公开(公告)号：US20230233551A1

公开(公告)日：2023-07-27

申请号：US17815256

申请日：2022-07-27

申请人： Novartis Pharmaceuticals Corporation

发明人： Thomas GADEK ,  John BURNIER

IPC分类号： A61K31/4725 ,  C07D217/00 ,  C07D217/02 ,  A61K31/198 ,  A61K31/404 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/541 ,  A61P27/02 ,  A61K31/381 ,  A61K45/06 ,  C07D333/38 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  A61K33/00 ,  A61K33/06 ,  C07D217/20 ,  C07D217/06 ,  A61K31/405 ,  A61K31/495 ,  A61K38/07 ,  A61K38/08 ,  A61K38/12 ,  A61K38/17 ,  G01N33/50 ,  G01N33/68 ,  A61K31/197 ,  A61K31/341 ,  A61K31/352 ,  A61K31/472 ,  C07D401/06 ,  A61K31/275 ,  A61K31/40 ,  A61K31/517 ,  C07C279/28 ,  C07C317/50 ,  C07D207/06 ,  C07D217/26 ,  C07D307/52 ,  C07D413/14 ,  A61K9/00 ,  G01N33/566 ,  A61B3/10 ,  A61B3/14

CPC分类号： A61K31/4725 ,  C07D217/00 ,  C07D217/02 ,  A61K31/198 ,  A61K31/404 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/541 ,  A61P27/02 ,  A61K31/381 ,  A61K45/06 ,  C07D333/38 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  A61K33/00 ,  A61K33/06 ,  C07D217/20 ,  C07D217/06 ,  A61K31/405 ,  A61K31/495 ,  A61K38/07 ,  A61K38/08 ,  A61K38/12 ,  A61K38/1703 ,  G01N33/5011 ,  G01N33/5032 ,  G01N33/6872 ,  A61K31/197 ,  A61K31/341 ,  A61K31/352 ,  A61K31/472 ,  C07D401/06 ,  G01N33/5047 ,  A61K31/275 ,  A61K31/40 ,  A61K31/517 ,  C07C279/28 ,  C07C317/50 ,  C07D207/06 ,  C07D217/26 ,  C07D307/52 ,  C07D413/14 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0048 ,  A61K9/0053 ,  G01N33/566 ,  A61B3/101 ,  A61K9/0051 ,  A61B3/145 ,  G01N2333/70525 ,  G01N2500/02 ,  G01N2500/10 ,  G01N2333/705 ,  G01N2333/70546 ,  G01N2500/20 ,  G01N2500/04 ,  G01N2800/16

摘要： The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.

公开(公告)号：US20230331711A1

公开(公告)日：2023-10-19

申请号：US18337565

申请日：2023-06-20

申请人： Novartis Pharmaceuticals Corporation

发明人： John BURNIER ,  Thomas GADEK ,  Frederic NAUD

IPC分类号： C07D405/06 ,  C07D217/26 ,  A61K31/4709 ,  A61P27/04 ,  A61K31/4725 ,  A61K45/06 ,  C07D405/10 ,  A61K9/06 ,  A61K9/08 ,  A61K47/02 ,  A61K47/06 ,  A61K47/10 ,  A61K47/14 ,  A61K47/22 ,  A61K47/38 ,  C07C317/48 ,  C07D217/02 ,  C07D217/04

CPC分类号： C07D405/06 ,  C07D217/26 ,  A61K31/4709 ,  A61P27/04 ,  A61K31/4725 ,  A61K45/06 ,  C07D405/10 ,  A61K9/06 ,  A61K9/08 ,  A61K47/02 ,  A61K47/06 ,  A61K47/10 ,  A61K47/14 ,  A61K47/22 ,  A61K47/38 ,  C07C317/48 ,  C07D217/02 ,  C07D217/04 ,  A61K47/183

摘要： Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention.

公开(公告)号：US20220073500A1

公开(公告)日：2022-03-10

申请号：US17323693

申请日：2021-05-18

申请人： NOVARTIS PHARMACEUTICALS CORPORATION

发明人： John BURNIER ,  Thomas GADEK ,  Frederic NAUD

IPC分类号： C07D405/06 ,  C07D217/26 ,  A61K31/4709 ,  A61K31/4725 ,  A61K45/06 ,  C07D405/10 ,  A61K9/06 ,  A61K9/08 ,  A61K47/02 ,  A61K47/06 ,  A61K47/10 ,  A61K47/14 ,  A61K47/22 ,  A61K47/38 ,  C07C317/48 ,  C07D217/02 ,  C07D217/04

摘要： Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention.