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1. 发明申请

WO2007130824A2 MGLUR5 MODULATORS V 审中-公开
标题翻译： MGLUR5调制器V
公开(公告)号：WO2007130824A2
公开(公告)日：2007-11-15
申请号：PCT/US2007/067371
申请日：2007-04-25
申请人： ASTRAZENECA AB , NPS PHARMACEUTICALS, INC. , WÅLLBERG, Andreas , NILSSON, Karolina , GRANBERG, Kenneth , GHOSAL, Saswati , SLASSI, Abdelmalik , EDWARDS, Louise , ISAAC, Methvin , XIN, Tao , STEFANAC, Tomislav , DOVE, Peter
发明人： WÅLLBERG, Andreas , NILSSON, Karolina , GRANBERG, Kenneth , GHOSAL, Saswati , SLASSI, Abdelmalik , EDWARDS, Louise , ISAAC, Methvin , XIN, Tao , STEFANAC, Tomislav , DOVE, Peter
CPC分类号： C07D487/04
摘要： The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
摘要翻译：本发明涉及新化合物，其制备方法，它们在治疗中的应用和包含新化合物的药物组合物。

2. 发明申请

WO2007130820A3 MGLUR5 MODULATORS I 审中-公开
公开(公告)号：WO2007130820A3
公开(公告)日：2007-11-15
申请号：PCT/US2007/067367
申请日：2007-04-25
申请人： ASTRAZENECA AB , WÅLLBERG, Andreas , NILSSON, Karolina , HOLM, Björn , NÅGÅRD, Mats , GRANBERG, Kenneth , SLASSI, Abdelmalik , EDWARDS, Louise , ISAAC, Methvin , XIN, Tao , STEFANAC, Tomislav
发明人： WÅLLBERG, Andreas , NILSSON, Karolina , HOLM, Björn , NÅGÅRD, Mats , GRANBERG, Kenneth , SLASSI, Abdelmalik , EDWARDS, Louise , ISAAC, Methvin , XIN, Tao , STEFANAC, Tomislav
IPC分类号： C07D413/14 , C07D401/14 , C07D403/14 , A61K31/513 , A61K31/501 , A61P25/02 , A61P25/22 , A61P1/04
摘要： The present invention is directed to novel compounds of Formula (I) for modulation of metabotropic glutamate receptors, in particular mGluRδ and their use in therapy, for instance disorders of the peripheral nervous system, reflux and irritable bowel syndrome.

3. 发明申请

WO2009054787A1 1,2,4-TRIAZOLE CARBOXYLIC ACID DERIVATIVES AS MODULATORS OF MGLUR5 审中-公开
标题翻译：作为MGLUR5的调节剂的1,2,4-三唑羧酸衍生物
公开(公告)号：WO2009054787A1
公开(公告)日：2009-04-30
申请号：PCT/SE2008/051190
申请日：2008-10-23
申请人： ASTRAZENECA AB , GRANBERG, Kenneth , SLASSI, Abdelmalik , STEFANAC, Tomislav , WÅLLBERG, Andreas
发明人： GRANBERG, Kenneth , SLASSI, Abdelmalik , STEFANAC, Tomislav , WÅLLBERG, Andreas
IPC分类号： C07D413/14 , A61K31/4196 , A61P1/04 , A61P25/04 , A61P25/22
CPC分类号： C07D413/14 , C07D413/04
摘要： 1,2,4-triazole carboxylic acid derivatives and their use as modulators of mGluR5 (F).
摘要翻译： 1,2,4-三唑羧酸衍生物及其作为mGluR5（F）的调节剂的用途。

4. 发明申请

WO2009054785A1 1,2,4-TRIAZOLE ETHER DERIVATIVES AS MODULATORS OF MGLUR5 审中-公开
标题翻译：作为MGLUR5的调节剂的1,2,4-三唑醚衍生物
公开(公告)号：WO2009054785A1
公开(公告)日：2009-04-30
申请号：PCT/SE2008/051188
申请日：2008-10-23
申请人： ASTRAZENECA AB , DOVE, Peter , GRANBERG, Kenneth , ISAAC, Methvin , NÅGÅRD, Mats , SLASSI, Abdelmalik
发明人： DOVE, Peter , GRANBERG, Kenneth , ISAAC, Methvin , NÅGÅRD, Mats , SLASSI, Abdelmalik
IPC分类号： C07D401/14 , A61K31/4196 , A61K31/4245 , A61K31/4439 , A61P1/00 , A61P11/00 , A61P25/00 , C07D403/12 , C07D413/12
CPC分类号： C07D257/04 , C07D249/12 , C07D261/08 , C07D401/14 , C07D403/12 , C07D413/12
摘要： The present invention relates to compounds of formula their use for the manufacture of a medicament for treatment of a mGluR5 receptor-mediated disorder. Formula (I)
摘要翻译：本发明涉及式的化合物，其用于制备用于治疗mGluR5受体介导的病症的药物。式（I）

5. 发明申请

WO2009054790A1 AMIDE LINKED HETEROAROMATIC DERIVATIVES AS MODULATORS OF MGLUR5 审中-公开
标题翻译：作为MGLUR5的调节剂的酰胺偶联异构体衍生物
公开(公告)号：WO2009054790A1
公开(公告)日：2009-04-30
申请号：PCT/SE2008/051193
申请日：2008-10-23
申请人： ASTRAZENECA AB , BRATT, Emma , GRANBERG, Kenneth , ISAAC, Methvin , NÅGÅRD, Mats , SLASSI, Abdelmalik
发明人： BRATT, Emma , GRANBERG, Kenneth , ISAAC, Methvin , NÅGÅRD, Mats , SLASSI, Abdelmalik
IPC分类号： C07D413/14 , A61K31/4439 , A61K31/501 , A61P1/04 , A61P25/04 , A61P25/22 , C07D403/14
CPC分类号： C07D403/14 , C07D403/04 , C07D413/14
摘要： Amide linked heteroaromatic derivatives and their use as modulators of mGluR5 (F).
摘要翻译：酰胺连接的杂芳族衍生物及其作为mGluR5（F）的调节剂的用途。

6. 发明申请

WO2009054786A1 1,2,4-TRIAZOLE ARYL N-OXIDES DERIVATIVES AS MODULATORS OF MGLUR5 审中-公开
标题翻译：作为MGLUR5的调节剂的1,2,4-三唑ARYL N-氧化物衍生物
公开(公告)号：WO2009054786A1
公开(公告)日：2009-04-30
申请号：PCT/SE2008/051189
申请日：2008-10-23
申请人： ASTRAZENECA AB , GRANBERG, Kenneth , WÅLLBERG, Andreas
发明人： GRANBERG, Kenneth , WÅLLBERG, Andreas
IPC分类号： C07D413/14 , A61K31/4439 , A61P1/04 , A61P25/04 , A61P25/22 , C07D401/14
CPC分类号： C07D401/14 , C07D401/04 , C07D413/14
摘要： The present invention is directed to 1,2,4-triazole aryl N-oxides derivatives, their use as modulators of mGluR5 and pharmaceutical compositions comprising said compounds.
摘要翻译：本发明涉及1,2,4-三唑芳基N-氧化物衍生物，其用作mGluR5的调节剂和包含所述化合物的药物组合物。

7. 发明申请

WO2012074469A1 NEW IKACH BLOCKERS 审中-公开
标题翻译：新的IKACH BLOCKERS
公开(公告)号：WO2012074469A1
公开(公告)日：2012-06-07
申请号：PCT/SE2011/051440
申请日：2011-11-29
申请人： ASTRAZENECA AB , BOSTRÖM, Jonas , GRANBERG, Kenneth , EMTENÄS, Hans , MOGEMARK, Mickael , LLINAS, Antonio
发明人： BOSTRÖM, Jonas , GRANBERG, Kenneth , EMTENÄS, Hans , MOGEMARK, Mickael , LLINAS, Antonio
IPC分类号： C07D205/04 , A61K31/397 , A61K31/401 , A61K31/44 , A61P7/02 , A61P9/06 , C07D207/09 , C07D207/10 , C07D207/12 , C07D211/38 , C07D211/40 , C07D211/58
CPC分类号： C07D295/13 , C07D205/04 , C07D207/08 , C07D207/12 , C07D211/38 , C07D211/46 , C07D211/62
摘要： The invention relates to compounds according to Formula (I): or a pharmaceutically acceptable salt thereof, wherein m, n, R 1 , R 2 , R 3 , R 4 , R 5 , x and y are as defined herein. Compounds according to Formula (I) are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current (i.e. IKACh blockers), and are believed to be useful in the treatment of cardiac arrhythmias, in particular supraventricular tacharrhythmias, such as atrial fibrillation and atrial flutter.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中m，n，R 1，R 2，R 3，R 4，R 5，x和y如本文所定义。根据式（I）的化合物作为钾通道抑制剂具有药理作用，特别是乙酰胆碱的操作向内整流钾通道电流（即IKACh阻断剂）的抑制剂，并被认为可用于治疗心律失常，特别是室上性心律失常，如房颤和心房扑动。

8. 发明申请

WO2009054789A1 1,2,3-TRIAZOLE PYRROLIDINE DERIVATIVES AS MODULATORS OF MGLUR5 审中-公开
标题翻译：作为MGLUR5的调节剂的1,2,3-三唑吡咯烷衍生物
公开(公告)号：WO2009054789A1
公开(公告)日：2009-04-30
申请号：PCT/SE2008/051192
申请日：2008-10-23
申请人： ASTRAZENECA AB , BRATT, Emma , GRANBERG, Kenneth
发明人： BRATT, Emma , GRANBERG, Kenneth
IPC分类号： C07D401/14 , A61K31/4439 , A61K31/501 , A61P1/00 , A61P1/04 , A61P25/00 , A61P25/22 , C07D403/04 , C07D403/14
CPC分类号： C07D403/14 , C07D401/14 , C07D403/04
摘要： The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
摘要翻译：本发明涉及新化合物，其制备方法，其在治疗中的应用和包含新化合物的药物组合物。

9. 发明申请

WO2007008146A1 HETEROCYCLIC SULFONAMIDE DERIVATIVES AS INHIBITORS OF FACTOR XA 审中-公开
标题翻译：异烟肼衍生物作为因子XA的抑制剂
公开(公告)号：WO2007008146A1
公开(公告)日：2007-01-18
申请号：PCT/SE2006/000840
申请日：2006-07-05
申请人： ASTRAZENECA AB , ALSTERMARK, Christer , AMIN, Kosrat , ANDERSSON, Kjell , FAHLANDER, Ulf , GRANBERG, Kenneth , HOVDAL, Daniel
发明人： ALSTERMARK, Christer , AMIN, Kosrat , ANDERSSON, Kjell , FAHLANDER, Ulf , GRANBERG, Kenneth , HOVDAL, Daniel
IPC分类号： C07D401/14 , A61K31/501 , A61P7/02
CPC分类号： C07D401/14
摘要： The invention relates to compounds of formula (I), Chemical formula should be inserted here. Please see paper copy wherein R 1 , R 2 , R 3 and R 4 are independently selected from carbon and nitrogen, and where at least one of R 1 , R 2 , R 3 and R 4 is nitrogen; A 1 is a single bond or a double bond; n is 0, 1, 2 or 3; each R 5 is independently selected from hydrogen, halogen, C 1-3 alkyl, oxo, oxy, oxido and thioxo; R 6 is hydrogen or oxo; m is 0, 1, 2 or 3; A 2 is a single bond or a double bond; each R 7 is independently selected from hydrogen, hydroxy, oxo, C 1-5 alkyl, carboxy, cyano, tetrazolyl, N -C 1-5 alkyltetrazolyl, oxazolyl, C 1-5 oxazolyl, isoxazolyl, C 1-5 isoxazolyl, hydroxyC 1-5 alkyl, carboxy C 1-5 alkyl, C 1-5 alkoxyoxo C 1-5 alkyl, carbamoyl, C 1-5 alkylcarbamoyl, di(C 1-5 alkyl)carbamoyl, carbamoyl C 1-4 alkyl, C 1-5 alkylcarbamoyl C 1-4 alkyl, di(C 1-5 alkyl)carbamoyl C 1-4 alkyl, hydroxy C 1-5 alkylcarbamoyl, C 1-5 alkoxy C 1-5 alkylcarbamoyl, hydroxy C 1-5 alkylcarbamoyl C 1-4 alkyl, C 1-5 alkoxy C 1-5 alkylcarbamoyl C 1-4 alkyl, -CONR 8 (CH 2 ) x S(O) p R 9 , -CONH(CH 2 ) q NR 10 R 11 , -C 1-5 alkyl-Y 1 , -COOCHR 17 R 18 and -CON R 17 R 18 ; and R 30 is hydrogen, amino, methyl or halogen; or a pharmaceutically acceptable salt thereof, said compounds possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the compounds, to their use, to pharmaceutical compositions comprising them, to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, and to combinations comprising them.
摘要翻译：本发明涉及式（I）化合物，其中应插入化学式。请参见其中R 1，R 2，R 3和R 4中的R 8独立地选自碳和氮，其中R 1，R 2，R 3和R 4中的至少一个为氮; A <1>是单键或双键; n为0,1,2或3; 每个R 5独立地选自氢，卤素，C 1-3烷基，氧代，氧基，氧代和硫代; R 6是氢或氧代; m为0,1,2或3; A <2>是单键或双键; 每个R 7独立地选自氢，羟基，氧代，C 1-5烷基，羧基，氰基，四唑基，NC 1-5 - 烷基四唑基，恶唑基，C 1-5 - 恶唑基，异恶唑基，C 1-5 - 异恶唑基，羟基C 1-5 - 烷基，羧基C 1-4烷基， C 1-5烷基，C 1-5烷氧基氧基C 1-5烷基，氨基甲酰基，C 1-5烷基氨基甲酰基，二（C 1-5烷基）氨基甲酰基，氨基甲酰基C 1-4烷基，C 1-5烷基氨基甲酰基C 1-4，（C 1-5烷基）氨基甲酰基C 1-4烷基，羟基C 1-5烷基氨基甲酰基，C 1 -C 6烷基氨基甲酰基，烷基氨基甲酰基，羟基C 1-5烷基氨基甲酰基C 1-4烷基，C 1-5烷氧基C 1-5烷基氨基甲酰基C 1-4烷基，-CONR 8（CH

10. 发明申请

WO2007008142A1 HETEROCYCLIC SULFONAMIDE DERIVATIVES AS INHIBITORS OF FACTOR XA 审中-公开
标题翻译：异烟肼衍生物作为因子XA的抑制剂
公开(公告)号：WO2007008142A1
公开(公告)日：2007-01-18
申请号：PCT/SE2006/000836
申请日：2006-07-05
申请人： ASTRAZENECA AB , ALSTERMARK, Christer , ANDERSSON, Kjell , FAHLANDER, Ulf , GRANBERG, Kenneth
发明人： ALSTERMARK, Christer , ANDERSSON, Kjell , FAHLANDER, Ulf , GRANBERG, Kenneth
IPC分类号： C07D401/14 , A61K31/501 , A61P7/02
CPC分类号： C07D401/14
摘要： The invention relates to heterocyclic derivatives of formula (I), Chemical formula should be inserted here. Please see paper copy wherein R 1 is hydrogen or C 1-3 alkyl; R 2 is selected from hydroxy, C 1-5 alkyl, carboxy, cyano, tetrazolyl, N -C 1-5 alkyltetrazolyl, oxazolyl, C 1-5 oxazolyl, isoxazolyl, C 1-5 isoxazolyl, hydroxyC 1-5 alkyl, carboxy C 1-5 alkyl, C 1-5 alkoxyoxo C 1-5 alkyl, carbamoyl, C 1-5 alkylcarbamoyl, di(C 1-5 alkyl)carbamoyl, C 1-5 alkylcarbamoyl C 1-4 alkyl, hydroxy C 1-5 alkylcarbamoyl, C 1-5 alkoxy C 1-5 alkylcarbamoyl; -C 1-5 alkyl-Y 1 , -COOCHR 17 R 18 and -CON R 17 R 18 ; and R 3 is hydrogen or halogen; or a pharmaceutically acceptable salt thereof, said compounds possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the compounds, to their use, to pharmaceutical compositions comprising them, to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, and to combinations comprising them.
摘要翻译：本发明涉及式（I）的杂环衍生物，此处应插入化学式。请参见其中R 1是氢或C 1-3烷基的纸张; R 2选自羟基，C 1-5烷基，羧基，氰基，四唑基，NC 1-5烷基四唑基，恶唑基， C 1-5 - 恶唑基，异恶唑基，C 1-5 - 异恶唑基，羟基C 1-5 - 烷基，羧基C 1-5 - 烷基，C 1-5烷氧基氧基C 1-5烷基，氨基甲酰基，C 1-5烷基氨基甲酰基，二（C 1） -5个烷基）氨基甲酰基，C 1-5烷基氨基甲酰基C 1-4烷基，羟基C 1-5烷基氨基甲酰基，C 1-5个烷氧基C 1-5烷基氨基甲酰基; -C 1-6烷基-Y 1，-COOCHR 17 R 18和-CON R“ 17 R 3是氢或卤素; 或其药学上可接受的盐，所述化合物具有抗血栓形成和抗凝血性质，因此可用于治疗人或动物的方法。本发明还涉及制备化合物，其用途，包含它们的药物组合物在制备用于产生抗血栓形成或抗凝血作用的药物中的用途以及包含它们的组合的方法。

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