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1. 发明授权

US08143263B2 Therapeutic agents 失效
标题翻译：治疗剂
公开(公告)号：US08143263B2
公开(公告)日：2012-03-27
申请号：US12535293
申请日：2009-08-04
申请人： Stuart Norman Lile Bennett , Roger John Butlin , Leonie Campbell , Robert Darren Morse Davies , Graeme Richard Robb , Rolf Peter Walker , Michael James Waring , Helen Claire Pointon , Mikael Dan Brink , Jonas Rickard Fägerhag , Ulrik Jurva , Volker Schnecke , Anette Marie Svensson Henriksson , Christer Ralf Westerlund , Peter Gustaf Bonn
发明人： Stuart Norman Lile Bennett , Roger John Butlin , Leonie Campbell , Robert Darren Morse Davies , Graeme Richard Robb , Rolf Peter Walker , Michael James Waring , Helen Claire Pointon , Mikael Dan Brink , Jonas Rickard Fägerhag , Ulrik Jurva , Volker Schnecke , Anette Marie Svensson Henriksson , Christer Ralf Westerlund , Peter Gustaf Bonn
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07D487/04
摘要： A compound of Formula (I): is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK or GK), leading to a decreased glucose threshold for insulin secretion.
摘要翻译：式（I）的化合物：可用于治疗或预防通过葡萄糖激酶（GLK或GK）介导的疾病或医学病症，导致胰岛素分泌的葡萄糖阈值降低。

2. 发明申请

US20100261733A1 THERAPEUTIC AGENTS 927 有权
标题翻译：治疗药物927
公开(公告)号：US20100261733A1
公开(公告)日：2010-10-14
申请号：US12756436
申请日：2010-04-08
申请人： Stuart Norman Lile Bennett , Rolf Peter Walker , Michael James Waring
发明人： Stuart Norman Lile Bennett , Rolf Peter Walker , Michael James Waring
IPC分类号： A61K31/519 , C07D487/04 , A61P3/10 , A61P3/04
CPC分类号： C07D487/04
摘要： (2S)-2-[1-(2-Chloro-6-cyano-phenyl)pyrazolo[4,5-e]pyrimidin-4-yl]oxy-3-[(1R)-2-hydroxy-1-methyl-ethoxy]-N-(5-methylpyrazin-2-yl)propanamide or a pharmaceutically acceptable salt thereof is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK or GK), leading to a decreased glucose threshold for insulin secretion.
摘要翻译：（2S）-2- [1-（2-氯-6-氰基 - 苯基）吡唑并[4,5-e]嘧啶-4-基]氧-3 - [（1R）-2-羟基-1-甲基 - 乙氧基] -N-（5-甲基吡嗪-2-基）丙酰胺或其药学上可接受的盐可用于治疗或预防通过葡萄糖激酶（GLK或GK）介导的疾病或医学病症，导致葡萄糖阈值降低用于胰岛素分泌。

3. 发明授权

US08071608B2 Therapeutic agents 有权
标题翻译：治疗剂
公开(公告)号：US08071608B2
公开(公告)日：2011-12-06
申请号：US12756436
申请日：2010-04-08
申请人： Stuart Norman Lile Bennett , Rolf Peter Walker , Michael James Waring
发明人： Stuart Norman Lile Bennett , Rolf Peter Walker , Michael James Waring
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07D487/04
摘要： (2S)-2-[1-(2-Chloro-6-cyano-phenyl)pyrazolo[4,5-e]pyrimidin-4-yl]oxy-3-[(1R)-2-hydroxy-1-methyl-ethoxy]-N-(5-methylpyrazin-2-yl)propanamide or a pharmaceutically acceptable salt thereof is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK or GK), leading to a decreased glucose threshold for insulin secretion.
摘要翻译：（2S）-2- [1-（2-氯-6-氰基 - 苯基）吡唑并[4,5-e]嘧啶-4-基]氧-3 - [（1R）-2-羟基-1-甲基 - 乙氧基] -N-（5-甲基吡嗪-2-基）丙酰胺或其药学上可接受的盐可用于治疗或预防通过葡萄糖激酶（GLK或GK）介导的疾病或医学病症，导致葡萄糖阈值降低用于胰岛素分泌。

4. 发明申请

US20100173958A1 COMPOUNDS FOR THE INHIBITION OF DGAT1 ACTIVITY 审中-公开
标题翻译：用于抑制DGAT1活性的化合物
公开(公告)号：US20100173958A1
公开(公告)日：2010-07-08
申请号：US12303862
申请日：2007-06-08
申请人： Stuart Norman Lile Bennett , Roger John Butlin , Alleyn Thomas Plowright
发明人： Stuart Norman Lile Bennett , Roger John Butlin , Alleyn Thomas Plowright
IPC分类号： A61K31/4245 , C07D271/07 , A61P3/10
CPC分类号： C07D271/113
摘要： Compounds of formula (I), or salts thereof, which inhibit acetyl CoA(acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein, for example, R1 is optionally substituted phenyl or naphthyl; Ring A is selected from (3-6C)cycloalkyl, (5-12C)bicycloalkyl and phenyl; n is 0, 1 or 2; R2 is, for example, hydrogen, fluoro, chloro or hydroxy; Ring B is selected from (3-6C)cycloalkyl, (5-12C)bicycloalkyl and phenyl; L1 is a direct bond or a defined linker group and R3 is, for example, hydroxy, carboxy or (1-6C)alkoxycarbonyl; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
摘要翻译：提供抑制乙酰CoA（乙酰辅酶A）：二酰基甘油酰基转移酶（DGAT1）活性的式（I）化合物或其盐，其中，例如，R 1为任选取代的苯基或萘基; 环A选自（3-6C）环烷基，（5-12C）双环烷基和苯基; n为0,1或2; R2是例如氢，氟，氯或羟基; 环B选自（3-6C）环烷基，（5-12C）双环烷基和苯基; L1是直接键或定义的连接基团，R 3是例如羟基，羧基或（1-6C）烷氧基羰基; 以及其制备方法，含有它们的药物组合物及其作为药物的用途。

5. 发明申请

US20080064691A1 Heterocyclic Amide Derivatives Which Possess Glycogen Phosphorylase Inhibitory Activity 审中-公开
标题翻译：具有糖原磷酸化酶抑制活性的杂环酰胺衍生物
公开(公告)号：US20080064691A1
公开(公告)日：2008-03-13
申请号：US10566063
申请日：2004-08-04
申请人： Alan Martin Birch , Stuart Norman Lile Bennett , Andrew Duncan Campbell , Iain Simpson , Paul Robert Owen Whittamore , David Paul Whalley , Linda Godfrey
发明人： Alan Martin Birch , Stuart Norman Lile Bennett , Andrew Duncan Campbell , Iain Simpson , Paul Robert Owen Whittamore , David Paul Whalley , Linda Godfrey
IPC分类号： A61K31/407 , A61K31/4178 , A61K31/4196 , A61K31/5377 , A61K31/541 , A61P3/00 , C07D495/04
CPC分类号： C07D495/04
摘要： A compound of the formula (1) or a pharmaceutically-acceptable salt, or pro-drug thereof; wherein, for example, Z is CH or nitrogen, R4 and R5 together are either —S—C(R6)═C(R7)— or —C(R7)═C(R6)—S—; R6 and R7 are independently selected from hydrogen, halo, nitro, cyano, hydroxy, fluoromethyl, difluoromethyl, trifluoromethyl, trifluoromethoxy, carboxy and carbamoyl; A is phenylene or heteroarylene; n is 0, 1 or 2; r is 1 or 2; R1 is halo, cyano or carboxy; Y is selected from —C(O)R2, —C(O)OR2, —C(O)NR2R3, -(1-4C)alkyl [optionally substituted] -(2-4C)alkenyl, —SO2NR2R3, and —S(O)cR2 (wherein c is 0, 1 or 2); R2 and R3 are independently selected from hydrogen, —O(1-4C)alkyl, —S(1-4C)alkyl, —N(1-4C)alkyl, heterocyclyl, aryl, and (1-4C)alkyl [optionally substituted]; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.
摘要翻译：式（1）的化合物或其药学上可接受的盐或其前体药物; 其中，例如，Z是CH或氮，R 4和R 5一起是-SC（R 6）-C（R 7）） - 或-C（R 7）C（R 6）-S-; R 6和R 7独立地选自氢，卤素，硝基，氰基，羟基，氟甲基，二氟甲基，三氟甲基，三氟甲氧基，羧基和氨基甲酰基; A是亚苯基或亚杂芳基; n为0,1或2; r为1或2; R 1是卤素，氰基或羧基; 其中Y选自-C（O）R 2，-C（O）OR 2，-C（O）NR 2 R 2，（1-4C）烷基[任选取代的] - （2-4C）烯基，-SO 2 NR 2 R 3和-S（O）C R 2（其中c是0,1或2）; R 2和R 3独立地选自氢，-O（1-4C）烷基，-S（1-4C）烷基，-N（1-4C）烷基，杂环基，芳基和（1-4C）烷基[任选取代的]; 具有糖原磷酸化酶抑制活性，因此具有与增加的糖原磷酸化酶活性相关的疾病状态的治疗价值。描述了制备含有它们的化合物和药物组合物的方法。

6. 发明授权

US07138415B2 Indolamid derivatives which possess glycogenphosphorylase inhibitory activity 失效
标题翻译：具有糖原磷酸化酶抑制活性的吲哚衍生物衍生物
公开(公告)号：US07138415B2
公开(公告)日：2006-11-21
申请号：US10506554
申请日：2003-03-04
申请人： Paul Robert Owen Whittamore , Stuart Norman Lile Bennett , Iain Simpson
发明人： Paul Robert Owen Whittamore , Stuart Norman Lile Bennett , Iain Simpson
IPC分类号： A61K31/454 , A61K31/41 , A61K31/404 , C07D401/12 , C07D257/04 , C07D209/30
CPC分类号： C07D401/12 , C07D209/42 , C07D403/12 , C07D409/12 , C07D413/12
摘要： Heterocyclic amides of formula (1) wherein: is a single or double bond; A is phenylene or heteroarylene; m is 0, 1 or 2; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; r is 1 or 2; Y is —NR2R3 or —OR3; R2 and R3 are selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R4 is selected from for example hydrogen, halo, nitro, cyano, hydroxy, C1-4alkyl, and C1-4alkanoyl; R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R9), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.
摘要翻译：式（1）的杂环酰胺其中：是单键或双键; A是亚苯基或亚杂芳基; m为0,1或2; n为0,1或2; R 1选自例如卤素，硝基，氰基，羟基，羧基; r为1或2; Y是-NR 2 R 3或-OR 3; R 2和R 3选自例如氢，羟基，芳基，杂环基和C 1-4 - 烷基（任选地被1或 2个R 8个基团）; R 4选自例如氢，卤素，硝基，氰基，羟基，C 1-4烷基和C 1-4烷酰基 ; R 8选自例如羟基，-COCOOR 9，-C（O）N（R 9）（R 9）），-NHC（O）R 9，（R 9）（R 10）N - 和-COOR ^{9 ; R 9和R 10选自例如氢，羟基，C 1-4烷基（任选被1或2个R SUP取代 > 13 ）; R 13选自羟基，卤素，三卤代甲基和C 1-4烷氧基; 或其药学上可接受的盐或前体药物; 具有糖原磷酸化酶抑制活性，因此具有与增加的糖原磷酸化酶活性相关的疾病状态的治疗价值。描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。}

7. 发明申请

US20110092526A1 Adamantyl Iminocarbonyl-Substituted Pyrimidines As Inhibitors Of 11-Beta-HSD1 826 审中-公开
标题翻译：金刚烷基亚氨基羰基取代的嘧啶作为11-β-HSD1抑制剂826
公开(公告)号：US20110092526A1
公开(公告)日：2011-04-21
申请号：US12907056
申请日：2010-10-19
申请人： Stuart Norman Lile Bennett , Frederick Woolf Goldberg , Andrew Leach , Paul Robert Owen Whittamore , Pernilla Sörme
发明人： Stuart Norman Lile Bennett , Frederick Woolf Goldberg , Andrew Leach , Paul Robert Owen Whittamore , Pernilla Sörme
IPC分类号： A61K31/506 , C07D239/28 , C07D239/38 , C07D239/47 , A61K31/505 , A61P3/00
CPC分类号： C07D405/12 , C07D239/42 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12
摘要： A compound of formula (I): and pharmaceutically-acceptable salts thereof, wherein the variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are also described herein.
摘要翻译：式（I）的化合物及其药学上可接受的盐，其中所述可变基团定义在其内; 它们在抑制11β和HSD1中的用途，制备它们的方法和包含它们的药物组合物也在本文中描述。

8. 发明授权

US07122567B2 Heterocyclic amide derivatives having glycogen phosphorylase inhibitory activity 失效
公开(公告)号：US07122567B2
公开(公告)日：2006-10-17
申请号：US10506746
申请日：2003-03-04
申请人： Paul Whittamore , Stuart Norman Lile Bennett , Iain Simpson
发明人： Paul Whittamore , Stuart Norman Lile Bennett , Iain Simpson
IPC分类号： A61K31/40 , A61K31/415 , C07D235/02 , C07D409/00
CPC分类号： C07D495/04
摘要： Heterocyclic amides of formula (1) wherein: Z is CH or nitrogen; R4 and R5 together are either —S—C(R6)═C(R7)— or —C(R7)═C(R6)—S—; R6 and R7 are selected from for example hydrogen, halo, C1-4alkyl, and C1-4alkanoyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; r is 1 or 2; Y is —NR2R3 or —OR3; R2 and R3 are selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R4 is selected from for example hydrogen, halo, nitro, cyano, hydroxy, C1-4alkyl, and C1-4alkanoyl; R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.

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