849675-66-7Relevant academic research and scientific papers
Discovery of Encequidar, First-in-Class Intestine Specific P-glycoprotein Inhibitor
Smolinski, Michael P.,Urgaonkar, Sameer,Pitzonka, Laura,Cutler, Murray,Lee, GwanSun,Suh, Kwee Hyun,Lau, Johnson Y. N.
, p. 3677 - 3693 (2021/04/12)
Many chemotherapeutics, such as paclitaxel, are administered intravenously as they suffer from poor oral bioavailability, partly because of efflux mechanism of P-glycoprotein in the intestinal epithelium. To date, no drug has been approved by the U.S. Foo
ALTERNATE PROCESS FOR THE PREPARATION OF ENCEQUIDAR
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Page/Page column 10, (2020/11/30)
The aspect of the present application relate to process for the preparation of Encequidar (HM-30181A) and salts thereof. Specific aspects relate to an improved process for the Encequidar and its mesylate salt, comprising the amidation of aniline precursor of Encequidar of formula II using 4-oxo-4H-chromene-2-carboxylic acid in the presence of an activating agent.
SOLID STATE FORMS OF N-[2-(2-{4-[2-(6,7-DIMETHOXY-3,4-DIHYDRO-2(LH)- ISOQUINOLINYL)ETHYL] PHENYL }-2H-TETRAZOL-5-YL)-4,5-DIMETHOXYPHENYL] -4- OXO-4H-CHROMENE-2-CARBOXAMIDE AND OF ITS MESYLATE SALT
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Paragraph 00148; 00162, (2020/08/28)
The present disclosure relates to solid state forms of Encequidar (previously referred to as HM-30181A) base, Encequidar ((HM-30181A) mesylate, co-crystals of Encequidar (HM-30181A) mesylate, processes for preparation thereof, as well as pharmaceutical compositions including the same.
SOLID FORMS OF ENCEQUIDAR MESYLATE AND PROCESSES THEREOF
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Page/Page column 13; 14, (2020/10/17)
Aspects of the present application relate to solid forms of Encequidar, its mesylate salt and pharmaceutical compositions thereof. Specific aspects relate to the crystalline Form E1 of Encequidar, crystalline Form EM1, crystalline Form EM2 and crystalline Form EM3 of Encequidar mesylate. Further aspects relate to processes for the preparation of solid forms of Encequidar and its mesylate salt.
METHOD FOR PREPARING TETRAZOLE METHANESULFONIC ACID SALTS, AND NOVEL COMPOUND USED IN SAME
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, (2012/12/13)
According to the present invention, a method for preparing tetrazole methanesulfonic acid salts comprises an acylation reaction using a novel 4-iodine-4H-chromene-2-carbothionic acid S-benzothiazole-2-yl ester. The method of the present invention can shor
METHOD FOR PREPARING TETRAZOLE METHANESULFONIC ACID SALTS, AND NOVEL COMPOUND USED IN SAME
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, (2013/02/28)
According to the present invention, a method for preparing tetrazole methanesulfonic acid salts comprises an acylation reaction using a novel 4-iodine-4H-chromene-2-carbothionic acid S-benzothiazole-2-yl ester. The method of the present invention can shor
