- 1,3,4-OXADIAZOLE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
-
The present invention relates to 1,3,4-oxadiazole derivative compounds having a histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, a use thereof in preparation of a medicament, a pharmaceutical composition comprising the same, a therapeutic method using the composition, and a method for preparing the same, and the 1,3,4-oxadiazole derivative compounds are represented by a following chemical formula (I).
- -
-
Page/Page column 140-141
(2020/12/11)
-
- Design, synthesis and identification of N, N-dibenzylcinnamamide (DBC) derivatives as novel ligands for α-synuclein fibrils by SPR evaluation system
-
PET imaging of α-synuclein (α-syn) deposition in the brain will be an effective tool for earlier diagnosis of Parkinson's disease (PD) due to α-syn aggregation is the widely accepted biomarker for PD. However, the necessary PET radiotracer for imaging is clinically unavailable until now. The lead compound discovery is the first key step for the study. Herein, we initially established an efficient biologically evaluation system well in high throughput based on SPR technology, and identified a novel class of N, N-dibenzylcinnamamide (DBC) compounds as α-syn ligands through the assay. These compounds were proved to have high affinities against α-syn aggregates (KD D) has been acquired, indicating its potential as a new lead compound for developing PET radiotracer.
- Chen, Yan-Fei,Bian, Jiang,Zhang, Peng,Bu, Lu-Lu,Shen, Yan,Yu, Wen-Bo,Lu, Xiu-Hong,Lin, Xin,Ye, De-Yong,Wang, Jian,Chu, Yong
-
-
- Compound capable of being strongly bound with alpha-synuclein aggregate, and preparation method and use of compound
-
The invention belongs to the technical field of medicine, and relates to a compound with a structural general formula I, and a preparation method and use of the compound. In the formula I, R1 is selected from phenyl, substituted phenyl, pyridyl and pyrimidinyl, and i is selected from 0 to 2, and is an integer; R2 is selected from alkyl, phenyl, substituted phenyl and 5-6-membered aromatic heterocyclic rings, and m is selected from 0 to 5, and is an integer; and R3 is selected from phenyl and substituted phenyl, and n is selected from 0 to 3, and is an integer. The compound comprises a cis-isomer, a trans-isomer or a mixture of the cis-isomer and the trans-isomer of the compound with the formula I structure. The compound can be strongly bound to an alpha-synuclein aggregate, can be used asan imaging tracer for the image technology such as PET, SPECT and the like, or can be used for preparing an imaging tracer and a composition containing the imaging tracer, the compound can be used forparticularly detecting Parkinson's disease or neurological disorders associated with the misfolding and aggregation of alpha-synuclein, and the compound has very good application prospects.
- -
-
Paragraph 0027; 0029-0031; 0093-0095
(2019/08/30)
-
- AMIDE-SUBSTITUTED ARYL PIPERIDINES
-
Amide-substituted aryl piperidines derivatives of the following Formulas are provided:(Formulas), in which the variables are as described herein. Such compounds may be used to modulate calcitonin gene-related peptide (CGRP) receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CGRP modulation in humans, domesticated companion animals and livestock animals, including headache, such as migraine. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such compounds for receptor localization studies and various in vitro assays.
- -
-
Page/Page column 66
(2008/12/05)
-
- BIARYL KETONE-SUBSTITUTED PIPERIDINES
-
Biaryl ketone-substituted piperidines of the following Formulas are provided:, and in which the variables are as described herein. Such compounds may be used to modulate calcitonin gene-related peptide (CGRP) receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CGRP modulation in humans, domesticated companion animals and livestock animals, including headache such as migraine. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such compounds for receptor localization studies and various in vitro assays.
- -
-
Page/Page column 58
(2008/12/06)
-
- CGRP receptor antagonists
-
The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.
- -
-
Page/Page column 138
(2008/06/13)
-
- Synthesis of (1-substituted piperidin-4-yl)-1H-benzimidazoles and (1-substituted piperidin-4-yl)-3,4-dihydroquinazolines as possible antihypertensive agents
-
Structural modifications of 4-piperidylbenzimidazolinones (I) by replacing the benzimidazolinone group with other heterocycles (2-cyanoamino, 2-ethoxy, and 2-methylbenzimidazole and 2-cyanoamino-3,4-dihydroquinazoline) has been made and a number of new pi
- Obase,Takai,Teranishi,Nakamizo
-
p. 565 - 573
(2007/10/02)
-