PHENYLPYRIDONE DERIVATIVE
    2.
    发明授权
    PHENYLPYRIDONE DERIVATIVE 有权
    苯基吡啶酮衍生物

    公开(公告)号:EP1921065B1

    公开(公告)日:2010-10-20

    申请号:EP06797001.2

    申请日:2006-08-23

    摘要: A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents -CH2-O-, -CH=CH- or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.

    摘要翻译: 含有由式(I)表示的化合物作为活性成分:其中R 1和R 2独立地表示氢原子,低级烷基等,或R 1与连接有L,Z 2和R 1的氮原子一起 可以形成脂肪族含氮杂环基,并且R 1和R 2与它们所连接的氮原子一起可以形成脂肪族含氮杂环基; X代表次甲基或氮原子; Y表示-CH 2 -O - , - CH = CH-等; Z1表示单键,C1-4亚烷基等; Z2表示单键或C1-4亚烷基; L表示亚甲基,C 3-8亚环烷基等; Ar表示芳族碳环基团等。 该化合物可用作中枢神经系统疾病,心血管疾病或代谢疾病的药物。

    SPIROCHROMANON DERIVATIVES
    8.
    发明公开
    SPIROCHROMANON DERIVATIVES 有权
    螺旋色素衍生物

    公开(公告)号:EP2120569A2

    公开(公告)日:2009-11-25

    申请号:EP08705516.6

    申请日:2008-01-08

    IPC分类号: A01N43/16 A61K31/35

    摘要: The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-b]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a methine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.

    摘要翻译: 本发明涉及通式(I)的化合物:其中Ar 1表示由选自苯,吡唑,异恶唑,吡啶,吲哚,1H-吲唑,1H-呋喃并[2,1- 1H-噻吩并[2,3-c]吡唑,苯并咪唑,1,2-苯并异恶唑,咪唑并[1,2-a]吡啶,咪唑并[1,5-a]吡啶和1H-吡唑并[ 3,4-b]吡啶,其具有Ar 2,并且任选地具有一个或两个或更多个选自R 3的取代基; R 1和R 2各自独立地表示氢原子,卤素原子,氰基,C 2 -C 6烯基,C 1 -C 6烷氧基,C 2 -C 7烷酰基,C 2 -C 7烷氧基羰基,芳烷氧基羰基, 氨基甲酰基-C1-C6烷氧基,羧基-C2-C6链烯基或-Q1-N(Ra)-Q2-Rb的基团; 或任选具有取代基的C1-C6烷基; 或任选具有取代基的芳基或杂环基团; 或具有芳基或杂环基的C1-C6烷基或C2-C6烯基; T和U各自独立地表示氮原子或次甲基; V代表氧原子或硫原子。 本发明的化合物可用作各种ACC相关疾病的治疗剂。

    NOVEL AMINOPYRIMIDINE DERIVATIVE AS PLK1 INHIBITOR
    9.
    发明公开
    NOVEL AMINOPYRIMIDINE DERIVATIVE AS PLK1 INHIBITOR 审中-公开
    使用氨基嘧啶衍生物ALS PLK1抑制剂

    公开(公告)号:EP2116543A1

    公开(公告)日:2009-11-11

    申请号:EP07851126.8

    申请日:2007-12-20

    CPC分类号: C07D471/04

    摘要: The present invention relates to a compound represented by Formula [I]:

    or a pharmaceutically acceptable salt or ester thereof, wherein R 1 and R 2 , which may be the same or different, are each a hydrogen atom, a lower alkyl group, a cycloalkyl group, or the like; R 3 and R 4 , which may be the same or different, are each a hydrogen atom, a lower alkyl group, NR a R b , a phenyl group, a lower alkyl group substituted with a phenyl group, a 4- to 7-membered aliphatic heterocyclic group, a lower alkyl group substituted with a 4- to 7-membered aliphatic heterocyclic group, a 5- or 6-membered aromatic heterocyclic group, a lower alkyl group substituted with a 5- or 6-membered aromatic heterocyclic group, or the like; and R 5 is a hydrogen atom, a cyano group, a halogen atom, or a lower alkyl group.

    摘要翻译: 本发明涉及由式[I]表示的化合物或其药学上可接受的盐或酯,其中R 1和R 2可以相同或不同,分别为氢原子,低级烷基, 环烷基等; R 3和R 4可以相同或不同,分别为氢原子,低级烷基,NR a R b,苯基,被苯基取代的低级烷基,4-至7- 被4至7元脂族杂环基取代的低级烷基,5或6元芳族杂环基,被5或6元芳族杂环基取代的低级烷基, 或类似物; R 5为氢原子,氰基,卤素原子或低级烷基。

    REACTION APPARATUS, AND REACTION METHOD
    10.
    发明公开
    REACTION APPARATUS, AND REACTION METHOD 审中-公开
    REAKTIONSAPPARAT UND REAKTIONSVERFAHREN

    公开(公告)号:EP2065354A1

    公开(公告)日:2009-06-03

    申请号:EP07807353.3

    申请日:2007-09-14

    摘要: The present invention is directed at obtaining a high yield of a target substance and simultaneously securing high productivity.
    A reaction apparatus 10 has: a main flow channel 12 having an inner diameter of 3 mm, in which a raw material M 1 flows; an introduction flow channel 14 in which a raw material M 2 that causes a chemical reaction with the raw material M 1 flows; and five branch introduction flow channels 16a to 16e which are branched from the introduction flow channel 14 and introduce the raw material M 2 to the main flow channel 12, at predetermined introduction points 12o to 12s in the main flow channel 12. Here, in the main flow channel 12, the flow channel lengths of the flow channels 12b to 12d between adjacent introduction points 12p to 12s are not longer than those of the flow channels 12a to 12c between the next previous adjacent introduction points 12o to 12r in a flow direction of the raw material M 1 . At least one length of the flow channels 12b to 12d between the adjacent introduction points 12p to 12s is shorter than lengths of the flow channels 12a to 12c between previous adjacent introduction points 12o to 12r in the flow direction of the raw material M 1 .

    摘要翻译: 本发明涉及获得高产率的目标物质并同时确保高生产率。 反应装置10具有:原料M 1流入的内径为3mm的主流路12; 导入与原料M 1发生化学反应的原料M 2的导入流路14; 以及从导入流路14分支并将原料M 2引导到主流路12的5个分支导入流路16a〜16e,在主流路12的规定的导入点12o〜12s。这里, 主流路12中,相邻导入点12p〜12s之间的流路12b〜12d的流路长度不比前一相邻导入点12o〜12r之间的流路12a〜12c的流路长度在流动方向 原料M 1。 相邻导入点12p〜12s之间的流路12b〜12d的至少一个长度比原料M 1的流动方向上的前一相邻导入点12o〜12r之间的流路12a〜12c的长度短。