- Experimental studies of spatial patterns produced by diffusion-convection-reaction systems
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The reactions between chlorite ions and a series of sulfur compounds are bistable and autocatalytic in hypochlorous acid. Unstirred solution mixtures of chlorite ions and thiourea, for example, can generate a travelling wave of chemical reactivity at the surface from a point of initial perturbation These reactions are highly exothermic and exhibit a sharp temperature jump at the wave front (ΔT ≈ 3-5°C). In stoichiometric excess of chlorite ions and in unstirred solutions the travelling wave is followed by spatial patterns in the bulk of the solution. The spatial patterns, which show areas of varying acid concentrations, can be sustained for up to 15 min. Formation of the travelling wave is due to thermocapillary effects. The transition to patterns is fuelled by the coupling of buoyancy forces with thermocapillary convection.
- Chinake, Cordelia R.,Simoyi, Reuben H.
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Read Online
- 1,2,4-TRIAZOLINOE CB1 INHIBITORS
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Disclosed are compounds according to Formula (I), and related pharmaceutical compositions. Also disclosed are therapeutic methods, e.g., of treating diseases such as diabetic kidney disease, diabetic nephropathy, obesity-related kidney disease, focal segmental glomerular sclerosis, IgA nephropathy, nephrotic syndrome, kidney fibrosis, Prader Willi syndrome, metabolic syndrome, gastrointestinal diseases, non-alcoholic liver disease, alcoholic liver disease, or non-alcoholic fatty liver disease, using the compounds of Formula (I).
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Page/Page column 45
(2021/09/11)
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- Highly efficient synthesis of hiv nnrti doravirine
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The development of an efficient and robust process for the production of HIV NNRTI doravirine is described. The synthesis features a continuous aldol reaction as part of a de novo synthesis of the key pyridone fragment. Conditions for the continuous flow aldol reaction were derived using microbatch snapshots of the flow process.
- Gauthier, Donald R.,Sherry, Benjamin D.,Cao, Yang,Journet, Michel,Humphrey, Guy,Itoh, Tetsuji,Mangion, Ian,Tschaen, David M.
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supporting information
p. 1353 - 1356
(2015/03/30)
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- PROCESS FOR MAKING REVERSE TRANSCRIPTASE INHIBITORS
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The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase and HIV replication, and the treatment of human immunodeficiency virus infection in humans.
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Page/Page column 13
(2015/06/18)
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- HETEROCYCLIC HYDRAZONE COMPOUNDS AND THEIR USES TO TREAT CANCER AND INFLAMMATION
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The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
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Page/Page column 65-66
(2011/02/24)
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- Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?
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Starting from potent aldehyde inhibitors with poor drug properties, derivatization to semicarbazones led to the identification of a series of semicarbazone-based cathepsin K inhibitors with greater solubility and better pharmacokinetic profiles than their parent aldehydes. Furthermore, a representative semicarbazone inhibitor attenuated bone resorption in an ex vivo rat calvarial bone resorption model. However, based on enzyme inhibition comparisons at neutral pH, semicarbazone hydrolysis rates, and 13C NMR experiments, these semicarbazones probably function as prodrugs of aldehydes.
- Adkison, Kim K.,Barrett, David G.,Deaton, David N.,Gampe, Robert T.,Hassell, Anne M.,Long, Stacey T.,McFadyen, Robert B.,Miller, Aaron B.,Miller, Larry R.,Payne, J. Alan,Shewchuk, Lisa M.,Wells-Knecht, Kevin J.,Willard Jr., Derril H.,Wright, Lois L.
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p. 978 - 983
(2007/10/03)
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- Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof
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This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention also is directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.
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- Nonlinear dynamics in the oxidations of substituted thioureas. I: The reaction of 4-methyl-3-thiosemicarbazide with acidic iodate
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The substituted thiourea, 4-methyl-3-thiosemicarbazide was oxidized by iodate in acidic medium. In high acid concentrations and in stoichiometric excess of iodate, the reaction displays an induction period followed by the formation of aqueous iodine. In stoichiometric excess of methylthiosemicarbazide and high acid concentration, the reaction shows a transient formation of aqueous iodine. Iodine formation is due to the Dushman reaction that produces iodine from iodide formed from the reduction of iodate. Transient iodine formation is due to the efficient acid catalysis of the Dushman reaction. The iodine produced is consumed by the methylthiosemicarbazide substrate. The direct reaction of iodine and methylthiosemicarbazide was also studied.
- Mundoma, Claudius,Simoyi, Reuben H.
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p. 193 - 203
(2007/10/03)
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