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    Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
    4.
    发明授权
    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：US07235543B2

    公开(公告)日：2007-06-26

    申请号：US10791910

    申请日：2004-03-03

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

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

    IPC分类号： C07D205/08 ,  A61K31/397 ,  A61K31/7052 ,  A61P3/06 ,  C07H7/02

    CPC分类号： C07D403/12 ,  C07D205/08 ,  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 vascular conditions, such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and 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， 用于制备相同的药物和治疗血管病症的方法，例如动脉粥样硬化或高胆固醇血症，糖尿病，肥胖症，中风，脱髓鞘和降低甾醇和/或甾醇的血浆水平。

    Substituted .beta.-lactam compounds useful as hypochlesterolemic agents and processes for the preparation thereof
    5.
    发明授权
    Substituted .beta.-lactam compounds useful as hypochlesterolemic agents and processes for the preparation thereof 失效

    公开(公告)号：US5688787A

    公开(公告)日：1997-11-18

    申请号：US588785

    申请日：1996-01-19

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

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

    IPC分类号： C07D205/08 ,  C07D205/085 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07F7/08 ,  C07F7/18 ,  A61K31/395 ,  C07D403/10

    CPC分类号： C07D401/04 ,  C07D205/08 ,  C07D205/085 ,  C07D403/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07F7/0812 ,  C07F7/186

    摘要： Novel compounds of the formula ##STR1## wherein A is --CH.dbd.CH--B; --C.tbd.C--B; --(CH.sub.2).sub.p --X--B, and X is a bone, --NH-- or --S(O).sub.0-2 --; optionally substituted heteroaryl or benzofused heteroaryl; --C(O)--B; or ##STR2## D is B'--(CH.sub.2).sub.m C(O)--, B'--(CH.sub.2).sub.q --, B'--(CH.sub.2).sub.e --Z--(CH.sub.2).sub.r, wherein Z is --O--, --C(O)--, phenylene, --NR.sub.8 -- or --S(O).sub.0-2 --, B'--(alkenylene)--; B'--(alkadienylene)--; B'--(CH.sub.2).sub.t --Z--(alkenylene), B'--(CH.sub.2).sub.f --V--(CH.sub.2).sub.g --, wherein V is cycloalkylene, B'--(CH.sub.2).sub.t --V--(alkenylene) or B'--(alkenylene)--V--(CH.sub.2).sub.t --, B'--(CH.sub.2).sub.a --Z--(CH.sub.2).sub.b --V--(CH.sub.2).sub.d --, T--(CH.sub.2).sub.s --, wherein T is cycloalkyl; naphthylmethyl or optionally substituted heteroarylmethyl; B is optionally substituted phenyl; B' is naphthyl, optionally substituted heteroaryl or optionally substituted phenyl; R is hydrogen, fluoro, alkyl, alkenyl, alkynyl, or B--(CH.sub.2).sub.n --; R.sub.4 is optionally substituted phenyl, indanyl, benzofuranyl, tetrahydronaphthyl, pyridyl, pyrazinyl, pyrimidinyl or quinolyl; are disclosed, the method of using compounds of the formula II ##STR3## wherein R.sub.20 is optionally substituted phenyl, naphthyl, heteroaryl, or benzofused heteroaryl, R.sub.21, R.sub.22 and R.sub.23 are H or R.sub.20 ; E, F and G are independently a bond; cycloalkylene; alkylene; alkenylene; alkynylene; a substituted alkylene, alkenylene or alkynylene chain; an interrupted alkylene, alkenylene or alkynylene chain; or an interrupted alkylene, alkenylene or alkynylene chain substituted by one or more substituents; or one of R.sub.21 --E and R.sub.22 --F is selected from the group consisting of halogeno, OH, alkoxy, --OC(O)R.sub.5, --NR.sub.10 R.sub.11, --SH or --S(alkyl); R.sub.5 is alkyl, phenyl, R.sub.14 -phenyl, benzyl or R.sub.14 -benzyl; R.sub.10 and R.sub.11 are independently selected from H and lower alkyl, or a pharmaceutically acceptable salt thereof, in a pharmaceutically aceptable carrier as hypocholesterolemic agents is also disclosed.

    Substituted Azetidinone Compounds, Processes for Preparing the Same, Formulations and Uses Thereof
    6.
    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：US20080234248A1

    公开(公告)日：2008-09-25

    申请号：US12108885

    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 ,  C07D205/02 ,  A61P9/00

    CPC分类号： C07D405/12 ,  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。

    Combinations of hydroxy-substituted azetidinone compounds and HMG CoA Reductase Inhibitors
    8.
    发明授权
    Combinations of hydroxy-substituted azetidinone compounds and HMG CoA Reductase Inhibitors 失效
    羟基取代的氮杂环丁酮化合物与HMG CoA还原酶抑制剂的组合

    公开(公告)号：US5846966A

    公开(公告)日：1998-12-08

    申请号：US953825

    申请日：1997-10-14

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

    CPC分类号： A61K45/06 ,  A61K31/21 ,  A61K31/35 ,  A61K31/395 ,  A61K31/40 ,  A61K9/2018 ,  A61K9/4858 ,  Y10S514/824

    摘要： Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar.sup.1 and Ar.sup.2 are aryl or R.sup.4 -substituted aryl; Ar.sup.3 is aryl or R.sup.5 -substituted aryl; X, Y and Z are --CH.sub.2 --, --CH(lower alkyl)-- or --C(dilower alkyl)--; R and R.sup.2 are --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 or --O(CO)NR.sup.6 R.sup.7 ; R.sup.1 and R.sup.3 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 0 and r is 1, the sum of m, q and n is 1-5; R.sup.4 is selected from lower alkyl, R.sup.5, --CF.sub.3, --CN, --NO.sub.2 and halogen; R.sup.5 is selected from --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --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 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --(lower alkylene)COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ; R.sup.6, R.sup.7 and R.sup.8 are H, lower alkyl, aryl or aryl-substituted lower alkyl; R.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, alone or in combination with a cholesterol biosynthesis inhibitor, pharmaceutical compositions containing them, and a process for preparing them.

    摘要翻译： 式（I）的羟基取代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和Ar 2是芳基或R 4取代的芳基; Ar 3是芳基或者R 5取代的芳基; X，Y和Z是-CH 2 - ， - 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; R1和R3是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中的至少一个是1，m，n，p，q和r的和是1-6; 并且当p为0且r为1时，m，q和n的和为1-5; R4选自低级烷基，R5，-CF3，-CN，-NO2和卤素; R5选自-OR6，-O（CO）R6，-O（CO）OR9，-O（CH2）1-5OR6，-O（CO）NR6R7，-NR6R7，-NR6（CO）R7，-NR6（ CO）OR 9，-NR 6（CO）NR 7 R 8，-NR 6 SO 2 R 9，-COOR 6，-CONR 6 R 7，-COR 6，-SO 2 NR 6 R 7，S（O）0-2R 9，-O（CH 2）1-10 -COOR 6，-O 1-10CONR6R7， - （低级亚烷基）COOR6和-CH = CH-COOR6; R6，R7和R8是H，低级烷基，芳基或芳基取代的低级烷基; R9是低级烷基，芳基或芳基取代的低级烷基; 以及通过单独或与胆固醇生物合成抑制剂组合使用所述化合物，含有它们的药物组合物及其制备方法来降低血清胆固醇的方法。

    4-[(heterocycloalkyl or heteroaromatic)-substituted phenyl]-2-azetidinones useful as hypolipidemic agents
    9.
    发明授权
    4-[(heterocycloalkyl or heteroaromatic)-substituted phenyl]-2-azetidinones useful as hypolipidemic agents 失效
    4 - [（杂环烷基或杂芳族） - 取代的苯基] -2-氮杂环丁酮，可用作降血脂药

    公开(公告)号：US5656624A

    公开(公告)日：1997-08-12

    申请号：US361265

    申请日：1994-12-21

    申请人： Wayne D. Vaccaro ,  Duane A. Burnett ,  John W. Clader

    发明人： Wayne D. Vaccaro ,  Duane A. Burnett ,  John W. Clader

    IPC分类号： A61K31/397 ,  A61K31/41 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  A61P3/06 ,  A61P9/10 ,  C07D205/08 ,  C07D205/12 ,  C07D401/10 ,  C07D403/12 ,  C07D413/10 ,  C07D491/08 ,  C07D491/10 ,  C07D491/113 ,  C07D521/00 ,  A61K31/395

    CPC分类号： C07D231/12 ,  C07D205/08 ,  C07D205/12 ,  C07D233/56 ,  C07D249/08 ,  C07D403/12 ,  C07D413/10 ,  C07D491/08 ,  C07D491/10

    摘要： 4-[(Heterocycloalkyl or heteroaromatic)-substituted phenyl]-2-azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: A is optionally substituted heterocycloalkyl, heteroaryl, benzofused heterocycloalkyl, or benzofused heteroaryl;Ar.sup.1 and Ar.sup.2 are optionally substituted aryl;Q is a bond or, with the 3-position ring carbon of the azetidinone, forms a spiro group; andR.sup.1 is alkylene; alkylene wherein a carbon in the chain is replaced by --O--, --C(O)--, phenylene, --NR.sup.8 --, --S(O).sub.0-2 -- or cycloalkylene; or alkenylene; or, when Q is a bond, R.sup.1 can be alkylene substituted by one or two hydroxy groups or hydroxy derivatives, wherein the alkylene chain can optionally be joined to Ar.sup.1 through --O-- or --S(O).sub.0-2 -- or joined to the azetidinone ring through a --S(O).sub.0-2 -- group;a method of lowering serum cholesterol by administering said compounds, pharmaceutical compositions containing them, and the combination of a substituted azetidinone and a cholesterol biosynthesis inhibitor for the treatment and prevention of atherosclerosis.

    摘要翻译： 4 - [（杂环烷基或杂芳族） - 取代的苯基] -2-氮杂环丁酮低血胆固醇药物或其药学上可接受的盐，其中：A是任选取代的杂环烷基，杂芳基，苯并稠合的杂环烷基或苯并稠合的杂芳基; Ar1和Ar2是任选取代的芳基; Q是键或与氮杂环丁酮的3-位环碳形成螺环; 并且R 1是亚烷基; 亚烷基，其中链中的碳被-O - ， - C（O） - ，亚苯基，-NR 8 - ， - S（O）0-2 - 或亚环烷基取代; 或亚烯基; 或者当Q为键时，R 1可以是被一个或两个羟基或羟基衍生物取代的亚烷基，其中亚烷基链可以任选地与Ar 1至-O-或-S（O）0-2-连接或连接到 氮杂环丁酮环通过-S（O）0-2-基团; 通过施用所述化合物，含有它们的药物组合物和取代的氮杂环丁酮和胆固醇生物合成抑制剂的组合来降低血清胆固醇的方法用于治疗和预防动脉粥样硬化。