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.

公开(公告)号：USRE45173E1

公开(公告)日：2014-09-30

申请号：US13929901

申请日：2013-06-28

Applicant: Novartis AG

Inventor： Mark Gary Bock ,  Christoph Gaul ,  Venkateshwar Rao Gunmadi ,  Saumitra Sengupta

IPC: A61K31/415 ,  C07D233/00

CPC classification number: A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

Abstract: The present invention provides compounds of Formula (I) and (II), or a pharmaceutically acceptable salts thereof, where R53, R54, p, q, and n are as defined herein. The compounds of the present invention have been found to be useful as 17α-hydroxylase/C17,20-lyase inhibitors.

Abstract translation: 本发明提供式（I）和（II）化合物或其药学上可接受的盐，其中R53，R54，p，q和n如本文所定义。 已经发现本发明的化合物可用作17α-羟化酶/ C17,20-裂解酶抑制剂。