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1
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Irreversible protein kinase inhibitors: balancing the benefits and risks

Barf, Tjeerd ; Kaptein, Allard

Journal of medicinal chemistry, 26 July 2012, Vol.55(14), pp.6243-62 [Peer Reviewed Journal]

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2
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Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia

Byrd, John C ; Harrington, Bonnie ; O'Brien, Susan ; Jones, Jeffrey A ; Schuh, Anna ; Devereux, Steve ; Chaves, Jorge ; Wierda, William G ; Awan, Farrukh T ; Brown, Jennifer R ; Hillmen, Peter ; Stephens, Deborah M ; Ghia, Paolo ; Barrientos, Jacqueline C ; Pagel, John M ; Woyach, Jennifer ; Johnson, Dave ; Huang, Jane ; Wang

The New England journal of medicine, 28 January 2016, Vol.374(4), pp.323-32 [Peer Reviewed Journal]

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In Vivo Knockdown of TAK1 Accelerates Bone Marrow Proliferation/Differentiation and Induces Systemic Inflammation

Vink, Paul ; Smout, Wendy ; Driessen-Engels, Lilian ; de Bruin, Alex ; Delsing, Dianne ; Krajnc-Franken, Magda ; Jansen, Aswin ; Rovers, Eric ; van Puijenbroek, André ; Nolte, Martijn ; Garritsen, Anja

PLoS One, Mar 2013, Vol.8(3), p.e57348 [Peer Reviewed Journal]

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4
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Preclinical Evaluation of the Novel BTK Inhibitor Acalabrutinib in Canine Models of B-Cell Non-Hodgkin Lymphoma

Harrington, Bonnie ; Gardner, Heather ; Izumi, Raquel ; Hamdy, Ahmed ; Rothbaum, Wayne ; Coombes, Kevin ; Covey, Todd ; Gulrajani, Michael ; Krejsa, Cecile ; Coss, Christopher ; Russell, Duncan ; Zhang, Xiaoli ; Urie, Bridget ; London, Cheryl ; Byrd, John ; Johnson, Amy ; Kisseberth, William

PLoS One, Jul 2016, Vol.11(7), p.e0159607 [Peer Reviewed Journal]

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The Bruton Tyrosine Kinase (BTK) Inhibitor Acalabrutinib Demonstrates Potent On-Target Effects and Efficacy in Two Mouse Models of Chronic Lymphocytic Leukemia

Herman, Sarah E M ; Montraveta, Arnau ; Niemann, Carsten U ; Mora-Jensen, Helena ; Gulrajani, Michael ; Krantz, Fanny ; Mantel, Rose ; Smith, Lisa L ; Mcclanahan, Fabienne ; Harrington, Bonnie K ; Colomer, Dolors ; Covey, Todd ; Byrd, John C ; Izumi, Raquel ; Kaptein, Allard ; Ulrich, Roger ; Johnson, Amy J ; Lannutti, Brian J ; Wiestner, Adrian ; Woyach

Clinical cancer research : an official journal of the American Association for Cancer Research, 01 June 2017, Vol.23(11), pp.2831-2841 [Peer Reviewed Journal]

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Severity of murine collagen‐induced arthritis correlates with increased CYP7B activity: Enhancement of dehydroepiandrosterone metabolism by interleukin‐1β

Dulos, John ; Verbraak, Evert ; Bagchus, Wilma M. ; Boots, Annemieke M. H. ; Kaptein, Allard

Arthritis & Rheumatism, October 2004, Vol.50(10), pp.3346-3353 [Peer Reviewed Journal]

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7
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Tumour necrosis factor-alpha stimulates dehydroepiandrosterone metabolism in human fibroblast-like synoviocytes: a role for nuclear factor-kappaB and activator protein-1 in the regulation of expression of cytochrome p450 enzyme 7b

Dulos, John ; Kaptein, Allard ; Kavelaars, Annemieke ; Heijnen, Cobi ; Boots, Annemieke

Arthritis research & therapy, 2005, Vol.7(6), pp.R1271-80 [Peer Reviewed Journal]

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8
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Novel ATP competitive MK2 inhibitors with potent biochemical and cell-based activity throughout the series

Oubrie, Arthur ; Kaptein, Allard ; de Zwart, Edwin ; Hoogenboom, Niels ; Goorden, Rianne ; van de Kar, Bas ; van Hoek, Maaike ; de Kimpe, Vera ; van Der Heijden, Ruud ; Borsboom, Judith ; Kazemier, Bert ; de Roos, Jeroen ; Scheffers, Michiel ; Lommerse, Jos ; Schultz-Fademrecht, Carsten ; Barf, Tjeerd

Bioorganic & Medicinal Chemistry Letters, 01 January 2012, Vol.22(1), pp.613-618 [Peer Reviewed Journal]

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9
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Acalabrutinib (ACP-196): A Covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profile

Barf, Tjeerd ; Covey, Todd ; Izumi, Raquel ; Van De Kar, Bas ; Gulrajani, Michael ; Van Lith, Bart ; Van Hoek, Maaike ; De Zwart, Edwin ; Mittag, Diana ; Demont, Dennis ; Verkaik, Saskia ; Krantz, Fanny ; Pearson, Paul G ; Ulrich, Roger ; Kaptein, Allard

The Journal of pharmacology and experimental therapeutics, November 2017, Vol.363(2), pp.240-252 [Peer Reviewed Journal]

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10
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The IL1 receptor accessory protein is responsible for the recruitment of the interleukin-1 receptor associated kinase to the IL1/IL1 receptor I complex

Volpe, Filippo ; Clatworthy, Jonathan ; Kaptein, Allard ; Maschera, Barbara ; Griffin, Anne-Marie ; Ray, Keith

FEBS Letters, 1997, Vol.419(1), pp.41-44 [Peer Reviewed Journal]

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11
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Cyp7b activity and mRNA expression is inhibited by SN50 in fibroblast-like synoviocytes

John Dulos ; Allard Kaptein ; Annemieke Kavelaars ; Cobi Heijnen ; Annemieke Boots

2011

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12
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Simplified diagram of the proposed signalling events leading to Cyp7b gene transcription in synovial fibroblasts

John Dulos ; Allard Kaptein ; Annemieke Kavelaars ; Cobi Heijnen ; Annemieke Boots

2011

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13
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Regulation of Cyp7b mRNA expression and activity in FLS

John Dulos ; Allard Kaptein ; Annemieke Kavelaars ; Cobi Heijnen ; Annemieke Boots

2011

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14
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The effect of the MAPK inhibitors PD98059 or SB203580 on TNF-α-induced Cyp7b activity

John Dulos ; Allard Kaptein ; Annemieke Kavelaars ; Cobi Heijnen ; Annemieke Boots

2011

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15
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The effect of the MAPK inhibitors PD98059 or SB203580 on TNF-α-induced Cyp7b activity

John Dulos ; Allard Kaptein ; Annemieke Kavelaars ; Cobi Heijnen ; Annemieke Boots

2011

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16
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Regulation of Cyp7b mRNA expression and activity in FLS

John Dulos ; Allard Kaptein ; Annemieke Kavelaars ; Cobi Heijnen ; Annemieke Boots

2011

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17
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PSI inhibits the TNF-α-induced increase in 7α-OH-DHEA

John Dulos ; Allard Kaptein ; Annemieke Kavelaars ; Cobi Heijnen ; Annemieke Boots

2011

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18
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Simplified diagram of the proposed signalling events leading to Cyp7b gene transcription in synovial fibroblasts

John Dulos ; Allard Kaptein ; Annemieke Kavelaars ; Cobi Heijnen ; Annemieke Boots

2011

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19
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Cyp7b activity and mRNA expression is inhibited by SN50 in fibroblast-like synoviocytes

John Dulos ; Allard Kaptein ; Annemieke Kavelaars ; Cobi Heijnen ; Annemieke Boots

2011

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20
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NF-κB and AP-1 binding sites within the Cyp7b promoter

John Dulos ; Allard Kaptein ; Annemieke Kavelaars ; Cobi Heijnen ; Annemieke Boots

2011

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21
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PSI inhibits the TNF-α-induced increase in 7α-OH-DHEA

John Dulos ; Allard Kaptein ; Annemieke Kavelaars ; Cobi Heijnen ; Annemieke Boots

2011

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22
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NF-κB and AP-1 binding sites within the Cyp7b promoter

John Dulos ; Allard Kaptein ; Annemieke Kavelaars ; Cobi Heijnen ; Annemieke Boots

2011

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23
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Article
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Discovery of 8-Amino-imidazo[1,5- a ]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis

Liu, Jian ; Guiadeen, Deodial ; Krikorian, Arto ; Gao, Xiaolei ; Wang, James ; Boga, Sobhana Babu ; Alhassan, Abdul-Basit ; Yu, Younong ; Vaccaro, Henry ; Liu, Shilan ; Yang, Chundao ; Wu, Hao ; Cooper, Alan ; de Man, Jos ; Kaptein, Allard ; Maloney, Kevin ; Hornak, Viktor ; Gao, Ying-Duo ; Fischmann, Thierry O ; Raaijmakers, Hans ; Vu-Pham, Diep ; Presland, Jeremy ; Mansueto, My ; Xu, Zangwei ; Leccese, Erica ; Zhang-Hoover, Jie ; Knemeyer, Ian ; Garlisi, Charles G ; Bays, Nathan ; Stivers, Peter ; Brandish, Philip E ; Hicks, Alexandra ; Kim, Ronald ; Kozlowski, Joseph A Argonne National Lab. (Anl), Argonne, Il (United States). Advanced Photon Source (APS) (Corporate Author)

ACS Medicinal Chemistry Letters, 11 February 2016, Vol.7(2) [Peer Reviewed Journal]

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24
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Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors

Kaptein, Allard ; Oubrie, Arthur ; Zwart, Edwin de ; Hoogenboom, Niels ; Wit, Joeri de ; Kar, Bas van de ; Hoek, Maaike van ; Vogel, Gerard ; Kimpe, Vera de ; Schultz-Fademrecht, Carsten ; Borsboom, Judith ; Zeeland, Mario van ; Versteegh, Judith ; Kazemier, Bert ; Roos, Jeroen de ; Wijnands, Frank ; Dulos, John ; Jaeger, Martin ; Leandro-Garcia, Paula ; Barf, Tjeerd

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(12), pp.3823-3827 [Peer Reviewed Journal]

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25
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Structure-based lead identification of ATP-competitive MK2 inhibitors

Barf, Tjeerd ; Kaptein, Allard ; Wilde, Sander de ; Heijden, Ruud van Der ; Someren, Richard van ; Demont, Dennis ; Schultz-Fademrecht, Carsten ; Versteegh, Judith ; Zeeland, Mario van ; Seegers, Nicole ; Kazemier, Bert ; Kar, Bas van de ; Hoek, Maaike van ; Roos, Jeroen de ; Klop, Henri ; Smeets, Ruben ; Hofstra, Claudia ; Hornberg, Jorrit ; Oubrie, Arthur

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(12), pp.3818-3822 [Peer Reviewed Journal]

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26
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Inhibition of cyclo-oxygenase 2 expression in colon cells by the chemopreventive agent curcumin involves inhibition of NF-κB activation via the NIK/IKK signalling complex

Simon M Plummer ; Karen A Holloway ; Margaret M Manson ; Rebecca Jl Munks ; Allard Kaptein ; Stuart Farrow ; Lynne Howells

Oncogene, 1999, Vol.18(44), p.6013 [Peer Reviewed Journal]

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27
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6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors

Cai, Jiaqiang ; Baugh, Mark ; Black, Darcey ; Long, Clive ; Jonathan Bennett, D ; Dempster, Maureen ; Fradera, Xavier ; Gillespie, Jonathan ; Andrews, Fiona ; Boucharens, Sylviane ; Bruin, John ; Cameron, Kenneth S ; Cumming, Iain ; Hamilton, William ; Jones, Philip S ; Kaptein, Allard ; Kinghorn, Emma ; Maidment, Maurice ; Martin, Iain ; Mitchell, Ann

Bioorganic & Medicinal Chemistry Letters, 01 August 2010, Vol.20(15), pp.4350-4354 [Peer Reviewed Journal]

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28
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Studies on the interaction between TWEAK and the death receptor WSL-1/TRAMP (DR3)

Kaptein, Allard ; Jansen, Mieke ; Dilaver, Gonul ; Kitson, Jeremy ; Dash, Laura ; Wang, Edward ; Owen, Michael J ; Bodmer, Jean-Luc ; Tschopp, Jurg ; Farrow, Stuart N

FEBS Letters, 2000, Vol.485(2), pp.135-141 [Peer Reviewed Journal]

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29
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Potency and Selectivity of BTK Inhibitors in Clinical Development for B-Cell Malignancies

Kaptein, Allard ; de Bruin, Gerjan ; Hoek, Maaike Emmelot-van ; van de Kar, Bas ; de Jong, Anouk ; Gulrajani, Michael ; Demont, Dennis ; Covey, Todd ; Mittag, Diana ; Barf, Tjeerd

Clinical Lymphoma, Myeloma and Leukemia, September 2019, Vol.19, pp.S316-S317 [Peer Reviewed Journal]

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30
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No Effect of Fibrates on Synthesis of Apolipoprotein(a) in Primary Cultures of Cynomolgus Monkey and Human Hepatocytes: Apolipoprotein A-I Synthesis Increased

Neele, Diana M ; Kaptein, Allard ; Huisman, Holger ; de Wit, Elly C.M ; Princen, Hans M.G

Biochemical and Biophysical Research Communications, 17 March 1998, Vol.244(2), pp.374-378 [Peer Reviewed Journal]

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31
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Apolipoprotein E polymorphism affects plasma levels of lipoprotein(a)

de Knijff, Peter ; Kaptein, Allard ; Boomsma, Dorret ; Princen, Hans M.G ; Frants, Rune R ; Havekes, Louis M

Atherosclerosis, 1991, Vol.90(2), pp.169-174 [Peer Reviewed Journal]

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32
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Butyrate stimulates the secretion of apolipoprotein B-100-containing lipoproteins from HepG2 cells by inhibiting the intracellular degradation

Kaptein, Allard ; de Wit, Elly C.M ; Princen, Hans M.G

Biochimica et Biophysica Acta (BBA)/Lipids and Lipid Metabolism, 1994, Vol.1213(3), pp.349-356

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33
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U.S. Patent and Trademark Office Receives Patent Application for Method for Inhibiting Binding to B-Cell Receptor from Farrow Stuart Neville, Kaptein Allard, Kitson Jeremy David Alisdair, Winder Alison Janet and Glaxo Group Limited

Global IP News. Pharmaceutical Patent News, Mar 7, 2014

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34
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Supporting smoking cessation in healthcare: obstacles in scientific understanding and tobacco addiction management

Korte, de, D. ; Schayck, van, O.C.P. ; Spiegel, van, P. ; Kaptein, A.A. ; Sachs, A.P.E. ; Rutten-van Mölken, M.P.M.H. ; Chavannes, N.H. ; Tromp-Beelen, T. ; Bes, R.E. ; Allard, R.H.B. ; Peeters, G. ; Kliphuis, L. ; Schouten, J.W. ; Gennip, van, L. ; Ommen, van, R. ; Asin, J.

Health (Irvine), 2010, Vol.02(11), pp.1272-1279 [Peer Reviewed Journal]

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35
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36
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Acerta Pharma BV Files Taiwan Patent Application for Therapeutic Combinations of a BTK Inhibitor, a Pi3k Inhibitor and/or a Jak-2 Inhibitor

Global IP News. Pharmaceutical Patent News, Oct 5, 2016

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37
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How Can Doctors Help Their Patients to Return to Work? (Best Practice)

Verbeek, Jos H

PLoS Medicine, 2006, Vol.3(3), p.e88 [Peer Reviewed Journal]

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38
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U.S. Patent and Trademark Office Publishes Acerta Pharma's Patent Application for Therapeutic Combinations of an Irak4 Inhibitor and a BTK Inhibitor

Global IP News. Pharmaceutical Patent News, Mar 8, 2020

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39
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PERCEPCION DE ENFERMEDAD: Una aproximación a partir del "Illness Perception Questionnaire"/ ILLNESS PERCEPTION

Quiceno, Japcy ; Vinaccia, Stefano

Psicología desde el Caribe, Jan 2010, Issue 25 [Peer Reviewed Journal]

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40
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British, Dutch Inventors Develop Tumor Necrosis Factors Ligand Family Member

US Fed News Service, Including US State News, Sep 22, 2008

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41
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US Patent Issued to Merck Sharp & Dohme on July 8 for "MK2 inhibitors" (Dutch, Italian Inventors)

US Fed News Service, Including US State News, Jul 8, 2014

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42
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WIPO ASSIGNS PATENT TO N.V. ORGANON FOR "MK2 INHIBITORS" (DUTCH INVENTORS)

US Fed News Service, Including US State News, Jun 24, 2011

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