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1. 发明申请

US20090326001A1 THIENOPYRIDINE DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：作为代谢性谷氨酸盐受体的调节剂的三烯酰基衍生物
公开(公告)号：US20090326001A1
公开(公告)日：2009-12-31
申请号：US12158554
申请日：2006-12-19
申请人： Katalin Nogradi , Gabor Wagner , Gyorgy Keseru , Janos Koti , Krisztina Gal , Monika Vastag , Attila Bielik , Tamas Gati , Viktor Hada , Amrita Agnes Bobok
发明人： Katalin Nogradi , Gabor Wagner , Gyorgy Keseru , Janos Koti , Krisztina Gal , Monika Vastag , Attila Bielik , Tamas Gati , Viktor Hada , Amrita Agnes Bobok
IPC分类号： A61K31/4365 , C07D495/04 , A61P25/00
CPC分类号： C07D495/04
摘要： The present invention relates to new mGluR1 and niGluR5 receptor subtype preferring ligands of formula (I): wherein X represents a group selected from (CH2)n, CH═CH, NH, N(CH3), NHCH2, N(CH3)CH2, O, OCH2, CH2COO, NHCH2COO; n is an integer of 0 to 2; Y represents a subtituent selected from H, CH3, F, Cl, Br; Z is H or CH3; R is alkyl, cycloalkyl, an optionally substituted phenyl or an optionally substituted heteroaryl, and/or geometric isomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluR1 mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain and neuromuscular dysfunctions of the lower urinary tract.
摘要翻译：本发明涉及优选式（I）配体的新的mGluR1和niGluR5受体亚型：其中X表示选自（CH 2）n，CH-CH，NH，N（CH 3），NHCH 2，N（CH 3） O，OCH 2，CH 2 COO，NHCH 2 COO; n为0〜2的整数， Y表示选自H，CH 3，F，Cl，Br的取代基; Z是H或CH 3; R是烷基，环烷基，任选取代的苯基或任选取代的杂芳基，和/或其几何异构体和/或其盐和/或水合物和/或溶剂化物，其制备方法，包含其的药物组合物和用于治疗和/或预防需要调节mGluR1 mGluR5受体的病理状况，例如神经系统疾病，精神疾病，急性和慢性疼痛以及下泌尿道的神经肌肉功能障碍。

2. 发明申请

US20100022521A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：US20100022521A1
公开(公告)日：2010-01-28
申请号：US12158568
申请日：2006-12-19
申请人： Katalin Nogradi , Gabor Wagner , Gyorgy Keseru , Attila Bielik , Tamas Gati , Viktor Hada , Janos Koti , Krisztina Gal , Monika Vastag , Amrita Agnes Bobok
发明人： Katalin Nogradi , Gabor Wagner , Gyorgy Keseru , Attila Bielik , Tamas Gati , Viktor Hada , Janos Koti , Krisztina Gal , Monika Vastag , Amrita Agnes Bobok
IPC分类号： A61K31/541 , C07D471/04 , C07D279/12 , C07D413/14 , C07D417/14 , A61K31/4365 , A61K31/5377 , A61K31/497 , A61P25/00 , A61P25/04
CPC分类号： C07D495/04
摘要： The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I) wherein X represents a group selected from SO, SO2; Y represents a group selected from (CH2)n, NH, NHCH2; n is an integer of 0 to 1; Z is H or monosubstituted by alkyl, nitro, halogen, alkoxy, trifluoromethyl, cyano, amino, alkylamino, dialkylamino, aminomethyl, e alkylaminomethyl, dialkylaminomethyl, hydroxyl, alkylsulfonylamino; R1 is an optionally substituted alkyl, cycloalkyl, phenyl, biphenyl, heterocyclyl; R2 is an optionally substituted phenyl, heterocyclyl, or NR3R4 group wherein R3 and R4 are independently selected from the group of hydrogen and an optionally substituted alkyl, or R3 and R4 together with the N atom to which they are attached form an optionally substituted C5-7 heterocyclyl group, containing one or more heteroatom(s), or NH—CO—NR5R6 group, wherein R5 and R6 are independently selected from the group of hydrogen and an optionally substituted alkyl, or R5 and R6 together with the N atom to which they are attached form an optionally substituted C5-7 heterocyclyl group, containing one or more heteroatom(s); and/or hydrates and/or solvates and/or pharmaceutically acceptable salts thereof formed with acids or bases, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluR1 and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain, neuromuscular dysfunctions of the lower urinary tract and gastrointestinal disorders.
摘要翻译：本发明涉及新的mGluR1和mGluR5受体亚型优选式（I）的配体，其中X表示选自SO，SO 2的基团; Y表示选自（CH 2）n，NH，NHCH 2; n为0〜1的整数; 卤素，烷氧基，三氟甲基，氰基，氨基，烷基氨基，二烷基氨基，氨基甲基，e烷基氨基甲基，二烷基氨基甲基，羟基，烷基磺酰基氨基; R 1是任选取代的烷基，环烷基，苯基，联苯基，杂环基; R 2是任选取代的苯基，杂环基或NR 3 R 4基团，其中R 3和R 4独立地选自氢和任选取代的烷基，或者R 3和R 4与它们所连接的N原子一起形成任选取代的C 5 - 7杂环基，其含有一个或多个杂原子或NH-CO-NR 5 R 6基团，其中R 5和R 6独立地选自氢和任选取代的烷基，或者R 5和R 6与其中的N原子一起它们连接形成任选取代的含有一个或多个杂原子的C 5-7杂环基; 和/或与酸或碱形成的水合物和/或其溶剂合物和/或其药学上可接受的盐与其制备方法相关的药物组合物及其在治疗和/或预防需要的病理状况中的用途 mGluR1和mGluR5受体的调节，例如神经障碍，精神疾病，急性和慢性疼痛，下尿路神经肌肉功能障碍和胃肠道疾病。

3. 发明申请

US20090149495A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：US20090149495A1
公开(公告)日：2009-06-11
申请号：US12158580
申请日：2006-12-19
申请人： Katalin Nogradi , Gabor Wagner , Gyorgy Keseru , Attila Bielik , Tamas Gati , Viktor Hada , Janos Koti , Krisztina Gal , Monika Vastag , Amrita Agnes Bobok
发明人： Katalin Nogradi , Gabor Wagner , Gyorgy Keseru , Attila Bielik , Tamas Gati , Viktor Hada , Janos Koti , Krisztina Gal , Monika Vastag , Amrita Agnes Bobok
IPC分类号： A61K31/4365 , C07D471/04 , A61P25/00
CPC分类号： C07D495/04
摘要： The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I) wherein X represents a group selected from CO, SO, SO2; Y represents a group selected from 0, OCH2, (CH2)n, NH, NHCH2; n is an integer of 0 to 2; R1 is an optionally substituted alkyl, cycloalkyl, phenyl, biphenyl, heterocyclyl; R2 is an optionally substituted phenyl, heterocyclyl or NR3R4 group wherein R3 and R4 are independently selected from the group of hydrogen, alkyl, or R3 and R4 together with the N atom to which they are attached can form an optionally substituted C5-7 heterocyclyl group, containing one or more heteroatom(s) selected from the group of N, O, S, and/or tautomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluR1 and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain, neuromuscular dysfunctions of the lower urinary tract and gastrointestinal disorders.
摘要翻译：本发明涉及新的mGluR1和mGluR5受体亚型优选式（I）的配体，其中X表示选自CO，SO，SO 2的基团; Y表示选自0，OCH 2，（CH 2）n，NH，NHCH 2的基团; n为0〜2的整数， R 1是任选取代的烷基，环烷基，苯基，联苯基，杂环基; R 2是任选取代的苯基，杂环基或NR 3 R 4基团，其中R 3和R 4独立地选自氢，烷基或R 3和R 4与它们所连接的N原子一起可以形成任选取代的C 5-7杂环基，含有一个或多个选自N，O，S和/或互变异构体和/或其盐和/或其水合物和/或溶剂合物的杂原子，其制备方法涉及含有与治疗和/或预防需要调节mGluR1和mGluR5受体如神经系统疾病，精神疾病，急性和慢性疼痛，下尿路神经肌肉功能障碍和胃肠道疾病的病理状况相同。

4. 发明申请

US20110184014A1 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：US20110184014A1
公开(公告)日：2011-07-28
申请号：US12158589
申请日：2006-12-19
申请人： Katalin Nogradi , Gyorgy Keseru , Attila Bielik , Tamas Gati , Krisztina Gal , Monika Vastag , Amrita Agnes Bobok
发明人： Katalin Nogradi , Gyorgy Keseru , Attila Bielik , Tamas Gati , Krisztina Gal , Monika Vastag , Amrita Agnes Bobok
IPC分类号： A61K31/4365 , C07D495/04 , A61P25/00
CPC分类号： C07D495/04
摘要： The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I); wherein Y represents a substituent selected from hydrogen, methyl, fluoro, chloro, bromo, methoxy; Z is hydrogen or methyl; R is an optionally substituted heteroaryl, and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluR1 and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain and neuromuscular dysfunctions of the lower urinary tract.
摘要翻译：本发明涉及新的mGluR1和mGluR5受体亚型优选式（I）的配体; 其中Y表示选自氢，甲基，氟，氯，溴，甲氧基的取代基; Z是氢或甲基; R是任选取代的杂芳基，和/或其盐和/或其水合物和/或溶剂合物，其制备方法，含有其的药物组合物及其在治疗和/或预防需要的病理状况中的用途 mGluR1和mGluR5受体的调节，如神经系统疾病，精神疾病，急性和慢性疼痛以及下泌尿道的神经肌肉功能障碍。

5. 发明申请

US20090216009A1 PROCESS FOR THE PRODUCTION OF EZETIMIBE AND INTERMEDIATES USED IN THIS PROCESS 有权
标题翻译：在本过程中使用的EZETIMIBE和中间体的生产方法
公开(公告)号：US20090216009A1
公开(公告)日：2009-08-27
申请号：US12097185
申请日：2006-12-18
申请人： Jozsef Bodi , Janos Eles , Katalin Szoke , Krisztina Vukics , Tamas Gati , Krisztina Temesvari , Dorottya Kiss-Bartos
发明人： Jozsef Bodi , Janos Eles , Katalin Szoke , Krisztina Vukics , Tamas Gati , Krisztina Temesvari , Dorottya Kiss-Bartos
IPC分类号： C07D205/08 , C07D413/06 , C07D317/30 , C07D405/06 , C07F7/18
CPC分类号： C07D205/08 , C07D317/30 , C07D405/06 , C07D413/06 , C07F7/1804 , C07F7/1892
摘要： An industrially easily realizable and economical process comprising only few steps, and built on new intermediates for the production of 1-(4-3(R)-[3(S)-(4-fluorophenyl)-3-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone (ezetimibe) according to the reaction scheme described herein.
摘要翻译：工业上容易实现和经济的方法仅包括几个步骤，并建立在生产1-（4-（（R） - [3（S） - （4-氟苯基）-3-羟丙基] -4（ S） - （4-羟基苯基）-2-氮杂环丁酮（依泽替米贝）。

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