199296-51-0Relevant articles and documents
Pyridine methylamine compound and preparation method thereof
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Paragraph 0117-0124, (2021/08/28)
The invention provides a pyridine methylamine compound and a preparation method thereof. The preparation method comprises the steps that tetrahydrofuran and sodium borohydride are sequentially added into a cyanopyridine compound, then an iodine-containing tetrahydrofuran solution is dropwise added, a reaction is conducted at the temperature of 20-30 DEG C, and after dropwise adding is completed, stirring is carried out continuously; after the reaction is finished, methanol is added for refluxing, extracting and spin-drying are carried out to obtain the pyridine methylamine compound; wherein a functional group in the cyanopyridine compound is selected from chlorine, bromine, methyl, ethyl, amino or hydrogen; according to the preparation method, high-temperature and high-pressure special equipment does not need to be used, so that the preparation method is relatively safe, and dangerous accidents such as explosion and fire disasters are avoided; besides, the preparation method is relatively environment-friendly, recycling treatment of hazardous waste (used Raney nickel) is not involved, the economic benefit is relatively high, borane generated by the synthesis method is converted into boric acid esters in the post-treatment process, the treatment cost is low, and the harm to the environment is much small.
Optimization of Substrate-Analogue Furin Inhibitors
Ivanova, Teodora,Hardes, Kornelia,Kallis, Stephanie,Dahms, Sven O.,Than, Manuel E.,Künzel, Sebastian,B?ttcher-Friebertsh?user, Eva,Lindberg, Iris,Jiao, Guan-Sheng,Bartenschlager, Ralf,Steinmetzer, Torsten
supporting information, p. 1953 - 1968 (2017/11/22)
The proprotein convertase furin is a potential target for drug design, especially for the inhibition of furin-dependent virus replication. All effective synthetic furin inhibitors identified thus far are multibasic compounds; the highest potency was found for our previously developed inhibitor 4-(guanidinomethyl)phenylacetyl-Arg-Tle-Arg-4-amidinobenzylamide (MI-1148). An initial study in mice revealed a narrow therapeutic range for this tetrabasic compound, while significantly reduced toxicity was observed for some tribasic analogues. This suggests that the toxicity depends at least to some extent on the overall multibasic character of this inhibitor. Therefore, in a first approach, the C-terminal benzamidine of MI-1148 was replaced by less basic P1 residues. Despite decreased potency, a few compounds still inhibit furin in the low nanomolar range, but display negligible efficacy in cells. In a second approach, the P2 arginine was replaced by lysine; compared to MI-1148, this furin inhibitor has slightly decreased potency, but exhibits similar antiviral activity against West Nile and Dengue virus in cell culture and decreased toxicity in mice. These results provide a promising starting point for the development of efficacious and well-tolerated furin inhibitors.
Substituted alkylamine derivatives and methods of use
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Page 96, (2010/02/05)
Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
