IP Library › Patent Application 15606835
Patent Application
App. No. 15/606,835

CONJUGATES FOR TREATING DISEASES CAUSED BY PSMA EXPRESSING CELLS

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Patent No.
US None
App. No.
15/606,835
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 (32)

1 - 29 . (canceled)

30 . A conjugate having a formula

B-L-(D) n

or a pharmaceutically acceptable salt thereof;

wherein B comprises a urea of lysine and glutamic acid;

wherein L is a polyvalent linker;

wherein D comprises a radioactive isotope of a metal coordinated to a chelating group; and

wherein n is 1.

31 . The conjugate of claim 30 or the pharmaceutically acceptable salt thereof, wherein B comprises a structure

32 . The conjugate of claim 30 or the pharmaceutically acceptable salt thereof, wherein B is selected from the group consisting of

33 . The conjugate of claim 30 or the pharmaceutically acceptable salt thereof, wherein B is selected from the group consisting of

34 . The conjugate of claim 30 or the pharmaceutically acceptable salt thereof, wherein B is selected from the group consisting of

35 . The conjugate of claim 30 or the pharmaceutically acceptable salt thereof, wherein L forms a urea with the lysine.

36 . The conjugate of claim 30 or the pharmaceutically acceptable salt thereof, wherein L comprises a chain of at least about 7 atoms.

37 . The conjugate of claim 30 or the pharmaceutically acceptable salt thereof, wherein L comprises a chain of at least about 8 atoms.

38 . The conjugate of claim 30 or the pharmaceutically acceptable salt thereof, wherein L comprises a chain of at least about 9 atoms.

39 . The conjugate of claim 30 or the pharmaceutically acceptable salt thereof, wherein L comprises a chain of at least 10 atoms.

40 . The conjugate of claim 30 or the pharmaceutically acceptable salt thereof, wherein the linker comprises an alkylene, a cycloalkylene, an alkylenecycloalkyl, an alkylenecarbonyl, or a cycloalkylenecarbonyl.

41 . The conjugate of claim 40 or the pharmaceutically acceptable salt thereof, wherein the alkylene, the cycloalkylene, the alkylenecycloalkyl, the alkylenecarbonyl, and the cycloalkylenecarbonyl are each independently optionally substituted with one or more substituents X 1 selected from the group consisting of aryl, substituted aryl, arylalkyl, and substituted arylaklyl.

42 . The conjugate of claim 41 or the pharmaceutically acceptable salt thereof, wherein X 1 comprises naphthyl.

43 . The conjugate of claim 30 or the pharmaceutically acceptable salt thereof, wherein B-L comprises a diradical of the formula

44 . A conjugate having a formula

B-L-D

or a pharmaceutically acceptable salt thereof;

wherein B comprises a urea of lysine and glutamic acid, and wherein B comprises a structure

wherein L is a polyvalent linker, wherein L forms a urea with the lysine, and wherein L comprises an alkylene, a cycloalkylene, an alkylenecycloalkyl, an alkylenecarbonyl, or a cycloalkylenecarbonyl; and

wherein D comprises a radioactive isotope of a metal coordinated to a chelating group.

45 . The conjugate of claim 44 or the pharmaceutically acceptable salt thereof, wherein the alkylene, the cycloalkylene, the alkylenecycloalkyl, the alkylenecarbonyl, and the cycloalkylenecarbonyl are each independently optionally substituted with one or more substituents X 1 selected from the group consisting of aryl, substituted aryl, arylalkyl, and substituted arylaklyl.

46 . The conjugate of claim 45 or the pharmaceutically acceptable salt thereof, wherein X 1 comprises naphthyl.

47 . The conjugate of claim 44 or the pharmaceutically acceptable salt thereof, wherein B is selected from the group consisting of

48 . The conjugate of claim 44 or the pharmaceutically acceptable salt thereof, wherein B is selected from the group consisting of

49 . The conjugate of claim 44 or the pharmaceutically acceptable salt thereof, wherein B is selected from the group consisting of