164033-11-8Relevant articles and documents
THERAPEUTIC COMPOUNDS AND COMPOSITIONS
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Page/Page column 126; 132, (2019/08/29)
The present invention provides compounds that inhibit Factor XIa or kallikrein and pharmaceutically acceptable salts thereof and compositions thereof. The present invention also provides methods of using these compounds and compositions.
A modified Curtius reaction: an efficient and simple method for direct isolation of free amine
Ma, Bin,Lee, Wen-Cherng
experimental part, p. 385 - 386 (2010/03/03)
The Curtius rearrangement and related reactions are often used to convert carboxylic acids to the corresponding primary amines. However, this reaction often requires harsh conditions for hydrolysis of the isocyanate intermediates to amines, and can also be contaminated by the formation of corresponding ureas due to the reactive nature of the intermediates. We have discovered that by quenching the isocyanate intermediates with sodium trimethylsilanolate, the free amines can be isolated after aqueous workup. This mild and fast procedure provides free amines in one pot with good yields.
Design, synthesis and pharmacological evaluation of 3-benzylazetidine-2-one-based human chymase inhibitors
Aoyama, Yasunori,Uenaka, Masaaki,Kii, Makoto,Tanaka, Mamoru,Konoike, Toshiro,Hayasaki-Kajiwara, Yoko,Naya, Noriyuki,Nakajima, Masatoshi
, p. 3065 - 3075 (2007/10/03)
3-Benzylazetidine-2-one derivatives were designed and evaluated as a novel series of chymase inhibitors. Structure-activity relationship studies of 3-benzylazetidine-2-ones led to compounds 23, which exhibited 3.1nM inhibition of human chymase and enhancement of stability in human plasma (t1/2 6 h). Copyright