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1.发明授权Novel 1.alpha.,24-dihydroxycholecalciferol compositions, novel precursors thereof, and processes for preparing them 失效新型1 {60,24-二羟基胆钙化甾醇组合物，其新型前体及其制备方法
公开(公告)号：US4022891A
公开(公告)日：1977-05-10
申请号：US583115
申请日：1975-06-02
申请人： Toru Takeshita , Yoshinobu Hashimoto , Hiroyuki Kawashima , Sachio Ishimoto , Nobuo Ikekawa , Masuo Morisaki
发明人： Toru Takeshita , Yoshinobu Hashimoto , Hiroyuki Kawashima , Sachio Ishimoto , Nobuo Ikekawa , Masuo Morisaki
CPC分类号： C07J9/00 , A23K20/174 , C07J71/001 , Y02P20/55
摘要： Novel 1.alpha., 24-dihydroxycholecalciferol and derivatives thereof which are useful with reduced side-effects for the treatment of abnormal metabolism of calcium and phosphorus caused by liver failure, renal failure, gastrointestinal tract failure and parathyroid failure, and related bone diseases. Preparation of the novel 1.alpha., 24-dihydroxycholecalciferol and their derivatives starts from 1.alpha., 24-dihydroxycholesterol prepared by reacting 1.alpha., 2.alpha.-epoxy-24-keto-cholesta-4,6-dien-3-one with an alkali metal and a proton donor in the presence of liquid ammonia or a liquid amine. Reaction of the 1.alpha., 24-dihydroxycholesterol with an allylic brominating agent, followed by contacting with a dehydrobrominating agent, affords 1.alpha.,3.beta., 24-trihydroxycholesta-5,7-diene derivative, which can then be converted to 1.alpha., 24-dihydroxycholocalciferol by ultraviolet irradiation in a organic solvent, followed by isomerization. Processes are also provided for separating 1.alpha., 24-dihydroxycholesterol into an (S)-epimer and an (R)-epimer, and also for separating at least one of 1.alpha., 3.beta., 24(S)-and 1.alpha., 3.beta., 24(R)-trihydroxycholesta-5,7-dienes from trihydroxycholesta-4,6-diene.
摘要翻译： 用于治疗由肝衰竭，肾衰竭，胃肠道衰竭和甲状旁腺功能衰竭引起的钙和磷的异常代谢的副作用的新型1α，24-二羟基胆钙化甾醇及其衍生物以及相关的骨疾病。 1α，24-二羟基胆钙化甾醇及其衍生物的制备从1α，24-二羟基胆固醇开始，其通过使1α，2α-环氧-24-酮 - 胆甾烯-4,6-二烯-3-酮与碱 金属和质子供体在液态氨或液态胺存在下进行。 1α，24-二羟基胆固醇与烯丙基溴化剂的反应，然后与脱氢溴化剂接触，得到1α，3β，24-三羟基胆甾-5,7-二烯衍生物，然后将其转化为1α， 通过紫外线照射在有机溶剂中进行异构化，得到24-二羟基胆钙化甾醇。 还提供了用于将1α，24-二羟基胆固醇分离成（S） - 对映体和（R） - 对映体的方法，还用于分离1α，3β，24（S） - 和1α， 3β，24（R） - 三羟基胆甾-5,7-二烯的三羟基胆甾-4,6-二烯。
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2.发明授权Novel 1.alpha.-hydroxy-24-oxovitamin D.sub.3, its preparing process and the novel precursors thereof 失效新型1α-羟基-24-氧维生素D3，其制备方法及其新型前体
公开(公告)号：US4199577A
公开(公告)日：1980-04-22
申请号：US939043
申请日：1978-09-01
申请人： Toru Takeshita , Takao Niki , Hiroyuki Kawashima , Kiyoshi Bannai
发明人： Toru Takeshita , Takao Niki , Hiroyuki Kawashima , Kiyoshi Bannai
摘要： Novel 1.alpha.,3.beta.-dihydroxy-24-oxocholesta-5,7-diene and the hydroxyl group-protected derivatives thereof.Said novel 1.alpha.-hydroxy-24-oxovitamin D.sub.3 and said novel intermediates are also useful as the intermediates of 1.alpha.,24-dihydroxyvitamin D.sub.3.1.alpha.,3.beta.-Dihydroxy-24-oxocholesta-5,7-diene and the hydroxyl group-protected derivatives thereof are prepared from fucosterol via 1.alpha.,3.beta.-diprotected hydroxy-24(24)-ethylenedioxycholest-5-ene. 1.alpha.-hydroxy-24-oxovitamin D.sub.3 is prepared by irradiation with ultraviolet rays to 1.alpha.,3.beta.-dihydroxy-24-oxocholesta-5,7-diene or a hydroxyl group-protected derivatives thereof, isomerization using heat energy, and, when necessary, elimination of the protecting groups.
摘要翻译： 新的1α，3β-二羟基-24-氧代胆甾-5,7-二烯及其羟基保护的衍生物。 所述新型1α-羟基-24-氧维生素D3和所述新型中间体也可用作1α，24-二羟基维生素D3的中间体。 1α，3β-二羟基-24-氧代胆甾烯-5,7-二烯及其羟基保护的衍生物通过1α，3β-双保护的羟基-24（24） - 亚乙基二氧胆甾-5-烯由岩藻甾醇制备。 1α-羟基-24-氧代维生素D3通过用1α，3β-二羟基-24-氧代胆甾烯-5,7-二烯或其羟基受保护的衍生物用紫外线照射制备，使用热能异构化， 必要时消除保护基团。
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公开(公告)号：US4305935A
公开(公告)日：1981-12-15
申请号：US196223
申请日：1980-04-09
IPC分类号： A61K31/59 , A61K31/60 , A61P3/02 , A61P3/14 , A61K31/605
CPC分类号： A61K31/60
摘要： This is a bone formation stimulant containing vitamin D.sub.3 or its derivative and acetylsalicylic acid or its formaceutically permissible salt. The present bone formation stimulant is used to cure or prevent the diseases caused by the deficiency of vitamin D or related diseases by dosing human beings or animals with it.
摘要翻译： 这是含有维生素D3或其衍生物和乙酰水杨酸或其营养允许的盐的骨形成兴奋剂。 目前的骨形成兴奋剂用于通过给予人或动物来治疗或预防由维生素D缺乏引起的疾病或相关疾病。
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4.发明授权公开(公告)号：US07537341B2
公开(公告)日：2009-05-26
申请号：US12048095
申请日：2008-03-13
申请人： Noriko Saito , Akio Kobayashi , Hiroyuki Kawashima
发明人： Noriko Saito , Akio Kobayashi , Hiroyuki Kawashima
CPC分类号： G02B26/06 , A61B3/1015 , A61B3/14 , G02B26/0825
摘要： A wavefront aberration compensating apparatus, which includes: a deformable mirror having electrodes and a thin-film mirror; an optical system provided with the deformable mirror and including an object; a wavefront sensor which measures a wavefront aberration of a light flux; and a controller configured to: calculate a first voltage value applied to each of the electrodes, on the basis of differences between application points on the thin-film mirror and target points both corresponding to the electrodes respectively; determine a superposition amplitude value of each expansion mode according to a polynomial of wavefront aberration, and calculate a second voltage value applied to each of the electrodes by using voltage templates previously stored, such that the wavefront aberration obtained by the wavefront sensor becomes a desired aberration; determine the voltage value applied to each of the electrodes, by mainly using the second voltage value in an initial stage of compensation of the configuration of the thin-film mirror and by mainly using the first voltage value in an end stage of the compensation; and repeat the compensation on the basis of the determined voltage value, such that the wavefront aberration of the light flux is suppressed.
摘要翻译： 一种波前像差补偿装置，包括：具有电极和薄膜反射镜的可变形反射镜; 设置有可变形反射镜并包括物体的光学系统; 测量光通量的波前像差的波前传感器; 以及控制器，其被配置为：基于薄膜反射镜上的应用点和分别对应于电极的目标点之间的差异来计算施加到每个电极的第一电压值; 根据波前像差的多项式确定每个扩展模式的叠加振幅值，并且通过使用预先存储的电压模板来计算施加到每个电极的第二电压值，使得由波前传感器获得的波前像差成为期望的像差 ; 通过在补偿薄膜反射镜的构造的初始阶段主要使用第二电压值，并且主要在补偿的最后阶段使用第一电压值来确定施加到每个电极的电压值; 并根据确定的电压值重复补偿，从而抑制光通量的波前像差。
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5.发明授权公开(公告)号：US07520613B2
公开(公告)日：2009-04-21
申请号：US12047946
申请日：2008-03-13
申请人： Noriko Saito , Akio Kobayashi , Hiroyuki Kawashima
发明人： Noriko Saito , Akio Kobayashi , Hiroyuki Kawashima
CPC分类号： G02B26/06 , A61B3/1015 , A61B3/12
摘要： A wavefront aberration compensating apparatus, including: a deformable mirror which compensates a wavefront aberration of a light flux and includes electrodes, and a thin-film mirror which changes a configuration thereof in accordance with a voltage value applied to each of the electrodes; an optical system provided with the deformable mirror and including an object subjected to aberration compensation; a wavefront sensor which measures the wavefront aberration of the light flux; a memory which stores therein a voltage template provided for each expansion mode according to a polynomial of wavefront aberration, as a voltage alignment data for the electrodes which induces the corresponding expansion mode; and a controller configured to determine a superposition amplitude value of each of the expansion modes and calculate the voltage value applied to each of the electrodes by using the voltage templates stored such that the wavefront aberration obtained by the wavefront sensor becomes a desired aberration, and to repeat compensation of the configuration of the thin-film mirror on the basis of the calculated voltage value, such that the wavefront aberration of the light flux measured by the wavefront sensor is suppressed.
摘要翻译： 一种波前像差补偿装置，包括：可变形反射镜，其补偿光束的波前像差并包括电极;以及薄膜反射镜，其根据施加到每个电极的电压值改变其配置; 设置有可变形反射镜并包括经受像差补偿的物体的光学系统; 测量光通量波前像差的波前传感器; 存储器，其中存储根据波前像差的多项式为每个扩展模式提供的电压模板作为引起相应扩展模式的电极的电压对准数据; 以及控制器，被配置为确定每个扩展模式的叠加振幅值，并且通过使用存储的电压模板来计算施加到每个电极的电压值，使得由波前传感器获得的波前像差成为期望的像差，并且 基于计算出的电压值重复补偿薄膜反射镜的结构，从而抑制由波前传感器测量的光通量的波前像差。
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公开(公告)号：US20080239528A1
公开(公告)日：2008-10-02
申请号：US12032871
申请日：2008-02-18
申请人： Kei Masunishi , Akihiro Koga , Ryo Furukawa , Tetsuya Kugimiya , Akio Kobayashi , Hiroyuki Kawashima
发明人： Kei Masunishi , Akihiro Koga , Ryo Furukawa , Tetsuya Kugimiya , Akio Kobayashi , Hiroyuki Kawashima
IPC分类号： G02B26/00
CPC分类号： G02B26/0825
摘要： It is made possible to provide a deformable mirror apparatus which is deformable to a complicated shape (high-order shape). A deformable mirror apparatus includes: a substrate; a plurality of electrodes provided on the substrate; a spacer fixed above the substrate, having a first opening passing through from a first face of the spacer facing to the substrate to a second face of the spacer facing opposite from the first face, surrounding the electrodes, and having a step on the second face; a drive part including a membrane part disposed so as to cover the step of the spacer and so as to be opposed to the electrodes, a casing part having an opening at a bottom face of which the membrane part is exposed and supporting the membrane part, and a reflection film provided on the membrane part; and a voltage generator configured to generate predetermined voltage patterns on the electrodes, respectively.
摘要翻译： 可以提供可变形为复杂形状（高阶形状）的可变形反射镜装置。 可变形反射镜装置包括：基板; 设置在所述基板上的多个电极; 固定在所述基板上方的间隔件，具有第一开口，所述第一开口从所述间隔件的面向所述基板的第一面穿过所述间隔件的与所述第一面相反的第二面，所述第二面围绕所述电极，并且在所述第二面上具有台阶 ; 驱动部，其具有设置成覆盖所述间隔件的台阶并且与所述电极相对的膜部;壳体部，其在所述膜部露出并支撑所述膜部的底面具有开口部， 以及设置在所述膜部上的反射膜; 以及电压发生器，其被配置为分别在所述电极上产生预定的电压图案。
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公开(公告)号：US20080225228A1
公开(公告)日：2008-09-18
申请号：US12047946
申请日：2008-03-13
申请人： Noriko Saito , Akio Kobayashi , Hiroyuki Kawashima
发明人： Noriko Saito , Akio Kobayashi , Hiroyuki Kawashima
CPC分类号： G02B26/06 , A61B3/1015 , A61B3/12
摘要： A wavefront aberration compensating apparatus, including: a deformable mirror which compensates a wavefront aberration of a light flux and includes electrodes, and a thin-film mirror which changes a configuration thereof in accordance with a voltage value applied to each of the electrodes; an optical system provided with the deformable mirror and including an object subjected to aberration compensation; a wavefront sensor which measures the wavefront aberration of the light flux; a memory which stores therein a voltage template provided for each expansion mode according to a polynomial of wavefront aberration, as a voltage alignment data for the electrodes which induces the corresponding expansion mode; and a controller configured to determine a superposition amplitude value of each of the expansion modes and calculate the voltage value applied to each of the electrodes by using the voltage templates stored such that the wavefront aberration obtained by the wavefront sensor becomes a desired aberration, and to repeat compensation of the configuration of the thin-film mirror on the basis of the calculated voltage value, such that the wavefront aberration of the light flux measured by the wavefront sensor is suppressed.
摘要翻译： 一种波前像差补偿装置，包括：可变形反射镜，其补偿光束的波前像差并包括电极;以及薄膜反射镜，其根据施加到每个电极的电压值改变其结构; 设置有可变形反射镜并包括经受像差补偿的物体的光学系统; 测量光通量波前像差的波前传感器; 存储器，其中存储根据波前像差的多项式为每个扩展模式提供的电压模板作为引起相应扩展模式的电极的电压对准数据; 以及控制器，被配置为确定每个扩展模式的叠加振幅值，并且通过使用存储的电压模板来计算施加到每个电极的电压值，使得由波前传感器获得的波前像差成为期望的像差，并且 基于计算出的电压值重复补偿薄膜反射镜的结构，从而抑制由波前传感器测量的光通量的波前像差。
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公开(公告)号：US20080158508A1
公开(公告)日：2008-07-03
申请号：US12005275
申请日：2007-12-27
IPC分类号： A61B3/14
CPC分类号： A61B3/14
摘要： An ophthalmologic apparatus includes an imaging system that illuminates a retina of an eye, and images the retina of the eye based on reflective luminous flux from the retina, an aberration measurement part that measures optical aberration of the eye, an aberration compensation device disposed in the imaging system to compensate the optical aberration of the eye based on a signal from the aberration measurement part, a first focusing device disposed in an optical path of the imaging system to perform focusing of the image of the retina of the eye according to a refractive property of the eye, and a second focusing device disposed in the optical path of the imaging system to compensate infinitesimal spherical aberration generated by the aberration compensation device after adjustment by the first focusing device.
摘要翻译： 眼科装置包括：照射眼睛的视网膜的成像系统，并且基于来自视网膜的反射光束对眼睛的视网膜进行成像，测量眼睛的光学像差的像差测量部，设置在眼睛中的像差补偿装置 成像系统，用于基于来自像差测量部分的信号补偿眼睛的光学像差;第一聚焦装置，其设置在成像系统的光路中，以根据折射特性进行眼睛的视网膜的图像的聚焦; 以及设置在成像系统的光路中的第二聚焦装置，以补偿由第一聚焦装置调节之后由像差补偿装置产生的无穷小的球面像差。
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9.发明申请Pharmaceutical composition containing 2,2-dichloro-12-(4-chlorophenyl)-dodecanoic acid 审中-公开含有2,2-二氯-12-（4-氯苯基） - 十二烷酸的药物组合物公开(公告)号：US20060051410A1
公开(公告)日：2006-03-09
申请号：US10500463
申请日：2003-01-15
CPC分类号： A61K31/192 , A61K9/2054 , A61K9/4866 , A61K2300/00
摘要： A highly stable pharmaceutical composition which comprises a mixture comprising a substance selected from the group consisting of 2,2-dichloro-12-(4-chlorophenyl)-dodecanoic acid, salts thereof, and esters thereof, and croscarmellose sodium.
摘要翻译： 一种高度稳定的药物组合物，其包含包含选自2,2-二氯-12-（4-氯苯基） - 十二烷酸及其盐及其酯的物质和交联羧甲基纤维素钠的混合物。
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公开(公告)号：US06753330B2
公开(公告)日：2004-06-22
申请号：US10414008
申请日：2003-04-16
IPC分类号： A61K3150
CPC分类号： A61K9/1652 , A61K9/146 , A61K9/1641 , A61K9/2077 , A61K31/50
摘要： The invention provides a solid dispersion composition containing 2-benzyl-5-(4-chlorophenyl)-6-[4-(methylthio)phenyl]-2H-pyridazin-3-one, hydroxypropylmethyl cellulose, and polyoxyethylene polyoxypropylene glycol. The solid dispersion composition of the present invention exhibits the excellent dissolvability of 2-benzyl-5-(4-chlorophenyl)-6-[4-(methylthio)phenyl]-2H-pyridazin-3-one in water, and enables this compound to be constant sequentially and thereby improve absorbability in blood.
摘要翻译： 本发明提供了含有2-苄基-5-（4-氯苯基）-6- [4-（甲硫基）苯基] -2H-哒嗪-3-酮，羟丙基甲基纤维素和聚氧乙烯聚氧丙烯二醇的固体分散体组合物。 本发明的固体分散体组合物表现出2-苄基-5-（4-氯苯基）-6- [4-（甲硫基）苯基] -2H-哒嗪-3-酮在水中的优异的溶解性，使该化合物 依次保持恒定，从而提高血液中的吸收性。
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