公开(公告)号：US20100144765A1

公开(公告)日：2010-06-10

申请号：US12707838

申请日：2010-02-18

申请人： Deidre Mary Bernadette HICKEY ,  Robert John IFE ,  Colin Andrew LEACH ,  Ivan Leo PINTO ,  Stephen Allan SMITH ,  Steven James STANWAY

发明人： Deidre Mary Bernadette HICKEY ,  Robert John IFE ,  Colin Andrew LEACH ,  Ivan Leo PINTO ,  Stephen Allan SMITH ,  Steven James STANWAY

IPC分类号： A61K31/519

CPC分类号： C07D239/56 ,  C07D239/60 ,  C07D239/70 ,  C07D239/95 ,  C07D401/12 ,  C07D403/12 ,  C07D495/04

摘要： Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atherosclerosis.

摘要翻译： 式（I）的嘧啶酮化合物：是Lp-PLA2酶的抑制剂，可用于治疗动脉粥样硬化。

公开(公告)号：US20080090853A1

公开(公告)日：2008-04-17

申请号：US11626882

申请日：2007-01-25

申请人： Colin Andrew LEACH

发明人： Colin Andrew LEACH

IPC分类号： A61K31/517 ,  A61K31/4427 ,  C07D471/04

CPC分类号： C07D471/04 ,  C07D401/12

摘要： A compound of formula (I) wherein: R1 is an aryl group, unsubstituted or substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from the group consisting of C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, aryl C1-C6 alkoxy, hydroxy, halo, CN, COR6, COOR6, NR6COR7, CONR8R9, SO2NR8R9, NR6SO2R7, NR8R9, halo C1-C4 alkyl, and halo C1-C4 alkoxy; W is CH and X is N, or W is N and X is CH, or W and X are CH; Y is C2-C4alkyl, R2 is hydrogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, aryl C1-C6 alkoxy, hydroxy, halo, CN, COR6, carboxy, COOR6, NR6COR7, CONR8R9, SO2NR8R9, NR6SO2R7, NR8R9, mono to perfluoro-C1-C6 alkyl, or mono to perfluoro-C1-C6 alkoxy; n is 0-5; R3 is C1-C4 alkyl; R4 is C1-C4 alkyl; R5 is hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, halo C1-C4 alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl C1-C4 alkyl, C5-C8cycloalkenyl, C5-C8cycloalkenyl C1-C4 alkyl, 3-8-membered heterocycloalkyl, 3-8-membered heterocycloalkyl C1-C4 alkyl, C6-C14 aryl, C6-C14 aryl C1-C10 alkyl, heteroaryl, or heteroaryl C1-C10alkyl; wherein each group is optionally one or more times by the same and/or a different group which is C1-C6 alkoxy, C1-C6 alkylthio, aryl C1-C6 alkoxy, hydroxy, halo, CN, NR8R9, or halo C1-C4 alkoxy R6 and R7 are independently hydrogen or C1-C10 alkyl; R8 and R9 are the same or different and are hydrogen or C1-C10 alkyl, or R9 and R10 together with the nitrogen to which they are attached form a 5- to 7 membered ring optionally containing one or more further heteroatoms selected from oxygen, nitrogen and sulphur, and optionally substituted by one or two substituents selected from the group consisting of hydroxy, oxo, C1-C4 alkyl, C1-C4 alkylcarboxy, aryl, and aryl C1-C4 alkyl; or a pharmaceutically acceptable salt thereof. These compounds are useful for treating atherosclerosis or other inflammatory diseases.

公开(公告)号：US20080090851A1

公开(公告)日：2008-04-17

申请号：US11626875

申请日：2007-01-25

申请人： Colin Andrew LEACH

发明人： Colin Andrew LEACH

IPC分类号： A61K31/519 ,  C07D487/04

CPC分类号： A61K31/519

摘要： A compound of formula (I) wherein the various groups are defined herein. or a pharmaceutically acceptable salt thereof.These compounds are useful for treating atherosclerosis and other inflammatory diseases.

公开(公告)号：US20080090852A1

公开(公告)日：2008-04-17

申请号：US11626879

申请日：2007-01-25

申请人： Colin Andrew LEACH

发明人： Colin Andrew LEACH

IPC分类号： A61K31/519 ,  C07D487/04

CPC分类号： C07D471/04

摘要： A compound of formula (I) wherein the various groups are defined herein, or a pharmaceutically acceptable salt thereof.These compounds are useful for treating atherosclerosis and other inflammatory diseases.

摘要翻译： 其中各种基团在本文中定义的式（I）化合物或其药学上可接受的盐。 这些化合物可用于治疗动脉粥样硬化和其他炎性疾病。