229625-50-7Relevant articles and documents
Synthesis and evaluation of prodrugs of corticotropin-releasing factor-1 (CRF1) receptor antagonist BMS-665053 leading to improved oral bioavailability
Hartz, Richard A.,Vrudhula, Vivekananda M.,Ahuja, Vijay T.,Grace, James E.,Lodge, Nicholas J.,Bronson, Joanne J.,Macor, John E.
, p. 1360 - 1363 (2017)
A series of phosphate and ester-based prodrugs of anilinopyrazinone 1 (BMS-665053) containing either a methylene or an (acyloxy)alkoxy linker was prepared and evaluated in rat pharmacokinetic studies with the goal of improving the oral bioavailability of the parent (1). The prodrugs, in general, had improved aqueous solubility and oral bioavailability compared to 1. Prodrug 12, which contains an (acyloxy)alkoxy linker, showed the greatest improvement in the oral bioavailability relative to the parent (1), with a seven-fold increase (from 5% to 36%) in rat pharmacokinetic studies.
A novel synthetic route for the preparation of alkyl and benzyl chloromethyl phosphates
M?ntyl?, Antti,Veps?l?inen, Jouko,J?rvinen, Tomi,Nevalainen, Tapio
, p. 3793 - 3794 (2002)
An efficient and simple synthesis is described for the production of various chloromethyl phosphates as useful reagents for the preparation of phosphonooxymethyl prodrugs.
PRODRUGS IN THE MODULATION OF INTERLEUKIN
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Page/Page column 33-34, (2021/02/12)
There are disclosed prodrugs of the compounds of the formula. The prodrugs are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.
TRIAZOLE ANTIMICROBIAL DERIVATIVE, PHARMACEUTICAL COMPOSITION AND USE THEREOF
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, (2020/01/04)
The present disclosure provides a triazole antibacterial derivative and a pharmaceutical composition thereof and a use thereof and in particular relates to a compound represented by the following formula (I), and a racemate, a stereoisomer, a tautomer, an oxynitride or a pharmaceutically acceptable salt thereof: The compound of the present disclosure has a desirable water solubility and can be formulated into an injection for use without adding a cosolvent having a potential safety risk (such as hydroxypropyl-β-cyclodextrin, sulfobutylether-β-cyclodextrin, and the like), facilitating drug administration for patients, and greatly improving clinical safety. The drug can be used even by patients with moderate or severe renal impairment, thereby expanding the application scope of the drug.
POMALIDOMIDE DERIVATIVES AND THE PREPARING METHOD THEREOF
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Paragraph 0111-0113, (2019/08/01)
The invention relates to pomalidomide derivatives and their stereoisomers or pharmaceutically acceptable salts, and their use in preparing medicaments for treating cancers.