18895-10-8Relevant articles and documents
2-AMINO-N-(AMINO-OXO-ARYL-LAMBDA6-SULFANYLIDENE)ACETAMIDE COMPOUNDS AND THEIR THERAPEUTIC USE
-
Page/Page column 212; 213, (2021/06/26)
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 2-amino-N-(amino-oxo-aryl-λ6- sulfanylidene)acetamide compounds (referred to herein as ANASIA compounds) that, inter alia, inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase (aaRS) (e.g., bacterial leucyl-tRNA synthetase, LeuRS). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase; to treat disorders that are ameliorated by the inhibition (e.g., selective inhibition) of bacterial aminoacyl-tRNA synthetase; to treat bacterial infections; etc.
Improved synthesis of 3-substituted-4-amino-[3,2-c]-thienopyridines
Engstrom, Kenneth M.,Baize, Amanda L.,Franczyk, Thaddeus S.,Kallemeyn, Jeffrey M.,Mulhern, Mathew M.,Rickert, Robert C.,Wagaw, Seble
experimental part, p. 3849 - 3855 (2009/09/26)
(Chemical Equation Presented) Two syntheses of 3-substituted-4-amino-[3,2- c]thienopyridines have been developed to replace the standard literature route to these compounds, which uses unattractive conditions involving azide and high temperatures. The fir
HCV INHIBITORS
-
Page/Page column 53, (2010/11/29)
The present invention provides HCV polymerase inhibiting compounds having the formula (I) where R1is cyclobutyl-N(Ra)-, n is 1, 2, 3 or 4, and at least one R5 is RaSO2N(Rj)alkyl-. In a non-
Novel thiophenes and analogues with anthelmintic activity against Haemonchus contortus
Gonzalez, Isabel C.,Davis, Leon N.,Smith II, Charles K.
, p. 4037 - 4043 (2007/10/03)
A new series of analogues of 4-(4-fluorophenyl)-2-methylthio-thiophene-3- carbonitrile (1) were synthesized and evaluated for their in vitro and in vivo anthelmintic activity against Haemonchus contortus.
Palladium-Catalyzed Cyanation Reactions of Thiophene Halides
Erker, Thomas,Nemec, Stephanie
, p. 23 - 25 (2007/10/03)
The described method provides an efficient cyanation reaction of thiophene halides using tris(dibenzylidene-acetone)dipalladium(0), 1,1′-bis- (diphenylphosphino)ferrocene) and zinc powder as the catalyst system and Zn(CN)2 as the cyanide source
Synthesis of Thieno--, -- and --thiophenes and Thieno--, -- and --thienopyrimidin-7(6H)-ones Starting from Thiophene
Hawkins, David W.,Iddon, Brian,Longthorne, Darren S.,Rosyk, Peter J.
, p. 2735 - 2744 (2007/10/02)
3-Bromo-, 3,5-dibromo- and 3,4,5-tribromo-2-thienyllithium have been prepared by bromine ->lithium exchange and converted into a number of thiophene derivatives, including the corresponding 2-carbaldehydes.The aldehydes have been converted into the corresponding thiophene-2-carbonitriles.Metallation of 2,5-dibromo- or 2,4,5-tribromo-thiophene with LDA occured at a vacant 3-position but the resulting 3-lithiated thiophenes rearranged (mechanism discussed) to 3,5-dibromo- and 3,4,5-tribromo-2-thienyllithium, which were quenched with various electrophiles.Attempts to dilithiate 2,5-dibromothiophene with LDA were unsuccessful. 3,4-Dibromo-2,5-dilithiothiophene was prepared from 2,3,4,5-tetrabromothiophene but it failed to yield the 2,5-dicarbaldehyde with N,N-dimethylformamide.The title thienothiophenes were prepared by reaction of a 3-bromothiophene-2-carbaldehyde, a 2-bromothiophene-3-carbaldehyde (prepared by bromination of a thiophene-3-carbaldehyde) or a 4-bromothiophene-3-carbaldehyde, or a corresponding nitrile, with ethyl 2-sulfanylacetate or 2-sulfanylacetamide.Thienothiophenes carrying an o-aminocarboxamide substitution pattern gave the title thienothienopyrimidinones with triethyl orthoformate.