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12 条记录 (耗时 0.014 秒)

    Method of producing a quinolonecarboxylic acid derivative
    1.
    发明授权
    Method of producing a quinolonecarboxylic acid derivative 失效
    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。

    Sucralfate aqueous suspension and its method of preparation
    2.
    发明授权
    Sucralfate aqueous suspension and its method of preparation 失效
    Sucralfate水悬浮液及其制备方法

    公开(公告)号：US5563258A

    公开(公告)日：1996-10-08

    申请号：US429512

    申请日：1995-04-26

    申请人： Kiyoshige Ochi ,  Kazuo Sasahara ,  Mituo Shiratori ,  Sakae Takaku

    发明人： Kiyoshige Ochi ,  Kazuo Sasahara ,  Mituo Shiratori ,  Sakae Takaku

    IPC分类号： A61K9/00 ,  A61K9/14 ,  A61K31/70 ,  C07H11/00 ,  A61K31/715 ,  C07H1/00

    CPC分类号： A61K9/0095 ,  A61K31/70 ,  A61K9/14 ,  C07H11/00

    摘要： This specification discloses a production process for an sucralfate aqueous suspension stock, the process being characterized by direct dispersement of an sucralfate aqueous stock for sucralfate preparations, which contains sucralfate particles with an average particle size of no more than 50 .mu.m in a concentration of 1-2 g/ml, in water or other aqueous medium without drying the synthesized sucralfate wet powder, followed by milling of the sucralfate particles to an average particle size of no more than 50 .mu.m. When the sucralfate aqueous suspension stock obtained directly from wet powder in accordance with this method is compared to the conventional suspension obtained from dry powder, equivalency of both stocks are obtained in terms of both properties and pharmacological activities. In comparison to the conventional process using dry powder, this wet milling method of production is economically and operationally superior and environmental pollution arising from the conventional process can be prevented.

    摘要翻译： 本说明书公开了硫糖铝水悬浮液的制备方法，该方法的特征在于用于硫糖铝制剂的硫糖铝水溶液的直接分散，其含有浓度为1的平均粒径不超过50μm的硫糖铝颗粒 -2g / ml，在水或其它水性介质中，不干燥合成的硫糖铝湿粉末，然后将硫糖铝粉末研磨至不超过50μm的平均粒度。 当将根据该方法直接从湿粉末获得的硫糖铝水性悬浮液与从干粉获得的常规悬浮液进行比较时，可以从性质和药理活性方面获得两种原料的等效性。 与使用干粉的常规方法相比，这种湿磨生产方法在经济上和操作上都是优越的，并且可以防止由常规方法引起的环境污染。

    22-oxacholecalciferol derivative and process for preparing the same
    4.
    发明授权
    22-oxacholecalciferol derivative and process for preparing the same 失效
    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。

    Vitamin D derivatives, process for producing the same and their use in the differentiation of tumor cells
    7.
    发明授权
    Vitamin D derivatives, process for producing the same and their use in the differentiation of tumor cells 失效
    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。

    Pentaerythritol derivative
    8.
    发明授权
    Pentaerythritol derivative 失效
    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。