公开(公告)号：US10507201B2

公开(公告)日：2019-12-17

申请号：US16289612

申请日：2019-02-28

Applicant: NOVARTIS AG

Inventor： Nicole Buschmann ,  Robin Alec Fairhurst ,  Pascal Furet ,  Diana Graus Porta ,  Carolina Haefliger ,  Bo Han ,  Thomas Knöpfel ,  Catherine Leblanc ,  Lv Liao ,  Robert Mah ,  Masato Murakami ,  Pierre Nimsgern ,  Michael Palmer ,  Dale Porter ,  Sebastien Ripoche ,  Can Wang ,  Youzhen Wang ,  Andreas Weiss ,  Jing Xiong ,  Xianglin Zhao

IPC: A61K31/475 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/55 ,  A61P35/00 ,  A61K31/4375

Abstract: The present invention relates to therapeutic uses of compounds of formula (I) or a pharmaceutically acceptable salt thereof

公开(公告)号：US10202371B2

公开(公告)日：2019-02-12

申请号：US15047574

申请日：2016-02-18

Applicant: Novartis AG

Inventor： Robin Alec Fairhurst ,  Pascal Furet ,  Frank Stephen Kalthoff ,  Andreas Lerchner ,  Heinrich Rueeger

IPC: A61K31/5377 ,  A61K45/06 ,  C07D417/14 ,  C07D413/14

Abstract: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.

公开(公告)号：US09751876B2

公开(公告)日：2017-09-05

申请号：US14511044

申请日：2014-10-09

Applicant: Novartis AG

Inventor： Ian Bruce ,  Sylvie Chamoin ,  Stephen Paul Collingwood ,  Pascal Furet ,  Vikki Furminger ,  Diana Janus ,  Sarah Lewis ,  Jon Christopher Loren ,  Valentina Molteni ,  Alex Michael Saunders ,  Duncan Shaw ,  Lilya Sviridenko ,  Christopher Thomson ,  Ryan West ,  Vince Yeh

IPC: C07D471/04 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/4745

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.

公开(公告)号：US09556180B2

公开(公告)日：2017-01-31

申请号：US14762051

申请日：2014-01-21

Applicant: Novartis AG

Inventor： Pascal Furet ,  Vito Guagnano ,  Philipp Holzer ,  Joerg Kallen ,  Robert Mah ,  Keiichi Masuya ,  Achim Schlapbach ,  Andrea Vaupel

IPC: C07D487/04 ,  A61K31/519

CPC classification number: C07D487/04 ,  A61K31/519

Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.

Abstract translation: 本发明涉及式（I）化合物：如本文所述，包含这些化合物的药物制剂，用于治疗由MDM2和/或MDM4的活性介导的疾病或疾病的这些化合物的用途和方法，以及 包含这些化合物的组合。

公开(公告)号：US20190382399A1

公开(公告)日：2019-12-19

申请号：US16224212

申请日：2018-12-18

Applicant: Novartis AG

Inventor： Robin Alec Fairhurst ,  Pascal Furet ,  Frank Stephen Kalthoff ,  Andreas Lerchner ,  Heinrich Rueeger

IPC: C07D417/14 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/14

Abstract: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.

公开(公告)号：US20190105309A1

公开(公告)日：2019-04-11

申请号：US16211139

申请日：2018-12-05

Applicant: Novartis AG

Inventor： Nicole Buschmann ,  Robin Alec Fairhurst ,  Pascal Furet ,  Thomas Knoepfel ,  Catherine Leblanc ,  Robert Mah

IPC: A61K31/444 ,  A61K31/497 ,  A61P35/00

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

公开(公告)号：US09949979B2

公开(公告)日：2018-04-24

申请号：US14365512

申请日：2012-12-14

Applicant: NOVARTIS AG

Inventor： Nigel Graham Cooke ,  Paulo Antonio Fernandes Gomes Dos Santos ,  Pascal Furet ,  Christina Hebach ,  Klemens Hoegenauer ,  Gregory Hollingworth ,  Christoph Kalis ,  Ian Lewis ,  Alexander Baxter Smith ,  Nicolas Soldermann ,  Frederic Stauffer ,  Ross Strang ,  Frank Stowasser ,  Nicola Tuffilli ,  Anette Von Matt ,  Romain Wolf ,  Frederic Zecri

IPC: A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/517 ,  A61K31/551 ,  C07D401/14 ,  C07D413/14 ,  C07D401/04 ,  C07D403/04 ,  C07D239/74 ,  C07D487/08

CPC classification number: A61K31/519 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  C07D239/74 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D413/14 ,  C07D487/08 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/414

Abstract: The invention relates to new uses of PI3K inhibitors, wherein said inhibitors have an inhibitory action on the PI3K isoform delta for the treatment of immunopathology in a subject suffering from a disease or disorder selected from malaria, leishmaniasis, trypanosomiasis, toxoplasmosis and/or neurocysticercosis, via functional inhibition of TLR9 of the infected subject.

公开(公告)号：US10786492B2

公开(公告)日：2020-09-29

申请号：US16211139

申请日：2018-12-05

Applicant: Novartis AG

Inventor： Nicole Buschmann ,  Robin Alec Fairhurst ,  Pascal Furet ,  Thomas Knoepfel ,  Catherine Leblanc ,  Robert Mah

IPC: C07D401/12 ,  C07D401/14 ,  A61K31/444 ,  A61K31/4427 ,  C07D213/75 ,  C07D405/14 ,  A61P35/00 ,  A61K31/497

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

公开(公告)号：US10130629B2

公开(公告)日：2018-11-20

申请号：US15561209

申请日：2016-03-23

Applicant: Novartis AG

Inventor： Nicole Buschmann ,  Robin Alec Fairhurst ,  Jorge Garcia Fortanet ,  Pascal Furet ,  Diana Graus Porta ,  Nafeeza Hafeez ,  Bo Han ,  Thomas Knoepfel ,  Matthew J. LaMarche ,  Catherine Leblanc ,  Lv Liao ,  Robert Mah ,  Dale Porter ,  Can Wang ,  Markus Wartmann ,  Jing Xiong ,  Xianglin Zhao

IPC: A61K31/496 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377

Abstract: A pharmaceutical combination comprising 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, or a pharmaceutically acceptable salt thereof, and at least one active ingredient, as defined herein, or a pharmaceutically acceptable salt thereof, and optionally a pharmaceutically acceptable carrier, for simultaneous or sequential administration; the uses of such combination in the treatment of proliferative diseases; and methods of treating a subject suffering from a proliferative disease comprising administering a therapeutically effective amount of such combination.

公开(公告)号：US20140336166A1

公开(公告)日：2014-11-13

申请号：US14353950

申请日：2012-10-26

Applicant: NOVARTIS AG

Inventor： Emmanuelle Briard ,  Pascal Furet ,  Andreas Lerchner ,  Peter Meier ,  Branko Radetich ,  David Andrew Sandham ,  Yanyi Zhu

IPC: C07D473/16 ,  C07D491/048 ,  C07D491/107 ,  A61K31/5377 ,  A61K31/553

CPC classification number: C07D473/16 ,  A61K31/5377 ,  A61K31/553 ,  C07D487/04 ,  C07D491/048 ,  C07D491/107 ,  C07D519/00

Abstract: The invention relates to PI3K inhibitors of the formula (I) • in which all of the variables are as defined in the specification, to their preparation, to their medical use, in particular to their use in the treatment of cancer and neurodegenerative disorders, and to medicaments comprising them.

Abstract translation: 本发明涉及式（I）的PI3K抑制剂，其中所有变量如说明书中所定义，其制备，其医疗用途，特别是其在治疗癌症和神经变性疾病中的用途，以及 包括它们的药物。