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1.发明公开1.ALPHA.-HYDROXY-2-(3'-HYDROXYPROPYLIDENE)-19-NOR-VITAMIN D COMPOUNDS AND METHODS OF MAKING AND USE THEREOF 审中-公开1.ALPHA.羟基-2-（3'-羟基亚）-19-NOR的维生素D化合物和方法的生产和使用
公开(公告)号：EP2010483A2
公开(公告)日：2009-01-07
申请号：EP07754958.2
申请日：2007-04-05
发明人： SICINSKI, Rafal R. , CLAGETT-DAME, Margaret , DELUCA, Hector F. , PLUM, Lora A. , GLEBOCKA, Agnieszka
IPC分类号： C07C401/00 , A61K31/59 , A61P35/00 , A61P3/02
CPC分类号： C07C401/00 , C07C45/29 , C07C2602/24 , C07C49/443
摘要： Disclosed are 1α-hydroxy-2-(3'-hydroxypropylidene)-19-nor- vitamin D compounds, pharmaceutical compositions, and methods of making and treatment thereof. The compounds are generally directed to biologically active 2-alkylidene-19-nor-vitamin D compounds and analogs thereof characterized by the presence of a 3'-hydroxypropylidene moiety at C-2 and the presence of an abbreviated alkyl side-chain free of any hydroxyl moiety.
摘要翻译： 本发明公开了1α羟基-2-（3'-羟基亚）-19-去甲维生素D化合物，药物组合物，以及制备和它们的治疗方法。 这些化合物基因反弹涉及不含任何生物活性2-亚烷基-19-降 - 维生素D化合物及其类似物在C-2通过一个3“羟基亚部分的存在及其特点和缩写的烷基侧链的存在 羟基基团。
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2.发明公开
公开(公告)号：EP3331533A1
公开(公告)日：2018-06-13
申请号：EP16747962.5
申请日：2016-07-26
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C35/21 , A61K31/59 , A61K31/593 , C07C401/00 , C07C2601/14 , C07C2602/24 , C07F7/1804
摘要： Disclosed are 2-methylene analogs of vitamin D3 and related compounds, their biological activities, and various pharmaceutical uses for these analogs. Particularly disclosed are 1α-hydroxy-2-methylene-vitamin D3, (20S)-1α-hydroxy-2-methylene-vitamin D3, and (5E)-1α,25-dihydroxy-2-methylene-vitamin D3, their biological activities, and various pharmaceutical uses for these compounds including methods of treating and/or preventing bone diseases and disorders.
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公开(公告)号：EP1656157B1
公开(公告)日：2011-12-21
申请号：EP04781584.0
申请日：2004-08-18
IPC分类号： A61K31/592 , C07C401/00 , A61P35/00
CPC分类号： A61K31/59 , C07C401/00
摘要： 2-Methylene-19-nor-24(S) and 24(R) derivatives of 1a,25-dihydroxyvitamin D2 are disclosed. These compounds are characterized by minimal bone calcium mobilization activity and relatively high intestinal calcium transport activity. This results in novel therapeutic agents for the treatment of diseases such as renal osteodystrophy, autoimmune diseases, and osteoporosis. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as anticancer agents and for use treating skin diseases such as psoriasis.
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公开(公告)号：EP1656157A1
公开(公告)日：2006-05-17
申请号：EP04781584.0
申请日：2004-08-18
CPC分类号： A61K31/59 , C07C401/00
摘要： 2-Methylene-19-nor-24(S) and 24(R) derivatives of 1a,25-dihydroxyvitamin D2 are disclosed. These compounds are characterized by minimal bone calcium mobilization activity and relatively high intestinal calcium transport activity. This results in novel therapeutic agents for the treatment of diseases such as renal osteodystrophy, autoimmune diseases, and osteoporosis. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as anticancer agents and for use treating skin diseases such as psoriasis.
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