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VX 787, PIMODIVIR, for Avian influenza
VRT-0928787
VX-787
vx 787
| Vertex Pharmaceuticals |
Janssen Pharmaceuticals, under license from Vertex Pharmaceuticals, is developing VX-787 and its back-up compound VX-353, an influenza A viral replication inhibitor, for treating influenza A virus infection, including pandemic and avian influenza strains. In May 2015, VX-787 was in phase II clinical trial.
Useful for treating influenza virus infection. For concurrent filing see WO2015073476 (claiming the polymorphic forms of VX-787) and WO2015073491 (claiming the composition comprising the hydrochloride salt of VX-787).
Polymorphic forms of hydrochloride (A,F and D) and tosylate salts (form A) of VX-787 are claimed. , useful for treating influenza virus infection. For concurrent filing see WO2015073481 (claiming the processes for the synthesis of VX-787 ) and WO2015073491 (claiming the composition comprising the hydrochloride salt of VX-787).
WO2010148197
http://www.google.com/patents/WO2010148197A1?cl=en
(1070) (2S,3S)-3-((2-(5-fluoro-1H-pyrrolo[2,3-b]pyridm-3-yl)-5- fluoropyrimidin-4-yl)amino)bicyclo[2.2.2]octane-2-carboxylic acid
(1070) (2S,3S)-3-((2-(5-fluoro-1H-pyrrolo[2,3-b]pyridm-3-yl)-5- fluoropyrimidin-4-yl)amino)bicyclo[2.2.2]octane-2-carboxylic acid
Compound 1070 was made in a similar fashion as described above for compounds 946 and 947.
………………….
WO 2013019828
http://www.google.com/patents/WO2013019828A1?cl=en
WO 2012083122
http://www.google.co.in/patents/WO2012083122A1?cl=en
Synthetic Scheme 1
(a) CHC13; (b) NaOMe, MeOH; (c) DPPA, Et3N, BnOH; (d) H2, Pd/C;
Synthetic Scheme 2
(a) Et3N, CH3CN; (b) cone. H2S04; (c) 9M H2S04; (d) Ag2C03, HOAc, DMSO, 100 °C; (e) X- phos, Pd2(dba)3, K3PO4, 2-methyl THF, H20, 120 °C (f) LiOH, THF, MeOH, 70 °C
Synthetic Scheme 3
(a) Et3N, THF; (b) chiral SFC separation; (c) 5-fluoro- l -(p-tolylsulfonyl)-3-(4,4,5,5-tetramethyl- l,3,2-dioxaborolan-
………………………
See new patents
WO2015073491
……………………………..
Discovery of a Novel, First-in-Class, Orally Bioavailable Azaindole Inhibitor (VX-787) of Influenza PB2
J. Med. Chem., 2014, 57 (15), pp 6668–6678
DOI: 10.1021/jm5007275
http://pubs.acs.org/doi/abs/10.1021/jm5007275
Vertex Pharmaceuticals Inc
Vertex Licenses VX-787 to Janssen Pharmaceuticals for the Treatment of Influenza
Vertex Pharmaceuticals Incorporated (Nasdaq: VRTX) today announced that it has entered into a licensing agreement with Janssen Pharmaceuticals, Inc. for the worldwide development and commercialization of VX-787, a novel medicine discovered by Vertex for the treatment of influenza. As part of the agreement, Vertex will receive an up-front payment of $30 million from Janssen and has the potential to receive additional development and commercial milestone payments as well as royalties on future product sales. Vertex completed a Phase 2a study of VX-787 in 2013 that showed statistically significant improvements in viral and clinical measurements of influenza infection. VX-787 is designed to directly inhibit replication of the influenza virus.
“With a deep history in developing new medicines for viral infections and diseases, Janssen is well-positioned to advance the global development of VX-787 for the treatment of influenza,” said Jeffrey Leiden, M.D., Ph.D., Chairman, President and Chief Executive Officer of Vertex. “This collaboration provides important support for the continued development of VX-787 in influenza and contributes to our financial strength to enable continued investment in our key development programs for cystic fibrosis and in research aimed at discovering new medicines.”
About the Collaboration
Under the terms of the collaboration, Janssen will have full global development and commercialization rights to VX-787. Vertex will receive a $30 million up-front payment from Janssen and could receive additional development and commercial milestone payments as well as royalties on future product sales. The collaboration, and the related $30 million up-front payment, is subject to the expiration of the waiting period under the Hart-Scott-Rodino Antitrust Improvements Act.
About VX-787
VX-787 is an investigational medicine that is designed to directly inhibit replication of influenza A, including recent H1 (pandemic) and H5 (avian) influenza strains, based on in-vitro data. VX-787’s mechanism represents a new class of potential medicines for the treatment of influenza, distinct from neuraminidase inhibitors, the current standard of care for the treatment of influenza. VX-787 is intended to provide a rapid onset of action and an expanded treatment window.
In a Phase 2a influenza challenge study, statistically significant improvements in viral and clinical measurements of influenza infection were observed after treatment with VX-787. The study met its primary endpoint and showed a statistically significant decrease in the amount of virus in nasal secretions (viral shedding) over the seven-day study period. In addition, at the highest dosing regimen evaluated in the study, there was a statistically significant reduction in the severity and duration of influenza-like symptoms. In this study, VX-787 was generally well-tolerated, with no adverse events leading to discontinuation. Those who took part in the study volunteered to be experimentally exposed to an attenuated form of live H3N2 influenza A virus. H3N2 is a common type of influenza virus and was the most common type observed in the 2012/2013 influenza season in the United States.
VX-787 was discovered by Vertex scientists.
About Influenza
Often called “the flu,” seasonal influenza is caused by influenza viruses, which infect the respiratory tract.1 The flu can result in seasonal epidemics2 and can produce severe disease and high mortality in certain populations, such as the elderly.3 Each year, on average 5 to 20 percent of the U.S. population gets the flu4 resulting in more than 200,000 flu-related hospitalizations and 36,000 deaths.5 The overall national economic burden of influenza-attributable illness for adults is $83.3 billion.5 Direct medical costs for influenza in adults totaled $8.7 billion including $4.5 billion for adult hospitalizations resulting from influenza-attributable illness.5 The treatment of the flu consists of antiviral medications that have been shown in clinical studies to shorten the disease and reduce the severity of symptoms if taken within two days of infection.6 There is a significant need for new medicines targeting flu that provide a wider treatment window, greater efficacy and faster onset of action.
About Vertex
Vertex is a global biotechnology company that aims to discover, develop and commercialize innovative medicines so people with serious diseases can lead better lives. In addition to our clinical development programs focused on cystic fibrosis, Vertex has more than a dozen ongoing research programs aimed at other serious and life-threatening diseases.
Founded in 1989 in Cambridge, Mass., Vertex today has research and development sites and commercial offices in the United States, Europe, Canada and Australia. For four years in a row, Science magazine has named Vertex one of its Top Employers in the life sciences. For additional information and the latest updates from the company, please visit www.vrtx.com.
Vertex’s press releases are available at www.vrtx.com.
| WO2002024705A1 | 13 Sep 2001 | 28 Mar 2002 | Charles Jackson Barnett | Stereoselective process for preparing cyclohexyl amine derivatives |
| WO2003015798A1 | 13 Aug 2002 | 27 Feb 2003 | Toyama Chemical Co Ltd | Novel virus proliferation inhibition/virucidal method and novel pyradine nucleotide/pyradine nucleoside analogue |
| WO2005095400A1 | 30 Mar 2005 | 13 Oct 2005 | Vertex Pharma | Azaindoles useful as inhibitors of jak and other protein kinases |
| WO2006069258A1 * | 20 Dec 2005 | 29 Jun 2006 | Amgen Inc | Substituted heterocyclic compounds and methods of use |
| WO2007084557A2 | 17 Jan 2007 | 26 Jul 2007 | Vertex Pharma | Azaindoles useful as inhibitors of janus kinases |
| WO2008079346A1 | 21 Dec 2007 | 3 Jul 2008 | Vertex Pharma | 5-cyan0-4- (pyrrolo [2, 3b] pyridine-3-yl) -pyrimidine derivatives useful as protein kinase inhibitors |
| WO2009073300A1 | 31 Oct 2008 | 11 Jun 2009 | Vertex Pharma | [1h- pyrazolo [3, 4-b] pyridine-4-yl] -phenyle or -pyridin-2-yle derivatives as protein kinase c-theta |
| WO2010011756A1 | 22 Jul 2009 | 28 Jan 2010 | Vertex Pharmaceuticals Incorporated | Pyrazolopyridine kinase inhibitors |
| WO2010011768A1 | 22 Jul 2009 | 28 Jan 2010 | Vertex Pharmaceuticals Incorporated | Tri-cyclic pyrazolopyridine kinase inhibitors |
| WO2010011772A2 | 22 Jul 2009 | 28 Jan 2010 | Vertex Pharmaceuticals Incorporated | Tri-cyclic pyrazolopyridine kinase inhibitors |
| WO2010148197A1 * | 17 Jun 2010 | 23 Dec 2010 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| WO2011008915A1 * | 15 Jul 2010 | 20 Jan 2011 | Abbott Laboratories | Pyrrolopyridine inhibitors of kinases |
| US20100038988 | 12 Aug 2008 | 18 Feb 2010 | Gannon Ramy | Stator and Method of Making the Same |
| WO2003015798A1 | Aug 13, 2002 | Feb 27, 2003 | Toyama Chemical Co Ltd | Novel virus proliferation inhibition/virucidal method and novel pyradine nucleotide/pyradine nucleoside analogue |
| WO2005095400A1 | Mar 30, 2005 | Oct 13, 2005 | Vertex Pharma | Azaindoles useful as inhibitors of jak and other protein kinases |
| WO2007084557A2 | Jan 17, 2007 | Jul 26, 2007 | Vertex Pharma | Azaindoles useful as inhibitors of janus kinases |
| WO2009073300A1 | Oct 31, 2008 | Jun 11, 2009 | Vertex Pharma | [1h- pyrazolo [3, 4-b] pyridine-4-yl] -phenyle or -pyridin-2-yle derivatives as protein kinase c-theta |
| WO2010011756A1 | Jul 22, 2009 | Jan 28, 2010 | Vertex Pharmaceuticals Incorporated | Pyrazolopyridine kinase inhibitors |
| WO2010011768A1 | Jul 22, 2009 | Jan 28, 2010 | Vertex Pharmaceuticals Incorporated | Tri-cyclic pyrazolopyridine kinase inhibitors |
| WO2010011772A2 | Jul 22, 2009 | Jan 28, 2010 | Vertex Pharmaceuticals Incorporated | Tri-cyclic pyrazolopyridine kinase inhibitors |
| WO2010148197A1 * | Jun 17, 2010 | Dec 23, 2010 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| US20100038988 | Aug 12, 2008 | Feb 18, 2010 | Gannon Ramy | Stator and Method of Making the Same |
……
.
Vertex Pharmaceuticals’ Boston Campus, United States of America
Lynette Hopkinson VP Commercial Regulatory Affairs, Global Regulatory Affairs Vertex Pharmaceuticals Incorporated, United States
swati Patel, a lead analyst, shared a toast with Mir Hussain, a systems engineer, at Vertex Pharmaceuticals during the Friday beer hour, which features beer and chips for employees.
On Fridays around 5 o’clock, after a hard week of work, Frank Holland likes to unwind with a beer. And he doesn’t have to leave work to get one.
Holland is a research scientist at Vertex Pharmaceuticals, which every Friday rings in “beer hour,” offering free adult beverages and munchies to its 1,300 Boston employees.
For Holland, the weekly ritual is a chance to escape the bubble of his chemistry lab and bump into colleagues from other departments — as well as Vertex’s top executives, who regularly attend. For those who prefer grapes to hops, there is also wine.
“Some of the other companies I worked at, you really had to go out of your way to meet people,” said Holland, 32. “At Vertex all you have to do is show up in the cafeteria on a Friday afternoon.”
Sure, free beer is common at hip tech offices; some even have their own bars. But Vertex, best known for its treatment for cystic fibrosis, was doing this way before it was cool. The beer-hour tradition goes back to the company’s founding days, in 1989. Back then, it was just two dozen people in a small office in Cambridge. Someone went to a corner store, bought a case of beer and some chips, and beer hour was born.
Virginia Carden Carnahan
Vice President, New Product Planning and Strategy, Vertex Pharmaceuticals
A scientist works in the lab at Boston-based Vertex Pharmaceuticals.
Vertex Pharmaceuticals Headquarters Lobby
…………
A Method to Identify Best Available Technologies (BAT) for Hydrogenation Reactors in the Pharmaceutical Industry
J. Flow Chem. 2012, 2(3), 77–82
http://www.akademiai.com/content/8652651g3378x686/?p=ab7c1bc4cd7740e1855623297649f542&pi=3
http://www.akademiai.com/content/8652651g3378x686/fulltext.pdf
| Journal of Flow Chemistry | |
| Publisher | Akadémiai Kiadó |
| ISSN | 2062-249X (Print) 2063-0212 (Online) |
| Subject | Flow Chemistry |
| Issue | Volume 2, Number 3/September 2012 |
| Pages | 77-82 |
| DOI | 10.1556/JFC-D-12-00014 |
Authors
* Author for correspondence: claude.debellefon@lgpc.cpe.fr1CNRS, CPE Lyon University of Lyon Villeurbanne France
Abstract
A methodology that may be applied to help in the choice of a continuous reactor is proposed. In this methodology, the chemistry is first described through the use of eight simple criteria (rate, thermicity, deactivation, solubility, conversion, selectivity, viscosity, and catalyst). Then, each reactor type is also analyzed from their capability to answer each of these criteria. A final score is presented using “spider diagrams.” Lower surfaces indicate the best reactor choice. The methodology is exemplified with a model substrate nitrobenzene and a target pharmaceutical intermediate, N-methyl-4-nitrobenzenemethanesulphonamide, and for three different continuous reactors, i.e., stirred tank, fixed bed, and an advanced microstructured reactor. Comparison with the traditional batch reactor is also provided.
Elemental Impurity Analysis in Pharmaceuticals.free download from Butterworth labs
Elemental Impurity Analysis in Pharmaceuticals
A method to identify the presence of heavy metals in pharmaceuticals was introduced in the United States Pharmacopeia more than 100 years ago.
Pharmaceutical companies are still using essentially the same method, known as the USP Heavy Metals Limit Test.
This paper will provide an overview of current method limitations, considerations for the new methodology and risk-based assessments being carried out by manufacturers.
see……Pharmaceuticals; Make in India
PM, MODI
Brand India Pharma aims to make the most of a booming domestic pharma industry
India’s pharma exports stood at 90,000 crore rupees ($15 billion) for the year 2013-2014, and are set to cross the 1 lakh crore rupees ($16.4 billion) mark in the current financial year. The Brand India Pharma campaign aims to tap into this value proposition, under the guidance of the Indian Ministry of Commerce and Industry, aiming to showcase the strengths of the Indian pharma industry.
With more than 10,500 manufacturing units and more than 3,000 pharma companies, India is ranked among the top six producers of pharmaceuticals worldwide, and is well-positioned to take advantage of its place in a global landscape.
READ AT
List of WHO Approved Pharma Plant in India
India’s spacecraft cost $74 million, a fraction of the $671 million spent by NASA’s MAVEN ……….SEPT 24 2014
READ AT
http://www.brandindiapharma.in/infographic-business/
India’s spacecraft reaches Mars orbit … and history
India’s spacecraft cost $74 million, a fraction of the $671 million spent by NASA’s MAVEN
24 sept 2014
India’s Mars Orbiter Mission successfully entered Mars’ orbit Wednesday morning, becoming the first nation to arrive on its first attempt and the first Asian country to reach the Red Planet.
“We have gone beyond the boundaries of human enterprise and human imagination,” declared India’s Prime Minister Narendra Modi, who watched from the space agency’s nerve center in Bangalore. “We have accurately navigated our spacecraft through a route known to a very few.”
The staff at the Indian Space Research Organization erupted into applause and cheers after learning that the Mars Orbiter Mission, also known as Mangalyaan, reached the planet’s orbit and made history.
Before Wednesday, only the United States, Europe and the Soviets have successfully sent spacecraft to Mars.
Photos: India’s first Mars orbiter“The odds were stacked against us,” Modi said. “Of the 51 missions attempted so far, a mere 21 had succeeded. But we have prevailed.”
And India reached Mars with significantly less money.
With a price tag of $74 million, the Mars Orbiter Mission cost a mere fraction of the $671 million NASA spent on its MAVEN spacecraft, which arrived to Mars earlier this week. Some space observers noted that India’s Mars orbiter cost less than the $100 million budget for the space thriller film “Gravity.”
Interactive: Exploring Mars from Viking to MAVEN
“It shows how optimal is the design, that way we’re able to cut cost and we’re not compromising quality,” said S. Satish, a space expert based in Bangalore.
The groundbreaking Mars mission wasn’t without controversy — with some critics who said India should spend the money on other issues.
The spacecraft launched on November 5, and has traveled over 650 million kilometers to enter Mars orbit. Its mission is to orbit the Red Planet, mapping its surface and studying the atmosphere. The Mars Orbiter kicked off its interplanetary debut with its own Twitter account.
The mission has been freighted with patriotic significance for India since its inception and is seen as a symbolic coup over its rival, China, which is also ramping up its space ambitions.
India launches mission to Mars
China’s joint mission with Russia in 2011, which contained the Chinese Mars satellite Yinhuo-1, stalled and eventually fell back to Earth. Japan’s 1998 attempt with the spacecraft Nozomi was also unsuccessful due to fuel problems.
Once nears Mars’ orbit, India’s spacecraft had to execute a series of complicated and critical maneuvers. About half of all spacecraft sent on missions to the planet have veered off course, malfunctioned or crashed.
India’s Mars Orbiter Mission is in the company of NASA’s two Mars rovers on the ground, a European orbiter and NASA orbiters including the MAVEN, which has been there since Sunday.
The United States has expressed interest in cooperating with India as their spacecraft gather data about the planet.
MAKE IN INDIA
http://makeinindia.com/sector/pharmaceuticals/
Piramal Drops Drug Discovery,…………. Pharmaceuticals: Risks and regulations convince the Indian company to reallocate resources
In a move that raises questions about the future of drug research in India, Piramal Enterprises will end its drug discovery activities. The decision—which involves possible job losses—will affect several hundred scientists, many of whom were recruited internationally to work in Mumbai in one of India’s most sophisticated pharmaceutical labs.
The company has been considered an Indian leader in drug research since opening its discovery labs in 2004. Within the firm, drug discovery was championed by the vice chairman, Swati A. Piramal, a medical doctor who also holds a master’s degree from the Harvard School of Public Health.
“After reevaluating the risk-benefits of new chemical entity research, the company decided to focus resources on our other areas of R&D with shorter development timelines and different risk profiles,” Piramal tells C&EN.
read all at
http://cen.acs.org/articles/92/i37/Piramal-Drops-Drug-Discovery.html
Piramal Enterprises, which sold off its domestic formulations business to Abbott in a multi-billion dollar deal a few years ago, is now shutting down its Mumbai-based R&D unit which would in effect bring to an end its early stage drug discovery business.
Separate media reports, citing Swati Piramal, part of the promoter group of the diversified firm and wife of group chief Ajay Piramal, said, the decision to move away from the drug discovery business was taken given the costs of basic research.
The company would now focus on molecules at an advanced stage of development; resources would be redeployed from basic research to the clinical unit.
Its other research facilities are located in Chennai, Hyderabad, Ahmedabad and Indore, which would continue to be functional.
Although Piramal Enterprises retains its exposure to healthcare as a sector, after selling the key pharma business, it is now more associated with financial services, including investments in infrastructure and real estate sectors.
In an unrelated development, the firm is forming a joint venture with Navin Fluorine International Limited, an Arvind Mafatlal Group company, to develop, manufacture and sell specialty fluorochemicals with a focus on applications in healthcare, according to a company release.
As per the agreement, Piramal Enterprises will hold 51 per cent of the equity share capital of the proposed joint venture company, whereas the remaining 49 per cent will be held by Navin.
In the first phase of development, the JV is expected to invest around Rs 120 crore in India for this project.
Mumbai-based Navin Fluorine has a turnover of around $100 million. It specialises in specialty fluorine. It had acquired UK-based Manchester Organics, a specialty fluorochemicals research company in 2011.
Read more at: http://www.livemint.com/Companies/7weGbimcrdp7lrKH0YaSnL/Piramal-to-exit-drug-discovery-business.html?utm_source=copy
New Drug Approvals 