Month: October 2013

From Academia to Industry

DR ANTHONY MELVIN CRASTO Ph.D Synthesis

AAPS Blog

Thiago CarvalhoJeff HemenwayThiago Carvalho, PH.D., is currently a pharmaceutical scientist in drug product science and technology at Bristol-Myers-Squibb.
Jeff Hemenway, Ph.D., is currently a pharmaceutical scientist in formulation and process development at Gilead Sciences.

The transition from academia to industry is extremely challenging for pharmaceutical scientists. The changes involved in this transition are huge, and there is always a great deal of uncertainty surrounding the entire process. This process and the time leading up to it can be very stressful and loaded with pitfalls.

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GOLCONDANE, molecule named after Golconda fort, Hyderabad

DR ANTHONY MELVIN CRASTO Ph.D funny, Synthesis ,

A  cage hydrocarbon was called Golcondane by the first people to synthesis it in 1993, Mehta and Reddy, in honour of the 400th anniversary of the founding of the Indian city of Hyderabad, whose ancient name was Golconda.

The interesting cage compound “Golcondane” (C20H24) has recently been synthesized, more or less according to the route shown here. (In the actual case, there were carbonyl groups that had to be reduced at the end of the synthesis.) Do MMX calculations on golcondane, on the three precursors, and on its decomposition product; discuss the relative stability of these compounds and identify the source(s) of their strain energy. [The origin of the name “golcondane” is so obscure that the interested reader should consult the cited reference.

A. Nickon and E.F. Silversmith, ‘Organic Chemistry: The Name Game‘, Pergamon, 1987; P. von R. Schleyer, E., and M.G.B. Drew. J. Am. Chem. Soc. 90, (1968) 5034.

“Golcondane: A Novel, Caged, Nonacyclic C20H24‐Hydrocarbon of D2d Symmetry”.G. Mehta and S.H.K. Reddy, Angew. Chem., Int. Ed. Engl. 32, (1993) 1160.  http://onlinelibrary.wiley.com/doi/10.1002/anie.199311601/abstract

Golconda Fort!! hyderabad India

The Beautiful Golconda Fort ,Hyderabad
The Beautiful Golconda Fort ,Hyderabad india

Branched Enynenynols

DR ANTHONY MELVIN CRASTO Ph.D ANTHONY MELVIN CRASTO, funny, Synthesis , , ,

“Old MacDonald Named a Compound: Branched Enynenynols”

that was originally published in the J. Chem. Ed. 74 (1997) 782, about what would happen if ‘Old MacDonald’ were a chemist, and made molecules that have the shapes of animals. Some are shown below.

http://pubs.acs.org/doi/abs/10.1021/ed074p782

Department of Chemistry, Hofstra University, Hempstead, NY 11590
J. Chem. Educ., 1997, 74 (7), p 782
DOI: 10.1021/ed074p782
Publication Date (Web): July 1, 1997

 

Development of a robust reagent for the two-carbon homologation of aldehydes to (E)-[small alpha],[small beta]-unsaturated aldehydes in water

DR ANTHONY MELVIN CRASTO Ph.D Synthesis

Green Chem., 2013, 15,3146-3149
DOI: 10.1039/C3GC41383G, Communication
James McNulty, Carlos Zepeda-Velazquez, David McLeod
Department of Chemistry & Chemical Biology, McMaster University, 1280 main Street West, Hamilton, Canada
Synthesis of a new pinacolacetal-phosphonium salt and its reaction with aldehydes in water to give homologated acetals and two-carbon homologated unsaturated aldehydes is presented.

Development of a robust reagent for the two-carbon homologation of aldehydes to (E)-[small alpha],[small beta]-unsaturated aldehydes in water

read at

http://pubs.rsc.org/en/Content/ArticleLanding/2013/GC/C3GC41383G?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract

 

Synthesis of a new pinacolacetal-phosphonium salt and its reaction with aldehydes to give homologated acetals and two-carbon homologated unsaturated aldehydes is presented. The chemistry takes place in water under mild conditions and the sequence can be performed in one-flask operation.

FDA approves Opsumit to treat pulmonary arterial hypertension

DR ANTHONY MELVIN CRASTO Ph.D Synthesis

 October 22 ,2013 | By Márcio Barra

Last Friday, the FDA approved Opsumit (macitentan) 10 mg once daily, from Actelion, for the treatment adults with pulmonary arterial hypertension (PAH). This is the second drug for the treatment of PAH on Actelion’s portfolio, following Tracleer (bosentan), which loses exclusivity from 2015, and the second drug approved for PAH this month by the FDA, after Adempas (riociguat), from Bayer.

PAH is high blood pressure condition that occurs in the arteries connecting the heart to the lungs. It causes the right side of the heart to work harder than normal, which can lead to limitations on exercise ability and shortness of breath. Opsumit is an endothelin receptor antagonist, which blocks endothelin receptors, thus relaxing the pulmonary arteries. This helps decrease the blood pressure within the lung vasculature that supply deoxygenated blood to the lungs.

The drug is being touted by Actelion as the…

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Monoclonal antibody (mAbs) 2013

DR ANTHONY MELVIN CRASTO Ph.D Synthesis

New Drug Approvals

2013——-29 monoclonal antibody (mAbs) drugs are in Phase III clinical development.

While around 350 therapeutic mAbs are currently in clinical development globally, only 28 had entered active Phase 2/3 or Phase 3 studies as of January 2013,  Additionally one mAb mixture was under evaluation in Phase III.

Historically, mAbs that target antigens relevant to cancer have comprised approximately 50% of the mAb clinical pipeline,

but in 2013 the picture has changed: 66% or 19 of the antibodies to watch in 2013 are for non-cancer indications.

The non-cancer mAbs include alirocumab (Regeneron; Sanofi, hypercholesterinemia);

AMG 145 (Amgen, hypercholesterinemia),

epratuzumab (UCB, SLE),

gantenerumab (Roche; Alzheimer’s disease),

gevokizumab (Xoma/Servier, Non-infectious uveitis),

itolizumab (Biocon, Plaque psoriasis), ixekizumab (Eli Lilly and Co., psoriasis),

lebrikizumab (Roche/Genentech, rheumatoid arthritis),

mepolizumab (GSK, Asthma, COPD etc.),

ocrelizumab (Roche/Genentech, multiple sclerosis),

reslizumab (Teva, Eosinophilic asthma), romosozumab (Amgen, Postmenopausal osteoporosis),

sarilumab (Regeneron; Sanofi, rheumatoid arthritis),

secukinumab (Novartis, rheuma, psoriasis),

sirukumab (Janssen…

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Nobel Prize in Medicine Awarded

DR ANTHONY MELVIN CRASTO Ph.D Synthesis

DownHouseSoftware

Three scientists were awarded the 2013 Nobel Prize in Medicine to:

James E. Rothman, Randy W. Schekman 
and Thomas C. Südhof

for their discoveries of machinery regulating vesicle traffic, 
a major transport system in our cells

– from the press release from nobelprize.org

ImageThe full release can be found here. The  website  includes a link to a summary page illustrating the contributions of each scientist and how they come together to form a unified picture of vesicular traffic.

The New York Times article describing the award including an astute remark by NIH Director Francis Collins about the state of research in the United States. 

Dr. Francis Collins, the N.I.H. director, said in an interview on Monday. “Today we celebrate the three N.I.H.-supported Nobel Prize winners, but we’re being slammed by sequestration and a government shutdown.”

Even before the shutdown, scientists were facing severe budgetary difficulties that restrict the kind…

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