265107-85-5Relevant academic research and scientific papers
HETEROCYCLIC COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, PREPARATION METHOD THEREFOR, AND USE THEREOF
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Paragraph 0459-0460, (2022/01/01)
The present invention relates to a heterocyclic compound, a pharmaceutical composition comprising same, a preparation method therefor, and a use thereof. Specifically, the compound of the present invention is represented by formula (I), and used for preventing or treating a disease or condition related to RET activity.
Design, Synthesis, and Preliminary Evaluation of SPECT Probes for Imaging β-Amyloid in Alzheimer's Disease Affected Brain
Okumura, Yuki,Maya, Yoshifumi,Onishi, Takako,Shoyama, Yoshinari,Izawa, Akihiro,Nakamura, Daisaku,Tanifuji, Shigeyuki,Tanaka, Akihiro,Arano, Yasushi,Matsumoto, Hiroki
, p. 1503 - 1514 (2018/06/26)
In this study, we synthesized of a series of 2-phenyl- and 2-pyridyl-imidazo[1,2-a]pyridine derivatives and examine their suitability as novel probes for single-photon emission computed tomography (SPECT)-based imaging of β-amyloid (Aβ). Among the 11 evaluated compounds, 10 showed moderate affinity to Aβ(1-42) aggregates, exhibiting half-maximal inhibitory concentrations (IC50) of 14.7 ± 6.07-87.6 ± 39.8 nM. In vitro autoradiography indicated that 123I-labeled triazole-substituted derivatives displayed highly selective binding to Aβ plaques in the hippocampal region of Alzheimer's disease (AD)-affected brain. Moreover, biodistribution studies performed on normal rats demonstrated that all 123I-labeled probes featured high initial uptake into the brain followed by a rapid washout and were thus well suited for imaging Aβ plaques, with the highest selectivity observed for a 1H-1,2,3-triazole-substituted 2-pyridyl-imidazopyridine derivative, [123I]ABC577. This compound showed good kinetics in rat brain as well as moderate in vivo stability in rats and is thus a promising SPECT imaging probe for AD in clinical settings.
NOVEL COMPOUND WITH AMYLOID AFFINITY
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Paragraph 0167, (2014/05/08)
A compound represented by the following formula (1), or a salt thereof: wherein R1 is a radioactive halogen substituent, 0 to 2 of A1, A2, A3 and A4 represent N, and the rest represent —(CH)— is effective as a diagnostic imaging probe targeting amyloid. A diagnostic agent for Alzheimer's disease contains a compound represented by the above formula (1) or a salt thereof. After administration to a patient, the compound and the diagnostic agent for Alzheimer's disease transfer into the patient's brain, and indicate good accumulation on amyloid deposited in the brain.
Substituted inmidazoles as bombesin receptor subtype-3 modulators
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Page/Page column 33, (2010/02/17)
Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.
