70978-88-0Relevant academic research and scientific papers
Preparation and application of aminourea-sensitive amine oxidase inhibitor
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Paragraph 0223-0224; 0228-0230, (2020/04/17)
The invention provides preparation and application of an aminourea-sensitive amine oxidase inhibitor. Specifically, the invention discloses a compound as shown in a formula I which is described in thespecification or a stereoisomer or racemate or a pharmaceutically acceptable salt thereof. The invention also discloses the capability of the compound in inhibition of aminourea-sensitive amine oxidase.
COMPOUNDS, DEVICES, AND USES THEREOF
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Paragraph 00544, (2018/04/21)
The present invention provides compounds, e.g., compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are implantable elements (e.g., devices and materials) comprising the same, as well as methods of use thereof, e.g., for treating or preventing a disease, disorder, or condition.
Nonpeptide Renin Inhibitors Employing a Novel 3-Aza(or oxa)-2,4-dialkyl Glutaric Acid Moiety as a P2/P3 Amide Bond Replacement
Baker, William R.,Fung, Anthony K. L.,Kleinert, Hollis D.,Stein, Herman H.,Plattner, Jacob J.,et al.
, p. 1722 - 1734 (2007/10/02)
A new series of renin inhibitors has been developed.The inhibitors feature a novel replacement for the P2/P3 dipeptide moiety normally associated with renin inhibitors.The dipeptide replacement was a (2S,4S)-3-aza(or oxa)-2,4-dialkylglutaric acid amide.Ex
2,4-Diamino-6,7-dimethoxyquinazolines. 4. 2-Derivatives as α1-Adrenoceptor Antagonists and Antihypertensive Agents
Campbell, Simon F.,Danilewicz, John C.,Greengrass, Colin W.,Plews, Rhona M.
, p. 516 - 520 (2007/10/02)
A series of 4-amino-6,7-dimethoxy-2-quinazoline derivatives (2) was synthesized and evaluated for α-adrenoceptor affinity and antihypertensive activity.Most compounds showed binding affinities within the nanomolar ranger for α1-receptors, although 25 and 26 showed enhanced potency (Ki, ca. 1.5x10-1o M), equivalent to that of prazosin.Series 2 also displaced 3H>clonidine from α2-adrenoceptors, but at relatively high doses of 10-6 M, and selectivity for α1 sites still predominated.In a rabbit pulmonary artery preparation , 12, 16, and 25 were potent antagonists of the α1-mediated, postjunctional vasoconstrictor activity of norepinephrine with no effect at the prejunctional α2 sites which modulate transmitter release.Physicochemical measurements gave a pKa of 7.63+/-0.10 for 12, and N-1 protonation will be favored (60percent) at physiological pH to provide the α1-adrenoceptor pharmacophore, 28.Antihypertensive activity of series 2 was evaluated following oral administration to spontaneously hypertensive rats, and blood pressure was measured after 1 and 6 h.Compounds 12, 13, 16, 23, and 37 displayed moderate efficacy and duration of action in lowering blood pressure, but the plasma half-life (ca. 2 h) of 16 in dogs was not compatible with potential once-daily administration in humans.
Antihypertensive 4-amino-2-[4-(substituted-alkoxy)piperidino)]quinazolines
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, (2008/06/13)
Regulators of the cardiovascular system and, in particular, in the treatment of hypertension having the formula STR1 pharmaceutically-acceptable bioprecursors thereof, and the pharmaceutically-acceptable acid addition salts thereof; wherein each of R
