US2016058768A1PendingUtilityA1

Substituted amide compounds

35
Assignee: PFIZERPriority: Apr 17, 2013Filed: Nov 12, 2015Published: Mar 3, 2016
Est. expiryApr 17, 2033(~6.7 yrs left)· nominal 20-yr term from priority
Inventors:Etzer DaroutRobert DulleaJulie Jia Li HawkinsAllyn T. LondreganPaula M. LoriaBruce MaguireKim F. McclureDonna N. PetersenDavid W. Piotrowski
A61P 9/04A61P 3/06A61P 9/10A61P 9/00A61P 7/02A61P 3/10A61P 43/00A61P 7/00A61P 25/28A61P 3/00A61P 27/02A61P 29/00A61P 13/12C07D 487/04C07D 471/04A61K 45/06C07D 413/14A61K 31/519A61K 31/4725A61K 31/4545C07D 401/14
35
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References
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Claims

Abstract

The present invention is directed at substituted amide compounds, pharmaceutical compositions containing such compounds and the use of such compounds to reduce plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.

Claims

exact text as granted — not AI-modified
1 .- 21 . (canceled) 
     
     
         22 . A method of treating dyslipidemia by administering to a patient in need thereof a therapeutically effective amount of a compound that selectively inhibits the translation of PCSK9 mRNA to PCSK9 protein. 
     
     
         23 . The method of  claim 22  wherein the compound is administered by oral administration. 
     
     
         24 . The method of  claim 23  wherein the compound has a MW of about 300 to about 650. 
     
     
         25 . The method of  claim 23  wherein the dyslipidemia is elevated LDL. 
     
     
         26 . The method of  claim 24  wherein the therapeutically effective amount is about 1 mg to about 4000 mg per day. 
     
     
         27 . The method of  claim 24  wherein the therapeutically effective amount is about 1 mg to about 2000 mg per day. 
     
     
         28 . The method of  claim 24  wherein the therapeutically effective amount is about 50 mg to about 500 mg per day. 
     
     
         29 . The method of  claim 25  wherein the compound has an IC 50  below about 50 μM in a Cell Free PCSK9 Assay. 
     
     
         30 . The method of  claim 25  wherein the compound has an IC 50  below about 30 μM in a Cell Free PCSK9 Assay. 
     
     
         31 . The method of  claim 25  wherein the compound has an IC 50  below about 20 μM in a Cell Free PCSK9 Assay. 
     
     
         32 . The method of  claim 24  wherein the selective inhibition of PCSK9 is such that less than 1% of non-PCSK9 proteins are inhibited in a global proteomic assay. 
     
     
         33 . The method of  claim 24  wherein the selective inhibition of PCSK9 is such that less than 0.5% of non-PCSK9 proteins are inhibited in a global proteomic assay. 
     
     
         34 . The method of  claim 24  wherein the selective inhibition of PCSK9 is such that less than 0.1% of non-PCSK9 proteins are inhibited in a global proteomic assay. 
     
     
         35 .- 44 . (canceled)

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