261904-39-6Relevant articles and documents
Meta -Non-flat substituents: A novel molecular design to improve aqueous solubility in small molecule drug discovery
Ichikawa, Yuki,Hiramatsu, Michiaki,Mita, Yusuke,Makishima, Makoto,Matsumoto, Yotaro,Masumoto, Yui,Muranaka, Atsuya,Uchiyama, Masanobu,Hashimoto, Yuichi,Ishikawa, Minoru
supporting information, p. 446 - 456 (2021/01/29)
Aqueous solubility is a key requirement for small-molecule drug candidates. Here, we investigated the regioisomer-physicochemical property relationships of disubstituted benzenes. We found that meta-isomers bearing non-flat substituents tend to possess the lowest melting point and the highest thermodynamic aqueous solubility among the regioisomers. The examination of pharmaceutical compounds containing a disubstituted benzene moiety supported the idea that the introduction of a non-flat substituent at the meta position of a benzene substructure would be a promising approach for medicinal chemists aiming to improve the thermodynamic aqueous solubility of drug candidates, even though it might not be universally effective. This journal is
Synthetic method for (2R)-3-bromo-2-hydroxy-2-methylpropionic acid
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Paragraph 0018; 0025-0027; 0038; 0041; 0049-0052; 0060-0062, (2019/09/13)
The invention belongs to the technical field of compound synthesis, and in particular relates to a synthetic method for (2R)-3-bromo-2-hydroxy-2-methylpropionic acid. Preparation of methacryloyl-D-proline comprises the following steps: uniformly mixing D-proline, NaOH, MTBE and resorcinol under stirring at 5-20 DEG C, adding methacryloyl chloride dropwise, performing uniform stirring at 15-25 DEGC, allowing the uniformly-stirred material to stand for layering, and taking an upper-layer organic phase to obtain the methacryloyl-D-proline. The method provided by the invention has short synthetictime and is convenient to operate, and the (2R)-3-bromo-2-hydroxy-2-methylpropionic acid has stable quality.
SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF
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Paragraph 00365; 00366, (2019/12/04)
This invention is directed to selective androgen receptor degrader (SARD) compounds including heterocyclic rings and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedys disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.