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公开(公告)号：US20230233551A1
公开(公告)日：2023-07-27
申请号：US17815256
申请日：2022-07-27
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.
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![COMPOUNDS CONTAINING S-N-VALERYL-N-{[2'-(1H-TETRAZOLE-5-YL)-BIPHENYL-4-YL]-METHYL}-VALINE AND (2R,4S)-5-BIPHENYL-4-YL-4-(3-CARBOXY-PROPIONYLAMINO)-2-METHYL-PENTANOIC ACID ETHYL ESTER MOIETIES AND CATIONS](/abs-image/US/2021/11/25/US20210361610A1/abs.jpg.150x150.jpg)
公开(公告)号：US20210361610A1
公开(公告)日：2021-11-25
申请号：US17395305
申请日：2021-08-05
发明人： Lili FENG , Sven Erik GODTFREDSEN , Paul Allen SUTTON , Mahavir PRASHAD , Michael J. GIRGIS , Bin HU , Yugang LIU , Thomas J. BLACKLOCK , Piotr Henryk KARPINSKI
IPC分类号： A61K31/216 , A61K31/41 , A61K45/06 , A61K31/4422 , A61K31/5415 , C07C233/47 , C07D257/04 , C07D207/50
摘要： A compound comprising of the angiotensin receptor antagonist (ARB) valsartan, the neutral endopeptidase inhibitor (NEPi) (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methylpentanoic acid ethyl ester and one or more monovalent cations such as Na+ useful for the treatment of hypertension and/or heart failure.
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公开(公告)号：US20040241706A1
公开(公告)日：2004-12-02
申请号：US10660113
申请日：2003-09-10
发明人： Kavita Shah , Fabien Vincent , Maria A. Cueto
IPC分类号： C12Q001/68 , C07H021/04 , A61K048/00
CPC分类号： C07H21/04
摘要： This invention provides methods and compositions related to modified GTPase sequences and GTPase modulators.
摘要翻译： 本发明提供了与修饰的GTPase序列和GTPase调节剂相关的方法和组合物。
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公开(公告)号：US20230331711A1
公开(公告)日：2023-10-19
申请号：US18337565
申请日：2023-06-20
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.
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公开(公告)号：US20220073500A1
公开(公告)日：2022-03-10
申请号：US17323693
申请日：2021-05-18
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.
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公开(公告)号：US20210145824A1
公开(公告)日：2021-05-20
申请号：US16939627
申请日：2020-07-27
发明人： Wang SHEN , Kenneth BARR , Johan D. OSLOB , Min ZHONG
IPC分类号： A61K31/4725 , 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 , A61K31/472 , A61K45/06 , C07D217/26 , A61K31/506 , A61K31/517
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).
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公开(公告)号：US10906892B2
公开(公告)日：2021-02-02
申请号：US16247843
申请日：2019-01-15
发明人： James Robert Zeller , Sripathy Venkatraman , Elisabeth C. A. Brot , Subashree Iyer , Michael Hall
IPC分类号： C07D407/06 , 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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![Amorphous solid form of compounds containing S—N-valeryl-N- {[2′-( 1 H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine and (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester moieties and sodium cations](/abs-image/US/2023/05/09/US11642329B2/abs.jpg.150x150.jpg)
公开(公告)号：US11642329B2
公开(公告)日：2023-05-09
申请号：US17847588
申请日：2022-06-23
发明人： Lili Feng , Sven Erik Godtfredsen , Paul Allen Sutton , Mahavir Prashad , Michael J. Girgis , Bin Hu , Yugang Liu , Thomas J. Blacklock , Piotr Henryk Karpinski
IPC分类号： A61K31/216 , A61K31/41 , C07C233/47 , C07D257/04 , A61K45/06 , A61K31/4422 , A61K31/5415 , C07D207/50
CPC分类号： A61K31/216 , A61K31/41 , A61K31/4422 , A61K31/5415 , A61K45/06 , C07C233/47 , C07D207/50 , C07D257/04 , A61K2300/00 , A61K31/216 , A61K2300/00 , A61K31/41 , A61K2300/00
摘要： An amorphous solid form of a compound comprising of the angiotensin receptor antagonist (ARB) valsartan, the neutral endopeptidase inhibitor (NEPi) (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methylpentanoic acid ethyl ester and sodium cations is provided. This is compound is useful for the treatment of hypertension and/or heart failure.
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![AMORPHOUS SOLID FORM OF COMPOUNDS CONTAINING S-N-VALERYL-N-{[2'-(1H-TETRAZOLE-5-YL)-BIPHENYL-4-YL]-METHYL}-VALINE AND (2R,4S)-5-BIPHENYL-4-YL-4-(3-CARBOXY-PROPIONYLAMINO)-2-METHYL-PENTANOIC ACID ETHYL ESTER MOIETIES AND SODIUM CATIONS](/abs-image/US/2022/10/20/US20220331282A1/abs.jpg.150x150.jpg)
公开(公告)号：US20220331282A1
公开(公告)日：2022-10-20
申请号：US17847588
申请日：2022-06-23
发明人： Lili FENG , Sven Erik GODTFREDSEN , Paul Allen SUTTON , Mahavir PRASHAD , Michael J. GIRGIS , Bin HU , Yugang LIU , Thomas J. BLACKLOCK , Piotr Henryk KARPINSKI
IPC分类号： A61K31/216 , A61K31/41 , A61K45/06 , A61K31/4422 , A61K31/5415 , C07C233/47 , C07D257/04 , C07D207/50
摘要： An amorphous solid form of a compound comprising of the angiotensin receptor antagonist (ARB) valsartan, the neutral endopeptidase inhibitor (NEPi) (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methylpentanoic acid ethyl ester and sodium cations is provided. This is compound is useful for the treatment of hypertension and/or heart failure.
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公开(公告)号：US20220313663A1
公开(公告)日：2022-10-06
申请号：US17611012
申请日：2019-05-14
IPC分类号： A61K31/4152 , A61P7/04 , A61K31/573
摘要： The present invention relates to a method of treating immune thrombocytopenia (ITP) by administering eltrombopag or a pharmaceutically acceptable salt thereof to a patient.
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