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公开(公告)号：US09073885B2
公开(公告)日：2015-07-07
申请号：US10543881
申请日：2004-01-29
申请人： Kazuya Takenouchi , Miyuki Anzai , Hiroshi Saito , Kazuhisa Okada , Seiichi Ishizuka , Daishiro Miura , Hiroaki Takayama , Atsushi Kittaka , Nozomi Saito , Toshie Fujishima
发明人： Kazuya Takenouchi , Miyuki Anzai , Hiroshi Saito , Kazuhisa Okada , Seiichi Ishizuka , Daishiro Miura , Hiroaki Takayama , Atsushi Kittaka , Nozomi Saito , Toshie Fujishima
IPC分类号： A61K31/593 , C07D307/58
CPC分类号： C07D307/58 , A61K31/593
摘要： A compound represented by the following Formula (1) that is effective for the treatment of Paget's disease of bone or hypercalcemia or a medically acceptable solvate thereof; [wherein R1 refers to hydrogen atom, C1-C6 alkyl group optionally substituted with hydrogen group or C1-C6 alkoxy group optionally substituted with hydroxyl group, R2a and R2b refer to hydrogen atom, C1-C10 alkyl group optionally substituted with hydroxyl group, C6-C10 aryl group optionally substituted with hydroxyl group or C7-C12 aralkyl group optionally substituted with a hydroxyl group, or are combined to represent ethylene group. However, a compound in which R1 is a hydrogen atom or a methyl group and R2a and R2b are hydrogen atoms is excluded].
摘要翻译： 由下式（1）表示的化合物可有效治疗佩吉特氏骨或高钙血症或其医学上可接受的溶剂合物; [其中，R1表示氢原子，可以被氢原子取代的C1-C6烷基或者被羟基取代的C1-C6烷氧基，R2a和R2b表示氢原子，可以被羟基取代的C1-C10烷基，C6 任选被羟基取代的-C 10芳基或任选被羟基取代的C 7 -C 12芳烷基，或被组合以代表亚乙基。 然而，除了R1是氢原子或甲基，R2a和R2b是氢原子的化合物]。
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公开(公告)号：US20090124819A1
公开(公告)日：2009-05-14
申请号：US12350040
申请日：2009-01-07
IPC分类号： C07C401/00
CPC分类号： A61K31/59 , C07C401/00
摘要： The object of the present invention is to synthesize novel vitamin D derivatives.According to the present invention, there are provided vitamin D derivatives represented by the following general formula (1): wherein R1 and R2 may be the same or different, and each represents a straight chain or branched chain alkyl group optionally substituted by a hydroxyl group, and R3 represents a straight chain or branched chain alkyl group optionally substituted by a hydroxyl group.
摘要翻译： 本发明的目的是合成新的维生素D衍生物。 根据本发明，提供了由以下通式（1）表示的维生素D衍生物：其中R 1和R 2可以相同或不同，并且各自表示任选被羟基取代的直链或支链烷基 R 3表示任选被羟基取代的直链或支链烷基。
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公开(公告)号：US20060148768A1
公开(公告)日：2006-07-06
申请号：US10543881
申请日：2004-01-29
申请人： Kazuya Takenouchi , Miyuki Anzai , Hiroshi Saito , Kazuhisa Okada , Seiichi Ishizuka , Daishiro Miura , Hiroaki Takayama , Atsushi Kittaka , Nozomi Saito , Toshie Fujishima
发明人： Kazuya Takenouchi , Miyuki Anzai , Hiroshi Saito , Kazuhisa Okada , Seiichi Ishizuka , Daishiro Miura , Hiroaki Takayama , Atsushi Kittaka , Nozomi Saito , Toshie Fujishima
IPC分类号： A61K31/59 , C07D307/02
CPC分类号： C07D307/58 , A61K31/593
摘要： A compound represented by the following Formula (1) that is effective for the treatment of Paget's disease of bone or hypercalcemia or a medically acceptable solvate thereof; [wherein R1 refers to hydrogen atom, C1-C6 alkyl group optionally substituted with hydrogen group or C1-C6 alkoxy group optionally substituted with hydroxyl group, R2a and R2b refer to hydrogen atom, C1-C10 alkyl group optionally substituted with hydroxyl group, C6-C10 aryl group optionally substituted with hydroxyl group or C7-C12 aralkyl group optionally substituted with a hydroxyl group, or are combined to represent ethylene group. However, a compound in which R1 is a hydrogen atom or a methyl group and R2a and R2b are hydrogen atoms is excluded].
摘要翻译： 由下式（1）表示的化合物可有效治疗佩吉特氏骨或高钙血症或其医学上可接受的溶剂合物; [其中R 1是氢原子，任选被氢或C 1 -C 6烷基取代的C 1 -C 6烷基， 任选被羟基取代的C 1 -C 6烷氧基，R 2a和R 2b是指氢原子，C 1〜 任选被羟基取代的C 1 -C 10烷基，任选被羟基取代的C 6 -C 10芳基或C 6 - 任选被羟基取代的或者被组合以代表亚乙基的C 1 -C 12芳烷基。 但是，不包括其中R 1是氢原子或甲基，R 2b和R 2b的氢原子的化合物。
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公开(公告)号：US20050131242A1
公开(公告)日：2005-06-16
申请号：US10499962
申请日：2002-12-25
IPC分类号： A61K31/59 , A61P3/02 , C07C401/00
CPC分类号： A61K31/59 , C07C401/00
摘要： According to the present invention, there are provided vitamin D derivatives represented by the following general formula (1): wherein R1 and R2 may be the same or different, and each represents a straight chain or branched chain alkyl group optionally substituted by a hydroxyl group, and R3 represents a straight chain or branched chain alkyl group optionally substituted by a hydroxyl group.
摘要翻译： 根据本发明，提供由以下通式（1）表示的维生素D衍生物：其中R 1和R 2可以相同或不同，并且 各自表示任选被羟基取代的直链或支链烷基，R 3表示任选被羟基取代的直链或支链烷基。
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公开(公告)号：US20050113349A1
公开(公告)日：2005-05-26
申请号：US10971041
申请日：2004-10-25
CPC分类号： C07C401/00
摘要： An object of the present invention is to synthesize a novel vitamin D3 derivative having a substituent at the 2α-position. The present invention provides vitamin D derivatives represented by-Formula (I): wherein R1 represents a saturated aliphatic C1-15hydrocarbon group optionally substituted with 1 to 3 hydroxy or protected hydroxy groups; and R2 represents a saturated aliphatic C1-10hydrocarbon group optionally substituted with one or more substituents, which may be the same or different and which are selected from the group consisting of a hydroxy group, a halogen atom, a cyano group, a lower alkoxy group, an amino group and an acylamino group, provided that when R2 represents a saturated aliphatic C1hydrocarbon group, R2 is substituted with at least one substituent.
摘要翻译： 本发明的目的是在2α-位上合成具有取代基的新的维生素D 3 N 3衍生物。 本发明提供由式（I）表示的维生素D衍生物：其中R 1表示任选被1至3个羟基取代的饱和脂肪族C 1-15烃基，或 保护的羟基; R 2表示任选被一个或多个取代基取代的饱和脂肪族C 1-10 1-10烃基，所述取代基可以相同或不同，并且选自 的羟基，卤素原子，氰基，低级烷氧基，氨基和酰基氨基，条件是当R 2表示饱和脂肪族C 1〜 >烃基，R 2 O 2被至少一个取代基取代。
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公开(公告)号：US06982257B1
公开(公告)日：2006-01-03
申请号：US09214155
申请日：1998-04-30
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： A61K31/59 , C07C401/00
摘要： Provided are 1,25-dihydroxy-2-methylvitamin D3 derivatives expressed by the general formula (I), [wherein each of R1 and R2 is independently a hydrogen atom or a tri(C1 to C7 alkyl)silyl group; herein configurations of asymmetric carbons at the 1-, 2- and 3-positions are each independently α-configuration or β-configuration] and their production methods. The compound is useful as a treating agent for osteoporosis, rickets, hyperthyroidism, etc.
摘要翻译： 提供由通式（I）表示的1,25-二羟基-2-甲基维生素D3衍生物，其中R 1和R 2各自独立地为氢原子 或三（C 1至C 7烷基）甲硅烷基; 在这里，1-，2-和3-位上的不对称碳的构型各自独立地为α构型或β-构型]及其制备方法。 该化合物可用作骨质疏松症，r ets病，甲状腺功能亢进等的治疗剂。
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公开(公告)号：US20050032754A1
公开(公告)日：2005-02-10
申请号：US10938588
申请日：2004-09-13
申请人： Hiroaki Takayama , Toshie Fujishima
发明人： Hiroaki Takayama , Toshie Fujishima
IPC分类号： A61K31/593 , A61P3/02 , C07C401/00 , A61K31/59
CPC分类号： C07C401/00 , A61K31/593
摘要： Object of the present invention is to synthesize novel vitamin D derivatives. The present invention provides 5,6-trans-2-alkyl-substituted vitamin D derivatives of Formula (1): wherein R1 is straight or branched-chain alkyl; and R2 is straight or branched-chain alkyl optionally substituted with hydroxy.
摘要翻译： 本发明的目的是合成新的维生素D衍生物。 本发明提供式（1）的5,6-反式-2-烷基取代的维生素D衍生物：其中R 1是直链或支链烷基; 并且R 2是任选被羟基取代的直链或支链烷基。
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公开(公告)号：US20050119240A1
公开(公告)日：2005-06-02
申请号：US10332125
申请日：2001-08-13
申请人： Hiroaki Takayama , Toshie Fujishima
发明人： Hiroaki Takayama , Toshie Fujishima
IPC分类号： A61P19/10 , C07C401/00 , A61K31/59
CPC分类号： C07C401/00
摘要： A vitamin D derivative which has a methyl group in the 1-position and has an epi form in the 20-position. The vitamin D derivative is represented by the general formula (1): wherein R represents linear or branched alkyl optionally substituted by hydroxy.
摘要翻译： 维生素D衍生物，其在1位具有甲基并且具有20位的外形。 维生素D衍生物由通式（1）表示：其中R表示任选被羟基取代的直链或支链烷基。
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公开(公告)号：US20060074255A1
公开(公告)日：2006-04-06
申请号：US11282643
申请日：2005-11-21
申请人： Hiroaki Takayama , Toshie Fujishima
发明人： Hiroaki Takayama , Toshie Fujishima
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00
摘要： The object of the present invention is to synthesize vitamin D derivatives in which the 3-position is substituted with methyl and the steric configuration at the 20-position is epimerized. The present invention provides vitamin D derivatives of Formula (1): wherein R is straight or branched alkyl optionally substituted with hydroxy.
摘要翻译： 本发明的目的是合成其中3-位被甲基取代的维生素D衍生物，并且在20位上的空间构型差向异构化。 本发明提供式（1）的维生素D衍生物：其中R是任选被羟基取代的直链或支链烷基。
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公开(公告)号：US4284577A
公开(公告)日：1981-08-18
申请号：US119390
申请日：1980-02-07
CPC分类号： C07J9/00 , C07J17/00 , C07J33/002 , C07J9/005
摘要： A novel vitamin D.sub.3 derivative of the formula ##STR1## (wherein R.sub.1 is hydrogen or a hydroxyl group) which exhibits strong biological activity like that of vitamin D and is useful as a medicine; and a process for producing the same are disclosed.
摘要翻译： 具有如维生素D的强生物活性的新颖维生素D3衍生物（其中R1是氢或羟基）可用作药物; 并公开了其制造方法。
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