US2020306275A1PendingUtilityA1

aPKC INHIBITORS AND METHODS OF TREATING A NEURODEGENERATIVE DISEASE OR DISORDER

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Assignee: FARESE ROBERT VITOPriority: Mar 25, 2016Filed: Mar 25, 2017Published: Oct 1, 2020
Est. expiryMar 25, 2036(~9.7 yrs left)· nominal 20-yr term from priority
A61P 25/28A61K 31/675C12Y 304/23046A61K 33/242A61K 31/194A61K 31/122A61K 31/28
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Claims

Abstract

Provided herein are formulations effective for and methods of treating or preventing a neurodegenerative disorder in a subject in need thereof that can include administering an amount of an aPKC inhibitor to a subject in need thereof.

Claims

exact text as granted — not AI-modified
1 . A method of treating or preventing a neurodegenerative disorder in a subject in need thereof, the method comprising:
 administering an amount of an aPKC inhibitor capable of crossing the blood brain barrier to the subject in need thereof.   
     
     
         2 . The method of  claim 1 , wherein the aPKC inhibitor is ICAPP. 
     
     
         3 . The method of  claim 1 , wherein the aPKC inhibitor is ACPD. 
     
     
         4 . The method of  claim 1 , wherein the amount of the aPKC inhibitor is an amount effective to decrease phosphorylation of PKC. 
     
     
         5 . (canceled) 
     
     
         6 . The method of  claim 1 , wherein the amount of the aPKC inhibitor is an amount effective decrease activity of β-secretase. 
     
     
         7 . The method of  claim 1 , wherein the amount of the aPKC inhibitor is an amount effective decrease the amount of Aβ 1-40/42 . 
     
     
         8 . The method of  claim 1 , wherein the amount of the aPKC inhibitor is an amount effective decrease the amount of thr-231-phospho-tau. 
     
     
         9 . The method of  claim 1 , wherein the amount of the aPKC inhibitor is an amount effective decrease the activity of 70 kDa PKC-λ/ι. 
     
     
         10 .- 12 . (canceled) 
     
     
         13 . The method of  claim 1 , wherein the subject in need thereof is hyperinsulinemic in the central nervous system. 
     
     
         14 .- 16 . (canceled) 
     
     
         17 . The method of  claim 1 , wherein the neurodegenerative disorder is Alzheimer's disease or a symptom thereof. 
     
     
         18 .- 22 . (canceled) 
     
     
         23 . A method of treating or preventing a neurodegenerative disorder in a subject in need thereof, the method comprising:
 administering systemically an amount of an aPKC inhibitor that is not capable of crossing the blood brain barrier to the subject in need thereof.   
     
     
         24 . The method of  claim 23 , wherein the aPKC inhibitor is aurothiomalate (ATM). 
     
     
         25 . The method of  claim 23 , wherein the amount of the aPKC inhibitor is an amount effective to decrease phosphorylation of PKC. 
     
     
         26 . The method of  claim 23 , wherein the amount of the aPKC inhibitor is an amount effective to decrease activity of aPKC. 
     
     
         27 . The method of  claim 23 , wherein the amount of the aPKC inhibitor is an amount effective decrease activity of β-secretase. 
     
     
         28 . The method of  claim 23 , wherein the amount of the aPKC inhibitor is an amount effective decrease the amount of Aβ 1-40/42 . 
     
     
         29 . The method of  claim 23 , wherein the amount of the aPKC inhibitor is an amount effective decrease the amount of thr-231-phospho-tau. 
     
     
         30 . The method of  claim 23 , wherein the amount of the aPKC inhibitor is an amount effective decrease the activity of 70 kDa PKC-λ/ι. 
     
     
         31 .- 33 . (canceled) 
     
     
         34 . The method of  , wherein the subject in need thereof is hyperinsulinemic in the central nervous system. 
     
     
         35 .- 37 . (canceled) 
     
     
         38 . The method of  claim 23 , wherein the neurodegenerative disorder is Alzheimer's disease or a symptom thereof. 
     
     
         39 .- 42 . (canceled)

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