title: HMG-CoA Reductase inhibitors: an updated review of patents of novel compounds and formulations (2011-2015).
abstract: Statins are remarkably safe and efficient medications that are the mainstay of hypercholesterolemia treatment and have proven to be an invaluable tool to lower the risk of acute cardiovascular events. These compounds are inhibitors of 3-hydroxy-methylglutaryl CoA reductase (HMG-R), the rate-limiting enzyme in cholesterol biosynthesis. In spite of their success, they present undesirable side effects and are now loosing patent protection, which provides a great opportunity for the development of new and improved statins. Areas covered: This review summarizes the new patents for HMG-R inhibitors for the 2011-2015 period. Combinations of existing statins with other drugs are also addressed, as well as novel applications of existing statins. Expert opinion: Recent efforts for the discovery of HMG-CoA-R inhibitors has resulted in several new molecules. Most of these are based on commercially available statins, including sterol and terpenoid derivatives. A few peptides have also been patented. However, the origin of the side effects caused by previous statins continues to be, to a large extent, unknown. Although the patents published in the past 5 years are promising, and might result in new drugs, there is still no way to know if they will present reduced toxicity. Only future clinical trials will answer this question.
authors.affiliation: a UCIBIO@REQUIMTE, Departamento de Química e Bioquímica, Faculdade de Ciências , Universidade do Porto , Porto , Portugal.
authors.forename: Eduardo Filipe
authors.initials: EF
authors.lastname: Oliveira
authors.affiliation: a UCIBIO@REQUIMTE, Departamento de Química e Bioquímica, Faculdade de Ciências , Universidade do Porto , Porto , Portugal.
authors.forename: Diogo
authors.initials: D
authors.lastname: Santos-Martins
authors.affiliation: a UCIBIO@REQUIMTE, Departamento de Química e Bioquímica, Faculdade de Ciências , Universidade do Porto , Porto , Portugal.
authors.forename: António Meireles
authors.initials: AM
authors.lastname: Ribeiro
authors.affiliation: a UCIBIO@REQUIMTE, Departamento de Química e Bioquímica, Faculdade de Ciências , Universidade do Porto , Porto , Portugal.
authors.forename: Natércia Fernandes
authors.initials: NF
authors.lastname: Brás
authors.affiliation: a UCIBIO@REQUIMTE, Departamento de Química e Bioquímica, Faculdade de Ciências , Universidade do Porto , Porto , Portugal.
authors.forename: Nuno Sousa
authors.initials: NS
authors.lastname: Cerqueira
authors.affiliation: a UCIBIO@REQUIMTE, Departamento de Química e Bioquímica, Faculdade de Ciências , Universidade do Porto , Porto , Portugal.
authors.forename: Sérgio Filipe
authors.initials: SF
authors.lastname: Sousa
authors.affiliation: a UCIBIO@REQUIMTE, Departamento de Química e Bioquímica, Faculdade de Ciências , Universidade do Porto , Porto , Portugal.
authors.forename: Maria João
authors.initials: MJ
authors.lastname: Ramos
authors.affiliation: a UCIBIO@REQUIMTE, Departamento de Química e Bioquímica, Faculdade de Ciências , Universidade do Porto , Porto , Portugal.
authors.forename: Pedro Alexandrino
authors.initials: PA
authors.lastname: Fernandes
mesh_terms: D000818:Animals; D002318:Cardiovascular Diseases / Q000517:prevention & control; D015195:Drug Design; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D006937:Hypercholesterolemia / Q000150:complications / Q000188:drug therapy*; D010330:Patents as Topic
chemical_list: D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors
keywords: HMG-R; Statins; cardiovascular diseases; formulations; new chemical entities; sterols; terpenoids