Patents and Publications

Publications

PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity. Gozgit, Joseph M.; Vasbinder, Melissa M.; Abo, Ryan P.; Kunii, Kaiko; Kuplast-Barr, Kristy G.; Gui, Bin; Lu, Alvin Z.; Molina, Jennifer R.; Minissale, Elena; Swinger, Kerren K.; et al. Cancer Cell (2021), 39(9), 1214-1226.e10.

Targeted Degradation of PARP14 Using a Heterobifunctional Small Molecule. Wigle, Tim J.; Ren, Yue; Molina, Jennifer R.; Blackwell, Danielle J.; Schenkel, Laurie B.; Swinger, Kerren K.; Kuplast-Barr, Kristy; Majer, Christina R.; Church, W. David; Lu, Alvin Z.; et al. ChemBioChem (2021), 22(12), 2107-2110.

A potent and selective PARP14 inhibitor decreases protumor macrophage gene expression and elicits inflammatory responses in tumor explants. Schenkel, Laurie B.; Molina, Jennifer R.; Swinger, Kerren K.; Abo, Ryan; Blackwell, Danielle J.; Lu, Alvin Z.; Cheung, Anne E.; Church, W. David; Kunii, Kaiko; KuplastBarr, Kristy G.; et al. Cell Chemical Biology (2021), 28(8), 1158-1168.e13.

In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement. Wigle, Tim J.; Blackwell, Danielle J.; Schenkel, Laurie B.; Ren, Yue; Church, W. David; Desai, Hetvi J.; Swinger, Kerren K.; Santospago, Andrew G.; Majer, Christina R.; Lu, Alvin Z.; et al. Cell Chemical Biology (2020), 27(7), 877887.

Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes. Wigle, Tim J.; Church, W. David; Majer, Christina R.; Swinger, Kerren K.; Aybar, Demet; Schenkel, Laurie B.; Vasbinder, Melissa M.; Brendes, Arne; Beck, Claudia; Prahm, Martin; et al. SLAS Discovery (2020), 25(3), 241-252.

Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation. Thomenius, Michael J.; Totman, Jennifer; Harvey, Darren; Mitchell, Lorna H.; Riera, Thomas V.; Cosmopoulos, Kat; Grassian, Alexandra R.; Klaus, Christine; Foley, Megan; Admirand, Elizabeth A.; et al. PLoS One (2018), 13(6), e0197372/1e0197372/21.

Identification of a peptide inhibitor for the histone methyltransferase WHSC1. Morrison, Michael J.; Boriack-Sjodin, P. Ann; Swinger, Kerren K.; Wigle, Tim J.; Sadalge, Dipti; Kuntz, Kevin W.; Scott, Margaret Porter; Janzen, William P.; Chesworth, Richard; Duncan, Kenneth W.; et al. PLoS One (2018), 13(5), e0197082/1-e0197082/14.

The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat. Kuntz, Kevin W.; Campbell, John E.; Keilhack, Heike; Pollock, Roy M.; Knutson, Sarah K.; Porter-Scott, Margaret; Richon, Victoria M.; Sneeringer, Chris J.; Wigle, Tim J.; Allain, Christina J.; et al. Journal of Medicinal Chemistry (2016), 59(4), 1556-1564.

Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor. Mitchell, Lorna H.; Boriack-Sjodin, P. Ann; Smith, Sherri; Thomenius, Michael; Rioux, Nathalie; Munchhof, Michael; Mills, James E.; Klaus, Christine; Totman, Jennifer; Kuntz, Kevin W.; et al. ACS Med. Chem. Lett. (2016), 7(2), 134-138.

EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity. Campbell, John E.;

Kuntz, Kevin W.; Knutson, Sarah K.; Warholic, Natalie M.; Keilhack, Heike; Wigle, Tim J.; Raimondi, Alejandra; Klaus, Christine R.; Rioux, Nathalie; Yokoi, Akira; et al. ACS Medicinal Chemistry Letters (2015), ACS Med. Chem. Lett. (2015), 6(5), 491-495.

A medium-throughput single cell CRISPR-Cas9 assay to assess gene essentiality. Grassian, A. R.; Scales, T. M. E.; Knutson, S. K.; Kuntz, K. W.; McCarthy, N. J.; Lowe, C. E.; Moore, J. D.; Copeland, R. A.; Keilhack, H.; Smith, J. J.; et al. Biological Procedures Online (2015), 17, 15/1-15/10.

A High-Throughput Mass Spectrometry Assay Coupled with Redox Activity Testing Reduces Artifacts and False Positives in Lysine Demethylase Screening. Wigle Tim J; Swinger Kerren K; Campbell John E; Admirand Elizabeth A; Boriack-Sjodin P Ann; Kuntz Kevin W; Chesworth Richard; Moyer Mikel P; Scott Margaret Porter; Copeland Robert A; et al. Journal of biomolecular screening (2015), 20(6), 810-820.

Synergistic anti-tumor activity of EZH2 inhibitors and glucocorticoid receptor agonists in models of germinal center non-hodgkin lymphomas. Knutson, Sarah K.; Warholic, Natalie M.; Johnston, L. Danielle; Klaus, Christine R.; Wigle, Tim J.; Iwanowicz, Dorothy; Littlefield, Bruce A.; Porter-Scott, Margaret; Smith, Jesse J.; Moyer, Mikel P.; Kuntz, Kevin W. et al. PLoS One (2014), 9(12), e111840/1e111840/22, DOI:10.1371/journal.pone.0111840

Reaction Coupling between Wild-Type and Disease-Associated Mutant EZH2 Swalm, Brooke M.; Knutson, Sarah K.; Warholic, Natalie M.; Jin, Lei; Kuntz, Kevin W.; Keilhack, Heike; Smith, Jesse J.; Pollock, Roy M.; Moyer, Mikel P.; Scott, Margaret Porter; et al. ACS Chemical Biology (2014), 9(11), 2459-2464.

Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2-Mutant NonHodgkin Lymphoma. Knutson, Sarah K.; Kawano, Satoshi; Minoshima, Yukinori; Warholic, Natalie M.; Huang, Kuan-Chun; Xiao, Yonghong; Kadowaki, Tadashi; Uesugi, Mai; Kuznetsov, Galina; Kumar, Namita; Kuntz, Kevin W.; et al. Molecular Cancer Therapeutics (2014), 13(4), 842-854.

Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. Knutson, Sarah K.; Warholic, Natalie M.; Wigle, Tim J.; Klaus, Christine R.; Allain, Christina J.; Raimondi, Alejandra; Scott, Margaret Porter; Chesworth, Richard; Moyer, Mikel P.; Copeland, Robert A.; Kuntz, Kevin W; et al. Proceedings of the National Academy of Sciences of the United States of America (2013), 110(19), 7922-7927, S7922/1-S7922/5.

Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L. Basavapathruni, Aravind; Jin, Lei; Daigle, Scott R.; Majer, Christina R. A.; Therkelsen, Carly A.; Wigle, Tim J.; Kuntz, Kevin W.; Chesworth, Richard; Pollock, Roy M.; Scott, Margaret P.; et al. Chemical Biology & Drug Design (2012), 80(6), 971-980.

A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Knutson, Sarah K.; Wigle, Tim J.; Warholic, Natalie M.; Sneeringer, Christopher J.; Allain, Christina J.; Klaus, Christine R.; Sacks, Joelle D.; Raimondi, Alejandra; Majer, Christina R.; Song, Jeffrey; Kuntz, Kevin W; et al. Nature Chemical Biology (2012), 8(11), 890-896.

A687V EZH2 is a gain-of-function mutation found in lymphoma patients. Majer, Christina R.; Jin, Lei; Scott, Margaret Porter; Knutson, Sarah K.; Kuntz, Kevin W.; Keilhack, Heike; Smith, Jesse J.; Moyer, Mikel P.; Richon, Victoria M.; Copeland, Robert A.; et al. FEBS Letters (2012), 586(19), 3448-3451.

The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states. Wigle, Tim J.; Knutson, Sarah K.; Jin, Lei; Kuntz, Kevin W.; Pollock, Roy M.; Richon, Victoria M.; Copeland, Robert A.; Scott, Margaret Porter. FEBS Letters (2011), 585(19), 3011-3014.

Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor. Daigle, Scott R.; Olhava, Edward J.; Therkelsen, Carly A.; Majer, Christina R.; Sneeringer, Christopher J.; Song, Jeffrey; Johnston, L. Danielle; Scott, Margaret Porter; Smith, Jesse J.; Xiao, Yonghong; Kuntz, Kevin W; et al. Cancer Cell (2011), 20(1), 53-65.

Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas. Sneeringer, Christopher J.; Scott, Margaret Porter; Kuntz, Kevin W.; Knutson, Sarah K.; Pollock, Roy M.; Richon, Victoria M.; Copeland, Robert A. Proceedings of the National Academy of Sciences of the United States of America (2010), 107(49), 20980-20985, S20980/1-S20980/3.

Discovery of GSK461364: a polo-like kinase 1 inhibitor for the treatment of cancer. Kuntz, Kevin W.; Emmitte, Kyle A. Edited By:Li, Rongshi; Stafford, Jeffrey A. Kinase Inhibitor Drugs (2009), 351-364.

Discovery of an inhibitor of insulin-like growth factor 1 receptor activation: Implications for cellular potency and selectivity over insulin receptor. Wood, Edgar R.; Shewchuk, Lisa; Hassel, Anne; Nichols, Jim; Truesdale, Anne T.; Smith, Danielle; Carter, H. Luke; Weaver, Kurt; Barrett, George; Leesnitzer, Tony; Kuntz, Kevin W. et al. Biochemical Pharmacology (2009), 78(12), 1438-1447.

Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. Emmitte, Kyle A.; Adjebang, George M.; Andrews, C. Webb; Badiang-Alberti, Jennifer G.; Bambal, Ramesh; Chamberlain, Stanley D.; Davis-Ward, Ronda G.; Dickson, Hamilton D.; Hassler, Daniel F.; Hornberger, Keith R.; Kuntz, Kevin W.; et al. Bioorganic & Medicinal Chemistry Letters (2009), 19(6), 1694-1697.

Discovery of thiophene inhibitors of polo-like kinase. Emmitte, Kyle A.; Andrews, C. Webb; Badiang, Jennifer G.; Davis-Ward, Ronda G.; Dickson, Hamilton D.; Drewry, David H.; Emerson, Holly K.; Epperly, Andrea H.; Hassler, Daniel F.; Knick, Victoria B.; Kuntz, Kevin W.; et al. Bioorganic & Medicinal Chemistry Letters (2009), 19(3), 1018-1021.

Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R) Emmitte, Kyle A.; Wilson, Brian J.; Baum, Erich W.; Emerson, Holly K.; Kuntz, Kevin W.; Nailor, Kristen E.; Salovich, James M.; Smith, Stephon C.; Cheung, Mui; Gerding, Roseanne M.; et al. Bioorganic & Medicinal Chemistry Letters (2009), 19(3), 1004-1008.

Imidazo[5,1-f][1,2,4]triazin-2-amines as novel inhibitors of polo-like kinase 1. Cheung, M.; Kuntz, K. W.; Pobanz, M.; Salovich, J. M.; Wilson, B. J.; Andrews, C. W., III; Shewchuk, L. M.; Epperly, A. H.; Hassler, D. F.; Leesnitzer, M. A.; et al. Bioorganic & Medicinal Chemistry Letters (2008), 18(23), 6214-6217.

Regioselective synthesis of benzimidazole thiophene inhibitors of polo-like kinase 1. Hornberger, Keith R.; Badiang, Jennifer G.; Salovich, James M.; Kuntz, Kevin W.; Emmitte, Kyle A.; Cheung, Mui. Tetrahedron Letters (2008), 49(44), 6348-6351

Total Synthesis of Anti-HIV Agent Chloropeptin I. Deng, Hongbo; Jung, Jae-Kyung; Liu, Tao; Kuntz, Kevin W.; Snapper, Marc L.; Hoveyda, Amir H. Journal of the American Chemical Society (2003), 125(30), 9032-9034.

Catalytic enantioselective synthesis of amino acids and macrocyclic peptides: application towards an enantioselective total synthesis of complestatin. Kuntz, Kevin Wayne. Thesis Dissertation (2002), 176 pp.

Mechanism of Enantioselective Ti-Catalyzed Strecker Reaction: Peptide-Based Metal Complexes as Bifunctional Catalysts. Josephsohn, Nathan S.; Kuntz, Kevin W.; Snapper, Marc L.; Hoveyda, Amir H. Journal of the American Chemical Society (2001), 123(47), 11594-11599.

High-throughput screening of titanium-tripeptide Schiff base complexes for catalytic asymmetrical addition of trimethylsilylcyanide to epoxides and imines. Kuntz, Kevin W.; Snapper, Marc L.; Hoveyda, Amir H. Edited By:Sucholeiki, Irving. High-Throughput Synthesis (2001), 283-292.

Ti-Catalyzed Regio- and Enantioselective Synthesis of Unsaturated α-Amino Nitriles, Amides, and Acids. Catalyst Identification through Screening of Parallel Libraries. Porter, James R.; Wirschun, Wolfgang G.; Kuntz, Kevin W.; Snapper, Marc L.; Hoveyda, Amir H. Journal of the American Chemical Society (2000), 122(11), 2657-2658.

Combinatorial catalyst discovery. Kuntz, Kevin W.; Snapper, Marc L.; Hoveyda, Amir H. Current Opinion in Chemical Biology (1999), 3(3), 313-319.

Ti-Catalyzed Enantioselective Addition of Cyanide to Imines. A Practical Synthesis of Optically Pure α-Amino Acids. Krueger, Clinton A.; Kuntz, Kevin W.; Dzierba, Carolyn D.; Wirschun, Wolfgang G.; Gleason, John D.; Snapper, Marc L.; Hoveyda, Amir H. Journal of the American Chemical Society (1999), 121(17), 4284-4285

Patents

Targeted protein degradation of PARP14 for use in therapy. Perl, Nicholas Robert; Kuntz, Kevin Wayne. PCT Int. Appl. (2024), WO2024026083 A1 20230728.

Targeted protein degradation of PARP14 for use in therapy. Perl, Nicholas Robert; Kuntz, Kevin Wayne; Downing, Jennifer. PCT Int. Appl. (2024), WO2024026081 A1 20230728.

Solid forms of a PARP14 inhibitor. Vasbinder, Melissa Marie; Schenkel, Laurie B.; Swinger, Kerren Kalai; Kuntz, Kevin Wayne; Perl, Nicholas Robert; Kremers, John Alphons; Li, Zheng Jane; Chen, Pengyuan. U.S. Pat. Appl. Publ. (2023), US20230303542 A1 20230208.

Dosage regimens, formulations and unit dose forms comprising Poly(ADP-ribose) polymerase PARP7 inhibitors for treating cancer. Vasbinder, Melissa Marie; Utley, Lucas J.; Bozon, Viviana; Kuntz, Kevin Wayne; Parasuraman, Sudha; McCulloch, William; Wood, Nolan. PCT Int. Appl. (2022), WO2022177877 A1 20220825.

Methods of treating inflammatory diseases using quinazolinones. Niepel, Mario; Kuntz, Kevin Wayne; Schenkel, Laurie B.; Swinger, Kerren Kalai; Vasbinder, Melissa Marie, PCT Int. Appl. (2022) WO2022165118 A1 20220804.

Quinolines and azaquinolines as inhibitors of CD38. Downing, Jennifer; Kuntz, Kevin Wayne; Schenkel, Laurie B.; Vasbinder, Melissa Marie. PCT Int. Appl. (2022) WO2022165114 A1 20220804.

Piperazine-pyridazinone derivatives as PARP7 inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. Perl, Nicholas Robert; Vasbinder, Melissa Marie; Schenkel, Laurie B.; Kuntz, Kevin Wayne. PCT Int. Appl. (2021), WO2021087018 A1 20210506.

Pyridazinones as PARP7 inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. Perl, Nicholas Robert; Vasbinder, Melissa Marie; Kuntz, Kevin Wayne. PCT Int. Appl. (2021), WO2021087025 A1 20210506.

Preparation of pyrazolopyrimidine carboxamides and related heterobicyclic amides as inhibitors of

CD38 useful in the treatment of cancer. Schenkel, Laurie B.; Vasbinder, Melissa Marie; Kuntz, Kevin Wayne; Perl, Nicholas Robert; Downing, Jennifer. PCT Int. Appl. (2021), WO2021021986 A1 20210204.

Preparation of quinazolinone derivatives for targeted protein degradation of PARP14 for treatment of cancer and inflammatory diseases. Schenkel, Laurie B.; Vasbinder, Melissa Marie; Kuntz, Kevin Wayne; Swinger, Kerren Kalai; Wigle, Timothy J. N. PCT Int. Appl. (2020), WO2020257416 A1 20201224.

Preparation, characterization and antitumor activity of solid forms of a PARP7 inhibitor. Vasbinder, Melissa Marie; Schenkel, Laurie B.; Swinger, Kerren Kalai; Kuntz, Kevin Wayne; Xu, Jun; Jiang, Meng; He, Xin. PCT Int. Appl. (2020), WO2020223229 A1 20201105.

Substituted cyclohexylamine compounds as SMYD protein inhibitors and their preparation. Foley, Megan Alene Cloonan; Kuntz, Kevin Wayne; Mitchell, Lorna Helen; Munchhof, Michael United States, U.S. Pat. Appl. Publ. (2020), US20200123142 A1 20200423.

Preparation of pyridazinones as PARP7 inhibitors. Vasbinder, Melissa Marie; Schenkel, Laurie B.; Swinger, Kerren Kalai; Kuntz, Kevin Wayne. U.S. Pat. Appl. Publ. (2019), US 20190330194 A1 20191031.

Preparation of BRET probes for screening methods for poly(ADP-ribose) polymerase catalytic site modulators. Wigle, Timothy J. N.; Blackwell, Danielle J.; Kuntz, Kevin Wayne; Vasbinder, Melissa Marie; Schenkel, Laurie B.; Swinger, Kerren Kalai. U.S. Pat. Appl. Publ. (2019), US 20190331688 A1 20191031.

Quinazolinones as PARP14 inhibitors and their preparation. Schenkel, Laurie B.; Vasbinder, Melissa Marie; Kuntz, Kevin Wayne; Swinger, Kerren Kalai. PCT Int. Appl. (2019), WO 2019126443 A1 20190627.

Amine-substituted aryl or heteroaryl compounds as EHMT1 and EHMT2 inhibitors and their preparation. Campbell, John Emmerson; Duncan, Kenneth William; Foley, Megan Alene; Harvey, Darren Martin; Kuntz, Kevin Wayne; Mills, James Edward John; Munchhof, Michael John. PCT Int. Appl. (2017), WO 2017181177 A1 20171019.

Arginine methyltransferase inhibitors and uses thereof for disease treatment. Mitchell, Lorna Helen;

Swinger, Kerren Kalai; Shapiro, Gideon; Boriack-Sjodin, Paula Ann; Chesworth, Richard; Duncan, Kenneth W.; Kuntz, Kevin Wayne; Moradei, Oscar Miguel. PCT Int. Appl. (2017), WO 2017136699 A1 20170810.

Arginine methyltransferase inhibitors and uses. Chesworth, Richard; Mitchell, Lorna Helen; Shapiro, Gideon; Moradei, Oscar Miguel; Kuntz, Kevin Wayne; Duncan, Kenneth W.; Jin, Lei. PCT Int. Appl. (2016), WO 2016044585 A1 20160324.

SMYD inhibitors as Antitumor agents. Foley, Megan Alene Cloonan; Kuntz, Kevin Wayne; Mills, James Edward John; Mitchell, Lorna Helen; Munchhof, Michael John; Harvey, Darren Martin. PCT Int. Appl. (2016), WO 2016040505 A1 20160317.

Isoxazole carboxamides as irreversible SMYD inhibitors. Chesworth, Richard; Foley, Megan Alene Cloonan; Kuntz, Kevin Wayne; Mitchell, Lorna Helen; Petter, Russell C.; Schwartz, Carl Eric. PCT Int. Appl. (2016), WO 2016040511 A1 20160317.

Substituted piperidine compounds as Antitumor agents. Mitchell, Lorna Helen; Bell, Andrew Simon; Chesworth, Richard; Foley, Megan Alene Cloonan; Kuntz, Kevin Wayne; Mills, James Edward John; Munchhof, Michael John. PCT Int. Appl. (2016), WO 2016040515 A1 20160317.

Substituted pyrrolidine compounds as Antitumor agents. Foley, Megan Alene Cloonan; Kuntz, Kevin Wayne; Mitchell, Lorna Helen; Munchhof, Michael John; Harvey, Darren Martin. PCT Int. Appl. (2016), WO 2016040504 A1 20160317.

Substituted cyclohexylamine compounds. Foley, Megan Alene Cloonan; Kuntz, Kevin Wayne; Mitchell, Lorna Helen; Munchhof, Michael John. PCT Int. Appl. (2016), WO 2016040502 A1 20160317.

Isoxazole carboxamide compounds. Foley, Megan Alene Cloonan; Kuntz, Kevin Wayne; Mills, James Edward John; Mitchell, Lorna Helen; Munchhof, Michael John; Harvey, Darren Martin. PCT Int. Appl. (2016), WO 2016040498 A1 20160317.

Substituted pyrrolidine carboxamide compounds as Antitumor agents. Foley, Megan Alene Cloonan; Kuntz, Kevin Wayne; Mitchell, Lorna Helen; Munchhof, Michael John; Harvey, Darren Martin. PCT Int.

Appl. (2016), WO 2016040508 A1 20160317.

Combination therapy for treating cancer comprising inhibitors of human histone methyltransferase EZH2 and one or more other therapeutic agents. Keilhack, Heike; Knutson, Sarah K.; Kuntz, Kevin W. PCT Int. Appl. (2015), WO 2015085325 A1 20150611.

Preparation of N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide monohydrochloride polymorph as an EZH2 inhibitor for cancer treatment. Kuntz, Kevin W.; Choi, Hyeong-Wook; Mathieu, Steven; Sanders, Kristen; Chanda, Arani. PCT Int. Appl. (2015), WO 2015057859 A1 20150423.

Preparation of benzamide derivatives for use as antitumor agents. Campbell, John Emmerson; Kuntz, Kevin Wayne. PCT Int. Appl. (2014), WO 2014172044 A1 20141023.

Indole-ethanediamine derivatives as arginine methyltransferase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. Chesworth, Richard; Mitchell, Lorna Helen; Shapiro, Gideon; Kuntz, Kevin Wayne. PCT Int. Appl. (2014), WO 2014153235 A2 20140925.

Preparation of pyrazole derivatives as PRMT1 inhibitors. Mitchell, Lorna Helen; Shapiro, Gideon; Chesworth, Richard; Boriack-Sjodin, Paula Ann; Moradei, Oscar Miguel; Kuntz, Kevin Wayne. PCT Int. Appl. (2014), WO 2014153172 A1 20140925.

Preparation of substituted 7-deazapurine nucleosides as DOT1 enzyme inhibitors and antitumor agents. Chesworth, Richard; Kuntz, Kevin Wayne. PCT Int. Appl. (2014), WO 2014152261 A1 20140925.

Preparation of substituted 6,5-fused bicyclic heteroaryl compounds as anticancer agents EZH2mediated cancers. Campbell, John Emmerson; Kuntz, Kevin Wayne. PCT Int. Appl. (2014), WO 2014144747 A1 20140918.

Pyrazole derivatives as PRMT1 inhibitors and uses thereof. Kuntz, Kevin Wayne; Mitchell, Lorna Helen; Shapiro, Gideon; Chesworth, Richard; Boriack-Sjodin, Paula Ann. PCT Int. Appl. (2014), WO 2014144659 A1 20140918.

Preparation of 1,4-pyridone bicyclic heteroaryl compounds and useful in the treatment of cancer. Kuntz, Kevin W.; Campbell, John Emmerson. PCT Int. Appl. (2014), WO 2014100665 A1 20140626.

Preparation of 1,4-pyridone compounds and useful in the treatment of cancer. Kuntz, Kevin W.; Campbell, John Emmerson. PCT Int. Appl. (2014), WO 2014100646 A1 20140626.

Preparation of substituted benzene compounds as anticancer agents. Kuntz, Kevin Wayne; Campbell, John Emmerson; Seki, Masashi. U.S. Pat. Appl. Publ. (2014), US 20140107122 A1 20140417.

Method of treating leukemia. Olhava, Edward J.; Chesworth, Richard; Kuntz, Kevin W.; Richon, Victoria M.; Pollock, Roy M.; Daigle, Scott Richard. PCT Int. Appl. (2014), WO 2014039839 A1 20140313.

Combination therapy for treating cancer. Keilhack, Heike; Knutson, Sarah Kathleen; Kuntz, Kevin Wayne. PCT Int. Appl. (2013), WO 2013155464 A1 20131017.

Preparation of N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide monohydrobromide polymorph as an EZH2 inhibitor for cancer treatment. Kuntz, Kevin Wayne; Huang, Kuan-Chun; Choi, Hyeong Wook; Sanders, Kristen; Mathieu, Steven; Chanda, Arani; Fang, Frank. PCT Int. Appl. (2013), WO 2013155317 A1 20131017.

Inhibitors of human histone methyltransferase EZH2, and methods of use thereof for treating cancer. Kuntz, Kevin Wayne; Knutson, Sarah Kathleen; Wigle, Timothy James Nelson. PCT Int. Appl. (2013), WO 2013138361 A1 20130919.

Inhibitors of human histone methyltransferase EZH2, and methods of use thereof for treating cancer. Kuntz, Kevin W.; Knutson, Sarah K.; Wigle, Timothy James Nelson. U.S. Pat. Appl. Publ. (2013), US 20130040906 A1 20130214.

Aryl-or heteroaryl-substituted benzamide compounds as anticancer agents and their preparation.

Kuntz, Kevin Wayne; Chesworth, Richard; Duncan, Kenneth William; Keilhack, Heike; Warholic, Natalie; Klaus, Christine; Zheng, Wanjun; Seki, Masashi; Shirotori, Syuji; Kawano, Satoshi. PCT Int. Appl. (2012), WO 2012142504 A1 20121018.

Substituted N-pyridinylmethyl benzamide compounds as anticancer agents and their preparation. Kuntz, Kevin Wayne; Chesworth, Richard; Duncan, Kenneth William; Keilhack, Heike; Warholic, Natalie; Klaus, Christine; Zheng, Wanjun. PCT Int. Appl. (2012), WO 2012142513 A1 20121018.

Substituted 6,5-fused bicyclic heteroaryl compounds as PRC2 inhibitors and their preparation. Kuntz, Kevin Wayne; Olhava, Edward James; Chesworth, Richard; Duncan, Kenneth William. PCT Int. Appl. (2012), WO 2012118812 A2 20120907.

Preparation of nucleosides as modulators of histone methyltransferase. Chesworth, Richard; Kuntz, Kevin Wayne; Olhava, Edward James; Patane, Michael A. PCT Int. Appl. (2012), WO 2012082436 A2 20120621.

Preparation of carbocycle-substituted purine and 7-deazapurine compounds for the treatment of cancer and neurological disorders. Olhava, Edward James; Chesworth, Richard; Kuntz, Kevin Wayne. PCT Int. Appl. (2012), WO 2012075492 A2 20120607.

Preparation of substituted purine and 7-deazapurine compounds as modulators of epigenetic enzymes. Olhava, Edward James; Chesworth, Richard; Kuntz, Kevin Wayne; Richon, Victoria Marie; Pollock, Roy Macfarlane; Daigle, Scott Richard. PCT Int. Appl. (2012), WO 2012075381 A1 20120607.

7-Deazapurines as Histone methyltransferase modulators. Chesworth, Richard; Kuntz, Kevin Wayne; Olhava, Edward James; Patane, Michael A. PCT Int. Appl. (2012), WO 2012075500 A2 20120607.

Inhibitors of human histone methyltransferase EZH2 and methods of use thereof for treating cancer.

Copeland, Robert Allen; Richon, Victoria Marie; Scott, Margaret Davis; Sneeringer, Christopher John; Kuntz, Kevin Wayne; Knutson, Sarah Kathleen; Pollock, Roy Macfarlane. PCT Int. Appl. (2012), WO 2012034132 A2 20120315.

Heterocyclic compounds as PI3kinase inhibitors and their preparation and use for the treatment of PI3 kinase-mediated diseases. Niu, Deqiang; Petter, Russell C.; Singh, Juswinder; Kluge, Arthur F.; Mazdiyasni, Hormoz; Zhu, Zhendong; Qiao, Lixin; Kuntz, Kevin. PCT Int. Appl. (2011), WO 2011031896 A2 20110317.

Preparation of benzenesulfonamidethiazole derivatives and analogs for use as B-Raf protein kinase inhibitors. Adams, Jerry Leroy; Dickerson, Scott Howard; Johnson, Neil W.; Kuntz, Kevin; Petrov, Kimberly; Ralph, Jeffrey M.; Rheault, Tara Renae; Schaaf, Gregory; Stellwagen, John; Tian, Xinrong; et al. PCT Int. Appl. (2009), WO 2009137391 A2 20091112.

Preparation of 2-[[2-(phenylamino)-1H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]benzamide derivatives as inhibitors of IGF-1R and IR receptor tyrosine kinase and ALK kinase for treating cancer. Chamberlain, Stanley Dawes; Deanda, Felix, Jr.; Gerding, Roseanne; Hasegawa, Masaichi; Kuntz, Kevin; Shotwell, John Brad; Wilson, Joseph; Lei, Huangshu John; Miyazaki, Yasushi; Nishigaki, Naohiko; et al. PCT Int. Appl. (2009), WO 2009020990 A1 20090212.

Benzimidazole thiophene compounds and their preparation, pharmaceutical compositions and use in the treatment of diseases. Kuntz, Kevin; Emmitte, Kyle Allen; Rheault, Tara Renae; Smith, Stephon; Hornberger, Keith; Dickson, Hamilton; Cheung, Mui. U.S. Pat. Appl. Publ. (2008), US 20080300247 A1 20081204.

Preparation of imidazopyridines as inhibitors of IGF-1R and IR and one or both of EGFR and ErbB2 kinases for treating neoplasm. Kuntz, Kevin; Uehling, David Edward; Waterson, Alex Gregory; Emmitte, Kyle Allen; Stevens, Kirk; Shotwell, John Brad; Smith, Stephon Cornell; Nailor, Kristen E.; Salovich, James M.; Wilson, Brian John; et al. U.S. Pat. Appl. Publ. (2008), US 20080300242 A1 20081204.

Preparation of benzimidazolylthiophene benzyl ether compounds as PLK1 inhibitors. Kuntz, Kevin Wayne; Emerson, Holly Kathleen; Cheung, Mui; Badiang, Jennifer Gabriel. PCT Int. Appl. (2007), WO 2007143506 A2 20071213.

Regioselective process for preparing benzimidazole thiophenes. Hornberger, Keith; Cheung, Mui; Pobanz, Mark Andrew; Emmitte, Kyle Allen; Kuntz, Kevin Wayne; Badiang, Jennifer Gabriel. PCT Int. Appl. (2007), WO 2007030366 A1 20070315.

Preparation of imidazotriazines as Polo-like kinases inhibitors for treatment of cancers. Cheung, Mui; King, Nigel Paul; Kuntz, Kevin Wayne; Mook, Robert Anthony, Jr.; Pobanz, Mark Andrew; Salovich, James Michael; Wilson, Brian John. PCT Int. Appl. (2004), WO 2004087652 A2 20041014.

Preparation of benzimidazolyl substituted thiophenes as Polo like kinases (PLK) inhibitors for treating cancer. Andrews, Clarence W., III; Cheung, Mui; Davis-Ward, Ronda G.; Drewry, David Harold; Emmitte, Kyle Allen; Hubbard, Robert Dale; Kuntz, Kevin W.; Linn, James Andrew; Mook, Robert Anthony; Smith, Gary Keith; et al. PCT Int. Appl. (2004), WO 2004014899 A1 20040219.

Preparation of chiral cyano amines and amino acids. Hoveyda, Amir H.; Snapper, Marc L.; Kuntz, Kevin; Krueger, Clinton A.; Dzierba, Carolyn. PCT Int. Appl. (2000), WO 2000015605 A2 20000323.