US Patent No. 10,363,250

FOLATE RECEPTOR BINDING CONJUGATES OF ANTIFOLATES


Patent No. 10,363,250
Issue Date July 30, 2019
Title Folate Receptor Binding Conjugates Of Antifolates
Inventorship Christopher Paul Leamon, West Lafayette, IN (US)
Iontcho Radoslavov Vlahov, West Lafayette, IN (US)
Philip Stewart Low, West Lafayette, IN (US)
Assignee Endocyte, Inc., West Lafayette, IN (US) Purdue Research Foundation, West ...

Claim of US Patent No. 10,363,250

1. A method for treating a population of cancer cells in a patient, the method comprising administering to the patient a therapeutically effective amount of a conjugate of formula ALDm, wherein A is an antifolate of the formula:
wherein:
(1) X?OH, R?H, and Y=Glu; or
(2) X?OCH3, R?H, and Y?Glu; or
(3) X?OH, R?H, and Y=Valine; or
(4) X?OH, R?H, and Y=Suberate; or
(5) X?OH, R?CH3, and Y=Glu;
m is 1 to 3;
D is an independently selected drug; and;
L is a linker comprising at least one releasable linker;
wherein the cancer cells overexpress a folate receptor, and wherein the cancer is chosen from carcinoma, sarcoma, lymphoma, Hodgkin's disease, melanoma, mesothelioma, Burkitt's lymphoma, nasopharyngeal carcinoma, leukemia, or myeloma.