118974-46-2Relevant academic research and scientific papers
Discovery and mechanism of action studies of 4,6-diphenylpyrimidine-2-carbohydrazides as utrophin modulators for the treatment of Duchenne muscular dystrophy
Vuorinen, Aini,Wilkinson, Isabel V.L.,Chatzopoulou, Maria,Edwards, Ben,Squire, Sarah E.,Fairclough, Rebecca J.,Bazan, Noelia Araujo,Milner, Josh A.,Conole, Daniel,Donald, James R.,Shah, Nandini,Willis, Nicky J.,Martínez, R. Fernando,Wilson, Francis X.,Wynne, Graham M.,Davies, Stephen G.,Davies, Kay E.,Russell, Angela J.
supporting information, (2021/05/03)
Duchenne muscular dystrophy is a fatal disease with no cure, caused by lack of the cytoskeletal protein dystrophin. Upregulation of utrophin, a dystrophin paralogue, offers a potential therapy independent of mutation type. The failure of first-in-class utrophin modulator ezutromid/SMT C1100 in Phase II clinical trials necessitates development of compounds with better efficacy, physicochemical and ADME properties and/or complementary mechanisms. We have discovered and performed a preliminary optimisation of a novel class of utrophin modulators using an improved phenotypic screen, where reporter expression is derived from the full genomic context of the utrophin promoter. We further demonstrate through target deconvolution studies, including expression analysis and chemical proteomics, that this compound series operates via a novel mechanism of action, distinct from that of ezutromid.
SYNERGISTIC EFFECTS OF ALKANOLAMINE ALKYLAMIDES AND OTHER MOISTURIZING AGENTS
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Paragraph 0061, (2017/08/21)
The disclosure provides personal care compositions that comprise a moisturizing agent of formula (I) wherein n is an integer from 2 to 5, R1 is independently H or C1-C3 alkyl and R2 is an unsubstituted linear or branched C1-C6 alkyl, at least one additional moisturizing agent and a cosmetically acceptable vehicle. In particular, the compound of formula (I) is diglycolamine acetamide. The compositions generally improve moisturization of skin and hair.
METHOD OF MAKING A COMPOSITION OF AN ALKANOLAMINE ALKYLAMIDE AND A POLYOL
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Paragraph 0072, (2017/08/22)
The disclosure generally provides methods for preparing compositions comprising alkanolamine alkylamides and polyols. This disclosure further relates to methods for preparing compositions comprising alkanolamine alkylamides and polyols that can be used in formulations that provide moisturization.
THIAZOLIDINONE COMPOUNDS AND USE THEREOF
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Paragraph 0638-0639, (2017/09/21)
A pharmaceutical composition containing a compound of Formula (I) for treating an opioid receptor-associated condition. Also disclosed is a method for treating an opioid receptor-associated condition using such a compound. Further disclosed are two sets of thiazolidinone compounds of formula (I): (i) compounds each having an enantiomeric excess greater than 90% and (ii) compounds each being substituted with deuterium.
Synthesis and in vitro antitumor activity of novel 2-alkyl-5- methoxycarbonyl-11-methyl-6H-pyrido[4,3-b]carbazol-2-ium and 2-alkylellipticin-2-ium chloride derivatives
Mori, Ryota,Kato, Asako,Komenoi, Kousuke,Kurasaki, Haruaki,Iijima, Touru,Kawagoshi, Masashi,Kiran,Takeda, Sho,Sakai, Norio,Konakahara, Takeo
, p. 16 - 35 (2014/06/09)
Twenty-one types of novel ellipticine derivatives and pyridocarbazoles (5-methoxycarbonyl-11-methyl-6H-pyrido[4,3-b]carbazoles) with a nitrosourea moiety, linked by an oxydiethylene unit at the 2 position, were synthesized, and their cytotoxicity against HeLa S-3 cells was evaluated. Some of these new compounds exhibited potent antitumor activity by comparison with that of ellipticine.
A Mild and Efficient Method for Selective Acetylation of Amines
Yang, Shyh-Chyun,Wang, Huey-Min,Chen, Ling-Ching
, p. 585 - 588 (2007/10/02)
Primary and secondary amines were acetylated under mild conditions by means of 3-acetyl-1,3-thiazolidine-2-thione .The reaction was successfully applied to selective acetylation of a primary amino group of diamines containing a primary and a secondary amino groups or exclusive N-acetylation of amino alcohols.Key Words Selective acetylation; 3-Acetyl-1,3-thiazolidine-2-thione.
A New Building Block Method to Synthesize Symmetrical and Asymmetrical Per-N-alkyl-Substituted Polyaza-Crown Compounds
Krakowiak, Krzysztof E.,Bradshaw, Jerald S.,Izatt, Reed M.,Zamecka-Krakowiak, Daria J.
, p. 4061 - 4067 (2007/10/02)
A new approach for the synthesis of a variety of per-N-alkylated polyaza-crown compounds is decscribed.N-acetamide (25) and its benzamide analogue 26 are the key building blocks for the synthesis of the new polyaza-crowns.These ch
NOVEL AND CONVENIENT SYNTHESES OF N-ALKYL-SUBSTITUTED TRIAZA- AND TETRAAZA-CROWN COMPOUNDS
Krakowiak, Krzysztof E.,Bradshaw, Jerald S.,Izatt, Reed M.
, p. 3521 - 3524 (2007/10/02)
A new short method to prepare N-alkyl-substituted triaza- and tetraaza-crown compounds in good overall yield by reacting the appropriate oligoazaoxadiamine with allyloxymethyl-substituted triethylene glycol diiodide or diglycolyl dichloride (followed by r
