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.
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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-
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See new patents
WO2015073491
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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 |
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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
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Filed under: Phase2 drugs, Uncategorized Tagged: Avian influenza, influenza virus, Pharmaceuticals, phase 2, VERTEX, Vertex Pharmaceuticals Incorporated, VX 787