[Patentability of an antibody: evolution of rules and practices and prospects]. / Brevetabilité d'un anticorps - Évolution des règles et des pratiques et perspectives.

TITLE: Brevetabilité d'un anticorps - Évolution des règles et des pratiques et perspectives. ABSTRACT: Les anticorps monoclonaux représentent aujourd'hui la classe médicamenteuse la plus importante en termes de ventes mondiales. L'obtention d'une protection par brevet de ces molécules est donc cruciale. Une dynamique active de dépôts de demandes de brevets pour protéger les inventions que ces molécules représentent existe donc autant dans l'industrie que dans le monde de la recherche académique. Cependant, les demandeurs doivent faire face à des difficultés récurrentes pour obtenir des brevets de portée importante et faire valoir leurs droits devant les tribunaux. Les trois critères les plus débattus autour des revendications d'anticorps sont : la suffisance/clarté de l'invention, la nouveauté et l'activité inventive. L'objectif de cet article est donc de faire un état des lieux de la pratique en la matière.

Mineralocorticoid receptor antagonists: a patent evaluation of US20150284376A1.

INTRODUCTION: Recent clinical studies showed that mineralocorticoid receptor antagonists are able to markedly reduce the overall and cardiovascular mortality in patients with left ventricular systolic dysfunction and mild or severe symptoms of chronic heart failure (HF). Beyond cardiac diseases, new indications of MRAs increase exponentially, especially in patients with impaired renal function. Most of the developed mineralocorticoid receptor antagonists are now non-steroidal. Identifying so-called "kidney friendly" compounds (i.e. with less renal potassium sparing properties as compared to classical steroidal MRA and therefore better safety profile in at-risk patients) would represent a clear breakthrough and many companies have developed intense patent activities in the field. Area covered: The present article provides an analysis of US20150284376 patent application which discloses non-steroidal compounds. Expert opinion: Of US20150284376 discloses a new class of MRA for which it is too early for determining the relevance in the absence of preclinical studies.

Immune checkpoint inhibitors: a patent review (2010-2015).

INTRODUCTION: Immune checkpoint inhibitors, like anti-PD-1/PD-L1 antibodies, are revolutionizing therapeutic concepts in the treatment of cancer. Said class of drugs will represent a multi-billion dollar market over the coming decade. Many companies have therefore developed important patent activities in the field. AREAS COVERED: The present review gives an overview of the patent literature during the period 2010-2015 in the field of immune checkpoint inhibitors. In particular, the review presents a selection of international patent applications related to inhibitors of PD-1/PD-L1, CTLA-4, IDO, TIM3, LAG3, TIGIT, BTLA, VISTA, ICOS, KIRs and CD39. EXPERT OPINION: Immune checkpoint inhibitors are now widely accepted as a key component of the therapeutic strategies in cancer. This fervent activity creates a maze of third-party patents that pose considerable risks for both newcomers and established companies. We can thus anticipate that the number of patent conflicts and disputes will increase in the near future. Treatments will involve combination therapy comprising at least one immune checkpoint inhibitor and companies will multiply patent filings in this field. Finally, we can expect that patents related to biomarkers that will render a patient eligible to a treatment with an immune checkpoint inhibitor will have tremendous commercial value.

Mineralocorticoid receptor modulators: a patent review (2007 - 2012).

INTRODUCTION: Considered for years as a 'renal hormone' leading to the control of renal excretion of minerals (explaining the term 'mineralocorticoid' used to describe this hormone), aldosterone is now recognized as a key factor in several diseases including hypertension, heart failure, arrhythmia, metabolic and kidney diseases, to cite only a few of them. AREAS COVERED: In this review article, the authors aim to cover information provided by patents of the years 2007 through 2012. The rationale of writing this article is to cover the most important patents that can progress the field with new important discoveries. EXPERT OPINION: The recognition of its proinflammatory and fibrogenic effects and the discovery of extrarenal sites of expression of its receptor (the mineralocorticoid receptor or MR) support a broader implication in diseases of MR activation than previously anticipated and the possible novel therapeutic indications of MR antagonists.

Strategies for proprotein convertase subtilisin kexin 9 modulation: a perspective on recent patents.

IMPORTANCE OF THE FIELD: Proprotein convertase subtilisin kexin 9 (PCSK9) is a new actor discovered in 2003 that is implicated in autosomal dominant hypercholesterolemia, cholesterol homeostasis and coronary heart disease. It has been shown to degrade the low-density lipoprotein (LDL) receptor independently of its catalytic activity. Several pharmacological strategies to reduce PCSK9 are being thoroughly investigated. AREAS COVERED IN THIS REVIEW: This article reviews all different strategies that are presently pursued to modulate the functional activity of PCSK9 which is a prime target for controlling LDL-cholesterol. It also provides a briefing of all the patents up to July 2010 from various organizations including pharmaceutical companies and academic institutions that have been submitted and/or approved. WHAT THE READER WILL GAIN: This review is addressed to researchers from academia and pharmaceutical companies who are engaged in PCSK9 research/cholesterol regulation and in the development of cholesterol lowering drugs. Readers will gain an up-to-date overview of the different strategies that have been investigated to reduce PCSK9 including antisense technology and specific antibodies. TAKE HOME MESSAGE: Clinical trials have been launched using RNA interference approaches to reduce PCSK9 expression or specific antibodies targeting and inhibiting PCSK9 interaction with the LDL receptor. They constitute very promising approaches to reducing cholesterol levels and coronary heart disease.