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：US10251868B2

公开(公告)日：2019-04-09

申请号：US15876619

申请日：2018-01-22

Applicant: NOVARTIS AG

Inventor： Jun Cao ,  Bernhard Erb ,  Robin Alec Fairhurst ,  Arnaud Grandeury ,  Shinji Hatakeyama ,  Magdalena Koziczak-Holbro ,  Xinzhong Lai ,  Philipp Lustenberger ,  Bernd Ulrich Riebesehl ,  Nicola Tufilli ,  Thomas Ullrich ,  Xiang Wu ,  Jianguang Zhou

IPC: A61K31/428 ,  A61K31/167 ,  C07D277/68 ,  C07C53/10 ,  A61K45/06

Abstract: The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.

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：US12226405B2

公开(公告)日：2025-02-18

申请号：US17241981

申请日：2021-04-27

Applicant: Novartis AG

Inventor： Robin Alec Fairhurst ,  Christine Fritsch ,  Marc Gerspacher ,  Jürgen Hans-Hermann Hinrichs ,  Jean-Baptiste Georges Armand Langlois ,  Catherine Leblanc ,  Tengfei Li ,  Edwige Liliane Jeanne Lorthiois ,  Christophe Mura ,  Cristina Montserrat Nieto-Oberhuber ,  Milen Todorov ,  Andrea Vaupel ,  Nicolas Warin ,  Rainer Wilcken

IPC: A61K31/437 ,  A61K31/155 ,  A61K31/436 ,  A61K31/4375 ,  A61K31/4747 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/635 ,  A61K31/675 ,  A61P35/00 ,  C07D471/10 ,  C07D471/20 ,  C07D491/20 ,  C07D491/22 ,  C07D495/20 ,  C07D495/22

Abstract: The present invention relates to compounds of formula (I) or a pharmaceutically acceptable salt form thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of disease.

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：US11229643B2

公开(公告)日：2022-01-25

申请号：US16347194

申请日：2017-11-01

Applicant: NOVARTIS AG

Inventor： Robin Alec Fairhurst ,  Diana Graus Porta ,  Jacqueline Kinyamu-Akunda ,  Andreas Joerg Mahl ,  Luigi Manenti ,  Andreas Weiss ,  Armin Wolf ,  Kuno Wuersch

IPC: A61K31/496 ,  A61K31/14

Abstract: The present invention relates to a pharmaceutical combination comprising an FGFR4 inhibitor and a bile acid sequestrant, to the use of the pharmaceutical combination in the treatment of cancer, to the use of a bile acid sequestrant to reduce or mitigate side-effects associated with FGFR4 inhibition therapy.

公开(公告)号：US09913828B2

公开(公告)日：2018-03-13

申请号：US15178579

申请日：2016-06-10

Applicant: Novartis AG

Inventor： Jun Cao ,  Bernhard Erb ,  Robin Alec Fairhurst ,  Arnaud Grandeury ,  Shinji Hatakeyama ,  Magdalena Koziczak-Holbro ,  Xinzhong Lai ,  Philipp Lustenberger ,  Bernd Ulrich Riebesehl ,  Nicola Tufilli ,  Thomas Ullrich ,  Xiang Wu ,  Jianguang Zhou

IPC: A61K31/428 ,  C07D277/68 ,  A61K45/06 ,  A61K31/167 ,  C07C53/10

CPC classification number: A61K31/428 ,  A61K31/167 ,  A61K45/06 ,  C07B2200/07 ,  C07C53/10 ,  C07D277/68 ,  Y02P20/55

Abstract: The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.

公开(公告)号：US08865894B2

公开(公告)日：2014-10-21

申请号：US13773947

申请日：2013-02-22

Applicant: Novartis AG

Inventor： Giorgio Caravatti ,  Robin Alec Fairhurst ,  Pascal Furet ,  Frédéric Stauffer ,  Frank Hans Seiler ,  Clive McCarthy ,  Heinrich Rueeger

IPC: C07D401/14 ,  A01N43/54 ,  C07D403/04 ,  C07D413/14 ,  A61K31/5377 ,  A61K45/06

CPC classification number: C07D498/04 ,  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.

Abstract translation: 本发明涉及作为PI3K（磷脂酰肌醇-3-激酶）抑制剂的恶唑烷-2-酮取代的嘧啶化合物及其药物组合物，其制备方法和用于治疗依赖于 PI3K。

公开(公告)号：US09623012B2

公开(公告)日：2017-04-18

申请号：US14770819

申请日：2014-02-26

Applicant: Novartis AG

Inventor： Miloud Achour ,  Robin Alec Fairhurst ,  Arnaud Grandeury ,  Shinji Hatakeyama ,  Magdalena Koziczak-Holbro ,  Nicola Tufilli ,  Thomas Ullrich

IPC: A61K31/428 ,  A61K31/19 ,  A61K9/00 ,  A61K9/20 ,  A61K9/48

CPC classification number: A61K31/428 ,  A61K9/0053 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/485 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/19

Abstract: The present invention relates to a pharmaceutical composition in solid oral dosage form comprising (R)-7-(2-(1-(4-butoxyphenyl)-2-methylpropan-2-ylamino)-1-hydroxyethyl)-5-hydroxybenzo[d]thiazol-2(3H)-one acetate salt.