Discovery and optimization of quinazolinone-pyrrolo-dihydropyrrolones as potent, selective, and orally bioavailable Pim1,2,3 kinase inhibitors

被引:0
|
作者
Pettus, Liping [1 ]
机构
[1] Amgen Inc, Med Chem, Thousand Oaks, CA USA
关键词
D O I
暂无
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
21
引用
下载
收藏
页数:2
相关论文
共 50 条
  • [41] Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation
    Liu, Zhiqing
    Chen, Haiying
    Wang, Pingyuan
    Li, Yi
    Wold, Eric A.
    Leonard, Paul G.
    Joseph, Sarah
    Brasier, Allan R.
    Tian, Bing
    Zhou, Jia
    JOURNAL OF MEDICINAL CHEMISTRY, 2020, 63 (10) : 5242 - 5256
  • [42] Discovery and Optimization of Quinolinone Derivatives as Potent, Selective, and Orally Bioavailable Mutant Isocitrate Dehydrogenase 1 (mIDH1) Inhibitors
    Lin, Jian
    Lu, Wei
    Caravella, Justin A.
    Campbell, Ann Marie
    Diebold, R. Bruce
    Ericsson, Anna
    Fritzen, Edward
    Gustafson, Gary R.
    Lancia, David R., Jr.
    Shelekhin, Tatiana
    Wang, Zhongguo
    Castro, Jennifer
    Clarke, Andrea
    Gotur, Deepali
    Josephine, Helen R.
    Katz, Marie
    Diep, Hien
    Kershaw, Mark
    Yao, Lili
    Kauffman, Goss
    Hubbs, Stephen E.
    Luke, George P.
    Toms, Angela V.
    Wang, Liann
    Bair, Kenneth W.
    Barr, Kenneth J.
    Dinsmore, Christopher
    Walker, Duncan
    Ashwell, Susan
    JOURNAL OF MEDICINAL CHEMISTRY, 2019, 62 (14) : 6575 - 6596
  • [43] Discovery of Selective and Orally Bioavailable Protein Kinase Cθ (PKCθ) Inhibitors from a Fragment Hit
    George, Dawn M.
    Breinlinger, Eric C.
    Friedman, Michael
    Zhang, Yang
    Wang, Jianfei
    Argiriadi, Maria
    Bansal-Pakala, Pratima
    Barth, Martine
    Duignan, David B.
    Honore, Prisca
    Lang, QiugYu
    Mittelstadt, Scott
    Potin, Dominique
    Rundell, Lian
    Edmunds, Jeremy J.
    JOURNAL OF MEDICINAL CHEMISTRY, 2015, 58 (01) : 222 - 236
  • [44] Discovery and Optimization of 1-Phenoxy-2-aminoindanes as Potent, Selective, and Orally Bioavailable Inhibitors of the Na+/H+ Exchanger Type 3 (NHE3)
    Rackelmann, Nils
    Matter, Hans
    Englert, Heinrich
    Follmann, Markus
    Maier, Thomas
    Weston, John
    Arndt, Petra
    Heyse, Winfried
    Mertsch, Katharina
    Wirth, Klaus
    Bialy, Laurent
    JOURNAL OF MEDICINAL CHEMISTRY, 2016, 59 (19) : 8812 - 8829
  • [45] Discovery of 5-substituent-N-arylbenzamide derivatives as potent, selective and orally bioavailable LRRK2 inhibitors
    Ding, Xiao
    Dai, Xuedong
    Long, Kai
    Peng, Cheng
    Andreotti, Daniele
    Bamborough, Paul
    Eatherton, Andrew J.
    Edge, Colin
    Jandu, Karamjit S.
    Nichols, Paula L.
    Philps, Oliver J.
    Stasi, Luigi Piero
    Wan, Zehong
    Xiang, Jia-Ning
    Dong, Kelly
    Dossang, Pamela
    Ho, Ming-Hsun
    Li, Yi
    Mensah, Lucy
    Guan, Xiaoming
    Reith, Alastair D.
    Ren, Feng
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2017, 27 (17) : 4034 - 4038
  • [46] Discovery of potent and selective orally bioavailable β-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors.
    Edmondson, SD
    Mastracchio, A
    Duffy, JL
    Eiermann, GJ
    He, HB
    Leiting, B
    Leone, JF
    Lyons, KA
    Makarewicz, AM
    Patel, RA
    Petrov, A
    Wu, JK
    Thornberry, NA
    Weber, AE
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 229 : U218 - U218
  • [47] Discovery of potent, selective, and orally bioavailable pyridone-based dipeptidyl peptidase-4 inhibitors
    Xu, JY
    Wei, L
    Mathvink, R
    Edmondson, SD
    Mastracchio, A
    Eiermann, GJ
    He, HB
    Leone, JF
    Leiting, B
    Lyons, KA
    Marsilio, F
    Patel, RA
    Petrov, A
    Wu, JK
    Thornberry, NA
    Weber, AE
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (05) : 1346 - 1349
  • [48] Discovery of Novel, Induced-Pocket Binding Oxazolidinones as Potent, Selective, and Orally Bioavailable Tankyrase Inhibitors
    Bregman, Howard
    Chakka, Nagasree
    Guzman-Perez, Angel
    Gunaydin, Hakan
    Gu, Yan
    Huang, Xin
    Berry, Virginia
    Liu, Jingzhou
    Teffera, Yohannes
    Huang, Liyue
    Egge, Bryan
    Mullady, Erin L.
    Schneider, Steve
    Andrews, Paul S.
    Mishra, Ankita
    Newcomb, John
    Serafino, Randy
    Strathdee, Craig A.
    Turci, Susan M.
    Wilson, Cindy
    DiMauro, Erin F.
    JOURNAL OF MEDICINAL CHEMISTRY, 2013, 56 (11) : 4320 - 4342
  • [49] Discovery of 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amines as potent, selective and orally bioavailable LRRK2 inhibitors
    Ding, Xiao
    Stasi, Luigi Piero
    Ho, Ming-Hsun
    Zhao, Baowei
    Wang, Hailong
    Long, Kai
    Xu, Qiongfeng
    Sang, Yingxia
    Sun, Changhui
    Hu, Huan
    Yu, Haihua
    Wan, Zehong
    Wang, Lizhen
    Edge, Colin
    Liu, Qian
    Li, Yi
    Dong, Kelly
    Guan, Xiaoming
    Tattersall, F. David
    Reith, Alastair D.
    Ren, Feng
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2018, 28 (09) : 1615 - 1620
  • [50] MEDI 370-Evolution of selective, potent, and orally bioavailable small molecule Tie-2 kinase inhibitors
    Olivieri, Philip R., II
    Geuns-Meyer, Stephanie D.
    Hughes, Paul E.
    Albrecht, Brian K.
    Bellon, Steve
    Bready, James
    Caenepeel, Sean
    Cee, Victor J.
    Chaffee, Stuart C.
    Coxon, Angela
    Emery, Maurice
    Fretland, Jenne
    Gallant, Paul
    Gu, Yan
    Hodous, Brian L.
    Hoffman, Doug
    Johnson, Rebecca E.
    Kendall, Richard
    Kim, Joseph L.
    Long, Alexander M.
    Morrison, Michael
    Patel, Vinod F.
    Polverino, Anthony
    Rose, Paul
    Tempest, Paul
    Wang, Ling
    Whittington, Douglas A.
    Zhao, Huilin
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2007, 234