Structure–Activity Relationships and Discovery of a G Protein Biased μ Opioid Receptor Ligand, [(3-Methoxythiophen-2-yl)methyl]({2-[(9R)‑9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the Treatment of Acute Severe Pain
Chen, Xiao-Tao, Pitis, Philip, Liu, Guodong, Yuan, Catherine, Gotchev, Dimitar, Cowan, Conrad L, Rominger, David H, Koblish, Michael, DeWire, Scott M, Crombie, Aimee L, Violin, Jonathan D, Yamashita, Dennis S
Published in Journal of medicinal chemistry (24.10.2013)
Published in Journal of medicinal chemistry (24.10.2013)
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An Efficient Synthesis of 3-Substituted 3H-Pyrimidin-4-ones
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Published in Organic letters (18.03.2004)
Published in Organic letters (18.03.2004)
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A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine
DeWire, Scott M, Yamashita, Dennis S, Rominger, David H, Liu, Guodong, Cowan, Conrad L, Graczyk, Thomas M, Chen, Xiao-Tao, Pitis, Philip M, Gotchev, Dimitar, Yuan, Catherine, Koblish, Michael, Lark, Michael W, Violin, Jonathan D
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Published in The Journal of pharmacology and experimental therapeutics (01.03.2013)
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Azepanone-based inhibitors of human cathepsin S: Optimization of selectivity via the P2 substituent
Kerns, Jeffrey K., Nie, Hong, Bondinell, William, Widdowson, Katherine L., Yamashita, Dennis S., Rahman, Attiq, Podolin, Patricia L., Carpenter, Donald C., Jin, Qi, Riflade, Benoit, Dong, Xiaoyang, Nevins, Neysa, Keller, Paul M., Mitchell, Laura, Tomaszek, Thaddeus
Published in Bioorganic & medicinal chemistry letters (01.08.2011)
Published in Bioorganic & medicinal chemistry letters (01.08.2011)
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Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors
Seefeld, Mark A., Rouse, Meagan B., McNulty, Kenneth C., Sun, Lihui, Wang, Jizhou, Yamashita, Dennis S., Luengo, Juan I., Zhang, ShuYun, Minthorn, Elisabeth A., Concha, Nestor O., Heerding, Dirk A.
Published in Bioorganic & medicinal chemistry letters (15.04.2009)
Published in Bioorganic & medicinal chemistry letters (15.04.2009)
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Total synthesis of calicheamicinone: new arrangements for actuation of the reductive cycloaromatization of aglycon congeners
Haseltine, John N, Paz Cabal, Maria, Mantlo, Nathan B, Iwasawa, Nobuharu, Yamashita, Dennis S, Coleman, Robert S, Danishefsky, Samuel J, Schulte, Gayle K
Published in Journal of the American Chemical Society (01.05.1991)
Published in Journal of the American Chemical Society (01.05.1991)
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2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles
Lin, Hong, Yamashita, Dennis S., Zeng, Jin, Xie, Ren, Verma, Sharad, Luengo, Juan I., Rhodes, Nelson, Zhang, Shuyun, Robell, Kimberly A., Choudhry, Anthony E., Lai, Zhihong, Kumar, Rakesh, Minthorn, Elisabeth A., Brown, Kristin K., Heerding, Dirk A.
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
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2,3,5-Trisubstituted pyridines as selective AKT inhibitors—Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity
Lin, Hong, Yamashita, Dennis S., Zeng, Jin, Xie, Ren, Wang, Wenyong, Nidarmarthy, Sirishkumar, Luengo, Juan I., Rhodes, Nelson, Knick, Victoria B., Choudhry, Anthony E., Lai, Zhihong, Minthorn, Elisabeth A., Strum, Susan L., Wood, Edgar R., Elkins, Patricia A., Concha, Nestor O., Heerding, Dirk A.
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
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Inhibition of Invariant Chain Processing, Antigen-Induced Proliferative Responses, and the Development of Collagen-Induced Arthritis and Experimental Autoimmune Encephalomyelitis by a Small Molecule Cysteine Protease Inhibitor
Podolin, Patricia L, Bolognese, Brian J, Carpenter, Donald C, Davis, T. Gregg, Johanson, Roy A, Fox, Josephine H, Long, Edward, III, Dong, Xiaoyang, Marquis, Robert W, LoCastro, Stephen M, Terfloth, Gerald J, Kurali, Edit, Peterson, John J, Smith, Brian R, McQueney, Michael S, Yamashita, Dennis S, Capper-Spudich, Elizabeth A
Published in The Journal of immunology (1950) (15.06.2008)
Published in The Journal of immunology (1950) (15.06.2008)
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Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines
Lin, Hong, Yamashita, Dennis S., Xie, Ren, Zeng, Jin, Wang, Wenyong, Leber, Jack, Safonov, Igor G., Verma, Sharad, Li, Mei, LaFrance, Louis, Venslavsky, Joseph, Takata, Dennis, Luengo, Juan I., Kahana, Jason A., Zhang, Shuyun, Robell, Kimberly A., Levy, Dana, Kumar, Rakesh, Choudhry, Anthony E., Schaber, Michael, Lai, Zhihong, Brown, Barry S., Donovan, Brian T., Minthorn, Elisabeth A., Brown, Kristin K., Heerding, Dirk A.
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
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Azepanone-Based Inhibitors of Human Cathepsin L
Marquis, Robert W, James, Ian, Zeng, Jin, Trout, Robert E. Lee, Thompson, Scott, Rahman, Attiq, Yamashita, Dennis S, Xie, Ren, Ru, Yu, Gress, Catherine J, Blake, Simon, Lark, Michael A, Hwang, Shing-Mei, Tomaszek, Thaddeus, Offen, Priscilla, Head, Martha S, Cummings, Maxwell D, Veber, Daniel F
Published in Journal of medicinal chemistry (03.11.2005)
Published in Journal of medicinal chemistry (03.11.2005)
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Design, synthesis, and kinetic evaluation of high-affinity FKBP ligands and the X-ray crystal structures of their complexes with FKBP12
Holt, Dennis A, Luengo, Juan I, Yamashita, Dennis S, Oh, Hye Ja, Konialian, Arda L, Yen, Hwa Kwo, Rozamus, Leonard W, Brandt, Martin, Bossard, Mary J
Published in Journal of the American Chemical Society (01.11.1993)
Published in Journal of the American Chemical Society (01.11.1993)
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Structure Activity Relationships and Discovery of a G Protein Biased mu Opioid Receptor Ligand, [(3-Methoxythiophen-2-yl)methyl]a2[(9R)-9-(pyridin-2-y1)-6-oxaspiro-[4.5]clecan-9-yl]ethylpamine (TRV130), for the Treatment of Acute Severe Pain
Chen, Xiao-Tao, Pitis, Philip, Liu, Guodong, Yuan, Catherine, Gotchev, Dimitar, Cowan, Conrad L., Rominger, David H., Koblish, Michael, DeWire, Scott M., Crombie, Aimee L., Violin, Jonathan D., Yamashita, Dennis S.
Published in Journal of medicinal chemistry (24.10.2013)
Published in Journal of medicinal chemistry (24.10.2013)
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Potent and Selective Cathepsin L Inhibitors Do Not Inhibit Human Osteoclast Resorption in Vitro
James, Ian E., Marquis, Robert W., Blake, Simon M., Hwang, Shing Mei, Gress, Catherine J., Ru, Yu, Zembryki, Denise, Yamashita, Dennis S., McQueney, Michael S., Tomaszek, Thaddeus A., Oh, Hye-Ja, Gowen, Maxine, Veber, Daniel F., Lark, Michael W.
Published in The Journal of biological chemistry (13.04.2001)
Published in The Journal of biological chemistry (13.04.2001)
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Use of Papain as a Model for the Structure-Based Design of Cathepsin K Inhibitors: Crystal Structures of Two Papain−Inhibitor Complexes Demonstrate Binding to S‘-Subsites
LaLonde, Judith M, Zhao, Baoguang, Smith, Ward W, Janson, Cheryl A, DesJarlais, Renee L, Tomaszek, Thaddeus A, Carr, Thomas J, Thompson, Scott K, Oh, Hye-Ja, Yamashita, Dennis S, Veber, Daniel F, Abdel-Meguid, Sherin S
Published in Journal of medicinal chemistry (05.11.1998)
Published in Journal of medicinal chemistry (05.11.1998)
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Potent dipeptidylketone inhibitors of the cysteine protease cathepsin K
Marquis, Robert W, Ru, Yu, Yamashita, Dennis S, Oh, Hye-Ja, Yen, Jack, Thompson, Scott K, Carr, Thomas J, Levy, Mark A, Tomaszek, Thaddeus A, Ijames, Carl F, Smith, Ward W, Zhao, Baoguang, Janson, Cheryl A, Abdel-Meguid, Sherin S, D'Alessio, Karla J, McQueney, M.S, Veber, Daniel F
Published in Bioorganic & medicinal chemistry (01.04.1999)
Published in Bioorganic & medicinal chemistry (01.04.1999)
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INHIBITORS OF AKT ACTIVITY
MCNULTY KENNETH C, ROUSE MEAGAN B, SEEFELD MARK ANDREW, YAMASHITA DENNIS S, HEERDING DIRK A, PEACE SIMON
Year of Publication 09.12.2014
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Year of Publication 09.12.2014
Patent
An Azepanone-Based Inhibitor of Human Cathepsin K with Improved Oral Bioavailability in the Rat and the Monkey
Marquis, Robert W, Ward, Keith W, Roethke, Theresa, Smith, Brian R, Ru, Yu, Yamashita, Dennis S, Tomaszek, Thaddeus A, Gorycki, Peter D, Cheng, H.-Y, James, Ian E, Stroup, George B, Lark, Michael W, Gowen, Maxine, Veber, Daniel F
Published in Molecular pharmaceutics (12.01.2004)
Published in Molecular pharmaceutics (12.01.2004)
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A new synthesis of substituted furans
Danheiser, Rick L, Stoner, Eric J, Koyama, Hiroo, Yamashita, Dennis S, Klade, Carrie A
Published in Journal of the American Chemical Society (01.06.1989)
Published in Journal of the American Chemical Society (01.06.1989)
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