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16.01.04

JOSEPH F. DELLARIA, JR. 10423 Kilbirnie Rd. ▪ Woodbury, MN 55129 ▪ (651) 436-6494

[email protected]

CAREER PROFILE

Demonstrated ability to successfully navigate complex chemistry and organizational issues. Productive and creative synthetic organic chemist with extensive experience in successfully directing, managing and synthesizing complex organic compounds for drug discovery. Selected competencies fall into five areas:

Proven ability to create and lead teams that influences organizational direction.

Expediting Innovation Discovery: Conceived and created a novel process to qualify and prioritize ideas in early phase discovery efforts. It finds “Better Ideas Faster,” saves time, and resources. The process is proven for science-based projects, identifying new organizational processes, and making personal decisions.

Patent Strategy Development: Worked in conjunction with patent counsels to create and implement patent strategies for novel chemical entities in 9 unique therapeutic areas. This led to 63 patents.

Innovative Synthesis of New Compounds: discovered three new reactions and published 30 papers describing new methods to efficiently prepare potent, biologically active compounds.

Extensive Understanding of Bioavailability Issues: participated and/or lead teams in the identification of potent and bioavailable NCEs.

RESULTS:

Patents 64 issued U.S. patents in 9 unique therapeutic areas

Medicinal Chemistry Responsible for the discovery of the lead compound for an IND in post-surgical scarring (effort was terminated with the sale of the division)

Discovered back-up compounds in four therapeutic areas (Renin, 5-LO and Matrix Metalloproteinase, IRMs for cancer)

Directed the medicinal chemistry efforts of over 40 chemists over the course of my career (bachelors, masters, and Ph.D.s)

Published Papers 30 Publications in major refereed journals

Presentations and Invited Lectures 22 professional presentations 11 invited university and college lectures Books “The IDEA Formula

PROFESSIONAL EXPERIENCE

Perceptive Realities, LLC, Woodbury, MN 2007-present

Founder and Principal Consulting firm dedicated to finding Better Ideas Faster through:

Building and implementing custom tailored processes for qualifying and prioritizing early R&D ideas (Innovation Discovery Process®).

o Saves time and money by learning how to identify and stop ideas that cannot work at the earliest possible time.

o Expedites the rate of discovering innovative ideas for late stage New Product Development.

Training to create and implement internally administered Innovation Discovery Processes®.

mailto:[email protected]

Joseph F. Dellaria, Jr.

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Medicinal/Process Chemistry Consulting October, 2008 – October 2011

3M Pharmaceuticals, St. Paul, MN 2000 – 2007

Lead Research Specialist Led a group of 11-14 chemists—Ph.D., M.S., and B.S.—in the design, synthesis and patenting of new compounds in the Immune Response Modifier class of compounds.

Devised and executed a department wide plan to synthesize compounds and file 26 patents in 6 months.

Co-inventor on 19 granted U.S. patents for new Immune Response Modifying compounds.

Initiated and co-lead a team effort to design and implement the process used to select new projects for the Pharmaceutical Discovery Division. 7 out of 50 ideas were selected for further scientific investigation.

Lead Chemist on the Discovery Opportunities Team which oversaw allocating resources and scientific strategy for potential new research programs.

Designed and played a leading role in implementing the hiring process to hire over thirty new employees over a three year period.

Co-led the exploratory Multi-Drug Resistance Project. Set overall research direction, priorities, and directed medicinal chemistry effort. Lead the team to make a data-driven no-go decision saving $1K/year in research expenses.

Served as the departmental liaison for the design and construction of a new state-of-the-art $2 million medicinal chemistry laboratory. Responsible for working with engineers and contractors to identify and resolve numerous construction issues.

Abbott Labs, Chicago, IL 1984 – 2000

Associate Research Fellow / Sr. Group Leader, 1992 – 2000 Led teams of 6-8 chemists in discovering new compounds for the inhibition of four unique therapeutic targets (5-Lipoxygenase, Cyclooxygenase II, Matrix Metalloproteinase, and Urokinase).

Identified potent (nanomolar to sub-nanomolar) inhibitors in each area.

Set and executed patent strategies for each area.

22 U.S. patents were granted during this time.

Maintained an active lab presence as time permitted.

Promoted to the first step of the Scientific Ladder (Associate Research Fellow, Volwiler Society, Aug. 1992).

Research Investigator, 1989 – 1992 Responsible for overseeing the work of two assistants and three summer students.

3 U.S. patents were granted during this period.

Designed and synthesized new amide-linked compounds for the inhibition of 5-Lipoxygenase.

EDUCATION

N.I.H. Post-doctoral Fellow: California Institute of Technology, Pasadena, CA and Harvard University, Cambridge, MA. Research Advisor: Professor David A. Evans.


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Ph.D., Organic Chemistry, University of Minnesota, Minneapolis, MN. Research Advisor: Professor T.R. Hoye.

Bachelor of Arts, Chemistry, Hope College, Holland, MI. Research Advisor: Michael P. Doyle.

PROFESSIONAL SOCIETY

American Chemical Society

HONORS AND AWARDS

National Institute of Health Postdoctoral Fellow

L.I. Smith Outstanding Graduate Student Award, U. of MN

Graduate School Dissertation Fellowship, U. of MN

E.I. DuPont Research Award, Hope College

Member Phi Beta Kappa, Hope College

PATENTS

64) Stoermer, Doris; Dellaria, Jr.; Joseph F.; Amos, David T.; Zimmermann, Bernhard M;

Dressel, Luke T.; Bonk, Jason D.; “Substituted imidazoquinolines, imidazopyridines, and

imidazonaphthyridines”, U.S. 9,006,264, 04/14/2015.

63) Bonk, Jason D.; Dellaria, Jr.; Joseph F.; “Arylalkenyl and arylalkynyl substituted

imidazoquinolines”, U.S. 8,802,853, 08/12/2014.

62) Krepski, Larry R.; Dellaria, Jr.; Joseph F.; Marszalek, Gregory J.; “Hydroxylamine and

Oxime Substituted Imidazoquinolines, Imidazopyridines, And Imidazonaphthyridines”, U.S.

8,778,963, 7/15/2014.

61) Bonk, Jason D.; Dellaria, Jr.; Joseph F.; “Imidazoquinolinyl sulfonamides”, U.S. 8,735,421,

5/27/2014.

60) Krepski, Larry R.; Dellaria, Jr.; Joseph F.; Duffy, Daniel, E.; Radmer, Matthew R.; Amos,

David T.; Zimmermann, Bernhard M.; Moser, William H.; “Amide substituted

imidazopyridines, imidazoquinolines, and imidazonaphthyridines”, U.S. 8,697,873, 4/15/2014.

59) Krepski, Larry R.; Dellaria, Jr.; Joseph F.; Duffy, Daniel, E.; Radmer, Matthew R.; Amos,

David T.; “Substituted imidazo ring systems and methods”, U.S. 8,691,837, 4/8/2014.

58) Kshirsagar, Tushar A.; Amos, David T.; Dellaria, Jr.; Joseph F.; Heppner, Philip D.; Langer,

Scott E.; Zimmermann, Bernhard M.; “Oxime substituted imidazo-containing compounds”,

U.S. 8,673,932, 3/18/2014.


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57) Kshirsagar, Tushar A.; Lundquist, Jr., Gregory D.; Amos, David T.; Dellaria, Jr., Joseph F.;

Zimmermann, Bernhard M.; Heppner, Philip D.; “Hydroxylamine substituted Imidazo-

quinolines”, U.S. 8,598,192, 12/03/2013.

56) Stoermer, Doris.; Dellaria, J. F.; Amos, David T.; Zimmermann, Bernhard M.; Dressel, Luke

T.; Bonk, Jason, D.; Radmer; Matthew R.; “Substituted imidazoquinolines, imidazopyridines,

and imidazonaphthyridines”, U.S. 8,541,438, 09/24/2013.

55) Kshirsagar, Tushar A.; Lundquist, Gregory D.; Dellaria, J. F.; Radmer; Matthew R.;

Zimmermann, Bernhard M.; “Oxime and hydroxylamine substituted imidazo[4,5-c] ring

compounds and methods”, U.S. 7,968,563, 06/28/2011.

54) Radmer; Matthew R.; Moser, William H.; Moseman, Joan T.; Dellaria, J. F. “Sulfone

Substituted Imidazo Ring Ethers”, U.S. 7,939,526, 05/10/2011.

53) Kshirsagar, Tushar A.; Lundquist, Gregory D.; Amos, David T.; Dellaria, J. F.; Zimmermann,

Bernhard M.; Heppner, Philip D. “Oxime Substituted Imidazoquinolines”, U.S. 7,897,767,

03/01/2011.

52) Stoermer, Doris; Dellaria, J. F.; Amos, David T.; Zimmermann, Bernhard M.; Dressel, Luke

T.; Bonk, Jason D.; Radmer, Matthew R. “Substituted Imidazoquinolines, Imidazopyridines,

and Imidazonaphthyridines” U.S. 7,884,207, 02/08/2011.

51) Kshirsagar, Tushar A.; Amos, David T.; Dellaria, J. F.; Heppner, P. D.; Langer, Scott E.;

Zimmermann, B. M. “Hydroxylamine Substituted Imidazoquinolines”, U.S. 7,648,997,

01/19/2010.

50) Dellaria, J. F.; Radmer, M. R.; Merrill, B. A.; “Thioether Substituted Imidazopyridines”, U.S.

7,288,550, 10/30/2007.

49) Dellaria, J. F.; Radmer, M. R. “Thioether Substituted Imidazopyridines”, U.S. 7,276,515,

10/2/2007.

48) Dellaria, J. F.; Lindstrom, K. J.; Dressel, L. T.; Heppner, P. D.; Jacobsen, J. R.; Moseman, J.

T.; Moser, W. H.; Radmer, M. R.; Stoermer, D. “Ether Substituted Imidazopyridines”, U.S.

7,220,758, 05/22/2007.

47) Dellaria, J. F.; Lindstrom, K. J.; Dressel, L. T.; Duffy, D. E.; Heppner, P. D.; Jacobsen, J. R.;

Moseman, J. T.; Moser, W. H.; Radmer, M. R.; Stoermer, D.; Zimmermann, B. M. “Ether

substituted imidazopyridines”, U.S. 7,125,890, 10/24/2006.

46) Heppner, P. D.; Charles, L. J.; Dellaria, J. F.; Merrill, B. A.; Mickelson, J. W. “Aryl Ether

Substituted Imidazoquinolines", U.S. 6,989,389, 1/24/2006.

45) Dellaria, J. F.; Mickelson, J. W. “Aryl Ether Substituted Imidazoquinolines", U.S. 6,953,804,

10/11/2005.

44) Bonk, J. D.; Dellaria, J. F.; Merrill, B. A.; Radmer, M. R. “Thioether Substituted

Imidazoquinolines", U.S. 6,949,649, 09/27/2005.

43) Dellaria, J. F.; Merrill, B. A.; Radmer, M. R. “Thioether Substituted Imidazoquinolines", U.S.

6,921,826, 07/26/2005.

42) Dellaria, J. F.; Lindstrom, K. J.; Dressel, L. T.; Heppner, P. D.; Jacobsen, J. R.; Radmer, M.

R.; Stoermer, D. “Ether Substituted Imidazopyridines", U.S. 6,797,718, 09/28/2004.


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41) Dellaria, J. F.; Haraldson, C. A.; Lindstrom, K. J.; Merrill, B. A.; “Amide Substituted

Imidazopyridines", U.S. 6,720,422, 04/13/2004.

40) Dellaria, J. F.; Haraldson, C. A., Heppner; P. D.; Lindstrom, K. J.; Merrill, B. A. “Urea

Substituted Imidazopyridines", U.S. 6,720,334, 04/13/2004.

39) Dellaria, J. F.; Haraldson, C. A.; Heppner, P. D.; Lindstrom, K. J.; Merrill, B. A. “Amide


38) Dellaria, J. F.; Haraldson, C. A.; Heppner, P. D.; Lindstrom, K. J.; Merrill, B. A. “Urea

Substituted Imidazopyridines ", U.S. 6,716,988, 04/06/2004.

37) Dellaria, J. F.; Haraldson, C. A.; Heppner, P. D.; Lindstrom, K. J.; Merrill, B. A.

“Sulfonamido Substituted Imiazopyridines", U.S. 6,696,465, 02/24/2004.

36) Heppner, P. D.; Charles, L. J.; Dellaria, J. F.; Merrill, B. A.; Mickelson, J. W. “Aryl Ether


35) Charles, L. J.; Dellaria, J. F.; Heppner, P. D.; Merrill, B. A.; Mickelson, J. W. “Aryl Ether


34) Bonk, J. D.; Dellaria, J. F.; Merrill, B. A.; Radmer, M. R.; “Thioether Substituted

Imidazopyridines", U.S. 6,667,312, 12/16/2003.

33) Dellaria, J. F.; Merrill, B. A.; Radmer, M. R. “Thioether Substituted Imidazopyridines", U.S.

6,664,264, 12/16/2003.

32) Charles, L. J.; Dellaria, J. F.; Griesgraber, G. W.; Heppner, P. D.; Manske, K. J.; Mickelson, J.

W.; Rice, M. J. “Heteroaryl Ether Substituted Imidazoquinolines”, U.S. 6,664,260, 12/16/2003.

31) Dellaria, J. F.; Haraldson, C. A.; Heppner, P. D.; Lindstrom, K. J.; Merrill, B. A. “Urea


30) Dellaria, J. F.; Haraldson, C. A.; Heppner, P. D.; Lindstrom, K. J.; Merrill, B. A. “Amide

Substituted Imidazopyridines", U.S. 6,545,016, 4/8/2003..

29) Dellaria, J. F.; Haraldson, C.A.; Heppner, P. D.; Lindstrom, K. J.; Merrill, B. A. “Sulfonamido


28) Curtin, M. L.; Dai, Y.; Davidsen, S. K.; Dellaria, J. F.; Florjancic, A. S.; Gong, J.; Guo, Y.;

Heyman, H. R.; Howard, R.; Holms, J. H.; Michaelides, M. R.; Stacey, J. R.; Steinman, D. H.;

Wada, C. K.; Xu, L. "Preparation of Hydroxamates as Matrix Metalloproteinase Inhibitors",

U.S. 6,294,573, 2001.

27) Dellaria, J. F. "Benzothiophene-based Urokinase Inhibitors", U.S. 6,207,701, 2001.

26) Dellaria, J. F.; Gane, T. H. "Prostaglandin Synthase-2 Inhibitors", U.S. 5,776,984, 07/07/98.

25) Dellaria, J. F.; Gane, T. H. "Prostaglandin Synthase-2 Inhibitors", U.S. 5,681,842, 1997.

24) Dellaria, J. F.; Chernesky, L. J. "Heteroatom Substituted Propanyl Derivatives Having 5-

Lipoxygenase Inhibitory Activity", U.S. 5,516,795, 1996.

23) Dellaria, J. F.; Brooks, D. W.; Sallin, K. J. ; Moore, J. L. "Arylamidoalkyl-N-hydroxyurea

Compounds Having Lipoxygenase Inhibitory Activity", U.S. 5,514,702, 1996.


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22) Dellaria, J. F.; Basha, A.; Black, L.; Chernesky, L. J.; Lee, W. "Pyran-4-ylmethyl Substituted

Arylalkylaryl-, Arylalkenylaryl-, and Arylalkynylary Urea Inhibitors of 5-Lipoxygenase", U. S.

5,484,786, 1996.

21) Chernesky, L. J.; Dellaria, J. F. "1,2-Dialkoxylethanes as 5-Lipoxygenase Inhibitors", U.S.

5,475,009, 1995.

20) Brooks, D. W.; Carter, G. W.; Dellaria, J. F.; Maki, R. G.; Rodriquez, K. E. "Indole

Derivatives Which Inhibit Leukotriene Biosynthesis", U.S. 5,459,150, 1995.

19) Dellaria, J. F.; Basha, A.; Black, L.; Chernesky, L. J.; Lee, W. "(4-Alkoxypyran-4-yl)

Substituted Ether, Arylalkyl-, Arylalkenyl-, and Arylalkynyl)urea Inhibitors of 5-

Liopxygenase", U. S. 5,446,062, 1995.

18) Dellaria, J. F.; Ratajczyk, J. R.; Brooks, C. D. W.; Basha, A. "Polyether Napthalenic Lignan

Lactones as Inhibitors of 5-Lipoxygenase", U.S. 5,446,055, 1995.


Substituted Arylalkylaryl-, Arylalkenylaryl-, and Alrylalkynylarylurea Inhibitors of 5-

Lipoxygenase", U. S. 5,432,194, 1995.

16) Dellaria, Joseph F.; Ratajczyk, J. D.; Brooks, C. D.W.; Basha, A. “[Alkoxy-, alkenyloxy-,

alkynyloxy-, and phenylmethyloxyalkoxycycloalkyl or alkoxycycloheteroalkyl]naphtho[2,3-c]

furan-1(3H)-one inhibitors of 5-lipoxygenase”, U.S. 5,426,111, 06/20/95.

15) Dellaria, J. F.; Basha, A.; Black, L.; Chernesky, L. J.; Lee, W. "(Trans-1,4-

dialkoxycyclohexyl) Substituted Arylalkylaryl-, Arylalkenylaryl-, and Alrylalkynyl-arylurea

Inhibitors of 5-Liopxygenase", U.S. 5,407,959, 1995.

14) Dellaria, J. F.; Brooks, D. W.; Dorn, L. J. "Phenylmethyl Derivatives Having 5-Lipoxygenase

Inhibitory Activity", U.S. 5,354,865, 1994.

13) Dellaria, J. F.; Brooks, D. W.; Moore, J. L. "Ether Containing Inhibitors of 5-Lipoxygenase",

U.S. 5,350,765, 1994.


Substituted arylalkylaryl-, arylalkenylaryl-, and alrylalkynylarylurea inhibitors of 5-

Lipoxygenase", U.S. 5,346,914, 1994.

11) Dellaria, J. F.; Brooks, D. W.; Moore, J. L. "Ether Containing Inhibitors of 5-Lipoxygenase",

U.S. 5,268,379, 1993.

10) Brooks, D. W.; Dellaria, J. F.; Summers, J. B. "Lipoxygenase Inhibiting Compounds Derived

From Nonsteroidal Antiinflammatory Carboxylic Acids”, U.S. 5,220,059, 1993.

9) Dellaria, J. F.; Brooks, D. W.; Sallin, K. J. ; Moore, J. L. "Arylamidoalkyl-N-hydroxyurea

Compounds Having Lipoxygenase Inhibitory Activity", U.S. 5,214,204, 1993.

8) De, B.; Zydowsky, T. N.; Baker, W. R.; Dellaria, J. F.; Rosenberg, S. H.; Jae, H. S.

“Heterocyclic peptide renin inhibitors”, U.S. 5,164,388, 11/17/92.

7) Brooks, D. W.; Dellaria, J. F.; Maki, R. G.; Rodriquez, K. E.: Carter, G. W. "Indole

Derivatives Which Inhibit Leukotriene Biosynthesis", U.S. 5,095,031, 1992.


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6) Brooks, D. W.; Summers, J. B.; Gunn, B. P.; Dellaria, J. F.; Holms, J. H.; Maki, R. G.;

Martin, J. G.; Moore, J. L.; Rodriques, K. E.; Stewart, A. O. , "Heteroaryl N-Hydroxy Amides

and Ureas With Polar Substituents As 5-Lipoxygenase Inhibitors", U.S. 4,992,464, 1991.

5) Rosenberg, S. H.; Dellaria, J. F.; Fung, A. K. L.; Kempf, D. J.; Luly, J. R.; Plattner, J. J. "Renin

Inhibiting Compounds", U.S. 4,857,507, 1989.

4) Dellaria, J. F.; Fung, A. K. L; Kempf, D. J.; Luly, J. R.; Plattner, J. J.;; Rosenberg, S. H.; Sham,

H. L. "Renin Inhibiting Analogs", U. S. 4,826,958, 1989.

3) Luly, J. R.; Dellaria, J. F.; Fung, A. K. L.; Kempf, D. J.; Plattner, J. J.; Rosenberg, S. H.; Sham,

H. L. "Renin Inhibiting Compounds", U.S. 4,826,815, 1989.

2) Luly, J. R.; Plattner, J. J.; Dellaria, J. F. "Renin Inhibiting Compounds", U.S. 4,652,551, 1987.

1) Luly, J. R.; Plattner, J. J.; Dellaria, J. F. "Renin Inhibiting Compounds", U.S. 4,645,759, 1987.

Publications

32) Dellaria, Joseph F. “Clearing The “Fog Of Innovation”: Evaluating Ideas Accurately By

Recognizing and Controlling Perceptions.” International Journal of Innovation Sciences, 2009,

Volume 1 (2), pgs. 73-86.

31) Dellaria, Joe. “What You See Is What You Get: Water Visibility and Stream Trout”

Midwest Fly Fishing, 2009 (March), Volume 14, Issue 1, pages 14-15, 27.

30) Dellaria, Joseph F. “Telescoping Light for Perfect Sight”, Wood, 2007, 117, p.10.

29) Bruncko, M.; McClellan, W. J.; Wendt, M. D.; Sauer, D. R.; Geyer, A.; Dalton, C. R.;

Kaminski, M. A.; Weitzberg, M.; Gong, J.; Dellaria, J. F.; Mantei, R.; Zhao, X.; Nienaber, V. L.;

Stewart, K.; Klinghofer, V.; Bouska, J.; Rockway, T. W.; Giranda, V. L. “Naphthamidine

Urokinase, Plasminogen Activator Inhibitors with Improved Pharmacokinetic Properties”, Biorg.

Med. Chem. Lett., 2005, 15, 93-98.

28) Curtin, M. L.; Florjancic, A. S.; Heyman, H. R.; Michaelides, M. R.; Garland, R. B.; Holms, J.

H.; Steinman, D. H.; Dellaria, J. F.; Gong, J.; Wada, C.K.; Guo, Y.; Elmore, I. B.; Tapang, P.;

Albert, D. H.; Magoc, T. J.; Marcotte, P. A.; Bouska, J. J.;Goodfellow, C. L.; Bauch, J. L.; Marsh,

K. C.; Morgan, D. W.; Davidsen, S. K. “Discovery and Characterization of the Potent, Selective,

and Orally Bioavailable, MMP Inhibitor ABT-770”, Biorg. Med. Chem. Lett., 2001, 11 (12),

1557-1560.

27) Michaelides, M. R.; Dellaria, J. F.; Gong, J.; Holms, J. H.; Bouska, J. J.; Stacey, J.; Wada, C.K.;

Heyman, H. R.; Curtin, M. L.; Guo, Y.; Goodfellow, C. L.; Elmore, I. B.; Albert, D. H.; Magoc, T.

J.; Marcotte, P. A.; Garland, R. B.; Morgan, D. W.; Davidsen, S. K. “Biaryl Ether Retohydroxamtes

as Potent Long-lived Orally Bioavailable MMP Inhibitors”, Biorg. Med. Chem. Lett., 2001, 11

(12), 1553-1556.


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26) Kolasa, T.; Brooks, C. D. W.; Rodriques, K. E.; Summers, J. B.; Dellaria, J. F.; Hulkower, K.

I.; Bouska, J.; Bell, R. L.; Carter, G. W. "Nonsteroidal Anti-Inflammatory Drugs As Scaffolds For

The Design Of 5-Lipoxygenase Inhibitors", J. Med. Chem., 1997, 40 (5), 819-824.

25) Dellaria*, J. F.; Sallin, K. J. ; Rodriques, K. "Synthesis of New Amide-linked N-hydroxyurea

5-Lipoxygenase Inhibitors by an Intramolecular Oxygen to Nitrogen Acyl Transfer", Biorg. Med.

Chem. Lett., 1993, 3 (2), 305-309.

24) Luly*, J. R.; Dellaria, J. F.; Davidsen, S.K. “Anti-Inflammatory Patents Highlights From the

First Half of 1992”, Current Opinion in Therapeutic Patents, 1992, 2(10), 1577.

23) Dellaria*, J. F.; Sallin, K. J. "Wittig Olefination in the Absence of an Exogenous Base: a New

Synthesis of -Substituted Primary Allylic Amines", Tetrahedron Lett., 1990, 31, 2661.

22) Rosenberg*, S. H., Dellaria*, J. F.; Kempf*, D. J.; Hutchins, C. W.; Woods, K. W.; Maki, R.

G.; de Lara, E.; Spina, K. P.; Stein H. H.; Cohen, J.; Baker, W. R.; Plattner, J. J.; Kleinert, H. D.;

Perun, T. J. "Potent, Low Molecular Weight Renin Inhibitors Containing a C-Terminal Heterocycle:

Hydrogen Bonding at the Active Site", J. Med. Chem., 1990, 32, 1582.

21) Dellaria*, J. F.; Maki, R. G.; Stein,H. H.; Cohen, J. "New Inhibitors of Human Renin That

Contain Novel Phospho-Statine Derived Leu-Val Replacements" , J. Med. Chem., 1990, 32, 534.

20) Dellaria*, J. F.; Denissen, J. F.; Kerdesky, F.; Maki, R. M.; Nellans, H.N. "An Iterative

Synthesis of Radiolabelled Polyethylene Oligomers", J. Label. Cmpds. Radiopharm., 1989, 27

(12), 1438-1450.

19) Dellaria*, J. F.; Santarsiero, B. D. "The Enantioselective Synthesis of Amino Acid

Derivatives via the Stereoselective Alkylation of a Homochiral Glycine Enolate Synthon", J. Org.

Chem., 1989, 54, 3916-3926.

18) Evans*, D. A., Britton, T. C., Dorow, R. L., Dellaria, J. F. "The Asymmetric Synthesis of -

Amino and -Hydrazino Acid Derivatives via The Stereoselective Amination of Chiral Enolates

with Azodicarboxylate Esters", Tetrahedron, 1988, 44(17), 5525-5540.

17) Plattner*, J. J.; Marcotte, P. A.; Kleinert, H. D.; Stein, H.H.; Greer, J.; Bolis, G.; Fung, A. K.

L.; Bopp, B. A.; Luly, J. R.; Sham, H. L.; Kempf, D. J.; Rosenberg, S. H.; Dellaria, J. F.; De, B.;

Merits, I.; Perun, T. J. "Renin Inhibitors. Dipeptide Analogues of Angiotensinogen Utilizing a

Structurally Modified Phenylalanine Residue to Impart Proteolytic Stability" J. Med. Chem., 1988,

31, 2277-2288.

16) Zydowsky, T. M.; Dellaria*, J. F.; Nellans, H. N. "Efficient and Versatile Synthesis of

Dipeptide Isosteres Containing Gamma- or Delta-Lactams" , J. Org. Chem, 1988, 53, 5607-5616.

15) Dellaria*, J. F.; Santarsiero, B. D. "Stereoselective Alkylation of Chiral Glycine Enolate

Synthons. The Enantioselective Synthesis of -Amino Acid Derivatives" Tetrahedron Lett.,

1988, 29, 6079-6082.

14) Luly*, J. R.; Bolis, G.; BaMaung, N.; Soderquist, J.; Dellaria, J. F.; Stein, H.; Cohen, J.; Perun,

T. J.; Greer, J.; Plattner, J. J. "New Inhibitors of Human Renin That Contain Novel Leu-Val

Replacements. Examination of the P1 Site" , J. Med. Chem., 1988, 31, 532-539.


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13) Dellaria*, J. F.; Maki, R. G.; Bopp, B. A.; Cohen, J.; Kleinert, H.D .; Luly, J. R.; Merits, I.;

Plattner, J. J.; Stein, H. H. "Optimization and in Vivo Evaluations of a Series of Small, Potent, and

Specific Renin Inhibitors Containing a Novel Leu-Val Replacement" , J. Med. Chem., 1987, 30,

2137.

12) Luly*, J. R.; Dellaria, J. F.; Plattner, J. J.; Soderquist, J. L.; Yi, N. "A Synthesis of Protected

Aminoalkyl Epoxides from Alpha-Amino Acids" , J. Org. Chem., 1987, 52, 1487.

11) Dellaria*, J. F.; Maki, R. G. "The Enantio- and Diastereoselective Synthesis of the First

Phospho-Statine Derivative" , Tetrahedron Lett., 1986, 27, 2337.

10) Dellaria*, J. F.; Nordeen, C.; Swett, L. R. "The Facile and Efficient Preparation of Phenolic

and Thiol Esters" , Synth. Commun. , 1986, 16, 1043.

9) Evans*, D. A.; Britton, T. C.; Dorow, R. L.; Dellaria, J. F. "Stereoselective Amination of Chiral

Enolates. A New Approach to the Asymmetric Synthesis of Alpha-Hydrazino and Alpha-Amino

Acids" , J. Am. Chem. Soc., 1986,108, 6395.

8) Luly*, J. R.; Plattner, J. J.; Stein, H. H.; Yi, N.; Cohen, J.; Tricarico, K.; Dellaria, J. F. "Renin

Inhibitors: Peptide Analogs of Angiotensinogen Which Display Potent and Specific Inhibition of

Human Renin" , Pharmacologist, 1985, 27, 260.

7) Hoye*, T. R.; Caruso, A. J.; Dellaria, J. F.; Kurth, M. J. "Two Syntheses of dl-Aplysistatin" , J.

Am. Chem. Soc., 1982, 104, 6704.

6) Hoye*, T. R.; Bottorff, K. J.; Caruso, A. J.; Dellaria, J. F. "Regio- and Stereoselectivity in the

Ene Reaction of N-Phenyl-1,2,4-triazoline-3,5-dione With Alpha,Beta-Unsaturated Carbonyl

Substrates" , J. Org. Chem., 1980, 45, 4287.

5) Doyle*, M. P.; Buhro, W. E.; Dellaria, J. F. "A Facile Synthesis of 1,2-Disubstituted

Cyclopropyl-carbonyl Compounds of High Isomeric Purity" , Tetrahedron Lett., 1979, 4429.

4) Doyle*, M. P.; Elliott, R. C.; Dellaria, J. F. "Ring-size Effects in Lewis Acid Promoted

Reactions of n-(1-Phenylcyclopropyl)alkanoyl Chlorides" , J. Org. Chem., 1978, 43, 4459.

3) Doyle*, M. P.; Dellaria, J. F.; Siegfried, B.; Bishop, S. W. "Reductive Deamination of

Arylamines to Aromatic Hydrocarbons" , J. Org. Chem., 1977, 42, 3494.

2) Doyle*, M. P.; Siegfried, B.; Dellaria, J. F. "Copper(II) Halide Catalyzed Conversion of Aryl

Amines to Aryl Halides" , J. Org. Chem., 1977, 42, 2426.

1) Doyle*, M. P.; Siegfried, B.; Elliott, R. C.; Dellaria, J. F. "A Convenient and Effective

Variation of the Meerwein Arylation Reaction" , J. Org. Chem., 1977, 42, 2431.

PRESENTED PAPERS

22) Dellaria, Joseph F. “Shaping and Harnessing Your Innovation Process: the Interplay Between

Perception and Reality”, Front End of Innovation Conference, Pre-Conference Symposium 2,

Boston, Massachusetts, May 8-11, 2007.


10

21) Kshirsagar, Tushar A.; Griesgraber, George W.; Stoermer, Doris; Amos, David T.; Lindstrom,

Kyle J.; Rice, Michael J.; Crooks, Stephen L.; Bonk, Jason D.; Dellaria, Joseph F.; Heppner,

Philip D.; Gerster, John F.; Merrill, Bryon A.; Johannessen, Sarah C.; Zimmermann, Bernhard M.;

Marszalek, Gregory; Dresssel, Luke T.; Haraldson, Chad A.; Squire, David J.; Wurst, Joshua R.;

Radmer, Matthew R.; Manske, Karl J.; Spessard, Sarah J.; Langer, Scott E.; Karp, Gregory P.;

Gibson, Sheila J.; Wurst, Lindsay R. “Imidazo[4,5-c]quinoline-based TLR7 and TLR8 immune

response modifiers: Structure-activity-relationships relating to potency, selectivity, and therapeutic

applications.” Abstracts of Papers, 232nd ACS National Meeting, San Francisco, CA, United

States, Sept. 10-14, 2006 (2006), MEDI-573.

20) Krepski, Larry R.; Manske, Karl J.; Griesgraber, George W.; Duffy, Daniel E.; Moseman, Joan

T.; Dressel, Luke T.; Stoermer, Doris; Heppner, Philip D.; Kshirsagar, Tushar A.; Dellaria, Joseph

F.; Gibson, Sheila J.; Wurst, Lindsay R. “Synthesis and SAR of TLR7 and TLR8 small molecule

immune response modifiers: Novel alkylamino and alkoxy functionalized imidazo[4,5-

c]quinolines.” Abstracts of Papers, 232nd ACS National Meeting, San Francisco, CA, United

States, Sept. 10-14, 2006 (2006), MEDI-218.

19) Rockway, T. W.; McClellan, W. J.; Dellaria, J. F.; Gong, J.; Mantei, R. A.; Wendt, M.; Zhao,

X.; Weitzberg, M.; Sauer, D.; Bruncko, M.; Dalton, C.; Kaminski, M.; Giranda, V.; Butler, C.;

Linghofer, V.; Joseph, M.; Nienaber, V.; Stewart, K. “Structure-based Design of Novel Urokinase

Inhibitors Derived from 2-Naphthamidine” 220th American Chemical Society National Meeting,

New Orleans, LA, Aug 20-244, 2000, MEDI-ABSTRACT #030.

18) Dellaria,* J. F.; Moore, J. L.; Hulkower, K. I.; Bouska, J.; Grayson, G. K.; Harris, R. R.: Bell,

R. L.; Brooks, C. D. W.; Carter, G. W. "Novel -Unsaturated Ethers Of 4-Methoxy

tetrahydropyran Are Orally Active 5-Lipoxygenase Inhibitors ." 211th American Chemical Society

National Meeting, New Orleans, LA, March 24-28, 1996, MEDI-ABSTRACT #246.

17) Black, * L. A.; Dellaria, J. F., Brooks,C. D. W., Bell, R. L., Harris, R.; Bouska, J.; Bures, M.

G. "Dialkoxycycloalkanes as Leukotriene Biosynthesis Inhibitors" 1989 International Chemical

Congress of Pacific Basin Societies, Honolulu, Hawaii, Dec 21, 1995, ORGN-ABSTRACT #532.

16) Dellaria, * J. F., Moore, J. L., Hulkower, K. I., Bouska, J., Bell, R. L., Brooks,C. D. W.,

Carter, G. W. "New Orally Active 5-Lipoxygenase Inhibitors: Unsaturated Ethers Of 4-

Methoxytetrahydropyran" 6th Interscience World Conference on Inflammation, Antirheumatics,

Analgesics, Immunomodulators, Geneva, Switzerland, March 28-30, 1995, Abstract # 53.

15) Dellaria,* J. F.; Sallin, K. J.; Moore, J. L.; Bell, R. L.; Lanni, C.; Bouska, J.; Young, P. R.;

Brooks, D. W.; Carter, G. W. "Amide-linked N-Hydroxyureas: A New Class of Potent, Long-lived,

and Orally Active 5-Lipoxygenase Inhibitors" 204th American Chemical Society National Meeting,

Washington, DC, August 23-28, 1992, MEDI-ABSTRACT #104.

14) Moore,* J. L.; Brooks, D. W.; Kolasa, T.; Rodriques, K. E.; Dellaria, J. F.; Lanni, C.; Young,

P. R.; Bell, R. L.; Carter, G. W. “5-Lipoxygenase Inhibitory Activity of Alkyl Hydroxyureas”

Abstracts 23rd National Med.Chem.Sym., Buffalo, NY., June 14-18, 1992, Abstract #49.

13) Zydowsky,* T. M.; Dellaria, J. F.; deLara, E.; Nellans, H. N.; Baker, W. R.; Barlow, J.;

Calzadilla, S.; Cohen, J.; Kleinert, H.; Klinghofer, V.; Polakowski, J.; Stein, H.; Verburg, K.;

Perun, T. J. “Synthesis of Renin Inhibitors Containing Conformationally Constrained Gamma- or

Delta-lactams as P-3 Site Replacements” XIIth International Symposium on Medicinal Chemistry,

Switzerland, September 13-17, 1992, 66, Abstract #OC-04.4.


11

12) Dellaria,* J. F.; Brooks, D. W.; Summers, J. B.; Sallin, K. J.; DeNinno, S. L.; Martin, M. B.;

Martin, J. G.;. G.; Moore, J. L.; Holms, J. H.; Lanni, C.; Bouska, J.; Young, SP. R.; Bell, R. L.;

Carter, G. W. "A-69412, a Long Lived, Orally Active, and Selective 5-Lipoxygenase Inhibitor" 4th

Chemical Congress of North America, New York, New York, August 25-30, 1991. MEDI-

ABSTRACT #176.

11) Dellaria,* J. F.; Sallin, K. J. "Allylic Amines, Via In situ Ylide Formation from N-acyl

Aziridines and Triphenylphosphine" 32nd Organic Chemistry Symposium, University of

Minnesota, Minneapolis, Minnesota, June 16-20, 1991, Abstract #A-11.

10) Dellaria,* J. F.; Brooks, D. W.; Summers, J. B.; DeNinno, S. L.; Martin, M. B.; Martin, J. G.;.

G.; Stewart, A. O.; Sallin, K. J.; Bouska, J.; Young, SP. R.; Bell, R. L.; Carter, G. W. "Thiophene-

Derived Inhibitors of 5-Lipoxygenase: Small, Potent, and Bioavailable N-Hydroxy Ureas" 199th

American Chemical Society National Meeting, Boston, Massachusetts, April 22-27, 1990. Abstr.

Pap. Am. Chem. Soc. 1990, 199(0). MEDI-ABSTRACT #76.

9) Brooks,* D. W.; Summers, J. B.; Gunn, B. P.; Dellaria, J. F.; Holms, J. H.; Maki, R. G.; Martin,

J. G.; Martin M. b.; Moore J. L.; Rodriquez, K. E.; Stewart, A. O.; Albert, D. H.; Bell, R. L.;

Bouska, J. B.; Dyer, R. D.; Malo, P. E; Young, P. R.; Rubin, P. Kesterson, J.; Carter, G. W.

"Abbott-64077, a Promising Therapeutic Agent for Treating Leukotriene Mediated Diseases", 199th

American Chemical Society National Meeting, Boston, Massachusetts, April 22-27, 1990. Abstr.

Pap. Am. Chem. Soc. 1990, 199(0). MEDI-ABSTRACT #148.

8) Rosenberg*, S. H.; Dellaria, J. F.; Kempf, D. J.; Woods, K. W.; Maki, R. G.; de Lara, E.;

Kleinert, H. D.;, Stein, H. H.; Cohen, J.; Plattner, J. J.; Baker, W. R.; Perun, T. J. "Renin Inhibitors

Containing A C-terminal Heterocycle", In Proceedings of the 11th Peptide Symposium; Rivier, J. E.

; Marshall, G. R., Eds; Escom: Leiden, 1990; pp402-403.

7) Dellaria*, J. F.; Sallin, K. J.; Maki, R. G.; De Ninno, S. L. "A New Primary Allylic Amine

Synthesis: In Situ Formation And Trapping Of An Ylide From The Reaction Of An N-Acyl

Aziridine, Triphenylphosphine, And An Aldehyde", 1989 International Chemical Congress of

Pacific Basin Societies, Honolulu, Hawaii, Dec 21, 1989, ORGN-ABSTRACT #532.

6) Dellaria*, J. F.; Maki, R. G.; Stein, H. H.; Cohen, J. "Phospho-Statine Derived Renin

Inhibitors" 194th American Chemical Society National Meeting, New Orleans, Louisiana, Sept. 2,

1987. Abstr. Pap. Am. Chem. Soc. 1987, 194(0). MEDI-ABSTRACT #86.

5) Luly*, J. R.; Soderquist, J. L.; Yi, N.; Plattner, J. J.; Dellaria, J. F.; Kleinert, H. D.; Stein, H. H.;

Perun, T. J. "Design and Synthesis of Novel Inhibitors of Renin" , 192nd American Chemical

Society National Meeting, Anaheim, California, September 7-12, 1986. Abstr. Pap. Am. Chem.

Soc., 1986, 192(0). MEDI-ABSTRACT #7.

4) Luly*, J. R.; Dellaria, J. F.; Plattner, J. J.; Soderquist, J. L.; Yi, N. "The Wittig Olefination of

Alpha-Amino Aldehydes with Minimal Racemization. Synthesis of Protected Aminomethyl

Epoxides" , 191st American Chemical Society National Meeting, New York, NY, April 13-18,

1986. Abstr. Pap. Am. Chem. Soc. 1986, 191(0). ORG-ABSTRACT # 42.

3) Luly*, J. R.; Soderquist, J. L.; Yi, N.; Plattner, J. J.; Dellaria, J. F.; Kleinert, H. D.; Maki, R.;

Stein, H. H.; Bopp, B. A.; Perun, T. J. "Low Molecular Weight, Nanomolar Renin Inhibitors" ,

191st American Chemical Society National Meeting, New York, NY, April 13-18, 1986. Abstr.

Pap. Am Chem. Soc. 1986, 191(0). MEDI-ABSTRACT #9.


12

2) Plattner*, J. J.; Fung, A. K. L.; Stein, H.; Kleinert, H. D.; Marcotte, P.; Smital, J.; Dellaria,J. F.;

Sham, H. L.; Luly, J. R.; Rosenberg, S. H.; Kempf, D. J.; Greer, J.; Perun, T. J. "Specific Inhibition

of Human Renin by a Small Peptide, Transition-State Analogs" , 191st American Chemical Society

National Meeting, New York, NY, April 13-18, 1986. Abstr. Pap. Am. Chem. Soc. 1986,191(0),

MEDI-ABSTRACT #28.

1) Dellaria*, J. F.; Evans, D. A. "The Enantioselective Synthesis of Alpha-Amino Acids

Employing a New Chiral Glycine Enolate Synthon" International Symposium of the Chemistry of

Natural Products, Edmonton, Alberta, Canada, June 23-26, 1985. Abstract #-CO-13.

INVITED LECTURES

11) “Part A. New Targets Requiring New Chemistry, Part B. Innovation, Perceptions, and

Information Poor Situations,C. Careers In Chemistry,” University of California, Davis, November

5, 2010.

10) "Medicinal Chemistry: A Mother Of Invention: Uses of Azridine Olefination and

Peptidomimetic Synthesis in Drug Discovery”, Macalester College, St. Paul, Minnesota, November

6, 2002.

9) "Medicinal Chemistry: A Mother Of Invention: Uses of Azridine Olefination and

Peptidomimetic Synthesis in Drug Discovery”, 2001 St. Louis Award Symposium, University of

Missouri-St. Louis, St. Louis, Missouri, April 20, 2001.

8) "Medicinal Chemistry: A Mother Of Invention" University of Kansas, Lawrence, Kansas,

September 9, 1993.

7) "Medicinal Chemistry: A Mother Of Invention" North Dakota State University , Fargo, ND,

November 9, 1989.

6) "Medicinal Chemistry: A Mother Of Invention" University of Minnesota, Minneapolis, MN,

November 8, 1989.

5) "Chemistry Enroute to Renin Inhibitors" University of California, Davis, February 23, 1989.

4) "Optimization of Renin Inhibitors Containing a Novel Leu-Val Replacements and Other

Pharmacological Evaluations" Reno, Nevada, American Association of Pharmaceutical Scientists

Western Regional Meeting, February 27, 1989.

3) "Chemistry Enroute to Renin Inhibitors" University of Nevada, Reno, March 1, 1989.

2) "In Search of Amide Bond Replacements" University of California, Davis, Chemistry

Department Industrial Symposium Program, October 10, 1986.

1) "Cardiovascular Drugs and Some Related Chemistry", Associated Colleges of the Chicago Area,

Argonne Labs, Chicago, Illinois, October 21, 1986.