US2007065362A1PendingUtilityA1

Gastrin receptor-avid peptide conjugates

66
Individually held — no corporate assignee on recordPriority: Apr 22, 1997Filed: Nov 3, 2006Published: Mar 22, 2007
Est. expiryApr 22, 2017(expired)· nominal 20-yr term from priority
Inventors:Timothy J. HoffmanWynn A. VolkertNing LiGary SieckmanChrys-Ann Higginbotham
A61K 51/088A61P 35/00C07K 14/57572C07F 15/008C07K 7/086C07F 5/003A61K 38/00
66
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Claims

Abstract

A compound for use as a therapeutic or diagnostic radiopharmaceutical includes a group capable of complexing a medically useful metal attached to a moiety which is capable of binding to a gastrin releasing peptide receptor. A method for treating a subject having a neoplastic disease includes administering to the subject an effective amount of a radiopharmaceutical having a metal chelated with a chelating group attached to a moiety capable of binding to a gastrin releasing peptide receptor expressed on tumor cells with subsequent internalization inside of the cell. A method of forming a therapeutic or diagnostic compound includes reacting a metal synthon with a chelating group covalently linked with a moiety capable of binding a gastrin releasing peptide receptor.

Claims

exact text as granted — not AI-modified
1 - 85 . (canceled)  
   
   
       86 . A compound having a structure of the formula X-(Y) n -B, wherein X is a metal binding moiety optionally bound to a metal, Y is a spacer group, n is selected from the integers 0 and 1, and B is a bombesin agonist.  
   
   
       87 . The compound of  claim 86 , wherein Y is selected from the group consisting of an amino acid sequence, a hydrocarbon chain, and a combination thereof.  
   
   
       88 . The compound of  claim 87 , wherein Y is a combination of L-glutamine and a hydrocarbon chain.  
   
   
       89 . The compound of  claim 88 , wherein Y is a combination of L-glutamine and a C 1  to C 10  hydrocarbon chain.  
   
   
       90 . The compound of  claim 86 , wherein X is selected from the group consisting of S 4 , N 3 S, N 2 S 2 , and NS 3 .  
   
   
       91 . The compound of  claim 90 , wherein X is N 3 S.  
   
   
       92 . The compound of  claim 86 , wherein said bombesin agonist is BBN(8-14).  
   
   
       93 . The compound of  claim 86 , wherein said bombesin agonist is BBN(8-13).  
   
   
       94 . A complex comprising a metal and a compound having a structure of the formula X-(Y) n -B, wherein X is a metal binding moiety, Y is a spacer group, n is selected from the integers 0 and 1, B is a bombesin agonist, and the metal is a diagnostically or therapeutically useful metal.  
   
   
       95 . The complex of  claim 94  wherein said metal is a β- or γ-emitting isotope.  
   
   
       96 . The complex of  claim 95 , wherein said metal is selected from the group consisting of  186 Re—,  188 Re—,  105 Rh—, and  99m Tc—.  
   
   
       97 . The complex of  claim 94 , wherein Y is selected from the group consisting of an amino acid sequence, a hydrocarbon chain, and a combination thereof.  
   
   
       98 . The complex of  claim 97 , wherein Y is a combination of L-glutamine and a hydrocarbon chain.  
   
   
       99 . The complex of  claim 98 , wherein Y is a combination of L-glutamine and a C 1  to C 10  hydrocarbon chain.  
   
   
       100 . The complex of  claim 94 , wherein X is selected from the group consisting of S 4 , N 3 S, N 2 S 2 , and NS 3 .  
   
   
       101 . The complex of  claim 100 , wherein X is N 3 S.  
   
   
       102 . The complex of  claim 94 , wherein said bombesin agonist is BBN(8-14).  
   
   
       103 . The complex of  claim 94 , wherein said bombesin agonist is BBN(8-13).  
   
   
       104 . A method of imaging a tumor site in a patient comprising administering to a subject a diagnostically effective amount of a compound comprising a metal complexed with a chelating group attached to a bombesin agonist and said compound has a structure of the formula X-(Y) n -B, wherein X is a metal binding moiety, Y is a spacer group, n is selected from the integers 0 and 1, and B is a bombesin agonist.  
   
   
       105 . The method of  claim 104 , wherein said metal is a β- or γ-emitting isotope.  
   
   
       106 . The method of  claim 105 , wherein said metal is selected from the group consisting of  186 Re—,  188 Re—,  105 Rh—, and  99m Tc—.  
   
   
       107 . The method of  claim 104 , wherein Y is selected from the group consisting of an amino acid sequence, a hydrocarbon chain, and a combination thereof.  
   
   
       108 . The method of  claim 107 , wherein Y is a combination of L-glutamine and a hydrocarbon chain.  
   
   
       109 . The method of  claim 108 , wherein Y is a combination of L-glutamine and a C 1  to C 10  hydrocarbon chain.  
   
   
       110 . The method of  claim 104 , wherein X is selected from the group consisting of S 4 , N 3 S, N 2 S 2 , and NS 3 .  
   
   
       111 . The method of  claim 110 , wherein X is N 3 S.  
   
   
       112 . The method of  claim 104 , wherein said bombesin agonist is BBN(8-14).  
   
   
       113 . The method of  claim 104 , wherein said bombesin agonist is BBN(8-13).

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