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：US09539260B2

公开(公告)日：2017-01-10

申请号：US13721805

申请日：2012-12-20

Applicant: Novartis AG

Inventor： Giorgio Caravatti ,  Sylvie Chamoin ,  Pascal Furet ,  Klemens Hogenauer ,  Konstanze Hurth ,  Karen Kammertoens ,  Ian Lewis ,  Henrik Moebitz ,  Alexander Baxter Smith ,  Nicolas Soldermann ,  Romain Wolf ,  Frederic Zecri

IPC: C07D498/04 ,  A61K31/538 ,  A61K31/5383 ,  C07D413/14 ,  C12Q1/25 ,  C12N9/12 ,  C12Q1/68

CPC classification number: A61K31/5383 ,  A61K31/538 ,  C07D413/14 ,  C07D498/04 ,  C12N9/12 ,  C12Q1/25 ,  C12Q1/686 ,  Y02A50/409 ,  Y02A50/411

Abstract: The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, V, W, U, Q, R1, R5, R7 and R30 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.

Abstract translation: 本发明涉及式（I）的二氢 - 苯并恶嗪和二氢 - 吡啶并恶嗪化合物和/或其药学上可接受的盐和/或溶剂合物，其中Y，V，W，U，Q，R 1，R 5，R 7 和R30如说明书中所定义。 这些化合物适用于治疗由PI3K酶的活性介导的病症或疾病。

公开(公告)号：US09840498B2

公开(公告)日：2017-12-12

申请号：US14907225

申请日：2014-07-24

Applicant: NOVARTIS AG ,  Zhenxing Du ,  Samuel Hintermann ,  Konstanze Hurth ,  Sebastien Jacquier ,  Hansjoerg Lehmann ,  Henrik Moebitz ,  Nicolas Soldermann ,  Aleksandar Stojanovic

Inventor： Zhenxing Du ,  Samuel Hintermann ,  Konstanze Hurth ,  Sébastien Jacquier ,  Hansjoerg Lehmann ,  Henrik Moebitz ,  Nicolas Soldermann ,  Aleksandar Stojanovic

IPC: C07D403/14 ,  C07D401/14 ,  C07D417/14 ,  C07D473/16 ,  A61K31/517 ,  A61K31/52

CPC classification number: C07D403/14 ,  A61K31/517 ,  A61K31/52 ,  C07D401/14 ,  C07D417/14 ,  C07D473/16

Abstract: Provided are substituted quinazolin-4-one compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein R1, R2, R3, R5, R6 and L 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 class I PI3K kinases.

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：US12083101B2

公开(公告)日：2024-09-10

申请号：US17201268

申请日：2021-03-15

Applicant: Novartis AG

Inventor： Vincent Bordas ,  Cara Brocklehurst ,  Patrick Chene ,  Pascal Furet ,  Vito Guagnano ,  Patricia Imbach-Weese ,  Joerg Kallen ,  Mickael Le Douget ,  Edwige Liliane Jeanne Lorthiois ,  Joseph McKenna ,  Bahaa Salem ,  Tobias Schmelzle ,  Holger Sellner ,  Nicolas Soldermann ,  Markus Voegtle ,  Markus Wartmann

IPC: A61K31/4155 ,  A61K31/343 ,  A61K31/351 ,  A61K31/357 ,  A61K31/4025 ,  A61K31/403 ,  A61K31/404 ,  A61K31/41 ,  A61K31/426 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/4525 ,  A61K31/506 ,  A61P35/00 ,  C07D307/81 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D407/12 ,  C07D413/04 ,  C07D417/04 ,  C07D491/04

CPC classification number: A61K31/4155 ,  A61K31/343 ,  A61K31/351 ,  A61K31/357 ,  A61K31/4025 ,  A61K31/403 ,  A61K31/41 ,  A61K31/426 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/4525 ,  A61K31/506 ,  A61P35/00 ,  C07D307/81 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D407/12 ,  C07D417/04

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：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：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.