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：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：US10011599B2

公开(公告)日：2018-07-03

申请号：US15460633

申请日：2017-03-16

Applicant: NOVARTIS AG

Inventor： Mark Gary Bock ,  Henrik Moebitz ,  Sunil Kumar Panigrahi ,  Ramulu Poddutoori ,  Susanta Samajdar

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

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

Abstract: 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：US09629836B2

公开(公告)日：2017-04-25

申请号：US14940717

申请日：2015-11-13

Applicant: NOVARTIS AG

Inventor： Mark Gary Bock ,  Henrik Moebitz ,  Sunil Kumar Panigrahi ,  Ramulu Poddutoori ,  Susanta Samajdar

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/513 ,  A61K31/53 ,  A61K45/06

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

Abstract: 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.