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
  • [41] Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa
    Pinto, Donald J. P.
    Orwat, Michael J.
    Koch, Stephanie
    Rossi, Karen A.
    Alexander, Richard S.
    Smallwood, Angela
    Wong, Pancras C.
    Rendina, Alan R.
    Luettgen, Joseph M.
    Knabb, Robert M.
    He, Kan
    Xin, Baomin
    Wexler, Ruth R.
    Lam, Patrick Y. S.
    JOURNAL OF MEDICINAL CHEMISTRY, 2007, 50 (22) : 5339 - 5356
  • [42] Synthesis,Crystal Structure and Anticoagulant Activity of 5-Chloro-N-[[(5S)-2-oxo-3-[4-(2-oxopyridin-1(2H)-yl)phenyl]oxazolidin-5-yl]methyl]thiophene-2-carboxamide
    刘巍
    袁静
    张士俊
    徐为人
    黄长江
    汤立达
    结构化学, 2014, 33 (07) : 1091 - 1095
  • [43] Discovery of (1R,2R)-N-(4-(6-isopropylpyridin-2-yl)-3-(2-methyl-2H-indazol-5-yl)isothiazol-5-yl)-2-methylcyclopropanecarboxamide, a potent and orally efficacious mGlu5 receptor negative allosteric modulator
    Hao, Junliang
    Dehlinger, Veronique
    Fivush, Adam M.
    Rudyk, Helene C. E.
    Britton, Thomas C.
    Hollinshead, Sean P.
    Vokits, Benjamin P.
    Clark, Barry P.
    Henry, Steven S.
    Massey, Steven M.
    Peng, Langu
    Dressman, Bruce A.
    Heinz, Beverly A.
    Roberts, Edda F.
    Bracey-Walker, Mallorie R.
    Swanson, Steven
    Catlow, John T.
    Love, Patrick L.
    Tepool, Anita D.
    Peters, Steven C.
    Simmons, Rosa Maria A.
    Iyengar, Smriti
    McKinzie, David L.
    Monn, James A.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2013, 23 (05) : 1249 - 1252
  • [44] computational design, synthesis, and assessment of 3-(4-(4-(1,3,4-oxadiazol-2-yl)-1H-imidazol-2-yl)phenyl)-1,2,4-oxadiazole derivatives as effective epidermal growth factor receptor inhibitors: a prospective strategy for anticancer therapy (vol 15, pg 1626, 2024)
    Khedkar, Nilesh Raghunath
    Sindkhedkar, Milind
    Joseph, Alex
    RSC MEDICINAL CHEMISTRY, 2024, 15 (11): : 3912 - 3912
  • [45] Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide (FTIDC)
    Suzuki, Gentaroh
    Kimura, Toshifumi
    Satow, Akio
    Kaneko, Naoki
    Fukuda, Junko
    Hikichi, Hirohiko
    Sakai, Naoko
    Maehara, Shunsuke
    Kawagoe-Takaki, Hiroko
    Hata, Mikiko
    Azuma, Tomoko
    Ito, Satoru
    Kawamoto, Hiroshi
    Ohta, Hisashi
    JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2007, 321 (03): : 1144 - 1153
  • [46] Discovery of 7-Methoxy-6-[4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazol-5-yl]-1,3-benzothiazole (TASP0382088): A Potent and Selective Transforming Growth Factor-β Type I Receptor Inhibitor as a Topical Drug for Alopecia
    Amada, Hideaki
    Asanuma, Hajime
    Koami, Takeshi
    Okada, Atsushi
    Endo, Mayumi
    Ueda, Yasuji
    Naruse, Takumi
    Ikeda, Akiko
    CHEMICAL & PHARMACEUTICAL BULLETIN, 2013, 61 (03) : 286 - 291
  • [47] SYNTHESIS AND BIOLOGICAL-ACTIVITY OF 1,2-DIHYDRO-5-[4-(1H-IMIDAZOL-1-YL)PHENYL]-6-METHYL-2-OXO-3-PYRIDINECARBONITRILES AND ANALOGS
    SIRCAR, I
    DUELL, BL
    BRISTOL, JA
    WEISHAAR, RE
    EVANS, DB
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1985, 189 (APR-): : 40 - MEDI
  • [48] A Crystallographic Study of a Highly Substituted Imidazolinone, (3S,4S,5R)-3-(((S)-4-((1H-Indol-3-yl)Methyl)-5-Oxo-4,5-Dihydro-1H-Imidazol-2-yl)Amino)-4-((Tert-Butyldimethylsilyl)Oxy)-5-Hydroxypiperidin-2-One
    Sanjay Dutta
    Sergey M. Dibrov
    Cody J. Higginson
    Thomas Hermann
    Journal of Chemical Crystallography, 2011, 41 : 1573 - 1578
  • [49] A Crystallographic Study of a Highly Substituted Imidazolinone, (3S,4S,5R)-3-(((S)-4-((1H-Indol-3-yl)Methyl)-5-Oxo-4,5-Dihydro-1H-Imidazol-2-yl)Amino)-4-((Tert-Butyldimethylsilyl)Oxy)-5-Hydroxypiperidin-2-One
    Dutta, Sanjay
    Dibrov, Sergey M.
    Higginson, Cody J.
    Hermann, Thomas
    JOURNAL OF CHEMICAL CRYSTALLOGRAPHY, 2011, 41 (10) : 1573 - 1578
  • [50] Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors
    Kettle, Jason G.
    Anjum, Rana
    Barry, Evan
    Bhavsar, Deepa
    Brown, Crystal
    Boyd, Scott
    Campbell, Andrew
    Goldberg, Kristin
    Grondine, Michael
    Guichard, Sylvie
    Hardy, Christopher J.
    Hunt, Tom
    Jones, Rhys D. O.
    Li, Xiuwei
    Moleva, Olga
    Ogg, Derek
    Overman, Ross C.
    Packer, Martin J.
    Pearson, Stuart
    Schimpl, Marianne
    Shao, Wenlin
    Smith, Aaron
    Smith, James M.
    Stead, Darren
    Stokes, Steve
    Tucker, Michael
    Ye, Yang
    JOURNAL OF MEDICINAL CHEMISTRY, 2018, 61 (19) : 8797 - 8810