About us-old

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IntelliSyn was founded by Jeffrey Albert in 2011 to bring together outstanding pharma researchers in the Montreal area following the closure of major sites by AstraZeneca, Boehringer Ingelheim, and Merck Frosst.  Within these companies, our team members worked with scientific CROs from all across the world and came to understand the frequent challenges and frustrations with these CROs.  IntelliSyn was formed to bring highly efficient capabilities and experienced personnel to rapidly advance client’s projects on a reliable, secure, and economical basis.

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April 2014:  IntelliSyn successfully reaches its milestone with Epigenetix and partners its BRD4 inhibitor project with the NeoMed Institute to advance to clinical trials.

July 2013:  IntelliSyn expands to new facilities at the NeoMed Institute the Montreal Technopark.  It is a first-tier R&D facility that has been specifically designed for early R&D work.

April 2013:  IntelliSyn receives NSERC grant in collaboration with Prof. N. Moitessier of McGill University to advance “Novel molecular scaffolds as epigenetic-directed anti-cancer drug candidates”.

January 2013:  IntelliSyn is named as a member of Pharmaqam; a consortium of 50 researchers from 17 different institutions with common interests in biopharmaceutical research. The center focuses on the molecular aspects of biopharmaceutical research and brings together complementary, cutting-edge research essential for efficient drug discovery.  http://www.pharmaqam.uqam.ca/

August 2012:  IntelliSyn is selected as the exclusive Med Chem partner for Epigenetix, a US-based biotechnology group focusing on novel epigenetic mechanisms for cancer and other indications. IntelliSyn provides full medicinal chemistry design, synthesis, and DMPK support.

June  2012:  IntelliSyn is founded at the Biotech Incubator at the University of Quebec in downtown Montreal.

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Jeffrey Albert, Ph.D. CEO and Director of Chemistry

Jeff has a 20-year track record in the identification and validation of new drug targets, discovering initial chemical leads, and in advancing those leads through pre-clinical discovery to Phase-1.  He served as Head of Lead Generation in Neuroscience Chemistry at AstraZeneca.  He has authored or co-authored 4 book chapters, 32 scientific publications, filed more than 40 patents, and frequently lectures on drug discovery both in the United States and internationally.

Malken Bayrakdarian, Ph.D. Associate Director of Chemistry

Malken has 15 years of experience in drug discovery at the AstraZeneca research center in Montreal and contributed to the discovery of several clinical drug candidates. Over the years, he has developed extensive experience in a research-driven organization, been involved in the evaluation of new biological targets, and managed collaborations with chemistry CROs across North America, Europe, and Asia. In his role as Project Chemistry Leader, he led chemistry activities to advance a clinical candidate development up to Phase-2 trials.

Eric Grazzini, Ph.D. Associate Director of Biology

Eric served for 16 years within major pharma as a pharmacology project leader.  He has extensive experience in assay development and mechanistic analysis.  He has particular expertise in the biology of GPCRs, ion channels, and transporters.  He has authored or co-authored >25 publications appearing in Nature, Nature Neuroscience, Nature Cell Biology, and PNAS.

Shawn Johnstone, Ph.D. Associate Director of Chemistry

Shawn served as a medicinal chemistry project leader within AstraZeneca for >10 years within their Canadian and Swedish research centers. He has driven numerous projects from concept up to Phase-2 trials.  He has particular expertise in the chemistry of GPCRs, ion channels as well as in total synthesis and organometallic chemistry. He has a Ph.D. in synthetic chemistry from the University of Montreal and an M.Sc. in organometallic chemistry from the University of Toronto.

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IntelliSyn is located at the NeoMed Institute, which is a state-of-the-art pharma research facilityfor chemistry, biology, and drug metabolism studies. We are within 5 miles from the Montreal International Airport. Our proximity to downtown Montreal facilitates collaborations with leading researchers in the pharma and academic communities and affords access to an outstanding pool of scientific talent.

Chemistry

IntelliSyn’s laboratories are fully-equipped to produce compounds from milligram up to kilogram quantities. We perform a full range of synthetic and organometallic chemistries, including anhydrous/air-sensitive, microwave, and photochemical reactions. Extensive purification systems include prep and semi-prep UV and mass-triggered HPLC, CombiFlash Rf, CombiFlash Companion, Companion XL, and chiral SFC. Analytical systems include a Bruker 500 MHz NMR, Waters mass spectrometers, polarimeters, and chiral SFC.

Screening

IntelliSyn, in partnership with the NeoMed Institute, offers to client’s extensive capabilities and screening technologies:

  • Cellular functional screening
    • Label free screening technology (EPIC)
    • Calcium imaging (Hammamatsu FDSS7000, FLIPR 384 wells plate format)
  • Biochemical assays
    • Intracellular signalling (cAMP, IP3, beta arrestin, ERK 1/2)
  • Radioligand binding
    • GTPgS binding (SPA and Filtration)
  • Electrophysiology
    • PatchXpress
    • Q-Patch
  • Drug mechanism of action analysis
    • Allosterism, inverse agonism, kinetics

DMPK

Using the in-house rodent vivarium and analytical facilities, we regularly carry out drug exposure studies (peripheral and central) and determine pharmacokinetic profiles (IV/PO/PK) in mouse and rat.

Security

IntelliSyn uses an internally-secured technology infrastructure with pharma-compliant data security. Our secured electronic laboratory notebooks (ELNs) system can be accessed by clients to keep up-to-date with the progress of their projects. All of our scientists have ready access to industry standard on-line literature and patent searching capabilities, such as SciFinder and scientific journals.

[/vc_column_text][dt_gap height=”25″][/vc_column][/vc_row][vc_row anchor=”publications” margin_top=”0″ margin_bottom=”0″ padding_left=”40″ padding_right=”40″ bg_position=”top” bg_repeat=”no-repeat” bg_cover=”false” bg_attachment=”false” padding_top=”40″ padding_bottom=”40″ parallax_speed=”0.1″][vc_column width=”1/1″][dt_fancy_title title=”Publications” title_align=”center” title_size=”h3″ title_color=”default” title_bg=”disabled” separator_color=”default”][dt_gap height=”25″][vc_column_text]Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors.  Varnes, J. G.; Geschwindner, S.; Holmquist, C. R.; Forst, J.; Wang, X.; Dekker, N.; Scott, C. W.; Tian, G.; Wood, M. W.; Albert, J. S. Bioorg. Med. Chem. Lett. 2016, 26, 197.  Link

Bromodomain inhibitors regulate the C9ORF72 locus in ALS. Zeier, Z.; Esanov, R.; Volmar, C.-H.; Johnstone, A. L.; Halley, P.; Khoury, N.; Brothers, S. P.; Belle, K. C.; DeRosa, B. A.; Dykxhoorn, D. M.; van, B. M.; Rademakers, R.; Albert, J.; Wuu, J.; Benatar, M.; Wahlestedt, C. Exp Neurol 2015.  Link

Discovery of a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine and a 1-aryloxyisoquinoline series of TRPA1 antagonists.  Hu, YJ; St.-Onge, M; Laliberte, S; Vallee, F, Jin, S; Bedard, L; Labrecque, J; Albert, JS. Biorg. Med. Chem. Lett., 2014, 24, 3199. Link

Discovery of a series of aryl-N-(3-(alkylamino)-5-(trifluoromethyl)phenyl)benzamides as TRPA1 antagonists.  Laliberte, S; Vallee, F; Fournier, PA; Bedard, L; Labrecque, J; Albert, JS. Biorg. Med. Chem. Lett., 2014, 24, 3204. Link

Development of a Plate-Based Optical Biosensor Fragment Screening Methodology to Identify Phosphodiesterase 10A Inhibitors.  Geschwindner S, Dekker N, Horsefield R, Tigerstrom A, Johansson P, Scott CW, Albert JS, J. Med. Chem., 2013.  Link

Multiple Roles of Transient Receptor Potential (TRP) Channels in Inflammatory Conditions and Current Status of Drug Development, Radresa, O,Paré, M, Albert, JS, 2013, Current Topics in Med. Chem., 2013Link

Targets and Emerging Therapies for Schizophrenia; 2012, Wiley Publications, Editors:  Albert, JS, Wood, MW.Link

Progress in the Exploration and Development of GlyT1 Inhibitors for Schizophrenia; Albert, JS, Wood, MW.;2012. Link

Isoquinucline-based GlyT1 inhibitors for schizophrenia: Discovery, optimization, synthesis, and in vivo pharmacology, Albert, JS; ACS National Symposium, 2012.

Potent and orally efficacious benzothiazole amides as TRPV1 antagonists.  Brown, W, Johnstone, S, Jones, P, Walpole, C, Griffin, AW, et al.  BMCL, 2012, 22, 6205.  Link

N-Methyl-3-(tetrahydro-2H-pyran-4-yl)-2,3,4,9-tetrahydro-1H-carbazole-6-carboxamides as a novel class of cannabinoid receptors agonists with low CNS penetration.  Zhongyong W; Tremblay, M; Johnstone, S; Tomaszewski, M; Brown, W; Walpole, C; Page, D; et al. BMCL, 2012, 22, 3884.  Link

Fragment-based lead discovery; Albert, JS, 2010, Wiley Publications.Link

Discovery of new high-affinity PDE10 inhibitors using fragment based lead generation and knowledge-based design, Albert, JS; ACS National Symposium, 2012

Identification of high-affinity β-secretase inhibitors using fragment-based lead generation; Albert, JS, Edwards, PD, 2008.Link

An integrated approach to fragment-based lead generation: philosophy, strategy and case studies from AstraZeneca’s drug discovery programmes, Albert, JS; Blomberg, N., et al.Link

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