公开(公告)号：US20180057457A1

公开(公告)日：2018-03-01

申请号：US15555103

申请日：2015-03-04

Applicant: Novartis AG

Inventor： Mark Clinton Davis ,  Baoqing Gong ,  Denis Har ,  Tobias Kapferer ,  Xuchun Zheng

IPC: C07D211/28 ,  C07D211/82 ,  C07D239/42

CPC classification number: C07D211/28 ,  C07D211/80 ,  C07D211/82 ,  C07D239/42

Abstract: The present disclosure relates to a method of synthesizing 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine (ceritinib) and/or intermediates thereof, their use as pharmaceuticals and pharmaceutical compositions and the use of intermediates for preparing ceritinib.

公开(公告)号：US10421755B2

公开(公告)日：2019-09-24

申请号：US15712279

申请日：2017-09-22

Applicant: Novartis AG

Inventor： Wolfgang Marterer ,  Mahavir Prashad ,  Edwin Bernard Villhauer ,  Liladhar Murlidhar Waykole ,  James Anthony Vivelo ,  Bertrand Sutter ,  Jean-Claude Bianchi ,  Raeann Wu ,  Denis Har ,  Piotr H. Karpinski ,  Massimo Pignone ,  Doris Stingelin ,  Eckart Buerger

IPC: C07D453/02 ,  A61K9/20 ,  A61K31/194 ,  A61K31/439 ,  C07C55/08 ,  C07C55/10 ,  C07C57/145 ,  C07C57/15 ,  C07C51/41

Abstract: The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments.

公开(公告)号：US20180009801A1

公开(公告)日：2018-01-11

申请号：US15712279

申请日：2017-09-22

Applicant: Novartis AG

Inventor： Wolfgang Marterer ,  Mahavir Prashad ,  Edwin Bernard Villhauer ,  Liladhar Murlidhar Waykole ,  James Anthony Vivelo ,  Bertrand Sutter ,  Jean-Claude Bianchi ,  Raeann Wu ,  Denis Har ,  Piotr H. Karpinski ,  Massimo Pignone ,  Doris Stingelin ,  Eckart Buerger

IPC: C07D453/02 ,  A61K31/439 ,  C07C55/10 ,  C07C57/145 ,  C07C51/41 ,  A61K9/20 ,  C07C57/15 ,  A61K31/194 ,  C07C55/08

Abstract: The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments.

公开(公告)号：US20200039935A1

公开(公告)日：2020-02-06

申请号：US16595860

申请日：2019-10-08

Applicant: Novartis AG

Inventor： Mark Clinton Davis ,  Baoqing Gong ,  Denis Har ,  Tobias Kapferer ,  Xuchun Zheng

IPC: C07D211/28 ,  C07D239/42 ,  C07D211/80 ,  C07D211/82

Abstract: The present disclosure relates to a method of synthesizing 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine (ceritinib) and/or intermediates thereof, their use as pharmaceuticals and pharmaceutical compositions and the use of intermediates for preparing ceritinib.

公开(公告)号：US09802931B2

公开(公告)日：2017-10-31

申请号：US14997207

申请日：2016-01-15

Applicant: Novartis AG

Inventor： Wolfgang Marterer ,  Mahavir Prashad ,  Edwin Bernard Villhauer ,  Liladhar Murlidhar Waykole ,  James Anthony Vivelo ,  Bertrand Sutter ,  Jean-Claude Bianchi ,  Raeann Wu ,  Denis Har ,  Piotr H. Karpinski ,  Massimo Pignone ,  Doris Stingelin ,  Eckart Buerger

IPC: C07C55/08 ,  C07D453/02 ,  A61K9/20 ,  A61K31/194 ,  A61K31/439 ,  C07C55/10 ,  C07C57/145 ,  C07C57/15 ,  C07C51/41

CPC classification number: C07D453/02 ,  A61K9/2054 ,  A61K31/194 ,  A61K31/439 ,  A61K2300/00 ,  C07B2200/07 ,  C07B2200/13 ,  C07C51/412 ,  C07C55/08 ,  C07C55/10 ,  C07C57/145 ,  C07C57/15

Abstract: The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments.

公开(公告)号：US20160145253A1

公开(公告)日：2016-05-26

申请号：US14997207

申请日：2016-01-15

Applicant: Novartis AG

Inventor： Wolfgang Marterer ,  Mahavir Prashad ,  Edwin Bernard Villhauer ,  Liladhar Murlidhar Waykole ,  James Anthony Vivelo ,  Bertrand Sutter ,  Jean-Claude Bianchi ,  Raeann Wu ,  Denis Har ,  Piotr H. Karpinski ,  Massimo Pignone ,  Doris Stingelin ,  Eckart Buerger

IPC: C07D453/02 ,  C07C57/145 ,  C07C55/10 ,  C07C55/08 ,  C07C57/15 ,  C07C51/41

CPC classification number: C07D453/02 ,  A61K9/2054 ,  A61K31/194 ,  A61K31/439 ,  A61K2300/00 ,  C07B2200/07 ,  C07B2200/13 ,  C07C51/412 ,  C07C55/08 ,  C07C55/10 ,  C07C57/145 ,  C07C57/15

Abstract: The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments.

Abstract translation: 本发明涉及（R）-3-（6-（4-甲基苯基） - 吡啶-3-基氧基）-1-氮杂 - 双环[2.2.2]辛烷的盐，其制备方法或其前体， 包含它们的药物组合物以及它们作为药物的用途。