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1. 发明申请

WO03074513A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO03074513A2
公开(公告)日：2003-09-12
申请号：PCT/GB0300893
申请日：2003-03-04
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , BIRCH ALAN MARTIN , MORLEY ANDREW DAVID
发明人： BIRCH ALAN MARTIN , MORLEY ANDREW DAVID
IPC分类号： A61K31/4709 , A61K31/497 , A61K31/501 , A61K31/506 , A61P3/04 , A61P3/10 , A61P7/00 , A61P9/10 , A61P43/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D417/14 , A61K31/404
CPC分类号： C07D401/12 , C07D401/14 , C07D417/14
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; R2 is hydrogen, hydroxy or carboxy;R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C 1-4 alkyl(optionally substituted by 1 or 2 R8 groups);R4 is independently selected from for example hydrogen, halo, nitro, cyano, hydroxy, C 1-4 alkyl, and C 1-4 alkanoyl; 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, C 1-4 alkyl (optionally substituted by 1 or 2 R13 );R13 is selected from hydroxy, halo, trihalomethyl and C 1-4 alkoxy;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 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基团取代）; R 4独立地选自例如氢，卤素，硝基，氰基，羟基，C 1-4烷基和C 1-4烷酰基; R8选自例如羟基，-COCOOR9，-C（O）N（R9）（R10），-NHC（O）R9，（R9）（R10）N-和-COOR9; R9和R10选自例如氢，羟基，C 1-4烷基（任选被1或2个R 13取代）; 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。

2. 发明申请

WO2009024821A3 OXADIAZOLE DERIVATIVES AS DGAT INHIBITORS 审中-公开
标题翻译：氧化氮衍生物作为DGAT抑制剂
公开(公告)号：WO2009024821A3
公开(公告)日：2009-04-09
申请号：PCT/GB2008050716
申请日：2008-08-15
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , BIRCH ALAN MARTIN , BUTLIN ROGER JOHN , GILL ADRIAN LIAM , GROOMBRIDGE SAMUEL DAVID , PLOWRIGHT ALLEYN , WARING MICHAEL JAMES
发明人： BIRCH ALAN MARTIN , BUTLIN ROGER JOHN , GILL ADRIAN LIAM , GROOMBRIDGE SAMUEL DAVID , PLOWRIGHT ALLEYN , WARING MICHAEL JAMES
IPC分类号： C07D413/12 , A61K31/4245 , A61P3/00
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; R1and R2are, 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; togetherwith processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
摘要翻译：提供了抑制乙酰CoA（乙酰辅酶A）：二酰基甘油酰基转移酶（DGAT1）活性的式（I）化合物或其药学上可接受的盐和/或前药，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，其各自任选被例如选自（1-4C）的一个取代基取代，烷基，（1-4C）烷氧基和（1-4C）烷氧基（1-4C）烷基; 或环A是任选取代的亚苯基，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。

3. 发明申请

WO0172741A3 N-BENZODIOXANYLMETHYL-1-PIPERIDYL-METHYLAMINE COMPOUNDS FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS 审中-公开
标题翻译：用于治疗中枢神经系统疾病的N-苯并咪唑-1-甲基-1-哌啶基 - 甲基胺化合物
公开(公告)号：WO0172741A3
公开(公告)日：2002-01-03
申请号：PCT/EP0103463
申请日：2001-03-27
申请人： KNOLL AG , BIRCH ALAN MARTIN , NEEDHAM PATRICIA LESLEY
发明人： BIRCH ALAN MARTIN , NEEDHAM PATRICIA LESLEY
IPC分类号： A61P25/00 , C07D405/12 , A61K31/44
CPC分类号： C07D405/12
摘要： Compound of formula (I) including pharmaceutically acceptable salts thereof in which R1 represents halo or pseudohalo and R2 represents H or an acyl group derived from a C7-C18 saturated aliphatic carboxylic acid; with the proviso that when R1 is Cl or CF3 and R2 is H then these compounds are in isolated form, their preparation and their use in the treatment of depression, anxiety, psychoses, Parkison'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, eating disorders, anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, drug-induced extrapyramidal symptoms or spasticity; are described.
摘要翻译：式（I）的化合物，其包括其药学上可接受的盐，其中R 1表示卤素或假卤素，R 2表示H或衍生自C 7 -C 18饱和脂族羧酸的酰基; 条件是当R1为Cl或CF3且R2为H时，这些化合物为分离形式，其制备及其用于治疗抑郁症，焦虑症，精神病，帕金森氏症，肥胖症，高血压，杜氏综合征，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，恐慌发作，饮食失调，厌食，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，神经内分泌紊乱系统，压力，前列腺肥大，药物诱导的锥体外系症状或痉挛状态; 被描述。

4. 发明申请

WO0100187A3 PHARMACEUTICAL COMPOSITION CONTAINING SIBUTRAMINE AND A LIPASE INHIBITOR 审中-公开
标题翻译：含有SIBUTRAMINE和脂肪酶抑制剂的药物组合物
公开(公告)号：WO0100187A3
公开(公告)日：2001-11-15
申请号：PCT/EP0005544
申请日：2000-06-16
申请人： KNOLL AG , BIRCH ALAN MARTIN , HEAL DAVID JOHN
发明人： BIRCH ALAN MARTIN , HEAL DAVID JOHN
IPC分类号： A61K45/00 , A61K31/00 , A61K31/135 , A61K31/137 , A61K45/06 , A61P3/04
CPC分类号： A61K45/06 , A61K31/135 , A61K2300/00
摘要： A method for the treatment of obesity and associated co-morbid conditions in a human in need of such treatment which comprises administration to the human of a therapeutically effective amount of a compound of formula (I), including enantiomers and pharmaceutically acceptable salts thereof, in which R1 and R2 are independently H or methyl, and a therapeutically effective amount of a lipase inhibitor with the exception of orlistat; wherein the compound of formula (I) and the lipase inhibitor are administered simultaneously, separately or sequentially.
摘要翻译：一种用于治疗需要这种治疗的人的肥胖症和相关并发病症的方法，其包括向人施用治疗有效量的式（I）化合物，包括其对映体和药学上可接受的盐，在其中R1和R2独立地为H或甲基，以及治疗有效量的除了奥利司他之外的脂肪酶抑制剂; 其中式（I）化合物和脂肪酶抑制剂分别或相继同时施用。

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