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1. 发明授权

US4613594A Fluorinated vitamin D.sub.3 compounds 失效
标题翻译：氟化维生素D3化合物
公开(公告)号：US4613594A
公开(公告)日：1986-09-23
申请号：US672059
申请日：1984-11-16
申请人： Enrico Baggiolini , Giacomo Pizzolato , Milan Uskokovic , Gary Truitt
发明人： Enrico Baggiolini , Giacomo Pizzolato , Milan Uskokovic , Gary Truitt
IPC分类号： C07C35/52 , A61K31/045 , A61K31/59 , A61P3/02 , A61P35/00 , C07C27/00 , C07C33/44 , C07C45/30 , C07C49/743 , C07C67/00 , C07C401/00 , C07F7/08 , C07F7/18 , C07J9/00
CPC分类号： C07F7/1856 , C07C33/44 , C07C401/00 , C07C45/305 , C07C49/743 , Y02P20/55
摘要： Novel hexafluoro-cholecalciferol compounds and processes for preparing such compounds are disclosed. Intermediates utilized in the preparation of such compounds and pharmaceutical preparations containing these compounds are also disclosed.
摘要翻译：公开了新的六氟 - 胆钙化甾醇化合物及其制备方法。还公开了用于制备这些化合物的中间体和含有这些化合物的药物制剂。

2. 发明申请

US20050113348A1 Vitamin D and vitamin D analogs or derivatives as new anti-hypertensive agents 审中-公开
标题翻译：维生素D和维生素D类似物或衍生物作为新的抗高血压药物
公开(公告)号：US20050113348A1
公开(公告)日：2005-05-26
申请号：US10962215
申请日：2004-10-08
申请人： Yanchun Li , Milan Uskokovic
发明人： Yanchun Li , Milan Uskokovic
IPC分类号： A61K31/59 , G01N33/82 , C12Q1/37
CPC分类号： A61K31/59 , G01N33/82 , G01N2333/96472 , G01N2500/10
摘要： Methods and compositions to suppress renin expression and blood pressure in mammals are disclosed. Vitamin D and its analogues and derivatives, including Gemini compounds, are negative regulators of renin synthesis and blood pressure. Renin expression and plasma angiotensin II production were increased several fold in vitamin D receptor (VDR) null mice, leading to hypertension, cardiac hypertrophy and increased water intake. Vitamin D or its analogue-mediated regulation of renin expression and blood pressure is independent of calcium metabolism. Vitamin D analogues or derivatives are novel preventive or therapeutic anti-hypertension agents. Assays to identify novel vitamin D analogues or derivatives as anti-hypertensive agents are disclosed.
摘要翻译：公开了抑制哺乳动物的肾素表达和血压的方法和组合物。维生素D及其类似物和衍生物，包括双子座化合物，是肾素合成和血压的负调节因子。维生素D受体（VDR）无效小鼠的肾素表达和血浆血管紧张素II的产生增加了数倍，导致高血压，心脏肥大和水分摄入增加。维生素D或其类似物介导的肾素表达和血压调节与钙代谢无关。维生素D类似物或衍生物是新型预防或治疗性抗高血压药。公开了鉴定新型维生素D类似物或衍生物作为抗高血压药物的分析。

3. 发明申请

US20100222307A1 VITAMIN D AND VITAMIN D ANALOGS OR DERIVATIVES AS NEW ANTI-HYPERTENSIVE AGENTS 审中-公开
标题翻译：维生素D和维生素D类似物或衍生物作为新型抗高血压药物
公开(公告)号：US20100222307A1
公开(公告)日：2010-09-02
申请号：US12715133
申请日：2010-03-01
申请人： Yanchun Li , Milan Uskokovic
发明人： Yanchun Li , Milan Uskokovic
IPC分类号： A61K31/593 , A61P9/12
CPC分类号： A61K31/59 , G01N33/82 , G01N2333/96472 , G01N2500/10
摘要： Methods and compositions to suppress renin expression and blood pressure in mammals are disclosed. Vitamin D and its analogues and derivatives, including Gemini compounds, are negative regulators of renin synthesis and blood pressure. Renin expression and plasma angiotensin II production were increased several fold in vitamin D receptor (VDR) null mice, leading to hypertension, cardiac hypertrophy and increased water intake. Vitamin D or its analogue-mediated regulation of renin expression and blood pressure is independent of calcium metabolism. Vitamin D analogues or derivatives are novel preventive or therapeutic anti-hypertension agents. Assays to identify novel vitamin D analogues or derivatives as anti-hypertensive agents are disclosed.
摘要翻译：公开了抑制哺乳动物的肾素表达和血压的方法和组合物。维生素D及其类似物和衍生物，包括双子座化合物，是肾素合成和血压的负调节因子。维生素D受体（VDR）无效小鼠的肾素表达和血浆血管紧张素II的产生增加了数倍，导致高血压，心脏肥大和水分摄入增加。维生素D或其类似物介导的肾素表达和血压调节与钙代谢无关。维生素D类似物或衍生物是新型预防或治疗性抗高血压药。公开了鉴定新型维生素D类似物或衍生物作为抗高血压药物的分析。

4. 发明申请

US20070032461A1 1,3 Aclyated 24-keto-vitamin d3 compounds and methods of use thereof 审中-公开
标题翻译： 1,3 Acetated 24-酮维生素D 3化合物及其使用方法
公开(公告)号：US20070032461A1
公开(公告)日：2007-02-08
申请号：US10554769
申请日：2004-04-30
申请人： Luciano Adorini , Giuseppe Penna , Milan Uskokovic , Hubert Maehr
发明人： Luciano Adorini , Giuseppe Penna , Milan Uskokovic , Hubert Maehr
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00
摘要： The invention provides 1,3 acylated, 24-keto vitamin D3 compounds of formula I: wherein: X1 and X1 are each independently H2 or ═CH2, provided X1 and X1 are not both ═CH2; R1 and R2 are each independently, hydroxyl, OC(O)C1-C4 alkyl, OC(O)hydroxyalkyl, OC(O)haloalkyl, provided that R1 and R2 are not both hydroxyl; R3 and R4 are each independently hydrogen, C1-C4 alkyl, hydroxyalkyl, or haloalkyl, or R3 and R4 taken together with C20 form C3-C6 cylcoalkyl; and R5 and R6 are each independently C1-C4 alkyl, hydroxyalkyl, or haloalkyl; and pharmaceutically acceptable esters, salts, and prodrugs thereof. Methods for using the compounds to treat vitamin D3 associated states, and phar,aceutical compositions containing the compounds are also disclosed.
摘要翻译：本发明提供1,3-酰化的24-酮维生素D 3 O 3式III化合物：其中：X 1和X 1各自独立地为 H 2或-CH 2，条件是X 1和X 1不同时为-CH 2 R 1和R 2各自独立地为羟基，OC（O）C 1 -C 4烷基， OC（O）羟基烷基，OC（O）卤代烷基，条件是R 1和R 2不都是羟基; R 3和R 4各自独立地为氢，C 1 -C 4烷基，羟基烷基或卤代烷基，或R 3和R 4 ＆lt; / SUB＆gt;与C 20 - C 3 -C 3 -C 6 - 环烷基一起取代; 和R 5和R 6各自独立地为C 1 -C 4烷基，羟基烷基或卤代烷基; 和其药学上可接受的酯，盐和前药。还公开了使用该化合物来治疗维生素D 3 3相关状态的方法，以及含有该化合物的药用组合物。

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