- PEPTIDOMIMETICS FOR THE TREATMENT OF CORONAVIRUS AND PICORNAVIRUS INFECTIONS
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Compounds, compositions and methods for preventing, treating or curing a coronavirus, picornavirus, and/or Hepeviridae virus infection in human subjects or other animal hosts. Specific viruses that can be treated include enteroviruses. In one embodiment, the compounds can be used to treat an infection with a severe acute respiratory syndrome virus, such as human coronavirus 229E, SARS, MERS, SARS-CoV-1 (OC43), and SARS-CoV- 2. In another embodiment, the methods are used to treat a patient co-infected with two or more of these viruses, or a combination of one or more of these viruses and norovirus.
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Page/Page column 115
(2020/12/29)
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- PEPTIDOMIMETICS FOR THE TREATMENT OF NOROVIRUS INFECTION
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The present invention is directed to compounds, compositions and methods for preventing, treating or curing Norovirus infection in human subjects or other animal hosts.
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Page/Page column 78
(2017/12/01)
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- Immunomodulators
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The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
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Paragraph 0480; 0481; 0482; 0483; 0484; 0485; 0486
(2016/08/29)
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- Enantioselective fluorescence recognition of chiral amines by n-acyl-(s)-1-naphthylalanyl-(s)-phenylglycine and n-acyl-(s)-1-naphthylalanyl- (s)-1-naphthylalanine dipeptides bridged by a 1,2-phenylene or an ethylene spacer chain
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This study sought to support the development of enantioselective dipeptide fluorescence sensors by examining the ability of the N-acyl-(S)-1- naphthylalanyl-(S)-phenylglycine and N-acyl-(S)-1-naphthylalanyl-(S)-1- naphthylalanine dipeptides (bridged by the 1,2-phenylene or ethylene spacer chain) to discriminate between aliphatic amine-derived (S)- and (R)-enantiomers. The results indicated that both hydrogen-bonding interactions in the ground state and charge-transfer interactions in the excited state are involved in the fluorescence quenching of these bridged dipeptides by chiral amines to produce the upward curving Stern-Volmer plots. In addition, the numerical analysis of these plots led to the conclusion that the bridged naphthylalanylphenylglycine dipeptide shows the highest ability to differentiate the (S)-enantiomer from (R)-enantiomer when the emission of this dipeptide is quenched by chiral alaninols.
- Ishikawa, Tomoe,Sonobe, Miho,Hayakawa, Akinori,Igarashi, Tetsutaro,Sakurai, Tadamitsu
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p. 1039 - 1058
(2013/05/23)
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- Studies on Cyclic Dipeptides, I: Aryl Modifications of cyclo-[Phe-His]
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Seven new cyclic dipeptides have been synthesized and tested for their applicability as tools to elucidate the mechanism of formation of mandelonitrile with (SS)-cyclo-[Phe-His] type catalysts. Conformational analyses based on 1H NMR spectra are presented for all prepared cyclic dipeptides.
- Noe,Weigand,Pirker
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p. 1081 - 1097
(2007/10/03)
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- Renin inhibitors. I. Synthesis and structure-activity relationship of transition-state inhibitors containing homostatine analogues at the scissile bond
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The synthesis and structure-activity relationships of transition-state renin inhibitors containing the homostatine analogues at the scissile bond are described. These inhibitors incorporate the amino acid side chains corresponding to positions 7-12 (Psub
- Atsuumi,Nakano,Koike,Tanake,Matsuyama,Nakano,Morishima
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p. 364 - 370
(2007/10/02)
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- Synthesis and Conformation of Aromatic Cyclic Dipeptides. Cyclo(phenylalanyl)2, Cyclo(1-naphthylalanyl)2, and Cyclo(2-naphthylalanyl)2
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Cyclic dipeptides of aromatic amino acids, cyclo(L-phenylalanyl)2, cyclo(L-1-naphthylalanyl)2, and cyclo(L-2-naphthylalanyl)2 were synthesized and subjected to spectroscopic analyses using 1H NMR, absorption, circular dichroism (CD), fluorescence, and fluoroscence-detected circular dichroism (FDCD).The 1H NMR data suggested that the 2,5-piperazinedione rings of the three cyclic dipeptides are in planar or nearly planar bowsplitboat-type conformation.The aromatic side groups of cyclo(1- and 2-naphthylalanyl)2's were found to take asymmetric configurations, one naphthyl group being folded onto the 2,5-piperazinedione ring, the order being unfolded.Strong exciton couplet was observed in CD spectra of the three compounds.The signs of the exciton splitting were opposite in the two naphthyl cyclic dipeptides.Fluorescence spectra of the two naphthyl cyclic dipeptides showed no excimer emission.The absence of strong interchromophoric interaction in the lowest excited state was also suggested by the virtual coincidence of CD spectrum with FDCD spectrum.From the above spectroscopic data, probable conformations were proposed for the naphthyl cyclic dipeptides.
- Egusa, Syun,Takagi, Jun,Sisido, Masahiko,Imanishi, Yukio
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p. 2195 - 2202
(2007/10/02)
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