MAG expression promoters
    1.
    发明申请
    MAG expression promoters 有权
    MAG表达启动子

    公开(公告)号:US20050090531A1

    公开(公告)日:2005-04-28

    申请号:US10969885

    申请日:2004-10-22

    摘要: The MAG expression promoter of the present invention contains a compound of the formula (I) wherein each symbol is as defined in the specification, an optically active form thereof or a pharmaceutically acceptable salt thereof. As a compound of the formula (1), 4-[α-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid is exemplified. The MAG expression promoter of the present invention is useful as an agent for the prophylaxis and/or treatment of a disease of mammals inclusive of humans, which mainly presents hypomyelination, further, dysmyelination or demyelination.

    摘要翻译: 本发明的MAG表达启动子含有式(I)化合物,其中每个符号如说明书中所定义,其光学活性形式或其药学上可接受的盐。 作为式(1)的化合物,例举了4- [α-羟基-5-(1-咪唑基)-2-甲基苄基] -3,5-二甲基苯甲酸。 本发明的MAG表达启动子可用作预防和/或治疗包括人类在内的哺乳动物疾病的药剂,其主要表现为脱髓鞘,进一步发生脱髓鞘或脱髓鞘。

    MAG expression promoters
    3.
    发明申请
    MAG expression promoters 审中-公开
    MAG表达启动子

    公开(公告)号:US20060270712A1

    公开(公告)日:2006-11-30

    申请号:US11499785

    申请日:2006-08-07

    IPC分类号: A61K31/4439 A61K31/4164

    摘要: The MAG expression promoter of the present invention contains a compound of the formula (I) wherein each symbol is as defined in the specification, an optically active form thereof or a pharmaceutically acceptable salt thereof. As a compound of the formula (I), 4-[α-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid is exemplified. The MAG expression promoter of the present invention is useful as an agent for the prophylaxis and/or treatment of a disease of mammals inclusive of human, which mainly presents hypomyelination, further, dysmyelination or demyelination.

    摘要翻译: 本发明的MAG表达启动子含有式(I)化合物,其中每个符号如说明书中所定义,其光学活性形式或其药学上可接受的盐。 作为式(I)的化合物,例举了4- [α-羟基-5-(1-咪唑基)-2-甲基苄基] -3,5-二甲基苯甲酸。 本发明的MAG表达启动子可用作预防和/或治疗包括人类在内的哺乳动物疾病的药剂,其主要表现为鞘内脱髓鞘,进一步脱髓鞘或脱髓鞘。

    Device for drawing drawable thermoplastic resin material
    4.
    发明授权
    Device for drawing drawable thermoplastic resin material 有权
    拉拔可拉伸热塑性树脂材料的装置

    公开(公告)号:US06406283B1

    公开(公告)日:2002-06-18

    申请号:US09622841

    申请日:2000-08-24

    IPC分类号: B29C5502

    摘要: A drawing device for handling a wide range of drawable thermoplastic resin materials including a first pressurizing tank and first buffer tank on an upstream side, and a second pressurizing tank and second buffer tank on a downstream side are disposed along a drawing tank having pressurized steam and a discharge unit connected to it. A medium supply and discharge may be connected to each of the first and second pressurizing tanks, and the first and second buffer tanks. Opening members may be disposed on respective upstream and downstream ports along the drawing tank. Small amounts of pressurizing medium may then be allowed to flow into the drawing tank through upstream and downstream ports. Next, material may be supplied from the upstream port into the drawing tank where pressurized steam may be introduced in airtight conditions, and then drawn to the downstream port, thereby producing a drawable thermoplastic resin material.

    摘要翻译: 一种用于处理各种可拉伸热塑性树脂材料的拉丝装置,其具有上游侧的第一加压槽和第一缓冲罐,以及下游侧的第二加压槽和第二缓冲罐,沿着具有加压蒸汽的拉伸槽, 与其连接的排出单元。 中等供给和排出可以连接到第一和第二加压罐以及第一和第二缓冲罐中的每一个。 打开构件可以沿着拉伸槽布置在相应的上游和下游端口上。 然后允许少量的加压介质通过上游和下游端口流入拉伸槽。 接下来,可以将材料从上游端口供给到可在气密条件下引入加压蒸汽的拉伸槽中,然后被吸入下游端口,由此制造可拉伸的热塑性树脂材料。

    Imidazole derivatives
    5.
    发明授权
    Imidazole derivatives 失效
    咪唑衍生物

    公开(公告)号:US4581369A

    公开(公告)日:1986-04-08

    申请号:US556231

    申请日:1983-10-31

    摘要: An imidazole derivative of the formula: ##STR1## wherein each of R.sup.1 and R.sup.4 is a hydrogen atom or a lower alkyl group; each of R.sup.2 and R.sup.3 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, an aralkyloxy group, a nitro group or an amino group; A is --O--, --S--, --CH.dbd.CH-- pr --CH.dbd.N--; Z is an aryl group, a thienyl group, a pyridyl group or a furyl group, in which definition these aromatic (heterocyclic) rings may have 1 to 3 substituents, each substituent being independently selected from a halogen atom, a lower alkyl group, a cyclic alkyl group, a lower alkoxy group, a hydroxyl group, a carboxyl group, a lower alkoxycarbonyl group, a carboxy-lower-alkoxy group, a di-lower-alkylamino-lower-alkoxy group and a nitro group; and a pharmaceutically acceptable acid addition salt thereof, a method for preparing the same and a pharmaceutical composition containing such compound. Such compounds have inhibitory activities on biosynthesis of thromboxane A.sub.2, inhibitory activities on platelet aggregation, vasodilative activities and protective effects on liver disorders.

    摘要翻译: PCT No.PCT / JP83 / 00060 Sec。 371日期:1983年10月31日 102(e)1983年10月31日日期PCT提交1983年2月28日PCT公布。 出版物WO83 / 03096 日期:1983年9月15日。下式的咪唑衍生物:其中R 1和R 4各自为氢原子或低级烷基; R2和R3各自为氢原子,卤素原子,羟基,低级烷基,低级烷氧基,芳烷氧基,硝基或氨基; A是-O - , - S - , - CH = CH-Pr -CH = N-; Z是芳基,噻吩基,吡啶基或呋喃基,其中这些芳族(杂环)环可以具有1至3个取代基,每个取代基独立地选自卤素原子,低级烷基, 羟基,羧基,低级烷氧基羰基,羧基 - 低级烷氧基,二低级烷基氨基 - 低级烷氧基和硝基; 及其药学上可接受的酸加成盐,其制备方法和含有该化合物的药物组合物。 这些化合物对凝血恶烷A2的生物合成,对血小板聚集的抑制活性,血管扩张活性和对肝脏疾病的保护作用具有抑制活性。

    Production method of optically active imidazole compound, synthetic
intermediate therefor and production method thereof
    6.
    发明授权
    Production method of optically active imidazole compound, synthetic intermediate therefor and production method thereof 失效
    光学活性咪唑化合物的制备方法及其合成中间体及其制备方法

    公开(公告)号:US6166221A

    公开(公告)日:2000-12-26

    申请号:US511782

    申请日:2000-02-23

    摘要: The present invention provides a method for producing an optically active 4-[.alpha.-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid or a pharmaceutically acceptable salt thereof, which includes subjecting a compound of the formula (I) wherein each symbol in the formula is as defined in the specification, to optical resolution by fractional crystallization to give an optically active compound thereof and subjecting the compound to hydrolysis reaction. According to this method, a resolution method useful for industrial large-scale production of the optically active compound of 4-[.alpha.-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid, which is useful as a thromboxane synthetase inhibitor and an agent for the prophylaxis and treatment of diabetic complications, can be obtained.

    摘要翻译: 本发明提供了一种制备光学活性的4- [α-羟基-5-(1-咪唑基)-2-甲基苄基] -3,5-二甲基苯甲酸或其药学上可接受的盐的方法,其包括使 其中式中每个符号如本说明书中所定义的式(I)通过分级结晶得到其光学活性化合物并使该化合物进行水解反应的光学拆分。 根据该方法,可以用于工业大规模生产4- [α-羟基-5-(1-咪唑基)-2-甲基苄基] -3,5-二甲基苯甲酸的光学活性化合物的分辨方法,其为 可用作血栓素合成酶抑制剂和用于预防和治疗糖尿病并发症的药剂。

    Process for producing optically active imidazole compounds,
intermediates for synthesizing the same, and process for producing the
same
    7.
    发明授权
    Process for producing optically active imidazole compounds, intermediates for synthesizing the same, and process for producing the same 失效
    光学活性咪唑化合物的制造方法,其合成用中间体及其制造方法

    公开(公告)号:US6066739A

    公开(公告)日:2000-05-23

    申请号:US355096

    申请日:1999-07-23

    摘要: The present invention provides a method for producing an optically active 4-[.alpha.-hydro-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid or a pharmaceutically acceptable salt thereof, which includes subjecting a compound of the formula (I) ##STR1## wherein each symbol in the formula is as defined in the specification, to optical resolution by fractional crystallization to give an optically active compound thereof and subjecting the compound to hydrolysis reaction. According to this method, a resolution method useful for industrial large-scale production of the optically active compound of 4-[.alpha.-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid, which is useful as a thromboxane synthetase inhibitor and an agent for the prophylaxis and treatment of diabetic complications, can be obtained.

    摘要翻译: PCT No.PCT / JP98 / 00150 Sec。 371日期:1999年7月23日 102(e)日期1999年7月23日PCT提交1998年1月14日PCT公布。 第WO98 / 32740号公报 日期:1998年7月30日本发明提供了一种光学活性的4- [α-氢-5-(1-咪唑基)-2-甲基苄基] -3,5-二甲基苯甲酸或其药学上可接受的盐的制备方法, 包括使式(I)化合物(其中式中的每个符号如说明书中所定义)通过分级结晶进行光学拆分,得到其光学活性化合物并使化合物进行水解反应。 根据该方法,可以用于工业大规模生产4- [α-羟基-5-(1-咪唑基)-2-甲基苄基] -3,5-二甲基苯甲酸的光学活性化合物的分辨方法,其为 可用作血栓素合成酶抑制剂和用于预防和治疗糖尿病并发症的药剂。

    8-methoxy-quinolonecarboxylic acid derivatives
    8.
    发明授权
    8-methoxy-quinolonecarboxylic acid derivatives 失效
    8-甲氧基 - 喹啉酮羧酸衍生物

    公开(公告)号:US5677316A

    公开(公告)日:1997-10-14

    申请号:US473357

    申请日:1995-06-07

    CPC分类号: C07D401/04

    摘要: 8-Methoxy-quinolonecarboxylic acid derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, a lower alkyl, a phenylalkyl or an ester residue hydrolyzable in the living body, R.sub.2 is a hydrogen atom or methyl and n is an integer of 1, optical isomers thereof, pharmaceutically acceptable salts thereof and hydrates thereof. The 8-methoxy-quinolonecarboxylic acid derivatives of the present invention have enforced and a wide range of in vitro and in vivo antibacterial effects against Gram-positive bacteria, while retaining a strong antibacterial effect against Gram-negative bacteria, that the conventional quinolonecarboxylic acid antibacterial agents have. In addition, the compounds of the present invention scarcely show problematic side-effects and are low toxic. Therefore, they are expected to show superior clinical effects as antibacterial agents.

    摘要翻译: 式(I)的8-甲氧基 - 喹啉酮羧酸衍生物,其中R1是氢原子,低级烷基,苯基烷基或可在生物体中水解的酯残基,R2是氢原子或甲基,n是 1的整数,其光学异构体,其药学上可接受的盐和其水合物。 本发明的8-甲氧基 - 喹诺酮羧酸衍生物对革兰氏阳性细菌的体外和体内抗菌作用具有广泛的应用范围,同时保留对革兰氏阴性细菌的强烈的抗菌作用,常规的喹诺酮羧酸抗菌剂 代理商有。 此外,本发明的化合物几乎不显示有问题的副作用,并且毒性低。 因此,作为抗菌剂,预期其具有优异的临床效果。