412352-68-2Relevant academic research and scientific papers
FERROPORTIN INHIBITORS AND METHODS OF USE
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Paragraph 0806; 0807, (2020/07/07)
The subject matter described herein is directed to Ferroportin inhibitor compounds of Formula I and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis.
Amine compound for inhibiting SSAO/VAP-1 and application thereof in medicines
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Paragraph 0538; 0540; 0553; 0554, (2018/09/08)
The present invention relates to an amine compound for inhibiting SSAO/VAP-1 and application thereof in medicines. In particular, the present invention relates to an amine compound for inhibiting a semicarbazide-sensitive oxidase (SSAO) and/or vascular adhesion protein-1 (VAP-1) inhibitor, or a pharmaceutically acceptable salt thereof, a stereoisomer or an/a E/Z isomer, further relates to a pharmaceutical composition containing the amine compound. The invention further relates to the application of the amine compound and the pharmaceutical composition in manufacture of the medicines for treatment of inflammation, inflammation-related diseases and immune diseases.
PHARMACEUTICAL COMPOSITION FOR RESPIRATORY ADMINISTRATION
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Paragraph 0185-0186, (2016/06/28)
The present invention provides a pharmaceutical composition for respiratory administration containing a polysaccharide derivative having a group derived from a polysaccharide and a group derived from a physiologically active substance that is covalently b
GLYCOSAMINOGLYCAN DERIVATIVE AND METHOD FOR PRODUCING SAME
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Paragraph 0252-0256, (2016/06/28)
The present invention provides a glycosaminoglycan derivative in which a group derived from glycosaminoglycan and a group derived from a physiologically active substance having at least one of a carboxy group and a hydroxy group are coupled by covalent bond with a spacer therebetween, in which the spacer is selected in accordance with the decomposition rate of the covalent bond to the group derived from the physiologically active substance.
Recognition of the minor groove of DNA by hairpin polyamides containing α-substituted-β-amino acids
Floreancig, Paul E.,Swalley, Susanne E.,Trauger, John W.,Dervan, Peter B.
, p. 6342 - 6350 (2007/10/03)
Incorporation of the flexible amino acid β-alanine (β) into hairpin polyamides composed of N-methylpyrrole (Py) and N-methylimidazole (Im) amino acids is required for binding to DNA sequences longer than seven base pairs with high affinity and sequence selectivity. Pairing the α-substituted-β- amino acids (S)-isoserine ((S)Is), (R)-isoserine ((R)Is), β-aminoalanine (Aa), and α-fluoro-β-alanine (Fb) side-by-side with β in hairpin polyamides alters DNA binding affinity and selectivity relative to the parent polyamide containing a β/β pairing. Quantitative DNase I footprinting titration studies on a restriction fragment containing the sequences 5'- TGCNGTA-3' (N = A, T, G, and C) show that the polyamide ImPy(S)IsImPy-γ- PyPyβImPy-β-Dp (S)Is/β pairing) binds to N = T (K(a) = 4.5 x 109 M-1) in preference to N = A (K(a) = 6.2 x 108 M-1). This result stands in contrast to the essentially degenerate binding of the parent ImPyβImPy-γ- PyPyβImPy-β-Dp (β/β pairing) to N = T and N = A, and to the slight preference of ImPyβImPy-γ-PyPy(S)IsImPy-β-Dp (β/(S)Is pairing) to N = A over N = T. Additionally, this study reveals that incorporation of (R)Is, Aa, and Fb into polyamides significantly reduces binding affinity. Therefore, DNA binding in the minor groove is sensitive to the stereochemistry, steric bulk, and electronics of the substituent at the α-position of β-amino acids in hairpin polyamides containing β/β pairs.
