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1. 发明申请

US20070135441A1 New derivatives of 6-{4-[4-(1h-indole-2-sulphonyl)-piperazin-1-carbonyl-phenyl]}pyradizin-3-one 失效
标题翻译： 6- {4- [4-（1H-吲哚-2-磺酰基） - 哌嗪-1-羰基 - 苯基]}嘧啶并[3'
公开(公告)号：US20070135441A1
公开(公告)日：2007-06-14
申请号：US10584473
申请日：2005-01-05
申请人： Emma Bratt , Yantao Chen , Kenneth Granberg , Ingemar Nilsson
发明人： Emma Bratt , Yantao Chen , Kenneth Granberg , Ingemar Nilsson
IPC分类号： C07D403/14 , A61K31/501
CPC分类号： C07D403/14
摘要： The invention relates to heterocyclic derivatives of formula (I), wherein R2 is amino, a group OR4 or a group —Y—R5 where R4 is hydrogen or C1-4alkyl, Y is C1-4alkylene, R5 is hydrogen, halo, hydroxy, C1-2alkoxy, C1-2alkoxyC1-2alkoxyC1-4, or a group NR7R8 where R7 and R8 are independently selected from hydrogen, C1-2alkyl, hydroxyC1-2alkyl or alkoxyC1-2alkyl, or R7 and R8 together with the nitrogen atom to which they are attached form a saturated 5-6-membered heterocyclic ring which optionally contains an additional heteroatom; n is one or two and each R1 is independently selected from halo, haloC1-2alkyl, hydroxy, oxo, amino C1-2alkylamino or di-C1-2dialkylamino; or a pharmaceutically acceptable salt thereof. These 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 heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.
摘要翻译：本发明涉及式（I）的杂环衍生物，其中R 2是氨基，或OR 4或基团-YR 5，其中 R 4是氢或C 1-4烷基，Y是C 1-4亚烷基，R 5是氢，卤素，羟基，C 1-12烷氧基，C 1-2烷氧基C 1-2烷氧基C 1-4，或者其中R 7和R 8独立地选自氢，氢， C 1-12烷基，羟基C 1-12烷基或烷氧基C 1-12烷基，或R 7和/或 R 8与它们所连接的氮原子一起形成饱和的5-6元杂环，其任选地含有另外的杂原子; n是一个或两个，并且每个R 1独立地选自卤素，卤代C 1-2 - 烷基，羟基，氧代，氨基C 1-12 烷基氨基或二-C 1-2二烷基氨基; 或其药学上可接受的盐。这些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。本发明还涉及制备杂环衍生物的方法，含有它们的药物组合物及其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。

2. 发明申请

US20090111822A1 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：US20090111822A1
公开(公告)日：2009-04-30
申请号：US12258161
申请日：2008-10-24
申请人： Emma BRATT , Kenneth Granberg
发明人： Emma BRATT , Kenneth Granberg
IPC分类号： A61K31/501 , C07D249/08 , C07D403/14 , A61K31/497 , A61P1/04 , A61P25/22 , C07D401/14 , A61K31/4196
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。

3. 发明申请

US20090111824A1 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：US20090111824A1
公开(公告)日：2009-04-30
申请号：US12258169
申请日：2008-10-24
申请人： Emma Bratt , Kenneth Granberg , Methvin Isaac , Mats Nagard , Abdelmalik Slassi
发明人： Emma Bratt , Kenneth Granberg , Methvin Isaac , Mats Nagard , Abdelmalik Slassi
IPC分类号： A61K31/501 , C07D403/14 , C07D413/14 , C07D403/04 , A61K31/4439
CPC分类号： C07D403/14 , C07D403/04 , C07D413/14
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。

4. 发明授权

US07419979B2 Derivatives of 6-{4-[4-(1H-indole-2-sulphonyl)-piperazin-1-carbonyl-phenyl]}pyradizin-3-one 失效
标题翻译： 6- {4- [4-（1H-吲哚-2-磺酰基） - 哌嗪-1-羰基 - 苯基]}嘧啶并三酮的衍生物
公开(公告)号：US07419979B2
公开(公告)日：2008-09-02
申请号：US10584473
申请日：2005-01-05
申请人： Emma Bratt , Yantao Chen , Kenneth Granberg , Ingemar Nilsson
发明人： Emma Bratt , Yantao Chen , Kenneth Granberg , Ingemar Nilsson
IPC分类号： C07D403/12 , C07D403/14 , A61K31/501 , A61P7/02
CPC分类号： C07D403/14
摘要： The invention relates to heterocyclic derivatives of formula (I), wherein R2 is amino, a group OR4 or a group —Y—R5 where R4 is hydrogen or C1-4alkyl, Y is C1-4alkylene, R5 is hydrogen, halo, hydroxy, C1-2alkoxy, C1-2alkoxyC1-2alkoxyC1-4, or a group NR7R8 where R7 and R8 are independently selected from hydrogen, C1-2alkyl, hydroxyC1-2alkyl or alkoxyC1-2alkyl, or R7 and R8 together with the nitrogen atom to which they are attached form a saturated 5-6-membered heterocyclic ring which optionally contains an additional heteroatom; n is one or two and each R1 is independently selected from halo, haloC1-2alkyl, hydroxy, oxo, amino, C1-2alkylamino or di-C1-2dialkylamino; or a pharmaceutically acceptable salt thereof. These 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 heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.
摘要翻译：本发明涉及式（I）的杂环衍生物，其中R 2是氨基，或OR 4或基团-YR 5，其中 R 4是氢或C 1-4烷基，Y是C 1-4亚烷基，R 5是氢，卤素，羟基，C 1-12烷氧基，C 1-2烷氧基C 1-2烷氧基C 1-4，或者其中R 7和R 8独立地选自氢，氢， C 1-12烷基，羟基C 1-12烷基或烷氧基C 1-12烷基，或R 7和/或 R 8与它们所连接的氮原子一起形成饱和的5-6元杂环，其任选地含有另外的杂原子; n是一个或两个，并且每个R 1独立地选自卤素，卤代C 1-2 - 烷基，羟基，氧代，氨基，C 1-2 - 烷基氨基或二-C 1-2二烷基氨基; 或其药学上可接受的盐。这些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。本发明还涉及制备杂环衍生物的方法，含有它们的药物组合物及其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。

5. 发明申请

US20120142659A1 COMPOUNDS AND THEIR USE AS IKACH BLOCKERS 失效
标题翻译：化合物及其作为IKACH BLOCKERS使用
公开(公告)号：US20120142659A1
公开(公告)日：2012-06-07
申请号：US13306499
申请日：2011-11-29
申请人： Jonas Bostrõm , Hans Emtenäs , Kenneth Granberg , Mickael Mogemark , Antonio Llinas
发明人： Jonas Bostrõm , Hans Emtenäs , Kenneth Granberg , Mickael Mogemark , Antonio Llinas
IPC分类号： A61K31/397 , C07D207/09 , A61K31/40 , C07D211/46 , A61P9/00 , A61P9/06 , A61P11/00 , A61P9/04 , A61P7/02 , C07D205/04 , A61K31/445
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, R1, R2, R3, R4, R5, 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学有效性，特别是乙酰胆碱的操作内向整流钾通道电流（即IKACh阻断剂）的抑制剂，并且被认为可用于治疗心律失常，特别是室上性心律失常，例如室性心动过速作为心房颤动和心房扑动。

6. 发明申请

US20090111854A1 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：US20090111854A1
公开(公告)日：2009-04-30
申请号：US12258151
申请日：2008-10-24
申请人： Kenneth Granberg , Andreas Wallberg
发明人： Kenneth Granberg , Andreas Wallberg
IPC分类号： A61K31/4545 , C07D257/04 , A61K31/41 , A61K31/4439 , A61P1/00 , A61P25/22 , A61P29/00 , C07D413/14 , C07D401/14 , C07D211/06
CPC分类号： C07D401/14 , C07D401/04 , C07D413/14
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。

7. 发明申请

US20080200431A1 Heterocyclic Sulfonamide Derivatives as Inhibitors of Factor Xa 审中-公开
公开(公告)号：US20080200431A1
公开(公告)日：2008-08-21
申请号：US11994844
申请日：2006-07-05
申请人： Christer Alstermark , Kosrat Amin , Kjell Andersson , Ulf Fahlander , Kenneth Granberg , Daniel Hovdal
发明人： Christer Alstermark , Kosrat Amin , Kjell Andersson , Ulf Fahlander , Kenneth Granberg , Daniel Hovdal
IPC分类号： A61K31/727 , C07D401/14 , A61K31/501 , A61P7/00 , C07D487/04 , A61K31/496
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 R1, R2, R3 and R4 are independently selected from carbon and nitrogen, and where is nitrogen; A1 is a single bond or a double bond; n is 0, 1, 2 or 3; each R5 is independently selected from hydrogen, halogen, C1-3 alkyl, oxo, oxy, oxido and thioxo; R6 is hydrogen or oxo; m is 0, 1, 2 or 3; A2 is a single bond or a double bond; each R7 is independently selected from hydrogen, hydroxy, oxo, C1-5alkyl, carboxy, cyano, tetrazolyl, N—C1-5alkyltetrazolyl, oxazolyl, C1-5oxazolyl, isoxazolyl, C1-5 isoxazolyl, hydroxyC1-5alkyl, carboxy C1-5alkyl, C1-5alkoxyoxo C1-5alkyl, carbamoyl, C1-5alkylcarbamoyl, di(C1-5alkyl)carbamoyl, carbamoyl C1-4alkyl, C1-5alkylcarbamoyl C1-4alkyl, di(C1-5alkyl)carbamoyl C1-4alkyl, hydroxy C1-5alkylcarbamoyl, C1-5alkoxy C1-5alkylcarbamoyl, hydroxy C1-5alkylcarbamoyl C1-4alkyl, C1-5alkoxy C1-5alkylcarbamoyl C1-4alkyl, —CONR8(CH2)xS(O)pR9, —CONH(CH2)qNR10R11, —C1-5alkyl-Y1, —COOCHR17R18 and —CONR17R18; and R30 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.

8. 发明申请

US20090111857A1 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：US20090111857A1
公开(公告)日：2009-04-30
申请号：US12258119
申请日：2008-10-24
申请人： Peter DOVE , Kenneth Granberg , Methvin Isaac , Mats Nagard , Abdelmalik Slassi
发明人： Peter DOVE , Kenneth Granberg , Methvin Isaac , Mats Nagard , Abdelmalik Slassi
IPC分类号： A61K31/4439 , C07D257/04 , A61K31/41 , A61K31/4196 , A61K31/4245 , A61P1/00 , A61P29/00 , A61P25/00 , C07D271/06 , C07D249/08 , C07D401/02
CPC分类号： C07D257/04 , C07D249/12 , C07D261/08 , C07D401/14 , C07D403/12 , C07D413/12
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

US20070259860A1 MGluR5 modulators V 审中-公开
标题翻译： MGluR5调制器
公开(公告)号：US20070259860A1
公开(公告)日：2007-11-08
申请号：US11790429
申请日：2007-04-25
申请人： Andreas Wallberg , Karolina Nilsson , Kenneth Granberg , Saswati Ghosal , Abdelmalik Slassi , Louise Edwards , Methvin Isaac , Tao Xin , Tomislav Stefanac , Peter Dove
发明人： Andreas Wallberg , Karolina Nilsson , Kenneth Granberg , Saswati Ghosal , Abdelmalik Slassi , Louise Edwards , Methvin Isaac , Tao Xin , Tomislav Stefanac , Peter Dove
IPC分类号： A61K31/5513 , A61K31/519 , C07D487/04
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，其在治疗中的应用和包含新化合物的药物组合物。

10. 发明授权

US07678796B2 MGluR5 modulators I 失效
标题翻译： MGluR5调制器
公开(公告)号：US07678796B2
公开(公告)日：2010-03-16
申请号：US11790417
申请日：2007-04-25
申请人： Andreas Wallberg , Karolina Nilsson , Björn Holm , Mats Nagard , Kenneth Granberg , Abdelmalik Slassi , Louise Edwards , Methvin Isaac , Tao Xin , Tomislav Stefanac
发明人： Andreas Wallberg , Karolina Nilsson , Björn Holm , Mats Nagard , Kenneth Granberg , Abdelmalik Slassi , Louise Edwards , Methvin Isaac , Tao Xin , Tomislav Stefanac
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/513 , A61K31/497 , A61K31/496 , A61K31/501 , C07D413/02 , C07D417/14 , A61P1/00
CPC分类号： C07D413/14 , C07D401/14 , C07D403/14
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。

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