公开(公告)号：US20090018134A1

公开(公告)日：2009-01-15

申请号：US12170128

申请日：2008-07-09

申请人： Kurt Gordon PIKE ,  Jeffrey James Morris

发明人： Kurt Gordon PIKE ,  Jeffrey James Morris

IPC分类号： A61K31/5377 ,  C07D413/04 ,  A61P35/04 ,  C07D413/14

CPC分类号： C07D413/14 ,  C07D413/04 ,  C07D417/14

摘要： A compound of formula (I) or a pharamaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by an mTOR kinase and/or one or more PI3K enzyme.

摘要翻译： 式（I）化合物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治疗中的用途，例如用于治疗增殖性疾病如癌症，特别是在由mTOR激酶介导的疾病中的用途，以及 /或一种或多种PI3K酶。

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。

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。

公开(公告)号：US20080234273A1

公开(公告)日：2008-09-25

申请号：US11995079

申请日：2006-06-03

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

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

IPC分类号： C07D277/38 ,  A61K31/426 ,  A61K31/428 ,  C07D285/135 ,  A61K31/433 ,  A61K31/44 ,  C07D213/72 ,  C07D401/04 ,  A61K31/454 ,  A61K31/505 ,  C07D239/42 ,  A61K31/4965 ,  C07D241/20 ,  C07D403/14 ,  C07D403/02 ,  C07D237/20 ,  A61K31/50 ,  A61K31/415 ,  C07D231/38 ,  C07D413/04 ,  A61K31/5377 ,  A61K31/496 ,  C07D417/00 ,  A61P3/10

CPC分类号： C07D231/40 ,  C07D403/12

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R 1，R 2，R 3和HET-1的式（I）化合物如说明书中所述，它们的 盐是葡萄糖激酶（GLK）的激活剂，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：US20080171734A1

公开(公告)日：2008-07-17

申请号：US11876370

申请日：2007-10-22

申请人： Leonie Campbell ,  Kurt Gordon Pike ,  Abid Suleman ,  Michael James Waring

发明人： Leonie Campbell ,  Kurt Gordon Pike ,  Abid Suleman ,  Michael James Waring

IPC分类号： C07D401/00 ,  C07D403/02

CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D411/14 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14

摘要： The invention relates to a novel group of compounds of Formula (I) or a salt thereof: wherein R1, 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R 1，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。