73406-50-5Relevant academic research and scientific papers
COMPOUNDS, COMPOSITIONS AND METHODS FOR HISTONE LYSINE DEMETHYLASE INHIBITION
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Paragraph 0101; 0389, (2022/03/09)
The present disclosure relates generally to compounds and pharmaceutical compositions for the selective inhibition of histone lysine demethylase5 (KDM5), particularly KDM5B, and methods of their use in treating conditions and diseases associated with KDM5 activity.
Identification of Potent and Selective Inhibitors of Fat Mass Obesity-Associated Protein Using a Fragment-Merging Approach
Elboray, Elghareeb E.,Fujiwara, Yoshie,Itoh, Yukihiro,Kitao, Yuki,Kotoku, Masayuki,Mellini, Paolo,Oba, Makoto,Obika, Satoshi,Prakash, Muthuraj,Roy, Rohini,Singh, Ritesh,Suzuki, Takayoshi,Takada, Yuri,Takahashi, Yukari,Terao, Mitsuhiro,Wang, Dan Ohtan,Yamaguchi, Takao,Yamamoto, Chika,Yamashita, Yasunobu
supporting information, p. 15810 - 15824 (2021/11/18)
Fat mass obesity-associated protein (FTO) is a DNA/RNA demethylase involved in the epigenetic regulation of various genes and is considered a therapeutic target for obesity, cancer, and neurological disorders. Here, we aimed to design novel FTO-selective inhibitors by merging fragments of previously reported FTO inhibitors. Among the synthesized analogues, compound 11b, which merges key fragments of Hz (3) and MA (4), inhibited FTO selectively over alkylation repair homologue 5 (ALKBH5), another DNA/RNA demethylase. Treatment of acute monocytic leukemia NOMO-1 cells with a prodrug of 11b decreased the viability of acute monocytic leukemia cells, increased the level of the FTO substrate N6-methyladenosine in mRNA, and induced upregulation of MYC and downregulation of RARA, which are FTO target genes. Thus, Hz (3)/MA (4) hybrid analogues represent an entry into a new class of FTO-selective inhibitors.
BENZOFURAN AMIDES AND HETEROAROMATIC ANALOGUES THEREOF FOR USE IN THERAPY
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Page/Page column 138, (2019/01/07)
The present invention relatesto a pharmaceutical composition comprising acompound of the formula Ias described belowor a tautomeror a pharmaceutically acceptable salt thereof; to the compound of the formula Ias described below or a tautomer or a phar- mac
Discovery of pyridyl-based inhibitors of Plasmodium falciparum N-myristoyltransferase
Yu, Zhiyong,Brannigan, James A.,Rangachari, Kaveri,Heal, William P.,Wilkinson, Anthony J.,Holder, Anthony A.,Leatherbarrow, Robin J.,Tate, Edward W.
supporting information, p. 1767 - 1772 (2015/10/20)
N-Myristoyltransferase (NMT) represents an attractive drug target in parasitic infections such as malaria due to its genetic essentiality and amenability to inhibition by drug-like small molecules. Scaffold simplification from previously reported inhibitors containing bicyclic cores identified phenyl derivative 3, providing a versatile platform to study the effects of substitution on the scaffold, which yielded pyridyl 19. This molecule exhibited improved enzyme and cellular potency, and reduced lipophilicity compared to inhibitor 3. Further structure-based inhibitor design led to the discovery of 30, the most potent inhibitor in this series, which showed single-digit nM enzyme affinity and sub-μM anti-plasmodial activity.
Novel 3beta-amino azabicyclooctane heteroaromatic amid derivatives preparation method and therapeutic uses thereof
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Page/Page column 6, (2010/02/11)
The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a bicyclic fused heteroaromatic, such as thieno[2,3-b]pyridine, furo[2,3-b]pyridine, thieno[3,2-b]pyridine, furo[3,2-b]pyridine, thieno[2,3-b]pyrazine, furo[2,3-b]pyrazine, thieno[2,3-c]pyridine, furo[2,3-c]pyridine, thieno[3,2-c]pyridine and furo[3,2-c]pyridine; R1 represents a linear or branched C1-C6 alkoxy group, a linear or branched C1-C6 alkylthio group; R2 represents a linear, branched, cyclic C2-C8 group, a 2- or 3- thienylmethyl group, or a benzyl group optionally substituted by one or several halogens, F, Cl, Br, I, C1-C4 alkyl, C1-C4 alkoxy, CF3, CN, NO2, OH; and their pharmaceutically acceptable salts. Said compounds are anti-dopaminergic agents.
Heteroarylaminopyrazole derivatives useful for the treatment of diabetes
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Page/Page column 20-21, (2008/06/13)
The present invention relates to heteroarylaminopyrazole compounds, pharmaceutical compositions, and methods for treating diabetes and related disorders.
SPIROFUROPYRIDINE ARYL DERIVATIVES
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Page/Page column 15; 16, (2008/06/13)
Compounds of formula (I): and pharmaceutically-acceptable salts thereof, wherein: Ar is a moiety of formula (II) or (III): and A, B, and R1 are as defined in the specification, compositions containing such compounds and the use of such compounds and compositions for use in therapy.
Design and Synthesis of 4-Azaindoles as Inhibitors of p38 MAP Kinase
Trejo, Alejandra,Arzeno, Humberto,Browner, Michelle,Chanda, Sushmita,Cheng, Soan,Comer, Daniel D.,Dalrymple, Stacie A.,Dunten, Pete,Lafargue, JoAnn,Lovejoy, Brett,Freire-Moar, Jose,Lim, Julie,McIntosh, Joel,Miller, Jennifer,Papp, Eva,Reuter, Deborah,Roberts, Rick,Sanpablo, Florentino,Saunders, John,Song, Kyung,Villasenor, Armando,Warren, Stephen D.,Welch, Mary,Weller, Paul,Whiteley, Phyllis E.,Zeng, Lu,Goldstein, David M.
, p. 4702 - 4713 (2007/10/03)
Inhibition of the biosynthesis of proinflammatory cytokines such as tumor necrosis factor and interleukin-1 via p38 has been an approach toward the development of a disease modifying agent for the treatment of chronic inflammation and autoimmune diseases.
P38 MAP kinase inhibitors
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, (2008/06/13)
The present invention relates to compounds of Formula (I) that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
Synthesis of Functionalized Azomethine Ylides via the Rh(II)-Catalyzed Cyclization of α-Diazo Carbonyls onto Imino ?-Bonds
Padwa, Albert,Dean, Dennis C.,Osterhout, Martin H.,Precedo, Laura,Semones, Mark A.
, p. 5347 - 5357 (2007/10/02)
α-Diazo carbonyl compounds containing an imino group in the γ-position have been found to undergo a rhodium(II) acetate induced cyclization reaction to generate cyclic azomethine ylides.The reactive dipole undergoes a subsequent 1,3-dipolar cycloaddition
