422572-59-6Relevant articles and documents
HETEROAROMATIC DERIVATIVES AND PHARMACEUTICAL APPLICATIONS THEREOF
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Paragraph 00389, (2015/11/10)
Provided herein are novel heteroaromatic derivatives, or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a prodrug, a pharmaceutically acceptable salt or a prodrug thereof, and pharmaceutical compositions containing such compounds. Also provided herein are uses of such compounds or pharmaceutical compositions thereof in the manufacture of a medicament for treating respiratory diseases, especially chronic obstructive pulmonary disease (COPD).
SUBSTITUTED 2-AMINO- 1,2,4 TRIAZOLO 1,5-a PYRIMIDINE DERIVATIVE AND USE THEREOF
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Page/Page column 22, (2008/06/13)
Disclosed is a [1,2,4]triazolo[1,5-a]pyrimidine derivative represented by the general formula (I) below or a pharmaceutically acceptable salt thereof. Also disclosed is a medicine containing such a derivative or a salt thereof as an active constituent. In
Design, synthesis, and tripeptidyl peptidase II inhibitory activity of a novel series of (S)-2,3-dihydro-2-(4-alkyl-1H-imidazol-2-yl)-1H-indoles
Breslin, Henry J.,Miskowski, Tamara A.,Kukla, Michael J.,Leister, William H.,De Winter, Hans L.,Gauthier, Diane A.,Somers, Maria V. F.,Peeters, Dani?lle C. G.,Roevens, Peter W. M.
, p. 5303 - 5310 (2007/10/03)
Butabindide, 1, was previously reported as a potent inhibitor (IC50 = 7 nM) of the serine protease enzyme tripeptidyl peptidase II (TPPII), an endogenous protease that degrades cholecystokinin-8 (CCK-8). We found that 1 has some inherent chemical instability, yielding diketopiperazine 2 fairly readily under mimicked physiological conditions. We therefore prepared imidazoles 3, which are void of 1's inherent instability, and have found that our novel analogues maintained comparable TPPII inhibitory activity (e.g., for 3c, IC50 = 4 nM) as 1.
