248263-04-9Relevant articles and documents
A novel anti-Alzheimer agent inhibiting oligomerization and fibriliation of beta-amyloid protects neuronal cell from Aβ-induced cytotoxicity
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, (2017/04/25)
The present invention relates to development of a novel treatment agent for Alzheimerandprime;s disease, having ability of protecting neural cells and inhibiting fibrosis and oligomerization of beta-amyloid. A compound of the present invention is capable of, while maintaining therapeutic effects on Alzheimerandprime;s disease, recovering ability of directly inhibiting oligomerized and fibrous amyloid beta, which is inherent activities of existing curcumin, thereby being useful as a novel inhibitor.COPYRIGHT KIPO 2017
Nickel-catalyzed one-pot synthesis of biaryls from phenols and arylboronic acids via C-O activation using TCT reagent
Iranpoor, Nasser,Panahi, Farhad,Jamedi, Fereshteh
, p. 6 - 10 (2015/03/05)
In this study, the direct Nickel-catalyzed Suzuki-Miyaura coupling reaction of phenols and arylboronic acids via C-O bond activation using 2,4,6-trichloro-1,3,5-triazine (TCT) is described. Initially, phenols were reacted with TCT to give the corresponding 2,4,6-triaryloxy-1,3,5-triazine (TAT) products. Subsequently, arylboronic acid, base and Ni-catalyst were added to the generated aryl C-O electrophile to obtain the final biaryl product. This study represents a simple and direct method for the synthesis of biaryls from phenolic compounds using sub-stoichiometric amounts of TCT as a cheap and readily available C-O activating reagent.
Dicyanovinyl-substituted J147 analogue inhibits oligomerization and fibrillation of β-amyloid peptides and protects neuronal cells from β-amyloid-induced cytotoxicity
Kim, Kyoungdo,Park, Kwang-Su,Kim, Mi Kyoung,Choo, Hyunah,Chong, Youhoon
, p. 9564 - 9569 (2015/09/28)
A series of novel J147 derivatives were synthesized, and their inhibitory activities against β-amyloid (Aβ) aggregation and toxicity were evaluated by using the oligomer-specific antibody assay, the thioflavin-T fluorescence assay, and a cell viability assay in the transformed SH-SY5Y cell culture. Among the synthesized J147 derivatives, 3j with a 2,2-dicyanovinyl substituent showed the most potent inhibitory activity against Aβ42 oligomerization (IC50 = 17.3 μM) and Aβ42 fibrillization (IC50 = 10.5 μM), and disassembled the preformed Aβ42 fibrils with an EC50 of 10.2 μM. Finally, we confirmed that 3j is also effective at preventing neurotoxicity induced by Aβ42-oligomers as well as Aβ42-fibrils.
Nickel-catalyzed Suzuki-Miyaura coupling of heteroaryl ethers with arylboronic acids
Li, Xiao-Jian,Zhang, Jin-Ling,Geng, Yu,Jin, Zhong
, p. 5078 - 5084 (2013/06/27)
Nickel-catalyzed Suzuki-Miyaura coupling of heteroaryl ethers with arylboronic acids was described. Selective activation of the phenol C-O bonds was achieved by converting them into the corresponding aryl 2,4-dimethoxy-1,3,5- triazine-6-yl ethers, in which aryl C-O bond could be selectively cleaved with inexpensive, air-stable NiCl2(dppf) as a catalyst. Coupling of these readily accessible heteroaryl ethers proved tolerant of extensive functional groups.
A general palladium-catalyzed Suzuki-Miyaura coupling of aryl mesylates
So, Chau Ming,Lau, Chak Po,Kwong, Fuk Yee
supporting information; experimental part, p. 8059 - 8063 (2009/04/13)
(Chemical Equation Presented) Catalyze this! The first palladium-catalyzed Suzuki-Miyaura coupling of unactivated aryl mesylates is reported, with not only arylboronic acids, but also other organoboron nucleophiles (see picture; Z=B(OH)2, BF3K, BPin). The reaction conditions are compatible with various common functional groups (R1=alkyl, OMe, CHO, CO, CN, CO2R′, heteroaryl).
Purinenucleoside derivative modified in 8-position and medical use thereof
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Page/Page column 23, (2010/11/28)
The present invention provides an 8-modified purinenucleoside derivative which is useful for diseases associated with an abnormality of plasma uric acid level. An 8-modified purinenucleoside derivative represented by the following formula (I), a prodrug thereof or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, is useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; RA is a hydrogen atom or a hydroxyl group; R1 is a hydrogen atom, a hydroxyl group, a thiol group, an amino group or a chlorine atom; ring J represents an optionally substituted 2-naphthyl group, or a group represented by the following general formula (II) wherein Y represents a single bond or a connecting group; ring Z represents an optionally substituted aryl group or heteroaryl group or the like; and R2 to R4, P1 and Q represents a halogen atom, a cyano group or the like.
BENZIMIDAZOLE DERIVATIVES AND MEDICAL USES THEREOF
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Page/Page column 34, (2008/06/13)
The present invention providesbenzimidazole derivatives represented by the following formula (I) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an inhibitory activity on sodium-dependent nucleoside transporter 2 and are useful for a disease associated with an abnormality of plasma uric acid level. The compounds of the present invention are useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; R1 and R2 are H, a halogen atom, cyano group, optionally substituted alkyl group, optionally substituted aryl group or the like; R3 is H, a halogen atom, optionally substituted alkyl group or the like; R9 and R5 are H, a halogen atom, OH or the like; and R6 and RX are H or OH: RY is F or OH.
The first general palladium catalyst for the Suzuki-Miyaura and carbonyl enolate coupling of aryl arenesulfonates
Nguyen, Hanh Nho,Huang, Xiaohua,Buchwald, Stephen L.
, p. 11818 - 11819 (2007/10/03)
The first general method for the palladium-catalyzed Suzuki-Miyaura and carbonyl enolate coupling of unactivated aryl arenesulfonates was developed utilizing XPhos, 1, and Pd(OAc)2. This is of significant interest because aryl tosylates and aryl benzenesulfonates are more easily handled and considerably less expensive than aryl triflates. This catalyst system effects the coupling of a variety of aryl, heteroaryl, and extremely hindered arylboronic acids with different aryl tosylates, under mild conditions. The same catalyst was employed in the first carbonyl enolate coupling of aryl arensulfonates. Copyright