CHEMICAL PROCESSES FOR THE MANUFACTURE OF SUBSTITUTED BENZOFURANS
    2.
    发明申请
    CHEMICAL PROCESSES FOR THE MANUFACTURE OF SUBSTITUTED BENZOFURANS 审中-公开
    化学方法制备取代的苯甲醚

    公开(公告)号:WO2012006686A1

    公开(公告)日:2012-01-19

    申请号:PCT/AU2011/000900

    申请日:2011-07-15

    IPC分类号: C07D307/86

    摘要: The present invention relates to the scaled-up synthesis of biologically active compounds which display useful therapeutic activity in treating proliferative disorders. In particular the invention relates to process methods for the kilogram scale synthesis of a particular class of substituted benzofuran tubulin polymerisation inhibitors.

    摘要翻译: 本发明涉及在治疗增殖性疾病中显示有用的治疗活性的生物活性化合物的放大合成。 特别地,本发明涉及用于特定类别的取代的苯并呋喃微管蛋白聚合抑制剂的千克级合成的方法。

    3-ARYLOXY/ THIO-2, 3-SUBSTITUTED PROPANAMINES AND THEIR USE IN INHIBITING SEROTONIN AND NOREPINEPHRINE REUPTAKE
    4.
    发明申请
    3-ARYLOXY/ THIO-2, 3-SUBSTITUTED PROPANAMINES AND THEIR USE IN INHIBITING SEROTONIN AND NOREPINEPHRINE REUPTAKE 审中-公开
    3-ARYLOXY / THIO-2,3替代丙胺及其用于抑制丝氨酸和诺贝环素再次使用

    公开(公告)号:WO2004043903A1

    公开(公告)日:2004-05-27

    申请号:PCT/US2003/031513

    申请日:2003-10-24

    IPC分类号: C07C217/62

    摘要: There is provided a compound of formula (I) wherein A is selected from -O- and -S-; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C 1 -C 4 alkyl and C 1 -C 4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C 1 -C 4 alkyl, and C 2 -C 8 alkyl, C 2 -C 8 alkenyl, C 3 -C 8 cycloalkyl and C 4 -C 8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkyl-S(O)n- where n is 0, 1 or 2, -CF 3 , -CN and -CONH 2 ; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkyl-S(O)n- where n is 0, 1 or 2, nitro, acetyl, -CF 3 , -SCF 3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C 1 -C 4 alkyl; Z is selected from OR 3 or F, wherein R 3 is selected from H, C 1 -C 6 alkyl and phenyl C 1 -C 6 alkyl; R 1 and R 2 are each independently H or C 1 -C 4 alkyl; and pharmaceutically acceptable salts thereofwith the proviso that when Y is optionally substituted phenyl or optionally substituted 1,3-benzodioxolyl and Z is OR 3 and X is optionally substituted phenyl then A is -S-.

    摘要翻译: 提供式(I)的化合物,其中A选自-O-和-S-; X选自任选被至多5个独立地选自卤素,C 1 -C 4烷基和C 1 -C 4烷氧基的取代基取代的苯基,任选被至多3个独立地选自卤素和C 1 -C 4烷基的取代基取代的噻吩基, C 8烷基,C 2 -C 8烯基,C 3 -C 8环烷基和C 4 -C 8环烷基烷基,其各自可以任选被至多3个独立地选自卤素,C 1 -C 4烷基,C 1 -C 4烷氧基,C 1 -C 4烷基 -S(O)n - ,其中n为0,1或2,-CF 3,-CN和-CONH 2; Y选自苯基,萘基,二氢苯并噻吩基,苯并噻唑基,苯并异噻唑基,喹啉基,异喹啉基,萘啶基,噻吩并吡啶基,茚满基,1,3-苯并二恶唑基,苯并噻吩基,吲哚基和苯并呋喃基,其中每个可以任选被至多4个取代, 可能的是至多5个独立地选自卤素,C 1 -C 4烷基,C 1 -C 4烷氧基,C 1 -C 4烷基-S(O)n取代基的取代基,其中n为0,1或2,硝基,乙酰基,-CF 3 - SCF3和氰基; 当Y为吲哚基时,其可以被选自C 1 -C 4烷基的N-取代基取代或进一步取代; Z选自OR 3或F,其中R 3选自H,C 1 -C 6烷基和苯基C 1 -C 6烷基; R1和R2各自独立地为H或C1-C4烷基; 其药学上可接受的盐,条件是当Y是任选取代的苯基或任选取代的1,3-苯并二恶唑基,Z是OR 3,X是任选取代的苯基,则A是-S-。

    ORGANIC COMPOUNDS
    5.
    发明申请
    ORGANIC COMPOUNDS 审中-公开
    有机化合物

    公开(公告)号:WO2004000793A2

    公开(公告)日:2003-12-31

    申请号:PCT/EP2003/006490

    申请日:2003-06-18

    IPC分类号: C07C255/00

    摘要: The invention relates to compounds of the general formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 8’ , R 9 , W, a, b and n have the significances given in claim 1, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.

    摘要翻译: 本发明涉及通式(I)的化合物,其中R1,R2,R3,R4,R5,R6,R7,R8,R8',R9,W,a,b和n具有权利要求1中给出的含义, 和任选的其对映异构体。 活性成分具有有利的杀虫特性。 它们特别适用于控制温血动物的寄生虫。