- CERAMIDE GALACTOSYLTRANSFERASE INHIBITORS FOR THE TREATMENT OF DISEASE
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Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with the enzyme ceramide galactosyltransferase (CGT), such as, for example, lysosomal storage diseases. Examples of lysosomal storage diseases include, for example, Krabbe disease and Metachromatic Leukodystrophy.
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Paragraph 000458; 000460; 000568; 000570
(2018/01/17)
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- Indium-mediated regioselective synthesis of ketones from arylstannanes under solvent-free ultrasound irradiation
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The solvent-free indium-promoted reaction of alkanoyl chlorides with sterically and electronically diverse arylstannanes is a simple and direct method for the regioselective synthesis of primary, secondary and tertiary alkyl aryl ketones in good to excellent isolated yields (42-84%) under mild and neutral conditions. The protocol is also adequate for the synthesis of aryl vinyl ketones. Reaction times are drastically reduced (from 3-32 h to 10-70 min) under ultrasonic irradiation. Evidences for the involvement of a homolytic aromatic ipso-substitution mechanism, in which indium metal acts as radical initiator, are presented. It is possible the transference of two aryl groups from tin, thus improving effective mass yield, working with diarylstannanes as starting substrates.
- Lo Fiego, Marcos J.,Badajoz, Mercedes A.,Domini, Claudia,Chopa, Alicia B.,Lockhart, María T.
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p. 826 - 832
(2013/03/14)
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- MONOAM1NE REUPTAKE INHIBITORS
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The invention provides bupropion analogue compounds capable of inhibiting the reuptake of one or more monoamines. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine,and serotonin. Such compounds may be used to treat conditions that are responsive to inhibition of the reuptake of monoamines, including addiction, depression, and obesity
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Page/Page column 48
(2010/11/04)
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- Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction
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A series of bupropion (1a) analogues (1b-1ff) were synthesized, and their in vitro and in vivo pharmacological properties evaluated with the goal of developing a 1a analogue that had better properties for treating addictions. Their in vitro pharmacological properties were examined by [3H] dopamine ([3H]DA), [3H]serotonin ([3H]5HT), and [3H]norepinephrine ([3H]NE) uptake inhibition studies, and by binding studies at the dopamine, serotonin, and norepinephrine transporters using [125I]RTI-55 in cloned transporters. Several analogues showed increased [3H]DAuptake inhibition with reduced or little change in [3H]5HT and [3H]NE uptake inhibition relative to bupropion. Thirty-five analogues were evaluated in a 1 h locomotor activity observation test and 32 in an 8 h locomotor activity observation test and compared to the locomotor activity of cocaine. Twenty-four analogues were evaluated for generalization to cocaine drug discrimination after i.p. administration, and twelve analogues were tested in a time course cocaine discrimination study using oral administration. 2-(N-Cyclopropylamino)-3- chloropropiophenone (1x) had the most favorable in vitro efficacy and in vivo pharmacological profile for an indirect dopamine agonist pharmacotherapy for treating cocaine, methamphetamine, nicotine, and other drugs of abuse addiction. 2009 American Chemical Society.
- Carroll, F. Ivy,Blough, Bruce E.,Abraham, Philip,Mills, Andrew C.,Holleman, J. Ashley,Wolckenhauer, Scott A.,Decker, Ann M.,Landavazo, Antonio,McElroy, K. Timothy,Navarro, Hernán A.,Gatch, Michael B.,Forster, Michael J.
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supporting information; experimental part
p. 6768 - 6781
(2010/04/06)
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- Control of parasites in animals by the use of novel trifluoromethanesulfonanilide oxime ether derivatives
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Novel trifluoromethanesulfonanilide oxime ether compounds useful for controlling endo and/or ectoparasites in the environment are provided, together with methods of making the same, and methods of using the inventive compounds to treat parasite infestations in vivo or ex vivo.
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Page/Page column 33; 8/12
(2010/10/20)
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- Synthesis and evaluation of the anticonvulsant activity of a series of 2-amino-1-phenyl-1-propranols derived from the metabolites of the antidepressant bupropion
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A series of 2-amino-1-phenyl-1-propanols that are structurally related to known metabolites of bupropion, 1 (Wellbutrin) were synthesized and evaluated as potential anticonvulsants. The (R*,R*)-2-tert-butylamino-1-(3-trifluoromethylphenyl) propanol 20 had an ED50 of 16.5 ± 2.8 mg/kg ip in mice in the maximal electroshock screen and was chosen for further evaluation.
- Musso, David L.,Mehta, Nariman B.,Soroko, Francis E.
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