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1. 发明授权

US06392071B1 26,27-homologated-20-EPI-2-alkylidene-19-nor-vitamin D compounds 有权
标题翻译： 26,27同系的20-EPI-2-亚烷基-19-去甲维生素D化合物
公开(公告)号：US06392071B1
公开(公告)日：2002-05-21
申请号：US09540686
申请日：2000-03-31
申请人： Hector F. DeLuca , Rafal R. Sicinski
发明人： Hector F. DeLuca , Rafal R. Sicinski
IPC分类号： C07C40100
CPC分类号： C07C401/00 , C07F7/1804 , Y02P20/55
摘要： This invention provides a novel class of vitamin D related compounds, namely, the 2-alkylidene-19-nor-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 and R8, which may be the same or different, are each selected from hydrogen, alkyl, hydroxyalkyl and fluoroalkyl, or when taken together represent the group —(CH2)x— where x is an integer from 2 to 5, and where the group R represents any of the typical side chains known for vitamin D type compounds. These 2-substituted compounds are characterized by relatively high intestinal calcium transport activity and relatively high bone calcium mobilization activity resulting in novel therapeutic agents for the treatment of diseases where bone formation is desired, particularly low bone turnover 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 anti-cancer agents and for the treatment of diseases such as psoriasis.
摘要翻译：本发明提供了一类维生素D相关化合物，即2-亚烷基-19-去甲维生素D衍生物，以及它们的化学合成的一般方法。这些化合物具有下式：其中可以相同或不同的Y1和Y2各自选自氢和羟基保护基，各自选择可以相同或不同的R6和R8 从氢，烷基，羟基烷基和氟烷基，或当它们一起表示 - （CH 2）x - 基团，其中x是2至5的整数，并且其中基团R表示维生素D型化合物已知的任何典型侧链。这些2-取代的化合物的特征在于相对较高的肠钙运输活性和相对高的骨钙动员活性，导致用于治疗需要骨形成，特别是低骨转换性骨质疏松症的疾病的新型治疗剂。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

US06288249B1 Vitamin D analogs and methods of preparing these compounds 失效
标题翻译：维生素D类似物和制备这些化合物的方法
公开(公告)号：US06288249B1
公开(公告)日：2001-09-11
申请号：US09180136
申请日：1999-06-16
申请人： Sebastianus J. Halkes , Jan Paul Van De Velde , Silvia Kanzler , Wolfgang Reischl
发明人： Sebastianus J. Halkes , Jan Paul Van De Velde , Silvia Kanzler , Wolfgang Reischl
IPC分类号： C07C40100
CPC分类号： C07C33/38 , C07C2602/08
摘要： The invention relates to vitamin D analogs of general formula (I) wherein: R1 is a hydrogen atom or a substituent selected from the group consisting of hydroxy, CH2OH, CH2CH2OH, CH2CH2CH2OH, OCH3, OCH2OH, OCH2CH2OH and OCH2CH2CH2OH; R2 is a hydrogen atom or a substituent selected from the group consisting of OCH3, OCH2OH, CHm(CH2OH)n(CH2CH2OH)p, (CH2)qOH and O(CH2)rOH; wherein: m is 0 or 1, p, q and n are 0-3, r is 1-3 and m+n+p=3; with the proviso that R1 and/or R2 contain at least one OH group; R3 is a straight or branched, saturated or unsaturated aliphatic hydrocarbon of 6-13 C atoms which may be substituted with one or more substituents from the group hydroxy or fluoro. The invention further relates to methods of preparing these compounds, a pharmaceutical composition containing these compounds and to their use in pharmacotherapy and cosmetics.
摘要翻译：本发明涉及通式（I）的维生素D类似物，其中：R 1是氢原子或选自羟基，CH 2 OH，CH 2 CH 2 OH，CH 2 CH 2 CH 2 OH，OCH 3，OCH 2 OH，OCH 2 CH 2 OH和OCH 2 CH 2 CH 2 OH的取代基; R2是氢原子或选自OCH3，OCH2OH，CHm（CH2OH）n（CH2CH2OH）p，（CH2）qOH和O（CH2）rOH的取代基; 其中：m为0或1，p，q和n为0-3，r为1-3，m + n + p = 3; 条件是R1和/或R2含有至少一个OH基团; R3是6-13个碳原子的直链或支链饱和或不饱和脂族烃基，其可被一个或多个羟基或氟取代基取代。本发明还涉及制备这些化合物的方法，含有这些化合物的药物组合物及其在药物治疗和化妆品中的用途。

3. 发明授权

US06229030B1 Labeled vitamin D compounds and the use thereof 有权
公开(公告)号：US06229030B1
公开(公告)日：2001-05-08
申请号：US09345789
申请日：1999-07-01
申请人： Michael F. Holick , Rahul Ray
发明人： Michael F. Holick , Rahul Ray
IPC分类号： C07C40100
摘要： Kit comprising biotin, fluorescent and chemiluminescent labeled vitamin D compounds are disclosed. The disclosed kit may be used in assays for the presence of vitamin D, its metabolites and vitamin D analogs in biological fluids.

4. 发明授权

US06753435B1 Intermediates for vitamin D and processes for the preparation thereof 失效
标题翻译：维生素D的中间体及其制备方法
公开(公告)号：US06753435B1
公开(公告)日：2004-06-22
申请号：US10239778
申请日：2002-09-25
申请人： Masahiro Koga , Toru Minoshima
发明人： Masahiro Koga , Toru Minoshima
IPC分类号： C07C40100
CPC分类号： C07C401/00 , C07C309/65 , C07C2601/14 , C07C2601/16 , C07C2602/24 , C07F7/1804 , C07F7/1892
摘要： An object of the present invention is to provide intermediates for the synthesis of 1&agr;-hydroxyvitamin D derivatives useful as drugs and processes for the preparation thereof. Namely, the present invention is a process for the preparation of a compound represented by the formula (2), which comprises reacting a compound represented by the formula (1) with a compound represented by the formula (4) in the presence of a palladium catalyst, a process for the preparation of a compound represented by the formula (3), which comprises further catalytically reducing the resulting compound represented by the formula (2) in the presence of a Lindlar catalyst and hydrogen gas and heating the obtained product and a process for the preparation of a compound represented by the formula (5), which comprises further oxidizing the resulting compound represented by the formula (3) with an oxidizing agent and the compounds represented by the formulae (1) to (3):
摘要翻译：本发明的目的是提供用作合成作为药物的1α-羟基维生素D衍生物的中间体及其制备方法。本发明是制备式（2）表示的化合物的方法，其包括在钯催化剂存在下使式（1）表示的化合物与式（4）表示的化合物反应，制备由式（3）表示的化合物的方法，该方法还包括在Lindlar催化剂和氢气的存在下催化还原由式（2）表示的化合物，并加热得到的产物和制备由式（5）表示的化合物的方法，该方法包括进一步氧化所得由式（3）表示的化合物与氧化剂和由式（1）至（3）表示的化合物：

5. 发明授权

US06362350B1 Crystalline 1&agr;, 24(S)-dihydroxyvitamin D2 and method of purification thereof 失效
标题翻译：结晶1α，24（S） - 二羟基维生素D2及其纯化方法
公开(公告)号：US06362350B1
公开(公告)日：2002-03-26
申请号：US09437307
申请日：1999-11-10
申请人： Hector F. DeLuca , Rafal R. Sicinski , Hazel Holden , James Brian Thoden
发明人： Hector F. DeLuca , Rafal R. Sicinski , Hazel Holden , James Brian Thoden
IPC分类号： C07C40100
CPC分类号： C07C401/00
摘要： A method of purifying 1&agr;,24(S)-dihydroxyvitamin D2 to obtain 1&agr;,24(S)-dihydroxyvitamin D2 in crystalline form. The method includes the steps of boiling a solvent under inert atmosphere, dissolving a product containing 1&agr;,24(S)-dihydroxyvitamin D2 to be purified in the solvent, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of 1&agr;,24(S)-dihydroxyvitamin D2 crystals, and recovering the 1&agr;,24(S)-dihydroxyvitamin D2 crystals. The purification technique involves using one of several binary solvent systems, namely, acetone and hexane, 2-propanol and hexane, or ethyl formate and petroleum ether.
摘要翻译：纯化1α，24（S） - 二羟基维生素D 2以获得结晶形式的1α，24（S） - 二羟基维生素D 2的方法。该方法包括在惰性气氛下沸腾溶剂的步骤，将待纯化的1α，24（S） - 二羟基维生素D2的产物溶解在溶剂中，将溶剂和溶解的产物在环境温度下冷却足够的时间以形成 1（S） - 二羟基维生素D 2晶体的沉淀物，并回收1α，24（S） - 二羟基维生素D 2晶体。纯化技术涉及使用几种二元溶剂体系之一，即丙酮和己烷，2-丙醇和己烷，或甲酸乙酯和石油醚。

6. 发明授权

US06329538B1 Vitamin D3 analogs 失效
标题翻译：维生素D3类似物
公开(公告)号：US06329538B1
公开(公告)日：2001-12-11
申请号：US09648817
申请日：2000-08-25
申请人： Andrew David Batcho , Bernard Michael Hennessy , Jerome Anthony Iacobelli , Milan Radoje Uskokovic
发明人： Andrew David Batcho , Bernard Michael Hennessy , Jerome Anthony Iacobelli , Milan Radoje Uskokovic
IPC分类号： C07C40100
CPC分类号： C07C401/00 , A61K31/59
摘要： A compound of the formula wherein R is hydrogen or hydroxy, each R2 is independently H or halogen, X is ═CH2, or when R is hydroxy, X is hydrogen or ═CH2, and A is —C≡C—, or —CH2—CH2—, provided that when A is —CH2—CH2—, R2 is H.
摘要翻译：式R的化合物是氢或羟基，每个R 2独立地为H或卤素，X为= CH 2，或当R为羟基时，X为氢或= CH 2，A为-C = C-或-CH 2 - CH 2 - ，条件是当A是-CH 2 -CH 2 - 时，R 2是H.

7. 发明授权

US06448421B1 Crystals of vitamin D derivatives and process for the preparation thereof 失效
标题翻译：维生素D衍生物晶体及其制备方法
公开(公告)号：US06448421B1
公开(公告)日：2002-09-10
申请号：US09202144
申请日：1998-12-09
申请人： Tsuyoshi Yamauchi
发明人： Tsuyoshi Yamauchi
IPC分类号： C07C40100
CPC分类号： C07J9/00 , C07C401/00 , C07J71/001
摘要： The present invention provides crystals of the compound represented by formula (I): crystals of a vitamin D derivative which are obtained by purifying a crude or preliminarily purified product of the vitamin D derivative through a reverse phase chromatography and then crystallizing the purified derivative from an organic solvent; novel compounds which are formed during the synthesis of a vitamin D derivative as by-product; and a method for purifying a vitamin D derivative or the precursor thereof. The method of the present invention makes it possible to supply a highly purified vitamin D derivative, especially ED-71, in bulk and steadily.
摘要翻译：本发明提供由式（I）表示的化合物的晶体：维生素D衍生物的结晶，其通过反相色谱法纯化维生素D衍生物的粗产物或预纯化产物，然后将纯化的衍生物从有机溶剂; 在合成维生素D衍生物作为副产物期间形成的新化合物; 以及维生素D衍生物或其前体的纯化方法。本发明的方法使得可以大量和稳定地供应高度纯化的维生素D衍生物，特别是ED-71。

8. 发明授权

US06444098B2 Process for the preparation of tocol acylates and tocopherol acylates 失效
标题翻译：酰基转移酸和生育酚酰化物的制备方法
公开(公告)号：US06444098B2
公开(公告)日：2002-09-03
申请号：US09900587
申请日：2001-07-09
申请人： Werner Bonrath , Fabio Cirillo
发明人： Werner Bonrath , Fabio Cirillo
IPC分类号： C07C40100
CPC分类号： C07D311/72
摘要： The present invention relates to a process for preparing tocol acylate or tocopherol acylate having the following steps: a) combining tocol or tocopherol with an acylating agent to form a reaction mixture; b) irradiating the reaction mixture with microwave energy to from tocol acylate or tocopherol acylate; and c) isolating the tocol acylate or tocopherol acylate from the reaction mixture.
摘要翻译：本发明涉及一种制备酰化酰化物或生育酚酰化物的方法，其具有以下步骤：a）将酰基转移剂与母体或生育酚结合形成反应混合物; b）用微波能量将反应混合物照射到酰基转移酸或生育酚酰化物; 和c）从反应混合物中分离出酰基酸或生育酚酰化物。

9. 发明授权

US06441207B1 Method for making hydroxy-25-ene-vitamin D compounds 有权
标题翻译：制备羟基-25-烯 - 维生素D化合物的方法
公开(公告)号：US06441207B1
公开(公告)日：2002-08-27
申请号：US09716316
申请日：2000-11-20
申请人： Hans Wynberg , Ton Vries , Kees Pouwer
发明人： Hans Wynberg , Ton Vries , Kees Pouwer
IPC分类号： C07C40100
CPC分类号： C07C401/00 , C07C29/147 , C07C67/333 , C07C67/343 , C07C303/28 , C07C315/00 , C12P7/22 , C07C33/025 , C07C69/533 , C07C317/14 , C07C309/66
摘要： The present invention provides a method for preparing a novel class of vitamin D compounds in which the C-25 or equivalent position has a double bond. In addition, the side chain is optionally extended by one or two methylene or methyne groups. The compounds prepared by the method of the present invention are of value as prodrugs for active 1&agr;, 24-dihydroxylated vitamin D compounds.
摘要翻译：本发明提供一种制备其中C-25或等同位置具有双键的新一类维生素D化合物的方法。此外，侧链任选地被一个或两个亚甲基或甲炔基延伸。通过本发明的方法制备的化合物作为活性1α，24-二羟基化维生素D化合物的前药具有价值。

10. 发明授权

US06380408B1 Non-calcemic, antiproliferative, transcriptionally active sulfur-containing analogs of 1&agr;, 25-dihydroxy vitamin D3 有权
标题翻译： 1α，25-二羟维生素D3的非钙，抗增殖，转录活性含硫类似物
公开(公告)号：US06380408B1
公开(公告)日：2002-04-30
申请号：US09541060
申请日：2000-03-31
申请人： Gary H. Posner , Jae-Kyoo Lee , Qiang Wang , Kenneth R. Crawford , Gyoonhee Han
发明人： Gary H. Posner , Jae-Kyoo Lee , Qiang Wang , Kenneth R. Crawford , Gyoonhee Han
IPC分类号： C07C40100
CPC分类号： C07C401/00
摘要： Novel sulfur-containing analogs of 1&agr;,25-dihydroxy vitamin D3 are provided. These analogs are synthesized in a convergent manner by joining A-ring and C,D ring fragments. Each analog with 1&agr;,3&bgr;-substituent stereochemistry shows a pharmacologically desirable combination of high antiproliferative and high transcriptional activities in vitro and also low calcemic activity in vivo.
摘要翻译：提供了1α，25-二羟基维生素D3的新型含硫类似物。这些类似物通过连接A环和C，D环片段以收敛方式合成。每个具有1alpha，3beta取代基立体化学的类似物都显示体外高抗增殖和高转录活性以及体内低钙活性的药理学上希望的组合。

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