631909-08-5Relevant articles and documents
Discovery of a Novel Potent and Selective Calcium Release-Activated Calcium Channel Inhibitor: 2,6-Difluoro- N-(2′-methyl-3′-(4-methyl-5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)-[1,1′-biphenyl]-4-yl)benzamide. Structure-Activity Relationship and Preclinical Characterization
Ahirrao, Prajakta,Bakhle, Dhananjay,Bhankhede, Trupti,Bhonde, Mandar,Bokan, Sanjay,Budhe, Sagar,Dadke, Disha,Daler, Jagadeesh,Deshmukh, Gokul,George, Shaji K.,Gholve, Milind,Gundu, Jaysagar,Gupta, Rajesh,Ingawale, Sachin,Irlapatti, Nageswara Rao,Jachak, Santosh,Kalia, Anil,Kamalakannan, Prabakaran,Kamboj, Rajender Kumar,Kanoje, Vijay,Karche, Vijay,Khedkar, Nilesh Raghunath,Kizhakinagath, Praveenkumar Anidil,Kuldharan, Sandip,Kumar, Hemant,Kumar, Swaroop,Mallurwar, Sadanand,Mehta, Maneesh,Modi, Dipak,Naik, Kumar,Narasimham, Lakshmi,Nemade, Harshal Narendra,Nemmani, Kumar V. S.,Nigade, Prashant,Padiya, Kamlesh J.,Palle, Venkata P.,Pandey, Dilip,Pareek, Himani,Patil, Amit,Patil, Vinod,Pawar, Shashikant,Phukan, Samiron,Shah, Chirag,Shaikh, Zubair,Shankar, Rajesh,Sharma, Nidhi,Sharma, Sharad,Shinde, Vikas,Sindkhedkar, Milind,Singh, Minakshi,Sinha, Neelima,Tamane, Kaustubh,Venugopal, Spinvin,Vishwase, Gururaj,Wagh, Akshaya,Yeshodharan, Rajesh
, p. 17004 - 17030 (2021/12/09)
The role of calcium release-activated calcium (CRAC) channels is well characterized and is of particular importance in T-cell function. CRAC channels are involved in the pathogenesis of several autoimmune diseases, making it an attractive therapeutic target for treating inflammatory diseases, like rheumatoid arthritis (RA). A systematic structure-activity relationship study with the goal of optimizing lipophilicity successfully yielded two lead compounds, 36 and 37. Both compounds showed decent potency and selectivity and a remarkable pharmacokinetic profile. Further characterization in in vivo RA models and subsequent histopathological evaluation of tissues led to the identification of 36 as a clinical candidate. Compound 36 displayed an excellent safety profile and had a sufficient safety margin to qualify it for use in human testing. Oral administration of 36 in Phase 1 clinical study in healthy volunteers established favorable safety, tolerability, and good target engagement as measured by levels of IL-2 and TNF-α.
Aromatic ring-containing compound and application thereof
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Paragraph 0147-0152, (2019/10/01)
The present invention discloses an aromatic ring-containing compound and an application thereof, and provides an aromatic ring-containing compound represented by formula I, and a pharmaceutically acceptable salt, a hydrate, a solvate, a metabolite, a ster
Novel thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions
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, (2008/06/13)
Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4 and R7 are defined in the specification, Z is SO or SO2, and Ar is an aromatic or heteroaromatic group as defined herein.