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113 条记录 (耗时 0.055 秒)

    Seco-mevinic acid derivatives useful as antihypercholesterolemic agents and new intermediates
    72.
    发明授权
    Seco-mevinic acid derivatives useful as antihypercholesterolemic agents and new intermediates 失效
    山梨酸衍生物可用作抗高胆固醇血症药物和新中间体

    公开(公告)号：US5189180A

    公开(公告)日：1993-02-23

    申请号：US694515

    申请日：1991-05-01

    申请人： Donald S. Karanewsky

    发明人： Donald S. Karanewsky

    IPC分类号： C07C69/675 ,  C07D309/30 ,  C07D319/06 ,  C07D405/08 ,  C07D407/08 ,  C07D409/08 ,  C07F7/18

    CPC分类号： C07D405/08 ,  C07C69/675 ,  C07D309/30 ,  C07D319/06 ,  C07D407/08 ,  C07D409/08 ,  C07F7/1856

    摘要： Seco-mevinic acid derivatives are provided which have the structure ##STR1## including all stereoisomers thereof, wherein Z is ##STR2## R is H, alkali metal or lower alkyl, R.sup.1 is H, lower alkyl, aryl, lower alkoxy, cycloalkyl, heteroaryl, aralkyl, heteroaralkyl or heterocyclic; R.sup.2 is lower alkyl, cycloalkyl or aralkyl, and X is O or NR.sup.5 wherein R.sup.5 is H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis.New intermediates for preparing the above seco-mevinic acid derivatives are also provided.

    摘要翻译： 提供了具有包括其所有立体异构体的结构所述的羟甲基乙酸衍生物，其中Z是R，H是碱金属或低级烷基，R 1是H，低级烷基，芳基，低级烷氧基，环烷基，杂芳基 ，芳烷基，杂芳烷基或杂环基; R2是低级烷基，环烷基或芳烷基，X是O或NR5，其中R5是H或低级烷基，并且是HMG CoA还原酶抑制剂，因此可用作抗高胆固醇血症药物和治疗动脉粥样硬化。 还提供了用于制备上述仲维甲酸衍生物的新中间体。

    Process for preparing certain 5,6,7,8-tetrahydroindolizinyl (ethyl or ethynyl)-hydroxy or methoxy-phosphinyl-3-hydroxy-butanoates and derivatives thereof
    74.
    发明授权
    Process for preparing certain 5,6,7,8-tetrahydroindolizinyl (ethyl or ethynyl)-hydroxy or methoxy-phosphinyl-3-hydroxy-butanoates and derivatives thereof 失效
    制备某些5,6,7,8-四氢吲哚嗪（乙基或乙炔基） - 羟基或甲氧基 - 氧膦基-3-羟基 - 丁酸酯及其衍生物的方法

    公开(公告)号：US5124453A

    公开(公告)日：1992-06-23

    申请号：US646978

    申请日：1991-01-28

    申请人： Donald S. Karanewsky

    发明人： Donald S. Karanewsky

    IPC分类号： C07F9/6561

    CPC分类号： C07F9/6561

    摘要： Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesterolemic agents are provided which have the structure ##STR1## including salts thereof, wherein R is OH, or lower alkoxy; R.sup.x is H or alkyl;X is --(CH.sub.2).sub.a -- (where a is 1, 2, or 3), --CH.dbd.CH--, or --C.tbd.C--.New intermediates used in preparing the above compounds, pharmaceutical compositions containing such compounds and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.

    摘要翻译： 提供可用作胆固醇生物合成抑制剂并因此作为低胆固醇血症药物的化合物，其具有包括其盐的结构，其中R为OH或低级烷氧基; Rx是H或烷基; X是 - （CH 2）a - （其中a是1,2或3），-CH = CH-或-C 3 B-。 还提供了用于制备上述化合物的新中间体，含有这些化合物的药物组合物和使用这些化合物抑制胆固醇生物合成的方法。

    Phosphorus-containing HMG-CoA reductase inhibitor compounds
    76.
    发明授权
    Phosphorus-containing HMG-CoA reductase inhibitor compounds 失效
    含磷的HMG-CoA还原酶抑制剂化合物

    公开(公告)号：US5025000A

    公开(公告)日：1991-06-18

    申请号：US487366

    申请日：1990-03-02

    申请人： Donald S. Karanewsky

    发明人： Donald S. Karanewsky

    IPC分类号： A61K31/675 ,  A61P3/06 ,  A61P43/00 ,  C07F9/30 ,  C07F9/32 ,  C07F9/572 ,  C07F9/6561

    CPC分类号： C07F9/6561

    摘要： Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesterolemic agents are provided which have the structure ##STR1## including salts thereof, wherein R is OH, or lower alkoxy;R.sup.x is H or alkyl;X is --(CH.sub.2).sub.a -- (where a is 1, 2 or 3), --CH.dbd.CH--, or --C.tbd.C--.New intermediates used in preparing the above compounds, pharmaceutical compositions containing such compounds and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.

    Method for preparing phosphinic acids used in preparing ace inhibitors and intermediates produced thereby
    77.
    发明授权
    Method for preparing phosphinic acids used in preparing ace inhibitors and intermediates produced thereby 失效
    制备用于制备ace抑制剂的次膦酸的方法及其制备的中间体

    公开(公告)号：US4873356A

    公开(公告)日：1989-10-10

    申请号：US102694

    申请日：1987-09-30

    申请人： Edward W. Petrillo, Jr. ,  Donald S. Karanewsky ,  John K. Thottathil ,  James E. Heikes ,  John A. Grosso

    发明人： Edward W. Petrillo, Jr. ,  Donald S. Karanewsky ,  John K. Thottathil ,  James E. Heikes ,  John A. Grosso

    IPC分类号： A61K31/66 ,  A61P9/12 ,  A61P43/00 ,  B01J23/44 ,  C07B61/00 ,  C07F9/32 ,  C12N9/99

    CPC分类号： C07F9/3264 ,  C07F9/3211

    摘要： A method is provided for preparing phosphinic acid compounds, which are useful in preparing certain angiotensin converting enzyme inhibitors, which have the formula ##STR1## wherein R.sub.1 is lower alkyl, aryl, arylalkyl, cycloalkyl or cycloalkylalkyl;R.sub.2 is hydrogen, lower alkyl or arylalkyl;X is hydrogen, lower alkyl or phenyl;Y is hydrogen, lower alkyl, phenyl or alkoxy, or together X and Y are --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --CH.dbd.CH--, or ##STR2## and n is 0 or 1including salts thereof and stereoisomers thereof, which method includes the steps of reacting a phosphinic acid ester of the structure ##STR3## wherein R.sub.3 is a group removable by hydrogenolysis such as benzyl or substituted benzyl, with a halo ester of the structure ##STR4## in the presence of an organic base to form a phosphinic acid ester of the structure ##STR5## hydrogenating the above ester to form a diastereomic mixture of a phosphinic acid of the structure ##STR6## recrystallizing to recover the preferred racemic mixture and resolving same employing a resolving agent, preferably L-cinchonidine, to form the corresponding resolved salt which may be acidified to the corresponding acid. In addition, novel intermediates which are acids and salts as described above are also provided.

    摘要翻译： 提供了一种制备次膦酸化合物的方法，其可用于制备具有下式的其中R 1为低级烷基，芳基，芳烷基，环烷基或环烷基烷基的一些血管紧张素转换酶抑制剂; R2是氢，低级烷基或芳基烷基; X是氢，低级烷基或苯基; Y是氢，低级烷基，苯基或烷氧基，或者一起X和Y是 - （CH 2）2 - ， - （CH 2）3 - ， - CH = CH-或，n是0或1，包括其盐 该方法包括以下步骤：使结构式“其中R3是通过氢解可除去的基团如苄基或取代的苄基”的结构式的次膦酸酯与结构“IMAGE”的卤代酯在存在下 形成下述结构的次膦酸酯的有机碱，氢化上述酯以形成结构为重结晶的次膦酸的非对映体混合物，以回收优选的外消旋混合物，并使用拆分剂拆分，优选 形成相应的分解盐，其可以酸化成相应的酸。 此外，还提供了如上所述的酸和盐的新型中间体。