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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

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。

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。

6. 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。

7. 发明申请

US20090264401A1 SUBSTITUTED PYRIMIDIN-5-CARBOXAMIDES 281 审中-公开
标题翻译：取代的吡咯烷-5-羧酰胺281
公开(公告)号：US20090264401A1
公开(公告)日：2009-10-22
申请号：US12427170
申请日：2009-04-21
申请人： Adrian Liam GILL , Andrew Leach , Martin Packer , James Stewart Scott , Pernilla Sorme , John Gibbin Swales , Paul Robert Owen Whittamore
发明人： Adrian Liam GILL , Andrew Leach , Martin Packer , James Stewart Scott , Pernilla Sorme , John Gibbin Swales , Paul Robert Owen Whittamore
IPC分类号： A61K31/5377 , C07D413/04 , A61K31/505 , C07D239/28 , C07D239/38 , A61P3/10 , C07D413/14 , A61K31/554 , C07D419/04
CPC分类号： C07D239/42 , C07D239/28 , C07D239/38 , C07D239/47 , C07D239/48 , C07D239/557 , C07D239/58 , C07D401/14 , C07D403/04 , C07D405/12 , C07D405/14 , C07D413/04 , C07D417/04
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.
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; 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。

8. 发明授权

US5919793A Heterocyclic derivatives 失效
公开(公告)号：US5919793A
公开(公告)日：1999-07-06
申请号：US537827
申请日：1995-10-26
申请人： George Robert Brown , Paul Robert Owen Whittamore , David Robert Brittain
发明人： George Robert Brown , Paul Robert Owen Whittamore , David Robert Brittain
IPC分类号： A61K31/435 , A61P3/06 , A61P9/10 , C07D453/02 , C07D435/02
CPC分类号： C07D453/02
摘要： Compounds of formula (I) wherein R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen; or R.sup.1 and R.sup.2 are joined together so that CR.sup.1 14 CR.sup.2 is a double bond; X is selected from --Ch.sub.2 CH.sub.2 --, --C.dbd.CH--, --C.tbd.C--, --CH.sub.2 O--, --OCH.sub.2, CH.sub.2 NH--, --NHCH.sub.2 --, --CH.sub.2 CO--, --COCH.sub.2 --, --CH.sub.2 S(O).sub.n -- and --S(O).sub.n CH.sub.2 -- (wherein n is 0, 1 or 2); Ar is phenyl which bears one or more substituents independently selected from the groups (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (1-6C)alkoxy, (1-6C)alkoxycarbonyl, (1-6C)alkoxycarbonyl(1-6C)alkyl, (1-6C)alkoxy(1-6C)alkyl, (1-6C)alkylamino, di-�(1-6C)alkyl!amino, carbamoyl, (1-6C) alkylcarbamoyl, di-�(1-6C)alkyl!carbamoyl, (1-6C)alkenyl and oxime derivatives thereof and O--(1-6C)alkyl ethers of said oximes (1-6C)alkylthio, (1-6C)alkylsulphinyl and (1-6C)alkylsulphonyl when substituted by one or more groups selected from (1-6C)alkoxycarbonyl, (1-6C)alkanoyl and oxime derivatives thereof and O-(1-6C)alkyl ethers of said oxime derivatives, (1-6C)alkanoylamimo, (1-6C)alkanoyloxy, (1-6C)alkanoyloxy(1-6)alkyl, carbamoyl, N-(1-6C)alkylcarbamoyl, N,N-di�(1-6C)alkyl!carbamoyl, amino, (1-6C)alkylamino, di-�(1-6C)alkyl!amino, (1-6C)alkoxy, (2-6C)alkenyloxy, (1-6C)alkylthio, (1-6C)alkylsulphinyl, (1-6C)alkylsulphonyl, halogeno(1-6C)alkyl (2-6C)alkenyl, (2-6C)alkynyl, phenyl, phenoxy, cyano, nitro, hydroxy and carboxy; and wherein Ar may bear further substituents; and their pharmaceutically acceptable salts inhibit squalene synthese and are hence useful in lowering cholesterol levels in blood plasma Processes for preparing compounds of formula (I) are also referred to as well as pharmaceutical compositions containing them and their use in medicine.

9. 发明授权

US08344016B2 Pyrazole derivatives as 11-beta-HSD1 inhibitors 有权
标题翻译：吡唑衍生物作为11-β-HSD1抑制剂
公开(公告)号：US08344016B2
公开(公告)日：2013-01-01
申请号：US12878416
申请日：2010-09-09
申请人： Martin John Packer , James Stewart Scott , Andrew Stocker , Paul Robert Owen Whittamore
发明人： Martin John Packer , James Stewart Scott , Andrew Stocker , Paul Robert Owen Whittamore
IPC分类号： A61K31/415 , C07D321/02
CPC分类号： C07D231/18 , C07D231/14 , C07D403/06 , C07D405/12
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.
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; 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。

10. 发明申请

US20110224273A1 Pyrazole Derivatives as 11-Beta-HSD1 Inhibitors 有权
标题翻译：吡唑衍生物作为11-β-HSD1抑制剂
公开(公告)号：US20110224273A1
公开(公告)日：2011-09-15
申请号：US12878416
申请日：2010-09-09
申请人： Martin John Packer , James Stewart Scott , Andrew Stocker , Paul Robert Owen Whittamore
发明人： Martin John Packer , James Stewart Scott , Andrew Stocker , Paul Robert Owen Whittamore
IPC分类号： A61K31/4155 , C07D231/14 , A61K31/415 , C07D231/18 , C07D403/06 , A61P3/00
CPC分类号： C07D231/18 , C07D231/14 , C07D403/06 , C07D405/12
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.
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; 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。

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