- Computer-aided identification, synthesis and evaluation of substituted thienopyrimidines as novel inhibitors of HCV replication
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A structure-based virtual screening technique was applied to the study of the HCV NS3 helicase, with the aim to find novel inhibitors of the HCV replication. A library of ~450000 commercially available compounds was analysed in silico and 21 structures were selected for biological evaluation in the HCV replicon assay. One hit characterized by a substituted thieno-pyrimidine scaffold was found to inhibit the viral replication with an EC50value in the sub-micromolar range and a good selectivity index. Different series of novel thieno-pyrimidine derivatives were designed and synthesised; several new structures showed antiviral activity in the low or sub-micromolar range.
- Bassetto, Marcella,Leyssen, Pieter,Neyts, Johan,Yerukhimovich, Mark M.,Frick, David N.,Brancale, Andrea
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supporting information
p. 31 - 47
(2016/08/01)
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- A simple synthesis of alkyl 2-aminobenzo[ b ]thiophene-3-carboxylates via an unexpected dehydrogenation of alkyl 2-amino-4,5,6,7-tetrahydrobenzo[ b ]thiophene-3-carboxylates
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A simple method for the preparation of alkyl 2-aminobenzo[b]thiophene-3-carboxylates is described. Alkyl 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylates, generated from the Gewald three-component reaction between cyclohexanones, alkyl cyanoacet
- Adib, Mehdi,Bayanati, Maryam,Soheilizad, Mehdi,Ghazvini, Helia Janatian,Tajbakhsh, Mahmood,Amanlou, Massoud
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- A simple synthesis of alkyl 2-aminobenzo[ b ]thiophene-3-carboxylates via an unexpected dehydrogenation of alkyl 2-amino-4,5,6,7-tetrahydrobenzo[ b ]thiophene-3-carboxylates
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A simple method for the preparation of alkyl 2-aminobenzo[b]thiophene-3-carboxylates is described. Alkyl 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylates, generated from the Gewald three-component reaction between cyclohexanones, alkyl cyanoacetates and sulfur, undergo dehydrogenation in benzonitrile under an air atmosphere to afford alkyl 2-aminobenzo[b]thiophene-3-carboxylates in good to excellent yields.
- Adib, Mehdi,Bayanati, Maryam,Soheilizad, Mehdi,Ghazvini, Helia Janatian,Tajbakhsh, Mahmood,Amanlou, Massoud
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p. 2918 - 2922
(2015/01/09)
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- TRICYCLIC BENZO[4,5]THIENO-[2,3-D]PYRIMIDINE-4-YL-AMIN DERIVATIVES, THEIR SALTS, PROCESS FOR PRODUCING THE COMPOUNDS AND THEIR PHARMACEUTICAL USE
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The invention relates to novel tricyclic benzo[4,5]thieno-[2,3-d]pyrimidine-4-yl-amin derivatives, as well as their pharmaceutically acceptable salts. The subject of the invention too the process for producing the compounds and their use as a pharmaceutic
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Page/Page column 8
(2011/02/18)
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- TRICYCLIC BENZO[4,5]THIENO-[2,3-D]PYRIMIDINE-4-YL-AMIN DERIVATIVES, THEIR SALTS, PROCESS FOR PRODUCING THE COMPOUNDS AND THEIR PHARMACEUTICAL USE
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The invention relates to novel tricyclic benzo[4,5]thieno-[2,3-d]pyrimidine-4-yl-amin derivatives, as well as their pharmaceutically acceptable salts. The subject of the invention too the process for producing the compounds and their use as a pharmaceutic
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- BENZOTHIENO’2,3-D! PYRIMIDINE COMPOUNDS AS INHIBITORS OF TYROSINE KINASE ACTIVITIES OF THE EPIDERMAL GROWTH FACTOR RECEPTORS (EGFRS) FOR THE TREATMENT OF HYPERPROLIFERATIVE DISEASES
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This invention relates to novel compounds of formula (I) and processes for their preparation, their use for of treating diseases, particularly hyperproliferative diseases such as cancer, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly hyperproliferative diseases such as cancer. Wherein m is 0, 1 or 2; R3 is *-O(CH2)n AR, wherein Ar is phenyl, thienyl, furyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, pyridyl, pyrimidyl od pyridazinyl, wherein Ar can optionally be substituted.
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Page/Page column 54-55
(2010/11/08)
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- FUNGICIDES
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A method of combating phytopathogenic diseases on plants and harvested food crops which comprises applying to a plant, to the seed of a plant, to the locus of the plant or seed or to a harvested crop a fungicidally effective amount of 2-aminothiophene derivatives of formula (1). The invention further relates to fungicidal compositions containing these compounds, processes for preparing these compounds and to some of the compounds themselves.
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Page/Page column 104
(2010/02/11)
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- NF-KB INHIBITORS
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The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-β phosphorylation of IκB. In so doing these aminothiophene inhibitors block pathological activation of transcription factor N
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Page 10; 12-13
(2008/06/13)
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- Fused thiophene compounds and medicinal use thereof
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A condensed thiophene compound of the formula (I) wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof and hydrates thereof. The compound of the formula (I) of the present invention is useful as a novel antipsychotic agent which is effective for both positive symptoms and negative symptoms of schizophrenia, which is associated with less side effects such as extrapyramidal motor disorder and the like and which is less associated with serious side effects such as agranulocytosis and the like. In addition, this compound is also useful as a therapeutic agent of Alzheimer's disease and manic-depressive illness.
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