62009-34-1Relevant academic research and scientific papers
PYRIDINESULFONAMIDE DERIVATIVES AS TRAP1 MODULATORS AND USES THEREOF
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Paragraph 00288; 00531-00532, (2021/09/26)
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).
Acetylenyl-pyrazolo-pyrimidine derivatives
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Page/Page column 26, (2008/06/13)
The present invention relates to compounds of formula (I): wherein R1 to R3, A, M, L, E, G, and J are as defined in the description and claims. The invention also relates to a process for the manufacture of such compounds, pharmaceutical compositions containing them, and methods for treating CNS disorders.
Studies on Anticoccidial Agents. 13. Synthesis and Anticoccidial Activity of Nitropyridine-2- and -3-sulfonamides and Derivatives
Morisawa, Yasuhiro,Kataoka, Mitsuru,Nagahori, Hitoshi,Sakamoto, Toshiaki,Kitano, Noritoshi,et al.
, p. 1376 - 1380 (2007/10/02)
Eight nitropyridinesulfonamides andd pyridinesulfonamide N-oxides as their bioisosteres were prepared and evaluated for anticoccidial activity.Of these compounds, 2-, 4- and 5-nitropyridine-3-sulfonamides and pyridine-2- and -3-sulfonamide N-oxides were found to be active against Eimeria tenella.Thus, the relative positions, ortho or meta, of the substituents in nitropyridine-3-sulfonamides and pyridinesulfonamide N-oxides are important for anticoccidial activity.N-Substituted analogues of 5-nitropyridine-3-sulfonamide were also prepared and optimal anticoccidial activity was attained with the sulfonamide and its lower N-alkyl derivatives.The mode of action of 5-nitropyridine-3-sulfonamide was examined and found to be active in the sporozoite and the first schizogony stages.
Pyridine sulfonamides and their use as anticoccidial agents
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, (2008/06/13)
Pyridine derivatives having the formula STR1 wherein R1 represents hydrogen atom, amino group or a group STR2 in which R5 and R6 may be the same or different and each represents an alkyl group of 1 to 4 carbon atoms or R5 is hydrogen atom and R6 represents an alkyl group of 1 to 4 carbon atoms, an alkenyl group of 3 or 4 carbon atoms or a benzyl group optionally substituted with halogen, cyano, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms; R2 represents nitro group, amino group or an alkylamino group of 1 to 3 carbon atoms; R3 and R4 individually represent hydrogen atom, an alkyl group of 1 to 4 carbon atoms, an alkoxyalkyl group which has 1 to 4 carbon atoms in the alkoxy moiety and 2 to 4 carbon atoms in the alkyl moiety, an alkenyl group of 3 or 4 carbon atoms, an alkanoyl group of 1 to 18 carbon atoms or a benzyl group optionally substituted with halogen, cyano, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms; provided that when R1 is hydrogen atom and R2 is nitro group, R3 and R4 may be the same or different and each represents said alkyl group or said alkoxyalkyl group or R3 is hydrogen atom and R4 is hydrogen atom, said alkyl group, said alkoxyalkyl group, said alkenyl group, said alkanoyl group or said benzyl group, when R1 is hydrogen atom and R2 is amino group or said alkylamino group, R3 and R4 individually is hydrogen atom or they may be the same or different and each represents said alkyl group, when R1 is amino group and R2 is nitro group, R3 and R4 may be the same or different and each represents said alkyl group or R 3 is hydrogen atom and R4 is said alkyl group or said alkenyl group, and when R1 is said group STR3 and R2 is nitro group, R3 and R4 are the same as defined above with respect to the R5 and R6. They are highly effective in the treatment of coccidiosis, especially that caused by the protozoa belonging to the species Eimeria tenella or E. necatrix.
