- Carbon-14 radiolabelling and tissue distribution evaluation of a potential anti-TB compound
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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.
- Sonopo, Molahlehi S.,Venter, Kobus,Winks, Susan,Marjanovic-Painter, Biljana,Morgans, Garreth L.,Zeevaart, Jan R.
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Read Online
- Fused tricyclic compounds and application thereof in medicaments
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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
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Paragraph 0358-0362
(2020/03/17)
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- FUSED TRICYCLIC COMPOUNDS AND USES THEREOF IN MEDICINE
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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
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Paragraph 00209
(2020/03/23)
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- Manufacture of the PI3K β-Sparing Inhibitor Taselisib. Part 2: Development of a Highly Efficient and Regioselective Late-Stage Process
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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
- 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
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p. 783 - 793
(2019/04/01)
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- DGAT1 INHIBITOR AND PREPARATION METHOD AND USE THEREOF
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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.
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Paragraph 0213; 0220
(2016/08/23)
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- HETEROARYL COMPOUNDS AND PHARMACEUTICAL APPLICATIONS THEREOF
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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.
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Paragraph 00710
(2016/01/25)
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- THERAPEUTIC COMPOUNDS AND USES THEREOF
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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.
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Page/Page column 124; 125
(2016/05/02)
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- PROCESS FOR MAKING BENZOXAZEPIN COMPOUNDS
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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).
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Page/Page column 14; 28
(2014/09/29)
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- IMIDAZOPYRIDINE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSINE KINASES
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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.
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Page/Page column 132-133
(2010/01/07)
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- BICYCLIC TRIAZOLES AS PROTEIN KINASE MODULATORS
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The present disclosure provides bicyclic triazole protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity.
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Page/Page column 110
(2008/12/05)
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