53305-12-7Relevant academic research and scientific papers
BIARYL COMPOUND, PREPARATION METHOD AND USE THEREFOR
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Paragraph 0110; 0113, (2020/01/02)
The present invention belongs to the technical field of chemical pharmaceuticals, and relates to a compound represented by general formula (I) or formula (II) and a preparation method thereof. The compounds are biaryl derivatives with RORγt activation activity. The biaryl derivatives disclosed in this invention can effectively activate the RORγt protein receptor, and thereby promote the differentiation of Th17 cells and increasing the production of IL-17, which can be used as an immune modulator for the treatment of various cancers or viral infection-related diseases.
N - aryl sulfonamide compound, its pharmaceutical composition and its use (by machine translation)
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Paragraph 0321-0323, (2019/04/30)
The invention discloses a category represented by the following general formula I N - aryl sulfonamide compound, to the compound as the active ingredient of the pharmaceutical composition, and their preparation for treating Lp - PLA2 In the diseases related to the activity of the use. (by machine translation)
COMPOUNDS AND METHODS FOR INHIBITING CYP26 ENZYMES
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Page/Page column 23; 24, (2018/07/05)
Compounds described herein are inhibitors of retinoic acid inducible P450 (CYP26) enzymes, and are useful for treating diseases that are responsive to retinoids. Certain compounds have retinoid activity, are resistant to CYP26-mediated catabolism, and are used for treating diseases that are responsive to retinoids.
Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia
Deshpande, Anil M.,Bhuniya, Debnath,De, Siddhartha,Dave, Bhavesh,Vyavahare, Vinod P.,Kurhade, Santosh H.,Kandalkar, Sachin R.,Naik, Keshav P.,Kobal, Balasaheb S.,Kaduskar, Rahul D.,Basu, Sujay,Jain, Vaibhav,Patil, Pratima,Chaturvedi Joshi, Sandhya,Bhat, Ganesh,Raje, Amol A.,Reddy, Satyanarayana,Gundu, Jayasagar,Madgula, Vamsi,Tambe, Suhas,Shitole, Prasad,Umrani, Dhananjay,Chugh, Anita,Palle, Venkata P.,Mookhtiar, Kasim A.
, p. 268 - 286 (2017/04/13)
Glucokinase activators (GKAs) are among the emerging drug candidates for the treatment of type 2 diabetes (T2D). Despite effective blood glucose lowering in clinical trials, many pan-GKAs “acting both in pancreas and liver” have been discontinued from cli
Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
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Page/Page column 165, (2016/02/26)
The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.
HEPATITIS B VIRAL ASSEMBLY EFFECTORS
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Paragraph 00372, (2016/10/31)
Novel assembly effector compounds having a therapeutic effect against hepatitis B viral (HBV) infection are disclosed. Assembly effector molecules described herein can lead to defective viral assembly and also may affect other viral activities associated with chronic HBV infection. Also disclosed is a process to synthesize disclosed compounds, method of treatment of HBV by administration of disclosed compounds, and use of these compounds in the manufacture of medicaments against HBV.
A resin-linker-vector approach to radiopharmaceuticals containing 18F: Application in the synthesis of O-(2-[18F]- Fluoroethyl)-L-tyrosine
Topley, Amy C.,Isoni, Valerio,Logothetis, Thomas A.,Wynn, Duncan,Wadsworth, Harry,Gibson, Alex M. R.,Khan, Imtiaz,Wells, Neil J.,Perrio, Cécile,Brown, Richard C.D.
supporting information, p. 1720 - 1725 (2013/02/25)
A Resin-linker-vector (RLV) strategy is described for the radiosynthesis of tracer molecules containing the radionuclide 18F, which releases the labelled vector into solution upon nucleophilic substitution of a polystyrene-bound arylsulfonate linker with [18F]-fluoride ion. Three model linker-vector molecules 7 a-c containing different alkyl spacer groups were assembled in solution from (4-chlorosulfonylphenyl)alkanoate esters, exploiting a lipase-catalysed chemoselective carboxylic ester hydrolysis in the presence of the sulfonate ester as a key step. The linker-vector systems were attached to aminomethyl polystyrene resin through amide bond formation to give RLVs 8 a-c with acetate, butyrate and hexanoate spacers, which were characterised by using magic-angle spinning (MAS) NMR spectroscopy. On fluoridolysis, the RLVs 8 a, b containing the longer spacers were shown to be more effective in the release of the fluorinated model vector (4-fluorobutyl)phenylcarbamic acid tert-butyl ester (9) in NMR kinetic studies and gave superior radiochemical yields (RCY≈60 %) of the 18F- labelled vector. The approach was applied to the synthesis of the radiopharmaceutical O-(2-[18F]-fluoroethyl)-L-tyrosine ([ 18F]-FET), delivering protected [18F]-FET in >90 % RCY. Acid deprotection gave [18F]-FET in an overall RCY of 41 % from the RLV. Copyright
ACETAMIDE COMPOUNDS, THEIR PROCESS AND PHARMACEUTICAL APPLICATION
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, (2012/03/09)
This disclosure relates to a series of acetamide compounds of formula (I), their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof. The disclosure also relates to process of preparation of
Design and synthesis of small molecular dual inhibitor of falcipain-2 and dihydrofolate reductase as antimalarial agent
Huang, Huang,Lu, Weiqiang,Li, Xi,Cong, Xiaoli,Ma, Hongmei,Liu, Xiaofeng,Zhang, Yu,Che, Peng,Ma, Ruoqun,Li, Honglin,Shen, Xu,Jiang, Hualiang,Huang, Jin,Zhu, Jin
supporting information; experimental part, p. 958 - 962 (2012/03/26)
Resistance of malaria parasites has quickly developed to almost all used antimalarial drugs. Accordingly, the discovery of new effective drugs to counter the spread of malaria parasites that are resistant to existing agents, especially acting on multi-targets, is an urgent need. The cysteine protease falcipain-2 (FP-2) and dihydrofolate reductase (DHFR) play crucial roles in the Plasmodium life cycle. In this study, a series of first-gereration small molecular dual inhibitor of FP-2 and DHFR have been designed and synthesized based on the lead compound 1, which was randomly identified by screening FP-2 inhibitors in our laboratory. Six compounds (2f-g, 2j, and 2m-o) showed improved dual inhibitory activities against FP-2 (IC50 = 2.7-13.2 μM) and DHFR (IC50 = 1.8-19.8 μM), and the inhibitory capability of compound 2o against FP-2 and DHFR were increased ～8 and ～6 times than that of compound 1, respectively. Moreover, compound 2o exhibited moderate in vivo antimalarial activity in a dose dependent fashion, its safety and survival rate were slightly better than that of positive drug. The preliminary SAR was obtained, meanwhile, molecular modeling result provided the key structural information to maintain the dual inhibitory activity, and was helpful for future dual inhibitors design.
Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in composition and use thereof
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, (2009/12/02)
The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.
