公开(公告)号：US20110046127A1

公开(公告)日：2011-02-24

申请号：US12741765

申请日：2008-11-10

申请人： Paolo Pevarello ,  Ana Maria Garcia Collazo ,  Antonio Rodriguez Hergueta ,  Carl-Gustaf Pierre Saluste ,  Francisco Javier Ramos Lima ,  Esther Gonzalez Cantalapiedra ,  Julen Oyarzabal Santamarina

发明人： Paolo Pevarello ,  Ana Maria Garcia Collazo ,  Antonio Rodriguez Hergueta ,  Carl-Gustaf Pierre Saluste ,  Francisco Javier Ramos Lima ,  Esther Gonzalez Cantalapiedra ,  Julen Oyarzabal Santamarina

IPC分类号： A61K31/5377 ,  C07D487/04 ,  A61K31/5025 ,  C07D413/14 ,  A61P35/00

CPC分类号： C07D487/04

摘要： There is provided compounds of formula (I): wherein Z, M, R1, X, R3, R4 and R5 have meanings given in the description, an pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein kinase (e.g. a PIM family kinase or PI3-K) is desired and/or required, an particularly in the treatment of cancer.

摘要翻译： 提供式（I）化合物：其中Z，M，R 1，X，R 3，R 4和R 5具有在本说明书中给出的含义，其药学上可接受的酯，酰胺，溶剂化物或其盐，该化合物可用于 治疗其中期望和/或需要蛋白激酶（例如PIM家族激酶或PI3-K）的抑制的疾病，特别是治疗癌症。

公开(公告)号：US20130131057A1

公开(公告)日：2013-05-23

申请号：US13697499

申请日：2011-05-13

申请人： Joaquin Pastor Fernández ,  Sonia Martínez Gonzalez ,  Antonlo Rodriguez Hergueta ,  Francisco Javier Ramos Lima ,  Rosa Maria Alvarez Escobar ,  Ana Isabel Higueras Hernandez

发明人： Joaquin Pastor Fernández ,  Sonia Martínez Gonzalez ,  Antonlo Rodriguez Hergueta ,  Francisco Javier Ramos Lima ,  Rosa Maria Alvarez Escobar ,  Ana Isabel Higueras Hernandez

IPC分类号： C07D487/04 ,  A61K45/06 ,  A61K31/5377

CPC分类号： C07D487/04 ,  A61K31/5377 ,  A61K45/06

摘要： There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.

摘要翻译： 提供式（I）化合物，其中A1，A4，A4a，A5，B1，B1a，B2，B2a，B3，B3a，B4，B4a和R3具有说明书中给出的含义，以及药学上可接受的酯，酰胺 ，其溶剂合物或其盐，该化合物可用于治疗其中期望和/或需要蛋白质或脂质激酶（例如PI3-K和/或mTOR）的抑制的疾病，特别是在治疗癌症或 增生性疾病。

公开(公告)号：US09073927B2

公开(公告)日：2015-07-07

申请号：US13574018

申请日：2011-01-24

申请人： Joaquin Pastor Fernández ,  Sonia Martinez Gonzalez ,  Rosa Maria Álvarez Escobar ,  Antonio Rodriguez Hergueta ,  Jose Ignacio Martin Hernando ,  Francisco Javier Ramos Lima

发明人： Joaquin Pastor Fernández ,  Sonia Martinez Gonzalez ,  Rosa Maria Álvarez Escobar ,  Antonio Rodriguez Hergueta ,  Jose Ignacio Martin Hernando ,  Francisco Javier Ramos Lima

IPC分类号： A61K31/5377 ,  C07D413/14 ,  C07D487/04

CPC分类号： C07D487/04 ,  A61K31/5377 ,  C07D413/14

摘要： There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.

摘要翻译： 提供式（I）化合物，其中A1，A4，A4a，A5，B1，B1a，B2，B2a，B3，B3a，B4，B4a和R3具有说明书中给出的含义，以及药学上可接受的酯，酰胺 ，其溶剂合物或其盐，该化合物可用于治疗其中期望和/或需要蛋白质或脂质激酶（例如PI3-K和/或mTOR）的抑制的疾病，特别是在治疗癌症或 增生性疾病。

公开(公告)号：US09682991B2

公开(公告)日：2017-06-20

申请号：US13519872

申请日：2010-12-31

申请人： Joaquín Pastor Fernández ,  Francisco Javier Ramos Lima ,  Ana Isabel Hernandez Higueras ,  Sonia Martínez González ,  Jose Ignacio Martín Hernando ,  Carl-Gustave Pierre Saluste ,  Esther Gonzalez Cantalapiedra ,  Carmen Blanco Aparicio ,  Antonio Rodríguez Hergueta ,  Ana Maria Garcia Collazo ,  Antonio Salgado Serrano ,  Beatriz Noya Marino

发明人： Joaquín Pastor Fernández ,  Francisco Javier Ramos Lima ,  Ana Isabel Hernandez Higueras ,  Sonia Martínez González ,  Jose Ignacio Martín Hernando ,  Carl-Gustave Pierre Saluste ,  Esther Gonzalez Cantalapiedra ,  Carmen Blanco Aparicio ,  Antonio Rodríguez Hergueta ,  Ana Maria Garcia Collazo ,  Antonio Salgado Serrano ,  Beatriz Noya Marino

IPC分类号： C07D491/14 ,  C07D487/14

CPC分类号： C07D491/14 ,  C07D487/14

摘要： There is provided compounds of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description (and which compounds are optionally substituted as indicated in the description), and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease. There is also provided combinations comprising the compounds of formula (I).

公开(公告)号：US20130065881A1

公开(公告)日：2013-03-14

申请号：US13519872

申请日：2010-12-31

申请人： Joaquin Pastor Fernandez ,  Francisco Javier Ramos Lima ,  Ana Isabel Hernandez Higueras ,  Sonia Martinez Gonzalez ,  Jose Ignacio Martin Hernando ,  Carl-Gustave Pierre Saluste ,  Esther Gonzalez Cantalapiedra ,  Carmen Blanco Aparicio ,  Antonio Rodriguez Hergueta ,  Ana Maria Garcia Collazo ,  Antonio Salgado Serrano ,  Beatriz Noya Marino

发明人： Joaquin Pastor Fernandez ,  Francisco Javier Ramos Lima ,  Ana Isabel Hernandez Higueras ,  Sonia Martinez Gonzalez ,  Jose Ignacio Martin Hernando ,  Carl-Gustave Pierre Saluste ,  Esther Gonzalez Cantalapiedra ,  Carmen Blanco Aparicio ,  Antonio Rodriguez Hergueta ,  Ana Maria Garcia Collazo ,  Antonio Salgado Serrano ,  Beatriz Noya Marino

IPC分类号： C07D498/14 ,  C07D487/04 ,  A61K31/5025 ,  C07D519/00 ,  A61K31/55 ,  A61P35/00 ,  A61P9/00 ,  A61P37/02 ,  A61P31/12 ,  A61P29/00 ,  A61P3/00 ,  A61P5/00 ,  A61P25/00 ,  A61P11/00 ,  A61P37/08 ,  A61P17/06 ,  A61P19/08 ,  A61P25/28 ,  A61P9/10 ,  A61P3/10 ,  A61P1/16 ,  A61K31/5383

CPC分类号： C07D491/14 ,  C07D487/14

摘要： There is provided compounds of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description (and which compounds are optionally substituted as indicated in the description), and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease. There is also provided combinations comprising the compounds of formula (I).

摘要翻译： 提供式（I）化合物，其中R 1，R 2，R 3和R 4具有在说明书中给出的含义（和哪些化合物任选地如说明书所示取代）和其药学上可接受的酯，酰胺，溶剂化物或其盐 ，哪些化合物可用于治疗其中期望和/或需要抑制蛋白质或脂质激酶（例如PIM家族激酶，例如PIM-1，PIM-2和/或PIM-3）的疾病，以及 特别是在治疗癌症或增殖性疾病方面。 还提供了包含式（I）化合物的组合。