1201657-32-0Relevant articles and documents
Carbon-14 radiolabelling and tissue distribution evaluation of a potential anti-TB compound
Sonopo, Molahlehi S.,Venter, Kobus,Winks, Susan,Marjanovic-Painter, Biljana,Morgans, Garreth L.,Zeevaart, Jan R.
, p. 264 - 269 (2016)
This paper describes a five-step synthesis of a carbon-14-labelled pyrazole compound (11). A total of 2.96 MBq of 11 was obtained with the specific activity of 2242.4 MBq/mmol. The radiochemical purity was >99%, and the overall radiochemical yield was 60% based on the [14C6] 4-bromoaniline starting material. Biodistribution results showed that the radiotracer (administrated orally) has a high accumulation in the small intestine, large intestine and liver of both non-infected and tuberculosis (TB)-infected mice. Therefore, this suggests that compound 11 undergoes hepatobiliary clearance. The compound under investigation has been found to be slowly released from the liver between 2 and 8 h. The study revealed that 11 has no affinity for TB cells.
Fused tricyclic compounds and application thereof in medicaments
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Paragraph 0358-0362, (2020/03/17)
The invention relates to fused tricyclic compounds and an application thereof in medicaments, and in particular to an application of the fused tricyclic compounds in medicaments for treating and/or preventing hepatitis B. In particular, the invention rela
FUSED TRICYCLIC COMPOUNDS AND USES THEREOF IN MEDICINE
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Paragraph 00209, (2020/03/23)
The present invention relates to a fused tricyclic compound and application thereof in medicine, especially as a medicament for the treatment and/or prevention of hepatitis B. Specifically, the present invention relates to a compound having Formula (I) or
Manufacture of the PI3K β-Sparing Inhibitor Taselisib. Part 2: Development of a Highly Efficient and Regioselective Late-Stage Process
St-Jean, Frédéric,Remarchuk, Travis,Angelaud, Rémy,Carrera, Diane E.,Beaudry, Danial,Malhotra, Sushant,McClory, Andrew,Kumar, Archana,Ohlenbusch, Gerd,Schuster, Andreas M.,Gosselin, Francis
, p. 783 - 793 (2019/04/01)
A highly efficient and regioselective manufacturing route for the phosphoinositide 3-kinase β-sparing inhibitor taselisib was developed. Highlights of the synthesis include: (1) magnesium-mediated formation of a challenging cyclic amidine; (2) regioselect
DGAT1 INHIBITOR AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0213; 0220, (2016/08/23)
The present invention discloses a novel DGAT1 inhibitor, especially the compound of formula (I) or a pharmaceutically acceptable salt thereof, preparation and pharmaceutical composition thereof, as well as their uses in the preparation of a medicament for the prevention and treatment of Familial hyperchylomicronemia (FCS), obesity, hyperlipoproteinemia or hypertriglyceridemia.
HETEROARYL COMPOUNDS AND PHARMACEUTICAL APPLICATIONS THEREOF
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Paragraph 00710, (2016/01/25)
The present invention provides herein is a heteroaryl compound or a stereoisomer, a geometric isomer, a tautomer, a racemate, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, as well as a pharmaceutical composition containing the compound disclosed herein. The present invention also provides herein is use of the compound or the pharmaceutical composition thereof disclosed herein in the manufacture of a medicine for treating autoimmune diseases or proliferative diseases.
THERAPEUTIC COMPOUNDS AND USES THEREOF
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Page/Page column 124; 125, (2016/05/02)
The present invention relates to compounds of formula (I): and to salts thereof, wherein A has any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
PROCESS FOR MAKING BENZOXAZEPIN COMPOUNDS
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Page/Page column 14; 28, (2014/09/29)
Processes are described for the preparation of PI3K inhibitor, GDC-0032, Formula (I), having the structure: Formula (I) (GDC-0032), and intermediates useful for the preparation of (I).
IMIDAZOPYRIDINE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSINE KINASES
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Page/Page column 132-133, (2010/01/07)
The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
BICYCLIC TRIAZOLES AS PROTEIN KINASE MODULATORS
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Page/Page column 110, (2008/12/05)
The present disclosure provides bicyclic triazole protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity.