Patent Picks—Suprametallogels, Detecting Analytes, Vibroturbilization and Other R&D Processes

Patent Picks are compiled by the editors from publicly available sources. This edition features inventions related to processes and methods of forming suprametallogels, synthesizing stable resveratrol, detecting target analytes, surface-treating calcium carbonate, processing dispersed systems, enhancing dermal penetration, temporarily dyeing hair and more.

Forming suprametallogels
WIPO Patent Application WO/2015/120391
Publication date: Aug 13, 2015
Assignee: Massachusetts Institute of Technology

This patent describes nanostructures, e.g., nanospheres and nano-paddlewheels, formed through transition metal-ligand coordination and junction self-assembly, and connected by divalent linkers Y. These complexes are able to form gels, e.g., hydrogels, which exhibit excellent mechanical properties reportedly without sacrificing self-healing; they also show high robustness and storage modulus. These may be useful in delivering an agent to a subject, tissue or cell and in treating disease.

Forms for topical and/or transdermal administration may include ointments, pastes, creams, lotions, gels, powders, solutions, sprays, inhalants and/or patches. They can be prepared, for example, by dissolving and/or dispensing the active ingredient in the proper medium. Alternatively or additionally, the rate can be controlled by providing a rate-controlling membrane and/or by dispersing the active ingredient in a polymer matrix and/or gel. Generally, the active ingredient is admixed under sterile conditions with a carrier or excipient and/or any needed preservatives and/or buffers.

Synthesizing stable resveratrol salicylates
WIPO Patent Application WO/2015/120153
Publication date: Aug. 13, 2015
Assignee: Biocogent LLC, J.D. Ceccoli, M.L. Ingrassia, C.M. Judd and B.R. Costello

As is generally known, resveratrol is relatively unstable, thus there exists a need for improved methods for synthesizing it as well as compounds containing it. This invention relates, in particular, to methods of synthesizing resveratrol salicylates. One method consists of: a) activating resveratrol in the presence of a first solvent to produce activated resveratrol; b) activating salicylic acid in the presence of a second solvent to produce activated salicylic acid; and c) combining the activated resveratrol and the activated salicylic acid to produce a resveratrol salicylate mixture.

Another method involves synthesizing a mixture of mono-, di-, tri- or poly-substituted resveratrol salicylates by: a) combining activated salicylic acid with activated resveratrol in one or more solvents; and b) controlling the ratio or percentage of di-, tri- or poly-substituted resveratrol by controlling the molar ratio of activated salicylic acid to activated resveratrol.

Improving the detection of target analytes
WIPO Patent Application WO/2015/120147
Publication date: Aug. 13, 2015
Assignee: Scanogen Inc.

As this patent explains, when using known detection systems such as immunoassays, the ability to detect a target analyte is often limited by the low concentration of the analyte in the sample and by nonspecific interactions, such as binding of signal-producing molecules and sample molecules. Accordingly, there is a need for methods of detecting low concentrations of target analytes while distinguishing non-specific binding from specific binding in the sample. The present invention meets these objectives using a complex formed by a target and first and second probes, wherein the complex comprises an elongated region, a particle that is coupled to the first probe and a solid support that is coupled to the second probe. Specific binding of a target analyte can be distinguished from non-specific binding of the particle by measuring the displacement of the particle.

Surface-treating calcium carbonate
WIPO Patent Application WO/2015/120007
Publication date: Aug. 13, 2015
Assignee: Sensient Colors LLC

To render calcium carbonate useful in a range of personal care products, it is treated with a hydrophobic material. Current compounds used include lauroyl lysine, natural flower waxes and glutamate cysteine arginine. According to the inventors, however, these compounds only provide a physical surface treatment and do not bind to the calcium carbonate. Other surface treatments, such as hydrogenated lecithin, will bind to the particles but require water to apply the treatment.

Described here is a process that includes: a) wetting calcium carbonate particles slowly with water so the water is evenly blended into them, forming a smooth and homogeneously wetted surface; then b) quickly blending the surface treatment material into the water and calcium carbonate mixture to form a surface treated calcium carbonate particulate material. In one example, the calcium carbonate is surface-treated with a hydrophobic compound such as a trialkoxyalkylsilane, i.e., triethoxycaprylylsilane, fluoro high purity ammonium C6-16 perfluoroalkyl phosphate, or dimethicone trimethylsiloxysilane.

Vibroturbilization for processing dispersed systems
WIPO Patent Application WO/2015/119652
Publication date: Aug. 13, 2015
Assignee: L. Amusin

According to this patent, in chemical engineering, cavitation is often used to homogenize or mix and break down dispersed phase (particles) in a colloidal liquid compound. This approach tends to require expensive or complicated equipment. Also, depending on the application, the time it takes for a cavitation-related process to be completed can be the bottleneck in an industrial method. In response, disclosed here is a system and method designed for processing dispersed systems, wherein the dispersed system is processed in a reactor attached to a vibration unit and one or more supply lines for gases and liquids.

Vibroturbulization initially may look like cavitation. However, here an impact pseudo-boil forms a substantially homogeneous liquid-gas system that fills the internal volume of a sealed chemical apparatus when, under certain low-frequency vibration conditions, a dispersed liquid interacts with a dispersed gas. Thus, the use of vibroturbulization could make it possible to simplify many processes in applied technology and, at the same time, intensify them.

Enhancing transdermal penetration
WIPO Patent Application WO/2015/118512
Publication date: Aug. 13, 2015
Assignee: Troikaa Pharmaceuticals Ltd.

This invention relates to topical formulations including salts of the drug heparin that enhance its transdermal penetration. Clear, non-sticky liquid formulas containing the drug are described, which are suitable for administering the drug in the form of a solution or a spray. Further, the formulas do not form flaky or gel-like films on skin surface upon topical application. Specifically, the formulas comprise: 50 to 2500 IU/mL of pharmaceutically acceptable salts of heparin; less than or equal to 30% v/v of water; 10% to 30% v/v of a lower chain alcohol; and a water miscible vehicle selected from a group comprising: propylene glycol, glycerol, glycofurol, polyethylene glycols or mixtures thereof. The formulations are presented as "ready-for-absorption" and do not require partitioning of the drug from one phase to the other phase in the formulation, providing rapid penetration through the skin.

Penetrating skin with HMW anti-inflammatory agent
WIPO Patent Application WO/2015/118320
Publication date: Aug. 13, 2015
Assignee: Ziarco Pharma Limited

Diclosed in this patent is a pharmaceutical composition for topical administration comprising the high molecular weight (HMW) compound 3-{4-[2-{5-chloro-1-(diphenylmethyl)-2-[2-({[2- (trifluoromethyl)benzyl]sulfonyl}amino)ethyl]-1H-indol-3- yl}ethyl]sulfonyl}phenyl}propanoic acid or pharmaceutically acceptable salts thereof, and its use for treating inflammation. Previous research teaches that compounds with low molecular weight (< 500 daltons) and moderate log P (0-3) are ideal for this use; however, the present inventors have surprisingly found this compound, an inhibitor of cPLA2a developed for oral administration, to be efficacious and well-tolerated when delivered as part of a composition for topical administration.

Temporarily modifying keratin color
WIPO Patent Application WO/2015/118276
Publication date: Aug. 13, 2015
Assignee: BBR

This invention relates to a composition capable of temporarily modifying hair color, containing: a) a cosmetically acceptable solvent comprising at least one alcohol; b) at least one pigment chosen from metal oxides and hydroxides, in particular iron(II) or (III) oxides and hydroxides, and mixtures of at least two of these; mixtures of at least one iron(II) or iron(III) oxide with at least one iron(II) or iron(III) hydroxide; and mixtures of at least one iron(II) or iron(III) oxide and/or at least one iron(II) or (III) hydroxide with titanium dioxide; and c) at least one polymer for fixing said pigment. According to the inventors, the resulting liquid is capable of giving hair a natural color and of covering white hair.

This invention also relates to a process for temporarily dyeing the hair, with a view to giving it a natural color, according to which a solution containing at least one pigment, one polymer fixing said pigment and one cosmetically acceptable solvent is sprayed onto hair.

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