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VX 787, PIMODIVIR, for Avian influenza

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(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
(2S,3S)-3-((5-Fluoro-2-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl)amino)bicyclo[2.2.2]octane-2-carboxylic Acid
399.394
C20 H19 F2 N5 O2
JNJ-872
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

WO-2015073481

WO-2015073476

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

51

1H NMR (300 MHz, DMSO-d6) δ 12.71 (br s, 1H), 8.58 (s, 1H), 8.47 (dd, J = 9.6, 2.8 Hz, 1H), 8.41 (d, J = 4.8 Hz, 1H), 8.39–8.34 (m, 1H), 4.89–4.76 (m, 1H), 2.94 (d, J = 6.9 Hz, 1H), 2.05 (br s, 1H), 1.96 (br s, 1H), 1.68 (complex m, 7H);
13C NMR (300 MHz, DMSO-d6) δ 174.96, 157.00, 155.07, 153.34, 152.97, 145.61, 142.67, 140.65, 134.24, 133.00, 118.02, 114.71, 51.62, 46.73, 28.44, 28.00, 24.90, 23.78, 20.88, 18.98;
LCMS gradient 10–90%, 0.1% formic acid, 5 min, C18/ACN, tR = 2.24 min, (M + H) 400.14;
HRMS (ESI) of C20H20F2N5O2 [M + H] calcd, 400.157 95; found, 400.157 56.
Article
June 18, 2014

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

…………


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DR ANTHONY CRASTO

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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 GLENMARK PHARMACEUTICALS LTD, Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 29 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 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 29 year tenure till date Aug 2016, Around 30 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 9 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 25 Lakh plus views on dozen plus blogs, 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 13 lakh plus views on New Drug Approvals Blog in 212 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

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