Design Training

Sasikumar T Kuttappan, Ph.D

(Formerly T. K. Sasikumar)**

** **** ****, ******, *** Jersey, 08817

Home Phone: 732-***-**** ( Cell Phone: 908-***-**** ( email:

***********@*****.***

Highly experienced, result oriented medicinal chemist with proficiency in

synthetic organic chemistry, structure based drug design, combinatorial

chemistry and preclinical drug discovery. Excellent cross-functional team

work with chemists and biologists and experienced in supervising and

training highly productive associates. Proficient in analytical techniques

such as NMR, IR, HPLC, LC-MS and mass spec. Seeking challenging

managerial/scientific career position in preclinical drug discovery that

can utilize my skills in the best possible way to achieve the company

goals.

EXPERIENCE

Merck Research Laboratories, Kenilworth, NJ (Formerly Schering-Plough

Research Institute)

Principal Scientist

May 2007- Dec 20,

2011

. Worked on BACE inhibitor program for the treatment of Alzheimer's

Disease. Knowledge in structure based drug discovery. Extensively

collaborated with structural chemistry group to design novel chemotypes

and execute their synthesis.

. Challenging chemistry problems solved. Multiple patents filed. Excellent

analytical skills.

. Strictly adheres to the safety protocols in the lab.

. Member of BACE chemistry team that recommended an API for development in

2011.

. Worked on the long acting DPP-4 inhibitor program. This program was aimed

at the back-up of a multimillion dollar drug Januvia for the treatment of

type 2 diabetes with longer duration of action. Worked closely with the

structural chemistry team to come up with innovative structures. Patents

filed.

. A suitable lead for the LRRK2 program (hit-to-lead) for Parkinson's

Disease was discovered and later coordinated the successful transfer of

the program to the Merck West Point site. Patents under preparation.

Associate Principal Scientist

April 2002-May 2007

. Complex natural product like tetracyclic sulfonamide compounds prepared

as highly potent gamma secretase inhibitors for the treatment of

Alzheimer's Disease. Three patents published in this program.

. Multi-gram synthesis of tetracyclic compound, SCH 1391333, was achieved

in 16 step total synthesis with an overall yield of 1.6%. Extensive SAR

studies were carried out in this series.

. Member of gamma secretase team that discovered the Phase-1 human clinical

trial candidate SCH 1390499 (900229) for the treatment of Alzheimer's

Disease. Actively contributed to the design of efficient synthetic routes

and multi-gram scale-up campaign of SCH 1390499.

. New tricyclic gamma secretase inhibitors were discovered. Two analogs

(SCH 1391336 and 1391338) were considered as back-up candidates to the

current clinical candidate SCH 1390499.

. Experienced in large scale reactions (~200 g scale).

. Based on gamma secretase work, four papers have been published in peer

reviewed journals.

. Highly efficacious and orally active tricyclic triazinofluorenones were

synthesized as mGluR1 inhibitors. These compounds were evaluated in the

pain models in rats for the treatment of neuropathic pain.

. Novel MCH receptor antagonists have been designed and synthesized for the

treatment of obesity and related disorders.

. The conformation restriction approach generated structurally and

patentably novel drug candidates with excellent biological properties.

. Worked closely with external collaborators to generate compound

libraries.

. An invited review on the status of the MCH program was published in

BioDrugs. Article was cited several times by other research groups.

. Designed the original small molecule compound library at Schering-Plough

and produced around 1000 compounds in collaboration with a CRO for broad

biological screening. Received recognition award for this contribution.

This library proposal was used as a template for the future submission of

compound libraries.

. A large number of new library proposals have been completed in

collaboration with WuXi AppTec, China.

Senior Scientist

May 1999-April 2002

. Identified a series of highly potent analogs of the clinical candidate

Ecopipam (SCH 39166) for the treatment of obesity and related disorders

(Dopamine D1 back-up program).

. An aggressive parallel synthesis approach to SAR showed that amides,

sulfonamides, ureas, carbamates and biaryls are very well tolerated. Also

incorporated the catechol isosteres to ecopipam to generate high affinity

analogs with suitable PK. This work was awarded with Excellence in

Chemistry.

. High affinity and highly selective Dopamine D1/D5 analogs of clozapine

were discovered in the dopamine receptor antagonist program for treating

obesity.

. Briefly worked on the MC4 antagonist program for the treatment of

obesity. Established the need for conformational restriction at the

bridging site for MC4 affinity.

EDUCATION

Regulatory Affairs Certificate (2013)

Columbia University, New York, NY

June 1997- May 1999

Post Doctoral Research Scientist:

Studies on Taxol synthesis with Professor Gilbert Stork

CNRS, ICSN, Gif-sur-Yvette, France

June 1997- May 1999

Post Doctoral Research Scientist:

Studies on Esperamicin anticancer agents with Professor David Grierson

Council of Scientific and Industrial Research, RRL, NIIST (Kerala

University), India Sept 1991 - May 1996

Ph. D in Synthetic Organic Chemistry:

Novel [4?+2?] Cycloaddition Reactions of o-Quinones with Dr. Vijay Nair

PFOFESSIONAL DEVELOPMENT & TRAINING

. Successfully completed a number of online courses as a part of the job

requirement at Merck

. Attended several management training programs and work shops

SKILLS

Very strong background in total synthesis of complex natural products and

heterocyclic chemistry

Solution phase combinatorial, parallel chemistry and microwave assisted

reactions

Excellent knowledge in SAR analysis and selection of compounds for follow

up

Experienced in mentoring and coaching associate scientists for over ten

years

Expertise in writing patents and publications. Excellent team player.

Excellent presentation skills and cross-functional team work with program

chemists and biologists

Actively involved in chemistry discussions with chemists working on

different programs

Strong hands on experience with NMR techniques. Routinely use NMR for

structure elucidation.

Served as a local administrator for the LC-MS equipment (maintenance and

troubleshooting)

Use SciFinder, Beilstein, ISIS database, Chemdraw, Excel etc. on a daily

basis

LEADERSHIP ACTIVITIES / PROFESSIONAL AFFILIATIONS

. Received several shining performance awards at Merck primarily

highlighting cross-functional team work and collaboration skills

. Served as chemistry contact for DGAT FLASH and pre "hit-to-lead"

activities

. Excellence in Chemistry award

. Actively involved in Ph.D/Associate candidate selection

. CNRS France Fellowship

. Council of Scientific and Industrial research Fellowship and University

Grants Commission Fellowship

. Member of American Chemical Society

. Reviewer for Elsevier Journals: Tetrahedron Letters, Bioorganic Medicinal

Chemistry Letters and Bioorganic Medicinal Chemistry, European Journal of

Medicinal Chemistry

. First rank in MS Chemistry from Calicut University, India

LinkedIn Profile Web Link: http://www.linkedin.com/in/tksasikumar

PUBLICATIONS, PATENTS AND PRESENTATIONS

. 28 Publications, 18 Patents, 9 Presentations (A full list will be

available upon request)

Selected list of most recent publications

. Several manuscripts for publication is under preparation

1. J. Lee. L. Song, G. Terracina, T. Bara, H. Josien, T. Asberom, T. K.

Sasikumar, D. A. Burnett, J. Clader, E. M. Parker, L. Zhang,

Identification of Presenillin 1 Selective ?-Secretase Inhibitors with

Reconstituted ?-Secretase Complexes, Biochemistry, 2011, 50, 4973.

2. R. Xu, D. Cole, T. Asberom, T. Bara, C. Bennett, D. A. Burnett, J.

Clader, M. Domalski, W. J. Greenlee, L. Hyde, H. Josien, H. Li, M.

McBriar, B. McKittrick, D. Pissarnitski, L. Qiang, M. Rajagopalan, T.

K. Sasikumar, J. Su, H. Tang, W-L. Wu, L. Zhang, Z. Zhao. SAR of

tricyclic sulfones as ?-secretase inhibitors, Science China: Chemistry,

2011, 54, 1688-1701 (DOI: 10.1007/s11426-011-4388-6, November 2011)

3. T. K. Sasikumar, L. Qiang, D. A. Burnett, D. Cole, R. Xu, H. Li, W.

J. Greenlee, J. Clader, L. Zhang, L. Hyde. Tricyclic sulfones as orally

active ?-secretase inhibitors: Synthesis and structure activity

relationship studies, Bioorg. Med. Chem. Lett., 2010, 20, 3632.

4. T. K. Sasikumar, D. A. Burnett, T. Asberom, W-L. Wu, C. Bennett, D.

Cole, R. Xu, W. J. Greenlee, J. Clader, L. Zhang, L. Hyde. Tetracyclic

sulfones as potent and selective ?-secretase inhibitors. Synthesis and

structure activity relationship studies, Bioorg. Med. Chem. Lett.,

2010, 20, 3645.

5. T. K. Sasikumar, L. Qiang, D. A. Burnett, W. J. Greenlee, C. Li, M.

Grilli, R. Bertorelli, G. Lozza, A. Reggiani A-Ring modifications

on the triazafluorenone core structure and their mGluR1 antagonist

properties, Bioorg. Med. Chem. Lett., 2010, 20, 2474.

6. L. Qiang, T. K. Sasikumar, D. A. Burnett, J. Su, H. Tang, Y. Ye, R.

D. Mazzola Jr., Z. Zhu, B. A. McKittrick, W. J. Greenlee, A. Fawzi, M.

Smith, H. Zhang, J. E. Lachowicz. Discovery of new SCH 39166 analogs as

potent and selective dopamine D1 receptor antagonists, Bioorg. Med.

Chem. Lett., 2010, 20, 836.

7. T. K. Sasikumar, D. A. Burnett, W. J. Greenlee, M. Smith, A. Fawzi,

H. Zhang and J. E. Lachowicz Remote functionalization of SCH 39166:

Discovery of potent and selective benzazepine dopamine D1 receptor

antagonists, Bioorg. Med. Chem. Lett., 2010, 20, 832.

8. R. Xu, D. Cole, T. Asberom, T. Bara, C. Bennett, D. A. Burnett, J.

Clader, M. Domalski, W. Greenlee, L. Hyde, H. Josien, H. Li, M.

McBriar, B. McKittrick, A. T. McPhail, D. Pissarnitski, L. Qiang, M.

Rajagopalan, T. K. Sasikumar, J. Su, H. Tang, W-L Wu, L. Zhang and Z.

Zhao, Design and synthesis of tricyclic sulfones as ?-secretase

inhibitors with greatly reduced Notch toxicity, Bioorg. Med. Chem.

Lett., 2010, 20, 2591.

9. T. K. Sasikumar, L. Qiang, D. A. Burnett, W. J. Greenlee, C. Li, L.

Heimark, B. Pramanik, M. Grilli, R. Bertorelli, G. Lozza, A. Reggiani

Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as

orally efficacious mGluR1 antagonists for neuropathic pain, Bioorg.

Med. Chem. Lett., 2009, 19, 3199.

10. T. J. Kowalski and T. K. Sasikumar, MCH1-Receptor Antagonists as

Antiobesity Therapeutics: Current Status, BioDrugs, 2007, 21, 311.

11. T. K. Sasikumar, L. Qiang, D. A. Burnett, W. J. Greenlee, B. E.

Hawes, T. J. Kowalski, K. O'Neill, B. D. Spar and B. Weig, Bioorg.

Med. Chem. Lett., 2006, 16, 5427.

12. T. K. Sasikumar, L. Qiang, W.-L. Wu, D. A. Burnett, W. J. Greenlee,

K. O'Neill, B. E. Hawes, M. van Heek and M. Graziano, Bioorg. Med.

Chem. Lett., 2006, 16, 4917.

13. T. K. Sasikumar, D. A. Burnett, H. Zhang, A. Smith-Torhan, A. Fawzi

and J. E. Lachowicz, Bioorg. Med. Chem. Lett., 2006, 16, 4543.

14. W-L. Wu, D. A. Burnett, R. Spring, L Qiang, T. K. Sasikumar, M. S.

Domalski, W. J. Greenlee, K. O'Neill and B. E. Hawes, Bioorg. Med Chem

Lett., 2006, 16, 3668.

References:

1. Dr. Duane Burnett, ************@***.***

Director of Medicinal Chemistry, EnVivo Pharmaceuticals, Watertown, MA

2. Dr. Brian McKittrick, *****.**********@*****.***

Director of Chemical Research, Merck research Laboratories, 2015

Galloping Hill Road, Kenilworth, NJ

3. Dr. William Greenlee, (Former Chemistry Site Head, Merck),

*******@*******-********.***

Principal at MedChem Discovery Consulting, LLC

**Official name change documents available

upon request

Contact this candidate