Title:
PLK1 POLO BOX DOMAIN INHIBITORS AND METHOD OF TREATING CANCER
Document Type and Number:
WIPO Patent Application WO/2022/067100
Kind Code:
A3
Abstract:
Provided is a method of treating cancer, particularly cancers associated with an overexpression of polo-like kinase (Plk1), comprising administering a compound of formula (I) or a pharmaceutically acceptable salt thereof in which ring A, X1, X2, X3, X4, X5, R2, R3, R4, n, bond a, and bond b are described herein. Exemplary compounds of formula (I) and pharmaceutically acceptable salts thereof, especially those that selectively inhibit the polo box domain of Plk1, also are provided.
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Inventors:
LEE KYUNG (US)
JACOBSON KENNETH (US)
ALVEREZ CELESTE (US)
PARK JUNG-EUN (US)
OLIVA PAOLA (US)
LEE HOBIN (US)
PONGORNE KIRSCH KLARA (US)
JACOBSON KENNETH (US)
ALVEREZ CELESTE (US)
PARK JUNG-EUN (US)
OLIVA PAOLA (US)
LEE HOBIN (US)
PONGORNE KIRSCH KLARA (US)
Application Number:
PCT/US2021/052054
Publication Date:
May 05, 2022
Filing Date:
September 24, 2021
Export Citation:
Assignee:
US HEALTH (US)
LEE KYUNG S (US)
JACOBSON KENNETH A (US)
ALVEREZ CELESTE N (US)
PARK JUNG EUN (US)
OLIVA PAOLA (US)
LEE HOBIN (US)
PONGORNE KIRSCH KLARA (US)
LEE KYUNG S (US)
JACOBSON KENNETH A (US)
ALVEREZ CELESTE N (US)
PARK JUNG EUN (US)
OLIVA PAOLA (US)
LEE HOBIN (US)
PONGORNE KIRSCH KLARA (US)
International Classes:
A61K31/519; A61P35/00
Domestic Patent References:
| WO2019084271A1 | 2019-05-02 | |||
| WO2007006211A1 | 2007-01-18 |
Foreign References:
| CN105267217A | 2016-01-27 |
Other References:
AMEEN ALI ABU-HASHEM ET AL: "Synthesis of new pyrazole, triazole, and thiazolidine-pyrimido [4, 5-b] quinoline derivatives with potential antitumor activity", ARCHIVES OF PHARMACAL RESEARCH, PHARMACEUTICAL SOCIETY OF KOREA, HEIDELBERG, vol. 35, no. 3, 5 April 2012 (2012-04-05), pages 437 - 445, XP035040206, ISSN: 1976-3786, DOI: 10.1007/S12272-012-0306-5
RAM V J ET AL: "Latent leishmanicidal activity of quinazolinones and 1,2,4-triazoloquinazolinones", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM, NL, vol. 4, no. 17, 8 September 1994 (1994-09-08), pages 2087 - 2090, XP026650885, ISSN: 0960-894X, [retrieved on 19940908], DOI: 10.1016/S0960-894X(01)80107-4
ALANZY ASMAA L ET AL: "Synthesis and Evaluation of New Non-nucleoside Compounds Based on Theinopyrimidine Nucleus with Expected Biological Activity against Microorganisms", JOCPR, 1 September 2017 (2017-09-01), pages 195 - 234, XP055873019, Retrieved from the Internet [retrieved on 20211214]
BEKHIT ADNAN A. ET AL: "Synthesis, biological evaluation and molecular modeling of novel thienopyrimidinone and triazolothienopyrimidinone derivatives as dual anti-inflammatory antimicrobial agents", BIOORGANIC CHEMISTRY, vol. 77, 1 April 2018 (2018-04-01), US, pages 38 - 46, XP055873021, ISSN: 0045-2068, DOI: 10.1016/j.bioorg.2017.12.028
ATEF A HAMED ET AL: "Synthesis and structure of some thienopyrimidine derivatives", MONATSHEFTE FÜR CHEMIE - CHEMICAL MONTHLY ; AN INTERNATIONAL JOURNAL OF CHEMISTRY, SPRINGER-VERLAG, AU, vol. 139, no. 7, 26 May 2008 (2008-05-26), pages 809 - 820, XP019634222, ISSN: 1434-4475
ALVEREZ CELESTE N. ET AL: "Identification of a New Heterocyclic Scaffold for Inhibitors of the Polo-Box Domain of Polo-like Kinase 1", JOURNAL OF MEDICINAL CHEMISTRY, vol. 63, no. 22, 25 November 2020 (2020-11-25), US, pages 14087 - 14117, XP055872504, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.0c01669
RAM V J ET AL: "Latent leishmanicidal activity of quinazolinones and 1,2,4-triazoloquinazolinones", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM, NL, vol. 4, no. 17, 8 September 1994 (1994-09-08), pages 2087 - 2090, XP026650885, ISSN: 0960-894X, [retrieved on 19940908], DOI: 10.1016/S0960-894X(01)80107-4
ALANZY ASMAA L ET AL: "Synthesis and Evaluation of New Non-nucleoside Compounds Based on Theinopyrimidine Nucleus with Expected Biological Activity against Microorganisms", JOCPR, 1 September 2017 (2017-09-01), pages 195 - 234, XP055873019, Retrieved from the Internet
BEKHIT ADNAN A. ET AL: "Synthesis, biological evaluation and molecular modeling of novel thienopyrimidinone and triazolothienopyrimidinone derivatives as dual anti-inflammatory antimicrobial agents", BIOORGANIC CHEMISTRY, vol. 77, 1 April 2018 (2018-04-01), US, pages 38 - 46, XP055873021, ISSN: 0045-2068, DOI: 10.1016/j.bioorg.2017.12.028
ATEF A HAMED ET AL: "Synthesis and structure of some thienopyrimidine derivatives", MONATSHEFTE FÜR CHEMIE - CHEMICAL MONTHLY ; AN INTERNATIONAL JOURNAL OF CHEMISTRY, SPRINGER-VERLAG, AU, vol. 139, no. 7, 26 May 2008 (2008-05-26), pages 809 - 820, XP019634222, ISSN: 1434-4475
ALVEREZ CELESTE N. ET AL: "Identification of a New Heterocyclic Scaffold for Inhibitors of the Polo-Box Domain of Polo-like Kinase 1", JOURNAL OF MEDICINAL CHEMISTRY, vol. 63, no. 22, 25 November 2020 (2020-11-25), US, pages 14087 - 14117, XP055872504, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.0c01669
Attorney, Agent or Firm:
HARRELL, Kristen, J. et al. (US)
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