886732-29-2Relevant articles and documents
Nematic Triphenyltriazine Triesters and the Induction of the Columnar Mesophase by Fluorine Substitution
Vieira, André A.,Farias, Giliandro,Costa, Wallison C.,Eccher, Juliana,Bechtold, Ivan H.,Durola, Fabien,Bock, Harald
, p. 9003 - 9010 (2021)
Whereas their para homologs are not mesogenic, the disk-shaped triphenyltriazine meta-trialkylesters obtained via trimerization of 3-cyanobenzoic alkylester, which are configurationally more flexible, exhibit a monotropic nematic mesophase. Introduction of fluorine atoms into the alkyl chains or into the phenyl moieties leads to the appearance of an enantiotropic columnar mesophase. If fluorine is introduced both in the chains and in the phenyl moieties, only a monotropic mesophase remains. Fluorination of either the alkyl chains or the aromatic core, but not both, appears thus as a simple means of inducing or stabilizing columnar self-assembly in disk-shaped systems. As the homeotropically alignable columnar mesophase can thus be made to persist at room temperature, as energies higher than 3 eV of the first excited triplet state are computed in agreement with the value reported for the parent arene, and as they are not fluorescent themselves, these compounds are of promise as aligning host matrices for blue-emitting TADF devices with improved light outcoupling. Dilution of a columnar with a nonmesogenic homolog induces the nematic state, indicating that the nanoscopic make-up of both mesophases is closely related.
N3-SUBSTITUTED IMINOPYRIMIDINONES AS ANTIMALARIAL AGENTS
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Page/Page column 54, (2017/09/08)
The present invention provides methods of treating malaria comprising administration of an N3-substituted iminopyrimidinone of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables R1, R2, R3, R4, R5, A, B, L, m, and n are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin V activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.
Discovery and characterization of AZD9272 and AZD6538 - Two novel mGluR5 negative allosteric modulators selected for clinical development
Raboisson, Patrick,Breitholtz-Emanuelsson, Anna,Dahlloef, Henrik,Kers, Annika,Minidis, Alexander B. E.,Nordmark, Anna,Stroem, Peter,Terelius, Ylva,Wensbo, David,Edwards, Louise,Isaac, Methvin,Jarvie, Keith,Slassi, Abdelmalik,Wilson, Julie M.,Xin, Tao,Heaton, William L.,Sheehan, Susan M.,McLeod, Donald A.
supporting information, p. 6974 - 6979,6 (2020/09/02)
AZD9272 and AZD6538 are two novel mGluR5 negative allosteric modulators selected for further clinical development. An initial high-throughput screening revealed leads with promising profiles, which were further optimized by minor, yet indispensable, structural modifications to bring forth these drug candidates. Advantageously, both compounds may be synthesized in as little as one step. Both are highly potent and selective for the human as well as the rat mGluR5 where they interact at the same binding site than MPEP. They are orally available, allow for long interval administration due to a high metabolic stability and long half-lives in rats and permeate the blood brain barrier to a high extent. AZD9272 has progressed into phase I clinical studies.
IMINOPYRIDINE DERIVATIVE AND USE THEREOF
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Page/Page column 72, (2009/07/18)
Provided are an iminopyridine derivative having a selective α1D adrenergic receptor antagonistic action and useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like, and a screening method for a compound
ANTIPARASITIC AGENTS
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Page/Page column 23, (2008/12/07)
The present invention relates to compounds of the formula (I) or a tautomer or prodrug thereof, or a pharmaceutically acceptable salt of said compound, tautomer or prodrug, wherein: R1, R2, R3, R4 and R5 are each independently selected from H, halo, CN, CF3 and CONH2; compositions containing such compounds and the uses of such compounds as antiparasitic agents.
11beta-HSD1 Inhibitors
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Page/Page column 17, (2008/06/13)
The invention relates to compounds of formula (I) wherein A, Y, Z1, Z2, R1 to R3 and X1 to X4 have the meaning as cited in the description and the claims. For example A is 4'-fluorobiphen-4-yl; Y is -S(O)2NH-; R1, R2 are H; X1, X2, X4 are CH; X3 is C-F; Z1 is =O; and Z2-R3 is N(CH2CH3)2. Said compounds are useful as 11β-HSD1 inhibitors. The invention also relates to the preparation of such compounds as well as the production and use as medicament.
