19054-67-2Relevant academic research and scientific papers
A new class of antiarrhythmic-defibrillatory agents
Levy, Ofra,Erez, Mordechai,Varon, Dalia,Keinan, Ehud
, p. 2921 - 2926 (2001)
Novel dibenzoazepine and 11-oxo-dibenzodiazepine derivatives are shown to be effective ventricular defibrillating drug candidates. They exhibit significant in vivo defibrillatory activity with no observed changes in ECG either before or after the VF event. These compounds also exhibit antifibrillatory activity by elevating the fibrillation threshold potential, all suggesting that such drugs could be used to treat VF either by themselves or together with electrical defibrillators.
HECT E3 LIGASE INHIBITORS AND USES THEREOF
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Page/Page column 48; 53-54, (2020/12/29)
The present invention relates to tricyclic derivatives of formula (I), which are useful as inhibitors of HECT-domain-containing E3 ligases, in particular NEDD4. The present invention also refers to pharmaceutical compositions comprising compounds of formu
Tricyclic compounds and their uses as antiarrhythmic antifibrillatory and defibrillatory agents
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Page/Page column 7-8, (2010/02/12)
A compound having a general formula (II) wherein R1is saturated or unsaturated alkyl, amino-alcohol, diamino, cycloalkyl, and C(═O)(CH2)nNR′R″, (CH2)nCHOHCH2NR′R″, wherein n is an integer, RQ, RT, R′, and R″ are each independently a hydrogen, halogen, hydroxyl, saturated, unsaturated, aliphatic, or branched alkyl, substituted or unsubstituted (CH2)m-(hetero)aryl, and sulfonylamide; q and r are each an integer independently selected from 1-4; and pharmaceutically acceptable salts thereof, and the new therapeutic uses thereof and similar compounds as defibrillating, and/or anti-fibrillatory, and/or anti-arrhythmic and/or anti-ischemic drugs.
N-Substituted azaheterocyclic compounds
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, (2008/06/13)
The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Y, Z, A, R1, R2, r and s are as defined in the detailed part of the present description or salts thereof, to methods for
N-substituted azaheterocyclic carboxylic acids and esters thereof
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, (2008/06/13)
The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene
Runyon, Scott P.,Savage, Jason E.,Taroua, Mohamed,Roth, Bryan L.,Glennon, Richard A.,Westkaemper, Richard B.
, p. 655 - 658 (2007/10/03)
Comparison of the serotonin 5-HT2A receptor affinities of chain lengthened and N-alkylated analogues of the novel ligand 9-aminomethyl-9.10-dihydroanthracene (AMDA) and a structurally similar prototypical tricyclic amine imipramine suggests that the two agents bind to the receptor in different fashions. The demonstration that AMDA is highly selective for serotonin receptors (5-HT2A, Ki = 20 nM: 5-HT2C, Ki = 43 nM) versus the dopamine D2 receptor (Ki > 10,000 nM). as well as the serotonin and norepinephrine transporters (Ki >10.000nM) further suggests that AMDA and the nonselective ligand imipramine interact with these target macromolecules in different ways.
HETEROCYCLIC COMPOUNDS FOR TREATING DIABETES
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, (2008/06/13)
The present invention relates to novel N-substituted amino acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use fo
Substituted dibenz[b,f]azepines and uses thereof
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, (2008/06/13)
The present invention relates to novel N-substituted azaheterocyclic carboxylic acids andy esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
Tricyclic compounds in treating hyperalgesic conditions and NIDDM
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, (2008/06/13)
The present invention relates to novel N-substituted amino acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use fo
The synthesis of non-exchangeable deuterated internal standards for imipramine and its metabolites
Woodard,Cymerman Craig
, p. 321 - 333,324, 326 (2007/10/04)
The synthesis of 10,11-dihydro-5-(3-dimethylaminopropyl)-5H-dibenz[b,f]azepine (imipramine) and its 3-methylamino analogue (desipramine) labelled with deuterium in either the 1- or the 3-position of the side chain in high isotopic purity is described. The 3,3-d2 compounds are obtained from the common precursor 5-(2-cyanoethyl)-10, 11-dihydro-5H-dibenz[b,f]azepine by reduction and alkylation, while the 1,1-d2 products are accessible from the 5-(3-chloropropionyl) derivative by amination and reduction. These compounds are required for use as non-exchangeable mass spectrometric stable isotope internal standards for the simultaneous determination of imipramine and desipramine in biological fluids.
