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1. 发明申请

US20070123528A1 INDOLE-AMID DERIVATIVES WHICH POSSESS GLYCOGEN PHOSPHORYLASE INHIBITORY ACTIVITY 失效
标题翻译：含有胶原酶抑制活性的吲哚美辛衍生物
公开(公告)号：US20070123528A1
公开(公告)日：2007-05-31
申请号：US11565605
申请日：2006-11-30
申请人： Andrew Stocker , Paul Whittamore
发明人： Andrew Stocker , Paul Whittamore
IPC分类号： A61K31/5377 , A61K31/497 , A61K31/496 , A61K31/454 , A61K31/4439 , A61K31/433 , A61K31/4178 , A61K31/405 , C07D413/02 , C07D403/02
CPC分类号： C07D413/12 , C07D209/42
摘要： Heterocyclic amides of formula (1) and pharmaceutically acceptable salts or pro-drugs thereof wherein variable groups are as described herein; which possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity are described. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are also described.
摘要翻译：式（1）的杂环酰胺及其药学上可接受的盐或前药，其中可变基团如本文所述; 其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。还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。

2. 发明申请

US20050131015A1 Heterocyclic amide derivatives as inhibitors of glycogen phoshorylase 失效
标题翻译：杂环酰胺衍生物作为糖原磷酸化酶的抑制剂
公开(公告)号：US20050131015A1
公开(公告)日：2005-06-16
申请号：US10506741
申请日：2003-03-04
申请人： Alan Birch , Andrew Morley , Andrew Stocker , Paul Whittamore
发明人： Alan Birch , Andrew Morley , Andrew Stocker , Paul Whittamore
IPC分类号： A61K31/4375 , A61K31/4709 , A61K31/519 , A61P3/00 , A61P3/04 , A61P3/10 , A61P9/10 , A61P43/00 , C07D495/04 , C07D519/00 , C07D498/02
CPC分类号： C07D495/04
摘要： Heterocyclic amides of formula (1) wherein: X is N or CH; R4 and R5 together are either —S—C(R6)═C(R7)— or —C(R7)═C(R6)—S—; R6 and R7 are independently selected from, for example hydrogen, halo and Cl-4alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); 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.
摘要翻译：式（1）的杂环酰胺其中：X是N或CH; 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，例如氢，卤素和C 1-4烷基; A是亚苯基或亚杂芳基; n为0,1或2; R 1选自例如卤素，硝基，氰基，羟基，羧基; R 2是氢，羟基或羧基; R 3选自例如氢，羟基，芳基，杂环基和C 1-4烷基（任选被1或2个R 8取代）组）; R 8选自例如羟基，-COCOOR 9，-C（O）N（R 9）（R 10）），-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. 发明授权

US07166636B2 Indole-amid derivatives which possess glycogen phosphorylase inhibitory activity 失效
公开(公告)号：US07166636B2
公开(公告)日：2007-01-23
申请号：US10506729
申请日：2003-03-04
申请人： Andrew Stocker , Paul Whittamore
发明人： Andrew Stocker , Paul Whittamore
IPC分类号： C07D209/12 , C07D209/14 , A61K31/404
CPC分类号： C07D413/12 , C07D209/42
摘要： Heterocyclic amides of formula (1) wherein: m is 0, 1 or 2; n is 0, 1 or 2; B is phenyl or heterocyclyl; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 and R3 are independently selected from, for example, C5-7cycloalkyl, cyano(C1-4)alkyl, C1-4alkyl (optionally substituted with 1 or 2 R8 groups), —OR8 and R8; R4 is independently selected from for example hydrogen, halo, nitro, cyano, hydroxy, C1-4alkyl, and C1-4alkanoyl; R8 is selected from for example hydroxy, heterocyclyl, aryl, —COCOOR9, —C(O)N(R9)(R10), (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 for example, hydroxy, C1-4alkoxy, heterocyclyl and C1-4alkanoyl; R14 is selected from for example, hydrogen, halo, C1-4alkyl, C5-7cycloalkyl, C1-4alkoxy, cyano, cyano(C1-4)alkyl, —COR3, (R2)(R3)NCO—, and (R2)(R3)NSO2—; 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.

4. 发明申请

US20070043069A1 HETEROCYCLIC AMIDE DERIVATIVES AS INHIBITORS OF GLYCOGEN PHOSPHORYLASE 失效
标题翻译：作为GLYCOGEN PHOSPHORYLASE的抑制剂的杂环酰胺衍生物
公开(公告)号：US20070043069A1
公开(公告)日：2007-02-22
申请号：US11463144
申请日：2006-08-08
申请人： Alan Birch , Andrew Morley , Andrew Stocker , Paul Whittamore
发明人： Alan Birch , Andrew Morley , Andrew Stocker , Paul Whittamore
IPC分类号： C07D471/02 , A61K31/4745
CPC分类号： C07D495/04
摘要： Heterocyclic amides of formula (1) wherein: X is N or CH; R4 and R5 together are either —S—C(R6)═C(R7)— or —C(R7)═C(R6)—S—; R6 and R7 are independently selected from, for example hydrogen, halo and C1-4alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); 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.
摘要翻译：式（1）的杂环酰胺其中：X是N或CH; 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，例如氢，卤素和C 1-4烷基; A是亚苯基或亚杂芳基; n为0,1或2; R 1选自例如卤素，硝基，氰基，羟基，羧基; R 2是氢，羟基或羧基; R 3选自例如氢，羟基，芳基，杂环基和C 1-4烷基（任选被1或2个R 8取代）组）; R 8选自例如羟基，-COCOOR 9，-C（O）N（R 9）（R 10）），-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药具有糖原磷酸化酶抑制活性，因此在治疗与增加的糖原磷酸化酶活性相关的疾病状态方面具有价值。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。}

5. 发明申请

US20060264494A1 Heterocyclic amide derivatives which process glycogen phorylase inhibitory activity 审中-公开
标题翻译：处理糖原酶活性的杂环酰胺衍生物
公开(公告)号：US20060264494A1
公开(公告)日：2006-11-23
申请号：US10567801
申请日：2004-08-18
申请人： Stuart Bennett , Iain Simpson , Paul Whittamore
发明人： Stuart Bennett , Iain Simpson , Paul Whittamore
IPC分类号： A61K31/407 , C07D498/02
CPC分类号： C07D495/04
摘要： A compound of the formula (1) or a pharmaceutically-acceptable salt, or pro-drug thereof; (1) wherein, for example: 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 and halo; A is phenylene or heteroarylene; n 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, tifluoromethyl, 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和R 5一起是-SC（R 6 -C（R 7） - 或-C（R 7）C（R 6）-S-; R 6和R SUP > 7个独立地选自氢和卤素; A是亚苯基或亚杂芳基; n是0,1或2; R 1是卤素，氰基或羧基; R 2，例如甲基; R 3是例如选自卤素（1-4C）烷基，二卤代（1-4C）烷基，二氟甲基，羟基（1-4C）烷基，二羟基（ 2-4C）烷基，三羟基（3-4C）烷基，氰基（1-4C）烷基（任选在羟基烷基上取代），（1-4C）烷氧基（1-4C）烷基，（1-4C）烷氧基 1-4C）烷基，二[（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描述了用于制备含有它们的化合物和药物组合物的方法。

6. 发明申请

US20050131052A1 Heterocyclic amide derivatives having glycogen phosphorylase inhibitory activity 失效
公开(公告)号：US20050131052A1
公开(公告)日：2005-06-16
申请号：US10506746
申请日：2003-03-04
申请人： Paul Whittamore , Stuart Bennett , Ian Simpson
发明人： Paul Whittamore , Stuart Bennett , Ian Simpson
IPC分类号： A61K31/407 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61P3/04 , A61P3/10 , A61P9/10 , C07D495/04 , C07D498/02
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.

7. 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.

8. 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。

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