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20 条记录 (耗时 0.051 秒)

    Dihydroxy open-acid and salts of HMG-CoA reductase inhibitors
    4.
    发明授权
    Dihydroxy open-acid and salts of HMG-CoA reductase inhibitors 失效
    二羟基开酸和HMG-CoA还原酶抑制剂的盐

    公开(公告)号：US06569461B1

    公开(公告)日：2003-05-27

    申请号：US09558800

    申请日：2000-04-26

    申请人： Richard D. Tillyer ,  Paul J. Reider ,  Edward J. J. Grabowski ,  Feng Xu ,  Jose M. Vega ,  Mandana Asgharnejad

    发明人： Richard D. Tillyer ,  Paul J. Reider ,  Edward J. J. Grabowski ,  Feng Xu ,  Jose M. Vega ,  Mandana Asgharnejad

    IPC分类号： A61K900

    CPC分类号： A61K9/2833

    摘要： The instant invention provides methods and pharmaceutical compositions for inhibiting HMG-CoA reductase, as well as for treating and/or reducing the risk for diseases and conditions affected by inhibition of HMG-CoA reductase, comprising orally administering a therapeutically effective amount of a compound selected from a dihydroxy open acid statin and a pharmaceutically acceptable salt or ester thereof in a delayed-release pharmaceutical dosage form to a patient in need of such treatment wherein substantial release of the compound from the dosage form is delayed until after passage of the dosage form through the stomach.

    摘要翻译： 本发明提供用于抑制HMG-CoA还原酶的方法和药物组合物，以及用于治疗和/或降低受HMG-CoA还原酶抑制影响的疾病和病症的风险，包括口服施用治疗有效量的选择的化合物 从延迟释放药物剂型的二羟基开酸他汀类药物及其药学上可接受的盐或酯到需要这种治疗的患者，其中化合物从剂型中的实质性释放被延迟直到剂型通过后 肚子

    Process for the synthesis of carbapenem intermidiates, and compounds produced
    9.
    发明授权
    Process for the synthesis of carbapenem intermidiates, and compounds produced 失效
    合成碳青霉烯干扰素的方法和所生产的化合物

    公开(公告)号：US06395894B2

    公开(公告)日：2002-05-28

    申请号：US09292257

    申请日：1999-04-15

    申请人： Philip J. Pye ,  Paul J. Reider ,  Kai Rossen ,  Ralph P. Volante

    发明人： Philip J. Pye ,  Paul J. Reider ,  Kai Rossen ,  Ralph P. Volante

    IPC分类号： C07D47714

    CPC分类号： C07D477/04 ,  C07D205/08 ,  Y02P20/55

    摘要： A process of synthesizing a compound of structural formula 6 is disclosed wherein R1 represents H or a suitable protecting group for an alcohol; R2 represents a benzyl, C1-6 alkyl or aryl; Y represents C1-3 alkyl, O, NH or S; X represents O, NH, or S and R5 represents a carboxy protecting group, comprising reacting a compound of formula 5: wherein R1, R2, R5, X and Y are as previously described with a phosphite or phosphonite reagent to produce a compound of formula 6. Further disclosed is an efficient method for the synthesis of a compound of formula 2: which comprises reacting a 4-acyl-2-azetidinone with a titanium, zirconium or hafnium enolate of a 1-hydroxy-2-butanone derivative.

    摘要翻译： 公开了一种合成结构式6的化合物的方法，其中R1表示H或适当的醇保护基; R 2表示苄基，C 1-6烷基或芳基; Y表示C 1-3烷基，O，NH或S; X表示O，NH或S，R 5表示羧基保护基，其包括使式5化合物：其中R 1，R 2，R 5，X和Y如前所述与亚磷酸酯或亚膦酸酯试剂反应以制备式 6.还公开了合成式2化合物的有效方法：其包括使4-酰基-2-氮杂环丁酮与1-羟基-2-丁酮衍生物的钛，锆或锇烯醇化物反应。

    Preparation of betamethyl carbapenem intermediates
    10.
    发明授权
    Preparation of betamethyl carbapenem intermediates 失效
    二甲基碳青霉烯中间体的制备

    公开(公告)号：US06242596B1

    公开(公告)日：2001-06-05

    申请号：US08241958

    申请日：1994-05-12

    申请人： Woo-Baeg Choi ,  Guy R. Humphrey ,  Paul J. Reider ,  Ichiro Shinkai ,  Andrew S. Thompson ,  Ralph P. Volante

    发明人： Woo-Baeg Choi ,  Guy R. Humphrey ,  Paul J. Reider ,  Ichiro Shinkai ,  Andrew S. Thompson ,  Ralph P. Volante

    IPC分类号： C07D20508

    CPC分类号： C07D405/04 ,  C07D205/08 ,  Y02P20/55

    摘要： A process for making a beta methyl carbapenem intermediate is disclosed. A compound of formula I: is contacted in a non-reactive solvent with methyl Meldrum's acid and a base to produce a compound of formula III: Compound III is treated in an aprotic solvent with a scavenging base, an alkali metal halide and a tri-organo silyl protecting compound for nitrogen to produce a compound of formula IV: Compound IV may be reacted with a nucleophile Nu—X in a non-reactive solvent and base, and the mixture acidified to produce a compound of formula V. Compound V may be reacted with mild acid to produce a compound of formula VI.

    摘要翻译： 公开了一种制备β-甲基碳青霉烯中间体的方法。 将式I化合物在非反应性溶剂中与甲基Meldrum酸和碱接触以产生式III化合物：化合物III在非质子溶剂中用清除碱，碱金属卤化物和三 - 用于氮的有机甲硅烷基保护化合物以产生式IV的化合物：化合物IV可以在非反应性溶剂和碱中与亲核试剂Nu-X反应，并将该混合物酸化以产生式V化合物。化合物V可以是 与轻度酸反应生成式Ⅵ化合物。