US2022288078A1PendingUtilityA1

Salts of the Janus Kinase Inhibitor (R)-3-(4-(7h-Pyrrolo[2,3-D]Pyrimidin-4-YL)-1h-Pyrazol-1-Yl)-3- Cyclopentylpropanenitrile

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Assignee: INCYTE HOLDINGS CORPPriority: Jun 13, 2007Filed: Nov 29, 2021Published: Sep 15, 2022
Est. expiryJun 13, 2027(~0.9 yrs left)· nominal 20-yr term from priority
Inventors:Hui LiJames D. Rodgers
A61P 3/10A61P 31/22A61P 35/02A61P 31/20A61P 17/00A61P 31/14A61P 27/02A61P 17/08C07D 487/04A61P 1/04A61P 43/00A61P 9/00A61P 21/00A61K 31/519A61P 13/12A61P 35/04C07B 2200/13A61P 17/06A61P 9/10A61P 37/08A61P 11/00A61P 21/04A61P 17/12A61P 37/06C07B 2200/07A61P 29/00A61P 37/00A61P 37/02A61P 7/00A61P 31/12A61P 31/18A61P 19/02A61P 25/00A61P 35/00C07D 403/04A61K 9/20A61K 9/0053A61P 1/00
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Claims

Abstract

The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

Claims

exact text as granted — not AI-modified
1 - 60 . (canceled) 
     
     
         61 . A method of treating ulcerative colitis in a patient in need thereof comprising administering to said patient a therapeutically effective amount of a salt selected from:
 (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile maleic acid salt;   (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile sulfuric acid salt; and   ((R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt.   
     
     
         62 . The method of  claim 61 , wherein the salt is (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile maleic acid salt. 
     
     
         63 . The method of  claim 61 , wherein the salt is (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile sulfuric acid salt. 
     
     
         64 . The method of  claim 61 , wherein the salt is (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt. 
     
     
         65 . The method of  claim 64 , wherein (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt is a crystalline salt. 
     
     
         66 . The method of  claim 65 , wherein said crystalline salt is a 1:1 (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile:phosphoric acid salt. 
     
     
         67 . The method of  claim 61 , wherein the salt is administered as a tablet. 
     
     
         68 . The method of  claim 61 , wherein the salt is administered orally. 
     
     
         69 . A method of treating Crohn's disease in a patient in need thereof comprising administering to said patient a therapeutically effective amount of a salt selected from:
 (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile maleic acid salt;   (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile sulfuric acid salt; and   (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt.   
     
     
         70 . The method of  claim 69 , wherein the salt is (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile maleic acid salt. 
     
     
         71 . The method of  claim 69 , wherein the salt is (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile sulfuric acid salt. 
     
     
         72 . The method of  claim 69 , wherein the salt is (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt. 
     
     
         73 . The method of  claim 72 , wherein (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt is a crystalline salt. 
     
     
         74 . The method of  claim 73 , wherein said crystalline salt is a 1:1 (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt. 
     
     
         75 . The method of  claim 69 , wherein the salt is administered as a tablet. 
     
     
         76 . The method of  claim 69 , wherein the salt is administered orally.

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