-VDR）的修饰的配体结合结构域结合以测量维生素D衍生物。
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6.发明申请公开(公告)号：US20120094396A1
公开(公告)日：2012-04-19
申请号：US13318442
申请日：2010-05-03
CPC分类号： C07K14/705 , C07K14/70567 , C07K2319/60 , G01N33/542 , G01N33/82 , G01N2333/70567 , G01N2800/347
摘要： Methods and compositions for measuring the amount of vitamin D derivatives are disclosed. Fluorescence Resonance Energy Transfer (FRET) in combination with a modified ligand-binding domain of the vitamin D receptor (LBD-VDR) to measure vitamin D derivatives are also disclosed.
摘要翻译： 公开了用于测量维生素D衍生物的量的方法和组合物。 还公开了荧光共振能量转移（FRET）与维生素D受体（LBD-VDR）的修饰的配体结合结构域结合以测量维生素D衍生物。
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公开(公告)号：US20100120728A1
公开(公告)日：2010-05-13
申请号：US12597230
申请日：2008-04-25
IPC分类号： A61K31/59
CPC分类号： A61K31/592 , A61K31/593
摘要： The invention relates to methods and compositions for reducing toxicity associated with administration of vitamin D3, its 25-hydroxylated and 1-hydroxylated forms, and analogs thereof.
摘要翻译： 本发明涉及用于降低与施用维生素D3，其25-羟基化和1-羟基化形式及其类似物相关的毒性的方法和组合物。
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8.发明申请Methods Compositions, Uses, and Kits Useful for Vitamin D Deficiency and Related Disorders 有权方法用于维生素D缺乏症和相关疾病的组合物，用途和试剂盒公开(公告)号：US20110052567A1
公开(公告)日：2011-03-03
申请号：US12935139
申请日：2009-04-02
IPC分类号： A61K39/395 , C12Q1/02 , A61K31/7088 , A61K31/713 , C12Q1/68 , C12Q1/26 , A61P13/12 , A61K38/02 , A61K31/496 , A61P35/00 , A61P5/18
CPC分类号： G01N33/82 , A61K31/00 , A61K31/59 , A61K31/592 , A61K31/593 , A61K45/06 , C12Q1/6876 , C12Q1/6883 , C12Q2600/106 , C12Q2600/158 , G01N33/6893 , G01N2333/50 , G01N2333/90251 , G01N2800/04 , G01N2800/046 , G01N2800/347
摘要： Methods for diagnosing, treating, and preventing catabolism-related vitamin D deficiency and related disorders; related compositions, apparatus and kits, are disclosed. A method involves measuring CYP24 expression and/or activity, or a proxy thereof such as FGF23 level, in a patient and correlating abnormally elevated CYP24 expression and/or activity with catabolism-related vitamin D deficiency or with susceptibility for catabolism-related vitamin D deficiency. In response to abnormally elevated CYP24 expression and/or activity, the method further includes administering a CYP24 inhibitor to the vitamin D deficient or at-risk patient, and preferably avoiding activation of the vitamin D binding receptor, such as by avoiding administration of active vitamin D compounds to such patients. Optionally, a vitamin D prohormone or prohormone can be administered.
摘要翻译： 诊断，治疗和预防分解代谢相关维生素D缺乏症及相关疾病的方法; 相关的组合物，装置和试剂盒。 一种方法包括测量患者中的CYP24表达和/或活性或其代谢如FGF23水平，并将与异常升高的CYP24表达和/或活性与分解代谢相关的维生素D缺乏或与分解代谢相关的维生素D缺乏的易感性相关联 。 响应于异常升高的CYP24表达和/或活性，所述方法还包括向维生素D缺乏或危险患者施用CYP24抑制剂，并且优选地避免维生素D结合受体的活化，例如通过避免施用活性维生素 D化合物。 任选地，可以施用维生素D激素原或激素原。
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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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