Towards the ophthalmology patentome: a comprehensive patent database of ocular drugs and biomarkers.

We are currently building a database of all patent documents that contain substantial information related to pharmacology, drug delivery, tissue technology, and molecular diagnostics in ophthalmology. The goal is to establish a 'patentome', a body of cleaned and annotated data where all text-based, chemistry and pharmacology information can be accessed and mined in its context. We provide metrics on patent convention treaty documents, which demonstrate that ocular-related patenting has shown stronger growth than general patent cooperation treaty patenting during the past 25 years, and, while the majority of applications of this type have always provided substantial biological data, both data support and objections by patent examiners have been increasing since 2006-2007. Separately, we present a case study of chemistry information extraction from patents published during the 1950s and 1970s, which reveal compounds with corneal anesthesia potential that were never published in the peer-reviewed literature.

Pharmacological therapies for cataract and refractive errors: landscaping niches of ocular drug patenting.

We have used a focused and comprehensive ophthalmology patent database to characterize the international patenting landscape dedicated to the pharmacological treatment of cataract, corneal opacities and dystrophies, and complicated refractive errors. A total of 201 disclosures related to cataract or corneal clouding (published between 1982 and 2011), and 99 documents (published between 1991 and 2011) related to refractive or geometry errors were identified. Current applications for the treatment or prevention of primary cataract have ceased to address diabetic cataract specifically through the inhibition of glycation-specific mechanisms. The most innovative approaches for pharmacotherapy of the lens focus on phase separation inhibitors, modulators of the TGF-ß pathway, and matrix metalloproteinase inhibition. Patenting for the prevention of secondary cataracts as a delayed complication of intraocular lens insertion follows similar routes. For keratoconus, progressive myopia and Avellino corneal dystrophy, the focus remains on efficiently stabilizing the corrected shape of the cornea in the course of orthokeratology treatments. We expect future patenting in the fields of our investigation to concentrate more heavily on molecular medicine, in close lockstep with biotechnology and genetic testing.

Current drug patenting for retinal diseases: beyond VEGF inhibitors.

An analysis of patent applications that address strategies for the pharmacological treatment of retinal diseases that are not directly related to VEGF inhibition, published under the PCT during the 18-month period from January 2008 to June 2009, is presented. The largest number of therapeutic patent applications focused on attempts to correct visual cycle dysfunctions, complement overactivation or beta-amyloid deposition in drusen to control age-related macular degeneration (AMD). Biomarker-based and genetic diagnostic modalities that assess AMD risk were also frequently claimed in the patent applications, and have become a significant factor in patenting for ocular disorders. The fields of both visual cycle therapy and AMD biomarkers were dominated by non-corporate patent assignees. Diabetic retinopathy has not received as much attention from inventors compared with AMD; retinopathy of prematurity remains a field in which little specific patenting occurs.

International patenting in ophthalmology: An analysis of its structure and relevance for the development of drugs and diagnostics.

While investigative ophthalmologists access peer-reviewed journals as part of their daily routine, and while they regularly visit scientific congresses, they rarely peruse patent documents as an information source. Among the reasons for this negligence are the incompatibility of patent search algorithms with those known from journal databases, a legalistic and frequently redundant language, and misconceptions about the nature of the patenting system. Here we present key data and analyses from the ophthalmology module of a patent database system that we are developing to address some of these problems. We show that international patent applications consistently reflect developer interest in the ocular drug and diagnostics field; that they are technically focused lead indicators of developments that frequently feature in peer-reviewed patenting only much later; and that patenting targets are well aligned with the unmet therapeutic needs of populations in industrialized countries. Most applications (74%-78% in years since 2006) are supported with experimental data, and most (on average, 80%-90%) faced at least one objection to patentability during their initial stage of examination. In contrast to the peer-reviewed scenery that is highly diverse, the corresponding patenting arena shows a pronounced focus on the United States.