13168-99-5Relevant academic research and scientific papers
IDO INHIBITORS
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Paragraph 2152, (2016/10/27)
There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
Design, synthesis, and evaluation of no-donor containing carbonic anhydrase inhibitors to lower intraocular pressure
Huang, Qinhua,Rui, Eugene Y.,Cobbs, Morena,Dinh, Dac M.,Gukasyan, Hovhannes J.,Lafontaine, Jennifer A.,Mehta, Saurabh,Patterson, Brian D.,Rewolinski, David A.,Richardson, Paul F.,Edwards, Martin P.
, p. 2821 - 2833 (2015/04/14)
The antiglaucoma drugs dorzolamide (1) and brinzolamide (2) lower intraocular pressure (IOP) by inhibiting the carbonic anhydrase (CA) enzyme to reduce aqueous humor production. The introduction of a nitric oxide (NO) donor into the alkyl side chain of do
INHIBITORS OF CARBONIC ANHYDRASE
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Page/Page column 39-40, (2009/03/07)
The invention relates to a compound of formula (I) and to pharmaceutically acceptable salts and solvates thereof. The invention also relates to methods of treating glaucoma, ocular hypertension, age-related macular degeneration, diabetic macular edema, di
Substituted quinazoline derivatives
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, (2008/06/13)
This invention provides compounds of formula 1 having the structure wherein: X, R1, R2, R3, R4, Z, X, and n are as defined hereinbefore in the specification, which are useful as antineoplastic agents and in the treatment of certain kidney diseases, such as polycystic kidney disease.
Wittig reactions in the presence of silica gel
Patil, Vijay J.,Maevers, Ursula
, p. 1281 - 1284 (2007/10/03)
Wittig reactions, of stable phosphorous ylids, when carried out in presence of silica gel, in hexane, provide a fast, efficient and simple method to obtain α:β unsaturated compounds in high yields and high purity.
Carbonylation of allylic ethers to esters
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, (2008/06/13)
A method is disclosed for the production of esters by reaction of an allylic ether with carbon monoxide in the presence of a catalytically effective amount of a Group VIII noble metal catalyst and halide compound to obtain esters. The halide compound is present in an amount sufficient to prevent the catalyst from being converted into a Group VIII metal during the reaction. When the reaction is conducted in the presence of a quaternary ammonium salt the ester may be extracted by solvent extraction to minimize catalyst decomposition caused when extractive distillation is used to separate the ester.
Inversion de polarite par les groupes phosphore: inversion de regioselectivite dans l'addition des nucleophiles sur les allenes actives par des groupes attracteurs
Cristau, Henri-Jean,Viala, Jacques,Christol, Henri
, p. 980 - 998 (2007/10/02)
Change in the regioselectivity of the addition of nucleophilic compounds YH (ROH, RSH, RNH2) on α-allenic ketones and esters can be effected by using the triphenylphosphonio group as an umpolung agent.In this way α,β-unsaturated ketones and esters are obtained with heteroatomic substituents in the γ position.The umpolung scheme of the activated allene is characterized by a vinylphosphonium salt 7 or 10 as a synthetic equivalent of the a4 synthon .CH2-CH=CH-Z.The synthetic process requires three (Z = COCH3) or two (Z = CO2CH3) distinct manipulations and gives good overall yields (63 to 71percent).This umpolung method can also be applied to binucleophilic compounds as a new synthesis for functional heterocycles such as the substituted dioxan 15c or pyrrole 16d.Two separate side reactions of the intermediary phosphonium salts were found to occur: a) the isomerization of the vinylphosphonium salts with migration of the double bond, and, b) for β-substituted phosphonium salts, exchange of heteroatomic groups Y through elimination-addition.Both side reactions can however be completely controlled.
