US2023121489A1PendingUtilityA1

N-pyridinyl acetamide derivatives as wnt signalling pathway inhibitors

Assignee: REDX PHARMA PLCPriority: Oct 8, 2014Filed: Aug 29, 2022Published: Apr 20, 2023
Est. expiryOct 8, 2034(~8.2 yrs left)· nominal 20-yr term from priority
A61P 11/00A61P 13/12C07D 487/04A61K 31/519A61K 31/497A61K 2300/00A61P 25/16C07D 471/04A61P 13/02A61P 27/02A61K 45/06A61P 35/04A61P 19/02A61P 43/00A61K 31/5377A61P 35/00A61P 7/10A61P 37/06A61P 1/16A61P 17/00A61P 35/02
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Claims

Abstract

Disclosed are compounds useful as inhibitors of the Wnt signalling pathway. Specifically, inhibitors of Porcupine (Porcn) are contemplated by the invention. In addition, the invention contemplates processes to prepare the compounds and uses of the compounds. The compounds of the invention may therefore be used in treating conditions mediated by the Wnt signalling pathway, for example, in treating cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia; or enhancing the effectiveness of an anti-cancer treatment.

Claims

exact text as granted — not AI-modified
1 - 28 . (canceled) 
     
     
         29 . A method of treatment and/or prevention of a condition mediated by the Wnt signalling pathway, wherein the method comprises administering to a patient in need thereof a therapeutic amount of a compound having the formula (X): 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof. 
       
     
     
         30 . The method of  claim 29 , wherein the condition mediated by the Wnt signalling pathway is mediated by inhibition of Porcupine (Porcn). 
     
     
         31 . The method of  claim 29 , wherein the condition is selected from the group consisting of skin fibrosis, idiopathic pulmonary fibrosis, renal interstitial fibrosis, liver fibrosis, proteinuria, kidney graft rejection, osteoarthritis, Parkinson's disease, cystoid macular edema, uveitis associated cystoid macular edema, retinopathy, diabetic retinopathy and retinopathy of prematurity. 
     
     
         32 . The method of  claim 29 , wherein the condition is a fibrosis condition. 
     
     
         33 . The method of  claim 29 , wherein the condition is selected from the group consisting of skin fibrosis, idiopathic pulmonary fibrosis, pulmonary lung fibrosis, renal interstitial fibrosis and liver fibrosis. 
     
     
         34 . The method of  claim 29 , wherein the condition is idiopathic pulmonary fibrosis. 
     
     
         35 . The method of  claim 29 , wherein the compound of formula (X) is in the free base form. 
     
     
         36 . A method of treatment of idiopathic pulmonary fibrosis, wherein the method comprises administering to a patient in need thereof a therapeutic amount of a compound having the formula (X): 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof. 
       
     
     
         37 . The method of  claim 36 , wherein the compound of formula (X) is in the free base form. 
     
     
         38 . A method of prevention of idiopathic pulmonary fibrosis, wherein the method comprises administering to a patient in need thereof a therapeutic amount of a compound having the formula (X): 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof. 
       
     
     
         39 . The method of  claim 38 , wherein the compound of formula (X) is in the free base form.

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