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1. 发明授权

US07439258B2 Viral polymerase inhibitors 有权
公开(公告)号：US07439258B2
公开(公告)日：2008-10-21
申请号：US10851710
申请日：2004-05-21
申请人： Pierre Louis Beaulieu , Gulrez Fazal , James Gillard , George Kukolj , Volkhard Austel
发明人： Pierre Louis Beaulieu , Gulrez Fazal , James Gillard , George Kukolj , Volkhard Austel
IPC分类号： A61K31/4439 , C07D401/04
CPC分类号： C07D401/04 , C07D235/18 , C07D403/12 , C07D405/04 , C07D405/14 , C07D409/04 , C07D417/14 , C07D471/04 , Y10S514/894
摘要： A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl, cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-3)alkyl, (C6-10)bicycloalkyl, adamantyl, phenyl, and pyridyl, all of which is optionally substituted with from 1 to 4 substituents; R3 is selected from H, (C1-6)alkyl, (C3-6)cycloalkyl, (C3-6)cycloalkyl(C1-6)alkyl, (C6-10)aryl, (C6-10)aryl(C1-6)alkyl, (C2-6)alkenyl, (C3-6)cycloalkyl(C2-6)alkenyl, (C6-10)aryl(C2-6)alkenyl, N{(C1-6)alkyl}2, NHCOO(C1-6)alkyl(C6-10)aryl, NHCO(C6-10)aryl, (C1-6)alkyl-5- or 10-atom heterocycle, having 1 to 4 heteroatoms selected from O, N and S, and 5- or 10-atom heterocycle having 1 to 4 heteroatoms selected from O, N and S; wherein said alkyl, cycloalkyl, aryl, alkenyl and heterocycle are all optionally substituted with from 1 to 4 substituents; n is zero or 1; or a detectable derivative or salt thereof. The compounds of the invention may be used as inhibitors of hepatitis C virus replication.The invention further provides a method for treating or preventing hepatitis C virus infection.

2. 发明授权

US06448281B1 Viral polymerase inhibitors 有权
公开(公告)号：US06448281B1
公开(公告)日：2002-09-10
申请号：US09898297
申请日：2001-07-03
申请人： Pierre Louis Beaulieu , Gulrez Fazal , James Gillard , George Kukolj , Volkhard Austel
发明人： Pierre Louis Beaulieu , Gulrez Fazal , James Gillard , George Kukolj , Volkhard Austel
IPC分类号： A81K314184
CPC分类号： C07D401/04 , C07D235/18 , C07D403/12 , C07D405/04 , C07D405/14 , C07D409/04 , C07D417/14 , C07D471/04 , Y10S514/894
摘要： A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl, cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-3)alkyl, (C6-10)bicycloalkyl, adamantyl, phenyl, and pyridyl, all of which is optionally substituted with from 1 to 4 substituents; R3 is selected from H, (C1-6)alkyl, (C3-6)cycloalkyl, (C3-6)cycloalkyl(C1-6)alkyl, (C6-10)aryl, (C6-10)aryl(C1-6)alkyl, (C2-6)alkenyl, (C3-6)cycloalkyl(C2-6)alkenyl, (C6-10)aryl(C2-6)alkenyl, N{(C1-6) alkyl}2, NHCOO(C1-6)alkyl(C6-10)aryl, NHCO(C6-10)aryl, (C1-6)alkyl-5- or 10-atom heterocycle, having 1 to 4 heteroatoms selected from O, N and S, and 5- or 10-atom heterocycle having 1 to 4 heteroatoms selected from O, N and S; wherein said alkyl, cycloalkyl, aryl, alkenyl and heterocycle are all optionally substituted with from 1 to 4 substituents; n is zero or 1; or a detectable derivative or salt thereof. The compounds of the invention may be used as inhibitors of hepatitis C virus replication. The invention further provides a method for treating or preventing hepatitis C virus infection.

3. 发明授权

US06794404B2 Viral polymerase inhibitors 有权
公开(公告)号：US06794404B2
公开(公告)日：2004-09-21
申请号：US10238282
申请日：2002-09-10
申请人： Pierre Louis Beaulieu , Gulrez Fazal , James Gillard , George Kukolj , Volkhard Austel
发明人： Pierre Louis Beaulieu , Gulrez Fazal , James Gillard , George Kukolj , Volkhard Austel
IPC分类号： A61K314184
CPC分类号： C07D401/04 , C07D235/18 , C07D403/12 , C07D405/04 , C07D405/14 , C07D409/04 , C07D417/14 , C07D471/04 , Y10S514/894
摘要： A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl, cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-3)alkyl, (C6-10)bicycloalkyl, adamantyl, phenyl, and pyridyl, all of which is optionally substituted with from 1 to 4 substituents; R3 is selected from H, (C1-6)alkyl, (C3-6)cycloalkyl, (C3-6)cycloalkyl(C1-6)alkyl, (C6-10)aryl, (C6-10)aryl(C1-6)alkyl, (C2-6)alkenyl, (C3-6)cycloalkyl(C2-6)alkenyl, (C6-10)aryl(C2-6)alkenyl, N{(C1-6) alkyl}2, NHCOO(C1-6)alkyl(C6-10)aryl, NHCO(C6-10)aryl, (C1-6)alkyl-5- or 10-atom heterocycle, having 1 to 4 heteroatoms selected from O, N and S, and 5- or 10-atom heterocycle having 1 to 4 heteroatoms selected from O, N and S; wherein said alkyl, cycloalkyl, aryl, alkenyl and heterocycle are all optionally substituted with from 1 to 4 substituents; n is zero or 1; or a detectable derivative or salt thereof. The compounds of the invention may be used as inhibitors of hepatitis C virus replication. The invention further provides a method for treating or preventing hepatitis C virus infection.

4. 发明授权

US06479508B1 Viral polymerase inhibitors 有权
公开(公告)号：US06479508B1
公开(公告)日：2002-11-12
申请号：US09995099
申请日：2001-11-27
申请人： Pierre Louis Beaulieu , Gulrez Fazal , James Gillard , George Kukolj , Volkhard Austel
发明人： Pierre Louis Beaulieu , Gulrez Fazal , James Gillard , George Kukolj , Volkhard Austel
IPC分类号： A61K31437
CPC分类号： C07D401/04 , C07D235/18 , C07D403/12 , C07D405/04 , C07D405/14 , C07D409/04 , C07D417/14 , C07D471/04 , Y10S514/894
摘要： A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl , cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-3)alkyl, (C6-10)bicycloalkyl, adamantyl, phenyl, and pyridyl, all of which is optionally substituted with from 1 to 4 substituents; R3 is selected from H, (C1-6)alkyl, (C3-6)cycloalkyl, (C3-6)cycloalkyl(C1-6)alkyl, (C6-10)aryl (C6-10)aryl(C1-6)alkyl, (C2-6)alkenyl, (C3-6)cycloalkyl(C2-6)alkenyl, (C6-10)aryl(C2-6)alkenyl, N{(C1-6) alkyl}2, NHCOO(C1-6)alkyl(C6-10)aryl, NHCO(C6-10)aryl, (C1-6)alkyl-5- or 10-atom heterocycle, having 1 to 4 heteroatoms selected from O, N and S, and 5- or 10-atom heterocycle having 1 to 4 heteroatoms selected from O, N and S; wherein said alkyl, cycloalkyl, aryl, alkenyl and heterocycle are all optionally substituted with from 1 to 4 substituents; n is zero or 1; or a detectable derivative or salt thereof. The compounds of the invention may be used as inhibitors of hepatitis C virus replication. The invention further provides a method for treating or preventing hepatitis C virus infection.

5. 发明授权

US5958952A Substituted phenylamindines, medicaments containing these compounds and process for producing them 失效
标题翻译：取代的苯基亚胺，含有这些化合物的药物及其制备方法
公开(公告)号：US5958952A
公开(公告)日：1999-09-28
申请号：US945611
申请日：1997-12-17
申请人： Frank Himmelsbach , Volkhard Austel , Gunther Linz , Helmut Pieper , Brian Guth , Johannes Weisenberger
发明人： Frank Himmelsbach , Volkhard Austel , Gunther Linz , Helmut Pieper , Brian Guth , Johannes Weisenberger
IPC分类号： C07D295/14 , A61K31/155 , A61K31/215 , A61K31/4427 , A61K31/445 , A61K31/4465 , A61K31/495 , A61P7/02 , A61P9/00 , A61P9/10 , A61P9/12 , C07C257/18 , C07D211/06 , C07D211/34 , C07D211/74 , C07D211/76 , C07D241/08 , C07D295/15 , C07D401/12
CPC分类号： C07D295/15 , C07C257/18 , C07D211/34 , C07C2101/14
摘要： The present invention relates to phenyl amidines of general formula (I), ##STR1## in which R.sup.1 to R.sup.5 are as defined in claim 1, their tautomers, their stereoisomers and their mixtures and their salts, especially their physiologically acceptable salts with inorganic or organic acids or bases also having valuable pharmacological properties, preferably aggregation-limiting effects, producing them.
摘要翻译： PCT No.PCT / EP96 / 01615 Sec。 371 1997年12月17日第 102（e）1997年12月17日PCT PCT 1996年4月18日PCT公布。公开号WO96 / 33970 日期：1996年10月31日本发明涉及通式（I）的苯基脒，其中R 1至R 5如权利要求1所定义，其互变异构体，其立体异构体及其混合物及其盐，特别是其与无机的生理学上可接受的盐或具有有价值的药理学性质的有机酸或碱，优选聚集限制作用，产生它们。

6. 发明授权

US5922763A Biphenyl derivatives, pharmaceutical compositions containing these compounds and processes for preparing them 失效
标题翻译：联苯衍生物，含有这些化合物的药物组合物及其制备方法
公开(公告)号：US5922763A
公开(公告)日：1999-07-13
申请号：US978739
申请日：1997-11-26
申请人： Frank Himmelsbach , Helmut Pieper , Volkhard Austel , Gunter Linz , Thomas Muller , Wolfgang Eisert , Johannes Weisenberger
发明人： Frank Himmelsbach , Helmut Pieper , Volkhard Austel , Gunter Linz , Thomas Muller , Wolfgang Eisert , Johannes Weisenberger
IPC分类号： C07C211/44 , A61K38/00 , C07C211/48 , C07C211/50 , C07C211/53 , C07C233/65 , C07C237/36 , C07C237/38 , C07C243/22 , C07C255/54 , C07C255/56 , C07C255/57 , C07C255/58 , C07C255/59 , C07C255/60 , C07C257/18 , C07C271/64 , C07C275/28 , C07C275/32 , C07C275/38 , C07C275/42 , C07C279/18 , C07C307/10 , C07C309/11 , C07C311/04 , C07C311/06 , C07C311/08 , C07C311/11 , C07C311/16 , C07C311/19 , C07C311/21 , C07C311/29 , C07C317/14 , C07C317/44 , C07C317/46 , C07C321/24 , C07C323/60 , C07C323/62 , C07D207/08 , C07D207/26 , C07D211/34 , C07D211/60 , C07D211/62 , C07D211/70 , C07D257/04 , C07D295/192 , C07F9/40 , C07K5/06 , A61K31/24 , A61K31/19 , C07C229/34 , C07C251/16
CPC分类号： C07D295/192 , C07C237/36 , C07C237/38 , C07C243/22 , C07C255/56 , C07C255/57 , C07C255/59 , C07C255/60 , C07C257/18 , C07C271/64 , C07C275/42 , C07C307/10 , C07C309/11 , C07C311/04 , C07C311/06 , C07C311/08 , C07C311/19 , C07C311/21 , C07C311/29 , C07C317/44 , C07C317/46 , C07C323/60 , C07C323/62 , C07D211/34 , C07D211/60 , C07D211/62 , C07D211/70 , C07K5/06026 , A61K38/00 , C07C2101/14
摘要： The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.
摘要翻译：本发明涉及通式的联苯衍生物，其中A至E和X如权利要求1所定义，其立体异构体包括它们的混合物及其盐，特别是其与无机或有机酸或碱的生理上可接受的盐，其具有有价值的性质，优选聚集抑制作用，含有这些化合物的药物组合物及其制备方法。

7. 发明授权

US5852192A Cyclic urea derivatives, pharmaceutical compositions containing these compounds and processes for preparing them 失效
标题翻译：环状脲衍生物，含有这些化合物的药物组合物及其制备方法
公开(公告)号：US5852192A
公开(公告)日：1998-12-22
申请号：US847048
申请日：1997-05-01
申请人： Frank Himmelsbach , Helmut Pieper , Volkhard Austel , Guenter Linz , Johannes Weisenberger , Wolfgang Eisert , Thomas Mueller
发明人： Frank Himmelsbach , Helmut Pieper , Volkhard Austel , Guenter Linz , Johannes Weisenberger , Wolfgang Eisert , Thomas Mueller
IPC分类号： C07D211/58 , C07D233/36 , C07D235/26 , C07D239/10 , C07D239/36 , C07D249/12 , C07D285/10 , C07D309/12 , C07D401/04 , C07D403/04 , C07D471/04 , C07F9/6506 , C07D233/32
CPC分类号： C07D239/10 , C07D211/58 , C07D233/36 , C07D235/26 , C07D239/36 , C07D249/12 , C07D285/10 , C07D309/12 , C07D401/04 , C07D403/04 , C07D471/04 , C07F9/65061
摘要： The invention relates to cyclic urea derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, X and Y are as defined herein, pharmaceutical compositions containing the derivatives and processes for preparing them.
摘要翻译：本发明涉及通式为（I）的环脲衍生物，其中Ra，Rb，X和Y如本文所定义，含有衍生物的药物组合物及其制备方法。

8. 发明授权

US5817677A 5-membered heterocycles, medicaments containing these compounds, their use and processes for their preparation 失效
标题翻译： 5元杂环，含有这些化合物的药物，其用途及其制备方法
公开(公告)号：US5817677A
公开(公告)日：1998-10-06
申请号：US733898
申请日：1996-10-18
申请人： Gunter Linz , Frank Himmelsbach , Helmut Pieper , Volkhard Austel , Brian Guth , Johannes Weisenberger
发明人： Gunter Linz , Frank Himmelsbach , Helmut Pieper , Volkhard Austel , Brian Guth , Johannes Weisenberger
IPC分类号： C07D277/20 , A61K31/00 , A61K31/4427 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/495 , A61K31/4965 , A61K31/497 , A61P3/00 , A61P3/10 , A61P7/00 , A61P7/02 , A61P9/00 , A61P19/00 , A61P19/08 , A61P29/00 , A61P35/00 , C07D277/50 , C07D285/12 , C07D285/135 , C07D401/04 , C07D401/06 , C07D401/14 , C07D413/04 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , A61K31/455 , A61K31/41
CPC分类号： C07D401/04 , C07D401/06 , C07D417/04
摘要： 5-Membered heterocyclic compounds, of which the following compounds are exemplary: (a) 4-��trans-4-(2-carboxyethyl)cyclohexyl!aminocarbonyl!-1-(4-piperidyl)imidazole, (b) 5-��trans-4-(2-carboxyethyl)cyclohexyl!aminocarbonyl!-4-methyl-2-(4-piperidyl)-1,3-thiazole, (c) 5-��4-(carboxymethoxy)phenyl!aminocarbonyl!-4-methyl-2-(4-piperidyl)-1,3-thiazole, (d) 5-��trans-4-(2-carboxyethyl)cyclohexyl!aminocarbonyl!-2-(4-piperidyl)-1,3,4-thiadiazole, (e) 5-��4-(carboxymethoxy)phenyl!aminocarbonyl!-2-(4-piperidyl)-1,3,4-thiadiazole, (f) 5-��trans-4-(carboxymethoxy)cyclohexyl!aminocarbonyl!-2-(4-piperidyl)-1,3-thiazole, (g) 5-��4-(carboxymethoxy)phenyl!aminocarbonyl!-2-(4-piperidyl)-1,3-thiazole, (h) 5-��trans-4-(2-carboxyethyl)cyclohexyl!aminocarbonyl!-2-(4-piperidyl)-1,3-thiazole, and (i) 4-��trans-4-carboxycyclohexyl!aminocarbonyl!-1-�2-(4-piperidyl)ethyl!imidazole. These are useful for the treatment or prevention of illnesses in which relatively small or relatively large cell aggregates occur or cell-matrix interactions play a part.
摘要翻译： 5-部分杂环化合物，其中以下化合物是示例性的：（a）4 - [[反-4-（2-羧乙基）环己基]氨基羰基] -1-（4-哌啶基）咪唑，（b）5- [ [反-4-（2-羧乙基）环己基]氨基羰基] -4-甲基-2-（4-哌啶基）-1,3-噻唑，（c）5 - [[4-（羧基甲氧基）苯基]氨基羰基] 4-甲基-2-（4-哌啶基）-1,3-噻唑，（d）5 - [[反式-4-（2-羧乙基）环己基]氨基羰基] -2-（4-哌啶基）（e）5 - [[4-（羧甲氧基）苯基]氨基羰基] -2-（4-哌啶基）-1,3,4-噻二唑，（f）5 - [[反式-4- 羧基甲氧基）环己基]氨基羰基] -2-（4-哌啶基）-1,3-噻唑，（g）5 - [[4-（羧基甲氧基）苯基]氨基羰基] -2-（4-哌啶基）噻唑，（h）5 - [[反-4-（2-羧乙基）环己基]氨基羰基] -2-（4-哌啶基）-1,3-噻唑，和（i）4 - [[反-4-羧基环己基 ]氨基羰基] -1- [2-（4-哌啶基）乙基]咪唑。这些可用于治疗或预防其中相对较小或相对较大的细胞聚集物发生或细胞 - 基质相互作用发挥作用的疾病。

9. 发明授权

US5591769A Cyclic imino derivatives and pharmaceutical compositions containing them 失效
标题翻译：环状亚胺衍生物和含有它们的药物组合物
公开(公告)号：US5591769A
公开(公告)日：1997-01-07
申请号：US458096
申请日：1995-06-01
申请人： Frank Himmelsbach , Volkhard Austel , Helmut Pieper , Wolfgang Eisert , Thomas Mueller , Johannes Weisenberger , Guenter Linz , Gerd Krueger
发明人： Frank Himmelsbach , Volkhard Austel , Helmut Pieper , Wolfgang Eisert , Thomas Mueller , Johannes Weisenberger , Guenter Linz , Gerd Krueger
IPC分类号： A61K31/40 , A61K31/00 , A61K31/395 , A61K31/397 , A61K31/401 , A61K31/4015 , A61K31/402 , A61P7/00 , A61P7/02 , A61P9/08 , A61P9/10 , A61P11/00 , A61P35/00 , C07D205/08 , C07D207/00 , C07D207/04 , C07D207/08 , C07D207/12 , C07D207/26 , C07D207/267 , C07D207/27 , C07D207/273 , C07D207/277 , C07D211/76 , C07D223/10 , C07F9/572 , C07D207/02 , C07D207/48
CPC分类号： C07D207/26 , C07D207/273 , C07D207/277 , C07F9/5722
摘要： The invention relates to cyclic imino compounds which have, inter alia, valuable pharmacological properties, especially inhibitory effects on cell aggregation, pharmaceutical compositions which contain these compounds and processes for preparing them.
摘要翻译：本发明涉及具有有价值的药理学性质，特别是对细胞聚集的抑制作用的环状亚氨基化合物，其含有这些化合物的药物组合物及其制备方法。

10. 发明授权

US5442064A Carboxylic acid derivatives, pharmaceutical compositions containing these compounds and processes for preparing them 失效
标题翻译：羧酸衍生物，含有这些化合物的药物组合物及其制备方法
公开(公告)号：US5442064A
公开(公告)日：1995-08-15
申请号：US135041
申请日：1993-10-12
申请人： Helmut Pieper , Gunter Linz , Frank Himmelsbach , Volkhard Austel , Thomas Muller , Johannes Weisenberger , Brian Guth
发明人： Helmut Pieper , Gunter Linz , Frank Himmelsbach , Volkhard Austel , Thomas Muller , Johannes Weisenberger , Brian Guth
IPC分类号： A61K31/445 , A61K31/435 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/451 , A61K31/495 , A61P7/02 , A61P9/00 , A61P9/10 , A61P35/00 , C07D211/34 , C07D211/62 , C07D211/72 , C07D211/76 , C07D213/02 , C07D213/64 , C07D213/75 , C07D213/78 , C07D237/00 , C07D239/00 , C07D295/20 , C07D295/215 , C07D401/02 , C07D401/04 , C07D401/00 , C07D211/06 , C07D211/30 , C07D295/00
CPC分类号： C07D213/78 , C07D213/75 , C07D295/215 , C07C2101/14
摘要： The invention relates to carboxylic acid derivatives of general formulaA--B--C--D--E--F--G (I)whereinA to G are defined as in claim 1, the tautomers thereof, the stereoisomers thereof including the mixtures thereof and the addition salts thereof, particularly the physiologically acceptable salts with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably inhibitory effects on aggregation, and to pharmaceutical compositions containing the compounds and processes for preparing them.
摘要翻译：本发明涉及通式ABCDEFG（I）的羧酸衍生物，其中A至G如权利要求1所定义，其互变异构体，其立体异构体包括其混合物及其加成盐，特别是与无机或具有有价值的药理学性质，优选对聚集的抑制作用的有机酸或碱，以及含有这些化合物的药物组合物及其制备方法。

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