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1. 发明申请

US20200290960A1 BIAROMATIC VITAMIN D ANALOGS 审中-公开
公开(公告)号：US20200290960A1
公开(公告)日：2020-09-17
申请号：US16061418
申请日：2016-12-14
申请人： DSM IP ASSETS B.V.
发明人： Igor BENDIK , Piero GEOTTI-BIANCHINI , Marc HEIDL , Eileen JACKSON , Alexander SCHLIFKE-POSCHALKO
IPC分类号： C07C401/00 , A61K8/34 , A61Q19/08
摘要： Novel biaromatic compounds, which are vitamin D analogs, processes for their preparation and cosmetic, dermatological and pharmaceutical preparations containing one or more of these compounds.

2. 发明申请

US20190016677A1 COMPOSITIONS RELATING TO VITAMIN D 审中-公开
公开(公告)号：US20190016677A1
公开(公告)日：2019-01-17
申请号：US16135365
申请日：2018-09-19
申请人： Siemens Healthcare Diagnostics Inc.
发明人： Zhu Teng , Qimu Liao , Manoj Sharma , Martin A. Drinan , Tie Quan Wei
IPC分类号： C07C401/00 , G01N33/82
CPC分类号： C07C401/00 , C07C2601/14 , C07C2602/24 , G01N33/82
摘要： Compounds include compounds of the Formula I, namely, (R1)p-(L)q-Z wherein R1, L, p and q are as defined herein.

3. 发明申请

US20180265463A1 Vitamin D3 Derivatives and Pharmaceutical Use Thereof 审中-公开
公开(公告)号：US20180265463A1
公开(公告)日：2018-09-20
申请号：US15539260
申请日：2015-12-24
申请人： Kyoto University , National University Corporation Tokyo University of Agriculture and Technology
发明人： Mizuki Watanabe , Risa Asano , Kazuo Nagasawa , Motonari Uesugi
IPC分类号： C07C401/00 , C07D209/48 , C07D495/04 , A61P3/04 , A61P1/16 , A61P3/10 , A61P9/00 , A61P35/00
CPC分类号： C07C401/00 , A61K31/59 , A61K31/593 , A61P1/16 , A61P3/04 , A61P3/10 , A61P9/00 , A61P35/00 , C07C2601/14 , C07C2602/24 , C07D209/48 , C07D211/46 , C07D295/125 , C07D495/04
摘要： The present invention relates to vitamin D3 derivatives of the following formula, wherein each symbol has the same meaning as defined herein, and pharmaceutical or medical use thereof for treating metabolic disease, liver disease, obesity, diabetes, cardiovascular disease, or cancer in a patient in need thereof.

4. 发明授权

US09804176B2 Assays for vitamin D epimers 有权
公开(公告)号：US09804176B2
公开(公告)日：2017-10-31
申请号：US15319186
申请日：2015-06-22
申请人： Siemens Healthcare Diagnostics Inc.
发明人： Tie Quan Wei , Zhu Teng , Tatiana Mareeva , Jie Li , Martin A. Drinan , Izak Bahar , Manoj Sharma
IPC分类号： G01N33/82 , G01N33/532 , C07K16/44 , A61K39/385 , G01N21/76 , C07C401/00
CPC分类号： G01N33/82 , A61K39/385 , C07C401/00 , C07K16/44 , G01N21/76 , G01N33/532
摘要： Methods include determining an amount of an epimeric vitamin D analyte in a sample suspected of containing the epimeric vitamin D analyte. A combination is provided in an assay medium that includes the sample and a vitamin D epimer antibody that is specific for the epimeric vitamin D analyte. The assay medium is incubated under conditions for binding of the vitamin D epimer antibody to the epimeric vitamin D analyte to form an epimeric vitamin D antibody-bound complex. The amount of the epimeric vitamin D antibody-bound complex is determined and related to the amount of epimeric vitamin D analyte in the sample.

5. 发明授权

US09775903B2 1-deoxy analogs of 1,25-dihydroxyvitamin D3 compounds 有权
公开(公告)号：US09775903B2
公开(公告)日：2017-10-03
申请号：US13521980
申请日：2011-01-13
申请人： Gary H. Posner , Lindsey C. Hess , Alvin S. Kalinda , Rachel D. Slack , Uttam Saha , P. Martin Petkovich
发明人： Gary H. Posner , Lindsey C. Hess , Alvin S. Kalinda , Rachel D. Slack , Uttam Saha , P. Martin Petkovich
IPC分类号： A61K45/06 , C07C401/00 , A61K31/593
CPC分类号： A61K45/06 , A61K31/593 , C07C401/00 , C07C2601/14 , C07C2602/24
摘要： This present disclosure is directed to novel prodrugs of activated vitamin D3 compounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases.

6. 发明授权

US09517241B2 Amelioration of intestinal fibrosis and treatment of Crohn's disease 有权
公开(公告)号：US09517241B2
公开(公告)日：2016-12-13
申请号：US15051850
申请日：2016-02-24
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN
发明人： Robert U. Simpson , Peter D. R. Higgins , Laura A. Johnson
IPC分类号： A61K31/59 , C07C401/00 , A61K9/00 , A61K31/592 , A61K45/06
CPC分类号： A61K31/59 , A61K9/0053 , A61K31/592 , A61K45/06
摘要： Methods of treating patients with inflammatory bowel disease, intestinal fibrosis, or Crohn's disease involve administering a therapeutic amount of CARD-024 or related compound.

7. 发明申请

US20160195556A1 25-OH VITAMIN D DERIVATIVES FOR DETERMINING VITAMIN D METABOLITES 审中-公开
标题翻译：用于测定维生素D代谢物的25-OH维生素D衍生物
公开(公告)号：US20160195556A1
公开(公告)日：2016-07-07
申请号：US14910881
申请日：2014-08-01
申请人： ORGENTEC DIAGNOSTIKA GMBH
发明人： Vukic SOSKIC , Robert POPPE
IPC分类号： G01N33/82 , C07D495/04 , C07C401/00
CPC分类号： G01N33/82 , C07C401/00 , C07C2601/14 , C07C2602/24 , C07D495/04
摘要： The present invention relates to new vitamin D compounds which are bonded to a labelling group at the C3 stereocentre by means of a linker. The present invention further relates to a method for producing these vitamin D compounds and to the use of an intermediate for producing these compounds. The present invention also relates to a method for quantitatively determining vitamin D using a vitamin D compound according to the invention as a tracer. Furthermore, the present invention relates to a reagent for determining vitamin D, containing a compound according to the invention, and to the use thereof for determining vitamin D.
摘要翻译：本发明涉及通过接头与C 3立构中心的标记基团连接的新的维生素D化合物。本发明还涉及这些维生素D化合物的制造方法以及制备这些化合物的中间体的用途。本发明还涉及使用本发明的维生素D化合物作为示踪剂定量测定维生素D的方法。此外，本发明涉及用于测定含有本发明化合物的维生素D的试剂及其用于测定维生素D的用途。

8. 发明授权

US09315455B2 Process for isomerizing fused bicyclic structures and preparation of vitamin D analogs comprising the same 有权
标题翻译：异构化稠合双环结构的方法和包含其的维生素D类似物的制备方法
公开(公告)号：US09315455B2
公开(公告)日：2016-04-19
申请号：US13012084
申请日：2011-01-24
申请人： Jean-Luc Moutou , Florent Mouton , Gilles Pellegrino , Jean Lafay
发明人： Jean-Luc Moutou , Florent Mouton , Gilles Pellegrino , Jean Lafay
IPC分类号： C07C401/00 , C07C45/67
CPC分类号： C07C401/00 , C07B2200/07 , C07C45/67 , C07C2602/24 , C07C49/753
摘要： The present invention concerns a process of isomerizing trans fused bicyclic derivatives into cis fused bicyclic derivatives and the preparation of vitamin D or analogs thereof comprising said isomerization step.
摘要翻译：本发明涉及将反式稠合双环衍生物异构化为顺式稠合双环衍生物的方法，以及制备维生素D或其类似物，其包含所述异构化步骤。

9. 发明申请

US20150148552A1 23-YNE-VITAMIN D3 DERIVATIVE 有权
标题翻译： 23-YNE-VITAMIN D3衍生物
公开(公告)号：US20150148552A1
公开(公告)日：2015-05-28
申请号：US14612781
申请日：2015-02-03
申请人： TEIJIN PHARMA LIMITED
发明人： Hiroshi SAITO
IPC分类号： C07C401/00
CPC分类号： C07C401/00 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/24 , C07F7/1804 , C07F7/1852 , Y02P20/55
摘要： To provide a novel vitamin D3 derivative useful as a therapeutic agent for osteoporosis.Provided is a vitamin D3 derivative represented by the following formula (1) or a medicinally acceptable solvate thereof: wherein R1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkylcarbonyloxyalkyl group with each alkyl having 1 to 6 carbon atoms, or an arylcarbonyloxyalkyl group with the aryl having 6 to 10 carbon atoms and the alkyl having 1 to 6 carbon atoms; R2 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms or, together with the other R2 and the carbon atom to which they are bound to, may form a cyclic alkyl group having 3 to 6 carbon atoms; R3 represents an alkyl group having 1 to 6 carbon atoms or, together with the other R3 and the carbon atom to which they are bound to, may form a cyclic alkyl group having 3 to 6 carbon atoms; X represents an oxygen atom or a methylene group; and n represents an integer of 1 or 2.
摘要翻译：提供可用作骨质疏松症治疗剂的新型维生素D3衍生物。本发明提供由下式（1）表示的维生素D3衍生物或其药学上可接受的溶剂化物：其中，R1表示氢原子，碳原子数1〜6的烷基，碳原子数为1〜6的烷基的烷基羰氧基烷基或芳基具有6至10个碳原子的芳基羰氧基烷基和具有1至6个碳原子的烷基; R 2表示氢原子或碳原子数1〜6的烷基，或者与其它的R 2和与它们相连的碳原子一起形成可以形成碳原子数为3〜6的环状烷基。 R 3表示碳原子数为1〜6的烷基，或者与另外的R 3及与它们相连的碳原子一起形成碳原子数为3〜6的环状烷基。 X表示氧原子或亚甲基; n表示1或2的整数。

10. 发明授权

US09040728B2 Crystallization of (20R) 19-nor-24-difluoro-1α,25-dihydroxyvitamin D3 有权
标题翻译：（20R）19-去甲-24-二氟-1α，25-二羟基维生素D3的结晶
公开(公告)号：US09040728B2
公开(公告)日：2015-05-26
申请号：US13828223
申请日：2013-03-14
申请人： Wisconsin Alumni Research Foundation
发明人： Hector F. DeLuca , Agnieszka Flores , James B. Thoden , Hazel M. Holden
IPC分类号： C07C401/00
CPC分类号： C07C401/00 , C07B2200/13 , C07C2601/14 , C07C2602/24
摘要： Disclosed are methods of purifying the compound (20R)-19-nor-24-difluoro-1α,25-dihydroxyvitamin D3 to obtain the compound in crystalline form. The methods typically include the steps of dissolving a product containing the compound in a solvent comprising hexane and 2-propanol, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals.
摘要翻译：公开了纯化化合物（20R）-19-去甲-24-二氟-1α，25-二羟基维生素D3以获得结晶形式的化合物的方法。所述方法通常包括以下步骤：将含有该化合物的产物溶解在包含己烷和2-丙醇的溶剂中，将溶剂和溶解的产品在环境温度下冷却足够的时间以形成晶体沉淀并回收晶体。

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