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.
SOS1 INHIBITORS
-
Paragraph 0244, (2021/06/26)
The present invention relates to compounds that inhibit Son of sevenless homolog 1 (SOS1) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.
Aromatic ring-containing compound and application thereof
-
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
TETRAZOLINONE COMPOUND AND USE THEREOF
-
Paragraph 0878; 0885, (2015/11/16)
The compound represented by formula (1): wherein R4 and R5 each represents a hydrogen atom, a halogen atom, or a C1-C3 alkyl group; R6 represents a C1-C4 alkyl group, a C3-C6 cycloalkyl group, or the like; R7, R8, and R9 each represents a hydrogen atom, a halogen atom, or the like; R10 represents a C1-C3 alkyl group, or the like; R13 represents a C1-C3 alkyl group, or the like; and Q represents a phenyl group, or the like; has an excellent control effect on pests.
Novel thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions
-
, (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.
NOVEL THIOPHENE AMIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATING COMPLEMENT-MEDIATED DISEASES AND CONDITIONS
-
Page 84-85, (2010/02/05)
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.
PHENYLALKANOIC ACID AND PHENYLOXYALKANOIC ACID DERIVATIVES AS HPPAR ACTIVATORS
-
Page 70-71, (2010/02/05)
The present invention provides a compound of formula (I):wherein:R1 and R2 are independently H or C1-3 alkyl;X represents a O or (CH2)n where n is 0, 1 or 2;R3and R4 independently represent H, C1-3 alkyl, -OCH3, -CF3, allyl, or halogen;X1 represents O, S, SO2, SO, or CH2;R5 and R6 independently represent hydrogen, C1-6 alkyl (including branched alkyl and optionally substituted by one or more halogens or C1-6alkoxy), or together with the carbon atom to which they are bonded form a 3-6 membered cycloalkyl ring;R7 represents a phenyl or a 6 membered heteroaryl group containing 1, 2 or 3 nitrogen atoms wherein the phenyl or heteroaryl group is substituted by 1, 2 or 3 moieties selected from the group consisting of halogen, C1-6 alkoxy, C1-6 alkyl, CF3, hydroxy, or phenyl (which may be optionally substituted by one or more C1-3 alkyl, -OC1-3 alkyl, CN, acetyl, hydroxy, halogen or CF3).