WO2022259204 - O-LINKED THIADIAZOLYL COMPOUNDS AS DNA POLYMERASE THETA INHIBITORS

National phase entry:
Publication Number WO/2022/259204
Publication Date 15.12.2022
International Application No. PCT/IB2022/055384
International Filing Date 09.06.2022
Title **
[English] O-LINKED THIADIAZOLYL COMPOUNDS AS DNA POLYMERASE THETA INHIBITORS
[French] COMPOSÉS THIADIAZOLYLE LIÉS À O UTILISÉS EN TANT QU'INHIBITEURS DE L'ADN POLYMÉRASE THÊTA
Applicants **
IDEAYA BIOSCIENCES, INC.
GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.4) LIMITED
Inventors
BARSANTI, Paul A.
JAIPURI, Firoz Ali
SEVERANCE, Daniel Lee
WANG, Chenbo
DUFFY, Kevin J.
LAWHORN, Brian G.
ADAMS, Nicholas David
BOTYANSZKI, Janos
DARCY, Michael G.
KIESOW, Terence J.
MCATEE, John J.
MARTYR, Cuthbert
BUITRAGO SANTANILLA, Alexander
TIAN, Xinrong
Priority Data
63/209,555   11.06.2021   US
63/319,826   15.03.2022   US
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Quotation for National Phase entry

Country StagesTotal
China Filing, Examination, Granting8762
EPO Filing, Examination, Granting66809
Japan Filing, Examination, Granting3931
South Korea Filing, Examination, Granting5510
USA Filing, Examination, Granting23940
MasterCard Visa
Total: 108,952

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Abstract[English] Disclosed herein are certain thiadiazolyl derivatives Formula (I): (I) that inhibit DNA Polymerase Theta (Pol) activity, in particular inhibit Pol activity by inhibiting ATP dependent helicase domain activity of Pol. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Pol such as cancer, including homologous recombination (HR) deficient cancers.[French] L'invention concerne certains dérivés de thiadiazolyle de formule (I) : (I) Qui inhibent l'activité de l'ADN polymérase thêta (Pol), en particulier qui inhibent l'activité de Pol par inhibition de l'activité du domaine hélicase dépendant de l'ATP de Pol. L'invention concerne également des compositions pharmaceutiques comprenant de tels composés et des méthodes de traitement et/ou de prévention de maladies pouvant être traitées par inhibition de Pol telles que le cancer, y compris des cancers déficients en recombinaison homologue (HR).

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