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    Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
    42.
    发明授权
    Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents 失效
    用作降胆固醇药的羟基取代的氮杂环丁酮化合物

    公开(公告)号：US5631365A

    公开(公告)日：1997-05-20

    申请号：US257593

    申请日：1994-06-09

    Applicant: Stuart B. Rosenblum ,  Sundeep Dugar ,  Duane A. Burnett ,  John W. Clader ,  Brian A. McKittrick

    Inventor： Stuart B. Rosenblum ,  Sundeep Dugar ,  Duane A. Burnett ,  John W. Clader ,  Brian A. McKittrick

    IPC: A61K31/21 ,  A61K31/35 ,  A61K31/395 ,  A61K31/397 ,  A61K31/40 ,  A61P3/06 ,  A61P7/00 ,  A61P9/10 ,  C07D205/08

    CPC classification number: C07D205/08 ,  Y02P20/55

    Abstract: A process for preparing compounds of the formula ##STR1## wherein R and R.sup.2 are independently --OH, --O(lower alkyl) or --0-benzyl and the remaining variables are as defined in the specification, comprising(a) treating with a strong base in an anhydrous organic solvent a lactone of the formula ##STR2## respectively, wherein Ar.sup.10 is Ar.sup.1 or a suitably protected hydroxy- or amino-substituted aryl, and R' and R.sup.2' are R and R.sup.2 as defined above or are suitably protected hydroxy groups;(b) reacting a product of step (a) with an imine of the formula ##STR3## wherein Ar.sup.20 and Ar.sup.30 are Ar.sup.2 or Ar.sup.3 or suitably protected hydroxy- or amino-substituted aryl;c) quenching the reaction with an acid; andd) removing protecting groups as necssary.

    Abstract translation: 制备式IMA化合物的方法其中R和R 2独立地是-OH，-O（低级烷基）或-O-苄基，其余的变量如说明书中所定义，包括（a） 在无水有机溶剂中具有分子式为“IMAGE”的内酯的强碱，其中Ar10为Ar1或适当保护的羟基或氨基取代的芳基，R'和R2'为如上所定义的R和R 2，或者为 适当保护的羟基; （b）使步骤（a）的产物与下式的亚胺反应：其中Ar 20和Ar 30是Ar 2或Ar 3或适当保护的羟基或氨基取代的芳基; c）用酸淬灭反应; 和d）去除保护基团。

    Substituted azetidinone compounds useful as hypocholesterolemic agents
    43.
    发明授权
    Substituted azetidinone compounds useful as hypocholesterolemic agents 失效
    用作降胆固醇药的取代的氮杂环丁酮化合物

    公开(公告)号：US5627176A

    公开(公告)日：1997-05-06

    申请号：US403081

    申请日：1995-03-13

    Applicant: Michael P. Kirkup ,  Sundeep Dugar

    Inventor： Michael P. Kirkup ,  Sundeep Dugar

    IPC: A61K31/395 ,  A61K31/397 ,  A61P3/06 ,  A61P9/10 ,  C07B53/00 ,  C07C227/32 ,  C07C229/34 ,  C07C311/06 ,  C07C311/19 ,  C07C311/37 ,  C07C319/20 ,  C07C323/62 ,  C07D205/08 ,  C07D403/04 ,  C07D403/06

    CPC classification number: C07C227/32 ,  C07C229/34 ,  C07D205/08 ,  C07C2101/14

    Abstract: Substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar.sup.1 is R.sup.3 -substituted aryl;Ar.sup.2 is R.sup.4 -substituted aryl;Ar.sup.3 is R.sup.5 -substituted aryl;Y and Z are independently --CH.sub.2 --, --CH(lower alkyl)-- or --C(dilower alkyl)--;A is --O--, --S--, --S(O)-- or --S(O).sub.2 --;R.sup.1 is --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 or --O(CO)NR.sup.6 R.sup.7 ; R.sup.2 is hydrogen, lower alkyl or aryl; or R.sup.1 and R.sub.2 together are .dbd.O;q is 1, 2 or 3; p is 0, 1,2, 3 or 4;R.sup.5 is 1-3 substitutes independently selected from --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.9, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 -lower alkyl, --NR.sup.6 SO.sub.2 -aryl, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 -alkyl, S(O).sub.0-2 -aryl, --O(CH.sub.2).sub.1-10 -COOR.sup.6, --O(CH.sub.2).sub.0-10 CONR.sup.6 R.sup.7, o-halogeno, m-halogeno, o-lower alkyl, m-lower alkyl, -(lower alkylene)-COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ;R.sup.3 and R.sup.4 are 1-3 substituents independently selected from R.sup.5, hydrogen, p-lower alkyl, aryl, --NO.sub.2, CF.sub.3 and p-halogeno;R.sup.6, R.sup.7 and R.sup.8 are hydrogen, lower alkyl, aryl or aryl-substituted lower alkyl; andR.sup.9 is lower alkyl, aryl or aryl-substituted lower alkyl; are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, pharmaceutical compositions containing them, the combination of a substituted azetidinone and a cholesterol biosynthesis inhibitor for the treatment and prevention of atherosclerosis, novel intermediates and methods for preparing said intermediates.

    Abstract translation: 取代的式“IMAGE”的氮杂环丁酮降胆固醇剂或其药学上可接受的盐，其中：Ar 1是R 3取代的芳基; Ar2是R4-取代的芳基; Ar 3是R 5取代的芳基; Y和Z独立地是-CH 2 - ， - CH（低级烷基） - 或-C（二卤代烷基） - 。 A是-O - ， - S - ， - S（O） - 或-S（O）2 - ; R1是-OR6，-O（CO）R6，-O（CO）OR9或-O（CO）NR6R7; R2是氢，低级烷基或芳基; 或R 1和R 2一起为= O; q为1,2或3; p为0,1,2,3或4; R5是独立地选自-OR6，-O（CO）R6，-O（CO）OR9，-O（CH2）1-5OR9，-O（CO）NR6R7，-NR6R7，-NR6（CO） R 7，-NR 6（CO）OR 9，-NR 6（CO）NR 7 R 8，-NR 6 SO 2 - 低级烷基，-NR 6 SO 2 - 芳基，-CONR 6 R 7，-COR 6，-SO 2 NR 6 R 7，S（O） 0-2-芳基，-O（CH 2）1-10 -COOR 6，-O（CH 2）0-10 CONR 6 R 7，o-卤代，间 - 卤代，邻 - 低级烷基，间 - 低级烷基， - （低级亚烷基） COOR 6和-CH = CH-COOR 6; R3和R4是1-3个独立地选自R5，氢，对 - 低级烷基，芳基，-NO2，CF3和对 - 卤代的取代基; R6，R7和R8是氢，低级烷基，芳基或芳基取代的低级烷基; 并且R 9为低级烷基，芳基或芳基取代的低级烷基; 以及通过施用所述化合物，含有它们的药物组合物，取代的氮杂环丁酮和用于治疗和预防动脉粥样硬化的胆固醇生物合成抑制剂的组合来降低血清胆固醇的方法，新型中间体和制备所述中间体的方法。

    Inhibitors of acyl-coenzyme A: cholesterol acyl transferase
    44.
    发明授权
    Inhibitors of acyl-coenzyme A: cholesterol acyl transferase 失效
    酰基辅酶A抑制剂：胆固醇酰基转移酶

    公开(公告)号：US5326762A

    公开(公告)日：1994-07-05

    申请号：US885420

    申请日：1992-05-19

    Applicant: John Clader ,  Sundeep Dugar ,  Timothy Kogan ,  Bradley Tait ,  Wayne Vaccaro

    Inventor： John Clader ,  Sundeep Dugar ,  Timothy Kogan ,  Bradley Tait ,  Wayne Vaccaro

    IPC: C07C233/18 ,  C07C233/20 ,  C07C233/22 ,  C07C233/36 ,  C07C233/38 ,  C07C233/40 ,  C07C233/49 ,  C07C233/51 ,  C07C235/50 ,  C07C237/22 ,  C07C271/22 ,  C07C311/08 ,  H01N43/40 ,  C07D211/70

    CPC classification number: C07C233/20 ,  C07C233/18 ,  C07C233/22 ,  C07C233/36 ,  C07C233/38 ,  C07C233/40 ,  C07C233/49 ,  C07C233/51 ,  C07C235/50 ,  C07C237/22 ,  C07C271/22 ,  C07C311/08 ,  Y10S514/824

    Abstract: Amides of the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently heteroaryl, X-substituted heteroaryl, X-substituted phenyl, N-substituted triazinyl or N-substituted imidazolyl;and in addition, one of R.sub.1 and R.sub.2 can be as defined above and the other can be phenyl;R.sub.3 is an alkyl chain of 2 to 25 carbon atoms, saturated or unsaturated; an alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl; an alkyl chain as defined interrupted by one or more groups independently selected from the group consisting of --O--, --S--, --SO--, --SO.sub.2 --, --NH--, --N(lower alkyl)--, --C(O)--, phenylene, X-substituted phenylene, heteroarylene and X-substituted heteroarylene; or an interrupted alkyl chain as defined substituted by one or more substituents selected form the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl;R.sub.4 is hydrogen, lower alkyl, phenyl, X-substituted phenyl, heteroaryl or X-substituted heteroaryl; or a pharmaceutically acceptable salt thereof, useful as inhibitors of acyl-coenzyme A:cholesterol acyl transferase and therefore in the treatment of atherosclerosis are disclosed.

    Abstract translation: 其中R 1和R 2独立地是杂芳基，X取代的杂芳基，X取代的苯基，N-取代的三嗪基或N-取代的咪唑基; 此外，R 1和R 2中的一个可以如上所定义，另一个可以是苯基; R3是2至25个碳原子的饱和或不饱和的烷基链; 由一个或多个选自苯基，X取代的苯基，杂芳基和X取代的杂芳基的取代基取代的烷基链; 由一个或多个独立地选自-O - ， - S - ， - SO - ， - SO 2 - ， - NH - ， - N（低级烷基） - ， - C ） - ，亚苯基，X取代亚苯基，亚杂芳基和X取代亚杂芳基; 或被一个或多个选自苯基，X取代的苯基，杂芳基和X取代的杂芳基的取代基取代的中断的烷基链; R4是氢，低级烷基，苯基，X取代的苯基，杂芳基或X取代的杂芳基; 或其药学上可接受的盐，其可用作酰基辅酶A的抑制剂：胆固醇酰基转移酶，因此用于治疗动脉粥样硬化。

    Flavonoid compounds
    45.
    发明授权
    Flavonoid compounds 有权
    黄酮类化合物

    公开(公告)号：US09187448B2

    公开(公告)日：2015-11-17

    申请号：US14237167

    申请日：2012-08-06

    Applicant: Cyrus K. Becker ,  George F. Schreiner ,  Sundeep Dugar ,  Dinesh Mahajan

    Inventor： Cyrus K. Becker ,  George F. Schreiner ,  Sundeep Dugar ,  Dinesh Mahajan

    IPC: C07D311/62 ,  C07D405/10 ,  A61K31/353 ,  A61K31/496

    CPC classification number: C07D311/62 ,  A61K31/353 ,  A61K31/496 ,  C07D405/10

    Abstract: The present invention relates to compounds, compositions, and methods for treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more epicatechin derivatives in an amount effective to stimulate mitochondrial function in cells. The compounds, compositions, and methods described herein provide for reducing infarct size in the heart following permanent ischemia or ischemia/reperfusion event or method for delaying, attenuating or preventing adverse cardiac remodeling, and can assist in prevention of impaired mitochondria biogenesis and thus prevention of the consequences of impaired mitochondrial biogenesis in various diseases and conditions, as well as provide for the active therapy of mitochondrial depletion that may have already occurred.

    Abstract translation: 本发明涉及用于治疗与线粒体功能相关的病症的化合物，组合物和方法。 在各个方面，本发明包括施用一种或多种有效刺激细胞中线粒体功能的表儿茶素衍生物。 本文所述的化合物，组合物和方法提供了在永久性缺血或缺血/再灌注事件或心脏重建后延迟，减弱或预防的方法中减少心脏梗塞面积的大小，并可有助于预防线粒体生物发生受损，从而预防 在各种疾病和病症中受损的线粒体生物发生的后果，以及可能已经发生的线粒体消耗的主动治疗。

    FLAVONOID COMPOUNDS
    46.
    发明申请
    FLAVONOID COMPOUNDS 有权
    FLAVONOID化合物

    公开(公告)号：US20140256741A1

    公开(公告)日：2014-09-11

    申请号：US14237167

    申请日：2012-08-06

    Applicant: Cyrus K. Becker ,  George F. Schreiner ,  Sundeep Dugar ,  Dinesh Mahajan

    Inventor： Cyrus K. Becker ,  George F. Schreiner ,  Sundeep Dugar ,  Dinesh Mahajan

    IPC: C07D311/62

    CPC classification number: C07D311/62 ,  A61K31/353 ,  A61K31/496 ,  C07D405/10

    Abstract: The present invention relates to compounds, compositions, and methods for treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more epicatechin derivatives in an amount effective to stimulate mitochondrial function in cells. The compounds, compositions, and methods described herein provide for reducing infarct size in the heart following permanent ischemia or ischemia/reperfusion event or method for delaying, attenuating or preventing adverse cardiac remodeling, and can assist in prevention of impaired mitochondria biogenesis and thus prevention of the consequences of impaired mitochondrial biogenesis in various diseases and conditions, as well as provide for the active therapy of mitochondrial depletion that may have already occurred.

    Abstract translation: 本发明涉及用于治疗与线粒体功能相关的病症的化合物，组合物和方法。 在各个方面，本发明包括施用一种或多种有效刺激细胞中线粒体功能的表儿茶素衍生物。 本文所述的化合物，组合物和方法提供在永久缺血或缺血/再灌注事件或心脏延迟，减弱或预防不良心脏重塑后的心脏中降低梗死面积，并可有助于预防线粒体生物发生受损，从而预防 在各种疾病和病症中受损的线粒体生物发生的后果，以及提供可能已经发生的线粒体消耗的主动治疗。

    Process for the preparation of pyridopyrimidones
    49.
    发明授权
    Process for the preparation of pyridopyrimidones 有权
    吡啶并嘧啶酮的制备方法

    公开(公告)号：US07119199B2

    公开(公告)日：2006-10-10

    申请号：US11029139

    申请日：2004-12-31

    Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  Richland Tester ,  Aurelia Conte

    Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  Richland Tester ,  Aurelia Conte

    IPC: C07D239/91 ,  C07D471/04

    CPC classification number: C07D239/91 ,  C07D471/04

    Abstract: The present invention is directed to a method for producing a pyridopyrimidone of the formula wherein X is N or CH and R is an aryl, heteroaryl or alkyl group, said method comprising the step of reacting an acid derivative of the formula: wherein X is N or CH; Y is an appropriate leaving group; Z is a halogen, OR1, NHR1, or SR1; and R1 is a lower alkyl; and the amidine derivative is wherein R is an aryl, heteroaryl or alkyl group.

    Abstract translation: 本发明涉及一种制备下式的吡啶并吡啶酮的方法，其中X是N或CH，R是芳基，杂芳基或烷基，所述方法包括使下式的酸衍生物：其中X是N 或CH; Y是一个适当的离开组; Z是卤素，OR 1，NHR 1或SR 1; 并且R 1是低级烷基; 并且脒衍生物是其中R是芳基，杂芳基或烷基。

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