Search Results - "Hartz, Richard A."

Preclinical Profile of the HIV-1 Maturation Inhibitor VH3739937 by McAuliffe, Brian, Falk, Paul, Chen, Jie, Chen, Yan, Sit, Sing-Yuen, Swidorski, Jacob, Hartz, Richard A, Xu, Li, Venables, Brian, Sin, Ny, Meanwell, Nicholas A, Regueiro-Ren, Alicia, Wensel, David, Hanumegowda, Umesh, Krystal, Mark

“…The HIV-1 maturation inhibitor (MI) VH3739937 (VH-937) inhibits cleavage between capsid and spacer peptide 1 and exhibits an oral half-life in humans…”
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Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88 by Dzierba, Carolyn D., Bi, Yingzhi, Dasgupta, Bireshwar, Hartz, Richard A., Ahuja, Vijay, Cianchetta, Giovanni, Kumi, Godwin, Dong, Li, Aleem, Saadat, Fink, Cynthia, Garcia, Yudith, Green, Michael, Han, Jianxin, Kwon, Soojin, Qiao, Ying, Wang, Jiancheng, Zhang, Yulian, Liu, Ying, Zipp, Greg, Liang, Zhi, Burford, Neil, Ferrante, Meredith, Bertekap, Robert, Lewis, Martin, Cacace, Angela, Grace, James, Wilson, Alan, Nouraldeen, Amr, Westphal, Ryan, Kimball, David, Carson, Kenneth, Bronson, Joanne J., Macor, John E.

“…[Display omitted] Small molecule modulators of GPR88 activity (agonists, antagonists, or modulators) are of interest as potential agents for the treatment of a…”
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Synthesis and evaluation of carbamate and aryl ether substituted pyrazinones as corticotropin releasing factor-1 (CRF1) receptor antagonists by Ahuja, Vijay T., Hartz, Richard A., Molski, Thaddeus F., Mattson, Gail K., Lentz, Kimberley A., Grace, James E., Lodge, Nicholas J., Bronson, Joanne J., Macor, John E.

“…[Display omitted] A series of pyrazinone-based compounds incorporating either carbamate or aryl ether groups was synthesized and evaluated as…”
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A Strategy to Minimize Reactive Metabolite Formation: Discovery of (S)-4-(1-Cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a Potent, Orally Bioavailable Corticotropin-Releasing Factor-1 Receptor Antagonist by Hartz, Richard A, Ahuja, Vijay T, Zhuo, Xiaoliang, Mattson, Ronald J, Denhart, Derek J, Deskus, Jeffrey A, Vrudhula, Vivekananda M, Pan, Senliang, Ditta, Jonathan L, Shu, Yue-Zhong, Grace, James E, Lentz, Kimberley A, Lelas, Snjezana, Li, Yu-Wen, Molski, Thaddeus F, Krishnananthan, Subramaniam, Wong, Henry, Qian-Cutrone, Jingfang, Schartman, Richard, Denton, Rex, Lodge, Nicholas J, Zaczek, Robert, Macor, John E, Bronson, Joanne J

“…Detailed metabolic characterization of 8, an earlier lead pyrazinone-based corticotropin-releasing factor-1 (CRF1) receptor antagonist, revealed that this…”
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Comparative Biotransformation of Pyrazinone-Containing Corticotropin-Releasing Factor Receptor-1 Antagonists: Minimizing the Reactive Metabolite Formation by XIAOLIANG ZHUO, HARTZ, Richard A, BRONSON, Joanne J, WONG, Harvey, AHUJA, Vijay T, VRUDHULA, Vivekananda M, LEET, John E, HUANG, Stella, MACOR, John E, SHU, Yue-Zhong

“…( S )-5-Chloro-1-(1-cyclopropylethyl)-3-(2,6-dichloro-4-(trifluoromethyl)phenylamino)pyrazin-2(1 H )-one (BMS-665053), a pyrazinone-containing compound, is a…”
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Design, Structure–Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2‑b]pyridazines as Glycogen Synthase Kinase-3β (GSK-3β) Inhibitors by Hartz, Richard A., Ahuja, Vijay T., Sivaprakasam, Prasanna, Xiao, Hong, Krause, Carol M., Clarke, Wendy J., Kish, Kevin, Lewis, Hal, Szapiel, Nicolas, Ravirala, Ramu, Mutalik, Sayali, Nakmode, Deepa, Shah, Devang, Burton, Catherine R., Macor, John E., Dubowchik, Gene M.

“…Glycogen synthase kinase-3 (GSK-3) is a serine/threonine kinase that regulates numerous cellular processes, including metabolism, proliferation, and cell…”
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Atropisomerism Observed in Galactose-Based Monosaccharide Inhibitors of Galectin-3 Comprising 2-Methyl-4-phenyl-2,4-dihydro-3 H -1,2,4-triazole-3-thione by Yoon, David S, Liu, Chunjian, Jalagam, Prasada Rao, Feng, Jianxin, Wang, Wei, Swidorski, Jacob J, Xu, Li, Hartz, Richard A, Nair, Satheesh K, Beno, Brett R, Panda, Manoranjan, Ghosh, Kaushik, Kumar, Amit, Sale, Harinath, Shah, Devang, Mathur, Arvind, Ellsworth, Bruce A, Cheng, Dong, Regueiro-Ren, Alicia

“…Galectin-3 (Gal-3) is a carbohydrate binding protein that has been implicated in the development and progression of fibrotic diseases. Proof-of-principal…”
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Atropisomerism Observed in Galactose-Based Monosaccharide Inhibitors of Galectin‑3 Comprising 2‑Methyl-4-phenyl-2,4-dihydro‑3H‑1,2,4-triazole-3-thione by Yoon, David S., Liu, Chunjian, Jalagam, Prasada Rao, Feng, Jianxin, Wang, Wei, Swidorski, Jacob J., Xu, Li, Hartz, Richard A., Nair, Satheesh K., Beno, Brett R., Panda, Manoranjan, Ghosh, Kaushik, Kumar, Amit, Sale, Harinath, Shah, Devang, Mathur, Arvind, Ellsworth, Bruce A., Cheng, Dong, Regueiro-Ren, Alicia

“…Galectin-3 (Gal-3) is a carbohydrate binding protein that has been implicated in the development and progression of fibrotic diseases. Proof-of-principal…”
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Synthesis, Structure–Activity Relationships, and In Vivo Evaluation of Novel Tetrahydropyran-Based Thiodisaccharide Mimics as Galectin‑3 Inhibitors by Xu, Li, Hartz, Richard A, Beno, Brett R, Ghosh, Kaushik, Shukla, Jinal K, Kumar, Amit, Patel, Dipal, Kalidindi, Narasimharaju, Lemos, Nadine, Gautam, Shashyendra Singh, Kumar, Anoop, Ellsworth, Bruce A, Shah, Devang, Sale, Harinath, Cheng, Dong, Regueiro-Ren, Alicia

“…Galectin-3 is a member of a family of β-galactoside-binding proteins. A substantial body of literature reports that galectin-3 plays important roles in cancer,…”
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Synthesis, Structure–Activity Relationships, and In Vivo Evaluation of Novel C‑17 Amine Derivatives Based on GSK3640254 as HIV‑1 Maturation Inhibitors with Broad Spectrum Activity by Hartz, Richard A., Xu, Li, Sit, Sing-Yuen, Chen, Jie, Venables, Brian L., Lin, Zeyu, Zhang, Sharon, Li, Zhufang, Parker, Dawn, Simmons, Tara S., Jenkins, Susan, Hanumegowda, Umesh M., Dicker, Ira, Krystal, Mark, Meanwell, Nicholas A., Regueiro-Ren, Alicia

“…An investigation of the structure–activity relationships of a series of HIV-1 maturation inhibitors (MIs) based on GSK3640254 (4) was conducted by…”
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Discovery of 2‑(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase‑3 (GSK-3) Inhibitors by Hartz, Richard A., Ahuja, Vijay T., Luo, Guanglin, Chen, Ling, Sivaprakasam, Prasanna, Xiao, Hong, Krause, Carol M., Clarke, Wendy J., Xu, Songmei, Tokarski, John S., Kish, Kevin, Lewis, Hal, Szapiel, Nicolas, Ravirala, Ramu, Mutalik, Sayali, Nakmode, Deepa, Shah, Devang, Burton, Catherine R., Macor, John E., Dubowchik, Gene M.

“…Glycogen synthase kinase-3 (GSK-3) is a serine/threonine kinase that serves as an important regulator of a broad range of cellular functions. It has been…”
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The Discovery of GSK3640254, a Next-Generation Inhibitor of HIV‑1 Maturation by Regueiro-Ren, Alicia, Sit, Sing-Yuen, Chen, Yan, Chen, Jie, Swidorski, Jacob J., Liu, Zheng, Venables, Brian L., Sin, Ny, Hartz, Richard A., Protack, Tricia, Lin, Zeyu, Zhang, Sharon, Li, Zhufang, Wu, Dauh-Rurng, Li, Peng, Kempson, James, Hou, Xiaoping, Gupta, Anuradha, Rampulla, Richard, Mathur, Arvind, Park, Hyunsoo, Sarjeant, Amy, Benitex, Yulia, Rahematpura, Sandhya, Parker, Dawn, Phillips, Thomas, Haskell, Roy, Jenkins, Susan, Santone, Kenneth S., Cockett, Mark, Hanumegowda, Umesh, Dicker, Ira, Meanwell, Nicholas A., Krystal, Mark

“…GSK3640254 is an HIV-1 maturation inhibitor (MI) that exhibits significantly improved antiviral activity toward a range of clinically relevant polymorphic…”
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[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: Introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents by Deskus, Jeffrey A., Dischino, Douglas D., Mattson, Ronald J., Ditta, Jonathan L., Parker, Michael F., Denhart, Derek J., Zuev, Dmitry, Huang, Hong, Hartz, Richard A., Ahuja, Vijay T., Wong, Henry, Mattson, Gail K., Molski, Thaddeus F., Grace, James E., Zueva, Larisa, Nielsen, Julia M., Dulac, Heidi, Li, Yu-Wen, Guaraldi, Mary, Azure, Michael, Onthank, David, Hayes, Megan, Wexler, Eric, McDonald, Jennifer, Lodge, Nicholas J., Bronson, Joanne J., Macor, John E.

“…Based on a favorable balance between CRF-R1 affinity, lipophilicity and metabolic stability, compound 10 was evaluated for potential development as PET…”
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Discovery, Structure–Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2‑Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain by Hartz, Richard A, Ahuja, Vijay T, Nara, Susheel J, Kumar, C.M. Vijaya, Brown, Jeffrey M, Bristow, Linda J, Rajamani, Ramkumar, Muckelbauer, Jodi K, Camac, Daniel, Kiefer, Susan E, Hunihan, Lisa, Gulianello, Michael, Lewis, Martin, Easton, Amy, Lippy, Jonathan S, Surti, Neha, Pattipati, Sreenivasulu N, Dokania, Manoj, Elavazhagan, Saravanan, Dandapani, Kumaran, Hamman, Brian D, Allen, Jason, Kostich, Walter, Bronson, Joanne J, Macor, John E, Dzierba, Carolyn D

“…Effective treatment of chronic pain, in particular neuropathic pain, without the side effects that often accompany currently available treatment options is an…”
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Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2‑Associated Kinase 1 Inhibitors by Hartz, Richard A, Ahuja, Vijay T, Nara, Susheel J, Kumar, C. M. Vijaya, Manepalli, Raju K. V. L. P, Sarvasiddhi, Sarat Kumar, Honkhambe, Swarnamba, Patankar, Vidya, Dasgupta, Bireshwar, Rajamani, Ramkumar, Muckelbauer, Jodi K, Camac, Daniel M, Ghosh, Kaushik, Pokross, Matthew, Kiefer, Susan E, Brown, Jeffrey M, Hunihan, Lisa, Gulianello, Michael, Lewis, Martin, Lippy, Jonathan S, Surti, Neha, Hamman, Brian D, Allen, Jason, Kostich, Walter A, Bronson, Joanne J, Macor, John E, Dzierba, Carolyn D

“…Adaptor protein 2-associated kinase 1 (AAK1) is a serine/threonine kinase that was identified as a therapeutic target for the potential treatment of…”
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Synthesis and evaluation of prodrugs of corticotropin-releasing factor-1 (CRF1) receptor antagonist BMS-665053 leading to improved oral bioavailability by Hartz, Richard A., Vrudhula, Vivekananda M., Ahuja, Vijay T., Grace, James E., Lodge, Nicholas J., Bronson, Joanne J., Macor, John E.

“…A series of phosphate and ester-based prodrugs of BMS-665053 was prepared and evaluated in rat pharmacokinetic studies with the goal of improving the oral…”
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Design, Synthesis, and Biological Evaluation of 1,2,3,7-Tetrahydro-6H-purin-6-one and 3,7-Dihydro-1H-purine-2,6-dione Derivatives as Corticotropin-Releasing Factor1 Receptor Antagonists by Hartz, Richard A, Nanda, Kausik K, Ingalls, Charles L, Ahuja, Vijay T, Molski, Thaddeus F, Zhang, Ge, Wong, Harvey, Peng, Yong, Kelley, Michelle, Lodge, Nicholas J, Zaczek, Robert, Gilligan, Paul J, Trainor, George L

“…A growing body of evidence suggests that CRF1 receptor antagonism offers considerable therapeutic potential in the treatment of diseases resulting from…”
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Synthesis and evaluation of imidazo[1,5- a]pyrazines as corticotropin releasing hormone receptor ligands by Hartz, Richard A., Gilligan, Paul J., Nanda, Kausik K., Tebben, Andrew J., Fitzgerald, Larry W., Miller, Keith

“…A novel series of imidazo[1,5- a]pyrazines was synthesized and evaluated as corticotropin releasing hormone (CRH) receptor ligands. SAR studies focused…”
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In Vitro Intrinsic Clearance-Based Optimization of N 3-Phenylpyrazinones as Corticotropin-Releasing Factor-1 (CRF1) Receptor Antagonists by Hartz, Richard A, Ahuja, Vijay T, Rafalski, Maria, Schmitz, William D, Brenner, Allison B, Denhart, Derek J, Ditta, Jonathan L, Deskus, Jeffrey A, Yue, Eddy W, Arvanitis, Argyrios G, Lelas, Snjezana, Li, Yu-Wen, Molski, Thaddeus F, Wong, Harvey, Grace, James E, Lentz, Kimberley A, Li, Jianqing, Lodge, Nicholas J, Zaczek, Robert, Combs, Andrew P, Olson, Richard E, Mattson, Ronald J, Bronson, Joanne J, Macor, John E

“…A series of pyrazinone-based heterocycles was identified as potent and orally active corticotropin-releasing factor-1 (CRF1) receptor antagonists. Selected…”
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Potential CRF1R PET imaging agents: 1-Fluoroalkylsubstituted 5-halo-3-(arylamino)pyrazin-2(1H)-ones by Denhart, Derek J., Zuev, Dmitry, Ditta, Jonathan L., Hartz, Richard A., Ahuja, Vijay T., Mattson, Ronald J., Huang, Hong, Mattson, Gail K., Zueva, Larisa, Nielsen, Julia M., Kozlowski, Edward S., Lodge, Nicholas J., Bronson, Joanne J., Macor, John E.

“…A series of pyrazinones were prepared and evaluated as potential CRF1R PET imaging agents. Optimization of their CRF1R binding potencies and octanol–phosphate…”
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