Selected AMRI Publications and Patents from 2005–2019

publications patents

General

Publications

Frohlich, K.M.; Weintraub, S.F.; Bell, J.T.; Todd, G.C.; Väre, V.Y.P.; Schneider, R.; Kloos, Z.A.; Tabe, E.S.; Cantara, W.A.; Stark, C.J.; Onwuanaibe, U.J.; Duffy, B.C.; Basanta‐Sanchez, M.; Kitchen, D.B.; McDonough, K.A.; Agris, P.F. “Discovery of small‐molecule antibiotics against a unique tRNA‐mediated rRegulation of transcription in gram‐positive bacteria,” ChemMedChem 2019, 14(7), 758-769.
Gushurst, K.S.; Nyman, J.; Boerrigter, S.X.M. “The PO13 crystal structure of ROY,” CrystEngComm 2019, 21, 1363-1368.
Bhaduri,S.; Zhang, H.; Erramilli, S.; Cramer, W.A. “Structural and functional contributions of lipids to the stability and activity of the photosynthetic cytochrome b6f lipoprotein complex,” Journal of Biological Chemistry 2019, 294, 17758-17767.
Hao, J.; Beck, J.P.; Schaus, J.M.; Krushinski, J.H.; Chen, Q.; Beadle, C.D.; Vidal, P.; Reinhard, M.R.; Dressman, B.A.; Massey, S.M.; Boulet, S.L.; Cohen, M.P.; Watson, B.M.; Tupper, D.; Gardinier, K.M.; Myers, J.; Johansson, A.M.; Richardson, J.; Richards, D.S.; Hembre, E.J.; Remick, D.M.; Coates, D.A.; Bhardwaj, R.M.; Diseroad, B.A.; Bender, D.; Stephenson, G.; Wolfangel, C.D.; Diaz, N.; Getman, B.G.; Wang, X.; Heinz, B.A.; Cramer, J.W.; Zhou, X.; Maren, D.L.; Falcone, J.F.; Wright, R.A.; Mitchell, S.N.; Carter, G.; Yang, C.R.; Bruns, R.F.; Svensson,
K.A. “Synthesis and pharmacological characterization of 2-(2,6-dichlorophenyl)-1-((1S,3R)-5-(3-hydroxy-3- methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one (LY3154207), a potent, subtype selective, and orally available positive allosteric modulator of the human Dopamine D1 receptor,” Journal of Medicinal Chemistry 2019, 62(19), 8711-8732.
Devkota, K.P.; Charan, R.D.; Priedemann, C.; Donovan, R.; Snyder, T.M.; Ramirez, C.; Harrigan, G.; Ma, G.; Prakash, I. “Five new ent-atisene glycosides from Stevia rebaudiana,” Natural Product Communications 2019, 14(7), 1-9.
Cioffi, C.L.; Racz, B.; Varadi, A.; Freeman, E.E.; Conlon, M.P.; Chen, P.; Zhu, L.; Kitchen, D.B.; Barnes, K.D.; Martin, W.H.; Pearson, P.G.; Johnson, G.; Blaner, W.S.; Petrukhin, K. “Design, synthesis, and preclinical efficacy of novel nonretinoid antagonists of Retinol-Binding Protein 4 in the mouse model of hepatic steatosis,” Journal of Medicinal Chemistry 2019, 62(11), 5470-5500.
Gurney, M.E.; Nugent, R.A.; Mo, X.; Sindac, J.A.; Hagen, T.J.; Fox, III, D.; O’Donnell, J.M.; Zhang, C.; Xu, Y.; Zhang, H.-T.; Groppi, V.E.; Bailie, M.; White, R.E.; Romero, D.L.; Vellekoop, A.S.; Walker, J.R.; Surman, M.D.; Zhu, L.; Campbell, R.F. “Design and synthesis of selective Phosphodiesterase 4D (PDE4D) allosteric inhibitors for the treatment of Fragile X Syndrome and other brain disorders,” Journal of Medicinal Chemistry 2019, 62(10), 4884-4901.
Charan, R.; Devkota, K.P.; Bhanti, M.; Vadla, N.C.; Ma, G.; Walsh, A.; Harrigan, G.; Prakash, I. “Mogroside Via1, new isomer of Mogroside VI isolated from Luo Han Guo,” IOSR Journal of Applied Chemistry 2019, 12(5), 1-7.
Line, N.J. “Practical enantioselective synthesis of (3S,4R)-3-hydroxypiperidine-4-carboxylic acid,” Tetrahedron Letters 2019, 60(20), 1357-1358.
Jacobson, R.K.; Notaro, M.J.; Carr, G.J. “Comparison of Neisseria gonorrhoeae minimum inhibitory concentrations obtained using agar dilution versus microbroth dilution methods,” Journal of Microbiological Methods 2019, 157, 93-99.
Kharenko, O. A.; Patel, R. G.; Brown, S. D.; Calosing, C.; White, A.; Lakshminarasimhan, D.; Suto, R. K.; Duffy, B. C.; Kitchen, D. B.; McLure, K. G.; Hansen, H. C.; van der Horst, Ed. H.; Young, P. R. “Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine,” Journal of Medicinal Chemistry 2018, 61(18), 8202-8211.
Savarese, J. J.; Sunaga, H.; McGilvra, J. D.; Belmont, M. R.; Murrell, M. T.; Jeannotte, E.; Cooke, F. E.; Wastila, W. B.; Heerdt, P. M. “Preclinical Pharmacology in the Rhesus Monkey of CW 1759-50, a New Ultra-short Acting Nondepolarizing Neuromuscular Blocking Agent, Degraded and Antagonized by L-Cysteine,” Anesthesiology 2018, 129(5), 970-988.
Kroetsch, A.; Chin, B.; Nguyen, V.; Gao, J.; Park, S. “Functional expression of monomeric streptavidin and fusion proteins in Escherichia coli: Applications in flow cytometry and ELISA,” Applied Microbiology and Biotechnology 2018, 102(23), 10079-10089.
Ryan, K.; Kargbo, R.B. “Asymmetric hydrogenation of tetrasubstituted olefins” in Advances in Organic Synthesis, Series Volume 9, Atta-ur-Rahman, Ed., Bentham Science Publishers: Sharjah, UAE, 2018, Chapter 1, 1-24.
Martinez-Camara, S.; Rubio, S.; Del Rio, H.; Rodriguez-Saiz, M.; Barredo, J. L. “Lycopene Production by Mated Fermentation of Blakeslea trispora,” Methods in Molecular Biology 2018, 1852, 257-268.
Barreiro, C.; Barredo, J. L. “Carotenoids Production: A Healthy and Profitable Industry,” Methods in Molecular Biology 2018, 1852, 45-55.
Huang, Z.; Williams, R.; O’Neil-Johnson, M.; Starks, C.; Eldridge, G. “Preparation of a preclinical candidate SQ1274,” ORGN-649649: Abstracts of Papers, 256th ACS National Meeting & Exposition, Boston, MA, United States, August 19-23, 2018.
Huang, Z.; Williams, R. B.; Martin, S. M.; Lawrence, J. A.; Norman, V. L.; O’Neil-Johnson, M.; Harding, J.; Mangette, J. E.; Liu, S.; Guzzo, P. R.; Starks, C. M.; Eldridge, G. R. “Bifidenone: Structure-Activity Relationship and Advanced Preclinical Candidate,” Journal of Medicinal Chemistry 2018, 61(15), 6736-6747.
Ellery, J.; Dickson, L.; Cheung, T.; Ciuclan, L.; Bunyard, P.; Mack, S.; Buffham, W.J.; Farnaby, W.; Mitchell, P.; Brown, D.; Isaacs, R.; Barnes, M. “Identification of compounds acting as negative allosteric modulators of the LPA1 receptor,” European Journal of Pharmacology 2018, 833, 8-15.
Pasetto, P.; Naginskaya, J. “Synthesis of cyclic olefins via Mitsunobu C-alkylation followed by Ramberg-Backlund ring contraction,” Tetrahedron Letters 2018, 59(29), 2797-2799.
Richardson, J.; Mutton, S. P. “Improved Substrate Scope in the Potassium Hexacyanoferrate(II)-Based Cyanation for the Synthesis of Benzonitriles and Their Heterocyclic Analogues,” Journal of Organic Chemistry 2018, 83(9), 4922-4931.
Yu, T.; Zhang, Y.; Kerekes, A.D.; Tagat, J.R.; Doll, R.J.; Xiao, Y.; Esposite, S.; Hruza, A.; Belanger, D.B.; Voss, M.; Rainka, M.P.; Basso, A.; Liu, M.; Liang, L.; Sui, N.; Prelusky, D.; Rindgen, D.; Zhang, L. “Discovery of a highly potent orally bioavailable imidazo-[1,2-a]pyrazine Aurora inhibitor,” Bioorganic & Medicinal Chemistry Letters 2018, 28(8), 1397-1403.
Prakash, I.; Wang, B.; Ma, G.; Harrigan, G.; Sukits, S.F.; Devkota, K.P.; Charan, R.D.; Donovan, R.; Snyder,
T.M. “Novel ent-kaurene glycosides with eight glycosyl units from Stevia rebaudiana,” Natural Product Communications 2018, 13(2), 125-128.
Chowdhury, S.; Owens, K.N.; Herr, R.J.; Jiang, Q.; Chen, X.; Johnson, G.; Groppi, V.E.; Raible, D.W.; Rubel, E.W.; Simon, J.A. “Phenotypic optimization of urea-thiophene carboxamides to yield potent, well tolerated and orally active protective agents against aminoglycoside-induced hearing loss,” Journal of Medicinal Chemistry 2018, 61(1), 84-97.
Chittimalla, S.K.; Nakka, S.; Koodalingam, M.; Bandi, C. “N-Arylation of heterocycles via tandem aza-Michael addition reaction and aromatization sequence,” Synlett 2018, 29(1), 57-64.
Šašic, S.; Gilkison, A.; Henson, M. “Multivariate modeling of Diffuse Reflectance Infrared Fourier Transform (DRIFT) spectra of mixtures with low-content polymorphic impurities with analysis of outliers,” International Journal of Pharmaceutics 2018, 536(1), 251-260.
Šašic, S.; Gilkison, A.; Henson, M. “DRIFTS-based multivariate calibration and prediction of low-concentration polymorphic impurities in multiple lots of an active pharmaceutical ingredient, and outlier criteria,” Journal of Pharmaceutical and Biomedical Analysis 2018, 148, 265-272.
Cao, Y.; Teng, J.; Selbo, J. “Amorphous solid dispersion of epigallocatechin gallate for enhanced physical stability and controlled release,” Pharmaceuticals 2017, 10(4), 88.
Cao, Y.; Verian, K.P. “A VEDA simulation on cement paste: using dynamic atomic force microscopy to characterize cellulose nanocrystal distribution,” Materials Research Society Communications 2017, 7(3), 672-676.
Kargbo, R.B. “Bruton’s Tyrosine Kinase inhibitors for the treatment of autoimmune diseases and cancers,” ACS Medicinal Chemistry Letters 2017, 8(9), 911-913.
Kargbo, R.B. “New substituted cyanoindoline derivatives as MAP3K14 Kinase inhibitors for the treatment of cancer and autoimmune disorders,” ACS Medicinal Chemistry Letters 2017, 8(9), 908-910.
Kargbo, R.B. “Modulating GluN2B for the treatment of neurological and psychiatric disorders,” ACS Medicinal Chemistry Letters 2017, 8(9), 905-907.
Kargbo, R.B. “Allosteric modulators of the M4 Muscarinic Acetylcholine Receptor,” ACS Medicinal Chemistry Letters 2017, 8(9), 903-904.
Chittimalla, S,K.; Bandi, C.; Gadi, V.K.; Gunturu, S.R. “Facile synthesis of 2-arylindoles through Plancher-type rearrangement of 3-alkyl-3-arylindolenines,” Synlett 2017, 28(15), 1994-1999.
Martínez-Cámara, S.; Bahíllo, E.; Barredo, J.-L.; Rodríguez-Sáiz, M. “Scale-up of phytosterols bioconversion into androstenedione” in Microbial Steroids. Methods and Protocols, Methods in Molecular Biology Series Volume 1645, J.-L. Barredo and I. Herráiz, Eds., Humana Press: New York, NY, 2017, Chapter 14, 199-210.
Herráiz, I. “Chemical pathways of corticosteroids, industrial synthesis from sapogenins” in Microbial Steroids. Methods and Protocols, Methods in Molecular Biology Series Volume 1645, J.-L. Barredo and I. Herráiz, Eds., Humana Press: New York, NY, 2017, Chapter 2, 15-27.
Kraft, S.; Ryan, K.; Kargbo, R.B. “Recent advances in asymmetric hydrogenation of tetrasubstituted olefins,” Journal of the American Chemical Society 2017, 139(34), 11630-11641.
Kurissery, A.T.; Rajkumar, G.A.; Arvapalli, V.S.; Pitchumani, V. “Novel synthesis of spirocyclic-3,4-dihydro-2H- benzo[b][1,4]oxazine derivatives,” Tetrahedron Letters 2017, 58(37), 3607-3611.
Pham, T.V.; Murkin, A.S.; Moynihan, M.M.; Harris, L.; Tyler, P.C.; Shetty, N.; Sacchettinia, J.C.; Huang, H.; Meek, T.D. “Mechanism-based inactivator of isocitrate lyases 1 and 2 from Mycobacterium tuberculosis,” Proceedings of the National Academy of Sciences of the United States of America (PNAS) 2017, 114(29), 7617-7622.
Ely, R.; Richardson, P.; Zlota, A.; Steven, A.; Kargbo, R.; Nawrat, C.; Ramirez, A.; Day, D.P.; Knight, J. “Some items of interest to process R&D chemists and engineers,” Organic Process Research & Development 2017, 21(7), 897-910.
Luo, Q.; Yang, X.; Yu, S.; Shi, H.; Wang, K.; Xiao, L.; Zhu, G.; Sun, C.; Li, T.; Li, D.; Zhang, X.; Zhou ,M.; Huang, Y. “Structural basis for lipopolysaccharide extraction by ABC transporter LptB2FG,” Nature Structural & Molecular Biology 2017, 24(5), 469-474.
Tummanapalli, S.; Vangapandu, D.N.; Muthuraman, P.; Kambampati, S.; Shanmugavel, G. “A novel tandem Pd-catalyzed intramolecular allylic decarboxylative coupling and “diradical conjugated 1,3-dien-5-yne cycloaromatization”: An unusual ortho-selectivity in the cycloaromatization and the mechanistic implications,” Tetrahedron Letters 2017, 58(32), 3125-3131.
Galán, B.; Uhía, I.; García-Fernández, E.; Martínez, I.; Bahíllo, E.; de la Fuente, J.L.; Barredo, J.L.; Fernández- Cabezón, L.; García, J.L. “Mycobacterium smegmatis is a suitable cell factory for the production of steroidic synthons,” Microbial Biotechnology 2017, 10(1), 138-150.
Ely, R.; Richardson, P.; Zlota, A.; Steven, A.; Day, D.; Kargbo, R.; Nawrat, C.; Ramirez, A.; Knight, J. “Some items of interest to process R&D chemists and engineers,” Organic Process Research & Development 2017, 21(5), 675-688.
Chittimalla, S.K.; Bandi, C. “Tandem oxidative phenol dearomatization/formal [3+2] annulation protocol en route to highly functionalized benzothiophenes,” Synlett 2017, 28(9), 1051-1056.
Kitchen, D.B. “Computer-aided drug discovery research at a global contract research organization,” Journal of Computer-Aided Molecular Design 2017, 31(3), 309-318.
Zhao, W.; Zhao, D.; Guizzetti, S.; Schwindeman, J.A.; Daniels, D.S.B.; Guerrero, C.; Kargbo, R.; Raghuraman, A.; Knight, J. “Some items of interest to process R&D chemists and engineers,” Organic Process Research & Development 2017, 21(4), 469-478.
Huang, Z.; Williams, R.B.; Mark O’Neil-Johnson, M.; Eldridge, G.R.; Mangette, J.E.; Starks, C.M. “A total synthesis of bifidenone,” Journal of Organic Chemistry 2017, 82(8), 4235-4241.
Ely, R.; Richardson, P.; Zlota, A.; Steven, A.; Day, D.; Kargbo, R.; Nawrat, C.; Ramirez, A.; Knight, J. “Some items of interest to process R&D chemists and engineers,” Organic Process Research & Development 2017, 21(3), 279-291.
Prakash, I.; Ma, G.; Bunders, C.; Charan, R.D.; Ramirez, C.; Devkota, K.P.; Snyder, T.M. “A novel diterpene glycoside with nine glucose units from Stevia rebaudiana Bertoni,” Biomolecules 2017, 7(1), 10.
Zhao, W.; Zhao, D.; Guizzetti, S.; Schwindeman, J.A.; Daniels, D.S.B.; Guerrero, C.; Kargbo, R.; Knight, J. “Some items of interest to process R&D chemists and engineers,” Organic Process Research & Development 2017, 21(2), 142-152.
Chittimalla, S.K.; Koodalingam, M.; Gadi, V.K.; Anaspure, P. “α-Halogenation as a strategy to functionalize cyclohexa-2,4-dienones,” Synlett 2017, 28(4), 475-480.
Gurung, S.R.; Mitchell, C.; Huang, J.; Jonas, M.; Strawser, J.D.; Daia, E.; Hardy, A.; O’Brien, E.; Hicks, F.; Papageorgiou, C.D. “Development and scale-up of an efficient Miyaura borylation process using tetrahydroxydiboron,” Organic Process Research & Development 2017, 21(1), 65-74.
Li, J.; Smith, D.; Krishnananthan, S.; Wu, D.-R.; Sun, D.; Li, P.; Ryan, K.; Hu, M.; Cui, W.; Naginskaya, J.; Liu, S.; Lobben, P.C.; Ng, A.T.; Olson, R.; Mathur, A. “Enantioselective synthesis of BMS-911278: A triple reuptake inhibitor,” Tetrahedron: Asymmetry 2017, 28(1), 196-202.
Deng, Y.; DiMarco, C.N.; Vakhilt, T.; Jonas, M.; White, J.; Arefyev, D.; Tokala, R.; Akhtar, P.; Zhu, L.; Sun, X.; Haimowitz, T.; Condon, S.M. “Process development of the soft histone deacetylase enzyme inhibitor SHP-141: Acylation of methyl paraben and suberyl hydroxamic acid formation,” Organic Process Research & Development 2016, 20(10), 1812-1820.
McClurg, R.B. “Taxonomy of cocrystal ternary phase diagrams,” Journal of Chemical & Engineering Data 2016, 61(12), 4313-4320.
Scott, J.D.; Li, S.W.; Brunskill, A.P.J.; Chen, X.; Cox, K.; Cumming, J.N.; Forman, M.; Gilbert, E. J.; Hodgson, R.A.; Hyde, L.A.; Jiang, Q.; Iserloh, U.; Kazakevich, I.; Kuvelkar, R.; Mei, H.; Meredith, J.; Misiaszek, J.; Orth, P.; Rossiter, L.M.; Slater, M.; Stone, J.; Strickland, C.O.; Voigt, J.H.; Wang, G.; Wang, H.; Wu, Y.; Greenlee, W.J.; Parker, E.M.; Kennedy, M.E.; Stamford, A.W. “Discovery of the 3-imino-1,2,4-thiadiazinane 1,1-dioxide derivative Verubecestat (MK-8931) – A β-site Amyloid Precursor Protein Cleaving Enzyme 1 inhibitor for the treatment of Alzheimer’s Disease,” Journal of Medicinal Chemistry 2016, 59(23), 10435-10450.
Ely, R.; Ramirez, A.; Richardson, P.; Zlota, A.; Kargbo, R.; Steven, A.; Knight, J. “Some items of interest to process R&D chemists and engineers,” Organic Process Research & Development 2016, 20(11), 1839-1849.
Wu, W.-L.; Burnett, D.A.; Clader, J.; Greenlee, W.J.; Jiang, Q.; Hyde, L.A.; Del Vecchio, R.A.; Cohen-Williams, M.E.; Song, L.; Lee, J.; Terracina, G.; Zhang, Q.; Nomeir, A.; Parker, E.M.; Zhang,
L.“Design and synthesis of water soluble β-aminosulfone analogues of SCH 900229 as γ-secretase inhibitors,” Bioorganic and Medicinal Chemistry Letters 2016, 26(23), 5836-5841.
Cioffi, C.L.; Guzzo, P.R. “Inhibitors of Glycine Transporter-1: Potential therapeutics for the treatment of CNS disorders,” Current Topics in Medicinal Chemistry 2016, 16(29), 3404-3437.
Gazal, S.; Gupta, P.; Gunturu, S.R.; Isherwood, M.; Voss, M.E. “Application of Isayama-Mukaiyama cobalt catalyzed hydroperoxysilylation for the preparation of ritonavir hydroperoxide,” Tetrahedron Letters 2016, 57(46), 5099-5102.
Cioffi, C.L.; Liu, S.; Wolf, M.A.; Guzzo, P.R.; Sadalapure, K.; Parthasarathy, V.; Loong, D.T.J.; Maeng, J.-H.; Carulli, E.; Fang, X.; Karunakaran, K.; Matta, L.; Choo, S.H.; Panduga, S.; Buckle, R.N.; Davis, R.N.; Sakwa, S.A.; Gupta, P.; Sargent, B.J.; Moore, N.A.; Luche, M.M.; Carr, G.J.; Khmelnitsky, Y.L.; Ismail, J.; Chung, M.; Bai, M.; Leong, W.Y.; Sachdev, N.; Swaminathan, S.; Mhyre, A.J. “Synthesis and biological evaluation of N-((1- (4-(sulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide inhibitors of Glycine Transporter-1,” Journal of Medicinal Chemistry 2016, 59(18), 8473-8494.
Ely, R.; Ramirez, A.; Richardson, P.; Zlota, A.; Kargbo, R.; Steven, A.; Knight, J. “Some items of interest to process R&D chemists and engineers,” Organic Process Research & Development 2016, 20(9), 1547-1558.
Rynearson, K.D.; Buckle, R.N.; Barnes, K.D.; Herr, R.J.; Mayhew, N.J.; Paquette, W.D.; Sakwa, S. A.; Nguyen, P.D.; Johnson, G.; Tanzi, R.E.; Wagner, S.L. “Design and synthesis of aminothiazole modulators of the gamma- secretase enzyme,” Bioorganic & Medicinal Chemistry Letters 2016, 26(16), 3928-3937.
Bungard, C.J.; Williams, P.D.; Ballard, J.E.; Bennett, D.J.; Beaulieu, C.; Bahnck-Teets, C.; Carroll, S. S.; Chang, R.K.; Dubost, D.C.; Fay, J.F.; Diamond, T.L.; Greshock, T.J.; Hao, L.; Holloway,
Yu, W.; Vibulbhan, B.; Rosenblum, S.B.; Martin, G.S.; Vellekoop, A.S.; Holst, C.L.; Coburn, C.A.; Wong, M.; Selyutin, O.; Ji, T.; Zhong, B.; Hu, B.; Chen, L.; Dwyer, M.P.; Jiang, Y.; Nair, A.G.; Tong, L.; Zeng, Q.; Agrawal, S.; Carr, D.; Rokosz, L.; Liu, R.; Curry, S.; McMonagle, P.; Ingravallo, P.; Lahser, F.; Asante-Appiah, E.; Fells, J.; Kozlowski, J.A. “Discovery of potent macrocyclic HCV NS5A inhibitors,” Bioorganic & Medicinal Chemistry Letters 2016, 26(15), 3793-3799.
Ely, R.; Ramirez, A.; Richardson, P.; Zlota, A.; Kargbo, R.; Steven, A.; Knight, J. “Some items of interest to process R&D chemists and engineers,” Organic Process Research & Development 2016, 20(7), 1109–1117.
Ely, R.; Ramirez, A.; Richardson, P.; Zlota, A.; Kargbo, R.; Steven, A.; Knight, J. “Some items of interest to process R&D chemists and engineers,” Organic Process Research & Development 2016, 20(5), 841–851.
Si, C.; Fales, K.R.; Torrado, A.; Frimpong, K.; Kaoudi, T.; Vanderveer, H.G.; Njoroge, F.G. “Enantioselective synthesis of 3,3-sifluoropyrrolidin-4-ol, a valuable building block in medicinal chemistry,” Journal of Organic Chemistry 2016, 81(10), 4359-4363.
Patil, R.V.; Xu, S.; van Hoek, A.N.; Rusinko, A.; Feng, Z.; May, J.; Hellberg, M.; Sharif, N.A.; Wax, M.B.; Irigoyen, M.; Carr, G.; Brittain, T.; Brown, P.; Colbert, D.; Kumari, S.; Varadaraj, K.; Mitra, A.K. “Rapid identification of novel inhibitors of the human aquaporin-1 water channel,” Chemical Biology & Drug Design 2016, 87(5), 794- 805.
Dubbaka, S. R.; Atthunuri, A. R.; Prakash, K. C.; Rangabashyam, P.; Gadde, S.; Kothandaraman, R. “Copper- mediated oxidative trifluoromethylthiolation of potassium aryltrifluoroborates with elemental sulfur and Ruppert- Prakash reagent,” Synthesis 2016, 48(8), 1246-1252.
Golden, M.; Legg, D.; Milne, D.; Bharadwaj, A. M.; Deepthi, K.; Gopal, M.; Dokka, N.; Nambiar, S.; Ramachandra, P.; Santhosh, U.; Sharma, P.; Sridharan, R.; Sulur, M.; Linderberg, M.; Nilsson, A.; Sohlberg, R.; Kremers, J.; Oliver, S.; Patra, D. “The development of a manufacturing route to an MCHr1 antagonist,” Organic Process Research & Development 2016, 20(3), 675–682.
Wells, A. S.; Wong, J. W.; Michels, P. C.; Entwistle, D. A.; Fandrick, K.; Finch, G. L.; Goswami, A.; Lee, H.; Mix, S.; Moody, T. S.; Pang, L.; Sato, R. K.; Turner, N. J.; Watson, T. J. “Case studies illustrating a science and risk-based approach to ensuring drug quality when using enzymes in the manufacture of active pharmaceuticals ingredients for oral dosage form,” Organic Process Research & Development 2016, 20(3), 594–601.
McLaughlin, M.; Ely, R.; Ramirez, A.; Richardson, P.; Zlota, A.; Kargbo, R.; Steven, A.; Knight, J. “Some items of interest to process R&D chemists and engineers,” Organic Process Research & Development 2016, 20(3), 583–593.
Brown, D. B.; Ironside, M. D.; Shaw, S. M. “Safety notables: Information from the literature,” Organic Process Research & Development 2016, 20(3), 575–582.
Deng, Y.; Xie, Q.; LaPorte, M. G.; Chasnoff, A. T. A.; Mortensen, M. A.; Patra, D.; Putrelo, S. A.; Antonovich,R. S.; Cao, H. Yan, J.; Cooper, A. J.; Rippin, S. R.; Alexander, M. D.; Kumar, P. T.; Hendi, M. S.; Lee, Y.-H.; Haimowitz, T.; Condon, S. M. “Process development and synthesis of birinapant: Large scale preparation and acid-mediated dimerization of the key indole intermediate,” Organic Process Research & Development 2016, 20(2), 242-252.
Nair, A. G.; Zeng, Q.; Selyutin, O.; Rosenblum, S. B.; Jiang, Y.; Yang, D.-Y.; Keertikar, K.; Zhou, G.; Dwyer, M. P.; Kim, S. H.; Shankar, B.; Yu, W.; Tong, L.; Chen, L.; Mazzola, R.; Caldwell, J.; Tang, H.; Allard, M. L.; Buckle,
R. N.; Gauuan, P. J. F.; Holst, C. L.; Martin, G. S.; Naicker, K. P.; Vellekoop, S.; Agrawal, S.; Liu, R.; Kong, R.; Ingravallo, P.; Xia, E.; Zhai, Y.; Nomeir, A.; Kozlowski, J. A. “Discovery of silyl proline containing HCV NS5A inhibitors with pan-genotype activity: SAR development,” Bioorganic & Medicinal Chemistry Letters 2016, 26(5), 1475-1479.
Lobben, P. C.; Amin, R.; Chen, B.-C.; Cui, W.; Hu, M.; Isherwood, M.; Liu, S.; Nacro, K.; Miles, B.; Mobele, B.; Olson, R. E.; Wang, B.; Yang, Y.-L.; Zhao, R. “Enabling synthesis of triple reuptake inhibitor (+)-BMS-820836, a potential therapeutic agent for the treatment of depression,” Organic Process Research & Development 2016, 20(1), 44-50.
Kitchen, D. B.; Decornez, H. Y. “Computational Techniques to Support Hit Triage” in Small Molecule Medicinal Chemistry: Strategies and Technologies, W. Czechtizky and P. Hamley, Eds.; John Wiley & Sons, Inc., 2016, Chapter 7, 191-220.
Chittimalla, S. K.; Koodalingam, M.; Bandi, C.; Putturu, S.; Kuppusamy. R. “Expedient Baylis–Hillman reaction protocol to functionalize cyclohexa-2,4-dienones,” RSC Advances 2016, 6(2), 1460-1465.
Chittimalla, S. K.; Bandi, C. “Unanticipated participation of HCl in nucleophilic chlorination reaction: Expedient route to meta chlorophenols,” Tetrahedron Letters 2016, 57(1), 15-19.
Aziz, R. K.; Monk, Lewis, R. M.; Loh, S. I.; Mishra, A.; Nagle, A. A.; Satyanarayana, C.; Dhakshinamoorthy, S.; Luche, M.; Kitchen, D. B.; Andrews, K. A.; Fong, N. L.; Li, H. J.; Palsson, B. Ø.; Charusanti, P. “Systems biology-guided identification of synthetic lethal gene pairs and its potential use to discover antibiotic combinations,” Scientific Reports 2015, 5, article 16025.
Mishra, A.; Dobritsa, S. V.; Crouch, M.-L.; Rabenstein, J.; Lee, J. X. Y.; Dhakshinamoorthy, S. “Establishment and validation of a 384-well antibacterial assay amenable for high-throughput screening and combination testing,” Journal of Microbiological Methods 2015, 118, 173–175.
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Patents

Andres, P.; Diaz, K. M.; Smolenskaya, V. N. Solid forms of a toll-like receptor modulator. U.S. Patent 10,508,117, December 17, 2019.
Matsuo, Y.; Hisada, S.; Nakamura, Y.; Chakrabarti, A.; Rawat, M.; (Rai, S.; Satyanarayana, A. V.; Duan, Z.; Talukdar, A.; Ravula, S.; Decornez, H. Bicyclic compound and use thereof for inhibiting SUV39H2. U.S. Patent 10,508,109, December 17, 2019.
Wagner, S. L.; Mobley, W. C.; Tanzi, R. E.; Johnson, G.; Buckle, R.; Mayhew, N.; Herr; R. J.; Rynearson, K. D. Potent gamma-secretase modulators. U.S. Patent 10,472,346, November 12, 2019.
Han, Y.; Tummanapalli, S.; Siliphaivanh, P.; Spencer, K. Aryl sulfonamides as BLT1 antagonists. U.S. Patent 10,450,309, October 22, 2019.
Reichenbacher, K.; Duguid, R. J.; Ware, J. A.; Phillipson, D. Forms of R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5- yl)-3-fluorophenyl)-5- -hydroxymethyl oxazolidin-2-one dihydrogen phosphate. U.S. Patent 10,442,829, October 15, 2019.
Lippa, B. S.; Wu, X.; Li, Q.; Wrona, I.; Jackson, A. J.; Chenard, B. L.; Liu, C. M.; Liang, G.; Baevsky, M. F.; Earl, R. A.; Mcqueen, L.; Smit, J.; Cowans, B. A. Inhibiting the transient receptor potential A1 ion channel. U.S. Patent 10,428,072, October 1, 2019.
Petrukhin, K.; Cioffi, C.; Johnson, G.; Dobri, N.; Freeman, E.; Chen, P.; Conlon, M.; Zhu, L. Octahydrocyclopentapyrroles, their preparation and use. U.S. Patent 10,421,720, September 24, 2019.
Petrukhin, K.; Cioffi, C.; Johnson, G.; Allikmets, R.; Freeman, E.; Chen, P.; Conlon, M.; Zhu, L. Substituted 4-phenylpiperidines, their preparation and use. U.S. Patent 10,407,433, September 10, 2019.
Han, Y.; Tummanapalli, S.; Siliphaivanh, P.; Spencer, K. Aryl acylsulfonamides as BLT1 antagonists. U.S. Patent 10,370,368, August 6, 2019.
Gurney, M. E.; Hagen, T. J.; Mo, X.; Vellekoop, A. S.; Romero, D. L.; Campbell, R. F.; Walker, J. R.; Zhu, L. Heteroaryl inhibitors of PDE4. U.S. Patent 10,364,258, July 30, 2019.
Quinn, J. F.; Duffy, B. C.; Liu, S.; Wang, R.; Jiang, M. X.; Martin, G. S.; Wagner, G. S.; Young, P. R. Bicyclic bromodomain inhibitors. U.S. Patent 10,363,257, July 30, 2019.
Han, Y.; Lim, J.; Tummanapalli, S.; Siliphaivanh, P.; Spencer, K. Aryl acylsulfonamides as BLT1 antagonists. U.S. Patent 10,336,733, July 2, 2019.
Petrukhin, K.; Cioffi, C.; Johnson, G.; Dobri, N.; Freeman, E.; Chen, P.; Conlon, M.; Zhu, L. 4-phenylpiperidines, their preparation and use. U.S. Patent 10,273,243, April 30, 2019.
Tweedie, S.; Venkatraman, S.; Zeller, J. Continuous flow carboxylation reaction. U.S. Patent 10,273,212, April 30, 2019.
Speerschneider, A. C.; Yamashita, D. S.; Pitis, P. M.; Hawkins, M. J.; Liu, G.; Miskowski Daubert, T. A.; Yuan, C. C. K.; Borbo Kargbo, R.; Herr, R. J.; Romero, D.; Pacofsky, G. J. 6-membered aza-heterocyclic containing delta- opioid receptor modulating compounds, methods of using and making the same. U.S. Patent 10,246,436, April 2, 2019.
Kharenko, O.; Young, P. R.; Brown, S. D.; Duffy, B. C.; Liu, S. Guzzo, P. Inhibitors of bromodomains. U.S. Patent 10,231,953, March 19, 2019.
Liu, S.; Quinn, J. F.; Duffy, B. C.; Wang, R.; Jiang, M. X.; Martin, G. S.; Zhao, H.; Ellis, M.; Wagner, G. S.; Young, P. R. Substituted bicyclic compounds as bromodomain inhibitors. U.S. Patent 10,226,451, March 12, 2019.
Zeller, J. R.; Venkatraman, S.; Brot, E. C. A.; Iyer, S.; Hall, M. LFA-1 inhibitor and methods of preparation and polymorph thereof. U.S. Patent 10,214,517, February 26, 2019.
Scott, I. L.; Kuksa, V. A.; Gall, A.; Orme, M. W.; Gage, J.; Little, Jr., T. L.; Jiang, Q.; Rossiter, L. M.; McGee, Jr., K. F.; Kubota, R. Styrenyl derivative compounds for treating ophthalmic diseases and disorders. U.S. Patent 10,201,545, February 12, 2019.
Nonnenmacher, M,; Busch, T. Process for the preparation of aminoaryl- and aminoheteroaryl boronic acids and esters. U.S. Patent 10,196,406, February 5, 2019.
Jiang, M. X.; Molino, B. F.; Liu, S.; Wang, R.; Duffy, B. C.; Quinn, J. F.; Wagner, G. S. Substituted pyridines as bromodomain inhibitors. U.S. Patent 10,179,125, January 15, 2019.
Liu, S.; Quinn, J. F.; Duffy, B. C.; Wang, R.; Jiang, M. X.; Martin, G.S.; Zhao, H.; Ellis, M.; Wagner, G. S.; Young, P. R. Substituted bicyclic compounds as bromodomain inhibitors. U.S. Patent 10,166,215, January 1, 2019.
Grisenti, P.; Shahrzad Reza, E.; Guazzi, G.; Argese, M. Stable solid forms of regadenoson. U.S Patent 10,144,756, December 4, 2018.
Karlsson, J.-O.; Reineke, K.; Kurz, T.; Andersson, R.; Hall, M.; McLaughlin, C.; Jacobsson, S.; Nasstrom, J. Calmangafodipir, a new chemical entity, and other mixed metal complexes, methods of preparation, compositions, and methods of treatment. U.S. Patent 10,111,893, October 30, 2018.
Bevill, M. J.; Schultheiss, N. Cocrystals of p-coumaric acid. U.S. Patent 10,098,859, October 16, 2018.
Gurney, M. E.; Hagen, T. J.; Mo, X.; Vellekoop, A. S.; Romero, D. L.; Campbell, R. F.; Walker, J. R.; Zhu, L. Heteroaryl inhibitors of PDE4. U.S. Patent 10,093,686, October 9, 2018.
Blomgren, P. A.; Currie, K. S.; Kropf, J. E.; Lee, S. H.; Mitchell, S. A.; Stafford, D. G.; Xu, J. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors. U.S. Patent 10,093,684, October 9, 2018.
Langston, M.; Mazaik, D.; Elliott, E.; Peterson, A.; Andres, P.; Teng, J. Crystalline form of a proteasome inhibitor. U.S. Patent 10,072,029, September 11, 2018.
Petrukhin, K.; Cioffi, C.; Johnson, G.; Allikmets, R.; Freeman, E.; Chen, P.; Conlon, M.; Zhu, L. Substituted 4-phenylpiperidines, their preparation and use. U.S. Patent 10,072,016, September 11, 2018.
Reichenbacher, K.; Duguid, R. J.; Ware, J. A.; Phillipson, D. Forms of R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin- 5-yl)-3-fluorophenyl)-5- -hydroxymethyl oxazolidin-2-one dihydrogen phosphate. U.S. Patent 10,065,947, September 4, 2018.
Bonde-Larsen, A. L.; Sainz, Y. F.; Retuerto, J. I.; Nieto, J. G. Methods for the preparation of indacaterol and pharmaceutically acceptable salts thereof. U.S. Patent 10,040,765, August 7, 2018.
Quinn, J. F.; Duffy, B. C.; Liu, S.; Wang, R.; Jiang, M. X.; Martin, G. S.; Wagner, G. S.; Young, P. R. Bicyclic bromodomain inhibitors. U.S. Patent 10,010,556, July 3, 2018.
Bevill, M. J.; Schultheiss, N. Polymorphs of cocrystals of P-coumaric acid:nicotinamide. U.S. Patent 10,004,726, June 26, 2018.
Statler, J. A.; Shaw, A. A.; Imbert, D. C.; Nelson, J. L.; Andres, P.; McQueen, L. L.; Boerrigter, S. X. M.; Selbo, J. G. Andres, M. C. Glycopyrrolate salts. U.S. Patent 10,004,717, June 26, 2018.
McCauley, J. A.; Bennett, D. J.; Bungard, C. J.; Greshock, T. J.; Holloway, M. K.; Williams, P. D.; Beaulieu, C.; Crane, S.; Lessard, S.; Mckay, D.; Molinaro, C.; Moradei, O. M.; Sivalenka, V.; Truong, V. L.; Tummanapalli, S. HIV protease inhibitors. U.S. Patent 9,994,587, June 12, 2018.
Ferreiro, G.; Juan, J.; Iglesias Retuerto, J. M.; Gallo Nieto, F. J. Process for the preparation of estetrol. U.S. Patent 9,988,417, June 5, 2018.
Reichenbacher, K.; Duguid, R. J.; Ware, J. A.; Phillipson, D. Forms of R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin- 5-yl)-3-fluorophenyl)-5- -hydroxymethyl oxazolidin-2-one dihydrogen phosphate. U.S. Patent 9,988,406, June 5, 2018.
Numata, T.; Sudo, M.; Sun, X. Benzisoxazole derivative salt. U.S. Patent 9,988,370, June 5, 2018.
Albert, E.; Andres, P.; Bevill, M. J.; Smit, J.; Nelson, J. Cocrystals of progesterone. U.S. Patent 9,982,007, May 29, 2018.
DeCrescenzo, G.; Welsch, D.; Selbo, J. G.; Albert, E. V., Rigsbee, E. M. Crystalline C. sub.21H.sub.22Cl.sub.2N. sub.4O.sub.2 malonate. U.S. Patent 9,951,041, April 24, 2018.
Petrukhin, K.; Cioffi, C.; Johnson, G.; Dobri, N.; Freeman, E.; Chen, P.; Conlon, M.; Zhu, L. Octahydropyrrolopyrroles their preparation and use. U.S. Patent 9,944,644, April 17, 2018.
Petrukhin, K.; Cioffi, C.; Johnson, G.; Dobri, N.; Freeman, E.; Chen, P.; Conlon, M.; Zhu, L. N-alkyl-2- phenoxyethanamines, their preparation and use. U.S. Patent 9,938,291, April 10, 2018.
Petrukhin, K.; Cioffi, C.; Johnson, G.; Dobri, N.; Freeman, E.; Chen, P.; Conlon, M.; Zhu, L. Octahydrocyclopentapyrroles, their preparation and use. U.S. Patent 9,926,271, March 27, 2018.
Albert, E.; Nelson, J. L.; Seadeek, C. S.; Reineke, K.; Jonas, M.; Iyer, S.; Sun, X.; Cutshall, N. S.; Gage, J. L.; Little, T. L.; Luke, W. D.; Brot, E. C. A.; McDermott, M. J. Solid state forms of a PDE10 inhibitor. U.S. Patent 9,920,045, March 20, 2018.
Simon, J.; Johnson, G.; Rubel, E.; Chowdhury, S.; Herr, R. J.; Jiang, Q.; Chen, X.; Owens, K. N.; Raible, D. Compounds and methods for preventing, treating and/or protecting against sensory hair cell death. U.S. Patent 9,902,738, February 27, 2018.
Kamenecka, T. M.; He, Y.; Nguyen, W.; Jiang, R.; Song, X.; Herr, R. J.; Jiang, Q. Substituted prolines/piperidines as orexin receptor antagonists. U.S. Patent 9,896,452, February 20, 2018.
White, S. K.; Ivanisevic, I.; Stephens, K.; Andres, M.; Wolfe, B. S. Treatment methods using pharmaceutical solid state forms. U.S. Patent 9,877,972, January 30, 2018.
Liu, S.; Duffy, B. C.; Quinn, J. F.; Jiang, M. X.; Wang, R.; Martin, G. S.; Zhao, H.; Molino, B. F.; Young, P. R. Heterocyclic compounds as bromodomain inhibitors. U.S. Patent 9,861,637, January 9, 2018.
Gurney, M. E.; Hagen, T. J.; Mo, X.; Vellekoop, A. S.; Romero, D. L.; Campbell; R. F.; Walker, J. R.; Zhu, L. Heteroaryl inhibitors of PDE4. U.S. Patent 9,777,024, October 3, 2017.
Petrukhin, K.; Cioffi, C.; Johnson, G.; Allikmets, R.; Freeman, E.; Chen, P.; Conlon, M.; Zhu, L. Substituted 4-phenylpiperidines, their preparation and use. U.S. Patent 9,777,010, October 3, 2017.
Selbo, J.; Teng, J.; Kabir, M. A.; Golden, P. Formulations of rifaximin and uses thereof. U.S. Patent 9,737,610, August 22, 2017.
Tweedie, S,; Venkatraman, S.; Zeller, J. Continuous flow carboxylation reaction. U.S. Patent 9,725,413, August 8, 2017.
Zeller, J. R.; Venkatraman, S.; Brot, E. C. A.; Iyer, S.; Hall, M. LFA-1 inhibitor and methods of preparation and polymorph thereof. U.S. Patent 9,708,303, July 18, 2017.
Andres, P.; Datar, Y.; Gadiraju, R.; Kowalczyk, B. A.; Kuklis, G. C.; Mirmehrabi, M.; Paschalides, N. Solid salt form of alpha-6-mPEG6-O-hydroxycodone as opioid agonists and uses thereof. U.S. Patent 9,682,988, June 20, 2017.
Bonde-Larsen, A. L.; Retuerto, J. M. I.; Nieto, F. J. G.; Gil, J. J. F. Methods for the preparation of alcaftadine. U.S. Patent 9,682,984, June 20, 2017.
Christopher, M. P.; Fradera Llinas, F. X.; Machacek, M.; Martinez, M.; Reutershan, M. H.; Shizuka, M.; Sun, B.; Thompson, C. F.; Trotter, B. W.; Voss, M. E.; Yang, L. 2,6,7-substituted purines as HDM2 inhibitors. U.S. Patent 9,682,978, June 20, 2017.
DeCrescenzo, G.; Welsch, D.; Selbo, J. G.; Albert, E. V.; Rigsbee, E. M. Crystalline C21H22Cl2N4O2 malonate. U.S. Patent 9,670,177, June 6, 2017.
Quinn, J. F.; Duffy, B. C.; Liu, S.; Wang, R.; Jiang, M. X.; Martin, G. S.; Wagner, G. S.; Young, P. R. Bicyclic bromodomain inhibitors. U.S. Patent 9,663,520, May 30, 2017.
Liu, S.; Quinn, J. F.; Duffy, B. C.; Wang, R.; Jiang, M. X.; Martin, G. S.; Zhao, H.; Ellis, M.; Wagner, G. S.; Young, P. R. Substituted bicyclic compounds as bromodomain inhibitors. U.S. Patent 9,662,311, May 30, 2017.
Guzzo, P.; Surman, M. D.; Henderson, A. J.; Jiang, M. X.; Hadden, M.; Grabowski, J.; Usyatinsky, A. (1-azinone)- substituted pyridoindoles. U.S. Patent 9,650,378, May 16, 2017.
Resnick, L.; Topalov, G. T.; Boyd, S. A.; Belardi, J. K.; Flentge, C. A.; Hale, J. S.; Harried, S. S.; Mareska, D. A.; Zhang, K.; Heap, C. R.; Hadden, M.; Cui, W.; Decornez, H.; Liu, S. Imidazo(4,5-B) pyridin-2-yl amides as KV7 channel activators. U.S. Patent 9,650,376, May 16, 2017.
Cutshall, N. S.; Gage, J. L.; Little, T. L.; Luke, W. D.; Brot, E. C. A.; Jonas, M.; McDermott, M. J.; Reineke, K. E. Processes and intermediates for the preparation of a PDE10 inhibitor. U.S. Patent 9,650,368, May 16, 2017.
Dinsmore, C.; Fradera Llinas, F. X.; Kudale, A. A.; Machacek, M.; Reutershan, M. H.; Thompson, C. F.; Trotter, B. W.; Yang, L. Altman, M. D.; Bogen, S. L.; Doll, R. J.; Voss, M. E. Substituted pyrrolopyrimidines as HDM2 inhibitors. U.S. Patent 9,637,493, May 2, 2017.
Petrukhin, K.; Cioffi, C.; Johnson, G.; Dobri, N.; Freeman, E.; Chen, P.; Conlon, M.; Zhu, L. Octahydrocyclopentapyrroles, their preparation and use. U.S. Patent 9,637,450, May 2, 2017.
Liu, S.; Quinn, J. F.; Duffy, B. C.; Wang, R.; Jiang, M. X.; Martin, G. S.; Zhao, H.; Ellis, M.; Wagner, G. S.; Young, P. R. Substituted bicyclic compounds as bromodomain inhibitors. U.S. Patent 9,636,328, May 2, 2017.
Statler, J. A.; Shaw, A. A.; Imbert, D. C.; Nelson, J. L.; Andres, P.; McQueen, L. L.; Boerrigter, S. X. M.; Selbo, J. G.; Andres, M. C. Glycopyrrolate salts. U.S. Patent 9,610,278, April 4, 2017.
Liu, S.; Molino, B. F.; Nacro, K. Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof. U.S. Patent 9,604,960, March 28, 2017.
Seganish, W. M.; McElroy, W. T.; Brumfield, S.; Herr, R. J.; Yet, L.; Yang, J.; Harding, III, J. P.; Ho, G. D.; Tulshian, D.; Yu, W.; Wong, M. K.C.; Lavey, B.; Kozlowski, J. A. Inhibitors of IRAK4 activity. U.S. Patent 9,598,440, March 21, 2017.
Liu, S.; Duffy, B. C.; Quinn, J. F.; Jiang, M. X.; Wang, R.; Martin, G. S.; Zhao, H.; Molino, B. F.; Young, P. R. Heterocyclic compounds as bromodomain inhibitors. U.S. Patent 9,598,367, March 21, 2017.
Inukai, T.; Takeuchi, J.; Yasuhiro, T.; Wolf, M. A.; Pawar, V. D.; Chakrabarti, A.; Chittimalla, S. K. Pyrrolo pyrimidine derivative. U.S. Patent 9,586,967, March 7, 2017.
Mitchell, S. A.; Currie, K. S.; Blomgren, P. A.; Kropf, J. E.; Lee, S. H.; Xu, J.; Stafford, D. G. Substituted pyrazolo[1,5-a]pyrimidines as Syk inhibitors. U.S. Patent 9,567,348, February 14, 2017.
Williams, R. B.; Eldridge, G.; Starks, C. M.; Guzzo, P. R.; Huang, Z. Phenethyldihydro-benzodioxolones and methods of use. U.S. Patent 9,562,031. February 7, 2017.
Cammarano, C. M.; Christopher, M. P.; Dinsmore, C.; Doll, R. J.; Fradera Llinas, F. X.; Li, C.; Machacek, M.; Martinez, M.; Nair, L. G.; Pan, W.; Reutershan, M. H.; Shizuka, M.; Steinhuebel, D. P.; Sun, B.; Thompson, C. F.; Trotter, B. W.; Wang, Y.; Yang, L.; Bogen, S. L.; Voss, M. E.; Panda, J.; Kurissery, A. T. 2,6,7,8 substituted purines as HDM2 inhibitors. U.S. Patent 9,540,377, January 10, 2017.
Molino, B. F.; Liu, S.; Guzzo, P. R.; Beck, J. P. Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin. U.S. Patent 9,499,531, November 22, 2016.
Kamenecka, T. M.; He, Y.; Nguyen, W.; Jiang, R.; Song, X.; Herr, R. J.; Jiang, Q. Substituted prolines/piperidines as orexin receptor antagonists. U.S. Patent 9,499,517, November 22, 2016.
Qiu, J.; Gao, Q.; Liu, S.; Hu, M.; Yang, Y.-L. A.; Isherwood, M.; Amin, R. Crystalline form of 6-[(4S)-2-methyl-4- (2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyrida- zin-3-amine. U.S. Patent 9,498,476, November 22, 2016.
Kamenecka, T. M.; He, Y.; Jiang, R.; Nguyen, W.; Song, X.; Herr, R. J.; Jiang, Q. Substituted prolines/piperidines as orexin receptor antagonists. U.S. Patent 9,440,982, September 13, 2016.
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Poster: In Vitro Characterization of a Dual Antagonistic Anti-LILRB2/LILRB4 Monoclonal Antibody

We have identified a dual antiLILRB2/LILRB4 antagonist. Targeting MDSCs with this antibody offers great promise for immunotherapy for cancer as well as its immense potential for synergy with PD-1 blockade.

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Trends and Challenges in the Pharmaceutical Industry

Significant changes have taken place in the life sciences industry over the past few years. Since the Covid-19 pandemic, the U.S. government has urged biotech and pharmaceutical companies to increase domestic production in order to secure the drug su...