	US 11,926,631 B2
	Method of treating cancer using amanitin derivatives
Werner Simon, Ladenburg (DE); Susanne Werner-Simon, Ladenburg (DE); Christian Lutz, Ladenburg (DE); Christoph Müller, Ladenburg (DE); Torsten Hechler, Ladenburg (DE); and Michael Kulke, Ladenburg (DE)
Assigned to Heidelberg Pharma Research GmbH, Ladenburg (DE)
Filed by Heidelberg Pharma Research GmbH, Ladenburg (DE)
Filed on May 11, 2022, as Appl. No. 17/742,196.
Application 17/742,196 is a division of application No. 16/637,361, granted, now 11,420,971, previously published as PCT/EP2018/071265, filed on Aug. 6, 2018.
Claims priority of application No. 17185181 (EP), filed on Aug. 7, 2017.
Prior Publication US 2022/0274995 A1, Sep. 1, 2022
Int. Cl. A61P 35/00 (2006.01); A61K 47/68 (2017.01); C07D 487/04 (2006.01); C07K 1/06 (2006.01); C07K 7/64 (2006.01)

CPC C07D 487/04 (2013.01) [A61K 47/6831 (2017.08); A61P 35/00 (2018.01); C07K 1/063 (2013.01); C07K 7/64 (2013.01)]

4 Claims

1. A method of treating cancer in a patient, the method comprising administering to the patient a conjugate comprising:

(a) an amanitin derivative comprising a 6′-amino-substituted tryptophan moiety, which is selected from (i)S-desoxy-6′-amino-amanin, 6′-amino-amanin, (ii)S-desoxy-6′-amino-amanin-amide, 6′-amino-amaninamide, and (iii) a derivative of the amanitin derivative according to (i), wherein the free carboxylic acid moiety of amino acid 1 is converted to an carboxylic ester —C(═O)OR4 or to a moiety —C(═O)NH—OR4,

(b) a target-binding moiety, and

(c) optionally a linker linking said amanitin derivative and said target-binding moiety, wherein the cancer is selected from the group consisting of breast cancer, pancreatic cancer, cholangiocarcinoma, colorectal cancer, prostate cancer, leukemia, and malignant lymphoma, and

wherein the cancer is responsive to inhibition of mammalian RNA polymerase II.