Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973)
Rice, Kenneth D, Aay, Naing, Anand, Neel K, Blazey, Charles M, Bowles, Owen J, Bussenius, Joerg, Costanzo, Simona, Curtis, Jeffry K, Defina, Steven C, Dubenko, Larisa, Engst, Stefan, Joshi, Anagha A, Kennedy, Abigail R, Kim, Angie I, Koltun, Elena S, Lougheed, Julie C, Manalo, Jean-Claire L, Martini, Jean-Francois, Nuss, John M, Peto, Csaba J, Tsang, Tsze H, Yu, Peiwen, Johnston, Stuart
Published in ACS medicinal chemistry letters (10.05.2012)
Published in ACS medicinal chemistry letters (10.05.2012)
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Journal Article
Discovery of XL888: A novel tropane-derived small molecule inhibitor of HSP90
Bussenius, Joerg, Blazey, Charles M., Aay, Naing, Anand, Neel K., Arcalas, Arlyn, Baik, TaeGon, Bowles, Owen J., Buhr, Chris A., Costanzo, Simona, Curtis, Jeffrey K., DeFina, Steven C., Dubenko, Larisa, Heuer, Timothy S., Huang, Ping, Jaeger, Christopher, Joshi, Anagha, Kennedy, Abigail R., Kim, Angie I., Lara, Katherine, Lee, Jae, Li, Jonathan, Lougheed, Julie C., Ma, Sunghoon, Malek, Shiva, Manalo, Jean-Claire L., Martini, Jean-Francois, McGrath, Garth, Nicoll, Monique, Nuss, John M., Pack, Michael, Peto, Csaba J., Tsang, Tsze H., Wang, Longcheng, Womble, Scott W., Yakes, Michael, Zhang, Wentao, Rice, Kenneth D.
Published in Bioorganic & medicinal chemistry letters (01.09.2012)
Published in Bioorganic & medicinal chemistry letters (01.09.2012)
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Journal Article
The First Formal Asymmetric Synthesis of Phorbol
Wender, Paul A, Rice, Kenneth D, Schnute, Mark E
Published in Journal of the American Chemical Society (20.08.1997)
Published in Journal of the American Chemical Society (20.08.1997)
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Journal Article
Pyrazolopyrimidines as dual Akt/p70S6K inhibitors
Rice, Kenneth D., Kim, Moon H., Bussenius, Joerg, Anand, Neel K., Blazey, Charles M., Bowles, Owen J., Canne-Bannen, Lynne, Chan, Diva S.-M., Chen, Baili, Co, Erick W., Costanzo, Simona, DeFina, Steven C., Dubenko, Larisa, Engst, Stefan, Franzini, Maurizio, Huang, Ping, Jammalamadaka, Vasu, Khoury, Richard G., Klein, Rhett R., Laird, A.Douglas, Le, Donna T., Mac, Morrison B., Matthews, David J., Markby, David, Miller, Nicole, Nuss, John M., Parks, Jason J., Tsang, Tsze H., Tsuhako, Amy L., Wang, Yong, Xu, Wei
Published in Bioorganic & medicinal chemistry letters (15.04.2012)
Published in Bioorganic & medicinal chemistry letters (15.04.2012)
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Journal Article
Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors
Bussenius, Joerg, Anand, Neel K., Blazey, Charles M., Bowles, Owen J., Bannen, Lynne Canne, Chan, Diva S.-M., Chen, Baili, Co, Erick W., Costanzo, Simona, DeFina, Steven C., Dubenko, Larisa, Engst, Stefan, Franzini, Maurizio, Huang, Ping, Jammalamadaka, Vasu, Khoury, Richard G., Kim, Moon H., Klein, Rhett R., Laird, Douglas, Le, Donna T., Mac, Morrison B., Matthews, David J., Markby, David, Miller, Nicole, Nuss, John M., Parks, Jason J., Tsang, Tsze H., Tsuhako, Amy L., Wang, Yong, Xu, Wei, Rice, Kenneth D.
Published in Bioorganic & medicinal chemistry letters (15.03.2012)
Published in Bioorganic & medicinal chemistry letters (15.03.2012)
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Journal Article
MEK INHIBITORS AND METHOD FOR USING THE SAME
DEFINA STEVEN CHARLES, KIM ANGIE INYOUNG, JOSHI ANAGHA ABHIJIT, BOWLES OWEN JOSEPH, AAY NAING, COSTANZO SIMONA, KENNEDY ABIGAIL R, KOLTUN ELENA, MANALO JEAN-CLAIRE LIMUN, ANAND NEEL KUMAR, LARISA DUBENKO, BUSSENIUS JOERG, TSANG TSZE H, BLAZEY CHARLES M, CURTIS JEFFRY KIMO, PETO CSABA J, RICE KENNETH D
Year of Publication 26.11.2020
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Year of Publication 26.11.2020
Patent
MEK INHIBITOR AND APPLICATION METHOD THEREOF
DEFINA STEVEN CHARLES, KIM ANGIE INYOUNG, JOSHI ANAGHA ABHIJIT, BOWLES OWEN JOSEPH, AAY NAING, COSTANZO SIMONA, KENNEDY ABIGAIL R, KOLTUN ELENA, MANALO JEAN-CLAIRE LIMUN, ANAND NEEL KUMAR, LARISA DUBENKO, BUSSENIUS JOERG, TSANG TSZE H, BLAZEY CHARLES M, CURTIS JEFFRY KIMO, PETO CSABA J, RICE KENNETH D
Year of Publication 13.06.2019
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Year of Publication 13.06.2019
Patent
Dibasic inhibitors of human mast cell tryptase. Part 2: Structure–activity relationships and requirements for potent activity
Rice, Kenneth D, Wang, Vivian R, Gangloff, Anthony R, Kuo, Elaine Y.-L, Dener, Jeffrey M, Newcomb, William S, Young, Wendy B, Putnam, Daun, Cregar, Lynne, Wong, Martin, Simpson, Paul J
Published in Bioorganic & medicinal chemistry letters (16.10.2000)
Published in Bioorganic & medicinal chemistry letters (16.10.2000)
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Journal Article
Dibasic inhibitors of human mast cell tryptase. Part 1: Synthesis and optimization of a novel class of inhibitors
Rice, Kenneth D, Gangloff, Anthony R, Kuo, Elaine Y.-L, Dener, Jeffrey M, Wang, Vivian R, Lum, Robert, Newcomb, William S, Havel, Chris, Putnam, Daun, Cregar, Lynne, Wong, Martin, Warne, Robert L
Published in Bioorganic & medicinal chemistry letters (16.10.2000)
Published in Bioorganic & medicinal chemistry letters (16.10.2000)
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Journal Article
MEK INHIBITOR AND APPLICATION METHOD THEREOF
DEFINA STEVEN CHARLES, KIM ANGIE INYOUNG, JOSHI ANAGHA ABHIJIT, BOWLES OWEN JOSEPH, AAY NAING, COSTANZO SIMONA, KENNEDY ABIGAIL R, KOLTUN ELENA, MANALO JEAN-CLAIRE LIMUN, ANAND NEEL KUMAR, LARISA DUBENKO, BUSSENIUS JOERG, TSANG TSZE H, BLAZEY CHARLES M, CURTIS JEFFRY KIMO, PETO CSABA J, RICE KENNETH D
Year of Publication 12.04.2018
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Year of Publication 12.04.2018
Patent
Dibasic Inhibitors of Human Mast Cell Tryptase. Part 3: Identification of a Series of Potent and Selective Inhibitors Containing the Benzamidine Functionality
Dener, Jeffrey M., Rice, Kenneth D., Newcomb, William S., Wang, Vivian R., Young, Wendy B., Gangloff, Anthony R., Kuo, Elaine Y.-L., Cregar, Lynne, Putnam, Daun, Wong, Martin
Published in Bioorganic & medicinal chemistry letters (09.07.2001)
Published in Bioorganic & medicinal chemistry letters (09.07.2001)
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Journal Article
MEK INHIBITOR AND APPLICATION METHOD THEREOF
DEFINA STEVEN CHARLES, KIM ANGIE INYOUNG, JOSHI ANAGHA ABHIJIT, BOWLES OWEN JOSEPH, AAY NAING, COSTANZO SIMONA, KENNEDY ABIGAIL R, KOLTUN ELENA, MANALO JEAN-CLAIRE LIMUN, ANAND NEEL KUMAR, LARISA DUBENKO, BUSSENIUS JOERG, TSANG TSZE H, BLAZEY CHARLES M, CURTIS JEFFRY KIMO, PETO CSABA J, RICE KENNETH D
Year of Publication 08.06.2017
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Year of Publication 08.06.2017
Patent
Monocharged inhibitors of mast cell tryptase derived from potent and selective dibasic inhibitors
Dener, Jeffrey M, Wang, Vivian R, Rice, Kenneth D, Gangloff, Anthony R, Kuo, Elaine Y.-L, Newcomb, William S, Putnam, Daun, Wong, Martin
Published in Bioorganic & medicinal chemistry letters (03.09.2001)
Published in Bioorganic & medicinal chemistry letters (03.09.2001)
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Journal Article
MEK INHIBITOR AND USE METHOD THEREOF
DEFINA STEVEN CHARLES, KIM ANGIE INYOUNG, JOSHI ANAGHA ABHIJIT, BOWLES OWEN JOSEPH, AAY NAING, COSTANZO SIMONA, KENNEDY ABIGAIL R, KOLTUN ELENA, MANALO JEAN-CLAIRE LIMUN, ANAND NEEL KUMAR, LARISA DUBENKO, BUSSENIUS JOERG, TSANG TSZE H, BLAZEY CHARLES M, CURTIS JEFFRY KIMO, PETO CSABA J, RICE KENNETH D
Year of Publication 24.12.2015
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Year of Publication 24.12.2015
Patent
AZETIDINES AS MEK INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISEASES
DEFINA STEVEN CHARLES, KIM ANGIE INYOUNG, JOSHI ANAGHA ABHIJIT, BOWLES OWEN JOSEPH, AAY NAING, COSTANZO SIMONA, KENNEDY ABIGAIL R, KOLTUN ELENA, MANALO JEAN CLAIRE LIMUN, ANAND NEEL KUMAR, BUSSENIUS JOERG, TSANG TSZE H, BLAZEY CHARLES M, CURTIS JEFFRY KIMO, PETO CSABA J, RICE KENNETH D, DUBENKO LARISA
Year of Publication 03.06.2013
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Year of Publication 03.06.2013
Patent
BENZOXAZEPINES AS INHIBITORS OF PI3K/M TOR AND METHODS OF THEIR USE AND MANUFACTURE
DEFINA STEVEN CHARLES, KIM ANGIE INYOUNG, HARRIS JASON R, BOWLES OWEN JOSEPH, ARCALAS ARLYN, AAY NAING, MANALO JEAN CLAIRE LIMUN, BUSSENIUS JOERG, TSANG TSZE H, CURTIS JEFFRY KIMO, JACKSON UGUETO EILEEN E, PETO CSABA J, RICE KENNETH D, DUBENKO LARISA, PACK MICHAEL
Year of Publication 07.08.2012
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Year of Publication 07.08.2012
Patent
BENZOXAZEPINES BASED P13K/MTOR INTHIBITORS AGAINST PROLIFERATIVE DISEASES
NG STEPHANIE, DEFINA STEVEN CHARLES, KIM ANGIE INYOUNG, ZAHARIA CRISTIANA A, JACKSON UGUETO EILEEN, HARRIS JASON R, BOWLES OWEN JOSEPH, JOSHI ANAGHA, MANALO JEAN CLAIRE LIMUN, ANAND NEEL KUMAR, BUSSENIUS JOERG, TSANG TSZE H, BLAZEY CHARLES M, TSUHAKO AMY LEW, CURTIS JEFFRY KIMO, PETO CSABA J, RICE KENNETH D, BUHR CHRIS ALLEN, DUBENKO LARISA, MA, SUNG HOON
Year of Publication 12.04.2012
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Year of Publication 12.04.2012
Patent