Design and optimization of coagulation factor XIa inhibitors: Discovery of trans-N-((S)-1-(4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl)-2-phenylethyl)-4-(aminomethyl)cyclohexane-carboxamide, a potent factor XIa inhibitor with in vivo antithrombotic activity

被引:0
|
作者
Hangeland, Jon J. [1 ]
Friends, Todd J. [1 ]
Rossi, Karen A. [1 ]
Smallheer, Joanne M. [1 ]
Wang, Cailan [1 ]
Sun, Zhong [1 ]
Fang, Tianan [1 ]
Corte, James R. [1 ]
Wong, Pancras C. [1 ]
Rendina, Alan R. [1 ]
Luettgen, Joseph M. [1 ]
Barbera, Frank A. [1 ]
Bozarth, Jeffrey M. [1 ]
Watson, Carol A. [1 ]
Zhang, Ge [1 ]
Wei, Anzhi [1 ]
Morin, Paul F. [1 ]
Bisacchi, Gregory S. [1 ]
Seiffert, Dietmar A. [1 ]
Wexler, Ruth R. [1 ]
Quan, Mimi L. [1 ]
机构
[1] Bristol Myers Squibb Co, Res & Dev, Princeton, NJ 08543 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
216-MEDI
引用
收藏
页数:1
相关论文
共 50 条
  • [1] Discovery of trans-methyl N-(4-{2-[(1S)-1-{[4-(aminomethyl)cyclohexyl]formamido}-2-phenylethylipyridin-4-yl}phenyl)carbamate, a potent and selective factor XIa inhibitor
    Corte, James R.
    Fang, Tianan
    Hangeland, Jon J.
    Friends, Todd J.
    Pinto, Donald J.
    Orwat, Michael J.
    Rendina, Alan R.
    Luettgen, Joseph M.
    Bozarth, Jeffrey M.
    Barbera, Frank A.
    Rossi, Karen A.
    Wei, Anzhi
    Morin, Paul E.
    Ramamurthy, Vidhyashankar
    Sheriff, Steven
    Seiffert, Dietmar
    Wexler, Ruth R.
    Quan, Mimi L.
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2014, 247
  • [2] 4-(1H-Indazol-5-yl)-6-phenylpyrimidin-2(1H)-one analogs as potent CDC7 inhibitors
    Shafer, Cynthia M.
    Lindvall, Mika
    Bellamacina, Cornelia
    Gesner, Thomas G.
    Yabannavar, Asha
    Jia, Weiping
    Lin, Song
    Walter, Annette
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (16) : 4482 - 4485
  • [3] Design, synthesis and biological evaluation of novel 2-(4-(1H-indazol-6-yl)-1H-pyrazol-1-yl)acetamide derivatives as potent VEGFR-2 inhibitors
    Wang, Xing-Rong
    Wang, Shuai
    Li, Wen-Bo
    Xu, Kai-Yan
    Qiao, Xue-Peng
    Jing, Xue-Li
    Wang, Zi-Xiao
    Yang, Chang-jiang
    Chen, Shi-Wu
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021, 213
  • [4] Discovery of 3-Chloro-N-{(S)-[3-(1-ethyl-1H-pyrazol-4-yl)phenyl][(2S)-piperidine-2-yl]methyl}-4-(trifluoromethyl)pyridine-2-carboxamide as a Potent Glycine Transporter 1 Inhibitor
    Yamamoto, Shuji
    Shibata, Tsuyoshi
    Abe, Kumi
    Oda, Koji
    Aoki, Takeshi
    Kawakita, Yasunori
    Kawamoto, Hiroshi
    CHEMICAL & PHARMACEUTICAL BULLETIN, 2016, 64 (09) : 1321 - 1337
  • [5] Synthesis and biological evaluation of N-(3-fluorobenzyl)-4-(1-(methyl-d3)-1H-indazol-5-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-amine as a novel, potent ALK5 receptor inhibitor
    Kang, Byung-Nam
    Kang, Hong-Jun
    Kim, Sunjoo
    Lee, Jungwoo
    Lee, Jinwoo
    Jeong, Hee-Jin
    Jeon, Seeun
    Shin, Youngdo
    Yoon, Cheolhwan
    Han, Cheolkyu
    Seo, Jeongbeob
    Yun, Jaesook
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2023, 85
  • [6] 4-({(E)-[2-(But-3-en-1-yl)-1-(prop-2-en-1-yl)-4-sulfanyl-1H-imidazol-5-yl]methylidene}amino)-3-phenyl-1H-1,2,4-triazole-5(4H)-thione
    Natarajan, Sampath
    Mathews, Rita
    ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2011, 67 : O2828 - +
  • [7] SYNTHESIS OF 1-[3-METHYL-2(3H)-BENZAZOLON-5 OR 6-YL]-4-(4-[CIS-2-(2,4-DICHLOROPHENYL)-2-(1H-IMIDAZOL-1-YL-METHYL)-1,3-DIOXOLAN-4-YL]METHYLENEOXYPHENYL)PIPERAZINES
    ABDELAAL, SM
    KONG, SB
    BAUER, L
    JOURNAL OF HETEROCYCLIC CHEMISTRY, 1992, 29 (05) : 1069 - 1076
  • [8] Efficient synthesis of 4-(3-fluoro-5-{[4-(2-methyl-1H-imidazol-1-yl)benzyl]-oxy}phenyl)tetrahydro-2H-pyran-4-carboxamide, a novel 5-lipoxygenase inhibitor
    Mano, T
    Stevens, RW
    Nakao, K
    Okumura, Y
    Kawamura, K
    Ando, A
    Matsuoka, Y
    SYNTHESIS-STUTTGART, 2004, (16): : 2625 - 2628
  • [9] N-{4-[4-(4-Fluorophenyl)-1-(2-methoxyethyl)-2-methylsulfanyl-1H-imidazol-5-yl]-2-pyridyl}-2-methyl-3-phenylpropionamide
    Ziegler, Katharina
    Schollmeyer, Dieter
    Laufer, Stefan
    ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2009, 65 : O3128 - U914
  • [10] Discovery of N-(4-(3-isopropyl-2-methyl-2H-indazol-5-yl)pyrimidin-2-yl)-4-(4-methylpiperazin-1-yl)quinazolin-7-amine as a Novel, Potent, and Oral Cyclin-Dependent Kinase Inhibitor against Haematological Malignancies
    Huang, Jianhang
    Wang, Xinren
    Dong, Ruinan
    Liu, Xiaoyue
    Li, Hongmei
    Zhang, Tianyi
    Xu, Junyu
    Liu, Chenhe
    Zhang, Yanmin
    Hou, Shaohua
    Tang, Weifang
    Lu, Tao
    Chen, Yadong
    JOURNAL OF MEDICINAL CHEMISTRY, 2021, 64 (17) : 12548 - 12571