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    Quinazoline derivatives
    1.
    发明授权
    Quinazoline derivatives 失效
    喹唑啉衍生物

    公开(公告)号：US06806274B1

    公开(公告)日：2004-10-19

    申请号：US10019945

    申请日：2002-01-07

    申请人： Graham C Crawley ,  Laurent F A Hennequin ,  Darren McKerrecher ,  Patrick Ple ,  Jeffrey Philip Poyser ,  Christine M P Lambert

    发明人： Graham C Crawley ,  Laurent F A Hennequin ,  Darren McKerrecher ,  Patrick Ple ,  Jeffrey Philip Poyser ,  Christine M P Lambert

    IPC分类号： A61K31517

    CPC分类号： C07D231/12 ,  C07D215/54 ,  C07D233/56 ,  C07D239/94 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D487/04

    摘要： The invention concerns quinazoline derivatives of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3 includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2 and R3 is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal.

    摘要翻译： 本发明涉及式（I）的喹唑啉衍生物，其中Q 1包括任选被诸如卤代，三氟甲基和氰基的基团取代的喹唑啉环，或下式：Q 3 -X 1 - 的基团，其中 X 1包括直接键，O和Q 3包括芳基，芳基 - （1-6C）烷基，杂环基和杂环基 - （1-6C）烷基; R 2和R 3各自为氢或（1-6C）烷基; Z包括O，S和NH; 和Q 2包括芳基和芳基 - （1-3C）烷基或其药学上可接受的盐; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗温血动物中的T细胞介导的疾病或医学病症的药物中的用途。

    Quinazoline derivatives as angiogenesis inhibitors
    3.
    发明申请
    Quinazoline derivatives as angiogenesis inhibitors 审中-公开

    公开(公告)号：US20060004017A1

    公开(公告)日：2006-01-05

    申请号：US11169122

    申请日：2005-06-29

    申请人： Elaine Stokes ,  Darren McKerrecher ,  Laurent Hennequin ,  Patrick Ple

    发明人： Elaine Stokes ,  Darren McKerrecher ,  Laurent Hennequin ,  Patrick Ple

    IPC分类号： A61K31/517 ,  C07D43/02

    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, C1-3alkyl, C1-3alkoxy, C1-3alkylsulphanyl, —NR3R4 (wherein R3 and R4, which may be the same or different, each represents hydrogen or C1-3alkyl), or R5Xt— (wherein X1 and R5 are as defined herein; R1 represents hydrogen, oxo, halogeno, hydroxy, C1-4alkoxy, 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 R56X10 (wherein X10 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.

    Heteroaryl Benzamide Derivatives for Use as GLK Activators in the Treatment of Diabetes
    7.
    发明申请
    Heteroaryl Benzamide Derivatives for Use as GLK Activators in the Treatment of Diabetes 审中-公开
    用作糖尿病治疗中的GLK激活剂的杂芳基苯甲酰胺衍生物

    公开(公告)号：US20090253676A1

    公开(公告)日：2009-10-08

    申请号：US12336170

    申请日：2008-12-16

    申请人： Craig Johnstone ,  Darren McKerrecher ,  Kurt Gordon Pike ,  Michael James Waring

    发明人： Craig Johnstone ,  Darren McKerrecher ,  Kurt Gordon Pike ,  Michael James Waring

    IPC分类号： A61K31/4155 ,  C07D403/12 ,  A61K31/497 ,  C07D413/12 ,  A61K31/4245 ,  A61P3/10

    CPC分类号： C07D277/46 ,  C07D231/40 ,  C07D285/08 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

    摘要： Compounds of Formula (I): wherein: R1 is hydroxymethyl; 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.

    摘要翻译： 式（I）的化合物：其中：R1是羟甲基; R2选自-C（O）NR4R5，-SO2NR4R5，-S（O）pR4和HET-2; HET-1是5-或6-元，任选取代的C连接的杂芳基环; HET-2是4-，5-或6-元C-或N-连接的任选取代的杂环基环; R 3选自卤素，氟甲基，二氟甲基，三氟甲基，甲基，甲氧基和氰基; R4选自例如氢，任选取代的（1-4C）烷基和HET-2; R5是氢或（1-4C）烷基; 或R 4和R 5与它们所连接的氮原子一起可以形成由HET-3定义的杂环基环系统; HET-3是例如任选取代的N-连接的，4,5或6元饱和或部分不饱和的杂环基环; p是（每次出现时独立）0,1或2; m为0或1; n为0,1或2; 条件是当m为0时，n为1或2; 或其盐，前药或溶剂化物。 还描述了它们用作GLK活化剂，含有它们的药物组合物及其制备方法。

    Benzamide Derivatives and Their Use as Glucokinase Activating Agents
    9.
    发明申请
    Benzamide Derivatives and Their Use as Glucokinase Activating Agents 审中-公开
    苯甲酰胺衍生物及其作为葡萄糖激酶活化剂的用途

    公开(公告)号：US20080280872A1

    公开(公告)日：2008-11-13

    申请号：US10588334

    申请日：2005-02-15

    申请人： Craig Johnstone ,  Darren McKerrecher ,  Kurt Gordon Pike

    发明人： Craig Johnstone ,  Darren McKerrecher ,  Kurt Gordon Pike

    IPC分类号： A61K31/427 ,  C07D277/46 ,  A61K31/426 ,  C07D403/14 ,  C07D413/12 ,  A61P3/10 ,  A61K31/4245 ,  A61K31/496 ,  C07D417/12

    CPC分类号： C07D487/08 ,  C07D231/40 ,  C07D277/46 ,  C07D403/12 ,  C07D417/12

    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.

    摘要翻译： 式（I）的化合物：其中：R 1是甲氧基甲基; R 2选自-C（O）NR 4 R 5，-SO 2 NR 2， 4个，5个，-S（O）4个S 4和4个HET-2; HET-1是5-或6-元，任选取代的C连接的杂芳基环; HET-2是4-，5-或6-元C-或N-连接的任选取代的杂环基环; R 3选自卤素，氟甲基，二氟甲基，三氟甲基，甲基，甲氧基和氰基; R 4选自例如氢，任选取代的（1-4C）烷基和HET-2; R 5是氢或（1-4C）烷基; 或R 4和R 5与它们所连接的氮原子一起可以形成由HET-3定义的杂环基环系; HET-3是例如任选取代的N-连接的，4,5或6元饱和或部分不饱和的杂环基环; p是（每次出现时独立）0,1或2; m为0或1; n为0,1或2; 条件是当m为0时，n为1或2; 或其盐，前药或溶剂化物。 还描述了它们用作GLK活化剂，含有它们的药物组合物及其制备方法。