title: Case study of patents related to captopril, Squibb's first blockbuster.
abstract: Arterial hypertension affects over one billion people around the world, making the prevention and treatment of this disease vital. Despite the efforts made to develop new antihypertensive drugs, few new therapies have become available. Angiotensin-converting enzyme (ACE) inhibitors have heralded major steps forward in the treatment of arterial hypertension and cardiovascular diseases since the first compound of this class, captopril, was approved for clinical use in 1981. Areas covered: In this review, the authors investigated the patent documents that cite the priority patent for captopril, Squibb's first blockbuster, or any other patent from its patent family. The documents were classified into the following: new compounds, new compositions, treatment, process (preparation of a compound), use of a compound, and process for the preparation of an intermediate. Therefore, the readers can identify potential innovations in the field. Expert opinion: The pharmaceutical sector has attempted to provide significant technological developments on anti-hypertensive drugs based on the patenting of captopril, including the development of new compositions further comprising an ACE inhibitor and other antihypertensive agent, along with dual action compounds, novel molecules with dual activity. The target is to find a new agent with better blood pressure-lowering efficacy, improved safety and good tolerability proﬁle.
authors: a Postgraduate Program in Technology of Chemical & Biochemical Processes , Federal University of Rio de Janeiro (UFRJ)/National Institute of Industrial Property, Academy of Innovation and Intellectual Property (INPI-Brazil) , Rio de Janeiro , Brazil.
authors: Adelaide Maria de Souza
authors: AM
authors: Antunes
authors: b National Institute of Industrial Property, Academy of Innovation and Intellectual Property, General Coordination of International Affairs (INPI-Brazil) , Rio de Janeiro , Brazil.
authors: Rafaela Di Sabato
authors: RD
authors: Guerrante
authors: c Federal University of the State of Rio de Janeiro, Public Administration School (UNIRIO) , Rio de Janeiro , Brazil.
authors: Jorge de Paula Costa
authors: JP
authors: Ávila
authors: d School of Chemistry (SIQUIM) , Federal University of Rio de Janeiro (UFRJ) , Rio de Janeiro , Brazil.
authors: Flavia Maria
authors: FM
authors: Lins Mendes
authors: b National Institute of Industrial Property, Academy of Innovation and Intellectual Property, General Coordination of International Affairs (INPI-Brazil) , Rio de Janeiro , Brazil.
authors: Iolanda M
authors: IM
authors: Fierro
mesh_terms: D000806:Angiotensin-Converting Enzyme Inhibitors / Q000494:pharmacology; D000959:Antihypertensive Agents / Q000494:pharmacology*; D002216:Captopril / Q000494:pharmacology*; D002318:Cardiovascular Diseases / Q000188:drug therapy / Q000503:physiopathology; D015195:Drug Design; D004345:Drug Industry; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000503:physiopathology; D010330:Patents as Topic
chemical_list: D000806:Angiotensin-Converting Enzyme Inhibitors; D000959:Antihypertensive Agents; D002216:Captopril
keywords: Hypertension; captopril; patents