公开(公告)号：US20210299100A1

公开(公告)日：2021-09-30

申请号：US17201268

申请日：2021-03-15

Applicant: Novartis AG

Inventor： Vincent BORDAS ,  Cara BROCKLEHURST ,  Patrick CHENE ,  Zhongbo FEI ,  Pascal FURET ,  Vito GUAGNANO ,  Patricia IMBACH-WEESE ,  Joerg KALLEN ,  Mickael LE DOUGET ,  Jialiang LI ,  Wei LI ,  Edwige Liliane Jeanne LORTHIOIS ,  Joseph McKENNA ,  Bahaa SALEM ,  Tobias SCHMELZLE ,  Holger SELLNER ,  Nicolas SOLDERMANN ,  Markus VOEGTLE ,  Markus WARTMANN

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

Abstract: The present invention provides a compound of formula (1) 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：US20240382457A1

公开(公告)日：2024-11-21

申请号：US18776928

申请日：2024-07-18

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 ,  A61K31/41 ,  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：US20130165436A1

公开(公告)日：2013-06-27

申请号：US13721805

申请日：2012-12-20

Applicant: Novartis AG

Inventor： Giorgio CARAVATTI ,  Sylvie CHAMOIN ,  Pascal FURET ,  Klemens HOGENAUER ,  Konstanze HURTH ,  Christoph KALIS ,  Karen KAMMERTOENS ,  Ian LEWIS ,  Henrik MOEBITZ ,  Alexander Baxter SMITH ,  Nicolas SOLDERMANN ,  Romain WOLF ,  Frederic ZECRI

IPC: A61K31/538 ,  C07D413/14

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：US20240382600A1

公开(公告)日：2024-11-21

申请号：US18687615

申请日：2022-08-30

Applicant: Novartis AG

Inventor： Emilie CHAPEAU ,  Patrick CHENE ,  Pascal FURET ,  Laurence KIEFFER ,  Rainer MACHAUER ,  Anne PICARD ,  Tobias SCHMELZLE ,  Holger SELLNER ,  Nicolas SOLDERMANN ,  Markus VOEGTLE ,  Markus WARTMANN

IPC: A61K47/54 ,  A61K47/55 ,  C07D405/14 ,  C07D417/12

Abstract: The present disclosure relates to a conjugate comprising a YAP/TAZ-TEAD Protein Protein Interaction Inhibitor (PPII) linked to a Ligase Binder via a linker, or a pharmaceutically acceptable salt thereof, as well as methods of using such conjugates.

公开(公告)号：US20160168131A1

公开(公告)日：2016-06-16

申请号：US14907225

申请日：2014-07-24

Applicant: NOVARTIS AG

Inventor： Zhenxing DU ,  Samuel HINTERMANN ,  Konstanze HURTH ,  Sébastien JACQUIER ,  Hansjoerg LEHMANN ,  Henrik MOEBITZ ,  Nicolas SOLDERMANN ,  Aleksandar STOJANOVIC

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

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.

Abstract translation: 提供式（I）的取代喹唑啉-4-酮化合物和/或其药学上可接受的盐和/或溶剂合物，其中R1，R2，R3，R5，R6和L如说明书中所定义。 这些化合物适用于治疗由I型PI3K激酶的活性介导的病症或疾病。

公开(公告)号：US20150342951A1

公开(公告)日：2015-12-03

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 HOGENAUER ,  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 ,  A61K31/551 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/517

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.

Abstract translation: 本发明涉及PI3K抑制剂的新用途，其中所述抑制剂对PI3K同种型δ具有抑制作用，用于治疗患有选自疟疾，利什曼病，锥虫病，弓形虫病和/或神经囊尾erc病的疾病或病症的受试者的免疫病理学， 通过功能抑制受感染受试者的TLR9。