Compositions and methods for the treatment of inflammation
Inventors
Gjorstrup, Per • Schwartz, C. Eric
Assignees
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Publication Number
US-9315447-B2
Publication Date
2016-04-19
Expiration Date
Abstract
The invention relates to novel resolvin compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel resolvin compounds of the invention.
Core Innovation
The invention relates to ophthalmic pharmaceutical preparations for treating or preventing an ophthalmic condition in a human patient. The preparations comprise one or more pharmaceutically acceptable excipients together with one or more compounds selected from compounds of formulae I-IX, a compound of formula A, compounds of any one of formulae 1-49, a lipoxin compound, and/or an oxylipin compound. The preparation is characterized by the selected compound(s) being present in a concentration over 90 micromolar.
The pharmaceutical preparation is characterized as a solution with a pH in the range of 5.5 to 7.4 and/or further comprises one or more surfactants. The disclosure includes broad structural definitions, salts and esters, and multiple compound classes and formula embodiments with explicit substituent and stereochemical options.
The invention also provides methods of treating or preventing an ophthalmic condition by administering the described pharmaceutical preparation, and packaged pharmaceutical eyedrops configured for delivering the preparation to an eye in need of treatment. Dependent claim refinements describe application to dry eye.
Claims Coverage
The independent claims cover an ophthalmic pharmaceutical preparation, a method of treating or preventing an ophthalmic condition using that preparation, and a packaged eye-drop product delivering the preparation. Across the claims, the inventive features are centered on selecting specified compound formula sets, and on formulation characteristics defined by concentration over 90 micromolar and solution pH 5.5 to 7.4 and/or surfactants.
Ophthalmic pharmaceutical preparation with formula-set actives
A pharmaceutical preparation suitable for treating or preventing an ophthalmic condition in a human patient, comprising one or more of a compound of any of formulae I-IX, a compound of formula A, a compound of any one of formulae 1-49, a lipoxin compound, or an oxylipin compound, and one or more pharmaceutically acceptable excipients.
Concentration and pH characterization for ophthalmic solution
The pharmaceutical preparation is characterized in that the one or more selected compounds are present in a concentration over 90 micromolar, and the pharmaceutical preparation is a solution with a pH in the range of 5.5 to 7.4 and/or further comprises one or more surfactants.
Method using the ophthalmic pharmaceutical preparation
A method of treating or preventing an ophthalmic condition by administering a pharmaceutical preparation comprising one or more of the specified compounds and one or more pharmaceutically acceptable excipients, wherein the pharmaceutical preparation is characterized by a concentration over 90 micromolar and a solution pH in the range of 5.5 to 7.4 and/or inclusion of one or more surfactants.
Packaged ophthalmic eye drops delivering the characterized preparation
A packaged pharmaceutical for delivering eyedrops to an eye in need of treatment for an ophthalmic condition, wherein the eyedrops comprise a pharmaceutical preparation comprising one or more of the specified compounds and one or more pharmaceutically acceptable excipients, characterized by a concentration over 90 micromolar and a solution pH in the range of 5.5 to 7.4 and/or further comprising one or more surfactants.
Across the independent claims, the patent claims ophthalmic treatment and prevention using pharmaceutical preparations and eye drops containing selected compounds from specified formula sets, characterized by an active concentration over 90 micromolar and a solution pH of 5.5 to 7.4 and/or the presence of one or more surfactants.
Stated Advantages
Treating or preventing an ophthalmic condition in a human patient.
Improvement in ocular discomfort, grittiness, and dryness in a multi-center randomized placebo-controlled dry-eye study using topical compound 1001.
Documented Applications
Treating or preventing an ophthalmic condition in a human patient, including dry eye.
Delivering eyedrops to an eye in need of treatment for an ophthalmic condition using a packaged pharmaceutical.
Ocular pharmacokinetics evaluation of prodrugs/esters using compounds 1001/1002 and metabolite 1003.
Chemical stability assessment of compounds over time by HPLC.
A multi-center randomized placebo-controlled dry-eye clinical study using topical compound 1001.
Treatment or prevention of dry eye.
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