Latvian Institute of Organic Synthesis

Riga, Latvia

Latvian Institute of Organic Synthesis

Riga, Latvia
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Patent
Latvian Institute Of Organic Synthesis | Date: 2017-02-08

Use of 2-(5S-Methyl-2-oxo-4R-phenyl-pyrrolidin-1-yl)-acetamide or its pharmaceutically acceptable salt in manufacture of a medicament for prophylaxis and treatment of seizure.


Versilovskis A.,Latvian Institute of Organic Synthesis | de Saeger S.,Ghent University
Molecular Nutrition and Food Research | Year: 2010

Sterigmatocystin (STC) is a mycotoxin produced by fungi of many different Aspergillus species. Other species such as Bipolaris, Chaetomium, Emiricella are also able to produce STC. STC producing fungi were frequently isolated from different foodstuffs, while STC was regularly detected in grains, corn, bread, cheese, spices, coffee beans, soybeans, pistachio nuts, animal feed and silage. STC shows different toxicological, mutagenic and carcinogenic effects in animals and has been recognized as a 2B carcinogen (possible human carcinogen) by International Agency for Research on Cancer. There are more than 775 publications available in Scopus (and more than 505 in PubMed) mentioning STC, but there is no summary information available about STC occurrence and analysis in food. This review presents an overview of the worldwide information on the occurrence of STC in different foodstuffs during the last 40 years, and describes the progress made in analytical metho - dology for the determination of STC in food. © 2009 WILEY-VCH Verlag GmbH & Co.


Sokolovs I.,Latvian Institute of Organic Synthesis | Lubriks D.,Latvian Institute of Organic Synthesis | Suna E.,Latvian Institute of Organic Synthesis
Journal of the American Chemical Society | Year: 2014

A one-pot two-step method for intermolecular C-H amination of electron-rich heteroarenes and arenes has been developed. The approach is based on a room-temperature copper-catalyzed regioselective reaction of the in situ formed unsymmetrical (hetero)aryl-λ3-iodanes with a wide range of primary and secondary aliphatic amines and anilines. © 2014 American Chemical Society.


Arsenyan P.,Latvian Institute of Organic Synthesis
Tetrahedron Letters | Year: 2014

A simple strategy for the preparation of novel selenopheno[3,2-b] and [2,3-b]thiophenes by treatment of ethynylthiophenes with selenium(I), (II), and (IV) chlorides and bromides is elaborated. © 2014 Elsevier Ltd. All rights reserved.


Lubriks D.,Latvian Institute of Organic Synthesis | Sokolovs I.,Latvian Institute of Organic Synthesis | Suna E.,Latvian Institute of Organic Synthesis
Journal of the American Chemical Society | Year: 2012

A C-H bond of electron-rich heterocycles is transformed into a C-N bond in a reaction sequence comprising the formation of heteroaryl(phenyl)iodonium azides and their in situ regioselective fragmentation to heteroaryl azides. A Cu(I) catalyst ensures complete regiocontrol in the fragmentation step and catalyzes the subsequent 1,3-dipolar cycloaddition of the formed azido heterocycles with acetylenes. The heteroaryl azides can also be conveniently reduced to heteroarylamines by aqueous ammonium sulfide. The overall C-H to C-N transformation is a mild and operationally simple one-pot sequential multistep process. © 2012 American Chemical Society.


Kuka J.,Latvian Institute of Organic Synthesis
Journal of cardiovascular pharmacology and therapeutics | Year: 2012

Mildronate, an inhibitor of L-carnitine biosynthesis and uptake, is a cardioprotective drug whose mechanism of action is thought to rely on the changes in concentration of L-carnitine in heart tissue. In the present study, we compared the cardioprotective effect of mildronate (100 mg/kg) and a combination of mildronate and L-carnitine (100 + 100 mg/kg) administered for 14 days with respect to the observed changes in l-carnitine level and carnitine palmitoyltransferase I (CPT-I)-dependent fatty acid metabolism in the heart tissues. Concentrations of L-carnitine and its precursor γ-butyrobetaine (GBB) were measured by ultraperformance liquid chromatography with tandem mass spectrometry. In addition, mitochondrial respiration, activity of CPT-I, and expression of CPT-IA/B messenger RNA (mRNA) were measured. Isolated rat hearts were subjected to ischemia-reperfusion injury. Administration of mildronate induced a 69% decrease in L-carnitine concentration and a 6-fold increase in GBB concentration in the heart tissue as well as a 27% decrease in CPT-I-dependent mitochondrial respiration on palmitoyl-coenzyme A. In addition, mildronate treatment induced a significant reduction in infarct size and also diminished the ischemia-induced respiration stimulation by exogenous cytochrome c. Treatment with a combination had no significant impact on L-carnitine concentration, CPT-I-dependent mitochondrial respiration, and infarct size. Our results demonstrated that the mildronate-induced decrease in L-carnitine concentration, concomitant decrease in fatty acid transport, and maintenance of the intactness of outer mitochondrial membrane in heart mitochondria are the key mechanisms of action for the anti-infarction activity of mildronate.


Patent
Latvian Institute Of Organic Synthesis | Date: 2014-10-20

The invention relates to medicine, in particular S-Phenotropil ((S)-2-(2-oxo-4-phenylpyrrolidin-1-yl)acetamide) containing pharmaceutical compositions and their use in control of body mass gain.


Patent
Latvian Institute Of Organic Synthesis | Date: 2013-10-24

The invention discloses the use of pharmaceutical compositions containing 3-(2,2,2-trimethylhydrazinium)propionate dihydrate and pharmaceutically acceptable salts thereof for trimethylamine N-oxide level decrease in a body.


Patent
Latvian Institute Of Organic Synthesis | Date: 2013-06-11

The thieno[2,3-b]pyridines of general formula (I), wherein R^(1 )is Me, C_(6)H_(5), 3,4,5-(OMe)_(3)C_(6)H_(2), NH_(2);R^(2 )is H, CN, COMe, COOC_(1-4)alkyl, COOC_(2)H_(4)OMe, COOC_(2)H_(4)OPr(n);R^(3 )is C_(6)H_(4)R^(6), 3,4-OCH_(2)OC_(6)H_(3); 2-furanyl;


News Article | March 11, 2016
Site: motherboard.vice.com

Meldonium, the anti-ischemic drug that led to Maria Sharapova’s suspension, is witnessing a surge in popularity in the nootropics (“smart drugs”) community. “I have noticed a huge increase in meldonium sales over the last days; all people [are] coming in to buy meldonium,” Ricardas Tarvydas, who runs the website nootropic.eu, told me in a phone call from Lithuania, where he buys most of his products. Tarvydas explained that he usually sells just a couple of boxes of meldonium (also known as mildronate) every month; over the last 24 hours, though, he said he had received orders for 870 boxes. Some of Tarvydas’s customers explicitly mentioned Sharapova when placing their orders. The Russian tennis player revealed on Monday that she had tested positive for meldonium, also known as mildronate, which the World Anti-Doping Agency (WADA) banned last January. Sharapova claimed she hadn’t noticed the ban on the medicine, which she had been lawfully taking for a decade. The case has triggered a sudden spike in interest in meldonium online and rekindled the curiosity of the relatively niche “noonauts” community—folks looking to enhance their cognitive performance using nootropics. Just hours after Sharapova had made her announcement in Los Angeles, a post on the r/nootropics subreddit kickstarted the debate on whether meldonium could be used for “nootropic purposes” (to improve one’s brainpower as opposed to athletic ability.) Some users were sceptical; others were more positive, even recounting their personal experiences taking the drug as a brain-boosting aid. “I've taken mildronate. I personally liked it. Can't really tell you the effects being that I tried it quite a while ago,” Reddit user rmcfar11 wrote in a comment. “If it's banned by WADA, that's usually a good sign that it's reasonably effective at something lol.” While the substance is not a total debutante on the nootropic scene, until now there were only a few mentions of “meldonium” or “mildronate” on the r/nootropics subreddit. Originally designed as a medicine for cardiac and vascular conditions, Latvian-made meldonium is known for its beneficial effects on physical recovery and endurance, which likely account for WADA’s decision to prohibit it. The case for the drug’s potential nootropic virtues hinges mainly on a 2013 research paper authored, among others, by meldonium inventor Ivars Kalvins of the Latvian Institute of Organic Synthesis (the paper states the authors have no conflict of interest). The study suggests that meldonium can “stimulate learning and memory” and could “protect and treat neurological disorders, particularly those associated with neurodegeneration and a decline in cognitive function.” The drug is sold over the counter in Eastern Europe but it's largely unavailable in other countries. It has occasionally popped up on nootropics-themed forums over the last few years, and it has been on sale for a while from some nootropics online merchants, including Tarvydas. But Tarvydas said it hadn’t really been that popular until the Sharapova case threw it into the limelight this week. “I had to hire more people to work because I can't handle orders alone. And they are still coming in: from the US, Sweden, Denmark, the UK,” he said. Tarvydas added that he had personally used meldonium in the past; according to him, it improved his capability to perform aerobic exercise and his ability to focus and to work “without getting tired.” Russian nootropics merchant RUPharma echoed Tarvydas’s reports. “So far we have sold around 1,300 packs of Mildronate worldwide in the past 12 months. Out of the 1,300 packs, around 450 were sold in the past 3 days after the Sharapova news broke out,” company spokesman Alexei Adolshin wrote in an emailed statement. “As a joke we now call mildronate ‘the Sharaponate.’” It’s obviously hard to disentangle wannabe athletes from buyers who may be interested in the drug’s alleged cognition-enhancing properties. But it looks like in the wake of the Sharapova affair, meldonium is attracting a revived interest on nootropics sites.

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