** ******* ******, *** ** *******.*********@*****.***
Nutley NJ, 07110 (Cell) 314-***-****
SUMMARY
Innovative research scientist with strong problem solving skills. Demonstrated skills in designing and synthesizing pharmaceutically acceptable organic molecule. Proficient with modern analytical tools and techniques - method development, trouble shooting and routine maintenance, structure determination and characterization of complex organic molecules. Proven ability to utilize SAR interpretations for designing novel molecules (2 Patents, 15 publications). Well versed with literature searching tools such as “Sci-finder” and “Beilstein”, Molecular modeling programs, Library design.
DEMONSTRATED SKILLS
• Devised and performed multi-step organic synthesis of biologically active molecules using known and novel procedures.
• Designed structural templates utilizing SAR data to obtain pharmaceutically acceptable molecules. Applied SAR strategies to improve PK attributes, physical properties and safety profile.
• Sound knowledge of analytical tools ( HPLC, LC-MS, MPLC, ISCO, UPLC, NMR, TFIR, GC, GC-MS, Mass-link HPLC) for structure determination.
• Strong problem solving skills, excellent written and oral communication skills.
• Proficient with PMC (parallel medicinal chemistry) tools and techniques (library designing programs- PGVL) along with traditional medicinal chemistry approach.
• Well-versed with literature searching tools (e.g., Sci-Finder, Beilstein).
• Proficient with in-house SAR data storage/archival and analysis tools; Utilized structure based in silico drug design molecular modeling program for target selection and focused library design.
• Computer skills include E-note book (ELN) commercial programs such as Spotfire, PowerPoint, ISIS, Chem-Draw, MS-Excel, MS-Word.
• Experienced with “Statistical Design of Experiments”; useful for optimization of processes and/or reactions in laboratory or pilot plant setting.
• Prepared ( written and oral) power point status reports, presentations for scientific community.
RESEARCH EXPERIENCE
MERCK & COPANY, Rahway NJ. 2009- Dec 2011
Scientist: Discovery Medicinal Chemistry
• Efforts focused on developing a small molecule therapy for diabetes / obesity. Designed, synthesized and studied SAR data of two different pharmacophore. Efforts focused on – 1) optimizing PK attributes, 2) improving safety profile ( PXR activity) of a “Benzimidzole” pharmacophore. WO 201-***-****
• For a cardiovascular therapeutic area generated SAR targeting improvements in optimizing the PK profile and mitigating TDR ( time dependant syp inhibition) activity of a bicyclic chiral core.
PFIZER / PHARMACIA St. Louis, MO 2001-2009
Scientist: Discovery Medicinal Chemistry
GPCR regulated autoimmune inflammation target.
• Developed SAR around two structurally different series; modified scaffolds to optimize potency and selectivity.
• Designed novel analogs using in silico molecular modeling information. Devised a synthetic route to the scaffolds and synthesized in multi gram quantity for final analogs preparation.
Inhaled Glucocorticoid Receptor modulator for respiratory diseases therapy.
• Developed promising SAR for both partial and full agonist projects. Efforts focused on moving the project from conception to lead development status.
• Synthesized analogs that show sub-nanomolar potency in key functional assay. Reduced to practice a general synthesis of a novel scaffold (tricyclic / 4 chiral centers / 10 step synthesis). Synthesized benchmark analogs in multi-gram quantities for early proof of concept. The synthetic route was utilized by prep lab for scale up.
• Designed analogs suitable for inhaled therapy (low solubility, systemic exposure and stability).
• Efforts were made to design in phase-II metabolism handles (i.e. glucoronidation) while maintaining potency.
Phosphodiesterase 5 (PDE 5) inhibitor for hypertension therapy
• Designed and synthesized potent PDE 5 inhibitors suitable for QD dosing. Focused specifically on preparing compounds aimed at optimizing for half life clearance and solubility.
• Additional efforts on improving absorption (cell permeability), distribution (studying correlation between volume of Distribution and log D). Project team successfully delivered multiple clinical candidates. Project team delivered multiple drug candidates.
p38 MAP Kinase Inhibitors for Rheumatoid Arthritis therapy.
• Designed and synthesized potent molecules for p38 Map Kinase Inhibitors for Rheumatoid Arthritis therapy culminating in tow two clinical candidates. WO 200-***-**** and WO-200-***-****
ABBOTT LABORATORIES, Abbott Park IL 1993-2001
Research Chemist: Drug Discovery Medicinal chemistry
HIV-Protease inhibitor
• Focused on optimizing synthetic process. Project resulted in a commercial product “NORVIR / Ritonavir”
Endothelin receptor antagonist
• Synthesized analogs in two unique series with different pharmacophores. Project team delivered a drug candidate for treatment of prostate cancer.
LFA-1 ( Leukocyte Function associated Antigen-1) antagonist
• Primary focus was optimizing SAR in the lead series. Team efforts resulted in an active compound which was licensed to another company.
PTP-1B (Protein Tyrosine Phosphates –1B) Inhibitor for Diabetes therapy
• Generated valuable SAR focused on improving cell permeability and selectivity without negatively affecting potency.
PHILIPS PETROLEUM CO., Bartlesville OK 1990-1992
Research Chemist: R&D
• Synthesized organic intermediates of commercial value from petroleum byproducts. Scaled up processes for pilot plant experiments.
• Conducted experiments to develop a procedure for desulfurization of diesel fuel. Screened different catalyst systems, procedures, and routes.
• Developed a process for recovery of ethylene. This process was tested in pilot plant. Developed an "on line GC” method for pilot plant operation. Supervised a technician.
• Used “Statistical Design of Experiments” technique to study chemical processes in laboratory and pilot plant setting.
UNIVERSITY OF CHICAGO, Dept. of Chemistry, Chicago IL
Research assistant, Prof. Gerhard Closs,
• Conducted multi-step organic synthesis (7 -11 steps) of novel steroid molecules.
• The molecules were used to study the rate of electron transfer processes using EPR method at Univ. of Chicago and Argonne National Lab. Provided synthetic assistance to Prof. Closs’s research work in proving Nobel laureate Dr. Marcus’s theory (CIDNIP-theory).
Research assistant, Prof. L.M.Stock,
Performed organic reactions to introduce hydrophilic functional groups in order to solubilize natural coal. Developed synthetic methods useful for modifying physical properties of coal.
• The synthetically altered coal samples were studied at Institute of Gas technology
MAX-PLANCK INSTITUTE FUR KOHLENFORSCHUNG, Mulheim Germany. (1985-1986)
Research assistant Prof M.W. Haenel
• Synthesized organosulfur compounds. Extensively used methods involving organometallic reagents under inert atmosphere.
EDUCATION
M.Sc. (Analytical/Medicinal chemistry) University of Bombay / S.N.D.T. Univ
B.Sc. (Chemistry) University of Bombay
Patents
Devadas, Balekudru; Walker, John; Selness, Shaun R.; Boehm, Terri L.; Durley, Richard C.; Devraj, Rajesh; Hickory, Brian S.; Rucker, Paul V.; Jerome, Kevin D.; Madsen, Heather M.; Alvira, Edgardo; Promo, Michele A.; Blevis-Bal, Radhika M.; Marrufo, Laura D.; Hitchcock, Jeff; Owen, Thomas; Naing, Win; Xing, Li; Shieh, Huey S.; Sambandam, Aruna; Liu, Shuang; Scott, Ian L.; Mcgee, Kevin F. Preparation of substituted pyridinones as modulators of p38 MAP kinase. PCT Int. Appl. (2005), 968 pp. CODEN: PIXXD2 WO 200-***-****
Devadas, Balekudru; Walker, John; Selness, Shaun R.; Boehm, Terri L.; Durley, Richard C.; Devraj, Rajesh; Hickory, Brian S.; Rucker, Paul V.; Jerome, Kevin D.; Madsen, Heather M.; Alvira, Edgardo; Promo, Michele A.; Blevis-Bal, Radhika M.; Marrufo, Laura D.; Hitchcock, Jeff; Owen, Thomas; Naing, Win; Xing, Li; Shieh, Huey S.; Sambandam, Aruna; Liu, Shuang; Scott, Ian L.; McGee, Kevin F. Preparation of substituted pyridinones as modulators of p38 MAP kinase. PCT Int. Appl. (2003), 1052 pp. CODEN: PIXXD2 WO 200-***-****
PUBLICATIONS
Szczepankiewicz, Bruce G.; Bal, Radhika B.; Von Geldern, Thomas W.; Wu-Wong, Jinshyun R.; Chiou, William J.; Dixon, Douglas B.; Opgenorth, Terry J.; Hoffman, Daniel J.; Borre, Anthony J.; Marsh, Kennan C.; Nguyen, Bach N. The effects of diminishing albumin binding to some endothelin receptor antagonists. Life Sciences (1998), 63(21), 1905-1912.
Winn, Martin; von Geldern, Thomas W.; Opgenorth, Terry J.; Jae, Hwan-Soo; Tasker, Andrew S.; Boyd, Steven A.; Kester, Jeffrey A.; Mantei, Robert A.; Bal, Radhika; et al. 2,4-Diarylpyrrolidine-3-carboxylic Acids-Potent ETA Selective Endothelin Receptor Antagonists. 1. Discovery of A-127722. Journal of Medicinal Chemistry (1996), 39(5), 1039-48.
von Geldern, Thomas W.; Kester, Jeffrey A.; Bal, Radhika; Wu-Wong, Jinshyun R.; Chiou, William; Dixon, Douglas B.; Opgenorth, Terry J. Azole Endothelin Antagonists. 2. Structure-Activity Studies. Journal of Medicinal Chemistry (1996), 39(4), 968-81.
Szczepankiewicz B G; Bal R B; von Geldern T W; Wu-Wong J R; Chiou W J; Dixon D B; Opgenorth T J; Hoffman D J; Borre A J; Marsh K C; Nguyen B N The effects of diminishing albumin binding to some Endothelin receptor antagonists. Life sciences (1998), 63(21), 1905-12.
Winn M; von Geldern T W; Opgenorth T J; Jae H S; Tasker A S; Boyd S A; Kester J A; Mantei R A; Bal R; Sorensen B K; Wu-Wong J R; Chiou W J; Dixon D B; Novosad E I; Hernandez L; Marsh K C 2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722. Journal of Medicinal Chemistry (1996), 39(5), 1039-48.
von Geldern T W; Kester J A; Bal R; Wu-Wong J R; Chiou W; Dixon D B; Opgenorth T J Azole endothelin antagonists. 2. Structure-activity studies. Journal of Medicinal Chemistry (1996), 39(4), 968-81.
Miller, John R.; Paulson, Basil Pavlatos; Bal, Radhika; Closs, Gerhard L. Torsional Low-Frequency Reorganization Energy of Biphenyl Anion in Electron Transfer Reactions. Journal of Physical Chemistry (1995), 99(18), 6923-5.
Presentations (As Co-Author)
Heasley, Steven E.; Jacobsen, E. J.; Walker, John K.; Hughes, Robert O.; Freskos, John; Brown, David L.; Fobian, Yvette M.; Owen, Dafydd; Mischke, Brent V.; Tollefson, Michael B.; Molyneaux, John; Blevis-Bal, Radhika; Maddux, Todd; Brown, David G.; Moon, Joseph B.; Phillips, Christopher; Rogier, Joseph D.; Benson, Alan. Synthesis and optimization of pyridopyrazinones as PDE5 inhibitors. Abstracts of Papers, 236th ACS National Meeting, Philadelphia, PA, United States, August 17-21, 2008 (2008)
Walker, John K.; Jacobsen, E. J.; Hughes, Robert O.; Fobian, Yvette M.; Brown, David L.; Heasley, Steven E.; Owen, Dafydd; Freskos, John; Mischke, Brent V.; Molyneaux, John; Tollefson, Michael B.; Blevis-Bal, Radhika; Brown, David G.; Moon, Joseph B.; Phillips, Christopher; Rogier, Joseph D.; Maddux, Todd; Benson, Alan. Optimization of the pyridopyrazinone scaffold as novel inhibitors of PDE5. Abstracts of Papers, 236th ACS National Meeting, Philadelphia, PA, United States, August 17-21, 2008 (2008)
Szczepankiewicz, B. G.; Bal, R. B.; von Geldern, T. W.; Chiou, W. J.; Dixon, D. B.; Wessale, J. L.; Calzadilla, S. V.; Opgenorth, T. J.; Hoffman, D. J.; Borre, A. J.; Schmitt, E. A.; Marsh, K. C.; Nguyen, B. N. Potent and selective Endothelin-A receptor antagonists displaying reduced affinity for serum albumin. Book of Abstracts, 215th ACS National Meeting, Dallas, March 29-April 2 (1998),
Winn, Martin; Tasker, Andrew S.; Boyd, Steven A.; Jae, Hwan-Soo; von Geldern, Thomas W.; Bal, Radhika; Mantei, Robert A.; Wu-Wong, Ruth; Chiou, William; et al. Endothelin antagonists (I) - S.A.R. of 2,4 -diaryl -3- carboxy-pyrrolidine-1-acetamides. Book of Abstracts, 210th ACS National Meeting, Chicago, IL, August 20-24 (1995)
Sorensen, Bryan K.; Tasker, Andrew S.; Bal, Radhika B.; von Geldern, Thomas W.; Dixon, Doug; Calzadilla, Samuel; Dayton, Brian B.; Wu-Wong, J. Ruth; Opgenorth, Terry J. Potent and selective endothelin-A receptor antagonists based on phenylacetate-terminated oxazole-4-carboxylic acids. Book of Abstracts, 210th ACS National Meeting, Chicago, IL, August 20-24 (1995),
Mantei, R.; Boyd, S.; Tasker, A.; Bal, R.; Winn, M.; von Geldern, T.; Rickert, R.; Rasmussen, M. Large scale synthesis and resolution of A-127722, an endothelin receptor antagonist. Book of Abstracts, 210th ACS National Meeting, Chicago, IL, August 20-24 (1995).
Professional Affiliation -- American Chemical Society