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公开(公告)号：US10273212B2
公开(公告)日：2019-04-30
申请号：US15635632
申请日：2017-06-28
IPC分类号： B01J19/24 , C07D217/04
摘要： The present invention is related to a two-step carboxylation reaction of an aryl group using continuous flow reaction conditions. This process permits large scale synthesis of useful reaction products in high yield.
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公开(公告)号：US10214517B2
公开(公告)日：2019-02-26
申请号：US15621141
申请日：2017-06-13
发明人： James Robert Zeller , Sripathy Venkatraman , Elisabeth C. A. Brot , Subashree Iyer , Michael Hall
IPC分类号： C07D405/06 , C07D407/06
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：US10188641B2
公开(公告)日：2019-01-29
申请号：US14045159
申请日：2013-10-03
发明人： Thomas Gadek , John Burnier
IPC分类号： C07D405/06 , 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 , A61K31/381 , A61K45/06 , C07D333/38 , 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
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：US09085553B2
公开(公告)日：2015-07-21
申请号：US13950807
申请日：2013-07-25
发明人： James Robert Zeller , Sripathy Venkatraman , Elisabeth C. A. Brot , Subashree Iyer , Michael Hall
IPC分类号： C07D405/06
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.
摘要翻译： 公开了制备和纯化式I化合物的方法，其中间体，其多晶型物和相关化合物。 还公开了其在治疗LFA-1介导的疾病中的制剂及其用途。
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公开(公告)号：US09045457B2
公开(公告)日：2015-06-02
申请号：US14045131
申请日：2013-10-03
发明人： Thomas Gadek , John Burnier , Min Zhong , Wang Shen , Johan D. Oslob , Kenneth Barr
IPC分类号： C07D217/00 , C07D405/06 , 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.
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公开(公告)号：US20140378506A1
公开(公告)日：2014-12-25
申请号：US14275159
申请日：2014-05-12
发明人： Thomas Gadek , John Burnier , Min Zhong , Wang Shen , Johan D. Oslob , Kenneth Barr
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：US08871935B2
公开(公告)日：2014-10-28
申请号：US13710651
申请日：2012-12-11
发明人： John Burnier , Thomas Gadek , Frederic Naud
IPC分类号： C07D217/26 , A61K31/4709 , C07D405/06
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.
摘要翻译： 公开了已被发现是LFA-1的有效抑制剂的式I化合物的形式A，B，C，D和E的新型结晶多晶型物。 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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8.发明申请TOPICAL LFA-1 ANTAGONISTS FOR USE IN LOCALIZED TREATMENT OF IMMUNE RELATED DISORDERS 审中-公开用于本地化治疗免疫相关疾病的局限性LFA-1拮抗剂公开(公告)号：US20140051722A1
公开(公告)日：2014-02-20
申请号：US13961117
申请日：2013-08-07
发明人： John Burnier , Thomas Gadek
IPC分类号： C07D405/06
CPC分类号： C07D405/06 , A61K9/0014 , A61K9/0048 , A61K9/06 , A61K9/08 , A61K31/381 , A61K31/437 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/4725 , A61K38/13
摘要： This invention provides specifically formulated LFA-1 antagonists or pharmaceutically acceptable salts thereof that are suitable for topical delivery. In particular, the LFA-1 antagonists are particularly well suited for localized treatment by having a rapid systemic clearance rate. The invention also encompasses methods of treatment and prevention of immune related disorders using the LFA-1 topical formulations of the present invention.
摘要翻译： 本发明提供了适用于局部给药的特异性配制的LFA-1拮抗剂或其药学上可接受的盐。 特别地，LFA-1拮抗剂特别适用于通过具有快速的全身清除率的局部治疗。 本发明还包括使用本发明的LFA-1局部制剂治疗和预防免疫相关病症的方法。
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公开(公告)号：US20140031387A1
公开(公告)日：2014-01-30
申请号：US13950807
申请日：2013-07-25
发明人： James Robert Zeller , Sripathy Venkatraman , Elisabeth C. A. Brot , Subashree Iyer , Michael Hall
IPC分类号： C07D405/06
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.
摘要翻译： 公开了制备和纯化式I化合物的方法，其中间体，其多晶型物和相关化合物。 还公开了其在治疗LFA-1介导的疾病中的制剂及其用途。
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公开(公告)号：US20120107404A1
公开(公告)日：2012-05-03
申请号：US13289172
申请日：2011-11-04
申请人： John Burnier , Thomas Gadek , Frederic Naud
发明人： John Burnier , Thomas Gadek , Frederic Naud
IPC分类号： A61K9/14 , A61K31/4725 , A61K31/56 , A61P29/00 , A61P27/02 , A61P27/14 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/06 , A61P17/08 , A61P17/02 , A61P17/14 , A61K9/00 , C07D405/10 , B82Y5/00
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.
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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