907945-62-4Relevant academic research and scientific papers
HDAC inhibitor and preparation method and application thereof
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Paragraph 0197-0201, (2020/11/12)
The present invention discloses a compound represented by a formula I, a stereoisomer thereof, and a pharmaceutically acceptable salt thereof. The invention further relates to a pharmaceutical composition containing the compound shown in the formula I and application of the compound in preparation of HDAC inhibitor drugs. The compound or the pharmaceutical composition thereof can be used for treating cell proliferation diseases, autoimmune diseases, inflammation, neurodegenerative diseases or viral diseases.
INHIBITORS OF PLASMA KALLIKREIN AND USES THEREOF
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, (2019/09/30)
The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
CATHEPSIN K INHIBITOR AND APPLICATION THEREOF
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Paragraph 0215, (2018/07/29)
The invention relates to capthepsin K inhibitors and uses thereof, specifically relates to a class of compounds having the formula (I) which are used for treating or preventing cathepsin dependent diseases or conditions, specifically, wherein the cathepsin is capthepsin K. The compounds and compositions thereof can be used as bone resorption inhibitors for the treatment of associated diseases.
1,3-disubstituted ketene compound and application thereof
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Paragraph 0237; 0238, (2018/11/03)
The invention relates to a 1,3-disubstituted ketene compound with a structure as shown in a formula (I) and application thereof. The compound mainly activates a PPAR (Peroxisome Proliferators-Activated Receptor) alpha, and also has excitation activity for PPPA delta and PPPA gamma. The 1,3-disubstituted ketene compound can be used for treating various diseases related to the PPAR regulation abnormality, such as NASH (nonalcoholic steatohepatitis), and particularly treating nonalcoholic hepatitis, also has potentials for treating diabetes, obesity, fibrotic diseases, cardiovascular diseases (comprising a heart failure, atherosclerosis and the like), kidney diseases (comprising chronic nephrosis, a kidney failure and the like), brain degenerative diseases (comprising the alzheimer disease and the like) and the like, and has higher application value. The formula is shown in the description.
2'-carbonyl-3-bromo-spiro[benzofuran-2,4'-oxazolidine] compounds and preparation method thereof
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Paragraph 0196; 0198-0200, (2017/08/02)
The invention discloses 2'-carbonyl-3-bromo-spiro[benzofuran-2, 4'-oxazolidine] compounds and a preparation method thereof. The 2'-carbonyl-3-bromo-spiro[benzofuran-2,4'-oxazolidine] compounds are photoactive compounds shown in the structural formula II. The 2'-carbonyl-3-bromo-spiro[benzofuran-2,4'-oxazolidine] compounds are photoactive spiro compounds, photoactive chiral spiro compounds with multiple functional groups substituted, such as photoactive chiral spiro compounds with azido groups, hydroxyl groups, allyl groups and anisole groups substituted, can be obtained through substitution reactions of bromine atoms at site 3 under different reaction conditions. Therefore, different kinds of other photoactive chiral spiro compounds are prepared by using the substitution reactions of bromine atoms, the range of the compounds is enlarged, and the potential application value is great.
Structure-Activity Relationship Study of Heterocyclic Phenylethenyl and Pyridinylethenyl Derivatives as Tau-Imaging Agents That Selectively Detect Neurofibrillary Tangles in Alzheimers Disease Brains
Matsumura, Kenji,Ono, Masahiro,Kitada, Ayane,Watanabe, Hiroyuki,Yoshimura, Masashi,Iikuni, Shimpei,Kimura, Hiroyuki,Okamoto, Yoko,Ihara, Masafumi,Saji, Hideo
, p. 7241 - 7257 (2015/10/05)
In order to explore novel tau-imaging agents that can selectively detect neurofibrillary tangles in Alzheimers disease (AD) brains, we designed and synthesized a series of heterocyclic phenylethenyl and (3-pyridinyl)ethenyl derivatives with or without a dimethyl amino group. In in vitro autoradiography using AD brain sections, all radioiodinated ligands with a dimethyl amino group bound to Aβ deposits in the sections. In contrast, the ligands without a dimethyl amino group showed different patterns of radioactivity accumulation in the sections depending on the kind of heterocycle contained in their molecules. Particularly, a phenylethenyl benzimidazole derivative ([125I]64) showed marked radioactivity accumulation in the temporal lobe which corresponded with the distribution of tau deposits. [125I]64 also showed the most favorable pharmacokinetics in normal mouse brains (3.69 and 0.06% ID/g at 2 and 60 min postinjection, respectively) among all ligands in this study. Taken together, these results suggest that [123I]64 may be a new candidate tau-imaging agent.
Radioactive iodine labeled compound, and, radioactive pharmaceutical containing the same (by machine translation)
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Paragraph 0016; 0055; 0057, (2018/10/10)
PROBLEM TO BE SOLVED: and compatibility and affinity for both amyloidosis acryloyldimethyltauric, labeled compd. radioactive iodine. SOLUTION: the present invention, N, N-labeled compd. dimethyl benzene amine including radioactive iodine or its salt. Selected drawing: no (by machine translation)
Aminostyrylbenzofuran derivatives as potent inhibitors for Aβ fibril formation
Byun, Ji Hun,Kim, HyeYun,Kim, YoungSoo,Mook-Jung, Inhee,Kim, Dong Jin,Lee, Won Koo,Yoo, Kyung Ho
scheme or table, p. 5591 - 5593 (2009/06/18)
The synthesis of a novel series of aminostyrylbenzofuran derivatives 1a-w and their inhibitory activities for Aβ fibril formation were described. All the synthesized compounds were evaluated by thioflavin T (ThT) assay and displayed potent inhibitory activities for Aβ fibril formation. Among them, compounds 1i and 1q exhibited excellent inhibitory activities (IC50 = 0.07 and 0.08 μM, respectively) than those of Curcumin (IC50 = 0.80 μM) and IMSB (IC50 = 8.00 μM) as reference compounds. Both compounds were selected as promising candidates for further biological evaluation.
