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1. 发明申请

US20090253676A1 Heteroaryl Benzamide Derivatives for Use as GLK Activators in the Treatment of Diabetes 审中-公开
标题翻译：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。

2. 发明申请

US20080280874A1 Phenoxy Benzamide Compounds with Utility in the Treatment of Type 2 Diabetes and Obesity 审中-公开
标题翻译：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。

3. 发明授权

US07745475B2 Heteroaryl benzamide derivatives as GLK activators 失效
标题翻译：杂芳基苯甲酰胺衍生物作为GLK活化剂
公开(公告)号：US07745475B2
公开(公告)日：2010-06-29
申请号：US11628448
申请日：2005-06-01
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： A01N43/56 , C07D233/00
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。

4. 发明申请

US20080280872A1 Benzamide Derivatives and Their Use as Glucokinase Activating Agents 审中-公开
标题翻译：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。

5. 发明申请

US20090062351A1 Benzoyl amino pyridyl carboxylic acid derivatives useful as glucokinase (glk) activators 审中-公开
标题翻译：可用作葡萄糖激酶（glk）激活剂的苯甲酰氨基吡啶羧酸衍生物
公开(公告)号：US20090062351A1
公开(公告)日：2009-03-05
申请号：US10579782
申请日：2004-12-02
申请人： Peter William Rodney Caulkett , Craig Johnstone , Darren McKerrecher , Kurt Gordon Pike
发明人： Peter William Rodney Caulkett , Craig Johnstone , Darren McKerrecher , Kurt Gordon Pike
IPC分类号： A61K31/44 , C07D213/72 , A61P3/00
CPC分类号： C07D213/80
摘要： A compound of Formula (I): Formula (I) wherein: R1 is selected from hydrogen and C1-4alkyl; R2 is selected from: R4—C(R5aR5b)—, R4═C(R6)— and R7aC(R7b)═C(R6)—; R3X— is selected from methyl, methoxymethyl and; R4 is selected from (optionally substituted) C1-4alkyl, phenyl, C3-6cycloalkyl and heteroaryl; R5a and R5b are independently selected from hydrogen, fluoro and C1-4alkyl; R6 is selected from hydrogen and C1-4alkyl; R7a and R7b are optionally substituted C1-4alkyl; 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; R2选自：R4-C（R5aR5b） - ，R4-C（R6） - 和R7aC（R7b）-C（R6） - ; R3X-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; R5a和R5b独立地选自氢，氟和C1-4烷基; R6选自氢和C 1-4烷基; R7a和R7b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。

6. 发明申请

US20080312207A1 Compounds 审中-公开
标题翻译：化合物
公开(公告)号：US20080312207A1
公开(公告)日：2008-12-18
申请号：US10588315
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： A61K31/397 , C07D417/12 , A61K31/496 , C07D277/20 , A61K31/426 , C07D413/12 , A61K31/454 , A61K31/422 , C07D405/12 , A61K31/4155 , C07D403/12
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：R 1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。

7. 发明申请

US20090018157A1 Chemical compounds 审中-公开
标题翻译：化合物
公开(公告)号：US20090018157A1
公开(公告)日：2009-01-15
申请号：US10579552
申请日：2004-11-25
申请人： Craig Johnstone , Darren McKerrecher , Kurt Gordon Pike
发明人： Craig Johnstone , Darren McKerrecher , Kurt Gordon Pike
IPC分类号： A61K31/443 , A61P3/04 , A61P3/10 , C07D405/12 , A61K31/4433
CPC分类号： C07D405/12
摘要： Compounds of Formula (I) wherein: R1—X— is selected from: methyl, methoxymethyl and Formula (X); R2 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）; R2选自氢，甲基，氯和氟; n为1或2; 或其盐，前药或溶剂化物。还描述了它们用作GLK活化剂，含有它们的药物组合物及其制备方法。

8. 发明申请

US20080207636A1 Compounds Effecting Glucokinase 失效
标题翻译：影响葡萄糖激酶的化合物
公开(公告)号：US20080207636A1
公开(公告)日：2008-08-28
申请号：US12024561
申请日：2008-02-01
申请人： Scott Boyd , Peter William Rodney Caulkett , Rodney Brian Hargreaves , Suzanne Saxon Bowker , Roger James , Clifford David Jones , Darren McKerrecher , Michael Howard Block , Craig Johnstone
发明人： Scott Boyd , Peter William Rodney Caulkett , Rodney Brian Hargreaves , Suzanne Saxon Bowker , Roger James , Clifford David Jones , Darren McKerrecher , Michael Howard Block , Craig Johnstone
IPC分类号： A61K31/496 , C07D277/20 , A61K31/426 , A61K31/433 , A61P3/10 , A61K31/4436 , A61K31/415 , C07D231/10 , C07D213/02 , A61P3/04 , C07D285/12 , C07D295/00
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 R1, R2, R3, 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）如2型糖尿病介导的疾病状况的药物中的描述。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。

9. 发明授权

US07951830B2 Compounds effecting glucokinase 失效
标题翻译：影响葡萄糖激酶的化合物
公开(公告)号：US07951830B2
公开(公告)日：2011-05-31
申请号：US12363899
申请日：2009-02-02
申请人： Scott Boyd , Peter William Rodney Caulkett , Rodney Brian Hargreaves , Suzanne Saxon Bowker , Roger James , Clifford David Jones , Darren McKerrecher , Michael Howard Block , Craig Johnstone
发明人： Scott Boyd , Peter William Rodney Caulkett , Rodney Brian Hargreaves , Suzanne Saxon Bowker , Roger James , Clifford David Jones , Darren McKerrecher , Michael Howard Block , Craig Johnstone
IPC分类号： A61K31/425 , A61K31/415 , A61K31/496 , A61K31/433
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 R1, R2, R3, 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，溶剂合物或前药，其中R1，R2，R3，n和m如说明书中所述，用于制备用于治疗或预防通过葡萄糖激酶（GLK）介导的疾病状况，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。

10. 发明授权

US07524957B2 Compounds effecting glucokinase 失效
标题翻译：影响葡萄糖激酶的化合物
公开(公告)号：US07524957B2
公开(公告)日：2009-04-28
申请号：US12024561
申请日：2008-02-01
申请人： Scott Boyd , Peter William Rodney Caulkett , Rodney Brian Hargreaves , Suzanne Saxon Bowker , Roger James , Clifford David Jones , Darren McKerrecher , Michael Howard Block , Craig Johnstone
发明人： Scott Boyd , Peter William Rodney Caulkett , Rodney Brian Hargreaves , Suzanne Saxon Bowker , Roger James , Clifford David Jones , Darren McKerrecher , Michael Howard Block , Craig Johnstone
IPC分类号： C07D213/02 , C07D231/10 , C07D277/20 , C07D285/12 , C07D295/00 , A61K31/496 , A61K31/426 , A61K31/415 , A61K31/433
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 R1, R2, R3, 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，溶剂合物或前药，其中R1，R2，R3，n和m如说明书中所述，用于制备用于治疗或预防通过葡萄糖激酶（GLK）介导的疾病状况，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。

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