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公开(公告)号：EP0387077B1
公开(公告)日：1994-01-19
申请号：EP90302521.1
申请日：1990-03-09
发明人： DeLuca, Hector F. , Schnoes, Heinrich K. , Perlman, Kato L. , Sicinski, Rafal R. , Prahl, Jean Martin
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00
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公开(公告)号：EP0624573B1
公开(公告)日：1997-10-15
申请号：EP94303389.4
申请日：1994-05-11
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00
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3.发明公开Iodo vitamin D3 compounds and method for preparing same 失效Iodvitamin-D-Verbindungen und Verfahren zu ihrer Herstellung。
公开(公告)号：EP0624573A1
公开(公告)日：1994-11-17
申请号：EP94303389.4
申请日：1994-05-11
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00
摘要： Biologically active 1α-hydroxy-22-iodinated vitamin D₃ compounds and a process for the preparation of 1α-hydroxy-22-iodinated vitamin D₃ compounds are disclosed. The 22-iodo-vitamin D₃ compounds show relatively high binding affinity for the vitamin D receptor demonstrating their potential for high in vivo biological activity. Further, these compounds induce relatively high differentiation of malignant cells. Also, these 22-iodo compounds show high in vivo calcium transport activity with little or no bone calcium mobilization activity. These compounds thus show promise in the treatment of osteoporosis.
摘要翻译： 公开了生物活性的1α-羟基-22-碘化维生素D3化合物和1α-羟基-22-碘化维生素D3化合物的制备方法。 22维碘维生素D3化合物对维生素D受体的结合亲和力显示出较高的体内生物活性。 此外，这些化合物诱导恶性细胞的相对高的分化。 此外，这些22-碘化合物显示高体内钙转运活性，很少或没有骨钙动员活性。 因此，这些化合物在治疗骨质疏松症方面显示出希望。
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公开(公告)号：EP0387077A1
公开(公告)日：1990-09-12
申请号：EP90302521.1
申请日：1990-03-09
发明人： DeLuca, Hector F. , Schnoes, Heinrich K. , Perlman, Kato L. , Sicinski, Rafal R. , Prahl, Jean Martin
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00
摘要： This invention provides a novel class of vitamin D-related compounds, namely the 1α-hydroxy-19-nor-vitamin D analogs, as well as a general method for their chemical synthesis. The compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells, including malignant cells, and in inducing their differentiation, and thus represent novel therapeutic agents for the treatment of malignant and other diseases characterized by the proliferative grointh of undifferentiated cells. Formulations for therapeutic use and treatment methods are also provided.
摘要翻译： 本发明提供了一类维生素D相关化合物，即1α-羟基-19-去甲维生素D类似物，以及它们的化学合成的一般方法。 该化合物在阻止未分化细胞（包括恶性细胞）的增殖以及诱导其分化中表现出显着的活性，因此代表治疗以未分化细胞增殖性生长为特征的恶性和其它疾病的新型治疗剂。 还提供了治疗用途和治疗方法的制剂。
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公开(公告)号：EP1524264A3
公开(公告)日：2010-01-20
申请号：EP05001268.1
申请日：2001-05-31
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00
摘要： Biologically active 19-nor vitamin D analogs substituted at C-2 in the A-ring with an ethylidene group. These compounds have preferential activity on mobilising calcium from bone and either high or normal intestinal calcium transport activity which allows their in vivo administration for the treatment of metabolic bone diseases where bone loss is a major concern. These compounds are also characterised by high cell differentiation activity.
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公开(公告)号：EP1524264A2
公开(公告)日：2005-04-20
申请号：EP05001268.1
申请日：2001-05-31
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00
摘要： Biologically active 19-nor vitamin D analogs substituted at C-2 in the A-ring with an ethylidene group. These compounds have preferential activity on mobilising calcium from bone and either high or normal intestinal calcium transport activity which allows their in vivo administration for the treatment of metabolic bone diseases where bone loss is a major concern. These compounds are also characterised by high cell differentiation activity.
摘要翻译： 生物活性的19-或维生素D类似物在A环中被亚乙基取代为C-2。 这些化合物具有从骨骼中移动钙以及高或正常的钙运输活性的优先活性，其允许其体内施用以治疗骨质流失是主要关注的代谢性骨疾病。 这些化合物的特征还在于高细胞分化活性。
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