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    PENTAFLUOROSULPHOLANE-CONTAINING ANTIDIABETIC COMPOUNDS
    32.
    发明申请
    PENTAFLUOROSULPHOLANE-CONTAINING ANTIDIABETIC COMPOUNDS 审中-公开
    含芳香脂肪酸的抗菌化合物

    公开(公告)号：US20110313008A1

    公开(公告)日：2011-12-22

    申请号：US13145025

    申请日：2010-01-21

    申请人： Hubert B. Josien ,  John W. Clader ,  Andrew Stamford ,  William J. Greenlee ,  Michael John Mayer ,  Jason L. Davis ,  Ming Min Hsia ,  Shuangyi Wan

    发明人： Hubert B. Josien ,  John W. Clader ,  Andrew Stamford ,  William J. Greenlee ,  Michael John Mayer ,  Jason L. Davis ,  Ming Min Hsia ,  Shuangyi Wan

    IPC分类号： A61K31/426 ,  A61P3/10 ,  A61P3/00 ,  C07D277/04

    CPC分类号： C07D417/04 ,  C07D277/34

    摘要： This invention provides for certain pentafluorosulpholane-containing compounds of the formula or a pharmaceutically acceptable salt, ester, solvate or prodrug thereof, wherein the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.

    摘要翻译： 本发明提供了具有下式的某些五氟丁烷化合物或其药学上可接受的盐，酯，溶剂合物或前药，其中变量在本文中定义; 本发明化合物是G蛋白偶联受体40（GPR40，也称为游离脂肪酸受体FFAR）的激动剂。 本发明还涉及含有这些化合物的药物组合物，以及这些化合物在哺乳动物体内调节胰岛素水平的用途。 该化合物可用于例如预防和治疗2型糖尿病以及预防和治疗与2型糖尿病相关的病症，例如胰岛素抵抗，肥胖症和脂质疾病。

    Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
    33.
    发明申请
    Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof 有权
    取代的氮杂环丁酮化合物，其制备方法，制剂及其用途

    公开(公告)号：US20080200446A1

    公开(公告)日：2008-08-21

    申请号：US12108729

    申请日：2008-04-24

    申请人： Duane A. Burnett ,  John W. Clader

    发明人： Duane A. Burnett ,  John W. Clader

    IPC分类号： A61K31/397 ,  C07D205/08 ,  A61P9/10

    CPC分类号： C07D405/12 ,  C07D405/14 ,  Y10S930/28

    摘要： The present invention provides compounds represented by the structural formula (I): or pharmaceutically acceptable isomers, salts, solvates or esters of the compound of Formula (I), wherein each of the substituents is as specified herein, formulations including the above compounds, processes for preparing the same and methods for treating atherosclerosis, hypercholesterolemia, or sitosterolemia, and for lowering plasma levels of sterols and/or stanols.

    摘要翻译： 本发明提供由结构式（I）表示的化合物或式（I）化合物的药学上可接受的异构体，盐，溶剂合物或酯，其中每个取代基如本文所述，包括上述化合物的制剂，方法 用于制备它们以及用于治疗动脉粥样硬化，高胆固醇血症或静脉麻醉的方法，以及用于降低甾醇和/或甾醇的血浆水平。

    Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
    37.
    再颁专利
    Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents 有权
    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：USRE37721E1

    公开(公告)日：2002-05-28

    申请号：US09594996

    申请日：2000-06-15

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

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

    IPC分类号： C07D20508

    CPC分类号： C07D205/08 ,  A61K9/2018 ,  A61K9/4858 ,  A61K31/21 ,  A61K31/35 ,  A61K31/395 ,  A61K31/40 ,  A61K45/06 ,  Y02P20/55 ,  Y10S514/824 ,  A61K2300/00

    摘要： Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula or a pharmaceutically acceptable salt thereof, wherein: Ar1 and Ar2 are aryl or R4-substituted aryl; Ar3 is aryl or R5-substituted aryl; X, Y and Z are —CH2—, —CH(lower alkyl)— or —C(dilower alkyl)—; R and R2 are —OR6, —O(CO)R6, —O(CO)OR9 or —O(CO)NR6R7; R1 and R3 are H or lower alkyl; q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is O and r is 1, the sum of m, q and n is 1-5; R4 is selected from lower alkyl, R5, —CF3, —CN, —NO2 and halogen R5 is selected from —OR6, —O(CO)R6, —O(CO)OR9, —O(CH2)1-5OR6, —O(CO)NR6R7, —NR6R7, —NR6(CO)R7, —NR6(CO)OR9, —NR6(CO)NR7R8, —NR6SO2R9, —COOR6, —CONR6R7, —COR6, —SO2NR6R7, S(O)0-2R9, —O(CH2)1-10—COOR6, —O(CH2)1-10CONR6R7, —(lower alkylene)COOR6 and —CH═CH—COOR6; R6, R7 and R8 are H, lower alkyl or aryl-substituted Ic R9 is lower alkyl, aryl or aryl-substituted lower alkyl; are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, pharmaceutical compositions containing them; and a process for preparing them.

    摘要翻译： 羟基取代的氮杂环丁酮低胆固醇血症药或其药学上可接受的盐，其中：Ar1和Ar2是芳基或R4取代的芳基; Ar3是芳基或R5-取代的芳基; X，Y和Z是-CH2-，-CH（ 低级烷基） - 或-C（二卤代烷基） - ; R和R 2为-OR 6，-O（CO）R 6，-O（CO）OR 9或-O（CO）NR 6 R 7; R 1和R 3为H或低级烷基; q为0或1; r为0或1; m，n和p为0-4; 条件是q和r中的至少一个为1，m，n，p，q和r的和为1-6; 并且条件是当p为O且r为1时，m，q和n的和为1-5; R 4选自低级烷基，R 5，-CF 3，-CN，-NO 2，卤素R 5选自-OR 6 ，-O（CO）R 6，-O（CO）OR 9，-O（CH 2）1-5 OR 6，-O（CO）NR 6 R 7，-NR 6 R 7，-NR 6（CO）R 7，-NR 6（CO）OR 9，-NR 6 （CO）NR7R8，-NR6SO2R9，-COOR6，-CONR6R7，-COR6，-SO2NR6R7，S（O）0-2R9，-O（CH2）1-10-COOR6，-O（CH2）1-10CONR6R7， - （ 低级亚烷基）COOR 6和-CH = CH-COOR 6; R6，R7和R8是H，低级烷基或芳基取代的IcR9是低级烷基，芳基或芳基取代的低级烷基;以及降低血清的方法 通过单独或与胆固醇生物合成抑制剂组合施用所述化合物，含有它们的药物组合物; 和一个准备它们的过程。

    Muscarinic antagonists
    38.
    发明授权
    Muscarinic antagonists 有权
    毒蕈碱拮抗剂

    公开(公告)号：US06294554B1

    公开(公告)日：2001-09-25

    申请号：US09651652

    申请日：2000-08-30

    申请人： John W. Clader ,  Joseph A. Kozlowski ,  Stuart W. McCombie ,  Michael W. Miller ,  Susan F. Vice

    发明人： John W. Clader ,  Joseph A. Kozlowski ,  Stuart W. McCombie ,  Michael W. Miller ,  Susan F. Vice

    IPC分类号： A61K31445

    CPC分类号： C07D401/14 ,  C07D211/58 ,  C07D405/14

    摘要： Amide derivatives of 1,4 di-substituted piperidine compounds of the formula or a pharmaceutically acceptable salt, ester or solvate thereof, wherein Q and Q1 are each —CH═, or one of Q and Q1 is —CH═ and the other is —N═; X is —CH2— or Y and Z are —C(R5)═, or one of Y and Z is —C(R5)═ and the other is —N═; R1 is 1 to 3 substituents selected from H, halogen and alkoxy; R2 and R5 are 1 to 3 substituents selected from H, halogen, alkyl and alkoxy; and R3 and R4 are H or (C1-C6)alkyl are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed.

    摘要翻译： 式II的1,4-二取代哌啶化合物的酰胺衍生物或其药学上可接受的盐，酯或溶剂化物，其中Q和Q1各自为-CH =，或Q和Q1中的一个为-CH =，另一个为-N = ; X是-CH 2 - 或Y，Z是-C（R 5）=，或Y和Z之一是-C（R 5）=，另一个是-N =; R 1是1至3个选自H，卤素和 烷氧基; R2和R5是1至3个选自H，卤素，烷基和烷氧基的取代基; 和R 3和R 4是H或（C 1 -C 6）烷基是用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。 还公开了药物组合物和制备方法。

    Spirocycloalkyl-substituted azetidinones useful as hypocholesterolemic agents
    39.
    发明授权
    Spirocycloalkyl-substituted azetidinones useful as hypocholesterolemic agents 失效
    螺环烷基取代的氮杂环丁酮可用作低胆固醇血症药

    公开(公告)号：US5698548A

    公开(公告)日：1997-12-16

    申请号：US449980

    申请日：1995-05-25

    申请人： Sundeep Dugar ,  John W. Clader ,  Duane A. Burnett

    发明人： Sundeep Dugar ,  John W. Clader ,  Duane A. Burnett

    IPC分类号： A61K31/395 ,  A61K31/397 ,  A61K31/435 ,  A61K31/695 ,  A61P3/06 ,  A61P9/10 ,  C07D205/12 ,  C07D471/10 ,  C07F7/18 ,  C07D7/10

    CPC分类号： C07D471/10 ,  C07D205/12

    摘要： Novel compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R.sub.1 is ##STR2## R.sub.2 and R.sub.3 are independently selected from --CH.sub.2 --, --CH(lower alkyl)--, --C(di-lower alkyl)--, --CH.dbd.CH-- and --C(lower alkyl).dbd.CH--; or R.sub.1 with R.sub.2, or R.sub.1 with R.sub.3, form --CH.dbd.CH-- or --CH.dbd.C(lower alkyl)--; u and v are independently 0-3, provided both are not zero; R.sub.4 is B--(CH.sub.2).sub.m C(O)--; m is 0-5; B--(CH.sub.2).sub.q --; q is 0-6; B--(CH.sub.2).sub.e --Z--(CH.sub.2).sub.r ; Z is --O--, --C(O)--, phenylene, --N(R.sub.8)-- or --S(O).sub.0-2 --, e and r is 0-5; the sum of e and r is 0-6; B--(C.sub.2 -C.sub.6 alkenylene)--; B'--(C.sub.4 -C.sub.6 alkadienylene)--;B--(CH.sub.2).sub.t --Z--(C.sub.2 -C.sub.6 alkenylene)--; t is 0-3; the sum of t and the number of carbon atoms in the alkenylene chain is 2-6; B--(CH.sub.2).sub.f --V--(CH.sub.2).sub.g --; V is cycloalkylene, f is 1-5, g is 0-5; the sum of f and g is 1-6; B--(CH.sub.2).sub.t --V--(C.sub.2 -C.sub.6 alkenylene)-- or B'--(C.sub.2 -C.sub.6 alkenylene)--V--(CH.sub.2).sub.t --; the sum of t and the number of carbon atoms in the alkenylene chain is 2-6, B--(CH.sub.2).sub.a --Z--(CH.sub.2).sub.b --V--(CH.sub.2).sub.d --; a, b and d are 0-6; the sum of a, b and d is 0-6; T--(CH.sub.2).sub.s --; T is cycloalkyl, s is 0-6; or R.sub.1 and R.sub.4 together form ##STR3## B is optionally-substituted phenyl, indanyl, indenyl, naphthyl, tetrahydronaphthyl or optionally substituted-heteroaryl; and R.sub.20 and R.sub.21 are independently optionally-substituted phenyl, optionally-substituted naphthyl, indanyl, indenyl, tetrahydronaphthyl, benzodioxolyl, optionally-substituted heteroaryl, optionally-substituted benzofused heteroaryl or cyclopropyl, pharmaceutical compositions, the use as hypocholesterolemic agents, processes for preparing, and the use in combination with cholesterol biosynthesis inhibitors to treat or prevent athersclerosis.

    摘要翻译： 式（I）的新化合物或其药学上可接受的盐，其中：R 1是R 2和R 3独立地选自-CH 2 - ， - CH（低级烷基） - ， - C（二 - 低级 烷基） - ， - CH = CH-和-C（低级烷基）= CH-; 或R1与R2，或R1与R3形成-CH = CH-或-CH = C（低级烷基） - ; u和v独立为0-3，两者都不为零; R4是B-（CH2）mC（O） - ; m为0-5; B-（CH2）q-; q为0-6; B-（CH 2）e-Z-（CH 2）r; Z是-O - ， - C（O） - ，亚苯基，-N（R 8） - 或-S（O）0-2-，e和r是0-5; e和r的和为0-6; B-（C 2 -C 6亚烯基） - ; B' - （C 4 -C 6链二烯） - ; B-（CH 2）t-Z-（C 2 -C 6亚烯基） - ; t为0-3; 亚烯基链中t和碳原子数之和为2-6; B-（CH2）f-V-（CH2）g-; V是亚环烷基，f是1-5，g是0-5; f和g之和为1-6; B-（CH2）t-V-（C2-C6亚链烯基） - 或B' - （C2-C6亚烯基）-V-（CH2）t-; 亚烯基链中t和碳原子数之和为2-6，B-（CH2）a-Z-（CH2）b-V-（CH2）d-; a，b和d为0-6; a，b和d的和为0-6; T（CH 2）s - ; T是环烷基，s是0-6; 或R 1和R 4一起形成B是任选取代的苯基，茚满基，茚基，萘基，四氢萘基或任选取代的杂芳基; R20和R21独立地是任选取代的苯基，任选取代的萘基，茚满基，茚基，四氢萘基，苯并二恶唑基，任选取代的杂芳基，任选取代的苯并稠合的杂芳基或环丙基，药物组合物，用作低胆固醇血症药， 以及与胆固醇生物合成抑制剂组合用于治疗或预防硬化症的用途。