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1. 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。

2. 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。}

3. 发明申请

US20100137397A1 Chemical Compounds 审中-公开
标题翻译：化学化合物
公开(公告)号：US20100137397A1
公开(公告)日：2010-06-03
申请号：US11815418
申请日：2006-02-02
申请人： Alan Martin Birch , Craig Johnstone , Alleyn Thomas Plowright , Iain Simpson , Paul Robert Owen Whittamore
发明人： Alan Martin Birch , Craig Johnstone , Alleyn Thomas Plowright , Iain Simpson , Paul Robert Owen Whittamore
IPC分类号： A61K31/407 , C07D495/04 , A61P3/10 , A61P9/00 , A61P3/04
CPC分类号： C07D495/04
摘要： A compound of the formula (1) or a pharmaceutically-acceptable salt: possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity such as 2 diabetes. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.
摘要翻译：式（1）的化合物或药学上可接受的盐：具有糖原磷酸化酶抑制活性，因此在治疗与糖原磷酸化酶活性增加相关的疾病状态如2型糖尿病中具有价值。描述了制备含有它们的化合物和药物组合物的方法。

4. 发明申请

US20090124682A1 Indan-Amide Derivatives with 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茚满酰胺衍生物
公开(公告)号：US20090124682A1
公开(公告)日：2009-05-14
申请号：US11883770
申请日：2006-02-02
申请人： Alan Martin Birch , Craig Johnstone , Alleyn Thomas Plowright , Iain Simpson , Paul Robert Owen Whittamore
发明人： Alan Martin Birch , Craig Johnstone , Alleyn Thomas Plowright , Iain Simpson , Paul Robert Owen Whittamore
IPC分类号： A61K31/40 , C07D209/42 , A61P3/10 , A61P3/04 , A61P9/10
CPC分类号： C07D209/42
摘要： A compound of the formula (1) or a pharmaceutically-acceptable salt: (A chemical formula should be inserted here—please see paper copy enclosed herewith) (1) 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）化合物或其药学上可接受的盐：（化学式应插入此处，请参见随附的纸质复制品）（1）具有糖原磷酸化酶抑制活性，因此具有治疗疾病相关的价值具有增加的糖原磷酸化酶活性。描述了制备含有它们的化合物和药物组合物的方法。

5. 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.

6. 发明申请

US20060199966A1 Indol-2-amides as glycogen phosphorylase inhibitors 审中-公开
标题翻译：吲哚-2-酰胺作为糖原磷酸化酶抑制剂
公开(公告)号：US20060199966A1
公开(公告)日：2006-09-07
申请号：US10567798
申请日：2004-08-18
申请人： Stuart Norman Bennett , Iain Simpson , Paul Robert Owen Whittamore
发明人： Stuart Norman Bennett , Iain Simpson , Paul Robert Owen Whittamore
IPC分类号： C07D293/00
CPC分类号： C07D405/12 , C07D209/42
摘要： A compound of the formula (1) or a pharmaceutically-acceptable salt, or pro-drug thereof; (1) wherein, for example, R4 is halo or (1-4C)alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; m is 0, 1 or 2; R1 is halo, cyano or carboxy; R2 is for example methyl; R3 is for example selected from halo(1-4C)alkyl, dihalo(1-4C)alkyl, trifluoromethyl, hydroxy(1-4C)alkyl, dihydroxy(2-4C)alkyl, trihydroxy(3-4C)alkyl, cyano(1-4C)alkyl (optionally substituted on alkyl with hydroxy), (1-4C)alkoxy(1-4C)alkyl, (1-4C)alkoxy(1-4C)alkoxy(1-4C)alkyl, di[(1-4C)alkoxy](1-4C)alkyl, (hydroxy)[(1-4C)alkoxy](1-4C)alkyl; 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药; （1）其中例如R 4为卤素或（1-4C）烷基; A是亚苯基或亚杂芳基; n为0,1或2; m为0,1或2; R 1是卤素，氰基或羧基; R 2是例如甲基; R 3是例如选自卤代（1-4C）烷基，二卤代（1-4C）烷基，三氟甲基，羟基（1-4C）烷基，二羟基（2-4C）烷基，三羟基（（1-4C）烷基，（1-4C）烷氧基（1-4C）烷氧基（1-4C）烷氧基（1-4C）烷氧基（1-4C）（1-4C）烷氧基]（1-4C）烷基，（羟基）[（1-4C）烷氧基]（1-4C）烷基; 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。

7. 发明申请

US20060211760A1 Indolamide 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吲哚酰胺衍生物
公开(公告)号：US20060211760A1
公开(公告)日：2006-09-21
申请号：US10566068
申请日：2004-08-04
申请人： Alan Birch , Stuart Bennett , Linda Godfrey , Iain Simpson , Paul Whittamore
发明人： Alan Birch , Stuart Bennett , Linda Godfrey , Iain Simpson , Paul Whittamore
IPC分类号： C07D209/42 , A61K31/405
CPC分类号： C07D209/42
摘要： A compound of the formula (1) or a pharmaceutically-acceptable salt wherein, for example, A is phenylene or heteroarylene; 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); compounds which 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，其中例如A是亚苯基或亚杂芳基; 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）; 具有糖原磷酸化酶抑制活性的化合物，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。

8. 发明授权

US09150574B2 Enzyme inhibitor compounds 有权
公开(公告)号：US09150574B2
公开(公告)日：2015-10-06
申请号：US14344417
申请日：2011-09-14
申请人： David Evans , Allison Carley , Alison Stewart , Michael Higginbottom , Edward Savory , Iain Simpson , Marianne Nilsson , Martin Haraldsson , Erik Nordling , Tobias Koolmeister
发明人： David Evans , Allison Carley , Alison Stewart , Michael Higginbottom , Edward Savory , Iain Simpson , Marianne Nilsson , Martin Haraldsson , Erik Nordling , Tobias Koolmeister
IPC分类号： C07D471/02 , A61K31/55 , C07D471/04
CPC分类号： C07D471/04
摘要： 2-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}ethan-1-amine; 3-aminopropyl 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxylate; 1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}-4-(dimethylamino)butan-1-one; 5-amino-1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}pentan-1-one; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; N-(3-aminopropyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-N-[3-(dimethylamino)propyl]piperidine-1-carboxamide; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)piperazine; 4-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)morpholine; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)-1,4-diazepane; ethyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; ethyl 1-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylic acid; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxamide; 4-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4yl}carbonyl)morpholine; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4-yl}carbonyl)piperazine; {4-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl}methanol; {4-[1-(4-methyl-phenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-2-yl}methanol; [(3R)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl]methanol; methyl 4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3-carboxylate; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3-carboxamide; 2-{4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl}ethan-1-ol; methyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-2-carboxylate; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-2-carboxamide; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-2-yl}carbonyl)piperazine; 4-[1-(4-methylphenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]morpholine; 1-(4-chlorophenyl)-3-(piperidin-4-yl)-1H-pyrrolo[2,3-c]pyridin-4-ol; N-butyl-1-(4-chlorophenyl)-N-methyl-1H-pyrazolo[3,4-c]pyridin-3-amine; 1-[4-(fluoromethyl)phenyl]-3-(oxan-4-yl)-1H-pyrazolo[3,4-c]pyridine; and 3-({4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-1-yl}methyl)pyridine are useful for the inhibition of SSAO activity.

9. 发明申请

US20110275637A1 PIPERAZINE DERIVATIVES AND THEIR USE AS LEPTIN RECEPTOR MODULATORS 审中-公开
标题翻译：哌嗪衍生物及其作为受体调节剂的使用
公开(公告)号：US20110275637A1
公开(公告)日：2011-11-10
申请号：US12996614
申请日：2009-06-04
申请人： Emma Chapman , Michael Higginbottom , Viet-Anh Anne Horgan (nee Nguyen) , James Horton , Iain Simpson , Charles Tyzack
发明人： Emma Chapman , Michael Higginbottom , Viet-Anh Anne Horgan (nee Nguyen) , James Horton , Iain Simpson , Charles Tyzack
IPC分类号： A61K31/5377 , C07D401/12 , A61K31/4439 , A61K31/496 , A61K31/4545 , A61P3/04 , A61P3/10 , A61P5/50 , A61P3/00 , A61P3/06 , A61P1/16 , A61P5/02 , A61P9/12 , A61P7/00 , A61P15/08 , A61P17/00 , A61P15/00 , A61P37/04 , A61P29/00 , A61P9/10 , C07D413/12
CPC分类号： C07D213/30 , C07D213/40 , C07D401/12 , C07D413/12
摘要： The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.
摘要翻译：本发明涉及新的式（I）化合物，包含这些化合物的药物组合物以及这些化合物作为瘦素受体调节剂模拟物在制备与增重，2型糖尿病和血脂异常相关的病症的药物中的用途。

10. 发明申请

US20110195992A1 NEW COMPOUNDS II 失效
标题翻译：新化合物II
公开(公告)号：US20110195992A1
公开(公告)日：2011-08-11
申请号：US13062366
申请日：2009-09-16
申请人： Edward Savory , Iain Simpson
发明人： Edward Savory , Iain Simpson
IPC分类号： A61K31/437 , C07D471/04 , A61P19/02 , A61P29/00 , A61P1/04 , A61P25/00 , A61P25/28 , A61P11/00 , A61P17/06 , A61P17/00 , A61P3/10 , A61P9/00 , A61P9/10 , A61P1/16
CPC分类号： C07D471/04
摘要： The present invention relates to compounds of formula (I), and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment of medical conditions wherein inhibition of SSAO activity is beneficial, such as such as inflammatory diseases and immune disorders.
摘要翻译：本发明涉及作为SSAO活性抑制剂的式（I）化合物及其药学上可接受的盐，溶剂合物，水合物，几何异构体，互变异构体，旋光异构体或N-氧化物。本发明还涉及包含这些化合物的药物组合物和这些化合物用于治疗其中SSAO活性的抑制是有益的医学病症的用途，例如炎性疾病和免疫疾病。

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