公开(公告)号：WO2016151500A1

公开(公告)日：2016-09-29

申请号：PCT/IB2016/051633

申请日：2016-03-23

Applicant: NOVARTIS AG ,  BUSCHMANN, Nicole ,  FAIRHURST, Robin Alec ,  FURET, Pascal ,  KNOEPFEL, Thomas ,  LEBLANC, Catherine ,  MAH, Robert ,  MALLET, Franck ,  MARTZ, Julie ,  LIAO, Lv ,  XIONG, Jing ,  HAN, Bo ,  WANG, Can ,  ZHAO, Xianglin

Inventor： BUSCHMANN, Nicole ,  FAIRHURST, Robin Alec ,  FURET, Pascal ,  KNOEPFEL, Thomas ,  LEBLANC, Catherine ,  MAH, Robert ,  MALLET, Franck ,  MARTZ, Julie ,  LIAO, Lv ,  XIONG, Jing ,  HAN, Bo ,  WANG, Can ,  ZHAO, Xianglin

IPC: C07D471/04 ,  A61K31/4375 ,  A61P35/00

CPC classification number: C07D401/14 ,  C07B2200/13 ,  C07C51/412 ,  C07C59/265 ,  C07D471/04

Abstract: The present invention relates to particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7- formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide, to a process of making said particles, to pharmaceutical compositions comprising said particles and to method of treating cancers using said pharmaceutical compositions.

Abstract translation: 本发明涉及N-（5-氰基-4 - （（2-甲氧基乙基）氨基）吡啶-2-基）-7-甲酰基-6 - （（4-甲基-2-氧代哌嗪-1-基） ）甲基）-3,4-二氢-1,8-二氮杂萘-1（2H） - 甲酰胺，制备所述颗粒的方法，包含所述颗粒的药物组合物和使用所述药物组合物治疗癌症的方法。

公开(公告)号：WO2013171641A1

公开(公告)日：2013-11-21

申请号：PCT/IB2013/053770

申请日：2013-05-09

Applicant: NOVARTIS AG ,  FURET, Pascal ,  GROTZFELD, Robert Martin ,  JONES, Darryl Brynley ,  MANLEY, Paul ,  MARZINZIK, Andreas ,  MOUSSAOUI, Saliha ,  PELLE, Xavier Francois Andre ,  SALEM, Bahaa ,  SCHOEPFER, Joseph

Inventor： FURET, Pascal ,  GROTZFELD, Robert Martin ,  JONES, Darryl Brynley ,  MANLEY, Paul ,  MARZINZIK, Andreas ,  MOUSSAOUI, Saliha ,  PELLE, Xavier Francois Andre ,  SALEM, Bahaa ,  SCHOEPFER, Joseph

IPC: C07D213/81 ,  C07D213/85 ,  C07D317/60 ,  C07D231/12 ,  C07D233/38 ,  C07D233/54 ,  C07D401/04 ,  C07D239/26 ,  C07D239/30 ,  C07D239/34 ,  C07D407/14 ,  C07D241/12 ,  C07D241/20 ,  C07D277/20 ,  A61K31/505

CPC classification number: C07D239/26 ,  A61K31/36 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/426 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D213/81 ,  C07D213/85 ,  C07D231/12 ,  C07D233/38 ,  C07D233/54 ,  C07D233/56 ,  C07D239/30 ,  C07D239/34 ,  C07D241/12 ,  C07D241/20 ,  C07D277/22 ,  C07D277/30 ,  C07D317/60 ,  C07D333/22 ,  C07D333/38 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D407/14 ,  C07D409/06

Abstract: The present invention relates to compounds of formula I: in which Y, Y 1 , Y 4 , Y 5 , Y 6 , R 1 , R 2 , R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.

Abstract translation: 本发明涉及式I化合物：其中Y，Y 1，Y 4，Y 5，Y 6，R 1，R 2，R 3和R 4在发明概述中定义; 能够抑制BCR-ABL1及其突变体的活性。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌症的方法。

公开(公告)号：WO2013144249A1

公开(公告)日：2013-10-03

申请号：PCT/EP2013/056600

申请日：2013-03-27

Applicant: NOVARTIS AG ,  FURET, Pascal ,  FRITSCH, Christine ,  MAIRA, Sauveur-Michel

Inventor： FURET, Pascal ,  FRITSCH, Christine ,  MAIRA, Sauveur-Michel

IPC: A61K31/4439 ,  A61P35/00 ,  C12Q1/68 ,  G11B20/00 ,  C12N15/11

CPC classification number: A61K31/4439 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/156

Abstract: The invention is directed, in part, to selective cancer treatment regimes based on assaying for the presence or absence of a mutation in a nucleic acid that encodes glutamine at position 859 of the catalytic p110α subunit of PI3K.

Abstract translation: 本发明部分地针对基于在PI3K的催化性p110alpha亚基的位置859编码谷氨酰胺的核酸中存在或不存在突变的选择性癌症治疗方案。

公开(公告)号：WO2013030802A1

公开(公告)日：2013-03-07

申请号：PCT/IB2012/054501

申请日：2012-08-31

Applicant: NOVARTIS AG ,  IRM LLC ,  BRUCE, Ian ,  CHAMOIN, Sylvie ,  COLLINGWOOD, Stephen Paul ,  FURET, Pascal ,  FURMINGER, Vikki ,  LEWIS, Sarah ,  LOREN, Jon Christopher ,  MOLTENI, Valentina ,  SAUNDERS, Alex Michael ,  SHAW, Duncan ,  SVIRIDENKO, Lilya ,  THOMSON, Christopher ,  YEH, Vince ,  JANUS, Diana ,  WEST, Ryan

Inventor： BRUCE, Ian ,  CHAMOIN, Sylvie ,  COLLINGWOOD, Stephen Paul ,  FURET, Pascal ,  FURMINGER, Vikki ,  LEWIS, Sarah ,  LOREN, Jon Christopher ,  MOLTENI, Valentina ,  SAUNDERS, Alex Michael ,  SHAW, Duncan ,  SVIRIDENKO, Lilya ,  THOMSON, Christopher ,  YEH, Vince ,  JANUS, Diana ,  WEST, Ryan

IPC: C07D471/04 ,  A61K31/4162 ,  A61K31/4188 ,  A61P9/12

CPC classification number: C07D471/04 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06

Abstract: Bicyclic heterocyclic derivatives of formula (I) useful in inhibiting PDGF receptor mediated biological activity. Wherein A is and R1, R1a, R2, R3, R4, R5, R6 and X are as defined herein.

Abstract translation: 式（I）的双环杂环衍生物可用于抑制PDGF受体介导的生物活性。 其中A为且R1，R1a，R2，R3，R4，R5，R6和X如本文所定义。

公开(公告)号：WO2012176123A1

公开(公告)日：2012-12-27

申请号：PCT/IB2012/053095

申请日：2012-06-19

Applicant: NOVARTIS AG ,  FURET, Pascal ,  KALLEN, Joerg ,  LORBER, Julien ,  MASUYA, Keiichi

Inventor： FURET, Pascal ,  KALLEN, Joerg ,  LORBER, Julien ,  MASUYA, Keiichi

IPC: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D417/04 ,  C07D471/10 ,  A61K31/4178 ,  A61P35/00

CPC classification number: C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10

Abstract: The invention relates to 3-heterocyclyl indolyl compounds capable of inhibiting the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively, said compounds having the formula (I), in which: R 1 , R 2 , R 3 and R 4 are as defined in the Summary of the Invention. Due to their activity, the compounds are useful in the treatment of various disorders and diseases mediated by the activity of MDM2 and/or MDM4, or variants thereof, such as inflammatory or proliferative diseases or in the protection of cells.

Abstract translation: 本发明涉及能够分别抑制p53或其变体和MDM2和/或MDM4或其变体之间的相互作用的3-杂环基吲哚基化合物，所述具有式（I）的化合物，其中：R1，R2， R3和R4如发明概述中所定义。 由于它们的活性，所述化合物可用于治疗由MDM2和/或MDM4或其变体如炎性或增殖性疾病或保护细胞的活性介导的各种疾病和疾病。

公开(公告)号：WO2009141386A1

公开(公告)日：2009-11-26

申请号：PCT/EP2009/056154

申请日：2009-05-20

Applicant: NOVARTIS AG ,  FURET, Pascal ,  GRAUS PORTA, Diana ,  GUAGNANO, Vito

Inventor： FURET, Pascal ,  GRAUS PORTA, Diana ,  GUAGNANO, Vito

IPC: C07D215/48 ,  C07D241/44 ,  C07D403/12 ,  C07D403/14 ,  A61K31/4709 ,  A61K31/498 ,  A61P35/00

CPC classification number: A61K31/4709 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  C07D215/06 ,  C07D215/48 ,  C07D241/42 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14

Abstract: The invention relates to compounds of Formula (I), wherein the substituens are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.

Abstract translation: 本发明涉及式（I）化合物，其中取代基如说明书中所定义，为游离形式或其药学上可接受的盐，溶剂化物，酯，N-氧化物的形式; 制备方法; 涉及含有这些化合物的药物，特别是用于一种或多种蛋白质酪氨酸激酶介导的疾病。

公开(公告)号：WO2008138889A3

公开(公告)日：2009-04-30

申请号：PCT/EP2008055751

申请日：2008-05-09

Applicant: NOVARTIS AG ,  CAPRARO HANS-GEORG ,  CARAVATTI GIORGIO ,  FURET PASCAL ,  IMBACH PATRICIA ,  LAN JIONG ,  PECCHI SABINA ,  SCHOEPFER JOSEPH

Inventor： CAPRARO HANS-GEORG ,  CARAVATTI GIORGIO ,  FURET PASCAL ,  IMBACH PATRICIA ,  LAN JIONG ,  PECCHI SABINA ,  SCHOEPFER JOSEPH

IPC: A61K31/519 ,  A61K31/5025 ,  A61P11/00 ,  A61P11/06 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates to compounds are of the formula I, processes for the preparation thereof, more generally these compounds for use in the treatment of the human or animal body, in the treatment of an inflammatory or obstructive airway disease, disorders commonly occurring in connection with transplantation, or a proliferative disease, which disease responds to an inhibition of kinases of the PI3-kinase-related protein kinase family.

Abstract translation: 本发明涉及式I化合物，其制备方法，更一般地，这些用于治疗人或动物体的化合物，用于治疗炎性或阻塞性气道疾病，通常在连接中发生的疾病 移植或增殖性疾病，该疾病对PI3激酶相关蛋白激酶家族的激酶的抑制作出反应。

公开(公告)号：WO2008138889A2

公开(公告)日：2008-11-20

申请号：PCT/EP2008/055751

申请日：2008-05-09

Applicant: NOVARTIS AG ,  CAPRARO, Hans-Georg ,  CARAVATTI, Giorgio ,  FURET, Pascal ,  IMBACH, Patricia ,  LAN, Jiong ,  PECCHI, Sabina ,  SCHOEPFER, Joseph

Inventor： CAPRARO, Hans-Georg ,  CARAVATTI, Giorgio ,  FURET, Pascal ,  IMBACH, Patricia ,  LAN, Jiong ,  PECCHI, Sabina ,  SCHOEPFER, Joseph

IPC: A61K31/5025 ,  A61K31/519 ,  A61P29/00 ,  A61P37/00 ,  A61P35/00 ,  A61P11/00 ,  A61P11/06 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates to compounds are of the formula I, processes for the preparation thereof, more generally these compounds for use in the treatment of the human or animal body, in the treatment of an inflammatory or obstructive airway disease, disorders commonly occurring in connection with transplantation, or a proliferative disease, which disease responds to an inhibition of kinases of the PI3-kinase-related protein kinase family.

Abstract translation: 本发明涉及式I化合物，其制备方法，更一般地，这些用于治疗人或动物体的化合物，用于治疗炎性或阻塞性气道疾病，通常在连接中发生的疾病 移植或增殖性疾病，该疾病对PI3激酶相关蛋白激酶家族的激酶的抑制作出反应。

公开(公告)号：WO2008052974A1

公开(公告)日：2008-05-08

申请号：PCT/EP2007/061636

申请日：2007-10-29

Applicant: NOVARTIS AG ,  HOLZER, Philipp ,  IMBACH, Patricia ,  FURET, Pascal

Inventor： HOLZER, Philipp ,  IMBACH, Patricia ,  FURET, Pascal

IPC: C07D231/38 ,  A61K31/415 ,  A61P35/00

CPC classification number: C07D231/38

Abstract: The invention relates to novel heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.

Abstract translation: 本发明涉及式（I）的新型杂环化合物，其中所有变量如说明书中所定义，以游离形式或盐形式，其制备方法，用作药物和包含它们的药物。

公开(公告)号：WO2008052734A1

公开(公告)日：2008-05-08

申请号：PCT/EP2007/009382

申请日：2007-10-29

Applicant: NOVARTIS AG ,  FERRAND, Sandrine ,  GLICKMAN, Fraser ,  LEBLANC, Catherine ,  RITCHIE, Cathy ,  SHAW, Duncan ,  STIEFL, Nikolaus Johannes ,  FURET, Pascal ,  IMBACH, Patricia ,  STAUFFER, Frédéric ,  CAPRARO, Hans-Georg ,  GESSIER, François ,  GAUL, Christoph ,  ALBAUGH, Pamela A. ,  CHOPIUK, Greg

Inventor： FERRAND, Sandrine ,  GLICKMAN, Fraser ,  LEBLANC, Catherine ,  RITCHIE, Cathy ,  SHAW, Duncan ,  STIEFL, Nikolaus Johannes ,  FURET, Pascal ,  IMBACH, Patricia ,  STAUFFER, Frédéric ,  CAPRARO, Hans-Georg ,  GESSIER, François ,  GAUL, Christoph ,  ALBAUGH, Pamela A. ,  CHOPIUK, Greg

IPC: C07D487/04 ,  A61K31/5025 ,  A61P9/00 ,  A61P19/00 ,  A61P25/00

CPC classification number: C07D487/04

Abstract: A compound of Formula Ia or Ib in free or salt or solvate form, where R 1 , R 2 , R 3 , R 4 , R 5 R 20 , R 24 , R 25 , X, Y and Z have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. These compounds are also useful for treating diseases mediated by the Pi3k receptor, the JAK-2 receptor and the TRK receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Abstract translation: 式Ia或Ib的游离或盐或溶剂化物形式的化合物，其中R 1，R 2，R 3，R 3， 4，R 5，R 20，R 24，R 25，X，Y和Z 具有说明书中所示的含义，可用于治疗由ALK-5和/或ALK-4受体介导的疾病。 这些化合物也可用于治疗由Pi3k受体，JAK-2受体和TRK受体介导的疾病。 还描述了含有化合物的药物组合物和用于制备化合物的方法。