681484-29-7Relevant articles and documents
Discovery of Reversible Inhibitors of KDM1A Efficacious in Acute Myeloid Leukemia Models
Romussi, Alessia,Cappa, Anna,Vianello, Paola,Brambillasca, Silvia,Cera, Maria Rosaria,Dal Zuffo, Roberto,Fagà, Giovanni,Fattori, Raimondo,Moretti, Loris,Trifirò, Paolo,Villa, Manuela,Vultaggio, Stefania,Cecatiello, Valentina,Pasqualato, Sebastiano,Dondio, Giulio,So, Chi Wai Eric,Minucci, Saverio,Sartori, Luca,Varasi, Mario,Mercurio, Ciro
supporting information, p. 754 - 759 (2020/03/04)
Lysine-specific demethylase 1 (LSD1 or KDM1A) is a FAD-dependent enzyme that acts as a transcription corepressor or coactivator by regulating the methylation status of histone H3 lysines K4 and K9, respectively. KDM1A represents an attractive target for c
INDOLE DERIVATIVES AS HISTONE DEMETHYLASE INHIBITORS
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Paragraph 00164; 00220, (2019/03/05)
The present application relates to compounds of formula (I), wherein A, R, R1, and R2 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy.
NMR Biochemical Assay for Oxidosqualene Cyclase: Evaluation of Inhibitor Activities on Trypanosoma cruzi and Human Enzymes
Tani, Osamu,Akutsu, Yukie,Ito, Shinji,Suzuki, Takayuki,Tateishi, Yukihiro,Yamaguchi, Tomohiko,Niimi, Tatsuya,Namatame, Ichiji,Chiba, Yasunori,Sakashita, Hitoshi,Kubota, Tomomi,Yanagi, Tetsuo,Mizukami, Shusaku,Hirayama, Kenji,Furukawa, Koji,Yamasaki, Kazuhiko
supporting information, p. 5047 - 5053 (2018/05/29)
Oxidosqualene cyclase (OSC), a membrane-associated protein, is a key enzyme of sterol biosynthesis. Here we report a novel assay for OSC, involving reaction in aqueous solution, NMR quantification in organic solvent, and factor analysis of spectra. We evaluated one known and three novel inhibitors on OSC of Trypanosoma cruzi, a parasite causative of Chagas disease, and compared their effects on human OSC for selectivity. Among them, one novel inhibitor showed a significant parasiticidal activity.
IMIDAZOLES AS HISTONE DEMETHYLASE INHIBITORS
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Paragraph 0105, (2017/12/15)
The present invention relates to imidazole derivatives, wherein A, R, R1, and R2 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy.
AMIDINOANILINE DERIVATIVE
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Paragraph 0197-0199, (2013/03/26)
Provided are a novel amidine derivative having an activated blood coagulation factor X inhibitory activity, a production method thereof, a production intermediate therefor, and a pharmaceutical composition containing the amidine derivative. An amidinoanil
PYRIDYL NON-AROMATIC NITROGENATED HETEROCYCLIC-1-CARBOXYLATE ESTER DERIVATIVE
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Page/Page column 28, (2008/06/13)
[Problem] To provide a compound usable for treatment of diseases associated with fatty acid amide hydrolase (FAAH), especially for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. [Means for Solution] We have found that a novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative of the present invention has an excellent effect for increasing an effective bladder capacity, an excellent effect for relieving urinary frequency and an excellent anti-allodynia effect, and is therefore usable for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.
HYDANTOIN DERIVATIVES USEFUL AS METALLOPROTEINASE INHIBITORS
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Page/Page column 20; 25, (2008/06/13)
Formula (I) wherein R1 is a (2-4C)alkyl and is substituted by two or more fluorine groups and R2 is methyl or ethyl, or a pharmaceutically acceptable salt thereof; processes for their preparation, pharmaceutical compositions containi
