32683-00-4Relevant academic research and scientific papers
COMPOUNDS AND USES THEREOF
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, (2018/05/17)
The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
SUBSTITUTED HETEROCYCLES AS BROMODOMAIN INHIBITORS
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Paragraph 0161; 0162, (2016/06/28)
The present application relates to substituted heterocycles compound of Formula I and pharmaceutical compositions thereof useful for the inhibition of BET protein function by binding to bromodomains (Formula I).
Imidazole-derived agonists for the neurotensin 1 receptor
Hershberger, Paul M.,Hedrick, Michael P.,Peddibhotla, Satyamaheshwar,Mangravita-Novo, Arianna,Gosalia, Palak,Li, Yujie,Gray, Wilson,Vicchiarelli, Michael,Smith, Layton H.,Chung, Thomas D.Y.,Thomas, James B.,Caron, Marc G.,Pinkerton, Anthony B.,Barak, Lawrence S.,Roth, Gregory P.
, p. 262 - 267 (2014/01/17)
A scaffold-hop program seeking full agonists of the neurotensin-1 (NTR1) receptor identified the probe molecule ML301 (1) and associated analogs, including its naphthyl analog (14) which exhibited similar properties. Compound 1 showed full agonist behavior (79-93%) with an EC50 of 2.0-4.1 μM against NTR1. Compound 1 also showed good activity in a Ca mobilization FLIPR assay (93% efficacy at 298 nM), consistent with it functioning via the G q coupled pathway, and good selectivity relative to NTR2 and GPR35. In further profiling, 1 showed low potential for promiscuity and good overall pharmacological data. This report describes the discovery, synthesis, and SAR of 1 and associated analogs. Initial in vitro pharmacologic characterization is also presented.
Synthesis of di- and tri-substituted imidazole-4-carboxylates via PBu3-mediated [3+2] cycloaddition
Hsu, Mei-Yuan,Dietrich, Justin,Hulme, Christopher,Shaw, Arthur Y.
, p. 1538 - 1542 (2013/05/21)
Some new di- and trisubstituted imidazole-4-carboxylates were prepared from amidoacetic acids 3 in the present report. The key step to establish such imidazole- 4-carboxylates stemmed from the PBu3-mediated [3+2] cycloaddition between in situ-generated Δ2-oxazolinone 4 and ethyl cyanoformate6. Our results indicated that trisubstituted imidazoles 7-20 were afforded in better yields than those of disubstituted imidazoles 21-27. Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communications1 to view the free supplemental file. Copyright Taylor & Francis Group, LLC.
Highly efficient oxidation of 2-imidazoline-5-carboxylic derivatives to imidazole-5-carboxylic derivatives by dioxygen
Huang, Yue,Zu, Xiaodong,Wu, Fan,Xu, Jinyi,Wu, Xiaoming,Yao, Hequan
supporting information; experimental part, p. 3123 - 3128 (2012/06/01)
A highly efficient and environmental-benign oxidation by dioxygen (or air) as the sole oxidant was first applied for the conversion of 2-imidazoline-5- carboxylic derivatives to imidazole-5-carboxylic derivatives in very good and excellent yields. The sub
Carbene reactivity of 4-diazo-4H-imidazoles toward nucleophiles and aromatic compounds
Smith, Matthew R.,Blake, Alexander J.,Hayes, Christopher J.,Stevens, Malcolm F. G.,Moody, Christopher J.
experimental part, p. 9372 - 9380 (2010/03/04)
(Chemical Equation Presented) Carbenes derived from diazoimidazolecarboxylates 4 under thermal or photochemical conditions undergo O-H and N-H insertion reactions with alcohols and amines, respectively, in moderate yield, in competition with reduction in good H-donor solvents. Dichloromethane reacts to give the corresponding 4-chloroimidazole. Aromatic hydrocarbons are excellent traps for the imidazolylidene carbene and lead to a range of arylimidazole derivatives 7. Reaction with pyridine leads to the first example of a pyridinium ylide 8 formed from an imidazolylidene carbene, whereas irradiation in hexafluorobenzene gives the imidazoazocine 11, presumably by way of an initial norcaradiene intermediate.
CARBOXYLIC ACID DERIVATIVES AND DRUGS CONTAINING THE SAME
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, (2008/06/13)
The present invention provides a novel carboxylic acid compound, a salt thereof or a hydrate of them useful as an insulin-resistant improver, and a medicament comprising the compound as an active ingredient. That is, the present invention provides a carboxylic acid compound represented by the following formula (I), a salt thereof, an ester thereof or a hydrate of them. In the formula, R1 represents hydrogen atom, hydroxyl group or a C1-6 alkyl group etc. which may have one or more substituents; L represents a single or double bond or a C1-6 alkylene group etc. which may have one or more substituents; M represents a single bond or a C1-6 alkylene group etc. which may have one or more substituents; T represents a single bond or a C1-3 alkylene group which may have one or more substituents; W represents carboxyl group or a group represented by the formula -CON(Rw1)Rw2 (wherein Rw1 and Rw2 are the same as or different from each other and each represents hydrogen atom, formyl group etc.) etc.; represents a single or double bond; X represents oxygen atom or a C2-6 alkenylene group etc. which may have one or more substituents; Y represents a C5-12 aromatic hydrocarbon group etc. which may have one or more substituents and which may have one or more heteroatoms; and ring Z represents a C5-6 aromatic hydrocarbon group which may have 0 to 4 substituents and which may have one or more heteroatoms.
SYNTHESIS OF IMIDAZOLE DERIVATIVES FROM α-HALOOXIMES AND AMIDINES BY USE OF IRON CARBONYLS
Nakanishi, Saburo,Nantaku, Junji,Otsuji, Yoshio
, p. 341 - 342 (2007/10/02)
The reaction of α-halooximes with amidines in the presence of iron carbonyls gives imidazole derivatives in good yields.This reaction occurs via deoxygenation of 4H-1,2,5-oxadiazines by iron carbonyls.
