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DR ANTHONY MELVIN CRASTO Ph.D ( ICT, Mumbai) , INDIA 36Yrs Exp. in the feld of Organic Chemistry,Working for AFRICURE PHARMA as ADVISOR earlier with GLENMARK PHARMA at Navi Mumbai, INDIA. Serving chemists around the world. Helping them with websites on Chemistry.Million hits on google, NO ADVERTISEMENTS , ACADEMIC , NON COMMERCIAL SITE, world acclamation from industry, academia, drug authorities for websites, blogs and educational contribution, ........amcrasto@gmail.com..........+91 9323115463, Skype amcrasto64 View Anthony Melvin Crasto Ph.D's profile on LinkedIn Anthony Melvin Crasto Dr.

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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA, ROW2TECH, NIPER-G, Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, Govt. of India as ADVISOR, earlier assignment was with GLENMARK LIFE SCIENCES LTD, as CONSUlTANT, Retired from GLENMARK in Jan2022 Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 32 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 32 PLUS year tenure till date Feb 2023, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 100 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 100 Lakh plus views on dozen plus blogs, 227 countries, 7 continents, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 38 lakh plus views on New Drug Approvals Blog in 227 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc He has total of 32 International and Indian awards

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Recent Posts

Route Design in the 21st Century: The ICSYNTH Software Tool as an Idea Generator for Synthesis Prediction

February 5, 2015 6:04 am / 1 Comment on Route Design in the 21st Century: The ICSYNTH Software Tool as an Idea Generator for Synthesis Prediction


Figure

 

The new computer-aided synthesis design tool ICSYNTH has been evaluated by comparing its performance in predicting new ideas for route design to that of historical brainstorm results on a series of commercial pharmaceutical targets, as well as literature data. Examples of its output as an idea generator are described, and the conclusion is that it adds appreciable value to the performance of the professional drug research and development chemist team.

† Chemical Development, AstraZeneca R&D, Silk Road Business Park, Macclesfield, SK10 2NA Cheshire, U.K.
‡ Chemnotia AB, Forskargatan 20 J, 151 36 Södertälje,Sweden
§ InfoChem GmbH, Landsberger Straße 408/V, D-81241 München, Germany
Org. Process Res. Dev., Article ASAP
DOI: 10.1021/op500373e
Publication Date (Web): January 22, 2015
Copyright © 2015 American Chemical Society
*(H.-J.F.) E-mail: Hans-Jurgen.Federsel@astrazeneca.com., *(M.G.H.) E-mail: mghutchings@infochem.de.
Currently, ICSYNTH has assumed a place as a unique predictive tool for route design in Chemical Development in AZ. While it is finding valuable commercial application in our own and others’ hands, it remains a work in progress.
ICsynthInfoChem’s powerful synthesis planning tool now in Version 2.0. Read more …

InfoChem will be represented at the forthcoming ACS Meeting in San Diego. You will find Dr. Josef Eiblmaier, Dr. Valentina Eigner Pitto, and Dr. Peter Loew …
ICSYNTH
InfoChem’s ICSYNTH is a powerful computer aided synthesis design tool that enables chemists to generate synthetic pathways for a target molecule. The benefit is that ICSYNTH can facilitate innovation by stimulating ideas for alternative or novel synthetic routes that otherwise may not be considered. This may lead to improved route design, for example shorter pathways or more economical reaction modifications.

After inputting the target, users can select different synthetic strategies depending on requirements. ICSYNTH then automatically generates a multistep interactive synthesis tree – each node on the tree representing a precursor. The advantages are that the suggested reactions are based on, and linked to, published reactions (or their analogs) and the precursor availability is automatically checked in commercial catalogs. Users can modify the synthesis tree or select precursors for further analysis.

At the heart of ICSYNTH is an algorithmic chemical knowledge base of transform libraries that are automatically generated from reaction databases. The number of transform libraries is only limited by the availability of validated reaction databases.
In addition to retro synthesis design, ICSYNTH has a forward reaction prediction module that offers reactivity mapping for the target molecule. Version 2.0 of ICSYNTH was launched in April 2014. The completely re-designed user interface (based on JavaScript) and major improvements in the algorithm responsible of the precursor search are the main enhancements of Version 2.0. In addition the forward reaction prediction algorithm has been optimized. Click here to see a complete version history.

INFOCHEM GESELLSCHAFT FÜR CHEMISCHE INFORMATION MBH

Landsberger Straße 408/V
D-81241 München
Germany

Phone: +49 (0)89 58 30 02
Fax: +49 (0)89 580 38 39
Email: info@infochem.de

 

Historische Bilder der Landsberger Straße – An der Trambahnhaltestelle Holzapfelstraße endet – Münchner Straßen – München – Süddeutsche.de

 

USP Chapter Visual Inspection of Injections published

February 5, 2015 5:13 am / Leave a comment


DR ANTHONY MELVIN CRASTO Ph.D's avatarDRUG REGULATORY AFFAIRS INTERNATIONAL

The long-awaited USP Chapter <1790> regarding the 100% visual control of injections has been issued in the Pharmacopeial Forum 41(1) for commenting. Read on.

http://www.gmp-compliance.org/enews_4682_USP-Chapter–1790–Visual-Inspection-of-Injections-published_40007,9087,9200,Z-PEM_n.html

The long-awaited USP Chapter <1790> regarding the 100% visual control of injectables has now been issued as a first draft in the Pharmacopeial Forum 41(1) for commenting.

The new chapter is comprised of the following sub-chapters:
1. Scope
2. Introduction
3. Typical Inspection Process Flow
4. Inspection Life-Cycle
5. Interpretation of Results
6. Inspection Methods and Technologies
7. Qualification and Validation of Inspection Processes
8. Conclusions and Recommendations
9. References

This new informative chapter is applied to the manual, the half-automatic and the fully-automated inspection of parenterals. It mainly aims at controlling particles (>50 µm), but also comprises indications to further defects like cracks in primary containers or poorly fitting stoppers. In Chapter 2 there are also general statements regarding the patient risk due to…

View original post 329 more words

FDA approves Pfizer’s Ibrance (palbociclib) for postmenopausal women with advanced breast cancer

February 5, 2015 4:26 am / 1 Comment on FDA approves Pfizer’s Ibrance (palbociclib) for postmenopausal women with advanced breast cancer


PALBOCICLIB

Mechanism of action: selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6
Indication: Estrogen receptor-positive (ER+), HER2-negative (HER2 -) breast cancer

FDA approves Ibrance for postmenopausal women with advanced breast cancer

February 3, 2015

syn……….https://newdrugapprovals.org/2014/01/05/palbociclib/

The U.S. Food and Drug Administration today granted accelerated approval to Ibrance (palbociclib) to treat advanced (metastatic) breast cancer.

Breast cancer in women is the second most common type of cancer in the United States. It forms in the breast tissue and in advanced cases, spreads to surrounding normal tissue. The National Cancer Institute estimates that 232,670 American women were diagnosed with breast cancer and 40,000 died from the disease in 2014.

Ibrance works by inhibiting molecules, known as cyclin-dependent kinases (CDKs) 4 and 6, involved in promoting the growth of cancer cells. Ibrance is intended for postmenopausal women with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative metastatic breast cancer who have not yet received an endocrine-based therapy. It is to be used in combination with letrozole, another FDA-approved product used to treat certain kinds of breast cancer in postmenopausal women.

“The addition of palbociclib to letrozole provides a novel treatment option to women diagnosed with metastatic breast cancer,” said Richard Pazdur, M.D., director of the Office of Hematology and Oncology Products in the FDA’s Center for Drug Evaluation and Research. “The FDA is committed to expediting marketing approval of cancer drugs through our accelerated approval regulations.”

syn……….https://newdrugapprovals.org/2014/01/05/palbociclib/

The FDA granted Ibrance breakthrough therapy designation because the sponsor demonstrated through preliminary clinical evidence that the drug may offer a substantial improvement over available therapies. It also received a priority review, which provides for an expedited review of drugs intended to provide a significant improvement in safety or effectiveness in the treatment of a serious condition or meet an unmet medical need. Ibrance is being approved more than two months ahead of the prescription drug user fee goal date of April 13, 2015, the date when the agency was scheduled to complete its review of the application.

Ibrance is being approved under the FDA’s accelerated approval program, which allows approval of a drug to treat a serious or life-threatening disease based on clinical data showing the drug has an effect on a surrogate endpoint reasonably likely to predict clinical benefit to patients. This program provides earlier patient access to promising new drugs while the company conducts confirmatory clinical trials.

The drug’s efficacy was demonstrated in 165 postmenopausal women with ER-positive, HER2-negative advanced breast cancer who had not received previous treatment for advanced disease. Clinical study participants were randomly assigned to receive Ibrance in combination with letrozole or letrozole alone. Participants treated with Ibrance plus letrozole lived about 20.2 months without their disease progressing (progression-free survival), compared to about 10.2 months seen in participants receiving only letrozole. Information on overall survival is not available at this time.

The most common side effects of the drug were a decrease in infection-fighting white blood cells called neutrophils (neutropenia), low levels of white blood cells (leukopenia), fatigue, low red blood cell counts (anemia), upper respiratory infection, nausea, inflammation of the lining of the mouth (stomatitis), hair loss (alopecia), diarrhea, low blood platelet counts (thrombocytopenia), decreased appetite, vomiting, lack of energy and strength (asthenia), damage to the peripheral nerves (peripheral neuropathy) and nosebleed (epistaxis). Healthcare professionals should inform patients of these risks.

It is recommended that treatment begin with a 125 milligram dose for 21 days, followed by seven days without treatment. Healthcare professionals are advised to monitor complete blood count prior to start of therapy and at the beginning of each cycle, as well as on Day 14 of the first two cycles, and as clinically indicated.

Ibrance is marketed by New York City-based Pfizer, Inc.

see synthesis……….https://newdrugapprovals.org/2014/01/05/palbociclib/

 

New York City-based Pfizer, Inc.

 

Pfizer World Headquarters building in New York City. Zoetis, based in Madison, N.J., traces its roots back to 1952 as a Pfizer unit and has made at least 10 …

Pfizer’s NYC headquarters

 

Falsified Results of Analysis at Indian Pharmaceutical Manufacturer

February 5, 2015 3:56 am / Leave a comment


DR ANTHONY MELVIN CRASTO Ph.D's avatarDRUG REGULATORY AFFAIRS INTERNATIONAL

Indian pharmaceutical manufacturers increasingly attract attention by breaching GMP rules. In a further case the analysis results not complying with the requirements were deleted and the batch was released for the US market. Read more.

http://www.gmp-compliance.org/enews_4629_Falsified-Results-of-Analysis-at-Indian-Pharmaceutical-Manufacturer_9086,9087,9200,9122,Z-PEM_n.html

Indian pharmaceutical manufacturers increasingly attract attention by breaching GMP rules. We recently reported on theunannounced FDA inspections in India as one of the consequences of this practice. In a further case the analysis results not complying with the requirements were deleted and the batch was released for the US market. An employee of Sun Pharmaceutical Industries Ltd. in Vadodara, India simply deleted analytical data of an HPLC testing on impurities of an antibiotic that did not comply. The next day another sample was tested, considered to be fine and the batch was released. This incident took place three years ago.

This fundamental GMP violation of data integrity has become known only now. The…

View original post 266 more words

EDIVOXETINE REVISITED

February 3, 2015 4:05 am / Leave a comment


Edivoxetine structure.png

EDIVOXETINE, LY 2216684

(1R)-2-(5-fluoro-2-methoxyphenyl)-1-[(2S)-morpholin-2-yl]-1-(oxan-4-yl)ethanol

UNII-3W9N3F4JOO, 1194508-25-2, Edivoxetine [USAN], Edivoxetine (USAN/INN), Edivoxetine [USAN:INN], 3W9N3F4JOO
Molecular Formula:C18H26FNO4
Molecular Weight:339.401743 g/mol

Edivoxetine (INN; LY-2216684) is a drug which acts as a selective norepinephrine reuptake inhibitor and is currently under development by Eli Lilly for attention-deficit hyperactivity disorder (ADHD) and as an antidepressant treatment.[1][2] It was in phase IIIclinical trials, in 2012, for major depressive disorder, but failed to get approval.[1][3]

 

Effectiveness

In a study published in 2010, edivoxetine failed to prove superiority over placebo, as measured by Hamilton Depression Rating Scale. However, effectiveness could be observed using the Self-Rated Quick Inventory of Depressive Symptomatology.[4]

In a study published in 2011, using the Montgomery-Åsberg Depression Rating Scale and the Sheehan Disability Scale, edivoxetine showed superiority over placebo, with higher response and remission rates.[5]

In December 2013, Eli Lilly announced that the clinical development of edivoxetine will be stopped due to lack of efficacy compared to SSRI alone in three separate clinical trials.[6]

Side effects

Side effects significantly associated with edivoxetine are headache, nausea, constipation, dry mouth and insomnia.[4]

The above mention studies report increases of the cardiac rhythm, and one also increases of diastolic and systolic blood pressures.[4][5]

Figure

Org. Process Res. Dev., Article ASAP
DOI: 10.1021/op5003825

There is a growing trend in Ireland toward greater collaboration between academia and the pharmaceutical industry. This is an activity encouraged at a national policy level as a means of providing researchers from academic institutions the opportunity to gain important first-hand experience in a commercial research environment, while also providing industry access to expertise and resources to develop new and improved processes for timely medicines. The participating company benefits in terms of its growth, the evolution of its strategic research and development, and the creation of new knowledge that it can use to generate commercial advantage. The research institute benefits in terms of developing skill sets, intellectual property, and publications, in addition to access to identified current industry challenges. A case study is provided describing the collaborative partnership between a synthetic chemistry research team at University College Cork (UCC) and Eli Lilly and Company.

Department of Chemistry and School of Pharmacy, Analytical and Biological Chemistry Research Facility, Synthesis and Solid State Pharmaceutical Centre,University College Cork, Cork, Ireland

University College Cork

Systematic (IUPAC) name
(1R)-2-(5-fluoro-2-methoxyphenyl)-1-[(2S)-morpholin-2-yl]-1-(tetrahydro-2H-pyran-4-yl)ethanol
Clinical data
Legal status
?
Identifiers
CAS number 1194508-25-2
1194374-05-4 (hydrochloride)
ATC code None
PubChem CID 11186829
ChemSpider 9361913
Chemical data
Formula C18H26FNO4 
Molecular mass 339.402 g/mol

References

  1.  Jun Yan (March 2012). “Pipeline for new antidepressants flowing slowly”. Psychiatric News (American Psychiatric Association) 47 (5): 1b-29. Retrieved 2012-04-27.
  2.  “Statement on a nonproprietary name adopted by the USAN council – Edivoxetine” (Press release). American Medical Association. 2012. Retrieved 2012-04-12.
  3.  Chancellor D (November 2011). “The depression market”. Nature Reviews. Drug Discovery 10 (11): 809–10. doi:10.1038/nrd3585. PMID 22037032.
  4.  Dubé S, Dellva MA, Jones M, Kielbasa W, Padich R, Saha A, Rao P (April 2010). “A study of the effects of LY2216684, a selective norepinephrine reuptake inhibitor, in the treatment of major depression”. Journal of Psychiatric Research 44 (6): 356–363. doi:10.1016/j.jpsychires.2009.09.013. PMID 19909980.
  5.  Pangallo P, Dellva MA, D’Souza DN, Essink B, Russell J, Goldberger C (June 2011). “A randomized, double-blind study comparing LY2216684 and placebo in the treatment of major depressive disorder”. Journal of Psychiatric Research 45 (6): 748–755. doi:10.1016/j.jpsychires.2011.03.014. PMID 21511276.
  6.  https://investor.lilly.com/releasedetail.cfm?ReleaseID=811751
H-NMR spectral analysis
(1R)-2-(5-fluoro-2-methoxyphenyl)-1-[(2S)-morpholin-2-yl]-1-(oxan-4-yl)ethanol NMR spectra analysis, Chemical CAS NO. 1194508-25-2 NMR spectral analysis, (1R)-2-(5-fluoro-2-methoxyphenyl)-1-[(2S)-morpholin-2-yl]-1-(oxan-4-yl)ethanol H-NMR spectrum
CAS NO. 1194508-25-2, (1R)-2-(5-fluoro-2-methoxyphenyl)-1-[(2S)-morpholin-2-yl]-1-(oxan-4-yl)ethanol H-NMR spectral analysis
C-NMR spectral analysis
(1R)-2-(5-fluoro-2-methoxyphenyl)-1-[(2S)-morpholin-2-yl]-1-(oxan-4-yl)ethanol NMR spectra analysis, Chemical CAS NO. 1194508-25-2 NMR spectral analysis, (1R)-2-(5-fluoro-2-methoxyphenyl)-1-[(2S)-morpholin-2-yl]-1-(oxan-4-yl)ethanol C-NMR spectrum
CAS NO. 1194508-25-2, (1R)-2-(5-fluoro-2-methoxyphenyl)-1-[(2S)-morpholin-2-yl]-1-(oxan-4-yl)ethanol C-NMR spectral analysis

/////////////

MAHABALIPURAM, INDIA

Mahabalipuram – Wikipedia, the free encyclopedia

en.wikipedia.org/wiki/Mahabalipuram

Mahabalipuram, also known as Mamallapuram is a town in Kancheepuram district in the Indian state of Tamil Nadu. It is around 60 km south from the city of …‎Shore Temple – ‎Seven Pagodas – ‎Pancha Rathas – ‎

Map of mahabalipuram.

.

Krishna’s Butter Ball in Mahabalipuram, India. The surface below the rock is …


http://www.weather-forecast.com/locations/Mamallapuram


Come to Mahabalipuram (also known as Mammallapuram), an enchanting beach that is located on the east coast of India.
Moonraikers Restaurant, Mamallapuram
 

Hotel Mamalla Bhavan – Mahabalipuram Chennai – Food, drink and entertainment

.

A carving at the Varaha Temple, Mahabalipuram

/////////////

(sNDA)…..FDA okays Shire ADHD drug Vyvanse (lisdexamfetamine dimesylate) for binge eating

February 2, 2015 5:56 am / Leave a comment


 

 

Lisdexamfetamine-Structural Formula V.1.svg

Yet more good news for Shire has come with the US Food and Drug Administration approving its attention-deficit hyperactivity disorder blockbuster Vyvanse for binge-eating disorder, the first medicine approved by the agency to treat this condition.

The agency has expanded approval on Vyvanse (lisdexamfetamine dimesylate) for adults with BED based on two Phase III studies which showed that it was statistically superior to placebo in terms of number of binge days per week. BED affects around 2.8 million US adults and is more prevalent than anorexia nervosa and bulimia nervosa combined.

Read more at: http://www.pharmatimes.com/Article/15-01-30/FDA_okays_Shire_ADHD_drug_Vyvanse_for_binge_eating.aspx

 

Originally discovered and developed by New River Pharmaceuticals, the company entered into a collaborative agreement with Shire Pharmaceuticals in 2005 for global commercialization of the drug candidate. After Shire’s acquisition of New River Pharmaceuticals in April 2007, lisdexamfetamine entered the product portfolio of Shire.

 

 

 

In 2009, the compound was licensed to GlaxoSmithKline by Shire in the U.S. for comarketing for the treatment of attention deficit/hyperactivity disorder (ADHD). In 2010, this license agreement was terminated. The product was licensed to Shionogi by Shire in Japan for co-development, co-commercialization, and co-promotion for the treatment of attention deficit/hyperactivity disorder (ADHD).

Lisdexamfetamine (NRP-104), a conditionally bioreversible derivative of amphetamine, was launched in the U.S. in 2007 for the treatment of attention deficit hyperactivity disorder (ADHD) in children aged 6-12 years old. In 2008, the product was approved for use in adults, and in 2009 it was approved in Canada, followed by commercialization in 2010. In 2010, FDA approval was obtained for use in treatment of ADHD in adolescents aged 13 to 17 years and launch took place the same year. Approval for the treatment of adolescents was assigned in Canada in 2011.

 

In 2012, Shire filed a regulatory application in Europe via the decentralized procedure with the U.K. acting as the reference member state, for the treatment of ADHD in children and adolescent patients aged 6 to 17 years. This indication was approved in 2013. Also, in 2012 FDA approval was granted for the maintenance treatment for adults with ADHD. U.K., DK and SE are awaiting approval for the same indication in a decentralized procedure initiated in 2014 with the U.K. acting as the reference member state. In 2014, the company filed with priority review a supplemental New Drug Application (sNDA) in the U.S. for the treatment binge eating in adults.
cas 608137-33-3

(2S)-2,6-Diamino-N-[(1S)-1-methyl-2-phenylethyl]hexanamide dimethanesulfonate

Binge eating,,,,,, express their stress as temper tantrums or by indulging in compulsive eating spree


In terms of clinical development, phase III clinical trials are ongoing at Shionogi in Japan for the treatment of ADHD.. The National Institute on Drug Abuse (NIDA) is evaluating the compound in early clinical studies for the treatment of methamphetamine dependence. Phase III trials were underway as an adjunctive treatment of major depressive disorder; however, they were discontinued due to lack of efficacy. A phase II clinical trial for the treatment of excessive daytime sleepiness (EDS) has been completed. Shire had been evaluating the compound in clinical studies for the treatment of chronic fatigue syndrome.

In 2013, Shire cancelled its phase III program evaluating the product for the negative symptoms of schizophrenia based on a review and prioritization of the company’s development portfolio.

http://www.google.co.in/patents/US7662787

RIVER PHARMA

NEW RIVER PHARMACEUTICALS

 

Patent and Exclusivity Search Results from query on Appl No 021977 Product 003 in the OB_Rx list.

Patent Data

Appl No Prod No Patent No Patent
Expiration		 Drug Substance
Claim		 Drug Product
Claim		 Patent Use
Code		 Delist
Requested
N021977 003 7105486 Jun 29, 2023 U – 727
N021977 003 7223735 Jun 29, 2023 Y
N021977 003 7655630 Feb 24, 2023 Y
N021977 003 7659253 Feb 24, 2023 Y Y U – 727
N021977 003 7659254 Feb 24, 2023 U – 1034
N021977 003 7662787 Feb 24, 2023 Y
N021977 003 7662788 Feb 24, 2023 U – 727
N021977 003 7671030 Feb 24, 2023 Y U – 727
N021977 003 7671031 Feb 28, 2023 U – 727
N021977 003 7674774 Mar 18, 2023 Y U – 842
N021977 003 7678770 Mar 25, 2023 U – 842
N021977 003 7678771 Mar 25, 2023 Y U – 842
N021977 003 7687466 Feb 24, 2023 Y
N021977 003 7687467 Apr 8, 2023 Y U – 842
N021977 003 7700561 Jun 29, 2023 Y
N021977 003 7713936 Feb 24, 2023 U – 727
N021977 003 7718619 Feb 24, 2023 Y U – 842
N021977 003 7723305 Feb 24, 2023 Y U – 842

Exclusivity Data

Appl No Prod No Exclusivity Code Exclusivity Expiration
N021977 003 I – 645 Jan 31, 2015

Lead-oriented synthesis: a new concept to aid drug-discovery process

February 1, 2015 10:22 am / Leave a comment


 

Figure 2. a. Fragment-based screening: Small and structurally diverse molecules (circles represent functional groups) are screened for a biological target, and they are combined and modified to generate drug-like compounds. b. Diversity-oriented synthesis: Large collections of structurally diverse and complex molecules are made using a short number of reactions. The resulting compounds are optimized to produce the drug-like compounds. | Credit: P. J. Hajduk,W. R. J. D. Galloway & D. R. Spring Nature, 2011, 470, 42–43. DOI: 10.1038/470042a

 

The discovery and development of new drugs is a long and expensive process, and despite of it, essential to face present and new diseases. For small molecules, which account for the majority of the marketed drugs, the discovery process generally involves finding a starting point termed hit or lead compound. These molecules have biological activity but need to be optimized to enhance their potency and selectivity (i.e. minimize the toxicity) and improve pharmacokinetic parameters making them suitable to go to the next stage, the pre-clinical tests……….http://mappingignorance.org/2014/07/04/lead-oriented-synthesis-new-concept-aid-drug-discovery-process/

 

Author

pablo ortiz

Pablo Ortiz
Pablo Ortiz graduated in Pharmacy from the University of the Basque Country (UPV/EHU) and received a MSc in Synthetic and Industrial Chemistry by the same university. He is currently a PhD student in Synthetic Organic Chemistry at the University of Groningen (The Netherlands). His research is focused on novel copper catalysed transformations.

PhD at Rijksuniversiteit Groningen

Experience

PhD Student, Rijksuniversiteit Groningen

October 2013 – Present 

Asymmetric organometallic catalysis focused on tertiary alcohols and amines

Harutyunyan research group

Harutyunyan research group

Master Thesis Project

University of the Basque Country

February 2013 – September 2013 (8 months)Vitoria-Gasteiz Area, Spain

Estereoselective synthesis of quaternary alpha-aminophosphonic acid derivatives (organocatalysis)

Locum pharmacist

Community pharmacy

August 2012 – August 2012 (1 month)La Rioja, Spain

Pre-registration pharmacist

NHS Trust

January 2012 – June 2012 (6 months)Southport, England

In-patient and out-patient dispensing
Clinical pharmacy
Medicines information
Anticoagulant management
Aseptic preparation of medicines
Clinical audit of antimicrobial use

Publications

Tertiary α-diarylmethylamines derived from diarylketimines and organomagnesium reagents(Link)

Chem. Commun. 2015, 51, 703-706.

November 13, 2014

Organomagnesium reagents enable swift and versatile derivatisation of diarylimines to the corresponding α-substituted diarylmethylamines in excellent yields, through fast and clean reactions. Where it occurs, 1,2-reduction can be circumvented using readily accessible dialkylmagnesium reagents.

Asymmetric Synthesis of Functionalized Tetrasubstituted α-Aminophosphonates through Enantioselective Aza-Henry Reaction of Phosphorylated Ketimines(Link)

J. Org. Chem., 2015, 80, 156–164

November 2014

Bifunctional Cinchona alkaloid thioureas efficiently catalyze asymmetric nucleophilic addition of nitromethane to ketimines derived from α-aminophosphonic acids to afford tetrasubstituted α-amino-β-nitro-phosphonates.

Catalytic Asymmetric Alkylation of Aryl Heteroaryl Ketones(Link)

Eur. J. Org. Chem., 2015, 72–76.

November 2014

Tertiary diarylmethanols are highly bioactive structural motifs. A new strategy to access chiral tertiary diarylmethanols through copper-catalyzed direct alkylation of (di)(hetero)aryl ketones by using Grignard reagents was developed. The low reactivity and the similarity of the enantiotopic faces of bis-aromatic ketones were partially overcome, which resulted in moderate to good yields and…more

Education

Universidad del País Vasco/Euskal Herriko Unibertsitatea

Bachelor’s degree, Pharmacy, Extraordinary Degree Award, 9.06

2007 – 2012

(Open)1 honor or award
(Open)2 courses

Courses

Universidad del País Vasco/Euskal Herriko Unibertsitatea

  • How to write and publish a research article
  • X Pharmaceutical Chemistry Sessions: New strategies for the design and synthesis of drugs

Universidad del País Vasco/Euskal Herriko Unibertsitatea

  • II Organic Chemistry Synthesis and Catalysis Workshop: Methods and strategies in synthesis

 

GRONINGEN, NETHERLANDS

 

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AYURVEDA……..Dronapushpi (দ্রোনপুষ্পি)

February 1, 2015 3:30 am / Leave a comment


Dronapushpi is Sanskrit name of plant Leucas cephalotes. It is a medicinal herb that grows as a weed in India and many South East Asian countries. The folk use of this herb is for treating scorpion stings, snake bite, cough, fever etc. The whole plant has fever educing and insecticidal properties. The leaves are applied externally on snake bites and scorpion stings. To know more about this medicinal herb,

‘Leucas aspera ‘

‘Leucas aspera ‘. Common Leucas, known as Chhota halkusa in Hindi, Tumba in Malayalam, Tummachettu in Telugu, Ghal ghase in Bengali, Dronapushpi in Sanskrit and Thumbai in Tamil, is a medicinal plant.

 

SYNONYMS

 

  • Ksavapatra
  • Chatrini
  • Palepushpa
  • Guma
  • Nahula
  • Adhicchatra
  • Dvesyamesa
  • Gotamah
  • Putigandhika
  • Kumbhayoni
  • Kutumbaka
  • Drona
  • Swasanaka
  • Palindi
  • Chatrani
  • Chatraka
  • Koodinya
  • Vrakshasaraka
  • Dhirgapatra
  • Supuspa
  • Chitrapatrika

 

TYPES

 

According to Abhidhana ratnamala

  • Two varieties
  • Mahadrona
  • Dronapushpa

According to Raja narahari

  • Drona – Lucas aspera
  • Mahadrona – L. Cephalotus
  • Another species – L. indica

 

PART USED

  • Panchanga

 

FORMULATION

 

  • Plihari vati
  • Gorocanadi vati
  • Nimbadilepa
  • Sahacharadi taila

DOSAGE

 

  • Swarasa-5-10ml.
  • Churna-1-3gm

 

PROPERTIES

 

Rasa: katu, lavana, Madhura.

Guna: Guru, Ruksha, Theekshna

Veerya: Ushna.

Vipaka: Madhura

Doshsgnhtha: Kapha, vata, shamaka.

 

CHEMICAL COMPOSITION

  • Its Panchanga contains B-sisstesterol, flavinol, Glycoside.
  • Flowers  contain an essential oil, A bitter principle seeds a contain a fixed oil , caryophyllene, oxide, 26.56% Gama- Fenchene 12.02%, Alpha- cordional 2.13% , 1-hepten 3-01, 6.53%, menthol 6.30%, deca hydro naphthalene 5.15%, and trans –caryophyllene 4.05%.
  • Labdane, Noraladane, laballenic acid lauric acid, glutaric acid, Adipic acid , tridecanoic acid.

 

KARMA

  • Bhedana
  • Kaphagna
  • Amapacaka
  • Kamalahara
  • Shothoghna
  • Shvasagna
  • Krimigana
  • Swedajanana
  • Vata prashamana
  • Samsrana
  • Vishamajvarahara

 

PRAYOGA

  • Kaamala
  • Shotha
  • Shwasa
  • Vishamajvara
  • Kandu
  • Udara shoola
  • Pratisyaya
  • Jvara
  • Shira shoola

THERAPEUTIC USES

 

Vishamajvara– Fresh juice of dronapuspi and tulasi are useful.            [Sharangadhara Samhita madhyamakhanda]

 Kaamala: Anjana with the juice of dronapuspi useful. [Gadanigraha].                                            

Netrarogani: dronapuspi juice is mixed with rice water and used orally as well as topically.                                 [G.N]

Pittajavikara : Hima prepared by sariva, rasani, guduchi,  rakthachandana and dronapuspi.         [Siddhayogasangraha]

Paandu : Hima prepared by dronapuspi and padmaka, sariva drugs are useful.                 [Siddhayogasangraha]

 

PHARMACO THERAPEUTIC ACTION AND USES

 

Lecus cephalotes has been reported to exert hepatoprotective action in carbon tetra chloride induced hepatotoxicity in animals.

Juice of it has been reported to act as an antibilious in herbal therapy for jaundice

It has shown positive test in filariesis

The whole plant powder in the proportion of 70% in the herbal composition is patented to cure epileptic convulsions and cerebral function disorders.

It is also having the properties of antipyretic, stimulant , expectorant, aperients , diaphoretic, insecticidal, emmenagogue, and antioxidant, anti-inflammatory and anti diabetic.

They are useful in colic, dyspepsia arthralgia.

 

FOLKLORE USES

 

  • Plant decoction is used in the treatment of malarial fever .
  • The leaves juice is used topically in psoriasis, skin eruption , and scabies and internally for the treatment of urinary complaints.
  • The flowers are administered in the form of syrup or with honey for cough and cold.
  • The dried inflorescences are smoked and the smoke exhaled through the nose to treat nose bleeds.
  • Dried leaves along with tobacco (1:3) are smoked to treat bleeding as well as itching piles and fresh leaves eaten as a potent herb.

 

CULTIVATION

 

Cultivated fields as a weed , especially after a period of rain . It is collected for use as a leafy vegetable in rural areas . it is cultivated itself for its medicinal uses . And really available in market.

 

RESEARCH STUDIES

 

ANTIBACTERIAL

Leucas cephalotes a common ethanomedicinal plant’s used by folklore of tirupathi andrapradesh for fever and urinary tract infection.  Organic extracts hexane and methanolic extracts showed prominent antibacterial activity .

 

IN VITRO ANTHELMINTIC ACTIVITY

It is mild stimulant diaphoretic and used for fever

The overall study showed that dronapushpi decoction was beneficial to naveen (new) amavata.

The claim of folk ore amavata probably more beneficial if used with suitable vedanasthapana (analgesic)  drugs

Traditional medicinal uses

Dronapushpi is a weed that grows on wastelands. Medicinally, it has antimicrobial, insecticidal, fever reducing, larvicidal and inflammation reducing properties. It is useful in skin diseases. In malarial fever, the leaves juice is given. In some part of country, the decoction of whole plant is used for curing fever. The juice removes toxins from body. The leaves juice is applied externally for skin diseases and swelling. In cod and cough, the leaves juice is recommended.

Scorpion sting

In scorpion sting the plant is used internally as well externally. The leaves juice (few drops) is mixed with honey and taken orally.

Topically, the leaves juice is applied on place of sting.

Snake bite

The folk remedy is to put few drops of whole plant in nostrils.

Skin diseases, removing blood toxins

Skin diseases mainly occur due to toxins in blood. Dronapushpi plant has ability to flush the toxins from body.

In skin diseases, whole plant of Dronapushpi is used. The plant is dried. Five grams of dried powder is taken with three grams Neem/Margosa leaves in 2 glass water. This is boiled till volume reduce to one fourth. Then it filtered and taken two times a day.

Abnormally heavy bleeding at menstruation

The leaves of plant are taken a handful. These are washed and then ground to make fine paste. This paste is mixed with lemon juice and sesame oil/til oil (edible). The preparation is eaten empty stomach every morning for a week.

 

Asthma, cold, cough

The leaves juice of plant is taken in dose of 1-3 teaspoons.

Excessive thirst

The flowers (2 tablespoon) are boiled in water (150 ml) till volume reduces to half. This is filtered and taken thrice a day.

Cough, leucorrhoea

The leaves of plant are cooked and eaten with rice.

Skin diseases (itching, patchy skin, psoriasis, scabies etc.)

The paste of leaves is applied externally at the affected body areas.

Cough, congestion, blockage of nose, headache due to cough, Sinusitis, Migraine, Phlegm

The juice of leaves is put in nostrils as drops. For this purpose, the leaves juice is extracted and mixed with two times water. Then the diluted juice is put in nostrils (4 dops) for 3-4 days.

The flowers are heated in til/sesame oil and applied on head.

Fever (acute, chronic), Allergy

The decoction of plant (2-3 grams in boiled in two glass water till water reduces to one fourth) is used

This medicinal herb should be used in recommended doses only. It is hot in potency and heats up body. Avoid its use in excess. The leaves juice can be diluted for putting in nose of oral use.

DRONAPUSHPI

 

………..

SHIMOGA,  KARNATAKA, INDIA

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Generic drugs in the EU

January 31, 2015 3:50 am / Leave a comment


DR ANTHONY MELVIN CRASTO Ph.D's avatarDRUG REGULATORY AFFAIRS INTERNATIONAL

Process of reviewing and assessing the dossier to support a medicinal product in view of its marketing (also called licensing, registration, approval, etc.), obviously finalized by granting of a document also called marketing authorization (equivalent: product license). This process is performed within a legislative framework which defines the requirements necessary for application to the concerned (competent) regulatory authority, details on the assessment procedure (based on quality, efficacy and safety criteria) and the grounds for approval or rejection of the application, and also the circumstances where a marketing authorization already granted may be withdrawn, suspended or revoked.NOTE [1]
The application dossier for marketing authorization is called New Drug Application (NDA) in the USA or Marketing Authorization Application (MAA) in the European Union and other countries, or simply registration dossier. Basically, this consists of a dossier with data proving that the drug has quality, efficacy and safety properties suitable for the intended…

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Marketing Authorisation in Europe

January 31, 2015 3:49 am / Leave a comment


DR ANTHONY MELVIN CRASTO Ph.D's avatarDRUG REGULATORY AFFAIRS INTERNATIONAL

European Commission logo

Authorisation Procedures for medicinal products

Procedures for evaluating medicinal products and granting marketing authorisation

The European system for the authorisation of medicinal products for human and animal use was introduced in January 1995 with the objective of ensuring that safe, effective and high quality medicines could quickly be made available to citizens across the European Union.
The European system offers several routes for the authorisation of medicinal products:
  • The centralised procedure, which is compulsory for products derived from biotechnology, for orphan medicinal products and for medicinal products for human use which contain an active substance authorised in the Community after 20 May 2004 (date of entry into force of Regulation (EC) No 726/2004) and which are intended for the treatment of AIDS, cancer, neurodegenerative disorders or diabetes. The centralised procedure is also mandatory for veterinary medicinal products intended primarily for use as performance enhancers in order to promote growth…

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