50882-68-3Relevant articles and documents
IRREVERSIBLE COVALENT INHIBITORS OF THE GTPASE K-RAS G12C
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Page/Page column 70; 71, (2014/09/29)
Irreversible inhibitors of K-Ras, H-Ras or N-ras protein comprising a G12C mutation are provided. Also disclosed are methods to regulate the activity of K-Ras, H-Ras or N-ras protein comprising G12C mutation and methods to disease mediated by K-Ras, H-Ras or N-ras G12C.
Chiral aryloxyalkylamines: Selective 5-HT1B/1D activation and analgesic activity
Carocci, Alessia,Lentini, Giovanni,Catalano, Alessia,Cavalluzzi, Maria Maddalena,Bruno, Claudio,Muraglia, Marilena,Colabufo, Nicola Antonio,Galeotti, Nicoletta,Corbo, Filomena,Matucci, Rosanna,Ghelardini, Carla,Franchini, Carlo
scheme or table, p. 696 - 704 (2011/02/22)
A series of chiral 2,3-dichlorophenoxy and 1-naphthyloxy alkylamines were synthesized, and their binding affinities towards 5-HT1D and h5-HT1B receptors were evaluated. In the naphthyloxy series, the (R)-prolinol derivative was the most selective 5-HT1D ligand, while (S)-N-methyl-2-(1-naphthyloxy)propan-1-amine showed the highest selectivity for h5-HT1B. Both compounds performed as 5-HT1D agonists in the isolated guinea pig assay and showed higher analgesic activity than both sumatriptan and the achiral analogue 20b in the mouse hotplate test. Neither ligand displayed any affinity for nicotinic ACh receptors present in mouse brain membranes, thus indicating that their analgesic activity does not arise through interaction with these receptors.
Pyridinium derivatives, their production and use
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, (2008/06/13)
Novel pyridinium derivatives represented by the formula (I): STR1 wherein STR2 is an optionally substituted pyridinium ring; R1 is a lower alkyl group or aralkyl group; R7 and R10 are independently hydrogen, a lower alkyl group, aryl group or aralkyl group; l is 0 or 1; R5 is a phenylene group or an alkylene group which may be substituted; R11 is an alkyl group or aryl group; X is a group of the formula: --CH2 OCH2 -- or a group of the formula: STR3 wherein R6 is hydrogen, a lower alkyl or a lower alkoxy, and m is an integer of 0 to 3; U is a group of the formula: STR4 wherein R4 is hydrogen, a lower alkyl group, aryl group or aralkyl group; Y and Z are independently a divalent chain group consisting of one to six members which is selected from the class consisting of groups of the formulae: STR5 wherein R is hydrogen, a lower alkyl group, acyl group or aryl group and at least one of which is a group of the formula: STR6 with the proviso that R may be the same or different from each other, or may form a ring together when two or more groups of the formula: STR7 are present, that R may be bonded to R4 when Y contains a group of the formula: STR8 and that R may be bonded to R11 when Z contains a group of the formula: STR9 and W? is a counter anion; are useful as a platelet activating factor antagonist.