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1. 发明授权

US08455466B2 Vitamin d analogues, compositions comprising said analogues and their use 有权
标题翻译：维生素d类似物，包含所述类似物的组合物及其用途
公开(公告)号：US08455466B2
公开(公告)日：2013-06-04
申请号：US10532019
申请日：2003-10-23
申请人： Ernst Torndal Binderup , Kai Holst Hansen , Claus Aage Svensgaard Bretting , Martin John Calverley
发明人： Ernst Torndal Binderup , Kai Holst Hansen , Claus Aage Svensgaard Bretting , Martin John Calverley
IPC分类号： A61K401/00 , C07C31/59
CPC分类号： C07C401/00
摘要： Compounds according to formula I in which formula R1 and R2, which may be the same or different, represent halogen, (C1-C6)hydrocarbyl, optionally substituted with one or two hydroxyl group or one or more fluorine atoms, or, together with the carbon atom to which they are both attached, R1 and R2 form a (C3-C6)carbocyclic ring, or one of R1 and R2 taken together with R3 forms a direct bond, such that a triple bond is constituted, or R1 and R2 represent both hydrogen; R3 when not forming a direct bond with one of R1 and R2 represents hydrogen or (C1-C3)hydrocarbyl; X represents (E)-ethylene, (Z)-ethylene, ethynylene, or a bond; Y and Z independently represent hydrogen or methyl; and prodrugs and stereo isomeric forms thereof are provided together with their use in therapy, and their use in the manufacture of medicaments.
摘要翻译：根据式I的化合物，其中可以相同或不同的式R 1和R 2表示卤素，（C 1 -C 6）烃基，任选被一个或两个羟基或一个或多个氟原子取代，或者与碳原子，R 1和R 2形成（C 3 -C 6）碳环，R 1和R 2中的一个与R 3一起形成直接键，从而构成三键，或者R 1和R 2表示氢; 当不与R 1和R 2中的一个直接键合时，R 3表示氢或（C 1 -C 3）烃基; X表示（E） - 亚乙基，（Z） - 亚乙基，亚乙炔基或键; Y和Z独立地表示氢或甲基; 并且其前体药物和立体异构形式与其在治疗中的用途一起提供，以及它们在制备药物中的用途。

2. 发明授权

US06646143B2 Vitamin D analogues 失效
标题翻译：维生素D类似物
公开(公告)号：US06646143B2
公开(公告)日：2003-11-11
申请号：US09787664
申请日：2001-03-20
申请人： Kai Holst Hansen
发明人： Kai Holst Hansen
IPC分类号： A61K31593
CPC分类号： C07C401/00
摘要： Compounds of the formula I wherein X represents hydrogen or hydroxy; R1 and R2, which may be the same or different, represent hydrogen, (C1-C4)alkyl optionally substituted with one hydroxyl group or one or more fluorine atoms, or, together with the carbon atom to which they are attached, R1 and R2 form a (C3-C5)carbocyclic ring; R3 represents (C1-C4)alkyl, (C1-C4)alkoxy or a halogen atom, such as fluorine, chlorine, bromine, or iodine, and in-vivo hydrolyzable esters thereof with pharmaceutically acceptable acids, may be used in the prophylaxis and/or treatment of dieases characterized by abnormal cell differentiation and/or cell proliferation.
摘要翻译：式I的化合物，其中X表示氢或羟基; R 1和R 2可以相同或不同，表示氢，任选被一个羟基或一个或多个氟原子取代的（C 1 -C 4）烷基，或者与它们的碳原子一起连接，R 1和R 2形成（C 3 -C 5）碳环; R 3表示（C 1 -C 4）烷基，（C 1 -C 4）烷氧基或卤素原子，例如氟，氯，溴或碘，并且其体内可水解的酯与药学上可接受的酸可用于预防和/或治疗以异常细胞分化和/或细胞增殖为特征的病毒。

3. 发明授权

US06537980B1 Vitamin D analogues and their pharmaceutical use 失效
标题翻译：维生素D类似物及其药物用途
公开(公告)号：US06537980B1
公开(公告)日：2003-03-25
申请号：US09959306
申请日：2001-10-23
申请人： Kai Holst Hansen
发明人： Kai Holst Hansen
IPC分类号： A61K31593
CPC分类号： C07C401/00
摘要： The present invention relates to compounds of general formula (I) wherein R1 and R2, which may be the same or different, represent (C1-C4)alkyl, and R3 represents hydrogen, halogen, (C1-C4)alkyl, or O—(C1-C4)alkyl, and in-vivo hydrolysable esters there with pharmaceutically acceptable acids. The present compounds are of value in the human and veterinary practice.
摘要翻译：本发明涉及通式（I）的化合物，其中R1和R2可以相同或不同，代表（C1-C4）烷基，R3代表氢，卤素，（C1-C4）烷基或O- （C 1 -C 4）烷基，和其中具有药学上可接受的酸的体内可水解的酯。本化合物在人类和兽医实践中是有价值的。

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