117830-18-9Relevant articles and documents
[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINES
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Page/Page column 247, (2021/02/19)
The present invention covers [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds of general formula (I) in which R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
TRIAZOLE AGONISTS OF THE APJ RECEPTOR
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Paragraph 0322; 0323, (2016/12/07)
Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures where the definitions of the variables are provided herein.
Pyrido[4,3- e ][1,2,4]triazolo[4,3- a ]pyrazines as selective, brain penetrant phosphodiesterase 2 (PDE2) inhibitors
Rombouts, Frederik J. R.,Tresadern, Gary,Buijnsters, Peter,Langlois, Xavier,Tovar, Fulgencio,Steinbrecher, Thomas B.,Vanhoof, Greet,Somers, Marijke,Andrés, José-Ignacio,Trabanco, Andrés A.
supporting information, p. 282 - 286 (2015/03/30)
A novel series of pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazines is reported as potent PDE2/PDE10 inhibitors with drug-like properties. Selectivity for PDE2 was obtained by introducing a linear, lipophilic moiety on the meta-position of the phenyl ring pending from the triazole. The SAR and protein flexibility were explored with free energy perturbation calculations. Rat pharmacokinetic data and in vivo receptor occupancy data are given for two representative compounds 6 and 12.
High-throughput virtual screening identifies novel N ′-(1- phenylethylidene)-benzohydrazides as potent, specific, and reversible LSD1 inhibitors
Sorna, Venkataswamy,Theisen, Emily R.,Stephens, Bret,Warner, Steven L.,Bearss, David J.,Vankayalapati, Hariprasad,Sharma, Sunil
supporting information, p. 9496 - 9508 (2014/01/06)
Lysine specific demethylase 1 (LSD1) plays an important role in regulating histone lysine methylation at residues K4 and K9 on histone H3 and is an attractive therapeutic target in multiple malignancies. Here we report a structure-based virtual screen of
SUBSTITUTED (E)-N'-(1-PHENYLETHYLIDENE) BENZOHYDRAZIDE ANALOGS AS HISTONE DEMETHYLASE INHIITORS
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Page/Page column 93; 94, (2013/03/26)
In one aspect, the invention relates to substituted (E)-N'-(1- phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods fo
Acrylamide derivatives as antiallergic agents. 2. Synthesis and structure-activity relationships of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(3-pyridyl)acrylamides
Nishikawa,Shindo,Ishii,Nakamura,Kon,Uno
, p. 583 - 593 (2007/10/02)
A new series of 3-(3-pyridyl)acrylamides 16, 17, 19, and 26, and 5-(3-pyridyl)-2,4-pentadienamides 20-25 were prepared and evaluated for their antiallergic activity. Several of these compounds exhibited more potent inhibitory activities than the parent compounds 1a [(E)-N-[4 [4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(3-pyridyl)acrylamide] against the rat passive cutaneous anaphylaxis (PCA) reaction and the enzyme 5-lipoxygenase. Particularly, 4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(6-methyl-3-pyridyl)acrylamide (17p) showed an ED50 value of 3.3 mg/kg po in the rat PCA test, which was one-fifth of ketotifen and oxatomide. As compared with ketotifen and oxatomide, compound 17p (AL-3264) possessed a better balance of antiallergic properties due to inhibition of chemical mediator release, inhibition of 5-lipoxygenase, and antagonism of histamine.