23692-08-2Relevant academic research and scientific papers
HEPATITIS B CORE PROTEIN MODULATORS
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Page/Page column 106, (2018/04/13)
The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound of formula:
TRICYCLIC FUSED PYRIMIDINE COMPOUNDS AS INHIBITORS OF p97 COMPLEX
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Paragraph 0473, (2017/09/29)
Tricyclic fused pyrimidine compounds having an arylalkyl amine substituent at the P4 position and a substituted 1H-indol-1-yl, 1H-indol-3-yl, indanyl, indazol-1-yl, indazol-3-yl, benzotriazol-1-yl or 1H-benz[d]imidazol-1-yl group at the P2 position well as optional aliphatic, functional and/or aromatic components substituted at other positions of the tricyclic compounds of the invention. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity such as cancer.
NEW ANTIBACTERIAL COMPOUNDS
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Page/Page column 79, (2014/03/21)
The present invention is related to novel compounds of formula (I) that may inhibit the activity of the FabI enzyme, and which are useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compound
NEW ANTIBACTERIAL COMPOUNDS
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Page/Page column 73, (2014/03/21)
The present invention is related to novel compounds of formula (I) that may inhibit the activity of the FabI enzyme, and which are useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compound
Synthesis of the quinolizidine alkaloids (-)-lasubine II and (±)-myrtine by conjugate addition and intramolecular acylation of amino esters with acetylenic sulfones
Back, Thomas G.,Hamilton, Michael D.,Lim, Vania J. J.,Parvez, Masood
, p. 967 - 972 (2007/10/03)
(Chemical Equation Presented) The conjugate additions of (2-piperidyl)acetate esters to acetylenic sulfones, followed by LDA-promoted intramolecular acylations, afforded cyclic enaminones that were readily converted into the corresponding 4-substituted 2-
Asymmetric synthesis of β-amino acids by addition of chiral enolates to nitrones via N-acyloxyiminium ions
Kawakami,Ohtake,Arakawa,Okachi,Imada,Murahashi
, p. 2423 - 2444 (2007/10/03)
N-Acyloxyiminium ions, generated by the reaction of nitrones with acyl halides, are highly reactive species and undergo facile reaction with a wide range of nucleophiles, such as ketene silyl acetals, titanium(IV) and boron enolates, hydrido- and allyltin(IV) reagents, and alkynyltitanium(IV) reagents, to give α-substituted amine derivatives. Optically active β-amino acids can be prepared by the reaction of N-acyloxyiminium ions with both boron and titanium(IV) enolates bearing chiral auxiliaries. Reversal of diastereoselectivity was observed by the reactions of the boron and titanium(IV) enolates. Using these reactions, all of the four stereoisomers of α-methyl-β-phenylalanines, for example, can be prepared highly diastereoselectively. Cyclic N-acyloxyiminium ions are useful for the asymmetric synthesis of pyrrolidine and piperidine alkaloids; (5R,8R,8aS)-5-cyano-8-methylindolizidine, which is a common key intermediate for synthesis of 5-substituted 8-methylindolizidines, was prepared selectively.
Ring constrained analogues of β-alanine-containing GPIIb/IIIa receptor antagonists
Sielecki, Thais M.,Wityak, John,Liu, Jie,Mousa, Shaker A.,Thoolen, Martin,Wexler, Ruth R.,Olson, Richard E.
, p. 449 - 452 (2007/10/03)
A series of ring constrained analogues of the GPIIb/IIIa receptor antagonist XR299 (1) was investigated as potential inhibitors of glycoprotein IIb/IIIa, a platelet receptor that plays a key role in platelet aggregation and platelet adhesion. Ring size was found to have a large effect on in vitro potency. Selected compounds showed good in vitro activity, a preference for binding to activated platelets, and modest duration of action when dosed iv as a racemate in a canine model. (C) 2000 DuPont Pharmaceuticals Company. Published by Elsevier Science Ltd. All rights reserved.
INTRAMOLECULAR CYCLIZATION OF ω-PRIMARY AMINO ELECTROPHILIC OLEFINS TO FUNCTIONALIZED PYRROLIDINES AND PIPERIDINES.
Knouzi, N.,Vaultier, M.,Toupet, L.,Carrie, R.
, p. 1757 - 1760 (2007/10/02)
The intramolecular 1,4-Michael type addition of in situ chemoselectively generated primary amines bearing an electrophilic double bond in the ω position leads to functionalized pyrrolidines and piperidines under very mild conditions.
