US2019111025A1PendingUtilityA1

Mofezolac derivatives as multi-functions selective cox-1 inhibitors

Assignee: UNIV DEGLI STUDI DI BARI ALDO MOROPriority: Apr 27, 2016Filed: Apr 26, 2017Published: Apr 18, 2019
Est. expiryApr 27, 2036(~9.7 yrs left)· nominal 20-yr term from priority
A61K 49/00A61B 8/00C07D 413/12A61P 37/06A61K 31/7024A61K 31/415C07D 261/08C07D 413/14C07H 13/04
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Claims

Abstract

Multi-functions Selective COX inhibitors The invention relates to a new class of compounds targeting COX-1. The invention also relates to the use of some of such compounds as a tool to investigate the structure and function of the enzyme, in the treatment targeting COX-1 or detection of COX-1 in relating disorders or diseases such as cancer and neuroinflammation, in particular in neurological (e.g. autism spectrum disorders) and neurodegenerative diseases (e.g. Alzheimer's diseases, Parkinson's diseases, amyotrophic lateral sclerosis (ALS), multiple sclerosis (MS), traumatic brain injury (TBI), HIV dementia and prion diseases), and in gynecological tumour (e.g. ovarian cancer), neck and head tumor, and haematological tumours (e.g. multiple myeloma) and in the detection of COX-1 in “in vitro” (cells and tissues) and in “in vivo”.

Claims

exact text as granted — not AI-modified
1 - 35 . (canceled) 
     
     
         36 . A method of treating neuroinflammation comprising administering a compound selected from the group consisting of 
       
         
           
           
               
               
           
         
       
     
     
         37 . The method according to  claim 36 , wherein the neuroinflammation is a neurological or a neurodegenerative disease. 
     
     
         38 . The method according to  claim 37 , wherein the neurodegenerative disease is selected from the group consisting of Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis (ALS), multiple sclerosis (MS), traumatic brain injury (TBI), HIV, dementia, and prion disease. 
     
     
         39 . The method according to  claim 36 , wherein the neuroinflammation is autism. 
     
     
         40 . The method according to  claim 36 , wherein the compound is mofezolac or mofezolac methyl ester. 
     
     
         41 . The method according to  claim 36 , wherein the compound is GALMOF 0 . 
     
     
         42 . A pharmaceutical composition comprising as active principal the compound according to  claim 36  and a pharmacologically acceptable excipient and/or carrier. 
     
     
         43 . The pharmaceutical composition according to  claim 42 , wherein the compound is mofezolac or mofezolac methyl ester. 
     
     
         44 . The pharmaceutical composition according to  claim 42 , wherein the compound is GALMOF 0 .

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