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公开(公告)号：US20200087287A1
公开(公告)日：2020-03-19
申请号：US16411598
申请日：2019-05-14
发明人： John BURNIER
IPC分类号： C07D405/06 , C07D405/10
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.
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公开(公告)号：US20150183765A1
公开(公告)日：2015-07-02
申请号：US14556715
申请日：2014-12-01
发明人： John BURNIER
IPC分类号： C07D405/06
CPC分类号： C07D405/06 , C07D405/10
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.
摘要翻译： 公开了已被发现是LFA-1的有效抑制剂的式I化合物的新型结晶多晶型物形式A，B，C，D和E。 本发明还公开了其在治疗LFA-1介导的疾病中的制备方法及其用途。
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公开(公告)号：US20170143691A1
公开(公告)日：2017-05-25
申请号：US15364935
申请日：2016-11-30
发明人： Thomas GADEK , John BURNIER
IPC分类号： A61K31/4725 , A61B3/10 , A61K9/00
CPC分类号： A61K31/4725 , A61B3/101 , A61B3/145 , A61K9/0014 , A61K9/0019 , A61K9/0043 , A61K9/0048 , A61K9/0051 , A61K9/0053 , A61K31/197 , A61K31/198 , A61K31/275 , A61K31/341 , A61K31/352 , A61K31/381 , A61K31/40 , A61K31/404 , A61K31/405 , A61K31/4162 , A61K31/4184 , A61K31/4192 , A61K31/44 , A61K31/4709 , A61K31/472 , A61K31/4745 , A61K31/495 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/54 , A61K31/541 , A61K33/00 , A61K33/06 , A61K38/07 , A61K38/08 , A61K38/12 , A61K38/1703 , A61K45/06 , C07C279/28 , C07C317/50 , C07D207/06 , C07D217/00 , C07D217/02 , C07D217/06 , C07D217/20 , C07D217/26 , C07D307/52 , C07D333/38 , C07D401/06 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , G01N33/5011 , G01N33/5032 , G01N33/5047 , G01N33/566 , G01N33/6872 , G01N2333/705 , G01N2333/70525 , G01N2333/70546 , G01N2500/02 , G01N2500/04 , G01N2500/10 , G01N2500/20 , G01N2800/16 , Y10S514/912 , Y10S514/914
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.
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公开(公告)号：US20170029410A1
公开(公告)日：2017-02-02
申请号：US15144892
申请日：2016-05-03
发明人： John BURNIER
IPC分类号： C07D405/06
CPC分类号： C07D405/06 , C07D405/10
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.
摘要翻译： 公开了已被发现是LFA-1的有效抑制剂的式I化合物的新型结晶多晶型物形式A，B，C，D和E。 本发明还公开了其在治疗LFA-1介导的疾病中的制备方法及其用途。
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公开(公告)号：US20160368902A1
公开(公告)日：2016-12-22
申请号：US15235572
申请日：2016-08-12
发明人： John BURNIER , Thomas GADEK , Frederic NAUD
IPC分类号： C07D405/06 , A61K45/06 , A61K9/06 , A61K9/08 , A61K47/22 , A61K47/10 , A61K47/14 , A61K47/38 , A61K47/06 , A61K47/18 , A61K47/02 , C07D217/04 , C07D217/02 , C07C317/48 , A61K31/4725
CPC分类号： C07D405/06 , A61K9/06 , A61K9/08 , A61K31/4709 , A61K31/4725 , A61K45/06 , A61K47/02 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/183 , A61K47/186 , A61K47/22 , A61K47/38 , C07C317/48 , C07D217/02 , C07D217/04 , C07D217/26 , C07D405/10
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.
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公开(公告)号：US20160220702A1
公开(公告)日：2016-08-04
申请号：US14659789
申请日：2015-03-17
发明人： John BURNIER , Thomas Gadek , Charles Semba
IPC分类号： A61K49/00 , A61K31/4725 , A61K31/472 , A61K31/517 , A61K31/277 , A61F9/00 , A61K39/395 , A61K9/00 , A61K9/06 , A61K9/08 , G01N33/68 , C07K16/28 , A61K45/06
CPC分类号： A61K49/00 , A61F9/0017 , A61K9/0014 , A61K9/0048 , A61K9/06 , A61K9/08 , A61K31/14 , A61K31/198 , A61K31/277 , A61K31/341 , A61K31/343 , A61K31/381 , A61K31/4025 , A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/502 , A61K31/517 , A61K31/66 , A61K39/39533 , A61K45/06 , A61K2039/505 , A61K2039/507 , C07K16/2821 , C07K2317/92 , G01N33/6893 , G01N2333/70503 , G01N2333/70525 , G01N2800/042 , G01N2800/164
摘要： The present invention provides compounds and methods for the treatment of diabetic retinopathy. In particular, LFA-1 antagonists are described herein to be used in the treatment of diabetic retinopathy. One aspect of the invention provides for diagnosis of diabetic retinopathy and administration of a LFA-1 antagonist, after the patient is diagnosed with diabetic retinopathy.
摘要翻译： 本发明提供了治疗糖尿病性视网膜病变的化合物和方法。 特别地，本文描述了LFA-1拮抗剂用于治疗糖尿病性视网膜病变。 在患者被诊断患有糖尿病性视网膜病变之后，本发明的一个方面提供糖尿病性视网膜病变的诊断和LFA-1拮抗剂的施用。
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公开(公告)号：US20130150585A1
公开(公告)日：2013-06-13
申请号：US13713238
申请日：2012-12-13
发明人： John BURNIER
IPC分类号： C07D405/10
CPC分类号： C07D405/06 , C07D405/10
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.
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公开(公告)号：US20130144063A1
公开(公告)日：2013-06-06
申请号：US13710651
申请日：2012-12-11
发明人： John BURNIER , Thomas GADEK , Frederic NAUD
IPC分类号： C07D215/18
CPC分类号： C07D405/06 , A61K9/06 , A61K9/08 , A61K31/4709 , A61K31/4725 , A61K45/06 , A61K47/02 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/183 , A61K47/186 , A61K47/22 , A61K47/38 , C07C317/48 , C07D217/02 , C07D217/04 , C07D217/26 , C07D405/10
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.
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公开(公告)号：US20180251452A1
公开(公告)日：2018-09-06
申请号：US15882543
申请日：2018-01-29
发明人： John BURNIER
IPC分类号： C07D405/06 , C07D405/10
CPC分类号： C07D405/06 , C07D405/10
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.
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公开(公告)号：US20170143693A1
公开(公告)日：2017-05-25
申请号：US15373604
申请日：2016-12-09
发明人： Thomas GADEK , John BURNIER
IPC分类号： A61K31/4725 , G01N33/566 , A61K9/00
CPC分类号： A61K31/4725 , A61B3/101 , A61B3/145 , A61K9/0014 , A61K9/0019 , A61K9/0043 , A61K9/0048 , A61K9/0051 , A61K9/0053 , A61K31/197 , A61K31/198 , A61K31/275 , A61K31/341 , A61K31/352 , A61K31/381 , A61K31/40 , A61K31/404 , A61K31/405 , A61K31/4162 , A61K31/4184 , A61K31/4192 , A61K31/44 , A61K31/4709 , A61K31/472 , A61K31/4745 , A61K31/495 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/54 , A61K31/541 , A61K33/00 , A61K33/06 , A61K38/07 , A61K38/08 , A61K38/12 , A61K38/1703 , A61K45/06 , C07C279/28 , C07C317/50 , C07D207/06 , C07D217/00 , C07D217/02 , C07D217/06 , C07D217/20 , C07D217/26 , C07D307/52 , C07D333/38 , C07D401/06 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , G01N33/5011 , G01N33/5032 , G01N33/5047 , G01N33/566 , G01N33/6872 , G01N2333/705 , G01N2333/70525 , G01N2333/70546 , G01N2500/02 , G01N2500/04 , G01N2500/10 , G01N2500/20 , G01N2800/16 , Y10S514/912 , Y10S514/914
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.
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