39255-23-7Relevant academic research and scientific papers
Discovery and mechanism of action studies of 4,6-diphenylpyrimidine-2-carbohydrazides as utrophin modulators for the treatment of Duchenne muscular dystrophy
Vuorinen, Aini,Wilkinson, Isabel V.L.,Chatzopoulou, Maria,Edwards, Ben,Squire, Sarah E.,Fairclough, Rebecca J.,Bazan, Noelia Araujo,Milner, Josh A.,Conole, Daniel,Donald, James R.,Shah, Nandini,Willis, Nicky J.,Martínez, R. Fernando,Wilson, Francis X.,Wynne, Graham M.,Davies, Stephen G.,Davies, Kay E.,Russell, Angela J.
supporting information, (2021/05/03)
Duchenne muscular dystrophy is a fatal disease with no cure, caused by lack of the cytoskeletal protein dystrophin. Upregulation of utrophin, a dystrophin paralogue, offers a potential therapy independent of mutation type. The failure of first-in-class utrophin modulator ezutromid/SMT C1100 in Phase II clinical trials necessitates development of compounds with better efficacy, physicochemical and ADME properties and/or complementary mechanisms. We have discovered and performed a preliminary optimisation of a novel class of utrophin modulators using an improved phenotypic screen, where reporter expression is derived from the full genomic context of the utrophin promoter. We further demonstrate through target deconvolution studies, including expression analysis and chemical proteomics, that this compound series operates via a novel mechanism of action, distinct from that of ezutromid.
PYRAZOLOTRIAZOLOPYRIMIDINE DERIVATIVES AS A2A RECEPTOR ANTAGONIST
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Paragraph 0414-0416, (2020/02/16)
Disclosed herein is a pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as A2A receptor antagonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as A2A receptor antagonist.
Pyridine salt / 1,4-dihydropyridine derivative and preparation method thereof
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Paragraph 0102; 0103; 0104; 0106, (2016/10/09)
The present invention discloses a pyridine salt / 1,4-dihydropyridine derivative (NAD / NADH analog) with novel structure. The NAD / NADH analog can substitute natural NAD / NADH to be applied to a biochemical system for redox reactions, and can also be used as an electron carrier for the energy transfer of an enzymatic fuel cell. Further, the NAD / NADH analogs provided by the invention are easy to prepare, isolate and purify, and have a high yield.
6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site
Ghizzoni, Massimo,Wu, Jiang,Gao, Tielong,Haisma, Hidde J.,Dekker, Frank J.,George Zheng
supporting information; experimental part, p. 337 - 344 (2012/03/09)
Histone acetyltransferases are important enzymes that regulate various cellular functions, such as epigenetic control of DNA transcription. Development of HAT inhibitors with high selectivity and potency will provide powerful mechanistic tools for the elu
COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
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Page/Page column 41, (2008/12/06)
Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
3H-[1,2,4]-Triazolo[5,1-i]purin-5-amine derivatives as adenosine A2A antagonists
Silverman, Lisa S.,Caldwell, John P.,Greenlee, William J.,Kiselgof, Eugenia,Matasi, Julius J.,Tulshian, Deen B.,Arik, Leyla,Foster, Carolyn,Bertorelli, Rosalia,Monopoli, Angela,Ongini, Ennio
, p. 1659 - 1662 (2007/10/03)
A novel series of 3-substituted-8-aryl-[1,2,4]-triazolo[5,1-i]purin-5-amine analogs related to Sch 58261 was synthesized in order to identify potent adenosine A2A receptor antagonists with improved selectivity over the A1 receptor, physiochemical properties, and pharmacokinetic profiles as compared to those of Sch 58261. As a result of structural modifications, numerous analogs with excellent in vitro binding affinities and selectivities were identified. Moreover, compound 27 displayed both superior in vitro and highly promising in vivo profiles.
PYRROLO[2,3-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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Page/Page column 216, (2010/11/25)
Compounds of formula III which are active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
AROYL-O-PIPERIDINE DERIVATIVES FOR THE TREATMENT OF DIABETES-RELATED PROBLEMS
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Page/Page column 19, (2008/06/13)
The present invention relates to derivatives of aroyl-O-piperidine structure of the general formula (I): in which R1, R2, R3 and R4 are as defined in the description. Application of the compounds of the formula
2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: Highly potent, orally active, adenosine A2A antagonists. Part 1
Matasi, Julius J.,Caldwell, John P.,Zhang, Hongtao,Fawzi, Ahmad,Cohen-Williams, Mary E.,Varty, Geoffrey B.,Tulshian, Deen B.
, p. 3670 - 3674 (2007/10/03)
The structure-activity relationship of this novel class of compounds based on 2-(2-furanyl)-7-phenyl[1,2,4]-triazolo[1,5-c]pyrimidin-5-amine, 1, and its analogs was evaluated for their in vitro and in vivo adenosine A2A receptor antagonism. Several compounds displayed oral activity at 3 mg/kg in a rat catalepsy model. Specifically, compound 8g displayed an excellent in vitro profile, as well as a highly promising in vivo profile.
PIPERIDINYL-AND PIPERAZINYL-SULFONYLMETHYL HYDROXAMIC ACIDS AND THEIR USE AS PROTEASE INHIBITORS
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, (2008/06/13)
This invention is directed generally to proteinase (also known as "protease”) inhibitors, and, more particularly, to piperidinyl-and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as "matrix metalloprotease” or "MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E 3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity. "
