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1. 发明申请

WO2003015774A1 COMPOUNDS EFFECTING GLUCOKINASE 审中-公开
标题翻译：化合物对GLUCOKINASE有效
公开(公告)号：WO2003015774A1
公开(公告)日：2003-02-27
申请号：PCT/GB2002/003745
申请日：2002-08-15
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BOYD, Scott , CAULKETT, Peter, William, Rodney , HARGREAVES, Rodney, Brian , BOWKER, Suzanne, Saxon , JAMES, Roger , JOHNSTONE, Craig , JONES, Clifford, David , MCKERRECHER, Darren , BLOCK, Michael, Howard
发明人： BOYD, Scott , CAULKETT, Peter, William, Rodney , HARGREAVES, Rodney, Brian , BOWKER, Suzanne, Saxon , JAMES, Roger , JOHNSTONE, Craig , JONES, Clifford, David , MCKERRECHER, Darren , BLOCK, Michael, Howard
IPC分类号： A61K31/425
CPC分类号： C07D213/75 , A61K31/165 , A61K31/195 , A61K31/425 , A61K31/445 , C07D213/82 , C07D213/85 , C07D231/40 , C07D233/48 , C07D237/20 , C07D237/24 , C07D239/42 , C07D241/20 , C07D241/26 , C07D261/14 , C07D277/46 , C07D277/56 , C07D277/82 , C07D285/135 , C07D307/66 , C07D401/04 , C07D403/04 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R 1 , R 2 , R 3 , n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).
摘要翻译：本发明涉及式（I）化合物或其盐，溶剂合物或前体药物的用途，其中R 1，R 2，R 3，n和m如说明书中所述，在制备用于治疗或预防通过葡萄糖激酶（GLK）介导的疾病状况的药物，例如2型糖尿病。本发明还涉及一组新的式（I）化合物和制备式（I）化合物的方法。

2. 发明申请

WO2003000267A1 AMINO NICOTINATE DERIVATIVES AS GLUCOKINASE (GLK) MODULATORS 审中-公开
标题翻译： AMINO NICOTINATE衍生物作为GLUCOKINASE（GLK）调节剂
公开(公告)号：WO2003000267A1
公开(公告)日：2003-01-03
申请号：PCT/GB2002/002873
申请日：2002-06-24
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , HAYTER, Barry, Raymond , CURRIE, Gordon, Stuart , HARGREAVES, Rodney, Brian , JAMES, Roger , JONES, Clifford, David , MCKERRECHER, Darren , ALLEN, Joanne, Victoria , CAULKETT, Peter, William, Rodney , JOHNSTONE, Craig , GASKIN, Harold
发明人： HAYTER, Barry, Raymond , CURRIE, Gordon, Stuart , HARGREAVES, Rodney, Brian , JAMES, Roger , JONES, Clifford, David , MCKERRECHER, Darren , ALLEN, Joanne, Victoria , CAULKETT, Peter, William, Rodney , JOHNSTONE, Craig , GASKIN, Harold
IPC分类号： A61K31/496
CPC分类号： C07D213/80 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/496 , A61K31/506 , A61K31/5377 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention related to novel compounds of Formula (I) or a salt, solvate or prodrug thereof, wherein R?1?, R 2 , R 3 , n and m are as described in the specification, useful in the treatment of a (A chemical formula should be inserted here - please see paper copy enclosed) Formula (I) disease or condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to methods for preparing compounds of Formula (I) and their use as medicaments in the treatment of diseases mediated by glucokinase.
摘要翻译：本发明涉及新型式（I）化合物或其盐，溶剂合物或前药，其中R 1，R 2，R 3，n和m如说明书中所述，可用于治疗（一种化学式应该插在这里 - 请参见附有文件的副本）公式（I）通过葡萄糖激酶（GLK）介导的疾病或病症，如2型糖尿病。本发明还涉及制备式（I）化合物及其作为药物用于治疗由葡萄糖激酶介导的疾病的用途的方法。

3. 发明申请

WO2005056530A1 BENZOYL AMINO PYRIDYL CARBOXYLIC ACID DERIVATIVES USEFUL AS GLUCOKINASE (GLK) ACTIVATORS 审中-公开
标题翻译：苯甲酰氨基吡啶羧酸衍生物作为GLUCOKINASE（GLK）激活剂有用
公开(公告)号：WO2005056530A1
公开(公告)日：2005-06-23
申请号：PCT/GB2004/005068
申请日：2004-12-02
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , CAULKETT, Peter, William, Rodney , JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
发明人： CAULKETT, Peter, William, Rodney , JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
IPC分类号： C07D213/80
CPC分类号： C07D213/80
摘要： A compound of Formula (I): Formula (I) wherein: R 1 is selected from hydrogen and C 1-4 alkyl; R 2 is selected from: R 4 -C(R 5a R 5b )- , R 4 =C(R 6 )- and R 7a C(R 7b )=C(R 6 )-; R 3 X- is selected from methyl, methoxymethyl and ; R 4 is selected from (optionally substituted) C 1-4 alkyl, phenyl, C 3-6 cycloalkyl and heteroaryl; R 5a and R 5b are independently selected from hydrogen, fluoro and C 1-4 alkyl; R 6 is selected from hydrogen and C 1-4 alkyl; R 7a and R 7b are optionally substituted C 1-4 alkyl; 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：式（I）其中：R 1选自氢和C 1-4烷基; R 2选自：R 4 -C（R 5a R 5b） - ，R 4 = C（R 6） - 和R 7a（R 7b））= C（R <6>） - ; R 3选自甲基，甲氧基甲基和 R 4选自（任选取代的）C 1-4烷基，苯基，C 3-6环烷基和杂芳基; R 5a和R 5b独立地选自氢，氟和C 1-4烷基; R 6选自氢和C 1-4烷基; R 7a和R 7b是任选取代的C 1-4烷基; 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。

4. 发明申请

WO2005044801A1 PYRIDINE CARBOXYLIC ACID DERIVATIVES AS GLUCOKINASE MODULATORS 审中-公开
标题翻译：吡咯烷酮羧酸衍生物作为GLUCOKINASE调节剂
公开(公告)号：WO2005044801A1
公开(公告)日：2005-05-19
申请号：PCT/GB2004/004579
申请日：2004-10-28
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , CAULKETT, Peter, William, Rodney , JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
发明人： CAULKETT, Peter, William, Rodney , JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
IPC分类号： C07D213/80
CPC分类号： C07D213/80 , C07D405/12 , C07D409/12
摘要： A compound of Formula (I): wherein: A is phenyl or a 5- or 6-membered heteroaryl ring, optionally substituted; R 1 and R 2 are selected from hydrogen and methyl; with the proviso that at least one of R 1 and R 2 is methyl; 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：A是苯基或任选取代的5-或6-元杂芳基环; R 1和R 2选自氢和甲基; 条件是R 1和R 2中的至少一个是甲基; 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。

5. 发明申请

WO2005080360A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2005080360A1
公开(公告)日：2005-09-01
申请号：PCT/GB2005/000562
申请日：2005-02-15
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
发明人： JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
IPC分类号： C07D277/46
CPC分类号： C07D213/75 , C07D231/40 , C07D241/20 , C07D263/48 , C07D277/46 , C07D285/135 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/04 , C07D417/12
摘要： Compounds of Formula (I) wherein: R1 is methyl; 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。

6. 发明申请

WO2005054200A1 BENZOYL AMINO PYRIDYL CARBOXYLIC ACID DERIVATIVES USEFUL AS GLUCOKINASE (GLK) ACTIVATORS 审中-公开
标题翻译：苯甲酰氨基吡啶羧酸衍生物作为GLUCOKINASE（GLK）激活剂有用
公开(公告)号：WO2005054200A1
公开(公告)日：2005-06-16
申请号：PCT/GB2004/004966
申请日：2004-11-25
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
发明人： JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
IPC分类号： C07D213/80
CPC分类号： C07D213/80
摘要： Compounds of Formula: (I); wherein: R¹ is selected from: fluoro, chloro, C 1-3 alkyl and C 1-3 alkoxy; 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。

7. 发明申请

WO2006040528A1 PHENOXY BENZAMIDE COMPOUNDS WITH UTILITY IN THE TREATMENT OF TYPE 2 DIABETES AND OBESITY 审中-公开
标题翻译：在治疗2型糖尿病和肥胖中具有实用性的苯氧基苯甲酸化合物
公开(公告)号：WO2006040528A1
公开(公告)日：2006-04-20
申请号：PCT/GB2005/003888
申请日：2005-10-11
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon , WARING, Michael, James
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: R 1 is methoxymethyl; R 2 is selected from -C(O)NR 4 R 5 , SO 2 NR 4 R 5 , S(O) p R 4 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; R 3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R 4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R 5 is hydrogen or (1-4C)alkyl; or R 4 and R 5 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）化合物：其中：R

8. 发明申请

WO2005054233A1 BENZOYL AMINO PYRIDIL CARBOXYLIC ACID DERIVATIVES AS GLUOKINASE ACTIVATORS 审中-公开
标题翻译：作为GLUOKINASE激活剂的苯甲酰氨基吡啶羧酸衍生物
公开(公告)号：WO2005054233A1
公开(公告)日：2005-06-16
申请号：PCT/GB2004/004956
申请日：2004-11-25
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
发明人： JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
IPC分类号： C07D405/12
CPC分类号： C07D405/12
摘要： Compounds of Formula (I) wherein: R 1 -X- is selected from: methyl, methoxymethyl and Formula (X); R 2 is selected from hydrogen, methyl, chloro and fluoro; 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 -X-选自：甲基，甲氧基甲基和式（X）; R 2选自氢，甲基，氯和氟; n为1或2; 或其盐，前药或溶剂化物。还描述了它们作为GLK活化剂的用途，含有它们的药物组合物及其制备方法。

9. 发明申请

WO2005121110A1 HETROARYL BENZAMIDE DERIVATIVES FOR USE AS GLK ACTIVATORS IN THE TREATMENT OF DIABETES 审中-公开
标题翻译：用于治疗糖尿病的GLK激活剂的HETROARYL BENZAMIDE DERIVATIVES
公开(公告)号：WO2005121110A1
公开(公告)日：2005-12-22
申请号：PCT/GB2005/002166
申请日：2005-06-01
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon , WARING, Michael, James
发明人： JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon , WARING, Michael, James
IPC分类号： C07D277/46
CPC分类号： C07D277/46 , C07D231/40 , C07D285/08 , C07D403/12 , C07D413/12 , C07D417/12
摘要： Compounds of Formula (I) wherein: R 1 is hydroxymethyl; R 2 is selected from -C(O)NR 4 R 5 , SO 2 NR 4 R 5 , S(O) p R 4 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; R 3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R 4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R 5 is hydrogen or (1-4C)alkyl; or R 4 and R 5 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 R 5，S（O）p R 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。

10. 发明申请

WO2006040529A1 BENZAMIDE DERIVATIVES THAT ACT UPON THE GLUCOKINASE ENZYME 审中-公开
标题翻译：硼酸衍生物，其作用在葡萄糖激酶上
公开(公告)号：WO2006040529A1
公开(公告)日：2006-04-20
申请号：PCT/GB2005/003890
申请日：2005-10-11
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon , WARING, Michael, James
发明人： JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon , WARING, Michael, James
IPC分类号： C07D231/40
CPC分类号： C07D231/40
摘要： Compounds of Formula: (I); wherein: R 1 is hydroxymethyl; R 2 is selected from -C(O)NR 4 R 5 , SO 2 NR 4 R 5 , S(O)pR 4 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; R 3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R 4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R 5 is hydrogen or (1-4C)alkyl; or R 4 and R 5 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）化合物：其中：R

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