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1. 发明申请

WO2005065688A1 NEW DERIVATIVES OF 6-4{4-[1H-INDOLE-2-SULPHONYL)-PIPERAZIN-1-CARBONYL-PHENYL]}PYRADIZIN-3-ONE 审中-公开
标题翻译： 6-4 {4- [1H-吲哚-2-磺酰基） - 哌嗪-1-基] - 苯基]}的新衍生物}吡咯烷-3-酮
公开(公告)号：WO2005065688A1
公开(公告)日：2005-07-21
申请号：PCT/SE2005/000011
申请日：2005-01-05
申请人： ASTRAZENECA AB , BRATT, Emma , CHEN, Yantao , GRANBERG, Kenneth , NILSSON, Ingemar
发明人： BRATT, Emma , CHEN, Yantao , GRANBERG, Kenneth , NILSSON, Ingemar
IPC分类号： A61K31/501
CPC分类号： C07D403/14
摘要： The invention relates to heterocyclic derivatives of formula (I), wherein R 2 is amino, a group OR 4 or a group -Y-R 5 where R 4 is hydrogen or C 1-4 alkyl, Y is C 1-4 alkylene, R 5 is hydrogen, halo, hydroxy, C 1-2 alkoxy, C 1-2 alkoxyC 1-2 alkoxyC 1-4 , or a group NR 7 R 8 where R 7 and R 8 are independently selected from hydrogen, C 1-2 alkyl, hydroxyC 1-2 alkyl or alkoxyC 1-2 alkyl, or R 7 and R 8 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 R 1 is independently selected from halo, haloC 1-2 alkyl, hydroxy, oxo, amino, C 1-2 alkylamino or di-C 1-2 dialkylamino; 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，OR 4 OR或基团-YR 5，其中R 4是氢或C 1-4烷基，Y是C1- 4亚烷基，R 5是氢，卤素，羟基，C 1-2烷氧基，C 1-2烷氧基C 1-2烷氧基C 1-4或基团NR 7 R 8，其中R 7和R 8独立地选自氢，C 1-2烷基，羟基C 1-2烷基或烷氧基C 1-2烷基，或R 7和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制备抗血栓形成或抗凝血作用的药物中的用途。

2. 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。

3. 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。

4. 发明申请

WO2007008144A1 HETEROCYCLIC SULFONAMIDE DERIVATIVES AS INHIBITORS OF FACTOR XA 审中-公开
标题翻译：作为因子XA的抑制剂的杂环磺酰胺衍生物
公开(公告)号：WO2007008144A1
公开(公告)日：2007-01-18
申请号：PCT/SE2006/000838
申请日：2006-07-05
申请人： ASTRAZENECA AB , BRATT, Emma , GRANBERG, Kenneth
发明人： BRATT, Emma , GRANBERG, Kenneth
IPC分类号： C07D403/14 , A61K31/501 , A61P7/02
CPC分类号： C07D403/14
摘要： The invention relates to compounds of formula (I), Chemical formula should be inserted here. Please see paper copy wherein R 1 is hydrogen, C 1-3 alkyl, R 5 R 6 aminoC 1-5 alkyl, where R 5 and R 6 are each independently selected from hydrogen and C 1-3 alkyl, or R 5 and R 6 may, together with the nitrogen to which they are attached, form a five- or six-membered heterocyclic ring, where said heterocyclic ring has 0 or 1 additional heteroatom; n is 1 or 2; each R 2 are independently selected from hydrogen, oxo and C 1-3 alkyl, R 3 is an indolyl, and R 4 a hydrogen or a 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是氢，C 1-3烷基，R 5，R 6，C 6，C 6，其中R 5和R 6各自独立地选自氢和C 1-3烷基，其中R 5和R 6各自独立地选自氢和C 1-3烷基，或R 5和R 6可以与它们所连接的氮一起形成五元或六元杂环，其中所述杂环为0 或另外1个杂原子; n为1或2; 每个R 2独立地选自氢，氧代和C 1-3烷基，R 3是吲哚基，R 4 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。

5. 发明公开

EP1706120A1 NEW DERIVATIVES OF 6- 4 4 - 1 H - INDOLE-2-SULPHONYL)-PIPERA ZIN-1-CARBONYL-PHENYL PYRADIZIN-3-ONE 审中-公开
标题翻译：使用衍生物6- {4- [4-（1H-吲哚-2-磺酰基）哌嗪-1-羰基] - 苯基} - 吡咯烷-3-酮
公开(公告)号：EP1706120A1
公开(公告)日：2006-10-04
申请号：EP05704685.6
申请日：2005-01-05
申请人： AstraZeneca AB
发明人： BRATT, Emma , CHEN, Yantao , GRANBERG, Kenneth , NILSSON, Ingemar
IPC分类号： A61K31/501 , A61P7/02 , C07D403/12 , C07D403/14
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.

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