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：US20220267318A1

公开(公告)日：2022-08-25

申请号：US17399090

申请日：2021-08-11

Applicant: Novartis AG

Inventor： Nigel Graham Cooke ,  Paulo Fernandes Gomes Dos Santos ,  Nadege Graveleau ,  Christina Hebach ,  Klemens Hoegenauer ,  Gregory John Hollingworth ,  Alexander Baxter Smith ,  Nicolas Soldermann ,  Frank Stowasser ,  Ross Sinclair Strang ,  Nicola Tufilli ,  Anette von Matt ,  Romain Wolf ,  Frederic Zecri

IPC: C07D471/04 ,  A61P35/00 ,  A61K31/519 ,  A61K31/5377

Abstract: The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.

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.

公开(公告)号：US20190218217A1

公开(公告)日：2019-07-18

申请号：US16367525

申请日：2019-03-28

Applicant: Novartis AG

Inventor： Nigel Graham Cooke ,  Paulo Fernandes Gomes Dos Santos ,  Nadege Graveleau ,  Christina Hebach ,  Klemens Hoegenauer ,  Gregory John Hollingworth ,  Alexander Baxter Smith ,  Nicolas Soldermann ,  Frank Stowasser ,  Ross Sinclair Strang ,  Nicola Tufilli ,  Anette von Matt ,  Romain Wolf ,  Frederic Zecri

IPC: C07D471/04 ,  A61K31/519 ,  A61K31/5377

CPC classification number: C07D471/04 ,  A61K31/519 ,  A61K31/5377 ,  C07B2200/05

Abstract: The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.

公开(公告)号：US20190040061A1

公开(公告)日：2019-02-07

申请号：US16163106

申请日：2018-10-17

Applicant: Novartis AG

Inventor： Nigel Graham Cooke ,  Paulo Fernandes Gomes Dos Santos ,  Nadege Graveleau ,  Christina Hebach ,  Klemens Hoegenauer ,  Gregory John Hollingworth ,  Alexander Baxter Smith ,  Nicolas Soldermann ,  Frank Stowasser ,  Ross Sinclair Strang ,  Nicola Tufilli ,  Anette von Matt ,  Romain Wolf ,  Frederic Zecri

IPC: C07D471/04 ,  A61K31/5377 ,  A61K31/519

Abstract: The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.

公开(公告)号：US20180265509A1

公开(公告)日：2018-09-20

申请号：US15993051

申请日：2018-05-30

Applicant: Novartis AG

Inventor： Nigel Graham Cooke ,  Paulo Fernandes Gomes Dos Santos ,  Nadege Graveleau ,  Christina Hebach ,  Klemens Hoegenauer ,  Gregory John Hollingworth ,  Alexander Baxter Smith ,  Nicolas Soldermann ,  Frank Stowasser ,  Ross Sinclair Strang ,  Nicola Tufilli ,  Anette von Matt ,  Romain Wolf ,  Frederic Zecri

IPC: C07D471/04 ,  A61K31/5377 ,  A61K31/519

CPC classification number: C07D471/04 ,  A61K31/519 ,  A61K31/5377 ,  C07B2200/05

Abstract: The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.

公开(公告)号：US20250059181A1

公开(公告)日：2025-02-20

申请号：US18504244

申请日：2023-11-08

Applicant: Novartis AG

Inventor： Nigel Graham Cooke ,  Paulo Fernandes Gomes dos Santos ,  Nadege Graveleau ,  Christina Hebach ,  Klemens Högenauer ,  Gregory Hollingworth ,  Alexander Baxter Smith ,  Nicolas Soldermann ,  Frank Stowasser ,  Ross Sinclair Strang ,  Nicola Tufilli ,  Anette Von Matt ,  Romain Wolf ,  Frédéric Zecri

IPC: C07D471/04 ,  A61K31/519 ,  A61K31/5377 ,  A61P35/00

Abstract: The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.

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：US20150011555A1

公开(公告)日：2015-01-08

申请号：US14371593

申请日：2013-01-11

Applicant: NOVARTIS AG

Inventor： Catherine Leblanc ,  Stephen Carl McKeown ,  Anett Perlberg ,  Nicola Tufilli

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: The invention relates to salts of (7-(2,3-di-p-tolyl-7,8-dihydropyrido[2,3-b]pyrazin-5(6H)-yl)heptanoic acid which are useful for treating diseases affected by the activation of the IP receptor, pharmaceutical compositions that contain the salts and processes for preparing the salts are also described.

Abstract translation: 本发明涉及（7-（2,3-二 - 对甲苯基-7,8-二氢吡啶并[2,3-b]吡嗪-5（6H） - 基）庚酸的盐，其可用于治疗受影响的疾病 通过IP受体的激活，还描述了含有盐的药物组合物和用于制备盐的方法。