Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors
Keylor, Mitchell H, Gulati, Anmol, Kattar, Solomon D, Johnson, Rebecca E, Chau, Ryan W, Margrey, Kaila A, Ardolino, Michael J, Zarate, Cayetana, Poremba, Kelsey E, Simov, Vladimir, Morriello, Gregori J, Acton, John J, Pio, Barbara, Yan, Xin, Palte, Rachel L, McMinn, Spencer E, Nogle, Lisa, Lesburg, Charles A, Adpressa, Donovon, Lin, Shishi, Neelamkavil, Santhosh, Liu, Ping, Su, Jing, Hegde, Laxminarayan G, Woodhouse, Janice D, Faltus, Robert, Xiong, Tina, Ciaccio, Paul J, Piesvaux, Jennifer, Otte, Karin M, Wood, Harold B, Kennedy, Matthew E, Bennett, David Jonathan, DiMauro, Erin F, Fell, Matthew J, Fuller, Peter H
Published in Journal of medicinal chemistry (13.01.2022)
Published in Journal of medicinal chemistry (13.01.2022)
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Characterization of the Onset, Progression, and Reversibility of Morphological Changes in Mouse Lung after Pharmacological Inhibition of Leucine-Rich Kinase 2 Kinase Activity
Bryce, Dianne K, Ware, Chris M, Woodhouse, Janice D, Ciaccio, Paul J, Ellis, J Michael, Hegde, Laxminarayan G, Kuruvilla, Sabu, Maddess, Matthew L, Markgraf, Carrie G, Otte, Karin M, Poulet, Frederique M, Timmins, Lauren M, Kennedy, Matthew E, Fell, Matthew J
Published in The Journal of pharmacology and experimental therapeutics (01.04.2021)
Published in The Journal of pharmacology and experimental therapeutics (01.04.2021)
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Discovery and Optimization of N‑Heteroaryl Indazole LRRK2 Inhibitors
Logan, Kaitlyn M., Kaplan, Will, Simov, Vladimir, Zhou, Hua, Li, Derun, Torres, Luis, Morriello, Gregori J., Acton, John J., Pio, Barbara, Chen, Yi-Heng, Keylor, Mitchell H., Johnson, Rebecca, Kattar, Solomon D., Chau, Ryan, Yan, Xin, Ardolino, Michael, Zarate, Cayetana, Otte, Karin M., Palte, Rachel L., Xiong, Tina, McMinn, Spencer E., Lin, Shishi, Neelamkavil, Santhosh F., Liu, Ping, Su, Jing, Hegde, Laxminarayan G., Woodhouse, Janice D., Moy, Lily Y., Ciaccio, Paul J., Piesvaux, Jennifer, Zebisch, Matthias, Henry, Clare, Barker, John, Wood, Harold B., Kennedy, Matthew E., DiMauro, Erin F., Fell, Matthew J., Fuller, Peter H.
Published in Journal of medicinal chemistry (26.09.2024)
Published in Journal of medicinal chemistry (26.09.2024)
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Journal Article
Discovery of MK-1468: A Potent, Kinome-Selective, Brain-Penetrant Amidoisoquinoline LRRK2 Inhibitor for the Potential Treatment of Parkinson’s Disease
Kattar, Solomon D., Gulati, Anmol, Margrey, Kaila A., Keylor, Mitchell H., Ardolino, Michael, Yan, Xin, Johnson, Rebecca, Palte, Rachel L., McMinn, Spencer E., Nogle, Lisa, Su, Jing, Xiao, Dong, Piesvaux, Jennifer, Lee, Susi, Hegde, Laxminarayan G., Woodhouse, Janice D., Faltus, Robert, Moy, Lily Y., Xiong, Tina, Ciaccio, Paul J., Pearson, Kara, Patel, Mayankbhai, Otte, Karin M., Leyns, Cheryl E.G., Kennedy, Matthew E., Bennett, David Jonathan, DiMauro, Erin F., Fell, Matthew J., Fuller, Peter H.
Published in Journal of medicinal chemistry (09.11.2023)
Published in Journal of medicinal chemistry (09.11.2023)
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Journal Article
Inhibition of RORγT Skews TCRα Gene Rearrangement and Limits T Cell Repertoire Diversity
Guo, Yanxia, MacIsaac, Kenzie D., Chen, Yi, Miller, Richard J., Jain, Renu, Joyce-Shaikh, Barbara, Ferguson, Heidi, Wang, I-Ming, Cristescu, Razvan, Mudgett, John, Engstrom, Laura, Piers, Kyle J., Baltus, Gretchen A., Barr, Kenneth, Zhang, Hongjun, Mehmet, Huseyin, Hegde, Laxminarayan G., Hu, Xiao, Carter, Laura L., Aicher, Thomas D., Glick, Gary, Zaller, Dennis, Hawwari, Abbas, Correll, Craig C., Jones, Dallas C., Cua, Daniel J.
Published in Cell reports (Cambridge) (20.12.2016)
Published in Cell reports (Cambridge) (20.12.2016)
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Journal Article
Discovery and Optimization of Potent, Selective, and Brain-Penetrant 1‑Heteroaryl‑1H‑Indazole LRRK2 Kinase Inhibitors for the Treatment of Parkinson’s Disease
Candito, David A., Simov, Vladimir, Gulati, Anmol, Kattar, Solomon, Chau, Ryan W., Lapointe, Blair T., Methot, Joey L., DeMong, Duane E., Graham, Thomas H., Kurukulasuriya, Ravi, Keylor, Mitchell H., Tong, Ling, Morriello, Gregori J., Acton, John J., Pio, Barbara, Liu, Weiguo, Scott, Jack D., Ardolino, Michael J., Martinot, Theodore A., Maddess, Matthew L., Yan, Xin, Gunaydin, Hakan, Palte, Rachel L., McMinn, Spencer E., Nogle, Lisa, Yu, Hongshi, Minnihan, Ellen C., Lesburg, Charles A., Liu, Ping, Su, Jing, Hegde, Laxminarayan G., Moy, Lily Y., Woodhouse, Janice D., Faltus, Robert, Xiong, Tina, Ciaccio, Paul, Piesvaux, Jennifer A., Otte, Karin M., Kennedy, Matthew E., Bennett, David Jonathan, DiMauro, Erin F., Fell, Matthew J., Neelamkavil, Santhosh, Wood, Harold B., Fuller, Peter H., Ellis, J. Michael
Published in Journal of medicinal chemistry (22.12.2022)
Published in Journal of medicinal chemistry (22.12.2022)
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Journal Article
Discovery and Optimization of Potent, Selective, and Brain-Penetrant 1-Heteroaryl-1 H -Indazole LRRK2 Kinase Inhibitors for the Treatment of Parkinson's Disease
Candito, David A, Simov, Vladimir, Gulati, Anmol, Kattar, Solomon, Chau, Ryan W, Lapointe, Blair T, Methot, Joey L, DeMong, Duane E, Graham, Thomas H, Kurukulasuriya, Ravi, Keylor, Mitchell H, Tong, Ling, Morriello, Gregori J, Acton, John J, Pio, Barbara, Liu, Weiguo, Scott, Jack D, Ardolino, Michael J, Martinot, Theodore A, Maddess, Matthew L, Yan, Xin, Gunaydin, Hakan, Palte, Rachel L, McMinn, Spencer E, Nogle, Lisa, Yu, Hongshi, Minnihan, Ellen C, Lesburg, Charles A, Liu, Ping, Su, Jing, Hegde, Laxminarayan G, Moy, Lily Y, Woodhouse, Janice D, Faltus, Robert, Xiong, Tina, Ciaccio, Paul, Piesvaux, Jennifer A, Otte, Karin M, Kennedy, Matthew E, Bennett, David Jonathan, DiMauro, Erin F, Fell, Matthew J, Neelamkavil, Santhosh, Wood, Harold B, Fuller, Peter H, Ellis, J Michael
Published in Journal of medicinal chemistry (22.12.2022)
Published in Journal of medicinal chemistry (22.12.2022)
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Journal Article
Ileocolonic-Targeted JAK Inhibitor: A Safer and More Effective Treatment for Inflammatory Bowel Disease
Yadav, Vipul, House, Aileen, Matiz, Silvia, McCoubrey, Laura E, Bettano, Kimberly A, Bhave, Leena, Wang, Meiyao, Fan, Peter, Zhou, Siqun, Woodhouse, Janice D, Poimenidou, Eirini, Dou, Liu, Basit, Abdul W, Moy, Lily Y, Saklatvala, Robert, Hegde, Laxminarayan G, Yu, Hongshi
Published in Pharmaceutics (01.11.2022)
Published in Pharmaceutics (01.11.2022)
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Journal Article
Discovery of N‑(Indazol-3-yl)piperidine-4-carboxylic Acids as RORγt Allosteric Inhibitors for Autoimmune Diseases
Zhang, Hongjun, Lapointe, Blair T, Anthony, Neville, Azevedo, Rita, Cals, Jos, Correll, Craig C, Daniels, Matthew, Deshmukh, Sujal, van Eenenaam, Hans, Ferguson, Heidi, Hegde, Laxminarayan G, Karstens, Willem Jan, Maclean, John, Miller, J. Richard, Moy, Lily Y, Simov, Vladimir, Nagpal, Sunil, Oubrie, Arthur, Palte, Rachel L, Parthasarathy, Gopal, Sciammetta, Nunzio, van der Stelt, Mario, Woodhouse, Janice D, Trotter, B. Wesley, Barr, Kenneth
Published in ACS medicinal chemistry letters (13.02.2020)
Published in ACS medicinal chemistry letters (13.02.2020)
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Journal Article
Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors
Gulati, Anmol, Yeung, Charles S, Lapointe, Blair, Kattar, Solomon D, Gunaydin, Hakan, Scott, Jack D, Childers, Kaleen K, Methot, Joey L, Simov, Vladimir, Kurukulasuriya, Ravi, Pio, Barbara, Morriello, Greg J, Liu, Ping, Tang, Haiqun, Neelamkavil, Santhosh, Wood, Harold B, Rada, Vanessa L, Ardolino, Michael J, Yan, Xin Cindy, Palte, Rachel, Otte, Karin, Faltus, Robert, Woodhouse, Janice, Hegde, Laxminarayan G, Ciaccio, Paul, Minnihan, Ellen C, DiMauro, Erin F, Fell, Matthew J, Fuller, Peter H, Ellis, J. Michael
Published in MedChemComm (21.07.2021)
Published in MedChemComm (21.07.2021)
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Concomitant angiotensin AT1 receptor antagonism and neprilysin inhibition produces omapatrilat-like antihypertensive effects without promoting tracheal plasma extravasation in the rat
Hegde, Laxminarayan G, Yu, Cecile, Renner, Travis, Thibodeaux, Harold, Armstrong, Scott R, Park, Timothy, Cheruvu, Madhavi, Olsufka, Rachael, Sandvik, Erik R, Lane, Cassie E, Budman, Joe, Hill, Craig M, Klein, Uwe, Hegde, Sharath S
Published in Journal of cardiovascular pharmacology (01.04.2011)
Published in Journal of cardiovascular pharmacology (01.04.2011)
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Journal Article
Discovery of TD-0212, an Orally Active Dual Pharmacology AT 1 Antagonist and Neprilysin Inhibitor (ARNI)
McKinnell, R Murray, Fatheree, Paul, Choi, Seok-Ki, Gendron, Roland, Jendza, Keith, Olson Blair, Brooke, Budman, Joe, Hill, Craig M, Hegde, Laxminarayan G, Yu, Cecile, McConn, Donavon, Hegde, Sharath S, Marquess, Daniel G, Klein, Uwe
Published in ACS medicinal chemistry letters (10.01.2019)
Published in ACS medicinal chemistry letters (10.01.2019)
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Journal Article
Discovery of TD-0212, an Orally Active Dual Pharmacology AT1 Antagonist and Neprilysin Inhibitor (ARNI)
McKinnell, R. Murray, Fatheree, Paul, Choi, Seok-Ki, Gendron, Roland, Jendza, Keith, Olson Blair, Brooke, Budman, Joe, Hill, Craig M, Hegde, Laxminarayan G, Yu, Cecile, McConn, Donavon, Hegde, Sharath S, Marquess, Daniel G, Klein, Uwe
Published in ACS medicinal chemistry letters (10.01.2019)
Published in ACS medicinal chemistry letters (10.01.2019)
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Journal Article
The effects of stressful stimuli and hypothalamic–pituitary–adrenal axis activation are reversed by the melanin-concentrating hormone 1 receptor antagonist SNAP 94847 in rodents
Smith, Daniel G., Hegde, Laxminarayan G., Wolinsky, Toni D., Miller, Silke, Papp, Mariusz, Ping, Xiaoli, Edwards, Tanya, Gerald, Christophe P., Craig, Douglas A.
Published in Behavioural brain research (11.02.2009)
Published in Behavioural brain research (11.02.2009)
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Journal Article
RBx 6198 : A novel α1-adrenoceptor antagonist for the treatment of benign prostatic hyperplasia
NANDA, Kamna, NARUGANAHALLI, Krishna S, ANAND, Nitya, RAY, Abhijit, GUPTA, Suman, MALHOTRA, Shivani, TIWARI, Atul, HEGDE, Laxminarayan G, JAIN, Sanjay, SINHA, Neelima, GUPTA, Jung B, CHUGH, Anita
Published in European journal of pharmacology (01.04.2009)
Published in European journal of pharmacology (01.04.2009)
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Journal Article
Synthesis and SAR Investigations for Novel Melanin-Concentrating Hormone 1 Receptor (MCH1) Antagonists Part 1. The Discovery of Arylacetamides as Viable Replacements for the Dihydropyrimidinone Moiety of an HTS Hit
Jiang, Yu, Chen, Chien-An, Lu, Kai, Daniewska, Irena, De Leon, John, Kong, Ron, Forray, Carlos, Li, Boshan, Hegde, Laxminarayan G, Wolinsky, Toni D, Craig, Douglas A, Wetzel, John M, Andersen, Kim, Marzabadi, Mohammad R
Published in Journal of medicinal chemistry (09.08.2007)
Published in Journal of medicinal chemistry (09.08.2007)
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Comparative in vivo uroselectivity profiles of anticholinergics, tested in a novel anesthetized rabbit model
Naruganahalli, Krishna S., Sinha, Sandeep, Hegde, Laxminarayan G., Meru, Ashwinkumar V., Chugh, Anita, Kumar, Naresh, Gupta, Jung B, Ray, Abhijit
Published in European journal of pharmacology (31.10.2007)
Published in European journal of pharmacology (31.10.2007)
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Journal Article
Synthesis and SAR Investigations for Novel Melanin-Concentrating Hormone 1 Receptor (MCH1) Antagonists Part 2: A Hybrid Strategy Combining Key Fragments of HTS Hits
Chen, Chien-An, Jiang, Yu, Lu, Kai, Daniewska, Irena, Mazza, Christine G, Negron, Leonardo, Forray, Carlos, Parola, Tony, Li, Boshan, Hegde, Laxminarayan G, Wolinsky, Toni D, Craig, Douglas A, Kong, Ron, Wetzel, John M, Andersen, Kim, Marzabadi, Mohammad R
Published in Journal of medicinal chemistry (09.08.2007)
Published in Journal of medicinal chemistry (09.08.2007)
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Design, synthesis and activity of novel derivatives of Oxybutynin and Tolterodine
Kaur, Kirandeep, Aeron, Shelly, Bruhaspathy, Miriyala, Shetty, Shankar J., Gupta, Suman, Hegde, Laxminarayan H., Silamkoti, Arun D.V., Mehta, Anita, Chugh, Anita, Gupta, Jang B., Sarma, P.K.S., Kumar, Naresh
Published in Bioorganic & medicinal chemistry letters (15.04.2005)
Published in Bioorganic & medicinal chemistry letters (15.04.2005)
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