Publications
Singh, S.; Sarroza, D.; English, A.; Whittington, D.; Dong, A. Malamas, S. M.; Makriyannis, A.; Van der Stelt, M.; Li, Y.; Zweifel, L.; Bruchas, M.; Land, B.; Stella, N. P2X7 receptor-dependent increase in 2-AG production by neuronal cells in culture: Dynamics and mechanism. Br. J. of Pharm., 181(15):2459-2477, 2024.
Alkhelb D.; Tsoutsouva C.; Nikas, S.; Malamas S. M.; Makriyannis , A. ;Desai, R. Effects of Cannabinoid Agonists on Fentanyl-Induced Respiratory Depression. J. Pharm. Exper. Ther. 309, 315, 2024.
Avraham, S.; Avraham, H.; Benchama, O.; Tyukhenko, S.; Malamas, S. M.; Williams, M.; Makriyannis, A. Targeting Monoacylglycerol Lipase in Triple-Negative Breast Cancer Reduced Tumor-Associated Inflammation and Decreased Colonization in the Brain. Authorea, 711508, 2024.
Papadogkonaki, S.: Spyridakos, D.: Lapokonstantaki, E.; Chaniotakis, N.; Makriyannis, A.; Malamas, S. M.; Thermos, K. Investigating the role of exogenous and endogenous 2-arachidonoylglycerol on retinal CB1 cannabinoid receptors and reactive microglia in naïve and diseased retina. Inter. J. Mol. Science, 24(21):15689, 2023.
Malamas, S. M.; Lamani, M.; Farah, S.; Mohammad, K.; Miyabe, C.; Weerts, C.; Speziale, M.; Hilston, S.; Zvonok, N.; Chandrashekhar, C.; Ploss, M.; Straiker, A. Dual ABHD6/MGL inhibitors for the treatment of ocular disease. RCS Medicinal Chemistry, 2023.
Benchama, O.; Malamas, S. M.; Praveen, K.; Ethier, E.; Williams, M.; Makriyannis, A.; Avraham, H. Inhibition of triple negative breast cancer-associated inflammation and progression by N- acylethanolamine acid amide hydrolase (NAAA). Sci Rep 2022, 12, 22255.
Benchama, O.; Robert Donnelly, R.; Malamas, S. M.; Williams, M.; Tyukhtenko, S.; Chen, C.; Ethier, E.; Makriyannis, A.; Avraham, S.; Avraham, H. Inhibition of Monoacylglycerol Lipase in Triple Negative Breast Cancer Reduced Tumor-Associated Inflammation, Attenuated Blood- Brain Barrier Impairment and Decreased Colonization in the Brain. Sci Rep 2022, 12, 5328.
Romano, R.; Pagano, E.; Iannotti, F.; Piscitelli, F.; Brancaleone, V.; Fiorino, F.; Sparaco, R.; Vanacore, G.; Lucariello, G.; Di Tella, F.; Lionetti, R.; Makriyannis, Malamas, S. M.; De Luca, M.; Aprea, G.; D’Armiento, M.; Capasso, R.; Sbarro, B.; Venneri, T.; Di Marzo, V.; Borrelli, F.; Izzo, A. Pharmacological and genetic modulation of N-Acylethanolamine acid amidase (NAAA) impacts colorectal cancer growth. Br J Pharmacol. 2022, 179:1679-1694.
Mauricio, C.; Monti, A.; Sunny, S.; Lynch, O.; Xia, Y.; Lin, L.; Malamas, S. M.; Steelman, S.; Krishnamoorthy, S.; 1, Stewart, S.; Tozzo, E. Identification of Small Molecules That Induce Therapeutic Levels of Fetal Hemoglobin for Treatment of Sickle Cell Disease By Pairing Machine Learning with High-Resolution Single Cell RNA Sequencing Maps of Adult and Fetal Human Erythropoiesis. Blood, 13, 2022.
Malamas, S. M.; Pavlopoulos, S.; Alapafuja, S.; Farah, S.; Zvonok, A.; Mohammad, K.; West, J.; Perry, N.; Pelekoudas, D.; Rajarshi, G.; C.; Chandrashekhar, H.; Wood, J.; Makriyannis, A. Design and Structure-Activity Relationships of Isothiocyanates as Potent and Selective N‑Acylethanolamine-Hydrolyzing Acid Amidase Inhibitors. J. Med. Chem. 2021, 64, 5956-5972.
Malamas, S. M.; Lamani, M.; Farah, S.; Mohammad, K.; Miyabe, C.; Rajarshi, G.; Wu, S. Zvonok, N.; Chandrashekhar, H.; Wood, L.; Makriyannis, A. Design and Synthesis of Highly Potent and Specific ABHD6 Inhibitors. ChemMedChem, 2021, DOI: 10.1002/cmdc.202100406.
Congiu, M; Lara Micheli, L.; Santoni M.; Sagheddu C.; Muntoni, A; Makriyannis, A; Malamas, S. M.; Ghelardini, C; Mannelli, L.; Pistis, M. N-Acylethanolamine Acid Amidase Inhibition Potentiates Morphine Analgesia and Delays the Development of Tolerance. Neurotherapeutics, 2021, DOI: 10.1007/s13311-021-01116-4.
Toma, W.; Caillaud, M.; Donvito, G.; Roberts, J.; Bagdas, D.; Jackson, A.; Lichtman, A.; Gewirtz, D.; Makriyannis, A.; Malamas, S. M.; Damaj, I. Inhibition of N-acylethanolamine- hydrolyzing acid amidase by the selective ligand AM9053 is a new potential target to treat paclitaxel-induced neuropathy in mice. Eur. J. Pain 2021, DOI: 10.1002/ejp.1758.
Bottemanne, P.; Guillemot-Legris, O.; Paquot A.; Malamas, S. M.; Makryannis, A., Alhouayek, M.; Muccioli. G. N-acylethanolamine hydrolyzing acid amidase inhibition but not Fatty acid amide hydrolase inhibition prevents the development of experimental autoimmune encephalomyelitis in mice. Neurotherapeutics 2021, 18(3):1815-1833.
Kokona, D.; Spyridakos, D.; Tzatzarakis M.; Papadogkonaki, S; Filidou, E.; Arvanitidis, K.; Kolios, G.; Lamani, M.; Makiryannis, A.; Malamas S. M.; Thermos, K. The endocannabinoid 2- arachidonoylglycerol and dual ABHD6/MAGL enzyme inhibitors display neuroprotective and anti-inflammatory actions in the in vivo retinal model of AMPA excitotoxicity. Neuropharmacology 2021, 185, 108450.
Honrao, C.; Ma, X.; Kulkarni, S.; Joshi, V.; Malamas, S. M.; Wood, J.; Zvonok, A.; Strand, D.; Guo, J.; Makriyannis, A. Metabolic profiling of a CB2 agonist, AM9338, using LC-MS and microcoil-NMR: Identification of a novel dihydroxy adamantyl metabolite. Frontiers in Pharmacology, Section Drug Metabolism and Transport 2020, 11, 575691.
Malamas M. S.; Farah S.; Lamani M.; Pelekoudas D.; Perry N.; Rajarshi G.; Miyabe C.; Honrao C.; West J.; Pavlopoulos S.; Makriyannis A. Design and synthesis of cyanamides as potent and selective N-acylethanolamine acid amidase inhibitors. Bioorg. Med. Chem. 2020, 28, 115195.
Lamani M.; Malamas, M. S.; Farah S.; Shukla V.; Almeida M.; Weerts C.; Anderson J.; Wood J.; Farizatto K.; Bahr B.; Makriyannis A. Piperidine and piperazine inhibitors of fatty acid amide hydrolase targeting excitotoxic pathology. Bioorg. Med. Chem. 2019, 27, 115096.
Ogden S.; Malamas M. S.; Makriyannis A.; Eckel L. The novel cannabinoid CB1 receptor agonist AM11101 increases food intake in female rats. Br J Pharmacol. 2019; 176:3972–3982.
Sagheddu C.; Scherma M.; Congiu M.; Fadda P.; Carta G.; Banni S.; Wood J.; Makriyannis A.; Malamas M. S.; Pistis M. Inhibition of N-acylethanolamine acid amidase reduces nicotine- induced dopamine activation and reward. Neuropharmacology 2019, 144 327–336.
Alapafuja S.; Malamas M.S.; Shukla V.; Zvonok A.; Miller S.; Daily L.; Rajarshi G.; Miyabe C; Honrao C.; Wood J.; Tyukhtenko S.; Straiker A.; Makriyannis A. Synthesis and evaluation of potent and selective MGL inhibitors as a glaucoma treatment. Bioorg. Med. Chem. 2019, 27 55– 64
Malamas M. S.; Raghav J.; Xiaoyu, M.; Honrao C.; Wood J.; Benchama O.; Zhou H.; Mallipeddi S.; Makriyannis A. Oximes short-acting CB1 receptor agonists. Bioorg. Med. Chem. 2018, 26 4963–4970.
Golden, E.; Miyabe, C.; Wood, J.; Malamas, S.M.; Alapafuja, S.; Makriyannis, A. Optimization of a Medium-Throughput Cathepsin K Inhibition Assay for NAAA Inhibitors. FASEB, 609.3, 2018.
Pavlopoulos, S.; Pelekoudas, D.; Benchama, O.; Rawlins, C.; Agar, J.; West, J.; Malamas, M.S.; Zvonok, N.; Makriyannis, A. Secretion, Isotopic Labeling and Deglycosylation of N- Acylethanolamine Acid Amidase for Biophysical Studies. Protein Expr. Purif.2017, 17, S1046- 5928.
Malamas, M. S.; Ni, Y.; Erdei, J.; Stange, H.; Schindler, R.; Hans-Joachim Lankau, H-J.; Grunwald, C.; Fan, K.; Parris, K.; Langen, B.; Egerland, U.; Hage, T.; Marquis, K.; Harrison, B.; Robichaud, A.; Kronbach, T.; Pangalos, M.; Brandon, N.; Hofgen, N. Novel Triazines as Potent and Selective Phosphodiesterase 10A Inhibitors. Bioorg & Med. Chem. Lett. 2012, 22, 5786- 5784.
Malamas, M. S.; Ni, Y.; Erdei, J.; Stange, H.; Schindler, R.; Hans-Joachim Lankau, H-J.; Grunwald, C.; Fan, K.; Parris, K.; Langen, B.; Egerland, U.; Hage, T.; Marquis, K.; Harrison, B.; Robichaud, A.; Kronbach, T.; Pangalos, M.; Brandon, N.; Hofgen, N. Highly Potent, Selective, and Orally Active Phosphodiestarase 10A Inhibitors. J. Med. Chem. 2011, 54, 7621-7638.
Malamas, M. S.; Erdei, J.; Gunawan, I.; Barnes, K.; Hui, Y.; Johnson, M.; Robichaud, A.; Zhou, P.; Yan, Y.; Solvibile, W.; Turner, J.; Fan, K.; Chopra, R.; Bard, J.; Pangalos, M. New Pyrazolyl and Thienyl Aminohydantoins as Potent BACE1 Inhibitors: Exploring the S2’ Region. Bioorg & Med. Chem. Lett. 2011, 21, 5164-5170.
Malamas, M. S.; Erdei, J.; Gunawan, I.; Turner, J.; Hu, Y.; Wagner, E.; Fan, K.; Chopra, R.; Olland, A.; Bard, J.; Jacobsen, S.; Magolda, R.; Pangalos, M.; Robichaud, A. J. Design and Synthesis of 5,5′-Disubstituted Aminohydantoins as Potent and Selective Human Beta-Secretase (BACE1) Inhibitors. J. Med. Chem. 2010, 53, 1146-1158.
Malamas, M. S.; Barnes, K.; Johnson, M.; Hui, Y.; Zhou, P.; Turner, J.; Hu, Y.; Wagner, E.; Fan, K.; Chopra, R.; Olland, A.; Bard, J.; Pangalos, M.; Reinhart, P.; Robichaud, A. J. Di- substituted Pyridinyl Aminohydantoins as Potent and Highly Selective Human Beta-Secretase (BACE1) Inhibitors. Bioorg. Med. Chem. 2010, 18, 630-639.
Malamas, M. S.; Barnes, K.; Hui, Y.; Johnson, M.; Lovering, F.; Condon, J.; Fobare, W.; Solvibile, W.; Turner, J.; Hu, Y.; Manas, E.; Fan, K.; Chopra, R.; Bard, J.; Pangalos, M.; Reinhart, P.; Robichaud, A. Novel Pyrrolyl 2-Aminopyridines as Potent and Selective Human Beta-Secretase (BACE1) Inhibitors. Bioorg & Med. Chem. Lett. 2010, 20, 2068-2073.
Malamas, M. S.; Robichaud, A.; Erdei, J.; Quagliato, D.; Solvibile, W.; Zhou, P.; Morris, K.; Turner, J.; Wagner, E.; Fan, F.; Jacobsen, S.; Reinhart, P.; Pangalos, M.; and Riddell, D. Design and Synthesis of Aminohydantoins as Potent and Selective Human Beta-Secretase (BACE1) Inhibitors with Enhanced Brain Permeability. Bioorg & Med. Chem. Lett. 2010, 20, 6597-6605.
Christaki, E.; Opal, S. M.; Keith, J. C.; Kessinian, N.; Palardy, J. E.; Parejo, N. A.; Lavallie, E.; Racie, L.; Mounts, W.; Malamas, M. S.; Mewshaw, R.; Harris, H.; Vlasuk, G. Estrogen Receptor Beta (ERbeta) Agonism Increases Survival in Experimentally Induced Sepsis And Ameliorates The Genomic Sepsis Signature: A Pharmacogenomic Study. J. Infect. Dis., 2010, 201, 1250-1257.
Höfgen, N.; Stange, H.; Schindler, R.; Grunwald, C.; Egerland, U.; Langen, B.; Pangalos, M.; Marquis, K.; Hage, T.; Harrison, H.; Malamas, M. S.; Brandon, N.; Kronbach, T. Discovery of Imidazo[1,5-a]pyrido[3,2-e]pyrazines as a New Class of PDE10A Inhibitors, J. Med. Chem. 2010, 53, 4399-4411.
Zhou, P.; Li, Y.; Fan, K.; Wang, Z.; Chopra, C.; Hu, Y.; Magolda, R.; Pangalos, M.; Reinhart, P.; Turner, J.; Bard, J.; Malamas, M. S.; Robichaud, A. Pyridinyl aminohydantoins as small molecule BACE1 inhibitors. Bioorg & Med. Chem. Lett. 2010, 20, 2326-2329.
Zhou, P; Malamas, M. S.; Robichaud, A. An efficient synthesis of 2-amino-4-(4-fluoro-3-(2- fluoropyridin-3-yl)phenyl)-4-(4-methoxy-3-methylphenyl)-1-methyl-1H-imidazol-5(4H)-one, a potent BACE1 inhibitor. ARKIVOC, 2010, 84-88.
Malamas, M. S.; Erdei, J.; Gunawan, I.; Barnes, K.; Johnson, M.; Hui, Y.; Turner, J.; Hu, Y.; Erik Wagner, E.: Kristi Fan, K.; Olland, A.; Bard, J.; Robichaud, A. Amino-imidazoles as Potent and Selective Human Beta-Secretase (BACE1) Inhibitors. J. Med. Chem. 2009, 52, 6314-6323.
Nowak, P.; Cole, D.; Aulabaugh, A.; Bard, J.; Chopra, R.; Cowling, R.; Fan, K.; Hu, B.; Jacobsen, S.; Jani, M.; Jin, G.; Lo, M-C.; Malamas, M. S.; Manas, E.; Narasimhan, R.; Reinhart, P.; Robichaud. A.; Stock, J.; Subrath, J.; Turner, J.; Wagner, E.; Zhou, P.; Ellingboe, J. Discovery and Initial Optimization of 5,5’-Disubstituted Aminohydantoins as Potent Beta-Secretase (BACE1) Inhibitors. Bioorg & Med. Chem. Lett. 2010, 20, 632-635.
Grauer, S.; Pulito, V.; Navarra, R.; Kelly, M.; Kelley, C.; Graf, R.; Langen, B.; Logue, S.; Brennan, J.; Jiang, L.; Charych, E.; Egerland, U.; Liu, F.; Marquis, K.; Malamas, M. S.; Hage, T.; Comery T.; Brandon. N. PDE10A Inhibitors Show Anti-Psychotic, Pro-cognitive and Negative Symptom Activities Suggesting Broad-Spectrum Utility for the Treatment of Schizophrenia. J. Pharm. Exp. Ther. 2009, 331, 574-590.
Hirst, W.; Kubek, K.; Bard, J.; Turner, J.; Fan, K.; Malamas, M.S.; Reinhart, P.; Robichaud, Investigation of the critical amino acids in the BACE1 binding site that interact with small molecule inhibitors using a novel radioligand and X-ray crystallography. Alzheimer’s and Dementia 2009, 5, 429-450.
Cole, D.; Stock, J.; Chopra, R.; Cowling, R.; Ellingboe, J.; Fan, K.; Harrison, B.; Hu, Y.; Jacobsen, S.; Jennings, L.; Jin, G.; Lohse, P.; Malamas, M. S.; Manas, E.; Moore, W.; O’Donnell, M.; Olland,A.; Robichaud, A.; Svenson, K.; Wu, J. Wagner, E.; Bard, J. Acylguanidine inhibitors of beta-secretase: Optimization of the Pyrrole Ring Substituents Extending into the S1and S3 Substrate Binding Pockets. Bioorg & Med. Chem. Lett. 2008, 18, 1063-1066.
Jennings, L.; Cole, D.; Stock, J.; Sukhdeo, M.; Ellingboe, J.; Cowling, R.; Jin, G.; Manas, E.; Fan, K.; Malamas, M. S.; Harrison, B.; Jacobsen, S.; Chopra, R.; Lohse, P.; Moore, W.; O’Donnell, M.: Hu, Y.; Robichaud, A.; Turner, J.; Wagner, E.; Jonathan Bard. Acylguanidine Inhibitors of beta-Secretase: Optimization of the Pyrrole Ring Substituents Extending into the S1’ Substrate Binding Pocket. Bioorg & Med. Chem. Lett. 2008, 18, 767-771.
Fobare, W.; Solvibile, W.; Robichaud, A.; Malamas, M. S.; Manas, E.; Turner, J.; Hu, Y.; Wagner, E.; Sun, J.; Chopra, R.; Cowling, R.; Jin, G.; Bard, J. Thiophene Substituted Acyl- Guanidines as BACE1 Inhibitors. Bioorg & Med. Chem. Lett. 2007, 17, 5353-5356
Malamas, M. S.; Manas, E. S.; Harris, H. A.; Mewshaw, R. Case History: The Design of Estrogen Receptor-beta Selective Compounds. Structure-Based Drug Discovery, RCS Publishing, 2006, 219-256.
Cole D.; Manas, E.; Stock, J; Condon, J.; Jennings, L.; Aulabaugh, A.; Chopra, R.;| Cowling, R.; Ellingboe, J. Fan, F.; Harrison, B.; Hu, Y.; Jacobsen, S.; Jin, G.; Lin, L.; Lovering, F.; Malamas, M. S.; Stahl, M.; Strand, J.; Sukhdeo, M.; Svenson, K.; Turner, J.; Wagner, E.; Wu, J.; Bard. J. Acylguanidines as Small-Molecule Beta-Secretase Inhibitors. J. Med. Chem. 2006, 49, 6158- 6161.
Malamas, M. S.; Keith, J. C., Jr.; Harris, H. A. 2-(3-Fluoro-4-hydroxyphenyl)-7-vinyl-1,3- benzoxazol-5-ol (ERbeta-041). Drugs of the Future 2005, 30, 333-336.
McDevitt, R. E.; Malamas, M. S.; Manas, E. S.; Unwalla, R.; I.; Xu, Z. B.; Miller, C. P.; Harris, H. A. Estrogen Receptor Ligands: Design and Synthesis of New Arylindene-1-enodes. Bioorg. Med. Chem. Lett. 2005, 15, 3137-3142.
Malamas, M. S.; Manas, E. S.; McDevitt, R. E.; Gunawan, I.; Xu, Z. B.; Collini, M. D.; Miller, C. P.; Dinh, T.; Henderson, R. A.; Keith, J. C., Jr.; Harris, H. A. Design and Synthesis of Aryl Diphenolic Azoles as Potent and Selective Estrogen Receptor-beta Ligands. J. Med. Chem. 2004, 47, 5021-5040.
Manas, E. S.; Unwalla, R. J.; Xu, Z. B.; Malamas, M. S.; Miller, C. P.; Harris, H. A.; Hsiao, C.; Akopian, T.; Hum, W.; Malakian, K.; Wolfrom, S.; Bapat, A.; Bhat, R. A.; Stahl, M. L.; Somers, W. S.; Alvarez, J. C. Structure-Based Design of Estrogen Receptor-beta Selective Ligands. J. Am. Chem. Soc. 2004, 126, 15106-15119
Lo, M.C.; Aulabaugh, A.; Cowling, R.; Bard, J.; Malamas, M. S.; Ellestad, G. Evaluation of Fluorescence-Based Thermal Shift Assays for Hit Identification in Drug Discovery. Analytical Biochemistry, 2004, 332, 153-159.
Harris, H. A.; Albert, L. M.; Leathurby, Y.; Malamas, M. S.; Mewshaw, R. E.; Miller, C. P.; Kharode, Y. P.; Marzolf, J.; Komm, B. S.; Winneker, R. C.; Frail, D. E.; Hederson, R. A.; Zhu, Y.; Keith, J. C. Evaluation of an Estrogen Receptor-beta Agonist in animal Models of Human Disease. Endocrinology, 2003, 144, 4241-4249.
Hu, B., Malamas, M. S.; Ellingboe, J.; Synthesis of Heterocycle Substituted 1-Aryl-4- Piperidones. Heterocycles 2002, 57, 857-870.
Malamas, M. S.; Sredy, J.; McCaleb, M.; Gunawan, I.; Mihan, B.; Sullivan, D. Antihyperglycemic Activity of New 1,2,4-Oxadiazolidine-3,5-diones. Eur. J. Med. Chem. 2001, 36, 31-42.
Hu, B., Ellingboe, J.; Han, S.; Largis, E.; Lim, K.; Malamas, M. S.; Mulvey, R.; Niu, C.; Oliphant, A.; Pelletier, J.; Singanallore, T.; Sum, F. W.; Tillett, J.; Wong, V. Novel (4-Piperidin- 1-yl)-phenyl Sulfonamides as Potent and Selective Human beta3 Agonists. Bioorg. Med. Chem. 2001, 9, 2045-2059.
Hu, B.; Ellingboe, J.; Gunawan, I.; Han, S.; Largis, E.; Li, Z.; Malamas, M. S.; Mulvey, R.; Oliphant A.; Sum, F. W.; Tillet, J.; Wong, V. 2,4-Thiazolidinediones as Potent and Selective Human beta3 Agonists. Bioorg. Med. Chem. Lett. 2001, 11, 757-760.
Hu, B.; Malamas, M. S.; Ellingboe, J.; Largis, E.; Han, S.; Mulvey, R.; Tillet, F. New Oxadiazolidinedione Derivatives as Potent and Selective Human beta3 Agonists. Bioorg. Med. Chem. Lett. 2001 11, 981-984.
Malamas, M. S.; Largis, E.; Gunawan, I.; Li, Z.; Tillett, J.; Stella Han, S.; Mulvey, R. Potent, Selective Aminothiazolidinediones Agonists of the Human beta3 Adrenergic Receptor. Med. Chem. Res. 2000, 10, 164-177.
Malamas, M. S.; Sredy, J.; Moxham, C.; Katz, A.; Xu, W.; McDevitt, R.; Adebayo, F. O.; Di Sawicki, D. R.; Seestaller, L.; Sullivan, D.; Taylor, J. R. Novel Benzofuran and Benzothiophene Biphenyls as Inhibitors of Protein Tyrosine Phosphatase 1B with Antihyperglycemic Properties. J. Med. Chem. 2000, 43, 1293-1310.
Malamas, M. S.; Sredy, J.; Gunawan, I.; Mihan, B.; Sawicki, R. D.; Seestaller, L.; Sullivan, D.; Flam, B. R. New Azolidinediones as Inhibitors of Protein Tyrosine Phosphatase 1B with Antihyperglycemic Properties. J. Med. Chem. 2000, 43, 995-1010.
Singh, S.; Malamas, M. S.; Hohman, T.; Nilakantan, R.; Carper, D.; Kitchen, D. Molecular Modeling of the Aldose Reductase-Inhibitor Complex Based on the X-ray Crystal Structure and Studies with Single-Site-Directed Mutants J. Med. Chem. 2000, 43, 1062-1070.
Sum, F. W.; Gilbert, A.; Venkatesan, A. M.; Lim, K.; Wong, V.; O’Dell, M.; Francisco, G.; Chen, Z.; Grosu, G.; Baker, J.; Ellingboe, J.; Malamas, M. S.; Gunawan, I.; Primeau, J.; Largis, E.; Steiner, K. Prodrugs of CL-316243: A Selective beta3-Adrenergic Receptor Agonist for Treating Obesity and Diabetes. Bioorg. Med. Chem. Lett. 1999, 9, 1921-1926.
Hohman, T.C.; Malamas, M. S.; Lai, K.; El-Kabbani, O.; Putilina, T.; McGowan, M. H.; Old, S. E.; Carper D. E. Probing the Inhibitor Binding Sites of Aldose Reductase with Site-Directed Mutagenesis. Eur. J. Biochemistry 1998, 256, 310-316.
Malamas, M. S.; Palka, C. L. New Synthesis of Isoxazolidines. J. Heterocyclic Chem. 1996, 33, 475-478.
Malamas, M. S.; Carlson, R. P.; Grimes, D.; Howell, R.; Glaser, K.; Gunawan, I.; Kanzelberger, M.; Nelson, J. A.; Shah, U.; Hartman, D. A. Azole-Phenoxy-Hydroxyureas as Selective, and Orally Active Inhibitors of 5-Lipoxygenase. J. Med. Chem. 1996, 39, 237-245.
Malamas, M. S.; Hohman, T. C. Novel Cycloalkenone Acetic and Oxy-Acetic Acids as Aldose Reductase Inhibitors. Med. Chem. Res. 1995, 5, 245-254.
Malamas, M. S.; Hohman, T. C; Millen, J. Novel spirosuccinimide aldose reductase inhibitors derived from isoquinoline-1,3-diones: 2-[(4-Bromo-2-fluorophenyl)methyl]-6-fluorospiro[isoquinoline-4(1H),3′-pyrrolidine]-1,2’3,5′(2H)-tetrone and congeners. J. Med. Chem. 1994, 37, 2043-2058.
Malamas, M. S.; Hohman, T. C. N-Substituted Spirosuccinimide, Spiropyridazine, Spiroazetidine, and Acetic Acid Aldose Reductase Inhibitors Derived from Isoquinoline-1,3- diones. J. Med. Chem. 1994, 37, 2059-2070.
Malamas, M. S.; Hohman, T. C. ARI-509: 2-[(4-Bromo-2-fluorophenyl)methyl]-6- fluorospiro[isoquinoline-4(1H),3′-pyrrolidine]-1,2’3,5′(2H)-tetrone. Drugs of the Future, 1994, 19(5), 442-445.
Malamas, M. S. Facile Synthesis of Novel Spiro[azetidine-2,4′(1’h)-isoquinoline]-1′,3′,4(2’h)- triones. J. Heterocyclic Chem. 1994, 31, 565-568.
Malamas, M. S.; Hohman, T. C. Characterization of a Structurally Novel Highly Potent, Orally Active Aldose Reductase Inhibitor. Diabetologia 1992, 35, A-49.
Malamas, M. S.; Millen, J. Quinazolineacetic Acids and Related Analogues as Aldose Reductase Inhibitors. J. Med. Chem. 1991, 34, 1492-1503.
Malamas, M. S.; Sestanj, K.; Millen, J. Naphthalenylsulfonyl-hydantoins as Aldose Reductase Inhibitors. Eur. J. Med. Chem. 1991, 26, 369.
Malamas, M. S.; Sestanj, K.; Millen, J. Synthesis and Biological Evaluation of Tolrestat Metabolites. Eur. J. Med. Chem. 1991, 26, 197-200. Wrobel, J.; Millen, J.; Detroit, A.; Gorham, B. J.; Malamas, M. S.; Kelly, J. M. ;Bauman, J. G.; Harrison, M. C.; Jones, L. R.; Guinosso, C.; Sestanj, K. Syntheses of Tolrestat Analogues Containing Additional Substituents in The Ring and Their Evaluation as Aldose Reductase Inhibitors: Identification of Potent, Orally Active 2-Fluoro Derivatives. J. Med. Chem. 1991, 34, 2504-2520
Patents
Malamas M. S.; Dolle R.; Tan, D.; Kulkarni M. BAX activators and use thereof U.S. Patent Application No.: 63/504,547, 2023.
Malamas M. S.; Dolle R.; Tan, D.; Kulkarni M. BAX activators and use thereof U.S. Patent Application No.: 63/504,487, 2023.
Malamas M. S.; Makriyannis, A.; Subramanian, K.; Whitten, K.; Zvonok, N.; West, J.; McCormack, M.; Pavlopoulos, S. N-acylethanolamine hydrolyzing acid amidase (NAAA) inhibitors and use thereof. US Patent 10,640,494 B2, 2020
Malamas M. S.; Makriyannis, A.; Farah, S.; Zvonok, A.; Alapafuja, S. N-acylethanolamine hydrolyzing acid amidase (NAAA) inhibitors and use thereof. US Patent 10,689,357 B2, 2020
Malamas M. S.; Makriyannis, A.; Lamani, M.; Farah, S. ABHD6 and ABHD6/MGL inhibitors and their uses. US Patent 0152917, 2019
Malamas M. S. et.al. N-Acylethanolamine hydrolyzing acid amidase inhibitors and their use thereof. US Patent 9,963,444, 2018
Malamas, M. S.; Robichaud, A.; Porte, A.; Koi, M.; Solvibile, W.; Kim, J.; Schuyler, A. Amino- 5-[4-(difluoromethoxy)-phenyl]-5-phenylimidazolone compounds for the inhibition of beta- secretase. U.S. Patent 7723368, 2010.
Malamas, M. S.; Fobare, W.; Solvibile, W.; Lovering, F.; Condon, J.; Robichaud, A. Amino- pyridines as inhibitors of beta-secretase. U.S. Patent 7732457, 2010
Malamas, M. S.; Erdei, J.; Gunawan, I.; Nowak, P.; Harrison, B. Diphenylimidazopyrimidines inhibition of beta-secretase. U.S. Patent 7563796, 2009.
Malamas, M. S.; McDevvit R.; Gunawan, I.; Manas, E.; Harris, H.; Keith, J.; Lyttle, R. Substituted Benzoxazoles as Estrogenic Agents. U.S. Patent 7531564, 2009
Malamas, M. S.; Erdei, J.; Gunawan, I.; Barnes, K.; Johnson, M.; Hu, Y. Diphenylimidazopyrimidine and imidazole amines as inhibitors of beta-secretase. U.S. Patent 7482349, 2009.
Malamas, M. S.; Erdei, J.; Ni, Y.; Hoefgen, N.; Thorsten, H.; Egerland, U.; Langen, B. Pyrido[3,2-e]pyrazines, process for preparing the same, and their use as inhibitors of phosphodiesterase 10. U.S. Patent 0143661, 2009.
Malamas, M. S.; Erdei, J.; Ni, Y.; Hoefgen, N.; Thorsten, H.; Egerland, U.; Langen, B. Aryl and heteroaryl fused imidazo[1,5-a]pyrazines as inhibitors of phosphodiesterase 10, U.S. Patent 0143367, 2009.
Malamas, M. S.; Barnes, K.; Johnson, M.. Imidazole amines as inhibitors of beta-secretase. U.S. Patent 0051390, 2008.
Malamas, M. S.; Erdei, J.; Gunawan, I.; Barnes, K.; Johnson, M.; Hu, Y. Diphenylimidazopyrimidine and imidazole amines as inhibitors of beta-secretase. U.S. Patent 7456186, 2008.
Malamas, M. S.; Robichaud, A.; Porte, A.; Koi, M,; Solvibile, W.; Kim, J.; McDevitt, R. Preparation of amino-5-[4-(difluoromethoxy)phenyl-5-phenylimidazolone compounds as inhibitors of beta-secretase and their preparation, and use in the treatment of b-amyloid deposits and neurofibrillary tangles. WO 115552, 2008.
Malamas, M. S.; Robichaud, A.; Porte, A.; Solvibile, W.; Koi, M.; Schuyler A.; Kim, J. Preparation of amino-5-[4-(difluoromethoxy)phenyl-5-phenylimidazolone derivatives as inhibitors of beta-secretase. WO 118379, 2008.
Malamas, M. S.; Zhou, P.; Yan, Y.; Quagliato, D.; Robichaud, A. Amino-5-(6- membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation. U.S. Patent 7452885, 2008.
Malamas, M. S.; Erdei, J.; Fobare, W.; Quagliato, D.; Antane, S.; Robichaud, A. Amino-5-[4- (difluoromethoxy)-phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase. U.S. Patent 7423158, 2008.
Malamas, M. S., Elokhad, H. Substituted oxadiazolidinediones. U.S. Patent, 7351726, 2008.
Malamas, M. S.; Zhou, P.; Yan, Y.; Quagliato, D.; Robichaud, A. Amino-5-(6- membered) heteroarylimidazolone compounds and the use thereof for beta-secretase modulation. U.S. Patent 7417047, 2008.
Yan Y.; Ping, Z.; Fan, Y.; Robichaud, A.; Malamas, M. S. Preparation of indolylalkylpyridin-2- amines for the inhibition of beta-secretase. WO 036196, (2008)
Malamas, M. S.; Barnes, K.; Johnson, M. Imidazole amines as inhibitors of beta-secretase and their preparation, pharmaceutical compositions and use in the treatment of diseases associated with elevated beta-amyloid deposits. WO 022024, 2008.
Malamas, M. S.; Zhou, P.; Fobare, W.; Solvibile, W.; Erdei, J.; Gunawan, I.; Yan, Y.; Quagliato, D.; Andrae, P. Amino-5-(5-membered) heteroarylimidazolone compounds and the use thereof for beta-secretase modulation. U.S. Patent 0004786, 2007.
Malamas, M. S.; Erdei, J.; Gunawan, I.; Nowak, P.; Stock, J.; Yan, Y. Cycloalkyl amino- hydantoin compounds and the use thereof for beta-secretase modulation. U.S. Patent. 0027199, 2007.
Malamas, M. S.; Erdei, J.; Fobare, W.; Quagliato, D.; Schuyler, A.; Robichaud, A. Preparation of imidazolone derivatives as inhibitors of beta-secretase. U.S. Patent. 0072925, 2007.
Ping, Z.; Malamas, M. S.; Yanfang, L.; Robichaud, A.; Quagliato, D.; Preparation of aminoheteroarylimidazole compounds for use as beta-secretase modulators to treat beta-amyloid and neurofibrillary tangle associated diseases. U.S. Patent 0044730, 2007.
Malamas, M. S.; Fobare, W.; Solvibile, W.; Lovering, F.; Condon, J.; Robichaud, A. Amino-pyridines as inhibitors of beta-secretase. U.S. Patent 173049, 2006.
Malamas, M. S.; Erdei, J.; Gunawan, I.; Nowak, P.; Harrison, B. Preparation of 8,8-diphenyl- 2,3,4,8-tetrahydroimidazo[1,5-a]-pyrimidin-6-amines as beta-secretase inhibitors for the treatment of Alzheimer’s disease and related disorders. WO 076284, 2006.
Malamas, M. S.; Gunawan, I.; Manas, E. Substituted Benzoxazoles as Estrogenic Agents. U.S. Patent 7148247, 2006.
Malamas, M. S. Preparation of Oxazole-Aryl-Carboxylic Acids Useful in the Treatment of Insulin Resistance and Hyperglycemia. U.S. Patent 7141672, 2006.
Malamas, M. S.; Gunawan, I.; Manas, E. Substituted Benzoxazoles as Estrogenic Agents. U.S. Patent 7129258, 2006.
Sum, F. W.; Hu, B.; Malamas, M. S. Cyclic Amine Phenyl Beta Adrenergic Receptor Agonists. U.S. Patent 7022716, 2006
Malamas, M. S.; Erdei, J.; Gunawan, I.; Zhou, P.; Yan, Y.; Quagliato, D. Preparation of amino- 5,5-diphenylimidazolone derivatives for the inhibition of beta-secretase and treatment of amyloid diseases U.S. Patent 282825, 2005.
Malamas, M. S.; Erdei, J.; Gunawan, I.; Barnes, K.; Johnson, M.; Hu, Y. Diphenylimidazopyrimidine and imidazole amines as inhibitors of beta-secretase. U.S. Patent. 0282826, 2005.
Malamas, M. S.; Gunawan, I.; Harris, H. A.; Keith, J. C.; Albert. M. L. Naphthyl Benzoxazoles and Benzisoxazoles as Estrogenic Agents. U.S. Patent 6960607, 2005
Malamas, M. S.; Dinh, T. Q.; Gunawan, I.; Collini, M. D.; Harris, H. A.; Keith, J. C.; Albert. M. L. Phenyl Benzisoxazoles as Estrogenic Agents. U.S. Patent 6884814, 2005
Malamas, M. S.; Wrobel, J. E.; Dietrich A.; Li, Z.; Gunawan, I. Phenyl Oxo-Acetic Acids Useful in the Treatment of Insulin Resistance and Hyperglycemia. U.S. Patent, 6844358, 2005.
Hassan, E.; Malamas, M. S. Preparation of 2-[3-(benzofuranyl) pent-2-enyl]oxadiazolidine-3,5- diones as PAI-1 inhibitors for the treatment of disorders related to fibrinolytic system impairment. U.S. Patent, 070585, 2005.
Malamas, M. S.; Gunawan, I.; Manas, E. Substituted Benzoxazoles as Estrogenic Agents. U.S. Patent 6794403, 2004
Hu, B.; Malamas, M. S.; Sum, F. N-(4-Sulfonylaryl)cyclylamine-2-hydroxyethylamines as Beta-3 Adrenergic Receptor Agonists. U.S. Patent 6743787, 2004
Malamas, M. S. Preparation of Oxazole-Aryl-Carboxylic Acids Useful in the Treatment of Insulin Resistance and Hyperglycemia. U.S. Patent 6699896, 2004
Malamas, M. S.; Largis, E. E.; Gunawan, I.; Li, Z. Azolidines as beta3 Adrenergic Receptor Agonists. U.S. Patent 6569873, 2003
Sum, F. W.; Hu, B.; Malamas, M. S. Cyclic Amine Phenyl Beta Adrenergic Receptor Agonists. U.S. Patent 6525202, 2003
Malamas, M. S.; Wrobel, J. E.; Dietrich A.; Li, Z.; Gunawan, I. Phenyl Oxo-Acetic Acids Useful in the Treatment of Insulin Resistance and Hyperglycemia. U.S. Patent, 6509360, 2003.
Malamas, M. S.; McDevitt, R.; Robert, E.; Gunawan, I.; Manas, E.; Collini, M.; Heather, H.; Keith, J.; Albert, L.; Lyttle, R. Preparation of Benzoxazoles and Analogues as Estrogenic Agents. WO 050095, 2003.
Hu, B.; Malamas, M. S.; Sum, F. New Cyclic Amine Compounds Are Beta-3 Adrenergic Agonists Used for Treating Atherosclerosis, Glaucoma, Urinary Incontinence and Type-II Diabetes. WO 06232, 2002.
Hu, B.; Malamas, M. S.; Sum, F New N-(4-Sulfonylaryl)cyclylamine-2-hydroxyethylamines Are Selective Beta-3 Adrenergic Receptor Agonists Used for Treating Type-II Diabetes, Obesity, Incontinence, Metabolic Disorders, Atherosclerosis and Glaucoma. WO 06274, 2002.
Malamas, M. S.; Largis, E. E.; Gunawan, I.; Li, Z. Azolidines as beta3 Adrenergic Agonists. U.S. Patent 6465501, 2002.
Sum, F. W.; Hu, B.; Malamas, M. S. New N-(4-Sulfonylaryl) cyclylamine Substituted 2- Hydroxyethylamines As beta3 Adrenergic Receptor Agonists. U.S. Patent 6444685, 2002.
Malamas, M. S.; McDevitt, R.; Adebayo, F. Biphenyl Oxo-acetic Acids Useful in the Treatment of Insulin Resistance and Hyperglycemia U.S. Patent 6369072, 2002.
Malamas, M. S.; McDevitt, R.; Adebayo, F. Biphenyl Oxo-acetic Acids Useful in the Treatment of Insulin Resistance and Hyperglycemia U.S. Patent 6391897, 2002.
Malamas, M. S.; Largis, E. E.; Gunawan, I.; Li, Z. Preparation of Arylaminothizolidines and Analogs as beta3 Adrenergic Receptor Agonists. WO 006258, 2002.
Sum, F.; Malamas, M. S.; Preparation of [(2-hydroxyethylamino)-cycloamino]arylsulfonamides as 3-Adrenergic Receptor Agonits. WO 006274, 2002.
Malamas, M. S.; Adebayo, F.; Dollings, P. Biphenyl Sulfonyl Aryl Carboxylic Acids Useful in the Treatment of Insulin Resistance and Hyperglycemia. U.S. Patent 6310081, 2001
Malamas, M. S.; McDevitt, R.; Adebayo, F. Biphenyl Oxo-acetic Acids Useful in the Treatment of Insulin Resistance and Hyperglycemia U.S. Patent 6232322, 2001
Malamas, M. S.; Adebayo, F.; Dollings, P. Biphenyl Sulfonyl Aryl Carboxylic Acids Useful in the Treatment of Insulin Resistance and Hyperglycemia. U.S. Patent 6221902, 2001.
Malamas, M. S.; Gunawan, I. Amino-thiazolidinediones Useful in the Treatment of Insulin Resistance and Hyperglycemia. U.S. Patent 6214842, 2001.
Malamas, M. S.; Wrobel, J. E.; Dietrich A.; Li, Z.; Gunawan, I. Preparation of Phenyl Oxo- Acetic Acids Useful in the Treatment of Insulin Resistance and Hyperglycemia. U.S. Patent, 6166069, 2000.
Malamas, M. S. Aryl-Oxo-Acetic Acids Useful in the Treatment of Insulin Resistance and Hyperglycemia. U.S. Patent, 6110963, 2000.
Gilbert., A. M.; Grosu, G. T.; Malamas, M. S.; Sum, F.; Venkatesan, A. M.; Francisco, G. D. Preparation and Antidiabetic, Antihyperglycemia, and Antiobesity Activity of Substituted 1,3- Benzodioxoles. U.S. Patent, 5914339, 1999.
Malamas, M. S.; Adebayo, F.; Dollings, P. Preparation of Biphenylfuryl-biphenyloxy- sulfonylbenzoates and Related Compounds Useful in the Treatment of Insulin Resistance and Heperglycemia. WO 9958520, 1999.
Malamas, M. S.; McDevitt, R.; Adebayo, F. Preparation of beta-(Biphenyloxo)-alkanoic Acids for the Treatment of Insulin Resistance and Hyperglycemia WO 9958518, 1999.
Malamas, M. S. Preparation of Oxazole-Aryl-Carboxylic Acids Useful in the Treatment of Insulin Resistance and Hyperglycemia. WO 9958511, 1999.
Malamas, M. S.; Wrobel, J. E.; Dietrich A.; Li, Z.; Gunawan, I. Preparation of Phenyl Oxo- Acetic Acids Useful in the Treatment of Insulin Resistance and Hyperglycemia. WO 9958519, 1999.
Malamas, M. S.; Grosu, G. T.; Malamas, M. S.; Sum, F.; Venkatesan, A. M.; Francisco, G. D. Substituted 1,3-Benzodioxoles. European Patent 97924720, 1999.
Malamas, M. S.; Gunawan, I. Phenoxy Acetic Acids as Aldose Reductase Inhibitors and Antihyperglycemic Agents. European. Patent 96926208, 1998.
Malamas, M. S.; Gunawan, I. Preparation of 4-Formyl-2-(Naphthalenylmethyl)phenoxyacetic Acids as Aldose Reductase Inhibitors and Antihyperglycemic Agents. U.S. Patent 5677342, 1997.
Malamas, M. S. Benzyl and Naphthalenylmethyl Thiophenones, Cyclopentenones as Antihyperglycemic Agents. U.S. Patent 5610197, 1997.
Gilbert., A. M.; Grosu, G. T.; Malamas, M. S.; Sum, F.; Venkatesan, A. M.; Francisco, G. D. Preparation of 1,3-benzodioxole-2,2-dicarboxylates as beta3-Adrenoceptor Agonists. WO 9743273, 1997.
Malamas, M. S.; Gunawan, I. Preparation of 4-Formyl-2-(naphthalenylmethyl)phenoxyacetic Acids as Aldose Reductase Inhibitors and Antihyperglycemic Agents. WO 9708126, 1997.
Gilbert, A. M.; Grosu, G. T.; Malamas, M. S.; Sum, F.; Venkatesan, A. M.; Francisco, G. D. New Benzodioxole-2,2-dicarboxylic Acid Ester and Amide Derivatives Used as Selective Beta-3 Adrenergic Receptor Agonists for Treating Hyperglycemia, Diabetes and Obesity. WO 9743273, 1997.
Malamas, M. S.; Gunawan, I. Aryl-N-hydroxyureas as Inhibitors of 5-Lipoxygenase and Anti- Arteriosclerotic Agents. U.S. Patent 5541205, 1996.
Malamas, M. S.; Gunawan, I. New Azolidinediones and Thiadiazolidinediones as Antihyperglycemic Agents. U.S. Patent 5532256, 1996.
Malamas, M. S.; Gunawan, I. Azolidinediones as Antihyperglycemic Agents. U.S. Patent 5510360, 1996.
Malamas, M. S.; Nelson, J. N-Hydroxyureas as 5-Lipoxygenase Inhibitors and Inhibitors of Oxidative Modification of Low Density Lipoprotein. U.S. Patent 5504097, 1996.
Malamas, M. S. 2-(3,5-Di-tert-butyl-4-hydroxy-phenyl)-Oxazoles as Anti-Atherosclerotic Agents. U.S. Patent 5491159, 1996.
Malamas, M. S. Naphthalenylmethyl Cycloalkenone Acetic Acids and Analogues Thereof, Useful as Aldose Reductase Inhibitors. U.S. Patent 5482968, 1996.
Malamas, M. S.; Palka, C. L.; Gunawan, I. Aralkyl-1,2,4-oxazolidine-3,5-diones as Antihyperglycemic Agents. U.S. Patent 5480896, 1996.
Malamas, M. S.; Nelson, J. Aralkyl-N-Hydroxyureas as Inhibitors of 5-Lipoxygenase and Oxidation of Low-Density Lipoprotein. U.S. Patent 5468760, 1995.
Malamas, M. S.; Gunawan, I. New Azolidinediones as Antihyperglycemic Agents. U.S. Patent 5468762, 1995.
Malamas, M. S.; Nelson, J. N-Hydroxyureas as 5-Lipoxygenase Inhibitors and Inhibitors of Oxidative Modification of Low-Density Lipoprotein. U.S. Patent 5459154, 1995.
Malamas, M. S. Benzyl and Naphthalenylmethyl, Thiophenones, Cyclopentenones as Antihyperglycemic Agents. U.S. Patent 5444086, 1995.
Malamas, M. S.; Gunawan, I. Aryl-N-Hydroxyureas as Inhibitors of 5-Lipoxygenase and Anti- Arteriosclerotic Agents. U.S. Patent 5428048, 1995.
Malamas, M. S.; Palka, C. L.; Gunawan, I. Di-Oxadiazolidines as Antihyperglycemic Agents. U.S. Patent 5420146, 1995.
Malamas, M. S. Naphthalenylmethyl Cycloalkenone Acetic Acids and Analogues Thereof, Useful as Aldose Reductase Inhibitors. U.S. Patent 5399588, 1995.
Malamas, M. S. 1′-Amino-2-[(benzothiazolyl)methyl]spiro[isoquinoline-4(1H),3′-pyrrolidine]- 1,2′,3,5′(2H)-tetrones and Analogues Thereof Useful as Aldose Reductase Inhibitors. U.S. Patent 5189168, 1993.
Malamas, M. S. Alkylidene Analogues of 1′-Amino-2-[(benzothiazolyl)-methyl]- spiro[isoquinoline-4(1H),3′-pyrrolidine]-1,2′,3,5′(2H)-tetrones Useful as Aldose Reductase Inhibitors. U.S. Patent 5189167, 1993.
Malamas, M. S. Isoquinoline-1,3-dione Acetyl Carbamates Useful as Aldose Reductase Inhibitors. U.S. Patent 5189044, 1993
Malamas, M. S. Spiro[isoquinoline-pyrrolidine]tetrones. Eur. Patent 519600, 1992.
Malamas, M. S. Spiro-Pyridazines and Analogues Thereof Useful as Aldose Reductase Inhibitors. U.S. Patent 5081241, 1992.
Malamas, M. S. Spiro-Isoquinoline-Pyrrolidines and Analogues Thereof, as Aldose Reductase Inhibitors. U.S. Patent 5093496, 1992.
Malamas, M. S. Spiro-Lactams and Analogues Thereof Useful as Aldose Reductase Inhibitors. U.S. Patent 5130425, 1992.
Malamas, M. S. Process and Intermediates for the Preparation of Spiro[isoquinoline-4(1H),3′- pyrrolidine]-1,2′,3,5′(2H)-tetrones Which Are Useful as Aldose Reductase Inhibitors. U.S. Patent 5169948, 1992.
Malamas, M. S. Process and Intermediates for the Preparation of Spiro[isoquinoline-4(1H),3′- pyrrolidine]-1,2′,3,5′(2H)-tetrones Which Are Useful as Aldose Reductase Inhibitors. U.S. Patent 5106978, 1992.
Malamas, M. S. 1′-Aminospiro[isoquinoline-4(1H),3′-pyrrolidine]-1,2′,3,5′(2H)-tetrones and Analogues Thereof Useful as Aldose Reductase Inhibitors. U.S. Patent 5102886, 1992.
Malamas, M. S. New 1-Amino Spiro-Isoquinoline Pyrrolidine Tetrone Analogues Are Aldose Reductase Inhibitors Used To Treat Or Prevent Diabetes Mellitus Associated Complications. WO 9206974, 1992.
Malamas, M. S.; Ferdinandi, E.S.; Sestanj, K.; Sehgal, S.N. N-[[6-Methoxy-5-(trifluoromethyl)- 1-naphthalenyl]-thioxomethyl]-N-methylglycine S-oxide and The Amide Thereof. U.S. Patent 4994381, 1991.
Malamas, M. S. Isoquinoline Acetic Acids and Acetyl Carbamates Useful as Aldose Reductase Inhibitors. U.S. Patent 4983613, 1991.
Malamas, M. S. Spiro-Isoquinoline-Pyrrolidines and Analogues Thereof Useful as Aldose Reductase Inhibitors. U.S. Patent 5037831, 1991.
Malamas, M. S. N’-Alkyl-Spiro-Isoquinoline-Pyrrolidine Tetrones and Analogues as Aldose Reductase Inhibitors. U.S. Patent 5045544, 1991.
Malamas, M. S. Alkylidene Analogues of 1′-Aminospiro[isoquinoline-4(1H),3′-pyrrolidine]- 1,2′,3,5′(2H)-tetrones Useful as Aldose Reductase Inhibitors. U.S. Patent 5068332, 1991.
Malamas, M. S. Spiro-Isoquinoline-Pyrrolidine Tetrones and Analogues Thereof, Useful as Aldose Reductase Inhibitors. U.S. Patent 4927831, 1990.
Malamas, M. S. Preparation of Spiro-Isoquinoline-Pyrrolidine Tetrones and Analogs as Aldose Reductase Inhibitors. Eur. Patent 365324, 1990.
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