公开(公告)号：US20150299120A1

公开(公告)日：2015-10-22

申请号：US14382073

申请日：2013-03-01

Applicant: NOVARTIS AG

Inventor： Mark Gary BOCK ,  Chetan PANDIT ,  Sanjita SASMAL ,  Thomas ULLRICH

IPC: C07D209/54 ,  C07D263/52 ,  A61K31/423 ,  C07D413/06 ,  C07D405/06 ,  C07D401/06 ,  A61K31/4439 ,  C07D491/107 ,  A61K31/4188 ,  A61K31/4184 ,  A61K31/422

CPC classification number: C07D209/54 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/422 ,  A61K31/423 ,  A61K31/4439 ,  C07D233/72 ,  C07D235/02 ,  C07D263/44 ,  C07D263/52 ,  C07D401/06 ,  C07D405/06 ,  C07D413/06 ,  C07D491/107

Abstract: The present invention relates to a compound of formula (I-1) in free form or in pharmaceutically acceptable salt form in which the substituents are as defined in the specification; to its preparation, to its use as a medicament and to medicaments comprising it. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract translation: 本发明涉及游离形式或药学上可接受的盐形式的式（I-1）化合物，其中取代基如说明书中所定义; 用于其制备，用作药物和包含它的药物。 本发明还提供药理活性剂和药物组合物的组合。

公开(公告)号：US20170183348A1

公开(公告)日：2017-06-29

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 ,  A61K31/53 ,  A61K31/513 ,  A61K31/497 ,  A61K31/506 ,  A61K31/4745

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.