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Rescooped by Sarah Scarry from Multiple sclerosis New Drugs Review
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Top 10 Multiple Sclerosis Drugs - Genetic Engineering News

“ Genetic Engineering News Top 10 Multiple Sclerosis Drugs Genetic Engineering News Following is a list of 10 FDA-approved drugs for patients with multiple sclerosis—nine of 10 disease-modifying agents authorized by the agency, plus a drug whose...”
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Rescooped by Sarah Scarry from Natural Products Chemistry Breaking News
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Recent contributions from the asymmetric aza-Michael reaction to alkaloids total synthesis

Recent contributions from the asymmetric aza-Michael reaction to alkaloids total synthesis | Chemistry | Scoop.it
This review focuses on recent applications of the aza-Michael reaction in alkaloids total synthesis with a special emphasis on stereoselectivity. The report highlights achievements and challenges over the past five years and describes stereoselective intra- and inter-molecular conjugate addition of nitrogen-containing nucleophiles, including tandem and cascade processes. Total asymmetric syntheses of natural scaffolds, such as pyrrolidine, piperidine and “izidine” families, are depicted. Multi-step syntheses of highly challenging natural products are further detailed, assessing the scope of the stereocontrolled aza-Michael reaction as a powerful tool in alkaloid chemistry.Zacharias Amara,a Joachim Carona and Delphine Joseph Nat. Prod. Rep., 2013,30, 1211-1225 DOI: 10.1039/C3NP20121J
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Rescooped by Sarah Scarry from Natural Products Chemistry Breaking News
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Processes To Separate Enantiomers - Angewandte Chemie International Edition - DOI: 10.1002/anie.201302823

Processes To Separate Enantiomers - Angewandte Chemie International Edition - DOI: 10.1002/anie.201302823 | Chemistry | Scoop.it
The provision of pure enantiomers is of increasing importance not only for the pharmaceutical industry but also for agrochemistry and biotechnology. In general, there are two rival approaches to provide pure enantiomers. The “chiral” approach is based on developing an asymmetric synthesis of just one of the enantiomers, while the “racemic” approach is based on separating mixtures of the two enantiomers. In the last few years remarkable progress has been achieved in the latter area. This Review focuses in particular on enantioselective crystallization processes and preparative chromatography, including hybrid processes and the incorporation of racemization steps. Several examples from our research are used for illustration purposes.
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Rescooped by Sarah Scarry from The Frontier
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Chemists Find More Efficient Total Synthesis Route To Ingenol | Chemical & Engineering News

Chemists Find More Efficient Total Synthesis Route To Ingenol | Chemical & Engineering News | Chemistry | Scoop.it

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Rescooped by Sarah Scarry from New drug approvals
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A REVIEW AND METHODS TO HANDLE PHOSGENE, TRIPHOSGENE SAFELY DURING DRUG SYNTHESIS

A REVIEW AND METHODS TO HANDLE PHOSGENE,  TRIPHOSGENE SAFELY DURING DRUG SYNTHESIS | Chemistry | Scoop.it
“ Phosgene Phosgene is the chemical compound with the formula COCl2. This colorless gas gained infamy as a chemical weapon during World War I. It is also a valued industrial reagent and building bloc...”
Via Anthony M Crasto DR.
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Rescooped by Sarah Scarry from TLP Addiction Training News.
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Scientists discover how sodium controls opioid receptor signaling

Scientists discover how sodium controls opioid receptor signaling | Chemistry | Scoop.it
“ Scientists have unraveled a 40-year mystery surrounding how sodium controls opioid receptor signaling in the brain, which could lead to new drugs for brain-related medical issues.”
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Rescooped by Sarah Scarry from Pharma Biotech Industry Review (Krishan Maggon)
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Eluxadoline* (Mu Opioid Receptor Agonist and Delta Opioid Receptor Antagonist)

Eluxadoline* (Mu Opioid Receptor Agonist and Delta Opioid Receptor Antagonist) | Chemistry | Scoop.it
Eluxadoline Mode of Action Eluxadoline is a first-in-class, locally-acting mu opioid receptor agonist and delta opioid receptor antagonist in Phase III development for treatment of IBS-d. In vivo studies indicate that the activity of eluxadoline at the two different opioid receptors works to modulate GI motility and decrease intestinal pain, without the constipating effects of unopposed mu agonist activity. Eluxadoline is locally active in the gut with very limited systemic bioavailability, thus potentially decreasing central nervous system effects and other systemic side effects associated with therapies currently used to manage IBS-d. Eluxadoline Clinical Profile Furiex successfully completed a Phase II study establishing the safety and efficacy of an oral formulation of MuDelta in patients with IBS-d. A total of 807 patients with IBS-d (based on the Rome III diagnostic criteria) were enrolled in the trial and randomized to receive twice daily treatment with either placebo or eluxadoline at doses of 5 mg, 25 mg, 100 mg or 200 mg. The study achieved statistically and clinically significant results for the primary endpoint of improvements in baseline stool consistency and abdominal pain at week 4 as well as a number of key secondary endpoints. Eluxadoline also demonstrated durable efficacy in improving IBS diarrhea and pain symptoms throughout the 12-week treatment period. We performed additional analyses, based on the FDA's 2010 guidance, to assess patients' daily pain and diarrheal symptoms over the full 12-week treatment period. These analyses, which the FDA agreed will be suitable for Phase III pivotal trials, define study responders as patients who met the following daily criteria for at least 50 percent of the days in the study: At least a 30 percent reduction in worst abdominal pain from baseline, andA BSS score of less than five on the same day.As shown in the Figure below, patients receiving eluxadoline had statistically and clinically superior response rates compared to patients receiving placebo. A significantly greater percentage of patients met the study responder definition among patients treated with eluxadoline at 100 mg BID compared to placebo (28.0 percent vs 13.9 percent, respectively; OR = 2.41, P=0.002) and 200 mg BID as compared to placebo (28.7 percent vs 13.9 percent; OR = 2.49, P=0.002). Statistically significant treatment effects were also seen in pre-specified secondary analyses of patient reported outcomes collected at the end of study visit (week 12), including adequate relief of IBS-d symptoms (weeks 4, 8, and 12), and IBS Quality of Life and EuroQoL-5 questionnaires. Eluxadoline was well-tolerated and had a favorable safety profile. The most commonly reported adverse events included nausea, vomiting, and abdominal pain. Incidence rates of abdominal pain and nausea were comparable to placebo for eluxadoline doses of 100 mg. Eluxadoline has been studied in more than 700 subjects to-date. Program Status Eluxadoline is currently in Phase III development with two simultaneous trials in study centers in the United States, Canada and United Kingdom. In July 2013, we completed Phase III enrollment, with over 2400 subjects in the two studies. The FDA agreed at the End-of-Phase II meeting that the composite endpoint of improvement in pain and diarrheal symptoms from the Phase II post hoc responder analysis is an acceptable primary endpoint for Phase III pivotal studies, providing eluxadoline a clear regulatory path forward. The Phase III program is designed to capture the 12-week composite endpoints as specified in the FDA 2012 guidance on IBS, while also collecting longer term global outcomes and pain data that could support registration in the European Union. Granted fast-track status by the FDA, a process designed to facilitate the development and expedite the review of drugs to treat diseases with significant unmet medical need. In 2011, Furiex acquired full exclusive license rights from Janssen to develop and commercialize eluxadoline. We are in active discussions with potential partners for this program. *USAN adopted, INN adoption pending If you are interested in learning about eluxadoline clinical trials click here: http://clinicaltrials.gov/ct2/show/NCT01553591 http://clinicaltrials.gov/ct2/show/NCT01553747 Relevant PublicationsWade PR, Palmer JM, McKenney S, Kenigs V, Chevalier K, Moore BA, Mabus JR, Saunders PR, Wallace NH, Schneider CR, Kimballs ES, Breslin HJ, He W, Hornby PJ. Modulation of gastrointestinal function by MuDelta, a mixed µ opioid receptor agonist / µ opioid receptor antagonist. British Journal of Pharmacology 2012; 167:1111-1125. http://www.ncbi.nlm.nih.gov/pubmed/22671931?dopt=Citation Dove LS, Lembo A, Randall CW, Andrae D, Davenport JM, McIntyre G, Almenoff JS, Covington PS. Eluxadoline Benefits Patients with Irritable Bowel Syndrome with Diarrhea in a Phase 2 Study. Gastroenterology 2013; 145:329-338. http://www.sciencedirect.com/science/article/pii/S001650851300499X Levy-Cooperman N, McIntyre G, Bonifacio L, et al. Lack of Subjective Abuse-Related Effects of Intranasal Eluxadoline: A Novel Mu-delta Opiate Modulator for Oral Use in IBS-d.Neuropsychopharmacology. 2013; 38:s521-s522.http://www.nature.com/npp/journal/v38/n2s/pdf/npp2013281a.pdf
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Rescooped by Sarah Scarry from New drug approvals
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IBRUTINIB 依鲁替尼 A Btk protein inhibitor.

IBRUTINIB 依鲁替尼  A Btk protein inhibitor. | Chemistry | Scoop.it
“ IBRUTINIB 依鲁替尼 A Btk protein inhibitor. 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-...”
Via Anthony M Crasto DR.
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Rescooped by Sarah Scarry from Natural Products Chemistry Breaking News
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The role of biocatalysis in the asymmetric synthesis of alkaloids

The role of biocatalysis in the asymmetric synthesis of alkaloids | Chemistry | Scoop.it
Alkaloids are not only one of the most intensively studied classes of natural products, their wide spectrum of pharmacological activities also makes them indispensable drug ingredients in both traditional and modern medicine. Among the methods for their production, biotechnological approaches are gaining importance, and biocatalysis has emerged as an essential tool in this context. A number of chemo-enzymatic strategies for alkaloid synthesis have been developed over the years, in which the biotransformations nowadays take an increasingly ‘central’ role. This review summarises different applications of biocatalysis in the asymmetric synthesis of alkaloids and discusses how recent developments and novel enzymes render innovative and efficient chemo-enzymatic production routes possible.Alkaloids are not only one of the most intensively studied classes of natural products, their wide spectrum of pharmacological activities also makes them indispensable drug ingredients in both traditional and modern medicine. Joerg Schrittwieser and Verena ReschRSC Adv., 2013, Accepted Manuscript DOI: 10.1039/C3RA42123F
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Rescooped by Sarah Scarry from Natural Products Chemistry Breaking News
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Hot off the press - Natural Product Reports (RSC Publishing)

Hot off the press - Natural Product Reports (RSC Publishing) | Chemistry | Scoop.it
“A personal selection of 32 recent papers is presented covering various aspects of current developments in bioorganic chemistry and novel natural products such as thelepamide from Thelepus crispus. Synthesis III”
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Rescooped by Sarah Scarry from Natural Products Chemistry Breaking News
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Merging Chemical Synthesis and Biosynthesis: A New Chapter in the Total Synthesis of Natural Products and Natural Product Libraries

Merging Chemical Synthesis and Biosynthesis: A New Chapter in the Total Synthesis of Natural Products and Natural Product Libraries | Chemistry | Scoop.it
Natural product synthesis is a stressful task. Exploiting the understanding of biosynthetic pathways and implementing genetic engineering into the synthetic chemist’s portfolio paves the way for new alternatives for natural product synthesis. This Minireview describes “hybrid” strategies of organic synthesis and biosynthesis that result in facile access to complex natural products and libraries based on them.
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Rescooped by Sarah Scarry from Social Neuroscience Advances
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Chemical compound shows promise as alternative to opioid pain relievers

Chemical compound shows promise as alternative to opioid pain relievers | Chemistry | Scoop.it
“A drug targeting a protein complex containing two different types of opioid receptors may be an effective alternative to morphine and other opioid pain medications, without any of the side effects or risk of dependence, according to research led by...”
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Rescooped by Sarah Scarry from Body CT & MR
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Synthesis and Evaluation of 11C-LY2795050 as a {kappa}-Opioid Receptor Antagonist Radiotracer for PET Imaging

“ Kappa-opioid receptors (KOR) are believed to be involved in the pathophysiology of depression, anxiety disorders, drug abuse, and alcoholism. To date, only 1 tracer, the KOR agonist 11C-GR103545, has been reported to be able to image KOR in primates.”
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Rescooped by Sarah Scarry from Host Cell & Pathogen Interactions
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G Protein-Coupled Receptors (GPCRs) win 2012 Nobel Prize in Chemistry | The Curious Wavefunction, Scientific American Blog Network

G Protein-Coupled Receptors (GPCRs) win 2012 Nobel Prize in Chemistry | The Curious Wavefunction, Scientific American Blog Network | Chemistry | Scoop.it
“ Brian Kobilka (Stanford) and Robert Lefkowitz (Duke) have won the 2012 Nobel Prize in Chemistry for their work on one of the most important classes of ...”
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Scooped by Sarah Scarry
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1024 samples analysed on a single chip - Chemistry World

1024 samples analysed on a single chip - Chemistry World | Chemistry | Scoop.it
“ 1024 samples analysed on a single chip Chemistry World Many clinical diagnostic tests measure the amount of a specific protein in a patient's blood. If the levels of this protein are abnormal it is often an indicator for a disease.”
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