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1. 发明申请

US20080214495A1 Heterocyclic Sulfonamide Derivatives as Inhibitors of Factor Xa 审中-公开
公开(公告)号：US20080214495A1
公开(公告)日：2008-09-04
申请号：US11994846
申请日：2006-07-05
申请人： Christer Alstermark , Kosrat Amin , Kjell Andersson , Yantao Chen , Ulf Fahlander , Kevin Michael Foote , Kenneth Granberg , Daniel Hovdal
发明人： Christer Alstermark , Kosrat Amin , Kjell Andersson , Yantao Chen , Ulf Fahlander , Kevin Michael Foote , Kenneth Granberg , Daniel Hovdal
IPC分类号： A61K31/501 , C07D401/14 , A61K31/497 , A61K31/496 , A61K31/397 , A61P9/00
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14
摘要： The invention relates to compounds of formula (I), wherein R1 and R3 are independently selected from carbon and nitrogen; R2 is oxo or thioxo; n is 0, 1 or 2; each R10 is independently selected from hydrogen and C1-3alkyl; R4 and R5 are each selected from carbon and nitrogen, wherein at least one of R4 and R5 is nitrogen; R6 is hydrogen or oxo; R7 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 R11 is independently selected from hydrogen, hydroxy, oxo, C1-5alkyl, carboxy, hydroxyC1-5alkyl, carboxyC1-5alkyl, C1-5alkoxy-oxoC1-5alkyl, carbamoyl, C1-5alkylcarbamoyl, di (C1-5 alkyl)carbamoyl, carbamoylC1-4alkyl,C1-5alkylcarbamoylC1-4alkyl, di(C1-5alkyl)carbamoylC1-4alkyl, hydroxyC1-5alkylcarbamoyl, C1-5 alkoxyC1-5alkylcarbamoyl, hydroxyC1-5alkylcarbamoylC1-4alkyl, C1-5alkoxyC1-5 alkylcarbamoylC1-4 alkyl, CONR80(CH2)xS(O)pR90, CONH(CH2)qNR100R100, —C1-5 alkyl-Y1, —COOCHR170R180 and —CON R170R180; R8 is a bond, C1-4alkylene or C2-6alkenylene; R9 is an aromatic ring system having 0, 1 or 2 hetero atoms; wherein R9 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.

2. 发明申请

US20090181968A1 Novel 3-Bicyclocarbonylaminopyridine-2-Carboxamides or 3-Bicyclocarbonylaminopyrazine-2-Carboxamides 审中-公开
标题翻译：新型3-双环羰基氨基吡啶-2-羧酰胺或3-双羰基氨基吡嗪-2-羧酰胺
公开(公告)号：US20090181968A1
公开(公告)日：2009-07-16
申请号：US12094334
申请日：2006-11-22
申请人： Kosrat Amin , Johan Broddefalk , Yantao Chen , Karolina Nilsson , Claire Milburn , Helene Desfosses , Ziping Liu , Maxime Tremblay , Christopher Walpole , Zhong-yong Wei , Hua Yang
发明人： Kosrat Amin , Johan Broddefalk , Yantao Chen , Karolina Nilsson , Claire Milburn , Helene Desfosses , Ziping Liu , Maxime Tremblay , Christopher Walpole , Zhong-yong Wei , Hua Yang
IPC分类号： A61K31/5377 , C07D401/10 , C07D405/14 , A61K31/4439 , A61K31/497 , C07D413/14 , C07D405/12 , A61K31/4433 , A61K31/496 , C07D401/12 , A61K31/4709 , C07D409/14 , A61K31/4436 , C07D417/12 , A61K31/4375 , C07D413/12 , A61P29/00
CPC分类号： C07D213/82 , C07D213/84 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds of formula (I) [Chemical formula should be inserted here. Please see paper copy] as well as pharmaceutically acceptable salts and pharmaceutical compositions including the compounds are prepared or thereof: wherein, A1, A2, R1, R2, R3, R4, and R5 and n are as defined in the specification. The compounds of formula (I) are useful in therapy.
摘要翻译：本发明涉及式（I）化合物[化学式应在此插入。请参阅纸本]以及药学上可接受的盐和药物组合物，包括化合物的制备或其制备：其中，A1，A2，R1，R2，R3，R4和R5以及n如说明书中所定义。式（I）化合物可用于治疗。

3. 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。

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。

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