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    Heteroaryl Benzamide Derivatives for Use as Glk Activators in the Treatment of Diabetes
    1.
    发明申请
    Heteroaryl Benzamide Derivatives for Use as Glk Activators in the Treatment of Diabetes 失效
    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：US20080015203A1

    公开(公告)日：2008-01-17

    申请号：US11628448

    申请日：2005-06-01

    申请人： Craig Johnstone ,  Darren Mckerrecher ,  Kurt Pike ,  Michael Waring

    发明人： Craig Johnstone ,  Darren Mckerrecher ,  Kurt Pike ,  Michael Waring

    IPC分类号： A61K31/4965 ,  A61K31/415 ,  A61P3/10 ,  C07D241/00 ,  C07D277/02 ,  C07D231/00 ,  A61K31/427

    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：R 1是羟甲基; R 2选自-C（O）NR 4 R 5，SO 2 NR 4， S（O）S 4 S 4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; 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。

    Benzoyl Amino Pyridyl Carboxylic Acid Derivatives Useful as Glucokinase (Glk) Activators
    2.
    发明申请
    Benzoyl Amino Pyridyl Carboxylic Acid Derivatives Useful as Glucokinase (Glk) Activators 审中-公开
    可用作葡萄糖激酶（Glk）激活剂的苯甲酰基氨基吡啶羧酸衍生物

    公开(公告)号：US20070255062A1

    公开(公告)日：2007-11-01

    申请号：US10579337

    申请日：2004-11-25

    申请人： Craig Johnstone ,  Darren Mckerrecher ,  Kurt Pike

    发明人： Craig Johnstone ,  Darren Mckerrecher ,  Kurt Pike

    IPC分类号： A61K31/44 ,  A61P3/10 ,  C07D211/72

    CPC分类号： C07D213/80

    摘要： Compounds of Formula: (I); wherein: R1 is selected from: fluoro, chloro, C1-3alkyl and C1-3alkoxy; R2—X— is selected from: methyl, methoxymethyl and Formula: (X); n is 0,1 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）化合物： 其中：R 1选自：氟，氯，C 1-3烷基和C 1-3烷氧基; R 2 -X-选自：甲基，甲氧基甲基和式：（X）; n为0,1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。

    Phenoxy Benzamide Compounds with Utility in the Treatment of Type 2 Diabetes and Obesity
    3.
    发明申请
    Phenoxy Benzamide Compounds with Utility in the Treatment of Type 2 Diabetes and Obesity 审中-公开
    苯氧基苯甲酰胺化合物在治疗2型糖尿病和肥胖中的应用

    公开(公告)号：US20080280874A1

    公开(公告)日：2008-11-13

    申请号：US11665163

    申请日：2005-10-11

    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： A61K31/397 ,  C07D231/10 ,  A61P3/10 ,  A61K31/415

    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.

    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。

    Heteroarylbenzamide derivatives for use in the treatment of diabetes
    4.
    发明授权
    Heteroarylbenzamide derivatives for use in the treatment of diabetes 失效
    用于治疗糖尿病的杂芳基苯甲酰胺衍生物

    公开(公告)号：US07964725B2

    公开(公告)日：2011-06-21

    申请号：US12644249

    申请日：2009-12-22

    申请人： Nathaniel George Martin ,  Darren Mckerrecher ,  Kurt Gordon Pike ,  Michael James Waring

    发明人： Nathaniel George Martin ,  Darren Mckerrecher ,  Kurt Gordon Pike ,  Michael James Waring

    IPC分类号： C07D241/08

    CPC分类号： C07D403/12 ,  C07D241/24 ,  C07D401/12

    摘要： The invention relates to a novel group of compounds of Formula (I) or a salt thereof: wherein R1, R2, R3, n, A and HET-1 are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK) such as type 2 diabetes. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by GLK using said compounds and methods for preparing compounds of Formula (I).

    摘要翻译： 本发明涉及一组新的式（I）化合物或其盐：其中R1，R2，R3，n，A和HET-1如说明书中所述，其可用于治疗或预防 通过葡萄糖激酶（GLK）如2型糖尿病介导的疾病或医学病症。 本发明还涉及包含所述化合物的药物组合物，使用所述化合物治疗由GLK介导的疾病的方法和制备式（I）化合物的方法。

    HETEROARYL BENZAMIDE DERIVATIVES
    6.
    发明申请
    HETEROARYL BENZAMIDE DERIVATIVES 失效
    苯并噻吩衍生物

    公开(公告)号：US20100173825A1

    公开(公告)日：2010-07-08

    申请号：US12644249

    申请日：2009-12-22

    申请人： Nathaniel George Martin ,  Darren Mckerrecher ,  Kurt Gordon Pike ,  Michael James Waring

    发明人： Nathaniel George Martin ,  Darren Mckerrecher ,  Kurt Gordon Pike ,  Michael James Waring

    IPC分类号： A61K31/497 ,  A61P3/10 ,  A61P3/04 ,  A61K38/28

    CPC分类号： C07D403/12 ,  C07D241/24 ,  C07D401/12

    摘要： The invention relates to a novel group of compounds of Formula (I) or a salt thereof: wherein R1, R2, R3, n, A and HET-1 are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK) such as type 2 diabetes. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by GLK using said compounds and methods for preparing compounds of Formula (I).

    摘要翻译： 本发明涉及一组新的式（I）化合物或其盐：其中R1，R2，R3，n，A和HET-1如说明书中所述，其可用于治疗或预防 通过葡萄糖激酶（GLK）如2型糖尿病介导的疾病或医学病症。 本发明还涉及包含所述化合物的药物组合物，使用所述化合物治疗由GLK介导的疾病的方法和制备式（I）化合物的方法。

    Quinazoline derivatives as angiogenesis inhibitors
    7.
    发明授权
    Quinazoline derivatives as angiogenesis inhibitors 有权

    公开(公告)号：US07074800B1

    公开(公告)日：2006-07-11

    申请号：US09913020

    申请日：2000-02-08

    申请人： Elaine S E Stokes ,  Darren Mckerrecher ,  Laurent F A Hennequin ,  Patrick Ple

    发明人： Elaine S E Stokes ,  Darren Mckerrecher ,  Laurent F A Hennequin ,  Patrick Ple

    IPC分类号： A61K31/517 ,  C07D239/88

    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 R5X1— (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(C1-4alkylcarbamoyl, 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.

    Chemical Compounds
    10.
    发明申请
    Chemical Compounds 失效
    化学化合物

    公开(公告)号：US20080318968A1

    公开(公告)日：2008-12-25

    申请号：US11924888

    申请日：2007-10-26

    申请人： Nathaniel George Martin ,  Darren Mckerrecher ,  Kurt Gordon Pike ,  Michael James Waring

    发明人： Nathaniel George Martin ,  Darren Mckerrecher ,  Kurt Gordon Pike ,  Michael James Waring

    IPC分类号： A61K31/497 ,  C07D403/12 ,  A61P3/10 ,  C07D401/12 ,  A61K31/4439

    CPC分类号： C07D403/12 ,  C07D241/24 ,  C07D401/12

    摘要： The invention relates to a novel group of compounds of Formula (I) or a salt thereof: wherein R1, R2, R3, n, A and HET-1 are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK) such as type 2 diabetes. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by GLK using said compounds and methods for preparing compounds of Formula (I).

    摘要翻译： 本发明涉及一组新的式（I）化合物或其盐：其中R1，R2，R3，n，A和HET-1如说明书中所述，其可用于治疗或预防 通过葡萄糖激酶（GLK）如2型糖尿病介导的疾病或医学病症。 本发明还涉及包含所述化合物的药物组合物，使用所述化合物治疗由GLK介导的疾病的方法和制备式（I）化合物的方法。