US2022008516A1PendingUtilityA1

PTH Prodrugs

Assignee: ASCENDIS PHARMA BONE DISEASES ASPriority: Mar 1, 2016Filed: Sep 28, 2021Published: Jan 13, 2022
Est. expiryMar 1, 2036(~9.6 yrs left)· nominal 20-yr term from priority
A61P 5/18A61K 38/29A61K 47/60A61K 47/54A61K 9/0019A61P 19/02A61P 1/02A61P 19/10A61P 29/00A61P 7/04A61P 17/14A61K 47/545C07K 14/575A61P 5/20A61K 47/56
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Claims

Abstract

The present invention relates to PTH prodrugs, pharmaceutical compositions comprising such PTH prodrugs and their uses.

Claims

exact text as granted — not AI-modified
1 - 18 . (canceled) 
     
     
         19 . A parathyroid hormone (PTH) conjugate of formula (IIf-i) or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         wherein 
         the unmarked dashed line indicates the attachment to the N-terminal nitrogen of a PTH moiety having the sequence of SEQ ID NO:51; and 
         the dashed line marked with the asterisk indicates attachment to a moiety 
       
       
         
           
           
               
               
           
         
         wherein 
         m and p are independently an integer ranging from and including 400 to 500. 
       
     
     
         20 . The PTH conjugate or a pharmacological salt thereof of  claim 19 , wherein the moiety 
       
         
           
           
               
               
           
         
       
       has a molecular weight of about 40 kDa. 
     
     
         21 . The PTH conjugate or a pharmacological salt thereof of  claim 19 , wherein m and p are the same integer. 
     
     
         22 . The PTH conjugate or a pharmacological salt thereof of  claim 19 , wherein m and p are about 450. 
     
     
         23 . A pharmaceutical composition comprising at least one PTH conjugate or a pharmaceutically acceptable salt thereof of  claim 19  and at least one excipient. 
     
     
         24 . The pharmaceutical composition of  claim 19 , wherein the pharmaceutical composition has a pH ranging from and including pH 4 to pH 6. 
     
     
         25 . A method of treating a patient having hypoparathyroidism comprising administering an effective amount of the PTH conjugate or pharmaceutically acceptable salt thereof of claim  1  or a pharmaceutical composition comprising such PTH conjugate or pharmaceutically acceptable salt thereof to the patient.

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