Management Process

Ankush Argade, Ph.D.

*** ********** *****

Foster City, CA 94404

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

650-***-**** (Mobile); 650-***-**** (Home)

Dynamic and multi-tasking scientific team leader, team player and

experienced chemist offering extensive expertise in driving medicinal

chemistry programs from discovery to early stage development up to IND

filings

AREAS OF EXPERTISE

( Medicinal Chemistry ( Process Chemistry Optimization ( Peptide

Chemistry

( Combinatorial Chemistry ( Structure Based Drug Design (SBDD) ( Hands

on Expertise

( Team-Building, Mentoring & Motivation ( Management of Internal and

External Chemistry Research

( Leadership & Management of RA & PhD -Level Chemists ( Intellectual

Property Analysis, Creation & Protection

( New Program Development, Implementation & Pipeline Growth

PROFESSIONAL EXPERIENCE

COYOTE PHARMACEUTICALS, INC, Sunnyvale, CA 2011-

Present

Research/Scientific Director, Chemistry

. Responsible for directing and handling the drug discovery program which

includes medicinal chemistry, DMPK and formulation efforts while

selecting an ideal drug candidate for IND submission in CNS area

. Contributing towards scientific establishment and structuring of the

Company

RANIE BIOSCIENCES, INC. San Francisco Bay Area, CA

2008-present

. Providing discovery chemistry consultancy services for oncology,

immunology and CNS programs

. Handled scouting of the synthetic routes for the process chemistry

optimization of various API and intermediates

. Advising clients on IP protection, team building and associated

challenges

. Developed plans and research budget for chemistry and biology discovery

research

. Designed a target focused discovery research and early stage

development plans for oncology, immunology and CNS indications

RIGEL PHARMACEUTICALS, INC., South San Francisco, CA 11/99-

4/08

Senior Fellow (Scientific Director)

01/07-4/08

. Designed and directed new chemistry for HIV and SCF ligase research

programs with internal and with out-sourcing efforts

. Created and implemented chemistry approach to strengthen IP for JAK2

kinase program

. Established and managed process R&D for R348 (JAK3 inhibitor) on g

(GLP) to kg (GMP) scale

. Interfaced with senior management and SAB for developing research plans

and performing research reviews

Associate Director

01/05-1/07

. Led chemistry team on JAK3 inhibitors (inflammation, especially RA) to

optimize potency and selectivity, in vivo and in vitro DMPK,

formulation and pharmacology properties, leading to selection of R348

for IND filing

. Established process chemistry for R763 (oncology) and R406 (RA) and

managed process development with CROs

. Designed and synthesized novel linear and cyclic peptides for NS3/NS4

protease inhibitors to treat HepC

. Made presentations on chemistry issues (oncology and immunology) to

potential collaborative partners to attract the out-licensing deals

. Interfaced with senior management and SAB for developing research plans

and performing research reviews

Senior Scientist and Group Leader

11/99-1/05

. Led chemistry team on R112 (AR, reached Phase IIb), R406 (RA, in Phase

III), and R343 (asthma, with Pfizer)

. Instituted oncology program SAR with the aid of SBDD, resulting in R055

(pending) and R763 (licensed to EMD-Serono) identified as IND

candidates

. Established/managed process R&D for R112 (AR) and R343 (asthma)

. Launched mast cell inhibition (kinase targeting) chemistry program with

the selection of a versatile scaffold, which generated numerous leads

for IND filings and subsequent clinical trials

. Designed, synthesized and directed the synthesis of numerous solid and

solution phase libraries for new programs

. Interfaced with senior management and SAB for developing research plans

and performing research

ELI LILLY & COMPANY, Indianapolis, IN

09/97-11/99

Postdoctoral Research Scientist

. Discovered novel macrocyclic and non-macrocyclic Factor Xa inhibitors

based on SBDD and SAR

. Designed and synthesized novel t-BOC-resin for selective protection of

amino function

. Investigated electrophilic aromatic substitution reactions of

azidocarboxylates on resin-bound aminomethylphenols

PURDUE UNIVERSITY, West Lafayette, IN

07/90-09/97

Postdoctoral Research Fellow

. In collaboration with the National Cancer Institute (NCI), developed a

versatile diastereoselective Michael addition of thiols to -

brefeldin A (anti-cancer agent) to produce highly water soluble and

equipotent prodrugs with enhanced formulation properties

. Developed a catalytic method for the asymmetric allylic oxidation of

prochiral olefins to produce chiral allylic alcohols

. Discovered an efficient approach for the synthesis of octalactin

lactone and a key side chain using asymmetric crotylboration and

macrolactonization approaches, for the synthesizing octalactin A and B;

anti-cancer natural products

. Developed a simple and efficient method for the synthesis of chiral

organodichloroboranes in >99% ee

. Investigated a simple method for one carbon homologation of

organodichloroboranes to prepare tert-RBCl2

. Designed and synthesized biodegradable superabsorbent polyacrylates

with different cross-linking ratios and star-shaped polymers for

biomedical applications

NATIONAL CHEMICAL LABORATORY, Pune, India 04/89-

07/90

Research Scientist

. Developed a simple synthesis of ketene acetals using the Pinner

reaction

. Performed process research and process development on chemically

sensitive prostaglandins

EDUCATION

Ph. D. Organic Chemistry

04/1984-04/1989

Thesis: "Synthesis of Biologically Active Anthraquinone Derivatives via the

Marschalk Reaction"

. Performed modifications of the Marschalk reaction to produce key

intermediates and completed the total synthesis of -4-

demethoxydaunomycin, a drug candidate for cancer therapies

PROFESSIONAL DEVELOPMENT

. Short Course in Advanced Medicinal Chemistry (Professor R. B.

Silverman, at Eli Lilly & Company).

. Work-shop on Organometallic Chemistry (Professor B. M. Trost at Eli

Lilly & Company)

. Practical Approaches of Combinatorial Chemistry Applications to Drug

Discovery (at Eli Lilly & Company)

. Short Course on Drug Metabolism and Pharmacokinetics (at Eli Lilly &

Company)

. Research Commercialization Courses by NIH

AWARDS/AFFILIATIONS/ACTIVITIES

. Consulting Member of the TASA (Technical Advisory Service for

Attorneys) group (May 2010-present)

. Consulting Member at the Gerson Lehrman Group (2008- present)

. Membership Chair, Small Chemical Businesses (SCHB), Division of

American Chemical Society (2008-present)

. Research Rewards, Rigel Pharmaceuticals, Inc., South San Francisco, CA

(1999-2008)

. Research Fellowship, Council of Scientific & Industrial Research, New

Delhi, India (1984-1989)

. American Chemical Society (1994-present)

. Participated in the Horizons Program for teaching chemistry at Purdue

University (1995-1997)

ISSUED US PATENTS

1. Argade et al. "2,4-Pyrimidinediamine Compounds and Uses as Anti-

Proliferative Agents" US 7,884,111; Feb. 8, 2011

2. Singh et al. "Triazole Derivatives Useful as Axl Inhibitors" US

7,884,119; Feb. 8, 2011

3. Li et al. "Cycloalkyl Substituted Pyrimidinediamine Compounds and

Their Uses" US 7,868,013; Jan. 11, 2011

4. Argade et al. "Stereoisomerically Enriched 3-Aminocarbonyl

Bicycloheptene Pyrimidinediamine Compounds and Their Uses" US

7,863,286; Jan. 4, 2011

5. Li et al. "Cycloalkyl Substituted Pyrimidinediamine Compounds and

Their Uses" US 7,858,633; Dec. 28, 2010

6. Li et al. "Composition and Methods for Inhibition for JAK Pathways" US

7, 834,024; Nov. 16, 2010

7. Singh et al. " N2,N4-Bis-aryl-5-fluoro-2,4-pyrimidinediamines" US

7,825,116; Nov.2, 2010

8. Singh et al. "2,4-Pyrimidinediamine Compounds and Their Uses" US

7,820,819; Oct. 26, 2010

9. Singh et al. "Methods of Treating or Preventing Autoimmune Diseases

with 2,4-Pyrimidinediamine Compounds" US 7,812,029; Oct. 12, 2010

10. Singh et al. " 2,4-Pyrimidinediamine Compounds and Their Uses" US

7,803,939; Sept. 28, 2010

11. Li et al. "Cycloalkyl Substituted Pyrimidinediamine Compounds and

Their Uses" 7,754,714; July 13, 2010

12. Argade et al. "Aromatic Ether Derivatives Useful as Thrombin

Inhibitors" US7700628; April 20, 2010

13. Singh et al. "Intermediates for Making 2,4-Pyrimidinediamine

Compounds" US 7,655,797; Feb. 2, 2010

14. Singh et al. "2,4-Pyrimidinediamine Compounds and Their Uses" US

7,642,351; Jan. 5, 2010

15. Ding et al. "Kinase Inhibitors and Their Uses" US 7,601,713; Oct. 13,

2009

16. Singh et al. "5-Fluoro-4N-phenyl-4-pyrimidineamine Compounds" US

7,589,200; Sept. 15, 2009

17. Argade et al. "Substituted Pyridines and Their Uses" US 7,585,883;

Sept. 8, 2009

18. Singh et al. " Methods of Treating or Preventing Autoimmune Diseases

with 2,4-Pyrimidinediamine Compounds" US 7,582,648; Sept. 1, 2009

19. Singh et al. "Methods of Treating or Preventing Autoimmune Diseases

with 2,4-Pyrimidinediamine Compounds" US 7,560,466; July 14, 2009

20. Singh et al. "2,4-Pyrimidinediamine Compounds and Their Uses" US

7,557,210; July 7, 2009

21. Singh et al. "2,4-Pyrimidinediamine Compounds and Their Uses" US

7,550,460; June 23, 2009

22. Singh et al. "Methods of Treating or Preventing Autoimmune Diseases

with 2,4-Pyrimidinediamine Compounds" US 7,517,886; April 14, 2009

23. Singh et al. "2,4-Pyrimidinediamine Compounds and Their Uses" US

7,498,435; March 3, 2009

24. Li et al. "Compositions and Methods for Inhibition of the JAK Pathway"

US 7,491,732; Feb. 17, 2009

25. Singh et al. "2,4-Pyrimidinediamine Compounds and Their Uses" US

7,485,724; Feb. 3, 2009

26. Singh et al. "4-Pyrimidineamine Compounds and Their Uses as Anti-

Proliferative Agents" US 7,482,351; Jan. 27, 2009

27. Argade "Stereoisomerically Enriched N-Protected beta.-Lactams Using

Candida Antarctica" US 7,459,301; Dec. 2, 2008

28. Singh et al. "Methods of Treating or Preventing Autoimmune Diseases

with 2,4-Pyrimidinediamine Compounds" US 7,452,879; Nov.18, 2008

29. Singh et al. "2,4-Pyrimidinediamine Compounds and Their Uses" US

7,435,814; Oct. 14, 2008

30. Thota et al. "HCV Inhibitors and Methods of Using Them" US 7,358,259;

April 15, 2008

31. Singh et al. "2,4-Pyrimidinediamine Compounds and Their Uses" US

7,332,484; Feb. 19, 2008

32. Singh et al. "2,4-Pyrimidinediamine Compounds and Their Uses" US

7,329,672; Feb. 12, 2008

33. Singh et al. "2,4-Pyrimidinediamine Compounds and Their Uses" US

7,329,671; Feb. 12, 2008

34. Singh et al. "Methods of Treating or Preventing Autoimmune Diseases

with 2,4-Pyrimidinediamine Compounds" US 7,122,542; Oct. 17, 2006

35. Singh et al. "Intermediates Useful for Making 2,4-Pyrimidinediamine

Compounds" US 7,060,827; June 13, 2006

36. Cushman et al. "Brefeldin A Derivatives" US 6362218; March 26, 2002

PUBLISHED US PATENT APPLICATIONS: Total 66

PUBLICATIONS

1. McLaughlin et al. "Preclinical Characterization of Aurora Kinase

Inhibitor R763/AS703569 Identified Through an Image-Based Phenotypic

Screen" J Cancer Res Clin Oncol, Published 136(1): 99-113, Feb. 2010

1. Braselmann et al. "R406, An Orally Available Spleen Tyrosine Kinase

Inhibitor Blocks Fc Receptor Signaling and Reduces Immune Complex-

Mediated Inflammation" J. Pharmacology and Experimental Therapeutics,

319(3), 998-1008, 2006

2. Rossi et al. "Identification of the Syk Kinase Inhibitor R112 by a

Human Mast Cell Screen" J. of Allergy and Clinical Immunology, 118(3),

749-755, 2006

3. Peppas et al. "Preparation and Properties of Poly(ethyleneoxide) Star

Polymers" J. of Applied Polymer Science, 87(2), 322-327, 2003

4. Argade et al. "Poly(acrylic acid)-poly(vinylalcohol)copolymers with

Superabsorbent Properties" J. Applied Polymer Science, 70(4), 817-829,

1998

5. Argade et al. "Design and Synthesis of -Brefeldin A Sulfide

Derivatives as Prodrug Candidates with Enhanced Aqueous Solubilities"

J. Medicinal Chemistry, 41(18), 3337-3346, 1998

6. Argade at el "Highly Efficient Diastereoselective Michael Addition of

Various Thiols to -Brefeldin A" J. of Organic Chemistry, 63(2), 273-

278, 1998

7. Andrus et al. "Synthesis of Octalactin Lactone and Side Chains"

Tetrahedron Lett. 37(29), 5049-5052, 1996

8. Andrus et al. "The Asymmetric Kharasch Reaction. Catalytic

Enantioselective Acyloxylation of Olefins with Chiral Copper(I)

Complexes and tert-Butylperbenzoate" Tetrahedron Lett, 36(17), 2945-

2948, 1995

9. Argade et al. "A Short and Simple Synthesis of Ketene Acetals"

Synthetic Commun., 23 (14), 1979-1984, 1993

10. Argade et al. "Preparation and Characterization of Novel Biodegradable

Tri-and Tetraacrylate Intermediates" Polymer Bulletin (Berlin,

Germany), 31(4), 401-407, 1993

11. Brown et al. "Organoboranes. 55. An Improved Procedure for the

Conversion of Representative Achiral and Chiral Monoalkyl-, (E)- and

(Z)-Alkenyl-, and Arylboronates into the Corresponding

Organodichloroboranes" Organometallics, 11(9), 3094-3097, 1992

12. Ayyangar et al. "Marschalk Reaction Approaches for the Synthesis of -4-Demethoxydaunomycinone" Indian J. Chemistry Section B: Organic

Chemistry including Medicinal Chemistry, 31B(1), 3-8, 1992

13. Ayyangar et al. "Total Synthesis of -4-Demethoxydaunomycin" Indian

J. Chemistry Section B: Organic Chemistry Including Medicinal

Chemistry, 30B(4), 377-84, 1991

14. Ayyangar et al. "4-Bromo-2-acetoketal-1-butyraldehyde. An Elegant Key

Intermediate for the Synthesis of 4-demethoxy-7,9-dideoxydaunomycinone

by Marschalk reaction" Synthetic Commun., 17(16), 1959-1964, 1987

15. Argade et al. "Marschalk Reaction Approach for A Simple Synthesis of -4-demethoxydaunomycinone" Tetrahedron Lett. 27(30), 3529-3532,

1986

REFERENCES: Available upon request

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