公开(公告)号：US10947247B2

公开(公告)日：2021-03-16

申请号：US16456641

申请日：2019-06-28

申请人： UNIVERSITY OF PUERTO RICO

发明人： Cornelis P. Vlaar ,  Suranganie Dharmawardhane Flanagan ,  Eliud Hernandez-O'Farrill ,  Linette Castillo-Pichardo

IPC分类号： C07D401/14 ,  C07D403/14 ,  C07D491/048 ,  C07D403/04 ,  C07D409/14

摘要： Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases. Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

公开(公告)号：US11939337B2

公开(公告)日：2024-03-26

申请号：US17864198

申请日：2022-07-13

申请人： UNIVERSITY OF PUERTO RICO

发明人： Cornelis P. Vlaar ,  Suranganie Dharmawardhane Flanagan ,  Eliud Hernandez-O'Farrill ,  Linette Castillo-Pichardo

IPC分类号： C07D491/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D491/048

CPC分类号： C07D491/048 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14

摘要： Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases. Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

公开(公告)号：US10729689B2

公开(公告)日：2020-08-04

申请号：US16168612

申请日：2018-10-23

申请人： UNIVERSITY OF PUERTO RICO

发明人： Eliud Hernandez-O'Farrill ,  Cornelis P. Vlaar ,  Suranganie Dharmawardhane Flanagan ,  Linette Castillo-Pichardo

IPC分类号： A61K31/506 ,  C07D403/12 ,  C07D403/14 ,  C07D401/14 ,  A61P35/00 ,  A61K31/5377

摘要： A series of novel EHop-016 derivatives is presented herein via designing and synthesizing compounds that mimics its more favorable “U-shaped” conformation that appears to be critical for inhibitory activity against Rac. Based on modeling studies on EHop-016, compounds with a more rigid structural conformation can mimic this “U-shaped” conformation would improve the anti-migration activity against metastatic cells. Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases, for instance compounds of formula (I) Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

公开(公告)号：US10392396B2

公开(公告)日：2019-08-27

申请号：US15970268

申请日：2018-05-03

申请人： UNIVERSITY OF PUERTO RICO

发明人： Cornelis P. Vlaar ,  Suranganie Dharmawardhane Flanagan ,  Eliud Hernandez-O'Farrill ,  Linette Castillo-Pichardo

IPC分类号： C07D401/14 ,  C07D491/048 ,  C07D403/04 ,  C07D409/14 ,  C07D403/14

摘要： Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases. Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

公开(公告)号：US11446299B2

公开(公告)日：2022-09-20

申请号：US16923853

申请日：2020-07-08

申请人： UNIVERSITY OF PUERTO RICO

发明人： Eliud Hernandez-O'Farrill ,  Cornelis P. Vlaar ,  Suranganie Dharmawardhane Flanagan ,  Linette Castillo-Pichardo

IPC分类号： C07D403/12 ,  C07D403/14 ,  A61K31/506 ,  C07D401/14 ,  A61P35/00 ,  A61K31/5377

摘要： A series of novel EHop-016 derivatives is presented herein via designing and synthesizing compounds that mimics its more favorable “U-shaped” conformation that appears to be critical for inhibitory activity against Rac. Based on modeling studies on EHop-016, compounds with a more rigid structural conformation can mimic this “U-shaped” conformation and would improve the anti-migration activity against metastatic cells. Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases, for instance compounds of formula Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

公开(公告)号：US10995096B2

公开(公告)日：2021-05-04

申请号：US16814214

申请日：2020-03-10

申请人： UNIVERSITY OF PUERTO RICO

发明人： Cornelis P. Vlaar ,  Suranganie Dharmawardhane Flanagan ,  Eliud Hernandez-O'Farrill ,  Linette Castillo-Pichardo

IPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D491/048 ,  C07D409/14

摘要： Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases. Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

公开(公告)号：US09981980B2

公开(公告)日：2018-05-29

申请号：US15499532

申请日：2017-04-27

申请人： UNIVERSITY OF PUERTO RICO

发明人： Cornelis P. Vlaar ,  Suranganie Dharmawardhane Flanagan ,  Eliud Hernandez-O'Farrill ,  Linette Castillo-Pichardo

IPC分类号： C07D491/048 ,  C07D403/04 ,  C07D409/14 ,  C07D401/14

CPC分类号： C07D491/048 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14

摘要： Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases. Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.