66582-32-9Relevant academic research and scientific papers
IMPROVED PROCESS FOR THE PREPARATION OF TEZACAFTOR INTERMEDIATE
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Page/Page column 11-12, (2021/03/05)
The present invention relates to an improved process for the preparation of tezacaftor intermediate compound of formula II. More particularly, the present invention relates to an improved, commercially viable process for the preparation of tezacaftor inte
Evaluation of the Pharmacophoric Role of the O-O Bond in Synthetic Antileishmanial Compounds: Comparison between 1,2-Dioxanes and Tetrahydropyrans
Ortalli, Margherita,Varani, Stefania,Cimato, Giorgia,Veronesi, Ruben,Quintavalla, Arianna,Lombardo, Marco,Monari, Magda,Trombini, Claudio
, p. 13140 - 13158 (2020/11/13)
Leishmaniases are neglected diseases that can be treated with a limited drug arsenal; the development of new molecules is therefore a priority. Recent evidence indicates that endoperoxides, including artemisinin and its derivatives, possess antileishmanial activity. Here, 1,2-dioxanes were synthesized with their corresponding tetrahydropyrans lacking the peroxide bridge, to ascertain if this group is a key pharmacophoric requirement for the antileishmanial bioactivity. Newly synthesized compounds were examined in vitro, and their mechanism of action was preliminarily investigated. Three endoperoxides and their corresponding tetrahydropyrans effectively inhibited the growth of Leishmania donovani promastigotes and amastigotes, and iron did not play a significant role in their activation. Further, reactive oxygen species were produced in both endoperoxide-and tetrahydropyran-Treated promastigotes. In conclusion, the peroxide group proved not to be crucial for the antileishmanial bioactivity of endoperoxides, under the tested conditions. Our findings reveal the potential of both 1,2-dioxanes and tetrahydropyrans as lead compounds for novel therapies against Leishmania.
Stereoselective Synthesis of γ-Butyrolactones Subunit of Polycavernoside A
Kadari, Sudhakar,Yerrabelly, Hemasri,Gogula, Thirupathi,Erukala, Yadaiah Goud,Yerrabelly, Jayaprakash Rao,Begari, Prem Kumar
, p. 1986 - 1990 (2018/08/01)
An efficient and versatile linear synthesis of γ-butyrolactone subunit of polycavernolide A has been reported in 14.2% overall yield with 10 linear steps by employing Sharpless asymmetric epoxidation, ring-closing metathesis, and diastereoface selective h
SUBSTITUTED PYRAZOLOAZEPIN-8-ONES AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS
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Page/Page column 50, (2018/07/05)
The present invention relates to novel pyrazoloazepin-8-ones with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.
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 (2017/03/08)
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.
SUBSTITUTED TRICYCLICS AND METHOD OF USE
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Paragraph 1274, (2017/02/09)
The present invention provides for compounds of formula (I) wherein X, Y, and R1 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sj?gren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).
PYRAZOLYL SUBSTITUTED TETRAHYDROPYRANYLSULFONES
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Paragraph 0468; 0469, (2017/05/14)
The invention relates to pyrazolyl substituted tetrahydropyranylsulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
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Paragraph 00435, (2016/04/20)
Described herein are compounds of Formula (S-I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
Regioselective dihydropyran formation from 4-iodo-2,6-disubstituted tetrahydropyran derivatives using In(OAc)3/LiI system as the promoter
Chalopin, Thibaut,Jebali, Khaoula,Gaulon-Nourry, Catherine,Dénès, Fabrice,Lebreton, Jacques,Mathé-Allainmat, Monique
supporting information, p. 318 - 327 (2015/12/30)
The rapid and regioselective synthesis of a series of 2,6-disubstituted dihydropyranic building-blocks bearing an oxygenated side chain is described. The corresponding 4-iodo tetrahydropyran precursors, easily prepared by Prins cyclization, underwent regi
MULTICYCLIC COMPOUNDS AND METHODS OF USING SAME
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Paragraph 00509, (2015/04/15)
The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of
