157252-27-2Relevant academic research and scientific papers
5,8-DISUBSTITUTED-[1,2,4]TRIAZOLO[1,5-A]PYRIDINYL AND 5,8-DISUBSTITUTED-IMIDAZO[1,2-A]PYRIDINE DERIVATIVES USEFUL AS INHIBITORS OF ENTEROPEPTIDASE
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, (2021/01/29)
The present invention is directed to 5,8-disubstituted-[1,2,4]triazolo[1,5- a]pyridinyl and 5,8-disubstituted-imidazo[1,2-a]pyridine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the enteropeptidase enzyme.
Discovery of a novel series of guanidinebenzoates as gut-restricted enteropeptidase and trypsin dual inhibitors for the treatment of metabolic syndrome
Zhang, Xuqing,Zhu, Bin,Sun, Weimei,Wang, Mina,Albarazanji, Kamal,Ghosh, Brahma,Cummings, Maxwell,Lenhard, James,Leonard, James,Macielag, Mark,Lanter, James
, (2021/03/22)
A novel series of guanidinebenzoate enteropeptidase and trypsin dual inhibitors has been discovered and SAR studies were conducted. Optimization was focused on improving properties for gut restriction, including increased aqueous solubility, lower cellular permeability, and reduced oral bioavailability. Lead compounds were identified with efficacy in a mouse fecal protein excretion study.
IMIDAZOLINYLMETHYL ARALKYLSULFONAMIDES
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Page 20-21, (2010/02/06)
Compounds of the Formula: where R1-R6 are those defined herein and methods for producing the same. Also provided are pharmaceutical compositions comprising a Compound of Formula I and methods for their use as therapeutic agents.
Intermolecular photoaddition reaction of arenecarbothioamides to 2- methoxy- and 2-trimethylsiloxyfurans. Facile synthesis of arene-fused aminobenzoates by novel photoinduced benzannulation
Oda, Kazuaki,Sakai, Masayuki,Machida, Minoru
, p. 584 - 589 (2007/10/03)
Irradiation of arenecarbothioamides with 2-methoxyfuran in benzene solution gave arene-fused aminobenzoates in moderate yields accompanied by small amounts of arylpyrroles or arylthiophenes. In the case of 2- trimethylsiloxyfuran, arenecarbothioamides gave arene-fused aminobenzoates in good yields as sole products. It was demonstrated that certain furan derivatives are potentially useful as building blocks in photoinduced benzannulation.
Benzannulation of Heteroaromatics by Photoreaction of Arenecarbothioamides with 2-Methoxyfuran
Oda, Kazuaki,Machida, Minoru
, p. 1477 - 1478 (2007/10/02)
Irradiation of arenecarbothioamides 1 with 2-methoxyfuran 2 in benzene solution gives benzo-fused arene derivatives 3 in moderate yields.
