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    PHENOXY BENZAMIDE COMPOUNDS WITH UTILITY IN THE TREATMENT OF TYPE 2 DIABETES AND OBESITY
    2.
    发明公开
    PHENOXY BENZAMIDE COMPOUNDS WITH UTILITY IN THE TREATMENT OF TYPE 2 DIABETES AND OBESITY 审中-公开
    PHENOXYBENZAMIDVERBINDUNGEN参与了2型糖尿病和利益肥胖的治疗方法有

    公开(公告)号：EP1856056A1

    公开(公告)日：2007-11-21

    申请号：EP05791490.5

    申请日：2005-10-11

    申请人： AstraZeneca AB

    发明人： JOHNSTONE, Craig ,  MCKERRECHER, Darren ,  PIKE, Kurt Gordon ,  WARING, Michael James

    IPC分类号： C07D231/40 ,  C07D213/80 ,  C07D403/12

    CPC分类号： C07D213/80 ,  C07D231/40 ,  C07D403/12

    摘要： Compounds of Formula: (I); wherein: R1 is methoxymethyl; R2 is selected from -C(O)NR4R5, SO2NR4R5, S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.

    QUINAZOLINE DERIVATIVES AS ANGIOGENESIS INHIBITORS
    7.
    发明公开
    QUINAZOLINE DERIVATIVES AS ANGIOGENESIS INHIBITORS 有权
    喹唑啉衍生物的血管生成抑制剂

    公开(公告)号：EP1154774A1

    公开(公告)日：2001-11-21

    申请号：EP00902730.1

    申请日：2000-02-08

    申请人： AstraZeneca AB ,  Zeneca-Pharma SA

    发明人： HENNEQUIN, Laurent, François, Andre ,  PLE, Patrick ,  STOKES, Elaine, Sophie, Elizabeth ,  MCKERRECHER, Darren

    IPC分类号： A61K31/505 ,  C07D401/14 ,  C07D413/14 ,  C07D417/12 ,  C07D405/12 ,  C07D401/12

    CPC分类号： A61K31/505 ,  A61K31/517 ,  C07D231/12 ,  C07D233/56 ,  C07D239/88 ,  C07D239/94 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

    摘要： The invention relates to the use of compounds of formula (I), wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1-3 heteroatoms selected independently from O, N and S; Z is -O-, -NH-, -S-, -CH2- or a direct bond; n is 0-5; m is 0-3; R2 represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C¿1-3?alkyl, C1-3alkoxy, C1-3alkylsulphanyl, -NR?3R4¿ (wherein R?3 and R4¿, which may be the same or different, each represents hydrogen or C¿1-3?alkyl), or R?5X1¿- (wherein X?1 and R5¿ are as defined herein; R1 represents hydrogen, oxo, halogeno, hydroxy, C¿1-4?alkoxy, C1-4alkyl, C1-4alkoxymethyl, C1-4alkanoyl, C1-4haloalkyl, cyano, amino, C2-5alkenyl, C2-5alkynyl, C1-3alkanoyloxy, nitro, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylsulphanyl, C1-4alkylsulphinyl, C1-4alkylsulphonyl, carbamoyl, N-C1-4alkylcarbamoyl, N,N-di(C1-4alkyl)carbamoyl, aminosulphonyl, N-C1-4alkylaminosulphonyl, N,N-di(C1-4alkyl)aminosulphonyl, N-(C1-4alkylsulphonyl)amino, N-(C1-4alkylsulphonyl)-N-(C1-4alkyl)amino, N,N-di(C1-4alkylsulphonyl)amino, a C3-7alkylene chain joined to two ring C carbon atoms, C1-4alkanoylaminoC1-4alkyl, carboxy or a group R?56X10¿ (wherein X?10 and R56¿ are as defined herein); and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula (I). The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

    QUINAZOLINE DERIVATIVES AS ANGIOGENESIS INHIBITORS AND INTERMEDIATES THEREFORE
    9.
    发明公开
    QUINAZOLINE DERIVATIVES AS ANGIOGENESIS INHIBITORS AND INTERMEDIATES THEREFORE 有权
    ZWISCHENPRODUKTEDAFÜR的中华人民共和国

    公开(公告)号：EP1553097A1

    公开(公告)日：2005-07-13

    申请号：EP05004285.2

    申请日：2000-02-08

    申请人： AstraZeneca AB

    发明人： Hennequin, Laurent François André ,  PLE, Patrick ,  Stokes, Elaine Sophie ,  MCKERRECHER, Darren

    IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/12 ,  C07D405/12 ,  C07D401/12 ,  A61K31/505 ,  C07D209/08

    CPC分类号： A61K31/505 ,  A61K31/517 ,  C07D231/12 ,  C07D233/56 ,  C07D239/88 ,  C07D239/94 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

    摘要： The invention relates to the use of compounds of the formula I:
    wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1-3 heteroatoms selected independently from O, N and S; Z is -O-, -NH-, -S-, -CH 2 - or a direct bond; n is 0-5; m is 0-3; R 2 represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylsulphanyl, -NR 3 R 4 (wherein R 3 and R 4 , which may be the same or different, each represents hydrogen or C 1-3 alkyl), or R 5 X 1 - (wherein X 1 and R 5 are as defined herein; R 1 represents hydrogen, oxo, halogeno, hydroxy, C 1-4 alkoxy, C 1-4 alkyl, C 1-4 alkoxymethyl, C 1-4 alkanoyl, C 1-4 haloalkyl, cyano, amino, C 2-5 alkenyl, C 2-5 alkynyl, C 1-3 alkanoyloxy, nitro, C 1-4 alkanoylamino, C 1-4 alkoxycarbonyl, C 1-4 alkylsulphanyl, C 1-4 alkylsulphinyl, C 1-4 alkylsulphonyl, carbamoyl, N -C 1-4 alkylcarbamoyl, N , N -di(C 1-4 alkyl)carbamoyl, aminosulphonyl, N -C 1-4 alkylaminosulphonyl, N , N -di(C 1-4 alkyl)aminosulphonyl, N -(C 1-4 alkylsulphonyl)amino, N -(C 1-4 alkylsulphonyl)- N -(C 1-4 alkyl)amino, N , N -di(C 1-4 alkylsulphonyl)amino, a C 3-7 alkylene chain joined to two ring C carbon atoms, C 1-4 alkanoylaminoC 1-4 alkyl, carboxy or a group R 56 X 10 (wherein X 10 and R 56 are as defined herein); and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula I. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

    摘要翻译： 本发明涉及式I化合物：的用途，其中环C是8,9,10,12或13元双环或三环部分，其任选地可以含有1-3个独立地选自O，N 和S; Z是-O-，-NH-，-S-，-CH 2 - 或直接键; n为0-5; m为0-3; R 2表示氢，羟基，卤代，氰基，硝基，三氟甲基，C 1-3烷基，C 1-3烷氧基，C 1-3烷基硫基，-NR 3 R 4（其中R 3和R 4， 其可以相同或不同，各自表示氢或C 1-3烷基）或R 5 X 1 - （其中X 1和R 5如本文所定义; R 1表示氢， 氧代，卤代，羟基，C1-4烷氧基，C1-4烷基，C1-4烷氧基甲基，C1-4烷酰基，C1-4卤代烷基，氰基，氨基，C2-5烯基，C2-5炔基，C1-3烷酰氧基，硝基，C1-4烷酰基氨基，C1- C 1-4烷基磺酰基，C 1-4烷基亚磺酰基，C 1-4烷基磺酰基，氨基甲酰基，N-C 1-4烷基氨基甲酰基，N，N-二（C 1-4烷基）氨基甲酰基，氨基磺酰基，N-C 1-4烷基氨基磺酰基，N，N-二（C1- （C 1-4烷基磺酰基）氨基，N-（C 1-4烷基磺酰基）-N-（C 1-4烷基）氨基，N，N-二（C 1-4烷基磺酰基）氨基，连接到二 环C碳原子，C 1-4烷酰基氨基C 1-4烷基，羧基或基团R 56 X 10（其中X 10和R 56如本文所定义）;及其盐，在t 他制造用于生产温血动物中抗血管生成和/或血管通透性降低作用的药物，制备这些化合物的方法，含有式I化合物或其药学上可接受的盐作为活性物质的药物组合物 成分和式I的化合物。式I化合物及其药学上可接受的盐抑制VEGF在治疗许多疾病状态（包括癌症和类风湿性关节炎）中具有价值的性质。