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1. 发明申请

WO2008050101A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2008050101A2
公开(公告)日：2008-05-02
申请号：PCT/GB2007004018
申请日：2007-10-22
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , CAMPBELL LEONIE , PIKE KURT GORDON , SULEMAN ABID , WARING MICHAEL JAMES
发明人： CAMPBELL LEONIE , PIKE KURT GORDON , SULEMAN ABID , WARING MICHAEL JAMES
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D411/14 , C07D413/14 , C07D417/14 , C07D419/14
摘要： The invention relates to a novel group of compounds of Formula (I) or a salt thereof: wherein R 1 , A and HET-1 are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK) such as type 2 diabetes. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by GLK using said compounds and methods for preparing compounds of Formula (I).
摘要翻译：本发明涉及一组新的式（I）化合物或其盐：其中R 1，A和HET-1如说明书中所述，其可用于治疗或预防通过葡萄糖激酶（GLK）如2型糖尿病介导的疾病或医学病症。本发明还涉及包含所述化合物的药物组合物，使用所述化合物治疗由GLK介导的疾病的方法和制备式（I）化合物的方法。

2. 发明申请

WO2007007042A8 HETEROARYL BENZAMIDE DERIVATIVES FOR USE AS GLK ACTIVATORS IN THE TREATMENT OF DIABETES 审中-公开
标题翻译：用于治疗糖尿病的GLK激活剂的异氟烷苯甲酸衍生物
公开(公告)号：WO2007007042A8
公开(公告)日：2008-09-12
申请号：PCT/GB2006002472
申请日：2006-07-03
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , MCKERRECHER DARREN , PIKE KURT GORDON , WARING MICHAEL JAMES
发明人： MCKERRECHER DARREN , PIKE KURT GORDON , WARING MICHAEL JAMES
IPC分类号： C07D403/12 , A61K31/4155 , A61P3/04 , A61P3/06 , C07D231/40
CPC分类号： C07D231/40 , C07D403/12
摘要： Compounds of formula (I) wherein R 1 , R 2 , R 3 , and HET-1 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.
摘要翻译：其中R 1，R 2，R 3和HET-1的式（I）化合物如说明书中所述，它们盐是葡萄糖激酶（GLK）的活化剂，因此可用于治疗例如2型糖尿病。还描述了制备式（I）化合物的方法。

3. 发明申请

WO2010015849A3 PYRAZOLO [3,4] PYRIMIDIN-4-YL DERIVATIVES AND THEIR USES TO TREAT DIABETES AND OBESITY 审中-公开
标题翻译：吡咯并[3,4]吡咯烷-4-YL衍生物及其用于治疗糖尿病和肥胖症的用途
公开(公告)号：WO2010015849A3
公开(公告)日：2010-04-01
申请号：PCT/GB2009050970
申请日：2009-08-03
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , BENNETT STUART NORMAN LILE , BONN PETER GUSTAF , BRINK MIKAEL DAN , BUTLIN ROGER JOHN , CAMPBELL LEONIE , DAVIES ROBERT DARREN MORSE , FAEGERHAG JONAS RICKARD , JURVA ULRIK , POINTON HELEN CLAIRE , ROBB GRAEME RICHARD , SCHNECKE VOLKER , SVENSSON HENRIKSSON ANETTE MAR , WALKER ROLF PETER , WARING MICHAEL JAMES , WESTERLUND CHRISTER RALF
发明人： BENNETT STUART NORMAN LILE , BONN PETER GUSTAF , BRINK MIKAEL DAN , BUTLIN ROGER JOHN , CAMPBELL LEONIE , DAVIES ROBERT DARREN MORSE , FAEGERHAG JONAS RICKARD , JURVA ULRIK , POINTON HELEN CLAIRE , ROBB GRAEME RICHARD , SCHNECKE VOLKER , SVENSSON HENRIKSSON ANETTE MARIE , WALKER ROLF PETER , WARING MICHAEL JAMES , WESTERLUND CHRISTER RALF
IPC分类号： C07D487/04 , A61K31/519 , A61P3/04 , A61P3/10
CPC分类号： C07D487/04
摘要： A compound of Formula (I) is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK or GK), leading to a decreased glucose threshold for insulin secretion.
摘要翻译：式（I）的化合物可用于治疗或预防通过葡萄糖激酶（GLK或GK）介导的疾病或医学病症，导致胰岛素分泌的葡萄糖阈值降低。

4. 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。

5. 发明申请

WO2006024841A2 BENZAMIDE COMPOUNDS 审中-公开
标题翻译：苯甲酸化合物
公开(公告)号：WO2006024841A2
公开(公告)日：2006-03-09
申请号：PCT/GB2005003355
申请日：2005-08-31
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , GIBSON KEITH HOPKINSON , STOKES ELAINE SOPHIE ELIZABETH , WARING MICHAEL JAMES , ANDREWS DAVID MICHAEL , MATUSIAK ZBIGNIEW STANELY , GRAHAM MARK ANDREW
发明人： GIBSON KEITH HOPKINSON , STOKES ELAINE SOPHIE ELIZABETH , WARING MICHAEL JAMES , ANDREWS DAVID MICHAEL , MATUSIAK ZBIGNIEW STANELY , GRAHAM MARK ANDREW
IPC分类号： E01F
CPC分类号： C07D417/12 , C07D213/85 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D487/08
摘要： The invention concerns benzamide compounds of Formula (I), wherein R 1a , R 1b , R 1c , R 2 , R 3 , R 4 , m and n have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of histone deacetylase (HDAC).
摘要翻译：本发明涉及式（I）的苯甲酰胺化合物，其中R 1a，R 1b，R 1c，R 2， >，R 3，R 4，m和n具有在说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗对组蛋白脱乙酰酶（HDAC）的抑制敏感的肿瘤或其它增殖病症中的抗增殖剂的药物中的用途。

6. 发明申请

WO2006077387A3 NOVEL BENZAMIDE DERIVATIVES 审中-公开
标题翻译：新型苯甲酰胺衍生物
公开(公告)号：WO2006077387A3
公开(公告)日：2006-10-05
申请号：PCT/GB2006000134
申请日：2006-01-17
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , GIBSON KEITH HOPKINSON , STOKES ELAINE SOPHIE ELIZABETH , WARING MICHAEL JAMES , ANDREWS DAVID MICHAEL , MATUSIAK ZBIGNIEW STANELY
发明人： GIBSON KEITH HOPKINSON , STOKES ELAINE SOPHIE ELIZABETH , WARING MICHAEL JAMES , ANDREWS DAVID MICHAEL , MATUSIAK ZBIGNIEW STANELY
IPC分类号： C07D213/56 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/496 , A61K31/497 , A61P35/00 , C07D213/38 , C07D213/73 , C07D213/75 , C07D213/82 , C07D401/06 , C07D401/12
CPC分类号： C07D213/73 , C07D213/38 , C07D213/56 , C07D213/75 , C07D213/82 , C07D401/06 , C07D401/12
摘要： The invention concerns benzamide derivatives of Formula (I) wherein R 1a , R 1b , R 1c , R 2 , R 3 , R 4 , integer m, integer n and W have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of histone deacetylase (HDAC).
摘要翻译：本发明涉及式（I）的苯甲酰胺衍生物，其中R 1，R 1，R 1，R 1，R 2，R 3， R 3，R 4，整数m，整数n和W具有在说明书中定义的任何含义; 它们的制备方法，含有它们的药物组合物以及它们在制备用作抗增殖剂的药物中的用途，所述药物用于预防或治疗对抑制组蛋白脱乙酰酶（HDAC）敏感的肿瘤或其他增殖性病症。

7. 发明专利

IL190429A BENZAMIDE COMPOUNDS USEFUL AS HISTONE DEACETYLASE INHIBITORS 未知
公开(公告)号：IL190429A
公开(公告)日：2012-08-30
申请号：IL19042908
申请日：2008-03-25
申请人： ASTRAZENECA AB , STOKES ELAINE SOPHIE ELIZABETH , WARING MICHAEL JAMES , TURNER ANDREW , ANDREWS DAVID MICHAEL
发明人： STOKES ELAINE SOPHIE ELIZABETH , WARING MICHAEL JAMES , TURNER ANDREW , ANDREWS DAVID MICHAEL
IPC分类号： C07D401/06
摘要： The invention concerns benzamide compounds of formula (I): compound of formula (I): wherein R1 is a C-linked pyrazole ring, which is optionally substituted by one or more groups selected from C1-4alkyl, C3-4cycloalkyl, C1-4alkoxy and C3-4cycloalkoxy; or a pharmaceutically acceptable salt or pro-drug form thereof. The invention also concerns processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumors or other proliferative conditions, which are sensitive to the inhibition of histone deacetylase (HDAC).

8. 发明专利

IL164373A BENZAMIDE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, PROCESS FOR THEIR PREPARATION AND USE THEREOF IN THE MANUFACTURE OF MEDICAMENTS AND AS MEDICAMENTS IN THE TREATMENT OF DISEASES ASSOCIATED WITH CANCER 未知
公开(公告)号：IL164373A
公开(公告)日：2011-02-28
申请号：IL16437304
申请日：2004-10-03
申请人： ASTRAZENECA AB , STOKES ELAINE SOPHIE ELIZABETH , ROBERTS CRAIG ANTHONY , WARING MICHAEL JAMES
发明人： STOKES ELAINE SOPHIE ELIZABETH , ROBERTS CRAIG ANTHONY , WARING MICHAEL JAMES
IPC分类号： C07D251/14 , A61K31/341 , A61K31/426 , A61K31/427 , A61K31/435 , A61K31/4365 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/444 , A61K31/445 , A61K31/4465 , A61K31/4525 , A61K31/453 , A61K31/454 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/4965 , A61K31/497 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/53 , A61K31/5375 , A61K31/5377 , A61P7/06 , A61P25/14 , A61P35/00 , A61P43/00 , C07D211/34 , C07D213/56 , C07D213/74 , C07D215/12 , C07D237/08 , C07D239/26 , C07D239/42 , C07D241/12 , C07D241/18 , C07D241/20 , C07D251/18 , C07D277/20 , C07D277/24 , C07D277/30 , C07D295/14 , C07D295/155 , C07D307/54 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D407/06 , C07D409/04 , C07D413/04 , C07D413/06 , C07D417/06 , C07D487/04 , C07D495/04
摘要： The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by histone deacetylase.

9. 发明专利

JP2009263390A Heteroaryl benzamide derivative for use as glk activator in treatment of diabetes 审中-公开
标题翻译：用作治疗糖尿病的GLK激活剂的苯甲胆碱衍生物
公开(公告)号：JP2009263390A
公开(公告)日：2009-11-12
申请号：JP2009157686
申请日：2009-07-02
申请人： Astrazeneca Ab , アストラゼネカアクチボラグ
发明人： MCKERRECHER DARREN , PIKE KURT GORDON , WARING MICHAEL JAMES
IPC分类号： C07D401/12 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/506 , A61K31/5377 , A61P3/10 , A61P43/00 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14
CPC分类号： C07D417/14 , A61K31/397 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D487/08
摘要： PROBLEM TO BE SOLVED: To provide a compound which is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase, leading to a decreased glucose threshold for insulin secretion. SOLUTION: There is provided the compound represented by formula (I), (wherein, R 1 is a specific alkyl group such as isopropyl, cyclopropyl, 1,3-difluoropropyl, and HET-1 and HET-2 are each a specific heterocyclic ring). The compound has glucokinase (GLK) activating activity, and useful in the treatment of, for example, type II diabetes. COPYRIGHT: (C)2010,JPO&INPIT

10. 发明专利

JP2011046724A Benzoylaminoheterocyclyl compound as glucokinase (glk) activator 审中-公开
标题翻译：苯甲酰氨基胆碱化合物作为GLUCOKINASE（GLK）激活剂
公开(公告)号：JP2011046724A
公开(公告)日：2011-03-10
申请号：JP2010228109
申请日：2010-10-08
申请人： Astrazeneca Ab , アストラゼネカアクチボラグ
发明人： MARTIN NATHANIEL GEORGE , MCKERRECHER DARREN , PIKE KURT GORDON , WARING MICHAEL JAMES
IPC分类号： C07D237/24 , A61K31/4439 , A61K31/4965 , A61K31/497 , A61P3/10 , A61P43/00 , C07D401/12 , C07D403/12
CPC分类号： C07D403/12 , C07D241/24 , C07D401/12
摘要： PROBLEM TO BE SOLVED: To provide compounds and pharmaceutical compositions which may be useful in treatment or prevention of a disease or medical condition mediated through glucokinase (GLK) such as type 2 diabetes. SOLUTION: The invention relates to a new group of the compounds of formula (I) or a salt thereof (wherein ring A is a five- or six-membered heteroaryl ring containing one, two or three ring heteroatoms independently selected from O, S and N). The pharmaceutical compositions comprising the compounds, methods of treatment of diseases mediated by GLK using the compounds, and methods for producing the compounds of formula (I) are also provided. COPYRIGHT: (C)2011,JPO&INPIT

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