- PYRIDINESULFONAMIDE DERIVATIVES AS TRAP1 MODULATORS AND USES THEREOF
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The present disclosure provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof. The provided compounds may be tumor necrosis factor ("TNF") receptor associated protein 1 ("TRAP1") modulators (e.g., TRAP1 activators). The provided compounds may also rescue the activity in PTEN-induced kinase 1 ("PINK1") loss of function contexts. The provided compounds may also improve mitochondrial health, function, quality, quantity, and/or activity, and/or reduce the production of reactive oxygen species. The provided compounds may also refold or solubilize aggregated or misfolded proteins such as a-synuclein. The present disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g., for treating a disease in a subject in need thereof).
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- Synthesis of 2,4-Disubstituted Imidazoles via Nucleophilic Catalysis
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A convergent, microwave-assisted protocol for the synthesis of disubstituted NH-imidazoles via nucleophilic catalysis is described. The substituted imidazoles are accessed via the intramolecular addition of a variety of amidoxime substrates to activated a
- Camp, Jason E.,Dunsford, Jay J.,Gill, Duncan M.,Ngwerume, Simbarashe,Saunders, Alexandra R.,Shabalin, Dmitrii A.
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supporting information
p. 797 - 800
(2020/05/19)
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- HETEROARYL INHIBITORS OF PAD4
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The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.
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Paragraph 00187-00188
(2017/09/15)
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- Highly efficient oxidation of 2-imidazoline-5-carboxylic derivatives to imidazole-5-carboxylic derivatives by dioxygen
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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
- Huang, Yue,Zu, Xiaodong,Wu, Fan,Xu, Jinyi,Wu, Xiaoming,Yao, Hequan
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supporting information; experimental part
p. 3123 - 3128
(2012/06/01)
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- PIPERIDINE-CONTAINING COMPOUNDS AND USE THEREOF
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A method for preventing and/or treating a metabolic disease, cerebrovascular disease, etc. which comprises administering to a mammal an effective amount of the compound of the formula (I) wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. And a novel compound of the formula (I-1): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof has an anti-diabetic effect and a neuroprotective effect. Accordingly, the compound of the formula (I) and the compound of the formula (I-1) are useful in a method for preventing and/or treating for a metabolic disease such as diabetes, cerebrovascular disease such as stroke, etc.
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Page/Page column 167
(2010/08/04)
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- Design and synthesis of optically active 2-phenylimidazolecarboxamides featuring amino acid motive
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(Chemical Equation Presented) Overall sixteen new, optically active carboxamides 1-3 have been synthesized. These compounds based on the 2-phenylimidazole and featuring amino acid residues are linked on the 4-position by an amidic bond. Two general methods were used for their construction. Whereas the first method employs acylchlorides as a reactive species, the second one involves a condensation of mixed anhydrides with the amino acid counterparts. Actually, the second method proved to be more efficient than the first one. Carboxamides 1-3 were preliminarily tested as N-chelating ligands with an application in the Henry or Aldol reactions affording either poor yields or enantiomeric excesses.
- Sivek, Roman,Pytela, Oldrich,Bures, Filip
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experimental part
p. 1621 - 1627
(2009/06/28)
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- Two-step Synthesis of Imidazoles from Activated Alkynes
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Conjugate addition of 2-(tri-n-butylstannyl)tetrazoles (1) to activated alkynes gives 1-alkenyltetrazoles (4) and (5) predominantly.Use of the N-tributylstannyl derivatives, rather than the parent tetrazole, gives a high ratio of 1- to 2-alkenyl isomers and avoids the complication of further addition of the tetrazole or the alkyne to the initial adduct.Irradiation of the (Z)- and (E)-1-alkenyltetrazoles (4) and (5) at 254 nm then gives the expected imidazoles in moderate yield.However, 5-phenyl-2-(tri-n-butylstannyl)tetrazole (1a) reacted only slowly with ethyl phenylpropiolate to give ethyl 3,5-diphenylpyrazole-4-carboxylate (8), presumably via the 2-alkenyltetrazole (9) formed in preference to the 1-isomer for steric reasons.
- Casey, Michael,Moody, Christopher J.,Rees, Charles W.,Young, Richard G.
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p. 741 - 746
(2007/10/02)
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