139705-74-1Relevant academic research and scientific papers
READ-THROUGH INDUCER AND PHARMACEUTICAL USE THEREOF
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, (2020/08/04)
PROBLEM TO BE SOLVED: To provide a novel read-through inducer. SOLUTION: The present invention relates to a compound represented by the general formula (I) [each symbol in the formula is as described in the specification] or a pharmaceutically acceptable
1-Phenyl-: N -(benzothiazol-2-yl)methanimine derivatives as Middle East respiratory syndrome coronavirus inhibitors
Hu, Min-Qi,Li, Heng,Lin, Ying,Tang, Jie,Tang, Wei,Tong, Xian-Kun,Yang, Fan,Yu, Li-Fang,Zhang, Ying,Zuo, Jian-Ping
, p. 43299 - 43311 (2020/12/25)
Middle East respiratory syndrome coronavirus (MERS-CoV) poses a serious threat to human health, and currently there are no effective or specific therapies available to treat it. Herein a series of 1-phenyl-N-(benzothiazol-2-yl)methanimine derivatives with inhibitory activity against MERS-CoV are described. The compound 4f with a 50% inhibition concentration value of 0.09 μM is a promising inhibitor that warrants further evaluation, towards the development of potential anti-MERS-CoV drugs. This journal is
Discovery of novel N-(5-(tert-butyl)isoxazol-3-yl)-N′-phenylurea analogs as potent FLT3 inhibitors and evaluation of their activity against acute myeloid leukemia in vitro and in vivo
Xu, Ying,Wang, Ning-Yu,Song, Xue-Jiao,Lei, Qian,Ye, Ting-Hong,You, Xin-Yu,Zuo, Wei-Qiong,Xia, Yong,Zhang, Li-Dan,Yu, Luo-Ting
, p. 4333 - 4343 (2015/08/03)
FLT3 inhibitors have been explored as a viable therapy for acute myeloid leukemia (AML). However, the clinical outcomes of these FLT3 inhibitors were underwhelming except AC220. Therefore, the development of novel FLT3 inhibitors with high potency against
The flocculated acryloyldimethyltauric molecule ligand
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Paragraph 0420; 0689; 0690, (2016/10/08)
Provided are certain benzothiazole, imidazothiazole, imidazopyrimidine and imidazopyridine compounds, including, for example: formula (I) and pharmaceutically and physiologically acceptable salts, hydrates, and solvates thereof. Such compounds can be used as diagnostic ligands or labels of tau protein and PHF.
CYCLOPENTANECARBOXAMIDE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS AND THEIR USE
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, (2011/05/06)
The invention relates to cyclopentanecarboxamide derivatives of formula 1, to their use as Fatty Acid Synthase inhibitors, to methods for their therapeutic use and to pharmaceutical compositions containing them, wherein R1, R2, Rsup
HETEROCYCLIC INHIBITORS OF AN Hh-SIGNAL CASCADE, MEDICINAL COMPOSITIONS BASED THEREON AND METHODS FOR TREATING DISEASES CAUSED BY THE ABERRANT ACTIVITY OF AN Hh-SIGNAL SYSTEM
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, (2011/04/14)
The invention relates to novel heterocyclic compounds and to the use thereof, to pharmaceutical compositions containing said chemical compounds as an active ingredient and to the use thereof for producing medicinal preparations for the human being and warm-blood animals for treating diseases caused by the aberrant activity of an Hedgehog (Hh)-signal system, in particular oncological diseases. The invention also relates to the use of the above-mentioned compounds in the form of ‘molecular pharmacological tools’ for examining (in vitro and in vivo) the biochemical features of the Hh-signal system, in particular, the interaction of Hh protein and transmembrane proteins, namely, suppressor Patched (Ptc) and protooncogenic proteins. The eight groups of the claimed compounds comprise the derivatives of 2,6-dihydro-7H-pyrazolo[3,4-d]pyridazine-7-one and 1,4-dihydropyrazolo[3,4-b][1,4]thiazine-5-one; N-acidylated 4-imidazo[1,2-a]pyrimidine-2-il-anilines; ([4H-thino[3,2-b]pyrrol-5-il) carbonyl]piperidine-4-carbonic acid amides; 2-(4carbomoilpyperidine-1-il)-isonicotinic acid amides; N-sylphonyl-1,2,3,4-tetrahydroquinoline-6-carbonic acid amides; and pyridine 2-amino-4,5,6,7-tetrahydrothieno[2,3-c] N-acidylated 3-azole derivatives.
HYDRAZONE DERIVATIVE
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Page/Page column 33, (2010/11/08)
A compound represented by the following formula (I): wherein R1 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R2 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R3 represents hydrogen, etc.; Ar represents a divalent group derived from aromatic hydrocarbon, etc.; X represents a single bond, linear or branched alkylene having from 1 to 3 carbon atoms which may have a substituent, etc.; and G represents halogen, a saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc., a salt thereof or a solvate thereof; and an agent for inhibiting aggregation and/or deposition of an amyloid protein or an amyloid-like protein, which comprises the compound, a salt thereof or a solvate thereof
Substituent effects on fluorescent properties of imidazo[1,2- α]pyridine-based compounds
Tomoda, Haruhiko,Hirano, Takafumi,Saito, Shojiro,Mutai, Toshiki,Araki, Koji
, p. 1327 - 1334 (2007/10/03)
In order to search for novel fluorescent organic compounds, 20 derivatives of imidazo[1,2-a]pyridine (1) were synthesized, and their fluorescent properties were studied. Though the parent compound I (λ(fl) = 370.5 nm, Φ = 0.57 in ethanol) was in the liquid state at ambient temperature, 2-phenylimidazo[1,2-a]pyridine (5), 2-(2-naphthyl)imidazo[1,2- a]pyridine (16), 7-methylimidazo[1,2-a]pyridine (3), 7-methyl-2- phenylimidazo[1,2-a]pyridine (12), and 7-methyl-2(2-naphthyl)imidazo[1,2- a]pyridine (17) were found to give thermally stable solid compounds (mp 55- 190 °C) without much affecting the fluorescent properties of the parent compound (λ(fl) = 374-381 nm, Φ = 0.50-0.78 in ethanol). Among the 4'- substituted 2-phenyl derivatives, it was found that the introduction of the strong electron-donating amino and dimethylamino groups (2-(4- aminophenyl)imidazo[1,2-a]pyridine (7) and 2-[4- (dimethylamino)phenyl]imidazo[1,2-a]pyridine (8), respectively) caused marked red shift of their fluorescence (λ(fl) = 445 and 446 nm, respectively, in ethanol), thus providing the way for tuning the fluorescence color of the IP derivatives. The observed red shift of the fluorescence of 7 and 8 was ascribed to the contribution of the excited intramolecular charge transfer state.
