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1. 发明授权

US06359152B2 18-substituted-19-nor-vitamin D compounds 失效
标题翻译： 18-取代的19-维生素D化合物
公开(公告)号：US06359152B2
公开(公告)日：2002-03-19
申请号：US09855859
申请日：2001-05-15
申请人： Hector F. DeLuca , Zu Y. Cai
发明人： Hector F. DeLuca , Zu Y. Cai
IPC分类号： A61K31593
CPC分类号： C07C401/00 , Y02P20/55
摘要： This invention provides a novel class of vitamin D compounds, namely, 13-ethyl and 13-vinyl-18,19-dinor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have the formula: where Y1 and Y2, which may be the same or different, are each selected from the group consisting of hydrogen and a hydroxy-protecting group, R6 is selected from the group consisting of an ethyl or vinyl radical, and where the group R represents any of the typical side chains known for vitamin D type compounds. These 18-substituted compounds are characterized by minimal intestinal calcium transport activity and minimal bone calcium mobilization activity resulting in novel therapeutic agents for the treatment of secondary hyperparathyroidism. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as anti-cancer agents and for the treatment of diseases such as psoriasis.
摘要翻译：本发明提供了一类新颖的维生素D化合物，即13-乙基和13-乙烯基-18,19-二 - 维生素D衍生物，以及它们化学合成的一般方法。化合物具有下式：其中Y1和Y2可以相同或不同，各自选自氢和羟基保护基，R6选自乙基或乙烯基，和其中基团R表示维生素D型化合物已知的任何典型侧链。这些18-取代的化合物的特征在于肠内钙转运活性最小，骨钙移动活性最小，导致用于治疗继发性甲状旁腺功能亢进的新型治疗剂。这些化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面也表现出显着的活性，因此证明其用作抗癌剂并用于治疗诸如牛皮癣的疾病。

2. 发明授权

US06281249B1 18-substituted-19-nor-vitamin D compounds 失效
标题翻译： 18-取代的19-维生素D化合物
公开(公告)号：US06281249B1
公开(公告)日：2001-08-28
申请号：US09353866
申请日：1999-07-15
申请人： Hector F. DeLuca , Zu Y. Cai
发明人： Hector F. DeLuca , Zu Y. Cai
IPC分类号： G07C40100
CPC分类号： C07C401/00 , Y02P20/55
摘要： This invention provides a novel class of vitamin D compounds, namely, 13-ethyl and 13-vinyl-18,19-dinor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have the formula: where Y1 and Y2, which may be the same or different, are each selected from the group consisting of hydrogen and a hydroxy-protecting group, R6 is selected from the group consisting of an ethyl or vinyl radical, and where the group R represents any of the typical side chains known for vitamin D type compounds. These 18-substituted compounds are characterized by minimal intestinal calcium transport activity and minimal bone calcium mobilization activity resulting in novel therapeutic agents for the treatment of secondary hyperparathyroidism. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as anti-cancer agents and for the treatment of diseases such as psoriasis.
摘要翻译：本发明提供了一类新颖的维生素D化合物，即13-乙基和13-乙烯基-18,19-二 - 维生素D衍生物，以及它们化学合成的一般方法。化合物具有下式：其中Y1和Y2可以相同或不同，各自选自氢和羟基保护基，R6选自乙基或乙烯基，和其中基团R表示维生素D型化合物已知的任何典型侧链。这些18-取代的化合物的特征在于肠内钙转运活性最小，骨钙移动活性最小，导致用于治疗继发性甲状旁腺功能亢进的新型治疗剂。这些化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面也表现出显着的活性，因此证明其用作抗癌剂并用于治疗诸如牛皮癣的疾病。

3. 发明授权

US5976784A Calcitriol derivatives and their uses 失效
标题翻译：骨化三醇衍生物及其用途
公开(公告)号：US5976784A
公开(公告)日：1999-11-02
申请号：US43509
申请日：1998-05-22
申请人： Hector F. DeLuca , Heinrich K. Schnoes , Zu Y. Cai , Mary E. Phelps , Connie M. Smith
发明人： Hector F. DeLuca , Heinrich K. Schnoes , Zu Y. Cai , Mary E. Phelps , Connie M. Smith
IPC分类号： G01N33/68 , C12Q1/00 , A01N45/00
CPC分类号： G01N33/6893 , G01N2800/02
摘要： A method of treating metabolic bone diseases such as osteoporosis, as well as other disease states treatable with vitamin D compounds, comprises administering an effective amount of one or more modified vitamin D compound. The modified compound contains a typical vitamin D nucleus but with in vivo hydrolyzable groups at one or more of the 1, 3 and 25 carbon positions. The time of conversion of the modified compound to its active form, such as calcitriol, can be regulated to thus provide controlled release of the compound in vivo over time, by changing or modifying the hydrolyzable groups.
摘要翻译： PCT No.PCT / US96 / 15184 Sec。 371日期：1998年5月22日 102（e）日期1998年5月22日PCT提交1996年9月20日PCT公布。公开号WO97 / 11053 日期1997年3月27日一种治疗代谢骨疾病如骨质疏松症以及用维生素D化合物治疗的其他疾病状态的方法包括施用有效量的一种或多种改性维生素D化合物。修饰的化合物含有典型的维生素D核，但在1，3和25个碳位置中的一个或多个处具有体内可水解基团。可以调节修饰化合物转化为活性形式如骨化三醇的时间，从而通过改变或改变可水解基团随时间推移提供化合物在体内的受控释放。

4. 发明授权

US5939406A 18-substituted-19-nor-vitamin D compounds 失效
标题翻译： 18-取代的19-维生素D化合物
公开(公告)号：US5939406A
公开(公告)日：1999-08-17
申请号：US897553
申请日：1997-07-21
申请人： Hector F. DeLuca , Zu Y. Cai
发明人： Hector F. DeLuca , Zu Y. Cai
IPC分类号： C07C401/00 , A01N45/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： This invention provides a novel class of vitamin D compounds, namely, 13-ethyl and 13-vinyl-18,19-dinor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have the formula: ##STR1## where Y.sub.1 and Y.sub.2, which may be the same or different, are each selected from the group consisting of hydrogen and a hydroxy-protecting group, R.sub.6 is selected from the group consisting of an ethyl or vinyl radical, and where the group R represents any of the typical side chains known for vitamin D type compounds. These 18-substituted compounds are characterized by minimal intestinal calcium transport activity and minimal bone calcium mobilization activity resulting in novel therapeutic agents for the treatment of secondary hyperparathyroidism. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as anti-cancer agents and for the treatment of diseases such as psoriasis.
摘要翻译：本发明提供了一类新颖的维生素D化合物，即13-乙基和13-乙烯基-18,19-二 - 维生素D衍生物，以及它们化学合成的一般方法。化合物具有下式：其中Y1和Y2可以相同或不同，各自选自氢和羟基保护基，R6选自乙基或乙烯基，和其中基团R表示维生素D型化合物已知的任何典型侧链。这些18-取代的化合物的特征在于肠内钙转运活性最小，骨钙移动活性最小，导致用于治疗继发性甲状旁腺功能亢进的新型治疗剂。这些化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面也表现出显着的活性，因此证明其用作抗癌剂并用于治疗诸如牛皮癣的疾病。

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