06-02-2020 дата публикации
Номер: US20200039963A1
Автор:
Tomasz Cierpicki,
Jolanta Grembecka,
Weijiang Ying,
Yiwu Yao,
Felicia Gray,
Qingjie Zhao,
CIERPICKI TOMASZ,
GREMBECKA JOLANTA,
YING WEIJIANG,
YAO YIWU,
GRAY FELICIA,
ZHAO QINGJIE,
Cierpicki, Tomasz,
Grembecka, Jolanta,
Ying, Weijiang,
Yao, Yiwu,
Gray, Felicia,
Zhao, Qingjie
Принадлежит:
Provided herein are small molecule inhibitors of Polycomb Repressive Complex 1 (PRC1) activity, and methods of use thereof for the treatment of disease, including leukemia and other cancers, as well as other diseases dependent on the activity of PRC1. 2. (canceled)3. The PRC1 inhibitor of claim 1 , comprising a pyrrole claim 1 , furan claim 1 , or thiophene ring displaying the substituents of one or more of the compounds of Table A claim 1 , in any suitable combination.4. The PRC1 inhibitor of claim 3 , comprising a compound of Table A.6. The PRC1 inhibitor of claim 5 , wherein A claim 5 , A′ claim 5 , E claim 5 , and E′ are independently selected from the rings of Table 1.9. The PRC1 inhibitor of comprising any combination of substituents depicted on the compounds of Table A.10. The PRC1 inhibitor of claim 7 , wherein the compound is selected from the compounds of Table A.11. A pharmaceutical composition comprising the PRC1 inhibitor of and a pharmaceutically acceptable carrier.12. The pharmaceutical composition of claim 11 , wherein the pharmaceutical composition is formulated for oral administration.13. The pharmaceutical composition of claim 11 , wherein the pharmaceutical composition is formulated for injection.14. A method of inhibiting PRC1 with an effective amount of a pharmaceutical composition of .15. The method of claim 14 , wherein PRC1 activity is inhibited by binding of the compound or pharmaceutical composition to PRC1.16. A method of treating a subject comprising administering to the subject a pharmaceutical composition of .17. (canceled)18. The method of claim 16 , wherein the subject suffers from cancer.19. The method of claim 18 , wherein the cancer comprises leukemia claim 18 , hematologic malignancy claim 18 , solid tumor cancer claim 18 , breast cancer claim 18 , prostate cancer claim 18 , colon cancer claim 18 , pancreatic cancer claim 18 , ovarian cancer claim 18 , liver cancer or thyroid cancer.20. The method of claim 19 , wherein the ...
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