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1. 发明申请

WO2007008143A1 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：WO2007008143A1
公开(公告)日：2007-01-18
申请号：PCT/SE2006/000837
申请日：2006-07-05
申请人： ASTRAZENECA AB , ALSTERMARK, Christer , AMIN, Kosrat , ANDERSSON, Kjell , CHEN, Yantao , FAHLANDER, Ulf , FOOTE, Kevin, Michael , GRANBERG, Kenneth , HOVDAL, Daniel
发明人： ALSTERMARK, Christer , AMIN, Kosrat , ANDERSSON, Kjell , CHEN, Yantao , FAHLANDER, Ulf , FOOTE, Kevin, Michael , GRANBERG, Kenneth , HOVDAL, Daniel
IPC分类号： C07D401/14 , A61K31/497 , A61K31/501 , A61P7/02 , C07D401/12 , C07D403/14 , C07D409/14 , C07D413/14
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14
摘要： The invention relates to compounds of formula (I), wherein R 1 and R 3 are independently selected from carbon and nitrogen; R 2 is oxo or thioxo; n is 0, 1 or 2; each R 10 is independently selected from hydrogen and C 1 - 3 alkyl; R 4 and R 5 are each selected from carbon and nitrogen, wherein at least one of R 4 and R 5 is nitrogen; R 6 is hydrogen or oxo; R 7 is an aliphatic, partially saturated or aromatic carbocyclic ring, said carbocyclic ring having 0, 1 or 2 hetero nitrogen; m is 0, 1 or 2; each R 11 is independently selected from hydrogen, hydroxy, oxo, C 1-5 alkyl, carboxy, hydroxyC 1-5 alkyl, carboxyC 1-5 alkyl, C 1-5 alkoxyoxoC 1-5 alkyl, carbamoyl, C 1-5 alkylcarbamoyl, di (C 1-5 alkyl)carbamoyl, carbamoylC 1-4 alkyl,C 1-5 alkylcarbamoylC 1-4 alkyl, di(C 1-5 alkyl)carbamoylC 1-4 alkyl, hydroxyC 1-5 alkylcarbamoyl, C 1-5 alkoxyC 1-5 alkylcarbamoyl, hydroxyC 1-5 alkylcarbamoylC 1-4 alkyl, C 1-5 alkoxyC 1-5 alkylcarbamoylC 1-4 alkyl, CONR 80 (CH 2 ) x S(O) p R90, CONH(CH 2 ) q NR 100 R 100 , -C 1-5 alkyl-Y 1 , -COOCHR 170 R 180 and -CON R 170 R 180 ; R 8 is a bond, C 1-4 alkylene or C 2-6 alkenylene; R 9 is an aromatic ring system having 0, 1 or 2 hetero atoms; wherein R 9 is substituted by 0 or 1 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R 1和R 3独立地选自碳和氮; R 2是氧代或硫代; n为0,1或2; 每个R 10独立地选自氢和C 1 -C 3 - 烷基; R 4和R 5各自选自碳和氮，其中R 4和R 5中的至少一个 >是氮; R 6是氢或氧代; R 7是脂族，部分饱和或芳族碳环，所述碳环具有0,1或2个杂氮; m为0,1或2; 每个R 11独立地选自氢，羟基，氧代，C 1-5烷基，羧基，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 - 烷基，二（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烷氧基C 1-5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 烷基C 1-4烷基氨基甲酰基C 1-4烷基，CONR 80（CH 2）

2. 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

3. 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。

4. 发明申请

WO2000077000A1 NEW BISPIDINE COMPOUNDS USEFUL IN THE TREATMENT OF CARDIAC ARRHYTHMIAS 审中-公开
标题翻译：新的BISPIDINE化合物可用于治疗心脏病
公开(公告)号：WO2000077000A1
公开(公告)日：2000-12-21
申请号：PCT/SE2000/001254
申请日：2000-06-15
申请人： ASTRAZENECA AB , ALSTERMARK, Christer , ANDERSSON, Kjell , BJÖRE, Annika , BJÖRSNE, Magnus , LINDSTEDT ALSTERMARK, Eva-Lotte , NILSSON, Göran , POLLA, Magnus , STRANDLUND, Gert , ÖRTENGREN, Ylva
发明人： ALSTERMARK, Christer , ANDERSSON, Kjell , BJÖRE, Annika , BJÖRSNE, Magnus , LINDSTEDT ALSTERMARK, Eva-Lotte , NILSSON, Göran , POLLA, Magnus , STRANDLUND, Gert , ÖRTENGREN, Ylva
IPC分类号： C07D471/08
CPC分类号： C07D471/08
摘要： There is provided compounds of formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 41 , R 42 , R 43 , R 44 , R 45 , R 46 , A and B have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.
摘要翻译：提供式（I）化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 41， R 42，R 43，R 44，R 45，R 46，A和B具有在说明书中给出的含义，其可用于预防和治疗心律失常，特异性心房和室性心律失常。

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