ISOXAZOLIDINE COMPOUNDS USEFUL IN THE TREATMENT OF DIABETES, HYPERLIPIDEMIA, AND ATHEROSCLEROSIS
    54.
    发明申请
    ISOXAZOLIDINE COMPOUNDS USEFUL IN THE TREATMENT OF DIABETES, HYPERLIPIDEMIA, AND ATHEROSCLEROSIS 审中-公开
    用于治疗糖尿病,高脂血症和甲状腺功能亢进的ISOXAZOLIDINE化合物

    公开(公告)号:WO02024689A1

    公开(公告)日:2002-03-28

    申请号:PCT/US2001/029853

    申请日:2001-09-21

    摘要: The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, isoxazolidine compounds which have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the isoxazolidine compounds are also taught.

    摘要翻译: 本发明提供了可用于治疗II型糖尿病的药物化合物。 这些化合物是有利的,因为它们容易被代谢药物解毒系统代谢。 特别地,提供了已被设计为在化合物的结构内包含酯的异恶唑烷化合物。 本发明还涉及治疗疾病如糖尿病的方法,其包括施用治疗有效的组合物,其包含被设计为由血清或细胞内水解酶和酯酶代谢的化合物。 还教导了异恶唑烷化合物的药物组合物。

    NOVEL LIGANDS OF NUCLEAR RECEPTOR
    55.
    发明申请
    NOVEL LIGANDS OF NUCLEAR RECEPTOR 审中-公开
    核心受体的新配体

    公开(公告)号:WO00035867A1

    公开(公告)日:2000-06-22

    申请号:PCT/JP1999/007012

    申请日:1999-12-14

    摘要: It has been newly found out that ascochlorin, which is a publicly known fat-soluble antibiotic, and its homologs serve as a ligand of retinoid X receptor and react in vivo with the amino group of serum protein to form Schiff bases without showing any side effect of retinoid. Ascochlorin and its homologs are usable in treating and/or preventing diseases or conditions which can be relieved by the retinoid X receptor ligand-dependent gene signal transcriptional regulation (for example, diseases caused by the expression of insulin resistance, hypertension, cerebrovascular diseases, rheumatoid arthritis, autoimmune diseases, Ca metabolic error, complication of diabetes, arteriosclerosis, etc.). Moreover, they can inhibit denaturation and/or necrosis of pancreatic Langerhans islet beta -cells and, therefore, are usable in making these cells to sustain the insulin productivity.

    摘要翻译: 新近发现,作为公知的脂溶性抗生素的ascochlorin,其同系物作为类视黄醇X受体的配体,与血清蛋白的氨基反应形成希夫碱,而没有显示任何副作用 的类视黄醇。 异烟肼及其同系物可用于治疗和/或预防可被视黄酸X受体配体依赖性基因信号转录调节(例如,由胰岛素抵抗,高血压,脑血管疾病,类风湿病的表达引起的疾病)可减轻的疾病或病症 关节炎,自身免疫性疾病,Ca代谢异常,糖尿病并发症,动脉硬化等)。 此外,它们可以抑制胰腺胰岛β细胞的变性和/或坏死,因此可用于使这些细胞维持胰岛素的生产力。

    SUBSTITUTED DIHYDROBENZOPYRANS USEFUL AS ANTIARRHYTHMIC AGENTS
    56.
    发明申请
    SUBSTITUTED DIHYDROBENZOPYRANS USEFUL AS ANTIARRHYTHMIC AGENTS 审中-公开
    替代二氢苯并噻嗪类作为抗菌药物有用

    公开(公告)号:WO00014084A1

    公开(公告)日:2000-03-16

    申请号:PCT/US1999/020306

    申请日:1999-09-03

    CPC分类号: C07D311/68 C07D311/70

    摘要: Disclosed are novel dihydrobenzopyran compounds useful as antiarrhythmic and antifibrillatory agents. The compounds have a structure according to formula (A), or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification. Formula (A) also includes optical isomers, diastereomers or enantiomers. Also disclosed are pharmaceutical compositions and methods of treating disorders and conditions characterized by antiarrhythmic activity using these compounds or the pharmaceutical compositions containing them.

    摘要翻译: 公开了可用作抗心律不齐和抗纤维化剂的新型二氢苯并吡喃化合物。 所述化合物具有式(A)的结构或其药学上可接受的盐或可生物水解的酰胺,酯或酰亚胺,其中R1,R2,R3,R4,R5和R6如说明书中所定义。 式(A)还包括光学异构体,非对映体或对映异构体。 还公开了使用这些化合物或含有它们的药物组合物治疗特征为抗心律失常活性的病症和病症的药物组合物和方法。

    PROCESS FOR PREPARATION OF NEBIVOLOL AND IT'S SALTS
    58.
    发明申请
    PROCESS FOR PREPARATION OF NEBIVOLOL AND IT'S SALTS 审中-公开
    制备NEBIVOLOL及其销售的方法

    公开(公告)号:WO2016185492A1

    公开(公告)日:2016-11-24

    申请号:PCT/IN2016/050144

    申请日:2016-05-18

    IPC分类号: A61K31/00

    CPC分类号: C07D311/70 A61K31/353

    摘要: The present invention discloses a new process for preparation of Nebivolol or it's pharmaceutically acceptable salt. More particularly, the invention discloses an improved economical process for the preparation of intermediate, 6-fluoro-3,4- dihydro-2H-1-benzopyran-2-carboxaldehyde of Formula – II, converting the 6- fluoro-3,4-dihydro-2H-1-benzopyran-2-carboxaldehyde of Formula – II into mixture of [R*(S*)]-6-fluoro-3,4-dihydro-2-oxiranyl-2H-1-benzopyran and [R*(R*)]-6-fluoro-3,4-dihydro-2-oxiranyl-2H-1-benzopyran of Formula-V and separation of diastereomers of (R*)-6-Fluoro-3,4-dihydro-2-((S*)-oxiran-2-yl)- 2H-benzopran by forming azeotrope.

    摘要翻译: 本发明公开了一种制备奈比洛尔或其药学上可接受的盐的新方法。 更具体地说,本发明公开了制备式II的中间体6-氟-3,4-二氢-2H-1-苯并吡喃-2-甲醛的改进的经济方法,将6-氟-3,4-二氢-2H- 二氢-2H-1-苯并吡喃-2-甲醛与[R *(S *)] -6-氟-3,4-二氢-2-环氧乙烷基-2H-1-苯并吡喃和[R * (R *)] -6-氟-3,4-二氢-2-环氧乙烷基-2H-1-苯并吡喃,分离出(R *)-6-氟-3,4-二氢-2 - ((S *) - 环氧乙烷-2-基)-2H-苯并吡喃,通过形成共沸物。

    FORMATION OF CHROMANES AND CHROMENES BY USING SILVER(I) OR GOLD(I) SALTS OR COMPLEXES
    60.
    发明申请
    FORMATION OF CHROMANES AND CHROMENES BY USING SILVER(I) OR GOLD(I) SALTS OR COMPLEXES 审中-公开
    使用银(I)或金(I)盐或复合物形成铬和铬

    公开(公告)号:WO2015028463A1

    公开(公告)日:2015-03-05

    申请号:PCT/EP2014/068080

    申请日:2014-08-26

    IPC分类号: C07D311/70 C07D311/72

    CPC分类号: C07D311/70 C07D311/72

    摘要: The present invention relates to the method of preparing chiral chromanes and chromenes in high yields by intramolecular hydroarylation of chiral aryl alkynes catalysed by either a silver(I) or gold(I) salt or complex in combination of a specific acid or by a silver(I) or gold(I) metal salt or complex having specific anion. By the hydroarylation a chromene is formed which has a chiral centre in the 2 position. The corresponding chromane is obtained by hydrogenation of the chromenes.

    摘要翻译: 本发明涉及通过分子内加氢芳基化手性色烷和色烯的方法,所述手性芳基炔由银(I)或金(I)盐或络合物通过特定酸或银组合催化的手性芳基炔烃 I)或具有特定阴离子的金(I)金属盐或络合物。 通过加氢芳基化,形成了在2位具有手性中心的色烯。 通过色烯的氢化获得相应的苯并二氢吡喃。