142031-67-2Relevant academic research and scientific papers
Imaging and Profiling of Proteins under Oxidative Conditions in Cells and Tissues by Hydrogen-Peroxide-Responsive Labeling
Zhu, Hao,Tamura, Tomonori,Fujisawa, Alma,Nishikawa, Yuki,Cheng, Rong,Takato, Mikiko,Hamachi, Itaru
, p. 15711 - 15721 (2020)
Reactive oxygen species (ROS) such as hydrogen peroxide (H2O2) can inflict damage to biomolecules under oxidative stress and also act as signaling molecules at physiological levels. Here we developed a unique chemical tool to elucidate the biological role
Identification and structure–activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus
Deng, Xiaoyan,Jiang, Neng,Jiang, Weizhe,Li, Qing,Meng, Liuwei,Xing, Junhao,Xu, Yanjun
, (2021)
Our previously reported carboxyl-containing DPP-4 inhibitors were highly potent but were poorly bioavailable. Esters of the carboxyl analogs exhibited a significant DPP-4 potency loss albeit with enhanced oral absorption. Herein, we described identificati
Influence of fluorinated substituent and terminal length on phase behavior of mesogen-jacketed liquid crystalline polymers with a biphenyl mesogen
Jiang, Guoliang,Cai, Huanhuan,Shen, Zhihao,Fan, Xinghe,Zhou, Qifeng
, p. 557 - 564 (2013)
A series of mesogen-jacketed liquid crystalline polymers, poly{2,2,3,3,4,4,4-heptafluorobutyl 4′-hydroxy-2-vinylbiphenyl-4- carboxylate} (PF3Cm, where m is the number of carbon atoms in the alkoxy groups, and m = 1, 4, 6, and 8), the side chain of which c
COMPOUNDS AND USES THEREOF
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Page/Page column 187-188, (2021/08/06)
The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
Cross-coupling strategy for the synthesis of diazocines
Eleya, Nadi,Li, Shuo,Staubitz, Anne
, p. 1624 - 1627 (2020/03/13)
Ethylene bridged azobenzenes are novel, promising molecular switches that are thermodynamically more stable in the (Z) than in the (E) configuration, contrary to the linear azobenzene. However, their previous synthetic routes were often not general, and yields were poorly reproducible, and sometimes very low. Here we present a new synthetic strategy that is both versatile and reliable. Starting from widely available 2-bromobenzyl bromides, the designated molecules can be obtained in three simple steps.
INHIBITORS OF THE YAP/TAZ-TEAD INTERACTION AND THEIR USE IN THE TREATMENT OF CANCER
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Paragraph 0173, (2020/04/21)
The invention relates to compounds of formula (I): wherein R1; R2, R3, R4, R5 and are as defined in the description. The compounds of formula (I) are inhibitors of the YAP/TAZ-TEAD interaction and thu
COMPOUNDS TARGETING PROTEINS, COMPOSITIONS, METHODS, AND USES THEREOF
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Paragraph 0216, (2018/10/19)
The present invention provides modulators of protein function, to restore protein homeostasis, including GSPT1 activity. The invention provides methods of modulating protein-mediated diseases, such as GSPT1-mediated diseases, disorders, conditions, or responses. Compositions are also provided. Methods of treatment, amelioration, or prevention of protein-mediated diseases, disorders, and conditions, such as GSPT1-mediated diseases, disorders, and conditions, including cancer and astrogliosis.
3-ALKYL-4-AMIDO-BICYCLIC [4,5,0] HYDROXAMIC ACIDS AS HDAC INHIBITORS
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Paragraph 1097-1098, (2016/08/29)
The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
TBK/IKK INHIBITOR COMPOUNDS AND USES THEREOF
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Paragraph 0462; 0463, (2017/01/23)
The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.
Pharmacophore-based design of novel oxadiazoles as selective sphingosine-1-phosphate (S1P) receptor agonists with in vivo efficacy
Quattropani, Anna,Sauer, Wolfgang H. B.,Crosignani, Stefano,Dorbais, Jerome,Gerber, Patrick,Gonzalez, Jerome,Marin, Delphine,Muzerelle, Mathilde,Beltran, Fanny,Nichols, Anthony,Georgi, Katrin,Schneider, Manfred,Vitte, Pierre-Alain,Eligert, Valerie,Novo-Perez, Laurence,Hantson, Jennifer,Nock, Sebastien,Carboni, Susanna,De Souza, Adriano Luis Soares,Arrighi, Jean-Fran?ois,Boschert, Ursula,Bombrun, Agnes
, p. 688 - 714 (2015/04/14)
Sphingosine-1-phosphate (S1P) receptor agonists have shown promise as therapeutic agents for multiple sclerosis (MS) due to their regulatory roles within the immune, central nervous system, and cardiovascular system. Here, the design and optimization of novel [1,2,4]oxadiazole derivatives as selective S1P receptor agonists are described. The structure-activity relationship exploration was carried out on the three dominant segments of the series: modification of the polar head group (P), replacement of the oxadiazole linker (L) with different five-membered heterocycles, and the use of diverse 2,2′-disubstituted biphenyl moieties as the hydrophobic tail (H). All three segments have a significant impact on potency, S1P receptor subtype selectivity, physicochemical properties, and in vitro absorption, distribution, metabolism, excretion and toxicity (ADMET) profile of the compounds. From these optimization studies, a selective S1P1 agonist, N-methyl-N-(4-{5-[2-methyl-2′-(trifluoromethyl)biphenyl-4-yl]-1,2,4-oxadiazol-3-yl}benzyl)glycine (45), and a dual S1P1,5 agonist, N-methyl-N-(3-{5-[2′-methyl-2-(trifluoromethyl)biphenyl-4-yl]-1,2,4-oxadiazol-3-yl}benzyl)glycine (49), emerged as frontrunners. These compounds distribute predominantly in lymph nodes and brain over plasma and induce long lasting decreases in lymphocyte count after oral administration. When evaluated head-to-head in an experimental autoimmune encephalomyelitis mouse model, together with the marketed drug fingolimod, a pan-S1P receptor agonist, S1P1,5 agonist 49 demonstrated comparable efficacy while S1P1-selective agonist 45 was less potent. Compound 49 is not a prodrug, and its improved property profile should translate into a safer treatment of relapsing forms of MS.
