公开(公告)号：US07951833B2

公开(公告)日：2011-05-31

申请号：US12364949

申请日：2009-02-03

申请人： Gary Peter Tomkinson ,  Martin John Packer ,  James Stewart Scott ,  Paul Robert Owen Whittamore ,  Andrew Stocker

发明人： Gary Peter Tomkinson ,  Martin John Packer ,  James Stewart Scott ,  Paul Robert Owen Whittamore ,  Andrew Stocker

IPC分类号： A61K31/415 ,  C07D231/12

CPC分类号： C07D231/14

摘要： New crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are also described.

摘要翻译： 4- [4-（2-金刚烷基氨基甲酰基）-5-叔丁基 - 吡唑-1-基]苯甲酸的新结晶形式; 还描述了它们在抑制11β和HSD1中的用途，其制备方法和包含它们的药物组合物。

公开(公告)号：US20100278835A1

公开(公告)日：2010-11-04

申请号：US12720094

申请日：2010-03-09

申请人： Helen Blade ,  Heather Marie Jackson ,  Gary Peter Tomkinson ,  Elisa Ann Carron ,  James Andrew Lumley ,  Christopher John Pilkington ,  Alexander James Floyd Thomas ,  Justin Warne

发明人： Helen Blade ,  Heather Marie Jackson ,  Gary Peter Tomkinson ,  Elisa Ann Carron ,  James Andrew Lumley ,  Christopher John Pilkington ,  Alexander James Floyd Thomas ,  Justin Warne

IPC分类号： A61K31/519 ,  C07D403/06 ,  A61K31/517 ,  C07D471/04 ,  A61P31/14 ,  A61P11/00 ,  A61K39/42

CPC分类号： C07D403/06 ,  C07D471/04

摘要： The invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined in the specification, and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are useful in the treatment of respiratory syncytial virus (RSV).

摘要翻译： 本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 11和R 12如本说明书中所定义，及其旋光异构体，外消旋体和互变异构体， 其药学上可接受的盐; 以及其制备方法，含有它们的药物组合物及其在治疗中的用途。 该化合物可用于治疗呼吸道合胞病毒（RSV）。

公开(公告)号：US20100094009A1

公开(公告)日：2010-04-15

申请号：US12520223

申请日：2007-12-20

申请人： James McCabe ,  Gary Peter Tomkinson

发明人： James McCabe ,  Gary Peter Tomkinson

IPC分类号： C07D401/14

CPC分类号： C07D403/14

摘要： A novel crystalline form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-[(1-methylethyl)oxy]-N-1H-pyrazol-3-ylbenzamide is described in the specification. This compound is a glucokinase (GLK or GK) activator and useful as a pharmaceutical agent in the treatment or prevention of a disease or medical condition mediated through GLK, leading to a decreased glucose threshold for insulin secretion. Processes for the manufacture of the crystalline form, pharmaceutical compositions comprising the crystalline form and the use of the crystalline form in medical treatment are also described.

摘要翻译： 3 - {[5-（氮杂环丁烷-1-基羰基）吡嗪-2-基]氧基} -5 - [（1-甲基乙基）氧基] -N-1H-吡唑-3-基苯甲酰胺的新型结晶形式描述于 规格。 该化合物是葡萄糖激酶（GLK或GK）激活剂，可用作治疗或预防通过GLK介导的疾病或医学病症的药物，导致胰岛素分泌的葡萄糖阈值降低。 还描述了用于制造结晶形式的方法，包含结晶形式的药物组合物和在治疗中使用结晶形式的方法。

公开(公告)号：US07696191B2

公开(公告)日：2010-04-13

申请号：US11962838

申请日：2007-12-21

申请人： James McCabe ,  Gary Peter Tomkinson

发明人： James McCabe ,  Gary Peter Tomkinson

IPC分类号： A01N43/00 ,  A61K31/397 ,  A61K31/00 ,  A01N43/58 ,  A61K31/50 ,  A01N43/60 ,  A61K31/495 ,  A61K31/497 ,  A01N43/56

CPC分类号： C07D403/14

摘要： A novel crystalline form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-[(1-methylethyl)oxy]-N-1H-pyrazol-3-ylbenzamide is described in the specification. This compound is a glucokinase (GLK or GK) activator and useful as a pharmaceutical agent in the treatment or prevention of a disease or medical condition mediated through GLK, leading to a decreased glucose threshold for insulin secretion. Processes for the manufacture of the crystalline form, pharmaceutical compositions comprising the crystalline form and the use of the crystalline form in medical treatment are also described.

摘要翻译： 3 - {[5-（氮杂环丁烷-1-基羰基）吡嗪-2-基]氧基} -5 - [（1-甲基乙基）氧基] -N-1H-吡唑-3-基苯甲酰胺的新型结晶形式描述于 规格。 该化合物是葡萄糖激酶（GLK或GK）激活剂，可用作治疗或预防通过GLK介导的疾病或医学病症的药物，导致胰岛素分泌的葡萄糖阈值降低。 还描述了用于制造结晶形式的方法，包含结晶形式的药物组合物和在治疗中使用结晶形式的方法。

公开(公告)号：US20090221660A1

公开(公告)日：2009-09-03

申请号：US12364949

申请日：2009-02-03

申请人： Gary Peter Tomkinson

发明人： Gary Peter Tomkinson

IPC分类号： A61K31/415 ,  C07D231/14 ,  A61P3/10

CPC分类号： C07D231/14

摘要： New crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are also described.

摘要翻译： 4- [4-（2-金刚烷基氨基甲酰基）-5-叔丁基 - 吡唑-1-基]苯甲酸的新结晶形式; 还描述了其用于抑制11betaHSD1的用途，其制备方法和包含它们的药物组合物。

公开(公告)号：US20100184813A1

公开(公告)日：2010-07-22

申请号：US12642195

申请日：2009-12-18

申请人： Alan Martin BIRCH ,  Gary Peter Tomkinson ,  Sharmistha Pal ,  Anna Pettersen

发明人： Alan Martin BIRCH ,  Gary Peter Tomkinson ,  Sharmistha Pal ,  Anna Pettersen

IPC分类号： A61K31/4245 ,  C07D271/113 ,  A61P3/04 ,  A61P3/10

CPC分类号： B64D39/00 ,  C07D271/113

摘要： DGAT-1 inhibitor compounds of formula (I) and pharmaceutically-acceptable salts thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein n is 0, 1, 2 or 3, R is independently selected from fluoro, chloro, bromo, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy and Z is carboxy or a mimic or bioisostere thereof, hydroxyl, hydroxymethyl, or —CONRbRc wherein Rb and Rc are independently selected from hydrogen and (1-4C)alkyl, which (1-4C)alkyl group may be optionally substituted by carboxy or a mimic or bioisostere thereof.

摘要翻译： 已经描述了式（I）的DGAT-1抑制剂化合物及其药学上可接受的盐以及药物组合物，其制备方法及其用于治疗例如肥胖症，其中n为0,1,2或3，R 独立地选自氟，氯，溴，三氟甲基，甲氧基，二氟甲氧基和三氟甲氧基，Z是羧基或其模拟或生物电子等排物，羟基，羟甲基或-CONRbRc，其中Rb和Rc独立地选自氢和（1-4C） 烷基，其中（1-4C）烷基可以任选被羧基或其模拟物或生物电子等排物取代。

公开(公告)号：US20080153800A1

公开(公告)日：2008-06-26

申请号：US11962838

申请日：2007-12-21

申请人： James MCCABE ,  Gary Peter Tomkinson

发明人： James MCCABE ,  Gary Peter Tomkinson

IPC分类号： A61K31/497 ,  C07D403/14 ,  A61P3/10

CPC分类号： C07D403/14

摘要： A novel crystalline form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-[(1-methylethyl)oxy]-N-1H-pyrazol-3-ylbenzamide is described in the specification. This compound is a glucokinase (GLK or GK) activator and useful as a pharmaceutical agent in the treatment or prevention of a disease or medical condition mediated through GLK, leading to a decreased glucose threshold for insulin secretion. Processes for the manufacture of the crystalline form, pharmaceutical compositions comprising the crystalline form and the use of the crystalline form in medical treatment are also described.

摘要翻译： 3 - {[5-（氮杂环丁烷-1-基羰基）吡嗪-2-基]氧基} -5 - [（1-甲基乙基）氧基] -N-1H-吡唑-3-基苯甲酰胺的新型结晶形式描述于 规格。 该化合物是葡萄糖激酶（GLK或GK）激活剂，可用作治疗或预防通过GLK介导的疾病或医学病症的药物，导致胰岛素分泌的葡萄糖阈值降低。 还描述了用于制造结晶形式的方法，包含结晶形式的药物组合物和在治疗中使用结晶形式的方法。