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    Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
    23.
    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
    24.
    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
    25.
    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。

    Indole-type derivatives as inhibitors of p38 kinase
    30.
    发明授权
    Indole-type derivatives as inhibitors of p38 kinase 有权
    吲哚型衍生物作为p38激酶的抑制剂

    公开(公告)号：US07238712B2

    公开(公告)日：2007-07-03

    申请号：US10156997

    申请日：2002-05-28

    Applicant: Babu J. Mavunkel ,  Sarvajit Chakravarty ,  John J. Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

    Inventor： Babu J. Mavunkel ,  Sarvajit Chakravarty ,  John J. Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

    IPC: A61K31/445 ,  C07D401/06

    CPC classification number: C07D209/24 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

    Abstract: The invention is directed to methods to inhibit p38-α kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein represents a single or double bond; one Z2 is CA or CR8A and the other is CR1, CR12, NR6 or N wherein each R1, R6 and R8 is independently hydrogen or noninterfering substituent; A is —Wi—COXjY wherein Y is COR2 or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2–6 Å, and each of i and j is independently 0 or 1; Z3 is NR7 or O; each R3 is independently a noninterfering substituent; n is 0–3; each of L1 and L2 is a linker; each R4 is independently a noninterfering substituent; m is 0–4; Z1 is CR5 or N wherein R5 is hydrogen or a noninterfering substituent; each of l and k is an integer from 0–2 wherein the sum of l and k is 0–3; Ar is an aryl group substituted with 0–5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; and the distance between the atom of Ar linked to L2 and the center of the α ring is 4.5–24 Å.

    Abstract translation: 本发明涉及使用下式的化合物及其药学上可接受的盐或其药物组合物来抑制p38-α激酶的方法，其中表示单键或双键; 一个Z 2是CA或CR 8 A，另一个是CR 1，CR 1，2， 其中每个R 1，R 6和R 8独立为氢，NR 6，N 6， 或非干扰取代基; A是其中Y是COR 2或其等同体和R 2的-Wi-i-X 氢或非干扰取代基，W和X各自为2-6的间隔基，i和j各自独立地为0或1; Z 3是NR 7或O; 每个R 3独立地是非干扰取代基; n为0-3; L 1和L 2各自为连接体; 每个R 4独立地是非干扰取代基; m为0-4; Z 1是CR 5或N，其中R 5是氢或非干扰取代基; l和k中的每一个是0-2的整数，其中l和k的和为0-3; Ar是被0-5个非直链取代基取代的芳基，其中两个非干扰取代基可以形成稠环; 并且与L 2连接的Ar原子和α环的中心之间的距离为4.5-24埃。

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