`
`Chemistry & Drug Discovery Consulting, LLC
`
`+1-650 283-5604 (Cell)
`+49-170-271-8908 (Cell)
`E—mail: hans.maag@chemdisc.com
`
`Moosrain 77
`
`D-82418 Murnau
`
`Germany
`
`1877 SW 14th. Ave.
`
`Portland, OR 97201
`
`USA
`
`Qualifications
`
`- Broad experience in medicinal chemistry spanning most therapy areas
`
`0 Detailed knowledge in the area of prodrugs
`
`o Directed multi—discip|inary project teams, several of them through preclinical
`development to entry into man
`o Managed external alliances and outsourcing contracts as well as internal global
`project teams
`0 Successfully consulted for several biotech companies for lead identification and
`lead optimization programs
`
`flslflmt
`
`- Professional Experience:
`7/10 — present: Principal, Chemistry & Drug Discovery Consulting, LLC. Advising
`biotech companies in the United States and in Europe on all aspects of
`medicinal chemistry.
`1/03 — 6/10 Vice President and Deputy Head of Chemistry, Roche Palo Alto, LLC.
`Responsible for computational chemistry and a purifications group in
`addition to medicinal chemistry groups working on CNS or virology
`projects. Project leader of two pre—clinical CNS project teams, one of
`which with an outside alliance partner. Leader of a Roche global task
`force on lead generation. Co—manager of the department budget of over
`$30M.
`
`5/01 — 12/02 Vice President, Medicinal Chemistry, Neurobiology Unit, Roche
`Bioscience, Palo Alto. Responsibility for medicinal chemistry, including
`parallel synthesis and computational chemistry, and on a temporary basis
`(6 months) for the metabolism and pharmacokinetics group.
`4/O0 — 4/O1 Director Medicinal Chemistry, Neurobiology Unit, Roche Bioscience, Palo
`Alto, CA. Responsibility for medicinal chemistry, parallel synthesis for
`lead optimization and computational chemistry.
`10/99 — 4/00 Acting Director, Medicinal Chemistry, Neurobiology Unit, Roche
`Bioscience, Palo Alto, CA.
`6196 — 9/99: Senior Research Scientist, Neurobiology Unit, Roche Bioscience, Palo
`Alto, CA. Leader of a group engaged in the synthesis of novel ligands for
`biogenic amine receptors. Responsible for the computational chemistry
`group and for setting-up a new parallel synthesis lab in the Neurobiology
`unit. Primary contact person for combinatorial chemistry alliance with third
`party organization. Chemistry and later project leader for a lead
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2030 - 0001
`
`
`
`optimization program directed at an incontinence target.
`7/95 — 5/96: Principal Scientist and Program Leader, Neurobiology Unit, Roche
`Bioscience, Palo Alto, CA. Leader of a program on novel analgesics for
`the treatment of neuropathic pain.
`10/94 — 6/95: Principal Scientist, Institute of Organic Chemistry, Syntex Discovery
`Research, Palo Alto, CA. Leader of a medicinal chemistry group with the
`focus on novel analgesic agents and project team leader for the pre-
`clinical development of a prodrug of the antiviral agent Ganciclovir.
`8/85 - 9/94: Research Section Leader, Institute of Bio-organic Chemistry, Syntex
`Research, Palo Alto, CA. Leader of a group engaged in the synthesis of
`novel anti—vira| and immunosuppressive agents. Directed a task force
`during the early development phase of a potential anti-HIV agent. Co-
`leader of a program on novel immunosuppressive agents targeting the de-
`novo biosynthesis of purine nucleosides. Administrator of a CADD
`Workstation for the department.
`10/83 - 7/85: Research Fellow, Hoffmann-LaRoche Inc. Nutley N.J. Synthesis of 7-
`Fluoro-prostacyclins.
`8/82 — 9/83: Assistant Research Group Chief, Hoffmann-LaRoche Inc. Nutley, N.J.
`Synthesis of 7-Fluoro-prostacyclins.
`8/81 — 7/82: Visiting Scientist, F. Hoffmann-LaRoche & Co. AG. Basel, Switzerland.
`Synthesis of novel dihydrofolate reductase inhibitors.
`10/80 - 7/81: Assistant Research Group Chief, Hoffmann-LaRoche Inc. Nutley N.J.
`Synthesis of prostaglandins.
`8l75 - 9/80: Senior Scientist, Hoffmann-LaRoche Inc. Nutley, N.J.; Studies on the total
`synthesis of the antibiotic Bicyclomycin, synthesis of heterocyclic
`compounds as thromboxane synthetase inhibitors and CNS agents,
`synthesis of l3.—lactam compounds as l3.—|actamase inhibitors.
`
`- Education:
`
`11/73 — 7/75: Postdoctoral Fellow at California Institute of Technology, Pasadena, CA
`in the group of Prof. Robert E. Ireland; Studies on the synthesis of the
`steroidal antibiotic Fusidic acid.
`
`1969 - 1973: Graduate research under the direction of Prof. Albert Eschenmoser;
`Federal Institute of Technology (ETH). Dr. Sc. Techn. awarded October
`1973; Thesis entitled: "Total Synthesis of Vitamin B12: Dicyano-Co(|||)-
`
`cobyrinic acid hexamethyl ester f-amide".
`
`1965 - 1969: Undergraduate studies in chemistry at the Federal Institute of Technology
`(ETH), Zurich, Switzerland. Diploma in Chemistry October 1969; Diploma
`thesis under the direction of Prof. Duilio Arigoni (ETH) on the allylic
`Meisenheimer rearrangement.
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2030 - 0002
`
`
`
`- Teaching Experience:
`
`Spring Quarter 1995, Spring Quarter 1996 and Winter Quarter 1997: Consulting
`Professor, Department of Chemistry, Stanford University, Stanford, CA.
`Teaching introductory organic chemistry courses (Chem. 33 or Chem. 35).
`
`Publications
`
`1. Schreiber J.; Maag H.; Hashimoto N.; Eschenmoser A. "Dimethy|-(methylene)
`ammonium iodide", Angew. Chem. Int. Ed. Engl. E, 330-1(1971).
`
`2.
`
`Ireland R.E.; Beslin, P.; Giger, R.; Hengartner, U.; Kirst, H.A.;Maag, H. "Studies on
`the Total Synthesis of Steroidal Antibiotics. 2. Two Convergent Schemes for the
`Synthesis of Tetracyclic |ntermediates", J. Org. Chem. Q, 1267-1276 (1977).
`
`3. Maag, H.; Blount, J.F.; Coffen, D.L.; Steppe, T.V.; Wong, F. "Structure, Absolute
`Configuration, and Total Synthesis of an Acid-Catalyzed Rearrangement Product of
`Bicyc|omycin", J. Amer. Chem. Soc. E, 6786-6788, (1978).
`
`4. Maag, H.; Locher, R.; Daly, J.J.; Kompis, I. "5—(N—Ary|nortropan—3—yl)— and 5—(N—
`Arylpiperidin-4-yl)-2,4-diaminopyrimidines. Novel Inhibitors of Dihydrofolate
`Reductase." Helv. Chim. Acta Q, 887-97, (1986).
`
`5. Maag, H.; Rydzewski, R.M.; McRoberts, M.J.; Crawford-Ruth, D.; Verheyden, J.P.H.;
`Prisbe, E.J. "Synthesis and Anti—HlV Activity of 4‘—Azido— and 4‘-
`Methoxynuc|eosides." J. Med. Chem. E, 1440-1451 (1992).
`
`6. Maag, H.; Rydzewski, R.M. "An Allylic Azide Route to 4'-Azido Carbocyclic
`Nucleosides. Synthesis of (i)-(1‘a,2‘a,3'b)- and (i)-(1a‘,2‘b,3'b)-1-[1-Azido-2-
`hydroxy-1-(hydroxymethyl)-3-cyc|openty|]thymine." J. Org. Chem. fl, 5823-5831
`(1992).
`
`7. Prisbe, E.J.; Maag, H.; Verheyden, J.P.H.; Rydzewski, R.M. "Structure-Activity
`Relationships of HIV Inhibitory, 4'-Substituted Nucleosides." In Nucleosides and
`Nucleotides as Anfifumor and Antiviral Agents; Chu, C.K.; Baker, D.C. Eds.; Plenum
`Publishing Corp.: New York, 1993.
`
`8. Maag, H.; Gutierrez, A.J.; Prisbe, E.J.; Rydzewski, R.M.; Verheyden, J.P.H. "4'—
`Substituted Nucleosides as Antiviral Agents." In Antibiotics and Antiviral
`Compounds; Krohn, K.; Kirst, H.A.; Maag, H. Eds.; VCH Publishers; Weinheim,
`1993.
`
`9. Maag, H.; Nelson, J.T.; Rios Steiner, J.L.; Prisbe, E.J. "Solid State and Solution
`Conformation of the Potent HIV Inhibitor, 4‘-Azidothymidine." J. Med Chem. Q, 431-
`438 (1994).
`
`10.Maag, H.; Schmidt, B.; Rose S.J. "Oligodeoxynuc|eotide Probes with Multiple Labels
`Linked to the 4'-Position of Thymidine Monomers: Excellent Duplex Stability and
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2030 - 0003
`
`
`
`Detection Sensitivity", Tetrahedron Lett. 3_5, 6449-6452 (1994).
`
`11.Di||on, M.P.; Maag, H.; Muszynski, D.M. “The Regioselective Opening of 5-0-
`Benzyl—1,2:3,4-O—isopropylidene-D—psicofuranose With Organostannanes",
`Tetrahedron Lett. 3_6, 5469-5470 (1995).
`
`12. Ernst, L.; Maag, H. “Preparation and Structure Proof of the Four isomeric
`Dicyanocobyrinic Acid Hexamethyl Ester Monoamides Carrying the Amide Group on
`a Propionic Acid Side Chain, Liebigs Ann. Chem. 323-326 (1996).
`
`13. Dillon, M.P.; Cai, H., Maag, H. “Application of the “Trimethy| Lock" to Ganciclovir, a
`Prodrug with Increased Bioavailability”, Bioorg. Med. Chem. Lett. §, 1653-1656
`(1996).
`
`14. Salaski, E.J.; Maag, H. “GMP Synthase: Synthesis of stable Analog of the putative
`AM P-XMP Intermediate", SynLett, Special Issue, 897-900, (1999).
`
`15. Maag, H. "Prodrugs of Carboxylic Acids." In Prodrugs: Challenges and Rewards;
`Stella, V.J; Borchardt, R.T.; Hageman, M.J.; Oliyai, R.; Maag, H.; Tilley, J.W. Eds.;
`AAPS Press and Springer, Publishers; New York, 2007.
`
`16. Maag, H. "Va|gancio|ovir: A Prodrug of Gancic|ovir." In Prodrugs: Challenges and
`Rewards, Part 2, pp 677- 684; Stella, V.J; Borchardt, R.T.; Hageman, M.J.; Oliyai,
`R.; Maag, H.; Tilley, J.W. Eds.; AAPS Press and Springer, Publishers; New York,
`2007.
`
`17. Li, F.; Maag, H.; Alfredson, T. “Prodrugs of nucleoside analogues for improved oral
`absorption and tissue targeting", J. Pharmaceut. Sciences, fl, 1109-1134 (2007)
`[Volume Date 2008].
`
`18.Smith, D.B.; Kalayanov, G.; Sund, C.; Winqvist, A.; Pinho, P.; Maltseva, T.;
`Morisson, V.; Leveque, V.; Rajyaguru, 8.; Le Pogam, S.; Najera l.; Benkestock, K.;
`Zhou, X.X.; Maag, H.; Cammack, N.; Martin, J.A.; Swallow, S.; Johansson, N.G.;
`Klumpp, K.; Smith, M. “The design, synthesis and antiviral activity of 4'-azidocytidine
`analogues against hepatitis C virus replication: The discovery of 4’-
`azidoarabinocytidine", J. Med. Chem. Q, 219-223 (2009).
`
`19.Smith, D.B.; Kalayanov, G.; Sund, C.; Winqvist, A.; Maltseva, T.; Leveque, V.J.P.;
`Rajyaguru, S.; Le Pogam, S.; Najera, |.; Benkestock, K.; Zhou, X.X.; Kaiser, A.C.;
`Maag, H.; Cammack, N.; Martin, J.A.; Swallow, S.; Johansson, N.G.; Klumpp, K.;
`Smith, M. “The Design, Synthesis, and Antiviral Activity of Monofluoro and Difluoro
`Analogues of 4'-Azidocytidine against Hepatitis C Virus Replication: The Discovery
`of 4'-Azido-2'-deoxy-2'-fluorocytidine and 4'-Azido-2'-dideoxy-2',2'-difluorocytidine".
`J. Med. Chem. Q, 2971-2978 (2009).
`
`20.)/ang, Q.; Haney, B.P.; Vaux, A.; Riley, D.A.; Heidrich, L.; He, P.; Mason, P.; Tehim,
`A.; Fisher, L.E.; Maag, H.; Anderson, N.G. “Controlling the Genotoxins Ethyl
`Chloride and Methyl Chloride Formed During the Preparation of Amine
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2030 - 0004
`
`
`
`Hydrochloride Salts from Solutions of Ethanol and Methanol". Organic Process
`Research & Development, Q, 786-791 (2008).
`
`21 . Maag, H. “Overcoming poor permeability — the role of prodrugs for oral drug
`delivery”, Drug Discovery Today: Technologies, 9, e121—e130 (2012).
`
`22.Sahdeo, S.; Wallace, T.L.; Hirakawa, R.; Knoflach, F.; Bertrand, D.; Maag, H.;
`Misner, D.; Tombaugh, G.C.; Santarelli, L.; Brameld, K.; Milla, M.E.; and Button,
`D.C. “Characterization of RO5126946, a novel (17 nicotinic acetylcholine receptor
`positive allosteric modulator” J Pharmacol Exp Ther, 1, 455-468 (2014).
`
`PresentationsIAbstracts
`
`1. Maag, H.; Obata, N.; Holmes, A.; Schneider, P.; Schilling, W.; Schreiber, J.;
`Eschenmoser, A. "Tota|synthese von Vitamin B12: Endstufen", Chimia, Q, 320
`
`(1972). Abstract of a paper given at the Swiss Chemical Society Meeting, Zurich,
`April 21/22, 1972.
`
`2. Maag, H.; Blount, J.F.; Steppe, T.V. "Bicyclomycin: Approach to the Total
`Synthesis", 180th National ACS Meeting, Las Vegas, Nevada, August 24-29, 1980;
`Abstract ORGN 347. An extended version of this lecture was presented as follows:
`— Sandoz Research Institute, Vienna, Austria; November 30, 1981.
`- University of Innsbruck, Innsbruck, Austria; December 1, 1981.
`- Colorado State University, Fort Collins, Colorado, Nov. 10, 1983.
`
`3. Maag, H.; Sluboski, B.; Rosen, P. "7-Fluoro prostacyclin: A Chemically Stable
`Analog of Prostacyc|in", 185th National ACS Meeting, Seattle, Washington, March
`20-25, 1983; Abstract ORGN 178. A more complete account of this work was
`presented in a plenary lecture at the Medicinal Chemistry Gordon Conference,
`August 1984.
`
`4. Maag, H.; Locher, R.; Kompis, I. "5-(N-Ary|-tropan-3-y|)- and 5-(N-ary|-piperidin-4-y|)-
`2,4-diaminopyrimidines, Novel Inhibitors of Dihydrofolate Reductase (DHFR)". 188th
`National ACS Meeting, Philadelphia, Pennsylvania, August 26-31, 1984; Abstract
`MEDI 28.
`
`5. Maag, H.; Locher, R.; Kompis, I. "5-(N-Ary|-tropan-3-y|)- and 5-(N—ary|-piperidin-4-y|)-
`2,4-diaminopyrimidines, Novel Inhibitors of Dihydrofolate Reductase (DHFR)". Fall
`Meeting of the Swiss Chemical Society, October 19, 1984; Berne, Switzerland.
`
`6. Maag, H.; Chu, N.; Crawford-Ruth, D.; Eugui, E.; McRoberts, M.J.; Mirkovich, A.;
`Pettibone, M.; Prisbe, E.J.; Rydzewski, R.M.; Verheyden, J.P.H. "4'-Azidothymidine:
`Synthesis and in vitro anti—H|V activity". Fourth International Conference on Antiviral
`Research, New Orleans, Louisiana, April 21-26, 1991. Abstract published in
`Antiviral Research Suppl. 1, 43, (1991).
`
`7. Maag, H. "4'-Azidothymidine: Ein neues Nukleosid mit anti-retroviraler Wirkung."
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2030 - 0005
`
`
`
`6
`
`Organic Chemistry Seminar, University of Paderborn, Germany, July 4, 1991.
`
`8. Maag, H.; Barker, M.F.; Prisbe, E.J. “Synthesis and in vitro anti-HIV activity of 2’,3'-
`dideoxy-2',3’-methanonucleosides and of 3’-deoxy-2’,3'-(difluoromethano)thymidine".
`Fifth International Conference on Antiviral Research, Vancouver, B.C., Canada,
`
`March 8-13, 1992. Abstract published in Antiviral Research Sugpl. 1, 55, (1992).
`
`9. Maag, H. “Synthesis of 4’-Substituted Nucleosides as Antiviral Agents." Invited
`Lecture presented at the 3”‘. International Symposium on the Chemical Synthesis of
`Antibiotics and Related Microbial Products, Kloster Banz, Germany, September 23,
`1992.
`
`10.Maag, H. "Synthesis of 4'-Substituted Nucleosides." Lectures presented at the
`Pennsylvania State University, October 13, 1993 and at the University of Pittsburgh,
`October 14, 1993.
`
`10.Lou, L.; Nakamura, J.; Salaski, E.; Maag, H. “An Analog of the Adenyl-XMP
`Intermediate is a Potent Inhibitor of Human GMP Synthetase”. Poster at the
`ASBMB/DBC-ACS Meeting, San Francisco, CA, May 21-25, 1995. Abstract: FASEB
`J. 9(6), p. A1486, Abstr. 1330, 1995.
`
`11.Zhao, S.H.; Berger, J.; Miller, A.K.; Flippin, L.; Clark, R.; Maag, H.; Stepane, G.;
`Watson, N.; Shetty, S.G.; Cefalu, J.S.; Dawson, M.W.; Rocha, C. “Nove| 2-benzy|-
`piperidine derivatives as selective M2 muscarinic receptor antagonists." Abstracts of
`Papers, 221st ACS National Meeting, San Diego, CA, United States, April 1-5, 2001
`(2001), ORGN-597.
`
`12.Maag, H. "Gancic|ovir Pro-Drugs: Synthesis and pre-Clinical Development of
`Valganciclovir (Va|cyteT"")", Invited lecture presented at the symposium on 'Pro-
`Drugs: Understanding the Challenges and Reaping the Rewards‘ at the 2002 AAPS
`(American Association of Pharmaceutical Scientists) Meeting, Toronto, November
`10-14, 2002.
`
`13.Smith, M.; Martin, J.; Smith, D.; Maag, H.; Naiera, |.; Jiang, W.R.; Klumpp, K.;
`Leveque, V.; Cammack, N.; Johansson, N.G.; Kalayanov, G.; Belfrage, A.K.;
`Benkestock, K.; Farnell, K.; Hiscock, S.; Lindborg, B.; Maltseva, T.; Morisson, V.;
`Pinho, P.; Sund, C.; Tozer, M.; Winquist, A.; Zhou, X.X. Abstracts of Papers, 232nd
`ACS National Meeting, San Francisco, CA, United States, Sept. 10-14, 2006
`(2006), MEDI-236.
`
`14.Maag, H. “Prodrugs of Nucleoside Antiviral Agents: From Va|cyteT"" to R1626."
`Lecture presented at the 2"“ Drug Discovery Symposium, Shanghai, October 21,
`2006.
`
`15.Maag, H. “Antiviral Agents: Novel Treatments for Hepatitis C (HCV) Infections."
`Lecture presented at the 3'“ Drug Discovery Symposium, Shanghai, November 9,
`2007.
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2030 - 0006
`
`
`
`16.Ma|tseva, T.; Usova, E.; Johansson, NG.; Kalayanov, G.; Eriksson, S.; Sund, C.;
`Winqvist, A.; Zhou, X-X.; Smith, D.B.; Klumpp, K.; Smith, M.; Maag, H.; Martin, J.A."
`Structure- Activity studies of the deoxycytidine kinase with novel 4' -azido-2'deoxy-
`nucleosides using nmr analysis". SMASH 2008 Conference , Sep 7th-10th, 2008,
`Santa Fe, New Mexico. Poster 11.
`
`17.Maag, H.; Du Bois, D.J.; Loughhead, D.G.; Marika, J.; Misner, D.; Sahdeo, S.;
`Smith, D.B. “2,2-Dimethylcyclopropyl-benzamides: Novel Positive Allosteric
`Modulators of nAChR-07." Nicotinic Acetylcholine Receptors as Therapeutic Targets
`— 2009, Oct. 14-16, 2009, Chicago, Il. Abstract published in Biochemical
`Pharmacology, Q, 913, 2009.
`
`Patents (Generally, the U.S. Patent numbers are listed. In most cases, corresponding
`patents have been issued in additional countries.)
`
`1. Maag, H.; Holland, G.W.; Rosen, P. (Hoffmann-LaRoche Inc.) "7-Fluoro-prostacyclin
`analogues - useful as thrombocyte aggregation inhibitors, gastric secretion inhibitors
`and hypotensives".
`U.S. Pat. 4‘558‘142; issued December 10, 1985.
`
`U.S. Pat. 4'612'380; issued September 16, 1986.
`U.S. Pat. 4'650'883; issued March 17, 198?.
`U.S. Pat. 4‘665‘198; issued May 12, 1987.
`
`2. Kompis, |.; Locher, R.; Maag, H. (F. Hoffmann-LaRoche AG) "New 2,4—Diamino—
`pyrimidine derivatives with antibacterial, antimalarial, coccidiostatic and antitumor
`activity".
`U.S. Pat. 4'590'270; issued May 20, 1986.
`U.S. Pat. 4‘7T4'249; issued September 27, 1988.
`
`3. Holland, G.W.; Maag, H.; Rosen, P. (Hoffmann-LaRoche Inc.) "New 5-ha|o-7-f|uoro-
`prostacyclin derivatives — useful intermediates for active f|uoro—prostacyc|in
`derivatives".
`
`Brit. Pat. 2'158'822; issued June 18, 1986.
`
`4. Holland, G.W.; Maag, H.; Rosen, P. (Hoffmann-LaRoche Inc.) "New 6,9-epoxy-7-
`fluoro-1 1 ,15-dihydroxy-prostenoic acid compounds - useful as blood platelet anti-
`aggregating agents, and new 6-halo-prostanoic acid compound intermediates".
`U.S. Pat. 4'634'782; issued January 6, 1987.
`U.S. Pat. 4‘680‘415; issued July 14, 1987.
`
`5. Holland, G.W.; Maag, H.; Rosen, P. (Hoffmann-LaRoche Inc.) "New 7-f|uoro-11,15-
`bis-tri:a|kyI-silylzoxy-rosta-5-enoic acid cpds. - useful as intermediates to T-f|uoro-
`prostacyclin cpds. useful as blood platelet anti-aggregation agents".
`U.S. Pat. 4‘681‘962; issued July 21, 1987.
`
`6. Holland, G.W.; Maag, H.; Rosen, P. (Hoffmann-LaRoche AG) "New acylated 7-
`f|uoro—prostacyc|in derivs. — useful as circulatory and antiulcer medications".
`Brit. Pat. 2'198'130; issued June 8, 1988.
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2030 - 0007
`
`
`
`7. Holland, G.W.; Maag, H.; Rosen, P.; Lee, F. (Hoffmann-LaRoche AG) "New 16-
`cycloaIkyl-7-fluoro-prostacyclin derivs. - useful as circulatory, cyto:protective and
`antiulcer medicaments".
`
`U.S. Pat. 4‘808‘734; issued February 28, 1989.
`
`8. Maag, H.; Prisbe, E.J.; Verheyden, J.P.H. (Syntex (USA) Inc.) "2'-Deoxy-4'-azido-
`nuc|eoside(s) - useful as antibacterial, antifungal and partic. as antiviral agents in the
`treatment of AIDS".
`
`Europ. Pat. Appl. EP371366, published June 6, 1990.
`U.S. Pat. 5,449,664, issued September 12, 1995
`
`9. Maag, H.; Prisbe, E.J.; Verheyden, J.P.H. (Syntex (USA) Inc.) "New 4'—azido— and 4‘-
`methoxy-substd. nucleoside antiviral agents - have potent activity and high
`therapeutic ratio, and are used for treating HIV, bacterial and fungal infections".
`Europ. Pat. Appl. EP457326, published November 11, 1991.
`U.S. Pat. 5,449,664, issued September 12, 1995
`
`10.Maag, H.; Schmidt, B.; Rose S. (Syntex (USA) Inc.) "Preparation of oligonucleotides
`containing 4'—substituted nucleotides”.
`U.S. Pat. 5,446,137, issued August 29, 1995.
`U.S. Pat. 5,750, 343, issued May 12, 1998.
`
`11.Nestor, J.J.; Womble, S.W.; Maag, H. (Hoffmann-LaRoche AG) “2-(2-Amino-1,6-
`dihydro—6—oxo—purin—9—yl)methoxy—1,3—propanediol derivative.”
`Eur. Pat. Appl. EP694,547, published January 31, 1996.
`U.S. Pat. 6,083,953, issued July 4, 2000.
`
`12. Nestor, J.J.; Womble, S.W.; Maag, H. (Hoffmann-LaRoche AG) “Preparation of
`Ganciclovir derivatives as virucides".
`
`U.S. Pat. 5,543,414, issued August 6, 1996.
`
`13.Caroon, J.M., Clark, R.D., Dillon, M.P., Harris, R.H. III, Hegde, S.S., Lin, C.J.J.,
`Maag, H., Repke, D.B.
`(F. Hoffman-La Roche AG, Switz.). “Preparation of
`piperidinylmethylamino-ethylarenes as muscarinic receptor antagonists."
`PCT Int. Appl. (1999), WO 9943657 A1.
`
`14.Caroon, J.M., Clark, R.D., Dillon, M.P., Harris, R.H. lll, Hegde, S.S., Lin, C.J.J.,
`Maag, H., Repke, D.B. (Syntex (USA) Inc.) “2—Ary|ethy|—(piperidine—4—y|methy|)amine
`derivatives.”
`
`U.S. Pat. 6,319,920, issued November 20, 2001.
`
`15. Dvorak, C.A.; Fisher, L.E.; Green, K.L.; Harris, R.N., III; Maag, H.; Prince, A.; Repke,
`D.B.; Stabler, R.S.
`(F. Hoffmann-La Roche A.-G., Switz.). “Preparation of
`aminoalkyllactams as muscarinic receptor antagonists.”
`U.S. Pat. 6,667,301, issued December 23, 2003
`U.S. Pat. 7,094,778, issued August 22, 2006.
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2030 - 0008
`
`
`
`18.Maag, Hans; Sui, Meng; Zhao, Shu-hai. (Roche Palo Alto LLC, USA). “Preparation
`of substituted benzoxazinones as selective 5-HT6 antagonists for treating central
`nervous system diseases and gastrointestinal tract disorders."
`US7141562 B2, issued November 28, 2006.
`
`19. Dvorak, C.A.; Fisher, L.E.; Green, K.L.; Harris, R.N., Ill; Maag, H.; Prince, A.; Repke,
`D.B.; Stabler, R.S. (Roche Palo Alto, LLC, USA.). “Preparation of
`heterocyclylalkylamines as muscarinic receptor antagonists."
`US7361648 B2, issued April 22, 2008.
`
`20. Du Bois, D.J.; Elworthy, T.R.; Maag, H.; Sahdeo, S. “Preparation of tetrazo|e—
`substituted aryl amide derivatives as modulators of nicotinic receptors”. (F.
`Hoffmann—La Roche AG, Switz.).
`UST981914 B2, issued July 19, 2011.
`
`21.Du Bois, D.J.; Hurst, D.N.; Loughhead, D.G.; Maag, H.; Manka, J.; Smith, D.B.
`,,Preparation of arenecarboxylic acid cyclopropylamides as positive .a|pha.7 nAChR
`nicotinic acetylcholine receptor allosteric modulators“.
`(F. Hoffmann—La Roche AG,
`Switz.).
`US7723391 B2, issued May 25, 2010.
`
`22.Broka, C.A.; Hendricks, R.T.; Maag, H.; Smith, D.B.; Wanner, J. “Preparation of
`thieno[3,2-d]pyrimidines for treating hepatitis C virus infection”.
`(Roche Palo Alto
`LLC, USA).
`u.s. Pat. Appl. Publ. (2011), us 20110070190 A.
`
`23.Turner, W.W.; Arnold, L.D.; Maag, H.; Zlotnick, A. “Hepatitis b core protein allosteric
`modulators". (Indiana University Research and Technology Corporation and
`Assembly Biosciences, Inc.)
`PCT Int. Appl. Publ. (2015) WO2015138895 A1
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2030 - 0009