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1. 发明申请

WO2007141538A1 OXAZOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DIABETES AND OBESITY 审中-公开
标题翻译：奥沙唑衍生物及其在治疗糖尿病和肥胖症中的应用
公开(公告)号：WO2007141538A1
公开(公告)日：2007-12-13
申请号：PCT/GB2007/002119
申请日：2007-06-08
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BIRCH, Alan, Martin , DAVIES, Robert , WHALLEY, David, Paul
发明人： BIRCH, Alan, Martin , DAVIES, Robert , WHALLEY, David, Paul
IPC分类号： C07D263/48 , A61K31/421 , A61P3/04 , A61P3/10
CPC分类号： C07D263/48
摘要： Compounds of formula (I), or salts thereof, which inhibit acetyl CoA(acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein, for example, R 1 is an optionally substituted aryl or optionally substituted heteroaryl group; T is N, CH or CMe; Y is a direct bond, or a defined linking group and R 2 is an optionally substituted aryl, an optionally substituted cycloalkyl or an optionally substituted heterocyclic group; 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）化合物或其盐，其中例如R 1是任选取代的芳基或任选取代的杂芳基; T为N，CH或CMe; Y是直接键或定义的连接基团，R 2是任选取代的芳基，任选取代的环烷基或任选取代的杂环基; 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。

2. 发明申请

WO2005013981A1 HETEROCYCLIC AMIDE DERIVATIVES WHICH POSSESS GLYCOGEN PHOSPHORYLASE INHIBITORY ACTIVITY 审中-公开
标题翻译：杂环化合物酰胺衍生物，其具有磷酸酶抑制活性
公开(公告)号：WO2005013981A1
公开(公告)日：2005-02-17
申请号：PCT/GB2004/003345
申请日：2004-08-04
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BIRCH, Alan, Martin , BENNETT, Stuart, Norman, Lile , CAMPBELL, Andrew, Duncan , SIMPSON, Iain , WHITTAMORE, Paul, Robert, Owen , WHALLEY, David, Paul , GODFREY, Linda
发明人： BIRCH, Alan, Martin , BENNETT, Stuart, Norman, Lile , CAMPBELL, Andrew, Duncan , SIMPSON, Iain , WHITTAMORE, Paul, Robert, Owen , WHALLEY, David, Paul , GODFREY, Linda
IPC分类号： A61K31/407
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, R 4 and R 5 together are either -S-C(R 6 )=C(R7)- or -C(R 7 )=C(R 6 )-S- ; R 6 and R 7 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; R 1 is halo, cyano or carboxy; Y is selected from -C(O)R 2 , -C(O)OR 2 , -C(O)NR 2 R 3 , -(1-4C)alkyl [optionally substituted] -(2-4C)alkenyl, -SO 2 NR 2 R 3 , and -S(O) c R 2 (wherein c is 0, 1 or 2); R 2 and R 3 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-; 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; R 6和R 7独立地选自氢，卤素，硝基，氰基，羟基， 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; Y选自-C（O）R 2，-C（O）OR 2，-C（O）NR 2 R 3， - （1-4C）烷基[任意取代的] （2-4C）烯基，-SO 2 NR 2 R 3和-S（O）c R 2（其中c为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。

3. 发明申请

WO2008129319A1 SALTS OF OXADIAZOLE DERIVATIVES AS DGAT INHIBITORS 审中-公开
标题翻译：氧化氮衍生物作为DGAT抑制剂的盐
公开(公告)号：WO2008129319A1
公开(公告)日：2008-10-30
申请号：PCT/GB2008/050270
申请日：2008-04-18
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BACK, Kevin, Richard , WHALLEY, David, Paul
发明人： BACK, Kevin, Richard , WHALLEY, David, Paul
IPC分类号： C07D271/113 , A61K31/4245 , A61P3/10
CPC分类号： C07D271/113
摘要： Sodium, magnesium, tert -butylammonium salt, tris( hydroxymethyl)methylammonium, triethanolammonium, diethanolammonium, ethanolammonium, methylethanolammonium, diethylammonium and nicotinamide salts of a compound of formula (I) are provided, which compounds inhibit acetyl CoA(acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity: Formula (I) wherein R 1 is phenyl optionally substituted with 1, 2 or 3 substituents independently selected from fluoro, chloro, bromo, trifluoromethyl, methoxy, difluoromethoxy, trifluoromethoxy, cyano, methyl and ethyl; R A is hydrogen or methyl; p is 0 or 1; with the proviso that the salt of formula (I) is not sodium ( trans -4-{4-[({5-[(2,4,5- trifluorophenyl) amino]-1,3,4-oxadiazol-2-yl} carbonyl)amino]phenyl}c yclohexyl)acetate; together with processes for preparing such compounds, their utility in treating clinical conditions associated with obesity, methods for their therapeutic use and pharmaceutical compositions containing them.
摘要翻译：提供式（I）化合物的钠，镁，叔丁基铵盐，三（羟甲基）甲基铵，三乙醇铵，二乙醇铵，乙醇铵，甲基乙醇铵，二乙基铵和烟酰胺盐，这些化合物抑制乙酰辅酶A（乙酰辅酶A）：二酰基甘油酰基转移酶（DGAT1）活性：其中R 1是任选被1,2或3个独立地选自氟，氯，溴，三氟甲基，甲氧基，二氟甲氧基，三氟甲氧基，氰基，甲基和乙基的取代基取代的苯基的式（I） R A是氢或甲基; p为0或1; 条件是式（I）的盐不是钠（反-4- {4 - [（{5 - [（2,4,5-三氟苯基）氨基] -1,3,4-恶二唑-2-基吡啶-3-基}羰基）氨基]苯基}环己基）乙酸酯; 以及制备这些化合物的方法，它们在治疗与肥胖相关的临床病症中的应用，其治疗用途的方法和含有它们的药物组合物。

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