US2023355629A1PendingUtilityA1

Deuterated derivatives of ruxolitinib

82
Assignee: SUN PHARMACEUTICAL IND INCPriority: Jun 15, 2012Filed: Dec 9, 2022Published: Nov 9, 2023
Est. expiryJun 15, 2032(~5.9 yrs left)· nominal 20-yr term from priority
A61P 37/02C07D 487/04C07B 2200/05A61K 45/06A61K 31/7068A61K 31/5685A61K 31/454A61K 31/4045A61K 31/519A61P 35/02A61P 35/00
82
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Claims

Abstract

The present invention in one embodiment provides a compound of Formula A: or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising the compound; and methods of treating the indications disclosed herein.

Claims

exact text as granted — not AI-modified
1 - 9 . (canceled) 
     
     
         10 . A compound represented by the following structural formula: 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof, wherein each position in the compound designated specifically as deuterium has at least 90% incorporation of deuterium. 
       
     
     
         11 . The compound of  claim 10 , wherein, the pharmaceutically acceptable salt of the compound is the phosphate salt. 
     
     
         12 . The compound of  claim 10 , wherein each position designated specifically as deuterium has at least 95% incorporation of deuterium. 
     
     
         13 . The compound of  claim 12 , wherein, the pharmaceutically acceptable salt of the compound is the phosphate salt. 
     
     
         14 . The compound of  claim 10 , wherein each position designated specifically as deuterium has at least 97% incorporation of deuterium. 
     
     
         15 . The compound of  claim 14 , wherein the pharmaceutically acceptable salt of the compound is the phosphate salt. 
     
     
         16 . A pharmaceutical composition comprising the compound of  claim 10  or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. 
     
     
         17 . The pharmaceutical composition of  claim 16 , wherein, the pharmaceutically acceptable salt of the compound is the phosphate salt. 
     
     
         18 . A pharmaceutical composition comprising the compound of  claim 12  or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. 
     
     
         19 . The method of  claim 18 , wherein, the pharmaceutically acceptable salt of the compound is the phosphate salt. 
     
     
         20 . A pharmaceutical composition comprising the compound of  claim 14  or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. 
     
     
         21 . The method of  claim 20 , wherein, the pharmaceutically acceptable salt of the compound is the phosphate salt. 
     
     
         22 . A method of inhibiting the activity of one or more of JAK1 or JAK2, in a cell, comprising contacting the cell with a compound of  claim 10  or a pharmaceutically acceptable salt thereof. 
     
     
         23 . The method of  claim 22 , wherein, the pharmaceutically acceptable salt of the compound is the phosphate salt. 
     
     
         24 . A method of inhibiting the activity of one or more of JAK1 or JAK2, in a cell, comprising contacting the cell with a compound of  claim 12  or a pharmaceutically acceptable salt thereof. 
     
     
         25 . The method of  claim 24 , wherein, the pharmaceutically acceptable salt of the compound is the phosphate salt. 
     
     
         26 . A method of inhibiting the activity of one or more of JAK1 or JAK2, in a cell, comprising contacting the cell with a compound of  claim 14  or a pharmaceutically acceptable salt thereof. 
     
     
         27 . The method of  claim 26 , wherein, the pharmaceutically acceptable salt of the compound is the phosphate salt. 
     
     
         28 . A method of treating myelofibrosis, pancreatic cancer, prostate cancer, breast cancer, leukemia, non-Hodgkin's lymphoma, multiple myeloma, psoriasis, or a combination thereof in a subject in need thereof, comprising administering to the subject an effective amount of a compound represented by the following structural formula: 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof, wherein each position in the compound designated specifically as deuterium has at least 90% incorporation of deuterium. 
       
     
     
         29 . The method of  claim 28 , wherein the pharmaceutically acceptable salt of the compound is the phosphate salt.

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