32560-59-1Relevant academic research and scientific papers
Hybrid dopamine uptake blocker-serotonin releaser ligands: A new twist on transporter-focused therapeutics
Blough, Bruce E.,Landavazo, Antonio,Partilla, John S.,Baumann, Michael H.,Decker, Ann M.,Page, Kevin M.,Rothman, Richard B.
supporting information, p. 623 - 627 (2014/07/07)
As part of our program to study neurotransmitter releasers, we report herein a class of hybrid dopamine reuptake inhibitors that display serotonin releasing activity. Hybrid compounds are interesting since they increase the design potential of transporter related compounds and hence represent a novel and unexplored strategy for therapeutic drug discovery. A series of N-alkylpropiophenones was synthesized and assessed for uptake inhibition and release activity using rat brain synaptosomes. Substitution on the aromatic ring yielded compounds that maintained hybrid activity, with the two disubstituted analogues (PAL-787 and PAL-820) having the most potent hybrid activity.
NEW BICYCLIC DIHYDROISOQUINOLINE-1-ONE DERIVATIVES
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Page/Page column 127, (2013/06/27)
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4? R5, R6, A1, A2, A3, A4, A5 and n are as described herein,compositions including the compounds and methods of using the compounds as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrom.
Method of treating nausea and vomiting with certain substituted-phenylalkylamino (and aminoacid) derivatives and other serotonin depleting agents
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, (2008/06/13)
A method for the treatment of emesis in a mammal, which method comprises administering to said mammal an emesis inhibiting amount of a compound which depletes serotonin in the brain of mammals; among which are compounds having the formula: STR1 wherein, R is selected from hydrogen, loweralkyl, trifluoromethyl, carboxyl, or loweralkoxycarbonyl; R1 and R2 are hydrogen or loweralkyl; Z is trifluoromethyl or halogen; the optical isomers and pharmaceutically acceptable salts thereof; two of the preferred compounds of the invention are fenfluramine and norfenfluramine.
Phenylalkylamines and phenylalkylureas in combinations to suppress gastric bleeding in aspirin therapy
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, (2008/06/13)
Novel pharmaceutical methods, combinations and compositions for reducing gastric bleeding during aspirin therapy for inflammation are disclosed. Compounds used in combination with aspirin are phenylalkylamines and phenylalkylureas having the formula: STR1 wherein Z is selected from the group consisting of --NHR2 or STR2 and R is selected from the group consisting of hydrogen, halogen, lower-alkoxy and trifluoromethyl and R1, R2, R3 and R4 are selected from the group consisting of hydrogen and lower-alkyl, where R3 and R4 taken together with the adjacent nitrogen atom may form a heterocyclic ring selected from the group of piperidino, pyrrolidino, piperazino, and morpholino.
