262295-93-2Relevant articles and documents
Diaminoimidazopyrimidines: Access via the Groebke–Blackburn–Bienaymé Reaction and Structural Data Mining
Konstantinidou, Markella,Boiarska, Zlata,Butera, Roberto,Neochoritis, Constantinos G.,Kurpiewska, Katarzyna,Kalinowska-T?uscik, Justyna,D?mling, Alexander
, p. 5601 - 5605 (2020)
Imidazopyrimidines with diverse substitution patterns are a prime class of heterocycles, present in many commercially available or late-stage clinical trials drugs. Here, we describe a fast access to diaminoimidazopyrimidines by means of a powerful multicomponent reaction; the Groebke–Blackburn–Bienaymé reaction. We provide the design of such libraries of compounds, identifying all the structural motifs, and subsequently their synthesis. Scope and limitations are discussed, in addition to data mining in the Cambridge Structural Database and pharmacophore search with Crossminer. The presented approach highlights the vast amount of data available in the databases and provides potential future scaffold hopping alternatives for compounds with similar binding patterns. Further studies are ongoing to introduce more “drug-like” properties into this scaffold and to investigate cellular mechanism-based anti-cancer behaviours.
HETARYLAMINONAPHTHYRIDINES
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Page/Page column 91, (2011/09/19)
Novel hetarylaminonaphthyridine derivatives of formula (I) wherein X, R1, R2, R3, R4, W1, W2, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
CYANOPHENYL DERIVATIVES
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, (2008/06/13)
This application relates to a piperazino-substituted novel cyanophenyl derivative in which a substituted carbamoyl or substituted sulfamoyl group having an aryl, heterocyclic or the like group that may have a substituent group is bonded to one nitrogen atom on the piperazine ring. The compound of this application has an anti-androgen action and is useful in preventing or treating prostatic cancer, benign prostatic hyperplasia and the like diseases.