专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2003010163A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2003010163A1
公开(公告)日：2003-02-06
申请号：PCT/SE2002/001402
申请日：2002-07-19
申请人： ASTRAZENECA AB , GRIFFITHS, David , JOHNSTONE, Craig
发明人： GRIFFITHS, David , JOHNSTONE, Craig
IPC分类号： C07D407/04
CPC分类号： C07D409/04
摘要： The invention relates to thiophene carboxamides of formula (I),wherein R 1 , R 2 , R 3 , A, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明涉及式（I）的噻吩甲酰胺，其中R 1，R 2，R 3，A，n和X如说明书中所定义，其制备中使用的方法和中间体，含有它们的药物组合物及其在治疗中的用途。

2. 发明申请

WO2012066077A1 1,4 DI SUBSTITUTED PYRROLIDINE - 3 - YL -AMINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF METABOLIC DISORDERS 审中-公开
标题翻译： 1,4 DI替代吡咯烷-3-谷氨酸衍生物及其用于治疗代谢性疾病的用途
公开(公告)号：WO2012066077A1
公开(公告)日：2012-05-24
申请号：PCT/EP2011/070346
申请日：2011-11-17
申请人： PROSIDION LIMITED , BARBA, Oscar , BERTRAM, Lisa, Sarah , CARSWELL, Emma Louise , DAVIS, Susan, Helen , FRY, Peter, Timothy , GLEAVE, Robert James , JEEVARATNAM, Revathy, Perpetua , JOHNSTONE, Craig , KEILY, John , PROCTER, Martin, James , SCHOFIELD, Karen, Lesley , STEWART, Alan, John, William , SWAIN, Simon, Andrew
发明人： BARBA, Oscar , BERTRAM, Lisa, Sarah , CARSWELL, Emma Louise , DAVIS, Susan, Helen , FRY, Peter, Timothy , GLEAVE, Robert James , JEEVARATNAM, Revathy, Perpetua , JOHNSTONE, Craig , KEILY, John , PROCTER, Martin, James , SCHOFIELD, Karen, Lesley , STEWART, Alan, John, William , SWAIN, Simon, Andrew
IPC分类号： C07D413/14 , C07D401/14 , A61K31/506 , A61P3/10
CPC分类号： C07D413/14 , C07D401/14
摘要： Therapeutic compounds are disclosed having the general formula (1) that are useful for the treatment of metabolic disorders, including type II diabetes.The compounds have activity as agonists of GPR1 19. Compounds having the stereochemistry of formula (la) may also demonstrate DPP-IV inhibitory activity.
摘要翻译：公开了具有通式（1）的治疗化合物，其可用于治疗代谢紊乱，包括II型糖尿病。该化合物具有作为GPR119激动剂的活性。具有式（Ia）立体化学的化合物还可以显示DPP- IV抑制活性。

3. 发明申请

WO2006082401A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2006082401A1
公开(公告)日：2006-08-10
申请号：PCT/GB2006/000349
申请日：2006-02-02
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BIRCH, Alan, Martin , JOHNSTONE, Craig , PLOWRIGHT, Alleyn, Thomas , SIMPSON, Iain , WHITTAMORE, Paul, Robert, Owen
发明人： BIRCH, Alan, Martin , JOHNSTONE, Craig , PLOWRIGHT, Alleyn, Thomas , SIMPSON, Iain , WHITTAMORE, Paul, Robert, Owen
IPC分类号： C07D495/04 , A61K31/407 , A61P3/10
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。

4. 发明申请

WO2005080360A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2005080360A1
公开(公告)日：2005-09-01
申请号：PCT/GB2005/000562
申请日：2005-02-15
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
发明人： JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
IPC分类号： C07D277/46
CPC分类号： C07D213/75 , C07D231/40 , C07D241/20 , C07D263/48 , C07D277/46 , C07D285/135 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/04 , C07D417/12
摘要： Compounds of Formula (I) wherein: R1 is methyl; R2 is selected from -C (O) NR4R5, SO2NR4R5, S (O) pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C) alkyl and HET-2; R5 is hydrogen or (1-4C) alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them and processes for their preparation are also described.
摘要翻译：式（I）的化合物，其中：R1是甲基; R2选自-C（O）NR4R5，SO2NR4R5，S（O）pR4和HET-2; HET-1是5-或6-元，任选取代的C连接的杂芳基环; HET-2是4-，5-或6-元C-或N-连接的任选取代的杂环基环; R 3选自卤素，氟甲基，二氟甲基，三氟甲基，甲基，甲氧基和氰基; R4选自例如氢，任选取代的（1-4C）烷基和HET-2; R5是氢或（1-4C）烷基; 或R 4和R 5与它们所连接的氮原子一起可以形成由HET-3定义的杂环基环系统; HET-3是例如任选取代的N-连接的，4,5或6元饱和或部分不饱和的杂环基环; p是（每次出现时独立）0,1或2; m为0或1; n为0,1或2; 条件是当m为0时，n为1或2; 或其盐，前药或溶剂化物。还描述了它们用作GLK活化剂，含有它们的药物组合物及其制备方法。

5. 发明申请

WO2005054200A1 BENZOYL AMINO PYRIDYL CARBOXYLIC ACID DERIVATIVES USEFUL AS GLUCOKINASE (GLK) ACTIVATORS 审中-公开
标题翻译：苯甲酰氨基吡啶羧酸衍生物作为GLUCOKINASE（GLK）激活剂有用
公开(公告)号：WO2005054200A1
公开(公告)日：2005-06-16
申请号：PCT/GB2004/004966
申请日：2004-11-25
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
发明人： JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
IPC分类号： C07D213/80
CPC分类号： C07D213/80
摘要： Compounds of Formula: (I); wherein: R¹ is selected from: fluoro, chloro, C 1-3 alkyl and C 1-3 alkoxy; R²-X- is selected from: methyl, methoxymethyl and Formula: (X); n is 0,1 or 2; or a salt, pro-drug or solvate thereof are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.
摘要翻译：式（I）化合物：其中：R 1选自：氟，氯，C 1-3烷基和C 1-3烷氧基; R 2 -X选自：甲基，甲氧基甲基和式：（X）; n为0,1或2; 或其盐，前药或溶剂化物。还描述了它们用作GLK活化剂，含有它们的药物组合物及其制备方法。

6. 发明申请

WO1997032856A1 4-ANILINOQUINAZOLINE DERIVATIVES 审中-公开
标题翻译： 4-苯胺氮杂环丁烷衍生物
公开(公告)号：WO1997032856A1
公开(公告)日：1997-09-12
申请号：PCT/GB1997000550
申请日：1997-02-28
申请人： ZENECA LIMITED , ZENECA PHARMA S.A. , THOMAS, Andrew, Peter , HENNEQUIN, Laurent, François, André , JOHNSTONE, Craig
发明人： ZENECA LIMITED , ZENECA PHARMA S.A.
IPC分类号： C07D239/94
CPC分类号： C07D239/94
摘要： The invention relates to quinazoline derivatives of formula (I) (wherein: R represents hydrogen or methoxy; R represents methoxy, ethoxy, 2-methoxyethoxy, 3-methoxypropoxy, 2-ethoxyethoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, 2-hydroxyethoxy, 3-hydroxypropoxy, 2-(N,N-dimethylamino)ethoxy, 3-(N,N-dimethylamino)propoxy, 2-morpholinoethoxy, 3-morpholinopropoxy, 4-morpholinobutoxy, 2-piperidinoethoxy, 3-piperidinopropoxy, 4-piperidinobutoxy, 2-(piperazin-1-yl)ethoxy, 3-(piperazin-1-yl)propoxy, 4-(piperazin-1-yl)butoxy, 2-(4-methylpiperazin-1-yl)ethoxy, 3-(4-methylpiperazin-1-yl)propoxy or 4-(4-methylpiperazin-1-yl)butoxy; the phenyl group bearing (R )2 is selected from: 2-fluoro-5-hydroxyphenyl, 4-bromo-2-fluorophenyl, 2,4-difluorophenyl, 4-chloro-2-fluorophenyl, 2-fluoro-4-methylphenyl, 2-fluoro-4-methoxyphenyl, 4-bromo-3-hydroxyphenyl, 4-fluoro-3-hydroxyphenyl, 4-chloro-3-hydroxyphenyl, 3-hydroxy-4-methylphenyl, 3-hydroxy-4-methoxyphenyl and 4-cyano-2-fluorophenyl); and salts thereof, processes for their preparation and pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
摘要翻译：本发明涉及式（I）的喹唑啉衍生物（其中：R 1表示氢或甲氧基; R 2表示甲氧基，乙氧基，2-甲氧基乙氧基，3-甲氧基丙氧基，2-乙氧基乙氧基，三氟甲氧基， 2-（N，N-二甲基氨基）乙氧基，3-（N，N-二甲氨基）丙氧基，2-吗啉代乙氧基，3-吗啉代丙氧基，4-吗啉代丁氧基，2-哌啶子基乙氧基， 3-哌啶基丁氧基，2-（哌嗪-1-基）乙氧基，3-（哌嗪-1-基）丙氧基，4-（哌嗪-1-基）丁氧基，2-（4-甲基哌嗪-1-基）乙氧基，3-（4-甲基哌嗪-1-基）丙氧基或4-（4-甲基哌嗪-1-基）丁氧基;带有（R 3）2的苯基选自：2-氟-5 4-羟基苯基，4-溴-2-氟苯基，2,4-二氟苯基，4-氯-2-氟苯基，2-氟-4-甲基苯基，2-氟-4-甲氧基苯基，4-溴-3-羟基苯基，4 4-氟-3-羟基苯基，3-羟基-4-甲基苯基，3-羟基-4-甲氧基苯基和4-氰基-2-氟苯基）。及其盐，其制备方法和含有式（I）化合物或其药学上可接受的盐作为活性成分的药物组合物。式（I）化合物及其药学上可接受的盐抑制VEGF的作用，其在治疗许多疾病状态（包括癌症和类风湿性关节炎）中是有价值的。

7. 发明申请

WO2008068507A2 CHEMICAL COMPOUNDS-576 审中-公开
标题翻译：化学化合物-576
公开(公告)号：WO2008068507A2
公开(公告)日：2008-06-12
申请号：PCT/GB2007004697
申请日：2007-12-07
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , AQUILA BRIAN , COOK DONALD JAMES , JOHNSTONE CRAIG , LEE STEPHEN , LYNE PAUL , RUDGE DAVID ALAN , VASBINDER MELISSA , WANG HAIXIA
发明人： AQUILA BRIAN , COOK DONALD JAMES , JOHNSTONE CRAIG , LEE STEPHEN , LYNE PAUL , RUDGE DAVID ALAN , VASBINDER MELISSA , WANG HAIXIA
IPC分类号： C07D401/04 , A61K31/472 , A61P35/00
CPC分类号： C07D401/04
摘要： The invention relates to chemical compounds of the formula (I): or pharmaceutically or pharmaceutically acceptable salts thereof, which possess B-Raf inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.
摘要翻译：本发明涉及具有B-Raf抑制活性的式（I）化合物或其药学上可接受的盐，因此可用于其抗癌活性，因此可用于治疗人或动物体的方法。本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在制造用于在温血动物如人中产生抗癌作用的药物中的用途。

8. 发明申请

WO2006040529A1 BENZAMIDE DERIVATIVES THAT ACT UPON THE GLUCOKINASE ENZYME 审中-公开
标题翻译：硼酸衍生物，其作用在葡萄糖激酶上
公开(公告)号：WO2006040529A1
公开(公告)日：2006-04-20
申请号：PCT/GB2005/003890
申请日：2005-10-11
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon , WARING, Michael, James
发明人： JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon , WARING, Michael, James
IPC分类号： C07D231/40
CPC分类号： C07D231/40
摘要： Compounds of Formula: (I); wherein: R 1 is hydroxymethyl; R 2 is selected from -C(O)NR 4 R 5 , SO 2 NR 4 R 5 , S(O)pR 4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R 3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R 4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R 5 is hydrogen or (1-4C)alkyl; or R 4 and R 5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.
摘要翻译：式（I）化合物：其中：R

9. 发明申请

WO2005080359A1 BENZAMIDE DERIVATIVES AND THEIR USE AS GLUCOKINAE ACTIVATING AGENTS 审中-公开
标题翻译：苯甲酸衍生物及其作为GLUCOKINAE活化剂的用途
公开(公告)号：WO2005080359A1
公开(公告)日：2005-09-01
申请号：PCT/GB2005/000545
申请日：2005-02-15
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
发明人： JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
IPC分类号： C07D277/46
CPC分类号： C07D487/08 , C07D231/40 , C07D277/46 , C07D403/12 , C07D417/12
摘要： Compounds of Formula (I): wherein: R 1 is methoxymethyl; R 2 is selected from -C(O)NR 4 R 5 , -SO 2 NR 4 R 5 , -S(O) p R 4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R 3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R 4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R 5 is hydrogen or (1-4C)alkyl; or R 4 and R 5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; mis 0 or1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro-drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.
摘要翻译：式（I）的化合物：其中：R 1是甲氧基甲基; R 2选自-C（O）NR 4 R 5，-SO 2 NR 4 R 5，-S（O）p R 4和HET-2; HET-1是5-或6-元，任选取代的C连接的杂芳基环; HET-2是4-，5-或6-元C-或N-连接的任选取代的杂环基环; R 3选自卤素，氟甲基，二氟甲基，三氟甲基，甲基，甲氧基和氰基; R 4选自例如氢，任选取代的（1-4C）烷基和HET-2; R 5是氢或（1-4C）烷基; 或R 4和R 5与它们所连接的氮原子一起可以形成由HET-3定义的杂环基环系; HET-3是例如任选取代的N-连接的，4,5或6元饱和或部分不饱和的杂环基环; p是（每次出现时独立）0,1或2; 误0或1; n为0,1或2; 条件是当m为0时，n为1或2; 或其盐，前药或溶剂化物。还描述了它们用作GLK活化剂，含有它们的药物组合物及其制备方法。

10. 发明申请

WO2005056530A1 BENZOYL AMINO PYRIDYL CARBOXYLIC ACID DERIVATIVES USEFUL AS GLUCOKINASE (GLK) ACTIVATORS 审中-公开
标题翻译：苯甲酰氨基吡啶羧酸衍生物作为GLUCOKINASE（GLK）激活剂有用
公开(公告)号：WO2005056530A1
公开(公告)日：2005-06-23
申请号：PCT/GB2004/005068
申请日：2004-12-02
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , CAULKETT, Peter, William, Rodney , JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
发明人： CAULKETT, Peter, William, Rodney , JOHNSTONE, Craig , MCKERRECHER, Darren , PIKE, Kurt, Gordon
IPC分类号： C07D213/80
CPC分类号： C07D213/80
摘要： A compound of Formula (I): Formula (I) wherein: R 1 is selected from hydrogen and C 1-4 alkyl; R 2 is selected from: R 4 -C(R 5a R 5b )- , R 4 =C(R 6 )- and R 7a C(R 7b )=C(R 6 )-; R 3 X- is selected from methyl, methoxymethyl and ; R 4 is selected from (optionally substituted) C 1-4 alkyl, phenyl, C 3-6 cycloalkyl and heteroaryl; R 5a and R 5b are independently selected from hydrogen, fluoro and C 1-4 alkyl; R 6 is selected from hydrogen and C 1-4 alkyl; R 7a and R 7b are optionally substituted C 1-4 alkyl; or a salt, pro-drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.
摘要翻译：式（I）的化合物：式（I）其中：R 1选自氢和C 1-4烷基; R 2选自：R 4 -C（R 5a R 5b） - ，R 4 = C（R 6） - 和R 7a（R 7b））= C（R <6>） - ; R 3选自甲基，甲氧基甲基和 R 4选自（任选取代的）C 1-4烷基，苯基，C 3-6环烷基和杂芳基; R 5a和R 5b独立地选自氢，氟和C 1-4烷基; R 6选自氢和C 1-4烷基; R 7a和R 7b是任选取代的C 1-4烷基; 或其盐，前药或溶剂化物。还描述了它们用作GLK活化剂，含有它们的药物组合物及其制备方法。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式