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1. 发明申请

US20140155421A1 SUBSTITUTED PYRIMIDINYL-PYRROLES ACTIVE AS KINASE INHIBITORS 有权
标题翻译：作为激酶抑制剂的替代吡咯烷基吡啶
公开(公告)号：US20140155421A1
公开(公告)日：2014-06-05
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 , C07F5/02 , C07D405/14 , C07D403/04
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。

2. 发明授权

US08912200B2 Alkynyl substituted pyrimidinyl-pyrroles active as kinases inhibitors 有权
标题翻译：作为激酶抑制剂活化的炔基取代的嘧啶基吡咯
公开(公告)号：US08912200B2
公开(公告)日：2014-12-16
申请号：US14235477
申请日：2012-07-18
申请人： Maria Gabriella Brasca , Jay Aaron Bertrand , Paola Gnocchi , Ilaria Motto , Marcella Nesi , Achille Panzeri , Paola Vianello
发明人： Maria Gabriella Brasca , Jay Aaron Bertrand , Paola Gnocchi , Ilaria Motto , Marcella Nesi , Achille Panzeri , Paola Vianello
IPC分类号： A01N43/54 , C07D239/42 , C07D401/04 , A61K45/06 , A61K31/506 , C07D417/14 , C07D403/04 , C07D405/14 , A61K31/541 , C07D403/14
CPC分类号： A61K31/541 , A61K31/506 , A61K45/06 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/14
摘要： The present invention relates to alkynyl substituted pyrimidinyl-pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak and/or Src family 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炔基取代的嘧啶基 - 吡咯化合物，因此可用于治疗由失调的蛋白激酶活性引起的疾病，特别是Jak和/或Src家族激酶。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。

3. 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。

4. 发明申请

US20140194406A1 ALKYNYL SUBSTITUTED PYRIMIDINYL-PYRROLES ACTIVE AS KINASES INHIBITORS 有权
标题翻译：作为动物抑制剂活化的烷基取代的吡咯烷基吡啶
公开(公告)号：US20140194406A1
公开(公告)日：2014-07-10
申请号：US14235477
申请日：2012-07-18
申请人： Maria Gabriella Brasca , Jay Aaron Bertrand , Paola Gnocchi , Ilaria Motto , Marcella Nesi , Achille Panzeri , Paola Vianello
发明人： Maria Gabriella Brasca , Jay Aaron Bertrand , Paola Gnocchi , Ilaria Motto , Marcella Nesi , Achille Panzeri , Paola Vianello
IPC分类号： A61K31/541 , A61K31/506 , A61K45/06 , C07D405/14 , C07D417/14 , C07D403/04 , C07D403/14
CPC分类号： A61K31/541 , A61K31/506 , A61K45/06 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/14
摘要： The present invention relates to alkynyl substituted pyrimidinyl-pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak and/or Src family 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炔基取代的嘧啶基 - 吡咯化合物，因此可用于治疗由失调的蛋白激酶活性引起的疾病，特别是Jak和/或Src家族激酶。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。

5. 发明授权

US06291509B1 Synergistic immunosuppressant composition containing a 2,2'-bi-1H-pyrrole compound 失效
标题翻译：含有2,2'-双-1H-吡咯化合物的协同免疫抑制剂组合物
公开(公告)号：US06291509B1
公开(公告)日：2001-09-18
申请号：US09068555
申请日：1998-05-19
申请人： Mario Ferrari , Paola Gnocchi , Maria Chiara Fornasiero , Francesco Colotta , Roberto D′Alessio , Anna Maria Isetta
发明人： Mario Ferrari , Paola Gnocchi , Maria Chiara Fornasiero , Francesco Colotta , Roberto D′Alessio , Anna Maria Isetta
IPC分类号： A61K3140
CPC分类号： A61K45/06 , A61K38/13 , A61K31/40 , A61K2300/00
摘要： A product containing: (a) an immunosuppressant agent (A) and (b) at least one immunosuppressant 2,2′-bi-1H-pyrrole compound (B) having formula (I) wherein R1 is hydrogen, phenyl, C1-C20 alkyl or C2-C20 alkenyl, wherein the alkyl and alkenyl groups are unsubstituted or substituted by 1 to 3 substituents, which are the same or different, chosen independently from halogen, C1-C6 alkoxy, hydroxy, aryl and aryloxy; R2 is hydrogen, C1-C6 alkyl, cyano, carboxy or (C1-C6 alkoxy)carbonyl; R3 is halogen, hydroxy or C1-C11 alkoxy unsubstitued or substituted by phenyl; R4 is hydrogen, C1-C6 alkyl or phenyl; each of R5 and R6, which are the same or different, is independently hydrogen, C2-C20 alkanoyl, C3-C20 alkenoyl, phenyl, C1-C20 alkyl or C2-C20 alkenyl; or two of R4, R5 and R6, taken together, form a C4-C12 polymethylene chain, which is unsubstituted or substituted by a C1-C12 alkyl, by a C2-C12 alkenyl or by a C1-C12 alkylidene group; or a pharmaceutically acceptable salt thereof; as a combined preparation for simultaneous, separate or sequential use in immunosuppressant therapy, said preparation having a potentiated immunosuppressive activity with respect to products containing either the immunosuppressive agent (A) or the 2,2′-bi-1H-pyrrole immunosuppressive compound (B).
摘要翻译：一种产品，其包含：（a）免疫抑制剂（A）和（b）至少一种具有式（I）的至少一种免疫抑制剂2,2'-双-1H-吡咯化合物（B），其中R 1是氢，苯基，C 1 -C 20 烷基或C 2 -C 20烯基，其中烷基和烯基是未取代的或被1至3个取代基取代，所述取代基相同或不同，独立地选自卤素，C 1 -C 6烷氧基，羟基，芳基和芳氧基; R2是氢，C1-C6烷基，氰基，羧基或（C1-C6烷氧基）羰基; R3是卤素，羟基或未取代或被苯基取代的C1-C11烷氧基; R4是氢，C1-C6烷基或苯基; R 5和R 6各自相同或不同，独立地为氢，C 2 -C 20烷酰基，C 3 -C 20链烯酰基，苯基，C 1 -C 20烷基或C 2 -C 20烯基; 一起形成C4-C12聚亚甲基链，其未被取代或被C 1 -C 12烷基取代，被C 2 -C 12烯基或C 1 -C 12亚烷基组成; 或其药学上可接受的盐; 作为用于免疫抑制剂治疗的同时，单独或顺序使用的组合制剂，所述制剂对于含有免疫抑制剂（A）或2,2'-双-1H-吡咯免疫抑制化合物（B）的产品具有增强的免疫抑制活性）。

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