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31. 发明授权

US09283224B2 Substituted pyrimidinyl-pyrroles active as kinase inhibitors 有权
标题翻译：作为激酶抑制剂活性的取代的嘧啶基吡咯
公开(公告)号：US09283224B2
公开(公告)日：2016-03-15
申请号：US14112559
申请日：2012-04-05
申请人： Maria Gabriella Brasca , Tiziano Bandiera , Jay Aaron Bertrand , Paola Gnocchi , Danilo Mirizzi , Marcella Nesi , Achille Panzeri
发明人： Maria Gabriella Brasca , Tiziano Bandiera , Jay Aaron Bertrand , Paola Gnocchi , Danilo Mirizzi , Marcella Nesi , Achille Panzeri
IPC分类号： A61K31/506 , C07D403/04 , C07D405/14 , C07F5/02
CPC分类号： A61K31/506 , C07D403/04 , C07D405/14 , C07F5/025
摘要： The present invention relates to substituted pyrimidinyl-pyrrole compounds of formula (I) which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Janus kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
摘要翻译：本发明涉及调节蛋白激酶活性的式（I）的取代的嘧啶基 - 吡咯化合物，因此可用于治疗由失调蛋白激酶活性引起的疾病，尤其是Janus激酶。本发明还提供了制备这些化合物的方法，包含这些化合物的药物组合物，以及使用这些化合物治疗疾病的方法或含有它们的药物组合物。

32. 发明授权

US06284896B1 Abeo-ergoline derivatives as 5HT1A ligands 失效
标题翻译：二氢麦角灵衍生物作为5HT1A配体
公开(公告)号：US06284896B1
公开(公告)日：2001-09-04
申请号：US08998867
申请日：1997-12-29
申请人： Sergio Mantegani , Tiziano Bandiera , Enzo Brambilla , Carla Caccia , Nicola Carfagna
发明人： Sergio Mantegani , Tiziano Bandiera , Enzo Brambilla , Carla Caccia , Nicola Carfagna
IPC分类号： C07D48706
CPC分类号： C07D487/06
摘要： There are provided compounds of formula (I), wherein R1 is a hydrogen, chlorine or bromine atom or a methyl, methylthio, hydroxy, cyano or carboxamido group; R2 is C1-C3 alkyl or an alkyl group; R3 and R4 are independently a hydrogen atom, a C1-C5 alkyl group, a C3-C5 alkenyl group, a C5-C6 cycloalkyl C1-C3 alkyl group, a phenyl-C3-C5 alkenyl or phenyl group: which groups are optionally substituted by C1-C3 alkyl, C1-C3 alkoxy, triflouromethyl, hydroxy or amino group; or a group of formula (a), wherein R6 is hydrogen atom or a C1-C3 alkyl group and R7 is a phenyl group, a substituted phenyl group as described above or a heterocyclic ring, R5 is a hydrogen or bromine atom or an organic residue and R is H or an organic residue, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmaceutical compositions comprising them are also provided.
摘要翻译：提供式（I）化合物，其中R 1是氢，氯或溴原子或甲基，甲硫基，羟基，氰基或甲酰氨基; R2是C1-C3烷基或烷基; R3和R4独立地是氢原子，C1-C5烷基，C3-C5烯基，C5-C6环烷基C1-C3烷基，苯基-C3-C5链烯基或苯基：这些基团是任选取代的 C 1 -C 3烷基，C 1 -C 3烷氧基，三氟甲基，羟基或氨基; 或式（a）的基团，其中R6是氢原子或C1-C3烷基，R7是苯基，如上所述的取代苯基或杂环，R5是氢或溴原子或有机残基，R为H或有机残基，或其药学上可接受的盐。还提供了其制备方法和包含它们的药物组合物。

33. 发明授权

US5210194A Process for preparing ergoline derivatives 失效
标题翻译：制备葡萄糖衍生物的方法
公开(公告)号：US5210194A
公开(公告)日：1993-05-11
申请号：US761977
申请日：1991-09-25
申请人： Sergio Mantegani , Gabriella Traquandi , Tiziano Bandiera , Enzo Brambilla
发明人： Sergio Mantegani , Gabriella Traquandi , Tiziano Bandiera , Enzo Brambilla
IPC分类号： C07D457/00 , C07D457/02 , C07D457/12
CPC分类号： C07D457/12 , C07D457/02
摘要： Ergoline derivatives of the formula I: ##STR1## wherein R represents hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.1 represents hydrogen, chlorine, bromine or methyl; either R.sub.2 and R.sub.3 both represent hydrogen or together represent a chemical bond; R.sub.4 represents a C.sub.1 -C.sub.4 hydrocarbon group; each of R.sub.5, R.sub.6, R.sub.8 and R.sub.9 independently represents hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.7 represents hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or C.sub.3 -C.sub.7 cycloalkyl and n is 0, 1 or 2; are prepared by reaction between compounds of the formulae II and III: ##STR2## and subsequent cyclization of the resultant compounds. The compounds of the formula I are known useful anxiolytic, antipsychotic and anti-parkinson agents.
摘要翻译： PCT No.PCT / EP91 / 00104 Sec。 371日期1991年9月25日 102（e）1991年9月25日PCT 1991年1月21日PCT PCT。第WO91 / 11447号公报 1991年8月8日。式I的喹啉衍生物：其中R表示氢或C 1 -C 4烷基; R1代表氢，氯，溴或甲基; R2和R3均表示氢或一起代表化学键; R4代表C1-C4烃基; R5，R6，R8和R9各自独立地表示氢或C1-C4烷基; R 7表示氢，C 1 -C 4烷基，苯基或C 3 -C 7环烷基，n为0,1或2; 通过式II和III的化合物与所得化合物的环化反应制备。式I的化合物是已知的有用的抗焦虑药，抗精神病药和抗帕金森药。

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