57381-36-9Relevant articles and documents
CRYSTALLINE ALK5 INHIBITORS AND USES THEREOF
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, (2021/12/29)
The present disclosure provides crystalline forms of activin receptor-like kinase 5 (ALK5) inhibitors. Also disclosed are pharmaceutical compositions comprising the crystalline forms, methods of using the crystalline forms to modulate the activity of ALK5 and methods of treating disorders mediated by ALK5 using the crystalline forms.
ALK5 INHIBITORS
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Paragraph 0479; 0537; 0538, (2020/07/07)
The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.
Preparation method of halogenated benzothiazepine compound as well as product prepared by preparation method and application of halogenated benzothiazepine compound
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Paragraph 0052-0056; 0072-0076; 0077-0079; 0082-0083, (2020/09/02)
The invention discloses a preparation method of a halogenated benzothiazepine compound as well as a product prepared by the preparation method and an application of the halogenated benzothiazepine compound, and relates to the technical field of chemical s
Structure determination, synthesis, and biological evaluation of a metabolite of the selective α1Dadrenoceptor antagonist TAK-259
Sato, Ayumu,Sakauchi, Nobuki,Shirai, Junya,Furukawa, Hideki,Hara, Miki,Miwa, Katsuhiko,Fujita, Hisashi,Miyamoto, Maki,Tada, Norio,Kuno, Haruhiko,Kameoka, Nagako,Maezaki, Hironobu
, p. 6334 - 6339 (2016/09/23)
5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide hydrochloride (TAK-259) is a novel, selective, and orally active α1Dadrenoceptor antagonist with anti-urinary frequency effect. A metabolite (2) of TAK-259 was identified from monkey urine samples. To elucidate the structure of 2, extraction and purification of the metabolite from TAK-259-treated monkey urine was conducted. Structural analysis of the purified compounds using NMR indicated the compound to be 2-amino-5-chloro-1-[5-chloro-2-(methylsulfonyl)benzyl]-4-oxo-1,4-dihydropyridine-3-carboxamide (2a). An authentic sample of compound 2a was synthesized via regioselective alkylation of 4-methoxypyridin-2-amine. The biological activity of metabolite 2a was also evaluated, and the compound found not to possess affinity toward any known α1adrenoceptor subtype.
NEW COMPOUNDS
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Page 139, (2010/02/06)
The present invention relates to new compounds of formula I, (I) a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
NEW COMPOUNDS
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Page/Page column 61, (2010/11/30)
The present invention relates to new compounds of formula (I), wherein P, Q, X1, X2, X3, X4, R, R1, R2, R3, R4, R5, R6, R7, m, n, o, p and q are defined as in any one of claims 1 to 12, a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
Aryl triazines as LPAAT-SS inhibitors and uses thereof
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, (2008/06/13)
The invention relates to aryl triazines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase β (LPAAT-β) activity and/or proliferation of cells such as tumor cells.