123392-44-9Relevant academic research and scientific papers
NOVEL PYRAZINE AMIDE COMPOUNDS
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Page/Page column 100, (2015/02/25)
The present invention relates to compounds of formula 1 or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, R6 and X- have one of the meanings as indicated in the specification, to their use as a medicament, to their use in the treatment of a disease selected from among respiratory diseases or complaints and allergic diseases of the airways, to pharmaceutical composition comprising at least one of said compound or a pharmaceutically acceptable salt thereof, as well as to medicament combinations containing one or more of said compounds or a pharmaceutically acceptable salt thereof.
Synthesis and SAR study of new thiazole derivatives as vascular adhesion protein-1 (VAP-1) inhibitors for the treatment of diabetic macular edema: Part 2
Inoue, Takayuki,Morita, Masataka,Tojo, Takashi,Nagashima, Akira,Moritomo, Ayako,Imai, Keisuke,Miyake, Hiroshi
, p. 2478 - 2494 (2013/06/26)
Novel thiazole derivatives were synthesized and evaluated as vascular adhesion protein-1 (VAP-1) inhibitors. Although our previous compound 1 showed potent VAP-1 inhibitory activity, the activity differed between humans and rats. This issue was overcome by a hybrid design using human VAP-1 specific inhibitor 2, which was found by high-throughput screening (HTS), a docking study of a human VAP-1 homology model, and an analysis of sequence information for humans and rats. As a result, we identified compound 35c, which showed strong VAP-1 inhibitory activity (human IC50 of 20 nM; rat IC50 of 72 nM) and significant inhibitory effects in the ex vivo test.
SULFOXIMINES AS KINASE INHIBITORS
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Page/Page column 84-85, (2008/12/05)
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
THIAZOLE DERIVATIVES HAVING VAP-1 INHIBITORY ACTIVITY
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Page/Page column 80, (2008/06/13)
A compound of the formula (I), (II), (III) or (IV): wherein each symbol is as defined in the specification,or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a subject, and the like.
THIAZOLE DERIVATIVES AND THEIR USE AS VAP-1 INHIBITORS
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Page 114-115, (2010/02/07)
A compound of the formula (I): R1-NH-X-Y-Z (I) wherein R1 is acyl; X is a bivalent residue derived from optionally substituted thiazole; Y is a bond, lower alkylene or -COHN-; and Z is a groupe of the formulae (II) or (III) wherein R
Evaluation of the efficiency of the photocatalytic one-electron oxidation reaction of aromatic compounds adsorbed on a TiO2 surface
Tachikawa, Takashi,Yoshida, Akihiro,Tojo, Sachiko,Sugimoto, Akira,Fujitsuka, Mamoru,Majima, Tetsuro
, p. 5345 - 5353 (2007/10/03)
The TiO2 photocatalytic one-electron oxidation mechanism of aromatic sulfides with a methylene bridging group (-(CH2) n-, n = 0-4) between the 4-(methylthio)phenyl chromophore and the carboxylate binding group on the surfa
