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11. 发明授权

US06353002B2 Therapeutic agents 失效
标题翻译：治疗剂
公开(公告)号：US06353002B2
公开(公告)日：2002-03-05
申请号：US09748153
申请日：2000-12-27
申请人： Alan Martin Birch , Paul Anthony Bradley
发明人： Alan Martin Birch , Paul Anthony Bradley
IPC分类号： A61K31445
CPC分类号： C07D491/04 , C07D493/04 , C07D495/04
摘要： Compounds of formula I and pharmaceutically acceptable salts thereof in which A is methylene or —O—; B is methylene or —O—; G1—G2—G3 form a heteroaromatic or heteroaliphatic chain; g is 0, 1 or 2; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T is an optionally substituted aryl or heteroaryl group, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, and spasticity.
摘要翻译：式I化合物及其药学上可接受的盐，其中A是亚甲基或-O-; B是亚甲基或-O-; G1-G2-G3形成杂芳族或杂脂族链; g为0,1或2; U是任选被一个或多个烷基取代的亚烷基链; Q表示含有氮原子的二价基团; T是任选取代的芳基或杂芳基，可用于治疗中枢神经系统疾病，例如抑郁症，焦虑症，精神病（例如精神分裂症），迟发性运动障碍，帕金森病，肥胖症，高血压，图雷特综合征，性功能障碍，吸毒成瘾，药物滥用，认知障碍，阿尔茨海默病，老年痴呆，强迫症，惊恐发作，社交恐怖症，进食障碍和厌食症，心血管和脑血管疾病，非胰岛素依赖性糖尿病，高血糖症，便秘，心律失常，神经内分泌系统疾病，压力和痉挛状态。

12. 发明授权

US6136825A Sulfonamide compounds having 5-HT receptor activity 有权
标题翻译：具有5-HT受体活性的磺酰胺化合物
公开(公告)号：US6136825A
公开(公告)日：2000-10-24
申请号：US331066
申请日：1999-06-16
申请人： Neil Wishart , Alan Martin Birch
发明人： Neil Wishart , Alan Martin Birch
IPC分类号： A61K31/453 , A61P3/04 , A61P3/10 , A61P9/00 , A61P25/16 , A61P25/24 , A61P25/28 , A61P25/30 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D493/04 , A01N43/40
CPC分类号： C07D405/06 , C07D405/12 , C07D405/14 , C07D413/14 , C07D493/04
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof in which A is methylene or --O--; B is methylene or --O--; g is 0, 1, 2, 3 or 4; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents an aryl or heteroaryl group, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress and spasticity ##STR1##
摘要翻译： PCT No.PCT / EP97 / 07034 Sec。 371日期1999年6月16日第 102（e）日期1999年6月16日PCT 1997年12月15日PCT公布。公开号WO98 / 29411 日期：1998年7月9日，式（I）化合物及其药学上可接受的盐，其中A为亚甲基或-O-; B是亚甲基或-O-; g为0,1,2,3或4; U是任选被一个或多个烷基取代的亚烷基链; Q表示含有氮原子的二价基团; T代表芳基或杂芳基，可用于治疗中枢神经系统疾病，例如抑郁症，焦虑症，精神病（例如精神分裂症），迟发性运动障碍，帕金森病，肥胖症，高血压，图雷特综合征，功能障碍，药物成瘾，药物滥用，认知障碍，阿尔茨海默病，老年痴呆，强迫症，恐慌发作，社交恐怖症，进食障碍和厌食症，心血管和脑血管障碍，非胰岛素依赖性糖尿病，高血糖症，便秘，心律失常，神经内分泌系统，压力和痉挛状态

13. 发明授权

US07994179B2 Carbamoyl compounds as DGAT1 inhibitors 190 有权
标题翻译：氨基甲酰化合物作为DGAT1抑制剂190
公开(公告)号：US07994179B2
公开(公告)日：2011-08-09
申请号：US12339349
申请日：2008-12-19
申请人： Petra Johannesson , Jan Magnus Johansson , Annika Ulrika Petersson , Alan Martin Birch , Roger John Butlin
发明人： Petra Johannesson , Jan Magnus Johansson , Annika Ulrika Petersson , Alan Martin Birch , Roger John Butlin
IPC分类号： A61K31/4965
CPC分类号： C07D213/81 , C07D213/82 , C07D241/24 , C07D401/04 , C07D401/10 , C07D403/10
摘要： DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, Ring A is optionally substituted 2,6-pyrazindiyl; X is ═O; Ring B is optionally substituted 1,4-phenylene; Y1 is a direct bond or —O—; Y2 is —(CH2)r— wherein r is 2 or 3; n is 0 or n is 1 when Y1 is a direct bond between Ring B and Ring C and when Ring B is 1,4-phenylene and Ring C is (4-6C)cycloalkane; Ring C is optionally substituted (4-6C)cycloalkane, (7-10C)bicycloalkane, (8-12C)tricycloalkane, phenylene or pryidindiyl; L is a direct bond or —O—; p is 0, 1 or 2 and when p is 1 or 2 RA1 and RA2 are each independently hydrogen or (1-4C)alkyl; Z is carboxy or a mimic or bioisostere thereof.
摘要翻译：与药物组合物一起描述式（I）的DGAT-1抑制剂化合物，其药学上可接受的盐和前药与制备它们的方法及其用于治疗例如肥胖症的用途，其中例如环A为任选取代的2,6-吡嗪二基; X是= O; 环B为任选取代的1,4-亚苯基; Y1是直接键或-O-键; Y2是 - （CH2）r-，其中r是2或3; 当Y 1是环B和环C之间的直接键，当环B是1,4-亚苯基且环C是（4-6C）环烷烃时，n是0或n是1; 环C是任选取代的（4-6C）环烷烃，（7-10C）双环烷烃，（8-12C）三环烷烃，亚苯基或辛基二辛基; L是直接键或-O-键; p为0,1或2，当p为1或2时，RA1和RA2各自独立地为氢或（1-4C）烷基; Z是羧基或其模拟物或生物电子等排体。

14. 发明申请

US20110092547A1 CHEMICAL COMPOUNDS 979 审中-公开
标题翻译：化学化合物979
公开(公告)号：US20110092547A1
公开(公告)日：2011-04-21
申请号：US12673767
申请日：2008-08-15
申请人： Alan Martin Birch , Roger John Butlin , Adrian Liam Gill , Samuel David Groombridge , Alleyn Thomas Plowright , Michael James Waring
发明人： Alan Martin Birch , Roger John Butlin , Adrian Liam Gill , Samuel David Groombridge , Alleyn Thomas Plowright , Michael James Waring
IPC分类号： A61K31/4439 , C07D413/12 , A61P3/10 , A61P3/04
CPC分类号： C07D413/12
摘要： Compounds of formula (I), or pharmaceutically-acceptable salts and/or pro-drugs thereof, which inhibit acetyl CoA(acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein n is 0 to 3; p is 0 or 1; q is 0 to 2; R1 and R2 are, for example, independently fluoro, chloro, bromo, cyano or (1-4C)alkyl; X is —O—, —S— or —NRa— wherein Ra is hydrogen or (1-4C)alkyl; RA1 and RA2 are, for example, independently hydrogen or (1-4C)alkyl; Ring A is a di-linked ring or ring system chosen from (4-6C)cycloalkane, (7-10C)bicycloalkane and (8-12C)tricycloalkane each optionally substituted, for example, by one substituent selected from (1-4C)alkyl, (1-4C)alkoxy and (1-4C)alkoxy(1-4C)alkyl; or Ring A is phenylene optionally substituted, for example, by up to four substituents selected from fluoro, chloro, bromo, cyano, (1-4C)alkyl, (1-4C)alkoxy and (1-4C)alkoxy(1-4C)alkyl; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
摘要翻译：提供了抑制乙酰辅酶A（乙酰辅酶A）：二酰基甘油酰基转移酶（DGAT1）活性的式（I）化合物或其药学上可接受的盐和/或其前体药物，其中n为0-3; p为0或1; q为0〜2; R 1和R 2例如独立地为氟，氯，溴，氰基或（1-4C）烷基; X是-O - ， - S-或-NRa-，其中R a是氢或（1-4C）烷基; RA1和RA2例如独立地为氢或（1-4C）烷基; 环A是选自（4-6C）环烷烃，（7-10C）双环烷烃和（8-12C）三环烷烃的二联环或环系，每个任选被例如一个选自（1-4C）的取代基取代，烷基，（1-4C）烷氧基和（1-4C）烷氧基（1-4C）烷基; 或环A为任选取代的亚苯基，例如至多四个选自氟，氯，溴，氰基，（1-4C）烷基，（1-4C）烷氧基和（1-4C）烷氧基（1-4C））烷基; 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。

15. 发明申请

US20110065706A1 Therapeutic Agents 812 审中-公开
标题翻译：治疗剂812
公开(公告)号：US20110065706A1
公开(公告)日：2011-03-17
申请号：US12879631
申请日：2010-09-10
申请人： Alan Martin Birch , Roger John Butlin , David Stephen Clarke , Andrew Leach , Philip Alexander MacFaul , Charles John O'Donnell , James Stewart Scott , Paul Robert Owen Whittamore , Dan Anders Broo , Öjvind Percy Davidsson , Kjell Erik Johansson , Hanna De La Motte
发明人： Alan Martin Birch , Roger John Butlin , David Stephen Clarke , Andrew Leach , Philip Alexander MacFaul , Charles John O'Donnell , James Stewart Scott , Paul Robert Owen Whittamore , Dan Anders Broo , Öjvind Percy Davidsson , Kjell Erik Johansson , Hanna De La Motte
IPC分类号： A61K31/5377 , C07D403/04 , A61K31/506 , C07D403/14 , C07D401/14 , C07D413/14 , C07D487/08 , C07D405/14 , A61P3/04 , A61P3/10
CPC分类号： C07D239/47 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D471/08 , C07D487/08
摘要： A compound of formula I or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as GPR119 modulators, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus, and pharmaceutical compositions containing them.
摘要翻译：式I化合物或其药学上可接受的盐，制备此类化合物的方法，其用作GPR119调节剂，其治疗用途的方法，特别是治疗肥胖症和糖尿病，以及含有它们的药物组合物。

16. 发明授权

US07749997B2 Pyrimido [4,5-B] -Oxazines for use as DGAT inhibitors 失效
标题翻译：用作DGAT抑制剂的嘧啶并[4,5-B] -O-
公开(公告)号：US07749997B2
公开(公告)日：2010-07-06
申请号：US12158252
申请日：2006-12-19
申请人： Alan Martin Birch , Paul David Kemmitt
发明人： Alan Martin Birch , Paul David Kemmitt
IPC分类号： C07D498/04 , A61K31/5365
CPC分类号： C07D498/04
摘要： Compounds of formula (I) or salts thereof, wherein A, and R1 to R5 are as defined in the specification, are DGAT-1 inhibitors and are thereby useful in the treatment of, for example, obesity. Processes to make compounds of formula (I) are also described.
摘要翻译：式（I）化合物或其盐，其中A和R 1至R 5如说明书中所定义，为DGAT-1抑制剂，因此可用于治疗例如肥胖症。还描述了制备式（I）化合物的方法。

17. 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。

18. 发明授权

US06201004B1 Dioxino derivatives and their use as therapeutic agents 失效
标题翻译：二恶英衍生物及其作为治疗剂的用途
公开(公告)号：US06201004B1
公开(公告)日：2001-03-13
申请号：US09380375
申请日：1999-09-01
申请人： Alan Martin Birch , Paul Anthony Bradley
发明人： Alan Martin Birch , Paul Anthony Bradley
IPC分类号： A61K3140
CPC分类号： C07D491/04 , C07D493/04 , C07D495/04
摘要： Compounds of formula I and pharmaceutically acceptable salts thereof in which A is methylene or —O—; B is methylene or —O—; G1—G2—G3 form a heteroaromatic or heteroaliphatic chain; g is 0, 1 or 2; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T is an optionally substituted aryl or heteroaryl group, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, and spasticity.
摘要翻译：式I化合物及其药学上可接受的盐，其中A是亚甲基或-O-; B是亚甲基或-O-; G1-G2-G3形成杂芳族或杂脂族链; g为0,1或2; U是任选被一个或多个烷基取代的亚烷基链; Q表示含有氮原子的二价基团; T是任选取代的芳基或杂芳基，可用于治疗中枢神经系统疾病，例如抑郁症，焦虑症，精神病（例如精神分裂症），迟发性运动障碍，帕金森病，肥胖症，高血压，图雷特综合征，性功能障碍，吸毒成瘾，药物滥用，认知障碍，阿尔茨海默病，老年痴呆，强迫症，惊恐发作，社交恐怖症，进食障碍和厌食症，心血管和脑血管疾病，非胰岛素依赖性糖尿病，高血糖症，便秘，心律失常，神经内分泌系统疾病，压力和痉挛状态。

19. 发明授权

US6107310A Heteroarylcarboxamide derivatives for treating CNS disorders 失效
标题翻译：用于治疗CNS病症的杂芳基羧酰胺衍生物
公开(公告)号：US6107310A
公开(公告)日：2000-08-22
申请号：US91129
申请日：1998-06-16
申请人： Alan Martin Birch , Paul Anthony Bradley , Julie Carolyn Gill
发明人： Alan Martin Birch , Paul Anthony Bradley , Julie Carolyn Gill
IPC分类号： A61K31/00 , A61K31/365 , A61K31/366 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61P1/00 , A61P1/10 , A61P3/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/06 , A61P9/12 , A61P15/00 , A61P25/00 , A61P25/02 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D491/04 , C07D491/056 , C07D493/04 , C07D498/04 , C07D513/04 , C07D401/14
CPC分类号： C07D491/04
摘要： Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or --O--; B is methylene or --O--; G.sub.1 --G.sub.2 --G.sub.3 are absent or form a heteroaromatic chain; g is 0,1,2,3 or 4; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO. HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mrellitus, hyperglvcaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.
摘要翻译： PCT No.PCT / EP96 / 05637 371日期：1998年6月16日 102（e）日期1998年6月16日PCT 1996年12月16日PCT公布。公开号WO97 / 23485 日期：1997年7月3日，式I化合物及其药学上可接受的盐，其中A为亚甲基或-O-; B是亚甲基或-O-; G1-G2-G3不存在或形成杂芳族链; g为0,1,2,3或4; U是任选被一个或多个烷基取代的亚烷基链; Q表示含有氮原子的二价基团; T代表CO。HET可用于治疗中枢神经系统疾病，例如抑郁症，焦虑症，精神病（例如精神分裂症），迟发性运动障碍，帕金森病，肥胖症，高血压，图雷特综合征，性功能障碍，药物成瘾，药物滥用，认知障碍，阿尔茨海默病，老年痴呆症，强迫症，惊恐发作，社交恐怖症，进食障碍和厌食症，心血管和脑血管疾病，非胰岛素依赖型糖尿病，高血糖，便秘，心律失常，神经内分泌紊乱系统，压力，前列腺肥大和痉挛状态。

20. 发明申请

US20120289520A1 CHEMICAL COMPOUNDS 785 审中-公开
标题翻译：化学化合物785
公开(公告)号：US20120289520A1
公开(公告)日：2012-11-15
申请号：US13455275
申请日：2012-04-25
申请人： Alan Martin Birch , Roger John Butlin , Leonie Campbell , Clive Green , Andrew Leach , Michael James Waring , Paul Michael Murray , Per Olof Ryberg
发明人： Alan Martin Birch , Roger John Butlin , Leonie Campbell , Clive Green , Andrew Leach , Michael James Waring , Paul Michael Murray , Per Olof Ryberg
IPC分类号： C07D241/24 , A61P3/04 , C07D413/10 , A61P3/10 , A61K31/4965 , A61K31/497
CPC分类号： C07D241/24 , C07D401/12 , C07D413/10
摘要： DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity
摘要翻译：与药物组合物一起描述式（I）的DGAT-1抑制剂化合物，其药学上可接受的盐和前药，其制备方法及其用于治疗例如肥胖症

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