36076-25-2Relevant academic research and scientific papers
FUNCTIONALIZED LONG-CHAIN HYDROCARBON MONO- AND DI-CARBOXYLIC ACIDS AND THEIR USE FOR THE PREVENTION OR TREATMENT OF DISEASE
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Paragraph 0544-0545, (2021/01/29)
This invention provides compounds of Formulae (IA), (IB), (IC), (ID), (IE), (IF), (IG), (IH), (IJ), (IK), (IL), (II), (III), (IIIA), and (IIIB); pharmaceutically acceptable salts and solvates thereof; and compositions thereof. This invention further provides methods for treating a disease, including but not limited to, liver disease or an abnormal liver condition; cancer (such as hepatocellular carcinoma or cholangiocarcinoma); a malignant or benign tumor of the lung, liver, gall bladder, bile duct or digestive tract; an intra- or extra-hepatic bile duct disease; a disorder of lipoprotein; a lipid-and-metabolic disorder; cirrhosis; fibrosis; a disorder of glucose metabolism; a cardiovascular or related vascular disorder; a disease resulting from steatosis, fibrosis, or cirrhosis; a disease associated with increased inflammation (such as hepatic inflammation or pulmonary inflammation); hepatocyte ballooning; a peroxisome proliferator activated receptor-associated disorder; an ATP citrate lyase disorder; an acetyl-coenzyme A carboxylase disorder; obesity; pancreatitis; or renal disease.
BIARYL COMPOUND, PREPARATION METHOD AND USE THEREFOR
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Paragraph 0132-0133, (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.
Iridium-Catalyzed α-Methylation of α-Aryl Esters Using Methanol as the C1 Source
Tsukamoto, Yuya,Itoh, Satoshi,Kobayashi, Masaki,Obora, Yasushi
supporting information, p. 3299 - 3303 (2019/05/10)
IrCl(cod)2]/dppe-catalyzed α-methylation of aryl esters using methanol as the C1 source was developed. This methylation process is useful in several fields including organic chemistry, biochemistry, and medicinal chemistry. Readily available methanol as methylation reagent was successfully adapted. The reaction processed high atom economy and efficient. By applying the reaction system, the synthesis method of naproxen was provided.
Cyclic tris-[5]helicenes with single and triple twisted M?bius topologies and M?bius aromaticity
Naulet, Guillaume,Sturm, Ludmilla,Robert, Antoine,Dechambenoit, Pierre,R?hricht, Fynn,Herges, Rainer,Bock, Harald,Durola, Fabien
, p. 8930 - 8936 (2019/01/03)
A number of singly (180°) twisted, largely single-stranded and thus conformationally rather fragile, M?bius molecules have been synthesized within the last 15 years, which are aromatic with 4n electrons, thus violating the Hückel rule. Annulenes with sign
Synergistic Catalysis for the Umpolung Trifluoromethylthiolation of Tertiary Ethers
Xu, Wentao,Ma, Junyang,Yuan, Xiang-Ai,Dai, Jie,Xie, Jin,Zhu, Chengjian
supporting information, p. 10357 - 10361 (2018/08/06)
The first transition-metal-free, site-specific umpolung trifluoromethylthiolation of tertiary alkyl ethers has been developed, achieving the challenging tertiary C(sp3)–SCF3 coupling under redox-neutral conditions. The synergism of organophotocatalyst 4CzIPN and BINOL-based phosphorothiols can site-selectively cleave tertiary sp3 C(sp3)–O ether bonds in complex molecules initiated by a polarity-matching hydrogen-atom-transfer (HAT) event. The incorporation of several competing benzylic and methine C(sp3)?H bonds in alkyl ethers has little influence on the regioselectivity. Selective difluoromethylthiolation of C?O bonds has also been achieved. This represents not only an important step forward in trifluoromethylthiolation but also a promising means for site-selective C?O bond functionalization of unsymmetrical tertiary alkyl ethers.
Occupying a flat subpocket in a tRNA-modifying enzyme with ordered or disordered side chains: Favorable or unfavorable for binding?
Neeb, Manuel,Hohn, Christoph,Ehrmann, Frederik Rainer,H?rtsch, Adrian,Heine, Andreas,Diederich, Fran?ois,Klebe, Gerhard
supporting information, p. 4900 - 4910 (2016/10/04)
Small-molecule ligands binding with partial disorder or enhanced residual mobility are usually assumed as unfavorable with respect to their binding properties. Considering thermodynamics, disorder or residual mobility is entropically favorable and contrib
Application of biocatalysis towards asymmetric reduction and hydrolytic desymmetrisation in the synthesis of a β-3 receptor agonist
Badland, Matthew,Burns, Michael P.,Carroll, Robert J.,Howard, Roger M.,Laity, Daniel,Wymer, Nathan J.
, p. 2888 - 2894 (2011/12/05)
Chemoenzymatic syntheses of two key intermediates in the preparation of a potent β-3 receptor agonist 1 are described. A lipase-catalysed hydrolytic desymmetrisation is employed in a new synthesis of intermediate 7, which avoids the use of alkyl-tin reagents. A second biotransformation delivers chiral chlorohydrin 5 from its parent ketone in greater enantiomeric excess than the previously-described Noyori-reduction process. A brief discussion of the enantioselectivity of a set of single-point mutants of Sporobolomyces salmonicolor aldehyde reductase in this bioreduction is also presented.
Anti-cancer compositions and methods
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Page/Page column 19, (2011/09/15)
Anti-cancer compositions and methods are described including one or more compounds having the structural formula I: where R is phenyl, where R1 is (CH2)n—Se—C(═NH)—NH2, where R2 is (CH2)n—Se—C(═NH)—NH
PYRROLIDINE DERIVATIVE OR SALT THEREOF
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Page/Page column 47-48, (2008/06/13)
[PROBLEMS] To provide a compound which can be used for the treatment of a disease associated with a calcium-sensing receptor (CaSR), particularly hyperparathyroidism. [MEANS FOR SOLVING PROBLEMS] It is found that a novel pyrrolidine derivative having an aminomethyl group substituted by an arylaklyl group or the like or a salt thereof has an excellent CaSR agonistic modulation effect and also has an excellent selectivity in the inhibition of CYP2D6 which may cause a drug-drug interaction. Thus, the novel pyrrolidine derivative is useful as a therapeutic agent for a disease associated with CaSR (e.g., hyperparathyroidism, renal osteodystrophy and hypercalcemia).
