利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

6 条记录 (耗时 0.015 秒)

    Bis(benzylpyrrolidine) derivatives useful for treating congestive heart failure and acute renal failure
    1.
    发明授权
    Bis(benzylpyrrolidine) derivatives useful for treating congestive heart failure and acute renal failure 失效
    用于治疗充血性心力衰竭和急性肾衰竭的双（苄基吡咯烷）衍生物

    公开(公告)号：US5135944A

    公开(公告)日：1992-08-04

    申请号：US801244

    申请日：1991-12-03

    申请人： Lawrence E. Fisher ,  Joseph M. Muchowski ,  Edvige Galeazzi ,  Roberto P. Rosenkranz ,  Deborah L. McClelland

    发明人： Lawrence E. Fisher ,  Joseph M. Muchowski ,  Edvige Galeazzi ,  Roberto P. Rosenkranz ,  Deborah L. McClelland

    IPC分类号： C07D207/08 ,  C07D207/32 ,  C07D207/333

    CPC分类号： C07D207/08 ,  C07D207/333

    摘要： Compounds of Formula I ##STR1## in which: R.sub.1 is hydrogen, lower alkyl, --C(O)R.sub.3, or --C(O)NR.sub.3 R.sub.4, where R.sub.3 and R.sub.4 are independently lower alkyl, phenyl, or phenyl lower alkyl;R.sub.2 is hydrogen or lower alkyl; andX is --(CH.sub.2).sub.m -- where m is an integer of 1 to 10, or --(CH.sub.2).sub.n Y(CH.sub.2).sub.n -- where n is an integer of 1 to 3 and Y is oxygen or sulfur,their individual R,R-; R,S-; and S,S-stereoisomers, and racemic or non-racemic mixtures of stereoisomers, and their pharmaceutically acceptable salts are dopamine agonist compounds useful in the treatment of hypertension and congestive heart failure in mammals.

    摘要翻译： 式I的化合物其中：R 1是氢，低级烷基，-C（O）R 3或-C（O）NR 3 R 4，其中R 3和R 4独立地是低级烷基，苯基或苯基低级烷基 ; R2是氢或低级烷基; X为 - （CH 2）m - ，其中m为1〜10的整数，或 - （CH 2）n Y（CH 2）n - ，其中n为1〜3的整数，Y为氧或硫， R-; R，S-; 和S，S-立体异构体，以及立体异构体的外消旋或非外消旋混合物及其药学上可接受的盐是可用于治疗哺乳动物高血压和充血性心力衰竭的多巴胺激动剂化合物。

    Bis(benzylpyrrolidine) derivatives as dopamine agonists
    2.
    发明授权
    Bis(benzylpyrrolidine) derivatives as dopamine agonists 失效
    双（苄基吡咯烷）衍生物作为多巴胺激动剂

    公开(公告)号：US5100912A

    公开(公告)日：1992-03-31

    申请号：US631524

    申请日：1990-12-21

    申请人： Lawrence E. Fisher ,  Joseph M. Muchowski ,  Edvige Galeazzi ,  Roberto P. Rosenkranz ,  Deborah L. McClelland

    发明人： Lawrence E. Fisher ,  Joseph M. Muchowski ,  Edvige Galeazzi ,  Roberto P. Rosenkranz ,  Deborah L. McClelland

    IPC分类号： C07D207/08 ,  C07D207/32 ,  C07D207/333

    CPC分类号： C07D207/08 ,  C07D207/333

    摘要： Compound of Formula I ##STR1## in which: R.sub.1 is hydrogen, lower alkyl, --C(O)R.sub.3, or --C(O)NR.sub.3 R.sub.4, where R.sub.3 and R.sub.4 are independently lower alkyl, phenyl, or phenyl lower alkyl;R.sub.2 is hydrogen or lower alkyl; andX is --(CH.sub.2).sub.m --where m is an integer of 1 to 10, or --(CH.sub.2).sub.n Y(CH.sub.2).sub.n --where n is an integer of 1 to 3 and Y is oxygen or sulfur,their individual R,R--; R,S--; and S,S-stereoisomers, and racemic or non-racemic mixtures of stereoisomers, and their pharmaceutically acceptable salts are dopamine agonist compounds useful in the treatment of hypertension and congestive heart failure in mammals.

    摘要翻译： 式I的化合物其中：R 1是氢，低级烷基，-C（O）R 3或-C（O）NR 3 R 4，其中R 3和R 4独立地是低级烷基，苯基或苯基低级烷基 ; R2是氢或低级烷基; 其中m为 - （CH 2）m-，其中m为1至10的整数，或 - （CH 2）n Y（CH 2）n - ，其中n为1至3的整数，Y为氧或硫， R-; R，S-; 和S，S-立体异构体，以及立体异构体的外消旋或非外消旋混合物及其药学上可接受的盐是可用于治疗哺乳动物高血压和充血性心力衰竭的多巴胺激动剂化合物。

    Method for alkylating the alpha carbon of the 2-methylbutyrate secondary chain of lovastatin
    4.
    发明授权
    Method for alkylating the alpha carbon of the 2-methylbutyrate secondary chain of lovastatin 失效
    用于烷基化洛伐他汀2-甲基丁酸二级链的α碳的方法

    公开(公告)号：US06472542B1

    公开(公告)日：2002-10-29

    申请号：US09996664

    申请日：2001-11-29

    申请人： Edvige Galeazzi ,  Gustavo A. Garcia ,  Fernando Lara ,  Gema Lopez ,  Orestes Martinez ,  Eugenio Tisselli ,  Alicia Trejo

    发明人： Edvige Galeazzi ,  Gustavo A. Garcia ,  Fernando Lara ,  Gema Lopez ,  Orestes Martinez ,  Eugenio Tisselli ,  Alicia Trejo

    IPC分类号： C07D30930

    CPC分类号： C07D309/30 ,  C07C235/30 ,  C07C2602/28 ,  C07F7/1804 ,  C07F7/1892 ,  Y02P20/55

    摘要： Simvastatin is produced from lovastatin in high yield and in pharmaceutical purity by forming an amide of lovastatin and protecting the free hydroxyl groups of the lovastatin amide with hexamethyidisilazane (HMDS) to form a protected lovastatin amide. The &agr;-carbon of the 2-methylbutyrate secondary chain of the protected lovastatin amide may be methylated to form a protected simvastatin amide. The protecting groups may be removed therefrom by quenching the methylation reaction with water. The simvastatin amide which is obtained may be hydrolyzed to form simvastatin acid, followed by forming a simvastatin ammonium salt, lactonizing the salt to form simvastatin, and recrystallizing the thus formed crude Simvastatin to a high degree of purity. The HMDS protecting agent for the lactone hydroxyl groups of Lovastatin is selected so as to result in a reaction that does not produce acid so that a base, such as imidazole, is not required to neutralize the acidity of the reaction medium. Another advantage of using HMDS as a protecting agent is that the removal of the protecting agent after the methylation reaction is carried out simply, for example, by water quenching. The lactonization reaction of the present invention may be carried out using a low boiling point solvent, such as methylene chloride, in the presence of inorganic acids such as sulfuric, hydrochloric, methanesulfonic or phosphoric acid as catalyst.

    摘要翻译： 辛伐他汀通过形成洛伐他汀的酰胺并以六水合二硅氮烷（HMDS）保护洛伐他汀酰胺的游离羟基，形成受保护的洛伐他汀酰胺，以高产率和药物纯度从洛伐他汀生产。 被保护的洛伐他汀酰胺的2-甲基丁酸二级链的α-碳可被甲基化以形成受保护的辛伐他汀酰胺。 通过用水淬灭甲基化反应可以将保护基除去。 所获得的辛伐他汀酰胺可以水解形成辛伐他汀酸，然后形成辛伐他汀铵盐，将盐内酯化形成辛伐他汀，并将由此形成的粗制辛伐他汀重结晶至高纯度。 选择洛伐他汀的内酯羟基的HMDS保护剂，以产生不产生酸的反应，从而不需要碱例如咪唑来中和反应介质的酸度。 使用HMDS作为保护剂的另一个优点是在甲基化反应后除去保护剂简单地例如通过水淬。 本发明的内酯化反应可以在无机酸如硫酸，盐酸，甲磺酸或磷酸作为催化剂的存在下，使用低沸点溶剂如二氯甲烷进行。