- Synthesis of 3H, 2H4 and 14C-SCH 417690 (Vicriviroc)
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Vicriviroc or SCH 417690 is a potent and selective antagonist of the CCR5 receptor. CCR5 receptor antagonists have the potential for the treatment of HIV infections. Four distinct isotopically labelled forms of SCH 417690 were synthesized. Low specific activity [3H]SCH 417690 was prepared for a preliminary absorption, distribution, metabolism and excretion evaluation of the compound and [14C]SCH 417690 for more definitive absorption, distribution, metabolism and excretion work, including an absorption, metabolism and excretion study in man. In addition, high specific activity [3H]SCH 417690 was prepared for CCR5 receptor binding work and [2H4]SCH 417690 was prepared as an internal standard for a liquid chromatography-mass spectrometry bioanalytical method. The paper discusses the synthesis of four isotopically labelled forms of SCH 417690.
- Hesk,Borges,Hendershot,Koharski,McNamara,Ren,Saluja,Truong,Voronin
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- DEUTERATED IRAK DEGRADERS AND USES THEREOF
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The present invention provides deuterium-enriched compounds, compositions thereof, and methods of using the same.
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Paragraph 00426; 00532-00534
(2021/12/12)
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- Synthetic method of 3-hydroxy desloratadine metabolite
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The invention discloses a synthetic method of 3-hydroxy desloratadine metabolite, belongs to the field of drug metabolism and provides a synthetic method, which is reasonable in technical design, highin operability and high in yield, which is suitable for
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Paragraph 0010
(2019/07/01)
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- Substituted diaminopyrimidine compound
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The present invention provides a substituted diaminopyrimidine compound represented by a formula (I), or a pharmaceutically acceptable salt, a crystal form, a prodrug, a metabolite, a hydrate, a solvate, a stereoisomer or an isotope derivative thereof, as well as a pharmaceutical composition and uses thereof. The compound provided by the invention can be used for treating ALK-mediated related diseases, such as non-small cell lung cancer, breast cancer, neural tumor, esophageal cancer, soft tissue cancer, lymphoma and leukemia.
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Paragraph 0253-0258
(2019/07/04)
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- Deuterium-Substituted Pyridin- And Pyrimidin-2-yl-Methylamine Compounds
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Described are deuterium-substituted pyridin- and pyrimidin-2-yl-methylamine compounds of structural Formula (I), which are agonists of 5-hydroxytryptamine receptors. Also described are pharmaceutical compositions comprising the deuterium-substituted pyridin- and pyrimidin-2-yl-methylamine compounds, and methods of use thereof.
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Paragraph 0383; 0384
(2018/04/14)
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- COMPOUNDS
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Provided are novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, compositions containing them and their use in the treatment of or prevention of diseases associated with or characterized by LRRK2 kinase activity, for examp
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Page/Page column 82
(2018/09/08)
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- Synthesis of [2H4]; [3H]; and [14C] SCH 900875: A potent CXCR3 antagonist with potential therapeutic use in the treatment of psoriasis
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2H4, 3H and 14C-syntheses of the potent CXCR3 antagonist Sch 900875 were performed in order to aid the biological evaluation of this compound. Copyright
- Galliford, Chris V.,Voronin, Kimberly,Smith, Amy,Koharski, David,Truong, Van,Borges, Scott,Lavey, Carolee Flader,Hesk, David,Mcnamara, Paul
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scheme or table
p. 388 - 391
(2011/05/04)
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