公开(公告)号：US20240197715A1

公开(公告)日：2024-06-20

申请号：US18510836

申请日：2023-11-16

申请人： NOVARTIS AG

发明人： Rita ANDRAOS-REY ,  Sandra BLUM-KALLERT ,  Marta CORTES-CROS ,  Ruben DE KANTER ,  Stephane FERRETTI ,  Isabel Cristina Colaco Farias JACO ,  Jacques HAMON ,  Jürgen Hans-Hermann HINRICHS ,  Laurent LABORDE ,  Henrik MOEBITZ ,  Michele MOSCHETTA ,  Joseph SCHOEPFER ,  Ross Sinclair STRANG

IPC分类号： A61K31/4745 ,  A61K31/4535 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/506 ,  A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/7048 ,  A61K33/243 ,  A61P35/00

CPC分类号： A61K31/4745 ,  A61K31/4535 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/506 ,  A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/7048 ,  A61K33/243 ,  A61P35/00

摘要： The present invention provides a pharmaceutical combination comprising a WRN inhibitor in combination with at least one additional therapeutically active agent. It also provides a method of treating cancer, involving administering to a subject in need thereof the WRN inhibitor in combination with the at least one additional therapeutically active agent. For example, the WRN inhibitor compound, or a pharmaceutically acceptable salt thereof, is of formula (I):




wherein R1, R2, R3, R4, R5, R28, R27, y, R, M, W, L, V, T, Y, J, K and A are as described herein.

公开(公告)号：US20240245694A1

公开(公告)日：2024-07-25

申请号：US18483651

申请日：2023-10-10

申请人： Novartis AG

发明人： Vincent BORDAS ,  Markus FUREGATI ,  Jacques HAMON ,  Jürgen Hans-Hermann HINRICHS ,  Ziyue HONG ,  Fabio LIMA ,  Fatma LIMAM ,  Henrik MOEBITZ ,  Sandro NOCITO ,  Niko SCHMIEDEBERG ,  Joseph SCHOEPFER ,  Ross Sinclair STRANG ,  Frédéric ZECRI ,  Huangchao YU ,  Yong ZHANG ,  Xinkan YANG ,  Sisi ZHANG ,  Wei LI

IPC分类号： A61K31/5377 ,  A61K31/519 ,  C07D487/14 ,  C07D519/00

CPC分类号： A61K31/5377 ,  A61K31/519 ,  C07D487/14 ,  C07D519/00

摘要： The present invention provides a compound, or a pharmaceutically acceptable salt thereof, of formula (I):




wherein R1, R2, R3, x, R4, R5, y, R, M, W, L, V, T, Y, J, K and A are as described herein, therapeutic uses of said compounds, uses of said compounds as research chemicals, a pharmaceutical composition and combinations comprising said compounds, and methods for manufacturing the compounds of the invention.

公开(公告)号：US20170183348A1

公开(公告)日：2017-06-29

申请号：US15460633

申请日：2017-03-16

申请人： NOVARTIS AG

发明人： Mark Gary BOCK ,  Henrik MOEBITZ ,  Sunil Kumar Panigrahi ,  Ramulu PODDUTOORI ,  Susanta SAMAJDAR

IPC分类号： C07D471/04 ,  A61K31/53 ,  A61K31/513 ,  A61K31/497 ,  A61K31/506 ,  A61K31/4745

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/4745 ,  A61K31/497 ,  A61K31/506 ,  A61K31/513 ,  A61K31/53 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.

公开(公告)号：US20130165436A1

公开(公告)日：2013-06-27

申请号：US13721805

申请日：2012-12-20

申请人： Novartis AG

发明人： 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分类号： A61K31/538 ,  C07D413/14

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

摘要： 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.

摘要翻译： 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：US20160168131A1

公开(公告)日：2016-06-16

申请号：US14907225

申请日：2014-07-24

申请人： NOVARTIS AG

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

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

CPC分类号： C07D403/14 ,  A61K31/517 ,  A61K31/52 ,  C07D401/14 ,  C07D417/14 ,  C07D473/16

摘要： 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.

摘要翻译： 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。