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公开(公告)号：US09890141B2
公开(公告)日：2018-02-13
申请号：US15144892
申请日：2016-05-03
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：US09708303B2
公开(公告)日：2017-07-18
申请号：US14747745
申请日：2015-06-23
发明人： James Robert Zeller , Sripathy Venkatraman , Elisabeth C. A. Brot , Subashree Iyer , Michael Hall
IPC分类号： C07D405/06 , C07D407/06
CPC分类号： C07D407/06 , C07B2200/13 , C07D405/06
摘要： Methods of preparation and purification of a compound of Formula I, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed.
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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：US09353088B2
公开(公告)日：2016-05-31
申请号：US14556715
申请日：2014-12-01
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：US09216174B2
公开(公告)日：2015-12-22
申请号：US13969968
申请日：2013-08-19
发明人： Wang Shen , Kenneth Barr , Johan D. Oslob , Min Zhong
IPC分类号： C07D215/06 , C07D217/04 , A61K31/472 , C04B35/632 , C07D217/06 , C07D231/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D409/12 , C07D409/14 , C07D217/16 , C07D401/06 , C07D405/14 , A61K31/4725 , A61K45/06 , C07D217/26
CPC分类号： A61K31/4725 , A61K31/472 , A61K31/506 , A61K31/517 , A61K45/06 , C04B35/632 , C07D217/06 , C07D217/16 , C07D217/26 , C07D231/56 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
摘要： The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).
摘要翻译： 本发明提供了具有式（I）的化合物及其药学上可接受的衍生物，其中R 1 -R 4，n，p，A，B，D，E，L和AR 1如本文中一般和类别和亚类所述，另外 提供其药物组合物及其用于治疗CD11 / CD18家族细胞粘附分子（例如LFA-1）介导的病症的方法。
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公开(公告)号：US20150175580A1
公开(公告)日：2015-06-25
申请号：US14610414
申请日：2015-01-30
发明人： Thomas Gadek , John Burnier
IPC分类号： C07D405/06
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：US20150175579A1
公开(公告)日：2015-06-25
申请号：US14610370
申请日：2015-01-30
发明人： Thomas Gadek , John Burnier
IPC分类号： C07D405/06
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：US20150174119A1
公开(公告)日：2015-06-25
申请号：US14610464
申请日：2015-01-30
发明人： Thomas Gadek , John Burnier
IPC分类号： A61K31/4725
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：US20150152090A1
公开(公告)日：2015-06-04
申请号：US14610251
申请日：2015-01-30
发明人： Thomas Gadek , John Burnier
IPC分类号： C07D405/06 , A61K31/381 , A61K31/495 , G01N33/68 , A61K38/17 , A61K38/08 , A61K38/07 , A61K31/198 , A61K31/405
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：US09045458B2
公开(公告)日：2015-06-02
申请号：US14275159
申请日：2014-05-12
发明人： Min Zhong , Wang Shen , Johan D. Oslob , Kenneth Barr
IPC分类号： C07D405/06 , C07D217/00 , A61K31/198 , A61K31/404 , A61K31/4162 , A61K31/4184 , A61K31/4192 , A61K31/44 , A61K31/4709 , A61K31/4725 , A61K31/4745 , A61K31/496 , A61K31/5377 , A61K31/54 , A61K31/541 , A61K31/381 , A61K45/06 , C07D333/38 , C07D405/14 , C07D409/14 , C07D471/04 , A61K33/00 , A61K33/06 , C07D217/20 , C07D217/06
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.
摘要翻译： 本发明提供了用于治疗LFA-1介导的疾病的化合物和方法。 特别地，本文描述了LFA-1拮抗剂，并且这些拮抗剂用于治疗LFA-1介导的疾病。 在患者被诊断患有LFA-1介导的疾病之后，本发明的一个方面提供LFA-1介导的疾病的诊断和LFA-1拮抗剂的施用。 在一些实施方案中，治疗的LFA-1介导的疾病是干眼症。 本文还提供了用于鉴定LFA-1拮抗剂的化合物的方法。
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