IP Library › Patent Application 15245512
Patent Application
App. No. 15/245,512

CONJUGATES FOR TREATING DISEASES CAUSED BY PSMA EXPRESSING CELLS

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Quick Facts
Patent No.
US None
App. No.
15/245,512
Abstract

The invention described herein pertains to the diagnosis, imaging, and/or treatment of pathogenic cell populations. In particular, the invention described herein pertains to the diagnosis, imaging, and/or treatment of diseases caused by PSMA expressing cells, such as prostate cancer cells, using compounds capable of targeting PSMA expressing cells.

Claims (28)

1 - 39 . (canceled)

40 . The pharmaceutical composition of claim 30 further comprising one or a plurality of additional conjugates, wherein each of the one or the plurality of additional conjugates has a formula

B-L-(D) n

or a pharmaceutically acceptable salt thereof;

wherein B comprises a urea or thiourea of lysine and an amino acid selected from the group consisting of lysine, aspartic acid, glutamic acid, and homoglutamic acid, wherein the urea or thiourea is capable of binding to PSMA;

wherein L is a polyvalent linker;

wherein D is a radical of a drug; and

wherein n is 1.

41 . The pharmaceutical composition of claim 40 , wherein L is a polyvalent linker comprising an aminomethylphenylacetic acid diradical or an aminophenylacetic acid diradical.

42 . The pharmaceutical composition of claim 30 further comprising one or a plurality of additional conjugates, wherein each of the one or the plurality of additional conjugates has a formula

B-L-(D) n

or a pharmaceutically acceptable salt thereof;

wherein B is a radical of a PSMA binding ligand

wherein L is a polyvalent linker comprising at least one of an aminomethylphenylacetic acid diradical or an aminophenylacetic acid diradical;

wherein D is a radical of a drug; and

wherein n is 1.

43 . The pharmaceutical composition of claim 42 , wherein B comprises a urea or thiourea of lysine and an amino acid selected from the group consisting of lysine, aspartic acid, glutamic acid, and homoglutamic acid.

44 . The pharmaceutical composition of claim 40 , wherein B is selected from the group consisting of

45 . The pharmaceutical composition of claim 44 , wherein B is

46 . The pharmaceutical composition of claim 40 , wherein at least one drug is a tubulysin.

47 . The pharmaceutical composition of claim 40 , wherein L forms a urea or thiourea with the lysine.

48 . The pharmaceutical composition of claim 40 , wherein L comprises a cysteine diradical.

49 . The pharmaceutical composition of claim 40 , wherein L is a releasable linker.

50 . The pharmaceutical composition of claim 40 , wherein L comprises a disulfide.

51 . The pharmaceutical composition of claim 40 , wherein L comprises a diradical of the formula

52 . The pharmaceutical composition of claim 40 , wherein B-L comprises a diradical of the formula

53 . The pharmaceutical composition of claim 40 , wherein B-L comprises a diradical of the formula

54 . The pharmaceutical composition of claim 40 , wherein B-L comprises a diradical of the formula