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1. 发明授权

US07645864B2 Erythromycin derivative having novel crystal structures and processes for their production 失效
标题翻译：具有新晶体结构的红霉素衍生物及其生产方法
公开(公告)号：US07645864B2
公开(公告)日：2010-01-12
申请号：US10399146
申请日：2001-10-12
申请人： Akira Hiraide , Kaichiro Koyama , Hitoshi Shimizu , Kaname Tsuzaki
发明人： Akira Hiraide , Kaichiro Koyama , Hitoshi Shimizu , Kaname Tsuzaki
IPC分类号： C07H17/08
CPC分类号： C07H17/08 , A61K31/351 , A61K31/7048
摘要： The present invention provides an E-type crystal of N-demethyl-N-isopropyl-12-methoxy-11-oxo-8,9-anhydroerythromycin A-6,9-hemiacetal fumarate having strong diffraction peaks at diffraction angles (2θ) of 5.6° and 10.4° as measured by powder X-ray diffractometry, which is prepared by treating a C-type crystal of the compound in a mixed solvent of ethyl acetate and water at 20° C. to 40° C., and a D-type crystal prepared via the E-type crystal. These crystals have a reduced content of residual solvent and high suitability for formulation.
摘要翻译：本发明提供了N-去甲基-N-异丙基-12-甲氧基-11-氧代-8,9-去盐酸红霉素A-6,9-半缩醛富马酸盐的E型晶体，其衍射角（2θ）为通过粉末X射线衍射法测定的5.6°和10.4°，其通过在20℃至40℃下在乙酸乙酯和水的混合溶剂中处理化合物的C型晶体和D 型晶体通过E型晶体制备。这些晶体的残留溶剂含量降低，制剂适用性高。

2. 发明授权

US06897299B2 Process for producing erythromycin derivative 失效
标题翻译：红霉素衍生物的制备方法
公开(公告)号：US06897299B2
公开(公告)日：2005-05-24
申请号：US10363318
申请日：2001-08-31
申请人： Hitoshi Shimizu , Kaname Tsuzaki , Mitsuhiro Kurita
发明人： Hitoshi Shimizu , Kaname Tsuzaki , Mitsuhiro Kurita
IPC分类号： A61P1/00 , C07H17/08 , C07H1/00
CPC分类号： A61K31/7048 , C07H17/08
摘要： A method for preparing a fumarate salt of a compound represented by Formula (II): (wherein R1 represents a hydrogen atom or a lower alkyl group, and R2 represents a lower alkyl group), which comprises carbamating a compound represented by Formula (I): (wherein R1 represents a hydrogen atom or a lower alkyl group), removing all carbamate groups from this compound, alkylating the nitrogen atom at the 3′-position of the desosamine ring in the resulting compound to give the compound represented by Formula (II), and converting this compound into a fumarate salt, wherein the compound represented by Formula (I) is carbamated in the presence of a cyclic ether or a carboxylic ester. This method enables efficient preparation of high-quality erythromycin derivatives.
摘要翻译：一种制备由式（II）表示的化合物的富马酸盐的方法：其中R 1表示氢原子或低级烷基，R 2表示低级烷基），其包括将式（I）表示的化合物氨基甲酸酯化：（其中R 1表示氢原子或低级烷基），从该化合物中除去所有氨基甲酸酯基团，将氮烷基化（II）表示的化合物，并将该化合物转化成富马酸盐，其中式（I）所示的化合物在氨基甲酸酯化反应的存在下进行氨基甲酸酯化反应环醚或羧酸酯。该方法能够高效地制备高品质的红霉素衍生物。

3. 发明授权

US06767998B2 Method for preparing purified erythromycin 失效
标题翻译：纯化红霉素的制备方法
公开(公告)号：US06767998B2
公开(公告)日：2004-07-27
申请号：US10239523
申请日：2002-09-23
申请人： Kaname Tsuzaki , Megumi Ishii
发明人： Kaname Tsuzaki , Megumi Ishii
IPC分类号： C07H100
CPC分类号： A61K31/7048 , C07H17/08
摘要： The object of the present invention is to prepare purified erythromycin by removing erythromycin F from erythromycin. The present invention provides a method for preparing purified erythromycin from which erythromycin F is removed, which comprises the step of extracting erythromycin F from erythromycin using (i) an organic solvent and (ii) water or an aqueous solution of an inorganic and/or organic material.
摘要翻译：本发明的目的是通过从红霉素中除去红霉素F来制备纯化的红霉素。本发明提供一种从红霉素F中除去红霉素F的纯化红霉素的制备方法，该方法包括使用以下步骤从红霉素中提取红霉素F：（i）有机溶剂和（ii）水或无机和/或有机材料的水溶液。

4. 发明授权

US06902654B2 Ultraviolet irradiation apparatus for photochemical reaction and preparation process of vitamin D derivative making use of the same 有权
标题翻译：用于光化学反应的紫外线照射装置和使用其的维生素D衍生物的制备方法
公开(公告)号：US06902654B2
公开(公告)日：2005-06-07
申请号：US10727507
申请日：2003-12-05
申请人： Tadao Michishita , Satoshi Watanabe , Masahiro Katoh , Tetsuhiro Mikami , Kaname Tsuzaki , Koji Oikawa , Makoto Uehara
发明人： Tadao Michishita , Satoshi Watanabe , Masahiro Katoh , Tetsuhiro Mikami , Kaname Tsuzaki , Koji Oikawa , Makoto Uehara
IPC分类号： B01J19/12 , C07C401/00
CPC分类号： C07C401/00 , B01J19/123
摘要： A process for preparing a vitamin D derivative including providing an ultraviolet irradiation apparatus for photochemical reactions, which has an ultraviolet radiation-emitting lamp, an optical system which receives light from the ultraviolet radiation-emitting lamp and emits ultraviolet rays having a specific wavelength, and a quartz rod which receives the ultraviolet rays having the specific wavelength from the optical system and emits the ultraviolet rays, irradiating a solution of a provitamin D derivative with the ultraviolet rays emitted from the quartz rod to cause a photochemical reaction to the provitamin D derivative solution, thereby forming a previtamin D derivative, and subjecting the previtamin D derivative to a thermal isomerization reaction to prepare the vitamin D derivative.
摘要翻译：一种制备维生素D衍生物的方法，包括提供具有紫外线发射灯的光化学反应的紫外线照射装置，从紫外线发射灯接收光并发射具有特定波长的紫外线的光学系统，以及接收来自光学系统的具有特定波长的紫外线并发射紫外线的石英棒，照射由维生素D衍生物的溶液与从石英棒发射的紫外线引起对维生素D衍生物溶液的光化学反应，从而形成上维生素D衍生物，并将上维生素D衍生物进行热异构化反应以制备维生素D衍生物。

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