Search Results - "Hudkins, Robert L."

Discovery and Characterization of 6-{4-[3-(R)-2-Methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, Irdabisant): A Potent, Selective Histamine H3 Receptor Inverse Agonist by Hudkins, Robert L, Raddatz, Rita, Tao, Ming, Mathiasen, Joanne R, Aimone, Lisa D, Becknell, Nadine C, Prouty, Catherine P, Knutsen, Lars J. S, Yazdanian, Mehran, Moachon, Gilbert, Ator, Mark A, Mallamo, John P, Marino, Michael J, Bacon, Edward R, Williams, Michael

“…Optimization of a novel series of pyridazin-3-one histamine H3 receptor (H3R) antagonists/inverse agonists identified…”
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Recent advances in targeting the fatty acid biosynthetic pathway using fatty acid synthase inhibitors by Angeles, Thelma S, Hudkins, Robert L

“…Elevated lipogenesis has been associated with a variety of diseases including obesity, cancer and nonalcoholic fatty liver disease (NAFLD). Fatty acid synthase…”
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Anaplastic lymphoma kinase activity is essential for the proliferation and survival of anaplastic large-cell lymphoma cells by Wan, Weihua, Albom, Mark S., Lu, Lihui, Quail, Matthew R., Becknell, Nadine C., Weinberg, Linda R., Reddy, Dandu R., Holskin, Beverly P., Angeles, Thelma S., Underiner, Ted L., Meyer, Sheryl L., Hudkins, Robert L., Dorsey, Bruce D., Ator, Mark A., Ruggeri, Bruce A., Cheng, Mangeng

“…The roles of aberrant expression of constitutively active ALK chimeric proteins in the pathogenesis of anaplastic large-cell lymphoma (ALCL) have been well…”
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Synthesis and Mixed Lineage Kinase Activity of Pyrrolocarbazole and Isoindolone Analogs of (+)K-252a by Hudkins, Robert L, Johnson, Neil W, Angeles, Thelma S, Gessner, George W, Mallamo, John P

“…Structural modification of the indolecarbazole natural product (+)K-252a identified structural requirements for MLK activity and a novel series of potent fused…”
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Discovery of TYRA-300: First Oral Selective FGFR3 Inhibitor for the Treatment of Urothelial Cancers and Achondroplasia by Hudkins, Robert L., Allen, Eric, Balcer, Alexandra, Hoffman, Isaac D., Iyer, Samhita, Neal, Melissa, Nelson, Kirk J., Rideout, Marc, Ye, Qing, Starrett, Jacqueline H., Patel, Piyush, Harris, Todd, Swanson, Ronald V., Bensen, Daniel C.

“…Activating FGFR3 alterations have been identified in up to 15–20% of muscle-invasive bladder cancer and metastatic urothelial carcinoma (mUC), and as high as…”
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A Facile and Efficient Synthesis of 3-Amino-5-bromopyridine Derivatives Using Microwave Irradiation by reddy Dandu, Reddeppa, C. Rose, Adam, L. Hudkins, Robert

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Technically Extended MultiParameter Optimization (TEMPO): An Advanced Robust Scoring Scheme To Calculate Central Nervous System Druggability and Monitor Lead Optimization by Ghose, Arup K, Ott, Gregory R, Hudkins, Robert L

“…At the discovery stage, it is important to understand the drug design concepts for a CNS drug compared to those for a non-CNS drug. Previously, we published on…”
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Neurotrophic 3,9-Bis[(alkylthio)methyl]- and -Bis(alkoxymethyl)-K-252a Derivatives by Kaneko, Masami, Saito, Yutaka, Saito, Hiromitsu, Matsumoto, Tadashi, Matsuda, Yuzuru, Vaught, Jeffry L, Dionne, Craig A, Angeles, Thelma S, Glicksman, Marcie A, Neff, Nicola T, Rotella, David P, Kauer, James C, Mallamo, John P, Hudkins, Robert L, Murakata, Chikara

“…A series of 3,9-disubstituted [(alkylthio)methyl]- and (alkoxymethyl)-K-252a derivatives was synthesized with the aim of enhancing and separating the…”
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Synthesis and Biological Profile of the pan-Vascular Endothelial Growth Factor Receptor/Tyrosine Kinase with Immunoglobulin and Epidermal Growth Factor-Like Homology Domains 2 (VEGF-R/TIE-2) Inhibitor 11-(2-Methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): A Novel Oncology Therapeutic Agent by Hudkins, Robert L, Becknell, Nadine C, Zulli, Allison L, Underiner, Ted L, Angeles, Thelma S, Aimone, Lisa D, Albom, Mark S, Chang, Hong, Miknyoczki, Sheila J, Hunter, Kathryn, Jones-Bolin, Susan, Zhao, Hugh, Bacon, Edward R, Mallamo, John P, Ator, Mark A, Ruggeri, Bruce A

“…A substantial body of evidence supports the utility of antiangiogenesis inhibitors as a strategy to block or attenuate tumor-induced angiogenesis and…”
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Knowledge-Based, Central Nervous System (CNS) Lead Selection and Lead Optimization for CNS Drug Discovery by Ghose, Arup K, Herbertz, Torsten, Hudkins, Robert L, Dorsey, Bruce D, Mallamo, John P

“…The central nervous system (CNS) is the major area that is affected by aging. Alzheimer’s disease (AD), Parkinson’s disease (PD), brain cancer, and stroke are…”
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3-(1′-Cyclobutylspiro[4H-1,3-benzodioxine-2,4′-piperidine]-6-yl)-5,5-dimethyl-1,4-dihydropyridazin-6-one (CEP-32215), a new wake-promoting histamine H3 antagonist/inverse agonist by Hudkins, Robert L., Gruner, John A., Raddatz, Rita, Mathiasen, Joanne R., Aimone, Lisa D., Marino, Michael J., Bacon, Edward R., Williams, Michael, Ator, Mark A.

“…CEP-32215 is a new, potent, selective, and orally bioavailable inverse agonist of the histamine H3 receptor (H3R) with drug-like properties. High affinity in…”
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Current approaches for the treatment of cognitive deficits in CNS disease by Hudkins, Robert L

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3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity by Hudkins, Robert L., Becknell, Nadine C., Lyons, Jacquelyn A., Aimone, Lisa D., Olsen, Mark, Haltiwanger, R. Curtis, Mathiasen, Joanne R., Raddatz, Rita, Gruner, John A.

“…A novel series of 3,4-diaza-bicyclo[4.1.0]hept-4-en-2-ones were designed and synthesized as H3R analogs of irdabisant 6. Separation of the isomers, assignment…”
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Development and Scale-Up of an Optimized Route to the Pyridazin-3-one Histamine H3 Receptor Antagonist CEP-32215 by Wang, Yi, Przyuski, Katrin, Roemmele, Renee C, Hudkins, Robert L, Bakale, Roger P

“…The evolution of the process to prepare CEP-32215, 3-(1′-cyclobutylspiro[4H-1,3-benzodioxine-2,4′-piperidine]-6-yl)-5,5-dimethyl-1,4-dihydropyridazine-6-one,…”
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Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): Histamine H3 receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity by Hudkins, Robert L., Josef, Kurt A., Becknell, Nadine C., Aimone, Lisa D., Lyons, Jacquelyn A., Mathiasen, Joanne R., Gruner, John A., Raddatz, Rita

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Synthesis of constrained benzocinnolinone analogues of CEP-26401 (irdabisant) as potent, selective histamine H3 receptor inverse agonists by Josef, Kurt A., Aimone, Lisa D., Lyons, Jacquelyn, Raddatz, Rita, Hudkins, Robert L.

“…A novel class of benzocinnolinones analogs of irdabisant were designed and synthesized as histamine H3R antagonists/inverse agonists. Modifications to the…”
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Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists by Zulli, Allison L., Aimone, Lisa D., Mathiasen, Joanne R., Gruner, John A., Raddatz, Rita, Bacon, Edward R., Hudkins, Robert L.

“…Optimization of a series of aminomethyl ketone diamine H3R antagonists to reduce the brain exposure by lowering the pKa, led to molecules with improved…”
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Synthesis and evaluation of 4-alkoxy-[1′-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4′-piperidine)] analogues as histamine-3 receptor antagonists by Becknell, Nadine C., Dandu, Reddeppa Reddy, Lyons, Jacquelyn A., Aimone, Lisa D., Raddatz, Rita, Hudkins, Robert L.

“…A novel class of 4-alkoxy-[1′-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4′-piperidine)] analogues were designed and synthesized as H3R antagonists…”
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Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists by Becknell, Nadine C., Lyons, Jacquelyn A., Aimone, Lisa D., Huang, Zeqi, Gruner, John A., Raddatz, Rita, Hudkins, Robert L.

“…A novel series of 4-pyridazin-3-one and 5-pyridazin-3-one analogues were designed and synthesized as H3R antagonists. Structure–activity relationship revealed…”
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Synthesis and evaluation of a new series of 1′-cyclobutyl-6-(4-piperidyloxy)spiro[benzopyran-2,4′-piperidine] derivatives as high affinity and selective histamine-3 receptor (H3R) antagonists by Dandu, Reddeppa Reddy, Lyons, Jacquelyn A., Raddatz, Rita, Huang, Zeqi, Aimone, Lisa D., Hudkins, Robert L.

“…A novel class of 1′-cyclobutyl-6-(4-piperidyloxy)spiro[benzopyran-2,4′-piperidine] derivatives with low nanomolar affinity for the human and rat histamine-3…”
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