YUN OLIVER LONG

***** *** ***** ***** 858-***-****

San Diego, CA 92126 abm6be@r.postjobfree.com

SUMMARY

A senior organic and medicinal chemist with extensive experience in

different areas:

. Synthesis of biologically active compounds in various stages of drug

discovery research from hit identification and expansion, hit to lead

& lead optimization, till supporting IND enabling studies.

. Synthesis of compounds for drug discovery research with break through

in compound in vivo activity, selectivity, pharmacokinetics, and

toxicity profiles.

. Comparative patent analysis, circumventing IP coverage, and

establishing patentable chemistry areas.

. Structure-based and computation-aided drug design.

. Combinatorial synthesis of compound libraries for biologically active

"hit compound" identification.

. Compounds scale-up (grams, hundreds of grams) for advanced animal

efficacy and toxicity study.

. Synthesis and scale-up of photo sensors as initiators for photo-

induced polymerization (kilograms).

. Total synthesis of natural products.

. Novel synthesis of unnatural amino acids and peptides.

. Developing synthetic methodology for the preparation of heterocycles.

. Authoring and co-authoring scientific publications.

. Supervising research associates & working as lead chemist/project

coordinator.

KEY ACHIEVEMENTS

. Contributed to the discovery of clinical candidates for the treatment of

osteoporosis and frailty through conceptualizing and synthesizing novel

compounds for first generation non-steroidal tissue selective androgen

receptor modulators (SARMs) program.

. Independently developed a series of second-generation SARM compounds,

four of which have passed advanced animal studies, demonstrating greatly

improved tissue selectivity over clinical candidate LGD2941. Two were

selected by collaborator TAP and were ready to be developed into IND

track.

. Invented new SARM scaffold which demonstrated ideal 3rd generation

profile in primary assays, indicating the possibility of reaching potent

therapeutic compounds free of major side effects that challenge all SARM

researchers.

. Designed and synthesized novel series of small molecules that mimic the

activity of thrombopoietin (TPO), a protein factor that promotes growth

and production of blood platelets. These compounds defined new patent

areas in TPO research field, improved potency and efficacy over clinical

candidate LGD4665, and were considered as backup compounds for LGD4665 at

that stage of research.

. Discovered novel lead compounds for two kinase projects for the treatment

of osteoarthritis (targets confidential) through extensive patent study

and new core structure development aided by a rich source of structural

biology information, CADD evaluation, and compounds library synthesis.

. Discovered a novel structure series, which improved compounds potency and

metabolic stability for clinical candidate development in a new class

antibiotics discovery project for the broad-spectrum treatment of gram-

positive bacteria infection, including infections caused by clinically

relevant resistant strains.

. Achieved world first total synthesis of natural product Jatrophatrione,

teaming with a fellow student.

. Developed synthetic methodology for the preparation of unnatural amino

acids and heterocyclic structures.

PROFESSIONAL EXPERIENCE

Consultant for A Professor at Beckman Research Institute of City of Hope

October 2009

. Modified biologically active compound to improve its physiological and

biochemical profile.

. Scaled up compounds for in vivo animal efficacy study for treatment of

cancer.

. Wrote up business plan for drug discovery medicinal chemistry effort (SAR

strategies for IP establishment and lead optimization, goal, timeline,

cost, business model, etc)

BioFocus DPI, a Galapagos Company San Diego, CA

March 2007 - March 2009

Senior Research Scientist / Lead Scientist

. Led and participate kinase projects for the treatment of osteoarthritis:

lead compounds discovery through screening hits optimization, scaffolds

hopping, and compound library generation. Extensive patent study was

performed. Novel patent space was established.

. Significantly contributed to the development of DNA polymerase inhibitors

as new class antibiotics.

LIGAND PHARMACEUTICALS San Diego, CA

April 2001 - February 2007

Senior Research Scientist / Research Scientist

. Responsible for one of two chemistry research directions within the late-

stage SARM program; Engaged in communication across the researchers in

molecular biology, pharmacology, pharmacokinetics, new leads

department, and my supervisors in medicinal chemistry for compound

profile improvements. Strategized and implemented prioritization of

research activities, redirection of research, and selection of compounds

for advanced profiling.

. Designed novel SAR targets and optimized lead compounds using the

knowledge obtained from ligand-protein co-crystal structures in

collaboration with a computational chemist (structural-based design).

. Supported compound animal efficacy and toxicity study, IND enabling

studies by exploring new synthetic routes and optimizing reactions for

scale-up synthesis (up to 100+ grams).

. Discovered patentable small molecules with improved

potency and efficacy to mimic thrombopoietin activity

for increasing blood platelets count (TPO program).

. Supervised research associates.

. Authored and co-authored multiple publications and

patents based on SARM and TPO projects.

EDUCATION AND TRAINING

. Yale University

New Haven, CT 2000 - 2001

Postdoctoral Research Associate

Advisor: Professor Harry H. Wasserman

. Explored the synthetic values of vicinal tricarbonyl

compounds.

. Synthesized unnatural amino acids and novel

heterocyclic structures.

. Studied the total synthesis of cyclotheonamides, the

strong protease inhibitors with cyclic pentapeptide and

distinctive alpha-keto amide structures.

. The Ohio State University Columbus, OH

1994 - 2000

Ph.D., Synthetic Organic Chemistry

Advisor: Professor Leo A. Paquette

Dissertation Title: "Synthetic Studies Towards the Total Synthesis of

Zexbrevin and Jatrophatrione"

. Completed world first total synthesis of Jatrophatrione in

collaboration with a fellow student.

. Studied the generic synthesis of furanoheliangolide family of natural

products; achieved the final framework of Zexbrevin.

. Bowling Green State University Bowling Green, OH 1992 - 1994

M.S., Physical Organic Chemistry, Research Advisor: Professor George B.

Clemans

Thesis Title: "Gamma and Delta Substituent Effects in the 13C Spectra of

Some Norbornanes and Trimethylenenorbornanes"

. Synthesized new derivatives of norbornane and

trimethylenenorbornane.

. Observed and theorized the influences on 13C NMR

chemical shifts from various substituents at gamma and

delta positions.

M.S. Level Graduate Assistant, Photochemistry

Advisor: Professor Douglas Neckers

Collaborated project with Spectra Group Limited

. Synthesized sensitizer DIBF, a co-initiator in photo-

induced polymerization, from gram to kilo scale.

. Studied the application of DIBF and its derivatives as

co-initiators in polymerization.

YUN OLIVER LONG 858-***-**** Page Three

. Tsinghua University Beijing, China

1985 - 1990

B.S., Chemistry

Research Advisor: Professors Hongchang Shi and Banghe Chen

Thesis Title: "Extraction of Hyaluronic Acid from Chicken Crests and

Bovine Eyes"

HONORS

. Androgen Receptor Team Gold Star, Ligand

Pharmaceuticals. 2005 & 2006

. "Med Chem Big Award", Dept. of Medicinal Chemistry,

Ligand Pharmaceuticals, 2005

. Evans Fellowship, Department of Chemistry, The Ohio

State University.

. Industrial Fellowship, Merck Pharmaceuticals and

Department of Chemistry, The Ohio State University.

. William L. Evans Memorial Lecture Poster Presentation,

Department of Chemistry, The Ohio State University,

1998 First Prize

. Graduation With Honors, Tsinghua University, Beijing,

China.

WORK STATUS

US Permanent Resident

PRESENTATIONS

1. "Study Toward the Total Synthesis of Jatrophatrione"

Long, Y. O. Oral Presentation at The 221st ACS National

Meeting, San Diego, April 2001.

2. "Synthetic Studies Directed Toward the Synthesis of

Zexbrevin" Paquette, L. A.; Long, Y. O. Poster

Presentation at ACS 31st Central Regional Meeting,

Columbus, OH, June 1999.

3. "Development of a Generic Route Toward the

Furanoheliangolides" Paquette, L. A.; Long, Y. O.

Poster Presentation at The 1998 William Lloyd Evans

Memorial Lecture, The Ohio State University, Columbus,

OH, October 1998.

PUBLICATIONS AND PATENTS

1. "Novel Series of Potent, Nonsteroidal, Selective Androgen Receptor

Modulators Based on 7H-[1,4]Oxazino[3,2-g]quinolin-7-ones" Robert I.

Higuchi,* Kristen L. Arienti, Francisco J. Lopez, Neelakhanda S. Mani,

Dale E. Mais, Thomas R. Caferro, Yun Oliver Long, Todd K. Jones, James

P. Edwards, Lin Zhi, William T. Schrader, Andres Nero-Vilar, Keith B.

Marschke. Journal of Medicinal Chemistry 2007, 50(10), 2486-2496.

2. "Substituted 6-(1-Pyrrolidine)quinolin-2(1H)-ones as Novel Selective

Androgen Receptor Modulators" Esther Martinborough, Yixing Shen, Arjan

van Oeveren, Yun Oliver Long, Tom Lau, Keith B. Marschke, William Y.

Chang, Francisco Lopez, Eric Vajda, Andres Nero-Vilar, Lin Zhi. Journal

of Medicinal Chemistry 2007, 50(21), 5049-5052

3. "Selective Androgen Receptor Modulators Based on a Series of 7H-

[1,4]Oxazino[3,2-g]quinolin-7-ones with Improved in vivo Activity" Yun

Oliver Long*, Robert Higuchi, Thomas R. Caferro, Thomas L.S. Lau, Min

Wu, Marquis L. Cummings Esther Martinborough, Keith B. Marschke, William

Y. Chang, Francisco J. L pez., Donald S. Karanewsky, Zhi Lin.

Bioorganic & Medicinal Chemistry Letters 2008, 18, 2967-2971.

4. "Thrombopoietin Activity Modulating Compounds and Methods" Zhi, Lin;

Phillips, Dean P.; Dalgard, Jackline E.; Penulair, Richard J.; Mcneill,

Matthew H.; Chen, Jyun-Hung; Cuervo, Catalina; Higuchi, Robert; Li,

Yongkai; Nguyen, Bao N.; Long, Oliver; Van Oeveren, Corneilis Arjan.

Priority Date 20 November 2005; 14 August 2006. International Filling

Date 21 November, 2006. International Application Number

PCT/US2006/045129. International Publication Number WO 2007/062078.

YUN OLIVER LONG 858-***-**** Page Four

5. "6-Cycloamino-2-quinolinone Derivatives as Androgen Receptor Modulator

Compounds." Zhi, Lin; Martinborough, Esther; Shen, Yixing; Stevens Lau,

Thomas Lot; Wu, Min; Long, Yun Oliver International Publication Number

WO 200-***-****. Priority Date 22.08.2003 US. International Filling Date

23.08.2004. International Application Number PCT/US2004/027483.

6. Diketo nitriles as dielectrophiles. Formation of heterocyclic

derivatives of amino acids" Wasserman, Harry H.; Long, Y. O.; Parr,

J. Tetrahedron Letters (2002), Volume Date 2003, 44(2), 361-363.

7. "Alkenyl tricarbonyl derivatives of ?-amino acids as trielectrophiles.

Formation of heterocyclic-substituted products" Wasserman, Harry H.;

Long, Y. O.; Zhang, R.; Parr, J. Tetrahedron Letters 2002, 43(18), 3351-

3353.

8. "Vinyl vicinal tricarbonyl esters as trielectrophiles. Reactions with

diamines and related trinucleophiles" Wasserman, Harry H.; Long, Y. O.;

Zhang, R; Carr A. J.; Parr, J. Tetrahedron Letters 2002, 43(18), 3347-

3350.

9. "Formation of Heterocyclic Derivatives of ?-Amino Acids Using Vicinal

Tricarbonyl Methodology" Wasserman, Harry H; Long, Y. O.; Zhang, R;

Parr, Jonathan. Heterocycles 2002, 58, 393-403.

10. "Concise Total Syntheses of the Bioactive Mesotricyclic Diterpenoids

Jatrophatrione and Citlalitrione" Yang, J.; Long, Yun O.; Paquette, Leo

A.; J. Am. Chem. Soc. 2003, 125(6), 1567-1574.

11. "Concerning the Antileukemic Agent Jatrophatrione: The First Total

Synthesis of a [5.9.5] Tricyclic Diterpene" Paquette, Leo A.; Yang, J.;

Long, Y. O.; J. Am. Chem. Soc. 2002, 124(23), 6542-6543.

12. Non-enzymatic Kinetic Resolution of Racemic Alcohols with Chiral

Catalysts" Long, Y. O.; Paquette, Leo A. Chemtracts 2000, 13, 1.

13. "New Extensions of the Anionic oxy-Cope/Intramolecular-SN1' Reaction

Cascade" Johnston, J. N.; Long, Y. O.; Paquette, Leo A. Synthetic

Communication 1998, 28, 1509.

14. "Postcure Effects in Photopolymerization" Long, O. Y.; Marino, T.;

Neckers, D. C. Industrial and Engineering Chemistry Research 1995,

34(12), 4549-52.

15. "Postcure effects on photopolymerization using visible light

initiators." Marino, T.; Long, O. Y.; Neckers, D. C. Cent. Photochem.

Sci., Bowling Green State Univ., OH, USA. Report (1995), (Order No.

AD-A296652), 17 pp. From: Gov. Rep. Announce. Index (U.S.) 1996, 96(1),

Abstr. No. 01-11,764.

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