US2017258932A1PendingUtilityA1

Conjugates for treating diseases caused by psma expressing cells

Assignee: ENDOCYTE INCPriority: Nov 15, 2012Filed: May 26, 2017Published: Sep 14, 2017
Est. expiryNov 15, 2032(~6.3 yrs left)· nominal 20-yr term from priority
A61P 35/00A61P 13/08A61P 13/10A61K 38/00C07K 5/1019A61K 49/0002A61K 47/542A61K 47/547A61K 51/04A61K 38/05C07K 5/06113A61K 38/06A61K 47/64C07K 5/021A61K 38/08C07K 5/10A61K 38/07A61K 47/48038A61K 47/48246A61K 47/48023
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Claims

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

exact text as granted — not AI-modified
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

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