112004-83-8Relevant articles and documents
Tuning the fluorescence based on the combination of TICT and AIE emission of a tetraphenylethylene with D-π-A structure
Bai, Ming,Li, Jiale,Wang, Xi,Yu, Lirong,Zhang, Mengxing
, p. 14520 - 14524 (2020)
A simple D-π-A structured tetraphenylethylene with two electron-rich methyloxy groups and two electron withdrawing cyano groups, which features both twisted intramolecular charge-transfer (TICT) and aggregation-induced emission (AIE) properties, namely TP
NOVEL ARYL ETHANE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT
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Paragraph 0112; 0113, (2019/04/16)
The present invention relates to an aryl ethene derivative, for inhibiting an estrogen-related receptor gamma (ERRγ) activity, a prodrug of same, a solvate of same, a stereoisomer of same or pharmaceutically acceptable salts of same, and a pharmaceutical
NOVEL ARYL ETHENE DERIVATIVES AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT
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Paragraph 0229-0231, (2018/05/03)
The present invention relates to an aryl ethene derivative represented by chemical formula 1 which suppresses the activity of estrogen-related receptor gamma (ERRandgamma;), a prodrug thereof, a solvate thereof, a stereomer thereof, or a pharmaceutically acceptable salt thereof, and to a pharmaceutical composition comprising the same as an effective component. In the chemical formula 1, R^1, R^2, L and Ar are the same as defined in the detailed description of the invention.COPYRIGHT KIPO 2018
Synthesis and biological evaluation of novel 4-hydroxytamoxifen analogs as estrogen-related receptor gamma inverse agonists
Kim, Jina,Chin, Jungwook,Im, Chun Young,Yoo, Eun Kyung,Woo, Seoyeon,Hwang, Hee Jong,Cho, Joong-Heui,Seo, Kyung-Ah,Song, Jaeyoung,Hwang, Hayoung,Kim, Kyung-Hee,Kim, Nam Doo,Yoon, Suk Kyoon,Jeon, Jae-Han,Yoon, Seung-Yun,Jeon, Yong Hyun,Choi, Hueng-Sik,Lee, In-Kyu,Kim, Seong Heon,Cho, Sung Jin
, p. 338 - 352 (2016/07/06)
Estrogen-related receptor gamma (ERRγ) has recently been recognized as an attractive target for treating inflammation, cancer, and metabolic disorders. Herein, we discovered and demonstrated the in vitro pharmacology as well as the absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties of chemical entities that could act as highly selective inverse agonists for ERRγ. The results were comparable to those for GSK5182 (4), a leading ERRγ inverse agonist ligand. Briefly, the half-maximal inhibitory concentration (IC50) range of the synthesized compounds for ERRγ was 0.1-10 μM. Impressively, compound 24e exhibited potency comparable to 4 but was more selective for ERRγ over three other subtypes: ERRα, ERRβ, and estrogen receptor α. Furthermore, compound 24e exhibited a superior in vitro ADMET profile compared to the other compounds. Thus, the newly synthesized class of ERRγ inverse agonists could be lead candidates for developing clinical therapies for ERRγ-related disorders.
CHEMICAL COMPOUNDS
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Page/Page column 32; 33, (2008/06/13)
The present invention discloses to novel compounds with a variety of therapeutic uses. More particularly, the invention discloses novel symmetrical triphenyl compounds that are particularly useful for selective estrogen receptor modulation.
CHEMICAL COMPOUNDS
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Page/Page column 27, (2008/06/13)
The present invention discloses novel compounds with a variety of therapeutic uses. More particularly, the invention discloses novel symmetrical triphenyl compounds that are particularly useful for selective estrogen receptor modulation.
Optimised synthesis and photochemistry of antenna-sensitised 1-acyl-7-nitroindolines
Papageorgiou, George,Corrie, John E.T.
, p. 609 - 616 (2007/10/03)
Benzophenone antenna-sensitised 1-acyl-7-nitroindolines show a significantly enhanced extent of photochemical cleavage in aqueous solution over their non-sensitised analogues and release the carboxylate derived from their 1-acyl group. The present work in
(Acyloxy)benzophenones and (Acyloxy)-4-pyrones. A New Class of Inhibitors of Human Neutrophil Elastase
Miyano, Masateru,Deason, James R.,Nakao, Akira,Stealey, Michael A.,Villamil, Clara I.,et al.
, p. 1052 - 1061 (2007/10/02)
A series of 4-(acyloxy)- and 4,4'-bis(acyloxy)benzophenones were synthesized.Some of them, pivalates (trimethylacetates) and isobutyrates in particular, were found to be potent and selective inhibitors of human neutrophil (leukocyte) elastase.A series of 2--5-(acyloxy)-4-pyrones were synthesized regioselectively from kojic acid.The 4-pyrones bearing a long chain acyl group at the 2-position and either pivaloyloxy or isobutyryloxy at the 5-position were potent and selective inhibitors of the human elastase.A number of analogues and derivatives in both series were synthesized in order to study the structure-activity relationship as summarized in Tables I-VI and in Tables IX and X.The inhibition was selective to human neutrophil elastase.No inhibition of porcine pancreatic elastase or bovine pancreatic chymotrypsin (Tables VII and XI) was observed.The most likely mechanism of inhibition is discussed.The implication of these findings for the treatment of rheumatoid arthritis and emphysema is outlined.
PHENOLIC ESTER DERIVATIVES AS ELASTASE INHIBITORS
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, (2008/06/13)
Phenolic esters of the general formula I STR1 are useful for the prevention, management or alleviation of elastase mediated diseases or conditions.