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1. 发明授权

US5436401A 22-oxacholecalciferol derivative and process for preparing the same 失效
标题翻译： 22-氧代胆钙化甾醇衍生物及其制备方法
公开(公告)号：US5436401A
公开(公告)日：1995-07-25
申请号：US244818
申请日：1994-06-13
申请人： Masahiro Kato , Tetsuhiro Mikami , Kiyoshige Ochi , Hiroyoshi Watanabe , Noboru Kubodera
发明人： Masahiro Kato , Tetsuhiro Mikami , Kiyoshige Ochi , Hiroyoshi Watanabe , Noboru Kubodera
IPC分类号： A61K31/59 , A61P3/02 , A61P5/12 , A61P29/00 , A61P35/00 , C07C401/00 , C07J7/00 , C07J51/00 , C07J71/00 , C07J3/00 , C07J75/00
CPC分类号： C07C401/00 , C07J51/00 , C07J7/007 , C07J71/0042
摘要： A 22-oxacholecalciferol derivative represented by formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group; and R.sub.2 and R.sub.3, which may be the same or different, each represent a lower alkyl group having from 1 to 5 carbon atoms,and a process for preparing the same are disclosed. The compound of the present invention has potent differentiation inducing activity and cell proliferation inhibitory activity and is expected to be useful as an anti-tumor agent, an antirheumatic, a treating agent for psoriasis, and a treating agent for hyperparathyreosis. The process of the present invention makes it possible to efficiently produce a desired 22-oxacholecalciferol derivative while reducing by-production.
摘要翻译： PCT No.PCT / JP92 / 01662 Sec。 371日期1994年6月13日 102（e）日期1994年6月13日PCT 1992年12月18日PCT PCT。公开号WO93 / 12083 日本6月24日，1993.由式（I）表示的22-氧代胆钙化甾醇衍生物：其中R 1表示氢原子或羟基; 并且可以相同或不同的R 2和R 3各自表示具有1至5个碳原子的低级烷基，并且公开了其制备方法。本发明的化合物具有有效的分化诱导活性和细胞增殖抑制活性，并且预期可用作抗肿瘤剂，抗风湿剂，牛皮癣治疗剂和用于高血糖病的治疗剂。本发明的方法使得有可能有效地产生所需的22-氧代消化胆钙化醇衍生物，同时减少副产物。

2. 发明授权

US4415573A Novel uracil derivatives, process for preparing the same and a pharmaceutical composition containing the same 失效
标题翻译：新型尿嘧啶衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4415573A
公开(公告)日：1983-11-15
申请号：US291847
申请日：1981-08-10
申请人： Kiyoshige Ochi , Katsuhito Miyamoto , Hiroki Mitsui , Yumiko Tsuruma , Isao Matsunaga , Takashi Matsuno , Shigeru Takanashi , Minoru Shindo
发明人： Kiyoshige Ochi , Katsuhito Miyamoto , Hiroki Mitsui , Yumiko Tsuruma , Isao Matsunaga , Takashi Matsuno , Shigeru Takanashi , Minoru Shindo
IPC分类号： A61K31/505 , A61P35/00 , C07D239/54 , C07D239/553 , C07D405/06 , C07D239/10
CPC分类号： C07D239/54 , C07D239/553
摘要： Novel uracil derivatives of the formula ##STR1## (wherein R.sub.1, R.sub.2 R.sub.3 and X are defined in the description) and their pharmaceutically acceptable salts, process for preparing the same and pharmaceutical composition containing the same are disclosed. The uracil derivatives have good antitumor activity and, therefore, are useful as antitumor preparation.
摘要翻译：公开了新颖的式（ⅩⅧ）的尿嘧啶衍生物（其中R 1，R 2，R 3和X在说明书中定义）及其药学上可接受的盐，其制备方法和包含其的药物组合物。尿嘧啶衍生物具有良好的抗肿瘤活性，因此可用作抗肿瘤剂。

3. 发明授权

US4225524A Steroid derivatives and process for preparing the same 失效
标题翻译：类固醇衍生物及其制备方法
公开(公告)号：US4225524A
公开(公告)日：1980-09-30
申请号：US915988
申请日：1978-06-14
申请人： Kiyoshige Ochi , Isao Matsunaga , Minoru Shindo , Chikara Kaneko
发明人： Kiyoshige Ochi , Isao Matsunaga , Minoru Shindo , Chikara Kaneko
IPC分类号： C07J9/00
CPC分类号： C07J9/00 , C07J9/005
摘要： Steroid derivatives represented by the formula ##STR1## wherein R.sup.1 and R.sup.2 are as defined hereunder which is useful for easily producing a wide variety of active vitamin D, and a process for preparing the same are disclosed.
摘要翻译：由式“IMAGE”表示的类固醇衍生物，其中R1和R2如下文所定义，其可用于容易地生产各种活性维生素D及其制备方法。

4. 发明授权

US06335464B1 Process for selectively oxidizing primary hydroxyl groups of organic compounds, and resin containing adsorbed catalyst for use therein 失效
标题翻译：选择性氧化有机化合物的伯羟基和含有吸附催化剂的树脂用于其中的方法
公开(公告)号：US06335464B1
公开(公告)日：2002-01-01
申请号：US09508176
申请日：2000-03-08
申请人： Kiyoshige Ochi , Hidenori Takahashi , Hideki Tanaka , Hiroshi Sugiyama , Isao Fujisaki , Kazutomo Ori
发明人： Kiyoshige Ochi , Hidenori Takahashi , Hideki Tanaka , Hiroshi Sugiyama , Isao Fujisaki , Kazutomo Ori
IPC分类号： C07C2710
CPC分类号： B01J31/40 , B01J31/006 , B01J31/0235 , B01J31/08 , B01J2231/70
摘要： A method for selectively oxidizing the primary hydroxyl group of an organic compound which comprises reacting a resin having an amine oxide adsorbed thereon and an electrolytically oxidized product of a halogen-containing compound with the organic compound having the primary hydroxyl group.
摘要翻译：选择性氧化有机化合物的伯羟基的方法，其包括使其上吸附有氧化胺的树脂与含卤素化合物的电解氧化产物与具有伯羟基的有机化合物反应。

5. 发明授权

US5869661A Method of producing a quinolonecarboxylic acid derivative 失效
标题翻译：制备喹诺酮羧酸衍生物的方法
公开(公告)号：US5869661A
公开(公告)日：1999-02-09
申请号：US339404
申请日：1994-11-17
申请人： Kiyoshige Ochi , Hirohito Shimizu
发明人： Kiyoshige Ochi , Hirohito Shimizu
IPC分类号： C07D215/56 , C07D265/28 , C07D291/04 , C07D295/155
CPC分类号： C07D215/56 , C07D265/28 , C07D291/04 , C07D295/155
摘要： The present invention is a method of producing a 6-fluoro-7-substituted quinolonecarboxylic acid derivative represented by the general formula (4): ##STR1## wherein the variables are defined in the specification, which is characterized by adding an alkylboric acid ester represented by the general formula (3):B (OR.sub.5).sub.3 (3)wherein R.sub.5 represents a lower alkyl group, an aryl group, a substituted aryl group or a substituted aralkyl group to a 6-fluoroquinolonecarboxylic acid derivative represented by the general formula (1): ##STR2## wherein R.sub.1 and R.sub.2 are as defined in the specification; and R.sub.3 represents an optional, functional residue capable of participating in a nucleophilic substitution reaction, and a substituted saturated heterocyclic amine represented by the general formula (2): ##STR3## wherein X, Y and n are as defined in the specification, and condensing the reaction mixture with heating.
摘要翻译：本发明是由通式（4）表示的6-氟-7-取代喹诺酮羧酸衍生物的制造方法，其特征在于，加入通式（3）表示的烷基硼酸酯： B（OR 5）3（3）其中R 5表示通式（1）表示的6-氟喹诺酮羧酸衍生物的低级烷基，芳基，取代的芳基或取代的芳烷基：）其中R1和R2如说明书中所定义; 和R3表示任选的能够参与亲核取代反应的官能残基，以及由通式（2）表示的取代的饱和杂环胺：其中X，Y和n如说明书中所定义。，并加热反应混合物。

6. 发明授权

US4666634A vitamin D.sub.3 derivatives having a substituent at 2-position 失效
标题翻译：在2-位具有取代基的维生素D3衍生物
公开(公告)号：US4666634A
公开(公告)日：1987-05-19
申请号：US800320
申请日：1985-11-20
申请人： Katsuhito Miyamoto , Noboru Kubodera , Kiyoshige Ochi , Isao Matsunaga , Eigoro Murayama
发明人： Katsuhito Miyamoto , Noboru Kubodera , Kiyoshige Ochi , Isao Matsunaga , Eigoro Murayama
IPC分类号： A61K31/59 , A61P3/00 , A61P3/02 , A61P3/14 , C07C67/00 , C07C401/00 , C07J9/00 , C07J41/00 , C07J71/00
CPC分类号： C07J71/0042 , C07C401/00 , C07J41/0011 , C07J41/0027 , C07J71/001 , C07J9/00
摘要： A 1.alpha.-hydroxy vitamin D.sub.3 derivative of the formula: ##STR1## where R.sub.1 is a hydroxyl group, an amino group or the group: OR' (where R' is a lower alkyl group having 1 to 7 carbon atoms that may or may not be substituted by a hydroxyl group, a halogen atom, a cyano group, a lower alkoxy group having 1 to 3 carbon atoms, an amino group, or an acylamino group); R.sub.2 is a hydrogen atom or a hydroxyl group), and a process for preparing the same are disclosed.The compound represented by the formula above has the calcium control action and the ability to induce differentiation in tumor cells and, therefore, are useful as an antitumor agents and a medicine for treating calcium dysbolism-caused diseases.
摘要翻译： 1α-羟基维生素D3衍生物，其结构式如下：其中R1是羟基，氨基或基团：OR'（其中R'是具有1至7个碳原子的低级烷基，可以或可以不被羟基，卤素原子，氰基，具有1至3个碳原子的低级烷氧基，氨基或酰氨基取代）; R2是氢原子或羟基），以及其制备方法。由上式表示的化合物具有钙控制作用和诱导肿瘤细胞分化的能力，因此可用作抗肿瘤剂和用于治疗钙异常引起的疾病的药物。

7. 发明授权

US4022768A Process for preparation of 1.alpha.,25-dihydroxycholecalciferol 失效
标题翻译：制备1 {60,25-二羟基胆钙化甾醇的方法
公开(公告)号：US4022768A
公开(公告)日：1977-05-10
申请号：US657375
申请日：1976-02-12
申请人： Isao Matsunaga , Kiyoshige Ochi , Hiroyuki Nagano , Minoru Shindo , Masayuki Ishikawa , Chikara Kaneko , Hector F. DeLuca
发明人： Isao Matsunaga , Kiyoshige Ochi , Hiroyuki Nagano , Minoru Shindo , Masayuki Ishikawa , Chikara Kaneko , Hector F. DeLuca
IPC分类号： C07J9/00 , C07J71/00
CPC分类号： C07J71/0042 , C07J9/00
摘要： 1.alpha.,25-dihydroxycholecalciferol is prepared by reacting 1,5,7-trien-3.beta.,25-diol with a 1,2,4-triazoline-dione derivative represented by the formula: ##STR1## wherein R represents an alkyl group or an aryl or substituted-aryl group; reacting the resulting 1,4-cyclic adduct represented by the general formula ##STR2## wherein R is as defined above, with a peroxide to form a 1.alpha.,2.alpha.-epoxide compound represented by the general formula ##STR3## wherein R is as defined above, reducing the so formed compound with a metal hydride to form cholesta-5,7-diene-1.alpha.,3.beta.,25-triol, irradiating the so formed compound with ultraviolet rays to form 1.alpha.,25-dihydroxyprevitamin D.sub.3, isomerizing the so formed previtamin D.sub.3, and recovering 1.alpha.,25-dihydroxycholecalciferol.
摘要翻译： 1α，25-二羟基胆钙化醇通过使1,5,7-三烯-3β，25-二醇与下式表示的1,2,4-三唑啉二酮衍生物反应制备：其中R表示烷基或芳基或取代的芳基; 使得到的由通式“IMAGE”表示的所得1,4-环加成物与上述定义相同，与过氧化物反应，形成由通式“IMAGE”表示的1α，2α-环氧化合物，其中R为用金属氢化物还原形成的化合物以形成胆甾烯-5,7-二烯-1α，3β，25-三醇，用紫外线照射所形成的化合物以形成1α，25-二羟维生素D3，异构化所形成的维生素D3，并回收1α，25-二羟基胆钙化甾醇。

8. 发明授权

US4891364A Vitamin D derivatives, process for producing the same and their use in the differentiation of tumor cells 失效
标题翻译：维生素D衍生物，其制备方法及其在肿瘤细胞分化中的应用
公开(公告)号：US4891364A
公开(公告)日：1990-01-02
申请号：US211096
申请日：1988-06-13
申请人： Noboru Kubodera , Katsuhito Miyamoto , Kiyoshige Ochi , Isao Matsunaga , Eigoro Murayama
发明人： Noboru Kubodera , Katsuhito Miyamoto , Kiyoshige Ochi , Isao Matsunaga , Eigoro Murayama
IPC分类号： C07C401/00 , C07J7/00 , C07J41/00 , C07J51/00 , C07J71/00
CPC分类号： C07J7/002 , C07C401/00 , C07J41/005 , C07J51/00 , C07J7/007 , C07J71/0042
摘要： Vitamin D derivatives of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 which may be the same or different each represents a hydrogen atom or a hydroxyl group; X is an oxygen atom, the group of the formula OR.sub.4 (where R.sub.4 is either a hydrogen atom or a lower alkyl having 4 to 6 carbon atoms that may or may not be substituted by a hydroxyl group), or the group of the formula=N-OR.sub.5 (where R.sub.5 is either a hydrogen atom or a lower alkyl group having 1 to 5 carbon atoms that may or may not be substituted by a hydroxyl group, an amino group or a lower alkylamino group having 1 to 3 carbon atoms), provided that the carbon atom at 20-position is linked to X by a single bond when X is the group of the formula OR.sub.4, and by a double bond in other cases, and a process for preparing the derivatives are disclosed.The derivatives have both the immunoregulating action and the ability to induce differentiation in tumor cells and hence are useful as medicines such as antiallergic agents, antirheumatic agents and antitumor agents.
摘要翻译：其中R1，R2和R3可以相同或不同的维生素D衍生物表示氢原子或羟基; X是氧原子，式OR4（其中R4是氢原子或具有4-6个碳原子的低级烷基，可以被羟基取代或不被羟基取代）的基团，或式= N-OR5（其中R5为氢原子或碳原子数1〜5的低级烷基，可以被羟基，氨基或碳原子数1〜3的低级烷基氨基取代）条件是当X是式OR4的基团时，20位上的碳原子通过单键与X连接，并且在其它情况下通过双键，并且公开了制备衍生物的方法。所述衍生物具有免疫调节作用和在肿瘤细胞中诱导分化的能力，因此可用作药物如抗过敏剂，抗风湿剂和抗肿瘤剂。

9. 发明授权

US4650888A Pentaerythritol derivative 失效
标题翻译：季戊四醇衍生物
公开(公告)号：US4650888A
公开(公告)日：1987-03-17
申请号：US721850
申请日：1985-04-10
申请人： Kiyoshige Ochi , Yoshikazu Hinohara , Isao Matsunaga
发明人： Kiyoshige Ochi , Yoshikazu Hinohara , Isao Matsunaga
IPC分类号： A61K31/045 , A61K31/255 , A61P1/04 , C07C305/10 , C07F5/06
CPC分类号： C07F5/069 , C07C303/24
摘要： Complexes of pentaerythritol derivatives such as sulfuric acid ester of pentaerythritol or dipentaerythritol with a basic polyaluminum chloride and process for preparing the same are disclosed. The complex is novel and has a good anti-pepsin activity and therefore it is useful as an anti-ulcer agent.The complex is prepared by reacting pentaerythritol or dipentaerythritol with a sulfating agent and then reacting the resulting sulfate with a basic polyaluminum chloride.
摘要翻译：公开季戊四醇衍生物如季戊四醇或二季戊四醇硫酸酯与碱式聚氯化铝的配合物及其制备方法。该复合物是新颖的，具有良好的抗胃蛋白酶活性，因此可用作抗溃疡剂。该复合物通过使季戊四醇或二季戊四醇与硫酸化剂反应，然后使得到的硫酸盐与碱性聚氯化铝反应来制备。

10. 发明授权

US4179452A 3.alpha.,6.alpha.-Dihydroxy-5.beta.-cholestan-24-one derivatives and process for preparing the same 失效
标题翻译： 3α，6α-二羟基-5β-胆甾烷二酮-24衍生物及其制备方法
公开(公告)号：US4179452A
公开(公告)日：1979-12-18
申请号：US906866
申请日：1978-05-17
申请人： Kiyoshige Ochi , Isao Matsunaga , Minoru Shindo , Chikara Kaneko
发明人： Kiyoshige Ochi , Isao Matsunaga , Minoru Shindo , Chikara Kaneko
IPC分类号： C07J9/00 , C07J31/00
CPC分类号： C07J31/006 , C07J9/00 , C07J9/005
摘要： 3.alpha.,6.alpha.-Dihydroxy-5.beta.-cholestan-24-one or its derivative represented by the formula ##STR1## wherein R is as defined hereunder which is a useful intermediate for the production of an active vitamin D, and a process for preparing the compound of the formula are disclosed.
摘要翻译： 3α，6α-二羟基-5β-胆固醇-24-或其衍生物，其由下式定义，其中R如下文所定义，其为生产活性维生素D的有用中间体，以及用于公开了制备式的化合物。

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