公开(公告)号：US20100160286A1

公开(公告)日：2010-06-24

申请号：US12063252

申请日：2006-08-07

申请人： Darren McKerrecher ,  Gordon Kurt Pike ,  James Michael Warning

发明人： Darren McKerrecher ,  Gordon Kurt Pike ,  James Michael Warning

IPC分类号： A61K31/4155 ,  C07D403/10 ,  A61P3/10

CPC分类号： C07D403/12 ,  C07D405/14

摘要： Compounds of formula (I) wherein R1, R2, R3, and HET-1 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.

摘要翻译： 其中R1，R2，R3和HET-1如说明书中所述的式（I）化合物及其盐是葡糖激酶（GLK）的活化剂，因此可用于治疗例如2型糖尿病 。 还描述了制备式（I）化合物的方法。

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。

公开(公告)号：US20070287693A1

公开(公告)日：2007-12-13

申请号：US11665222

申请日：2005-10-11

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： A61K31/4155 ,  A61P3/10 ,  C07D231/40 ,  C07D403/12

CPC分类号： C07D231/40

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 hererocyclyl 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-连接的任选取代的二环基环; 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。

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。