Abstract: Responsive or degradable branched polymers may be prepared by the free radical polymerisation of a multivinyl monomer in the presence of a chain transfer agent, using a source of radicals, wherein the extent of propagation is controlled relative to the extent of chain transfer to prevent gelation of the polymer. The multivinyl monomer may comprise a cleavable group, for example an ester, or a multiplicity of such groups, between two vinyl groups. Said monomer may be a macromonomer containing multiple cleavage sites.

Abstract: Two enantiomers of a SElective Glucocorticoid Receptor Agonistic Modulator (SEGRAM) of Formula 1 or a derivative thereof; to a deuterated form of a SEGRAM of Formula 1 or a derivative thereof; and to the two deuterated enantiomers of a SEGRAM of Formula 1 or a derivative thereof: or a pharmaceutically acceptable salt, solvate and/or prodrug thereof. The present invention also relates to a SEGRAM of Formula 1 or a derivative thereof, or a pharmaceutically acceptable enantiomer, deuterated form, salt, solvate and/or prodrug thereof, for use in the prevention or treatment of an inflammatory disorder in a subject in need thereof.

Abstract: Two enantiomers of a SElective Glucocorticoid Receptor Agonistic Modulator (SEGRAM) of Formula 1 or a derivative thereof; to a deuterated form of a SEGRAM of Formula 1 or a derivative thereof; and to the two deuterated enantiomers of a SEGRAM of Formula 1 or a derivative thereof: or a pharmaceutically acceptable salt, solvate and/or prodrug thereof. The present invention also relates to a SEGRAM of Formula 1 or a derivative thereof, or a pharmaceutically acceptable enantiomer, deuterated form, salt, solvate and/or prodrug thereof, for use in the prevention or treatment of an inflammatory disorder in a subject in need thereof.

Abstract: Particles comprising a branched polymer and either a block copolymer or a linear dendritic hybrid represent a category of useful materials. They may be used in for example drug delivery applications. They may be prepared by a method comprising the steps of: dissolving the branched polymer and block copolymer or linear dendritic hybrid, and optionally other component(s), in a solvent to form a solution; adding said solution to a different liquid; and removing said solvent to form a dispersion of co-precipitated particles.

Abstract: A method of preparing a branched polymer comprises the free radical polymerisation of a multivinyl monomer in the presence of a chain transfer agent, using a source of radicals, wherein the extent of propagation is controlled relative to the extent of chain transfer to prevent gelation of the polymer. The average length of each vinyl polymer chain within the product is short.

Abstract: A method of preparing a polymer comprises the use of free radical vinyl polymerisation to form carbon-carbon backbone segments of the polymer, wherein the longest chains in the polymer comprise vinyl polymer chains interspersed with other chemical groups and/or chains. The product has the characteristics of a step-growth polymer comprising a mixture of polyfunctional step-growth monomer residues formed by vinyl polymerization.

Abstract: Particles comprising a branched polymer and either a block copolymer or a linear dendritic hybrid represent a category of useful materials. They may be used in for example drug delivery applications. They may be prepared by a method comprising the steps of: dissolving the branched polymer and block copolymer or linear dendritic hybrid, and optionally other component(s), in a solvent to form a solution; adding said solution to a different liquid; and removing said solvent to form a dispersion of co-precipitated particles.

Abstract: An oil-in-water emulsion comprises an emulsifier which is a non-gelled branched polymer (e.g. a branched vinyl polymer), wherein the ends of at least some of the chains of said polymer terminate in an alkyl chain of 5 carbon atoms or more, and wherein the oil-in-water emulsion takes the form of particles having a z-average diameter of no greater than about 1000 nm. This is useful in, for example, facilitating the carrying of hydrophobic materials within aqueous systems, to enhance oral drug delivery. The oil-in-water emulsion may be prepared by mixing an oil phase with an aqueous phase in the presence of an emulsifier, wherein said emulsifier is a non-gelled branched polymer, wherein the ends of at least some of the chains of said polymer terminate in an alkyl chain of 5 carbon atoms or more, and wherein the oil-in-water emulsion takes the form of particles having a z-average diameter of no greater than about 1000 nm.

Abstract: Disclosed are two enantiomers of a SElective Glucocorticoid Receptor Agonistic Modulator (SEGRAM) of Formula 1 or a derivative thereof; to a deuterated form of a SEGRAM of Formula 1 or a derivative thereof; and to the two deuterated enantiomers of a SEGRAM of Formula 1 or a derivative thereof: or a pharmaceutically acceptable salt, solvate and/or prodrug thereof. Also disclosed is a method for preventing or treating an inflammatory disorder for treating including administering to a subject in need thereof a SEGRAM of Formula 1 or a derivative thereof, or a pharmaceutically acceptable enantiomer, deuterated form, salt, solvate and/or prodrug thereof.

Abstract: Branched polyesters carrying dendrons are a useful class of nanomaterials which exhibit good handling properties and stability, can degrade to a high extent, and are effective encapsulation materials. They can be used to make nanoprecipitated particles which may for example be used in therapy. Furthermore, these materials can be synthesised by economical and tailorable processes. The materials can be prepared by the ring-opening polymerisation (ROP) of mono-functional lactone monomers and difunctional lactone monomers, using dendron initiators.

Abstract: An oil-in-water emulsion comprises an emulsifier which is a non-gelled branched polymer (e.g. a branched vinyl polymer), wherein the ends of at least some of the chains of said polymer terminate in an alkyl chain of 5 carbon atoms or more, and wherein the oil-in-water emulsion takes the form of particles having a z-average diameter of no greater than about 1000 nm. This is useful in, for example, facilitating the carrying of hydrophobic materials within aqueous systems, to enhance oral drug delivery. The oil-in-water emulsion may be prepared by mixing an oil phase with an aqueous phase in the presence of an emulsifier, wherein said emulsifier is a non-gelled branched polymer, wherein the ends of at least some of the chains of said polymer terminate in an alkyl chain of 5 carbon atoms or more, and wherein the oil-in-water emulsion takes the form of particles having a z-average diameter of no greater than about 1000 nm.

Abstract: Particles comprising a branched polymer and either a block copolymer or a linear dendritic hybrid represent a category of useful materials. They may be used in for example drug delivery applications. They may be prepared by a method comprising the steps of: dissolving the branched polymer and block copolymer or linear dendritic hybrid, and optionally other component(s), in a solvent to form a solution; adding said solution to a different liquid; and removing said solvent to form a dispersion of co-precipitated particles.

Abstract: A method of preparing a non-gelled branched vinyl polymer scaffold carrying dendrons, comprising the living or controlled polymerization of a monofunctional vinyl monomer and a difunctional vinyl monomer, using a dendron initiator and at least one further initiator.

Abstract: The present invention relates to a method for tightly temporally controlling the biological activity of a protein of interest in a vertebrate, upon induction of the activity of a fusion protein comprising said protein of interest and an ERM polypeptide containing a mutated ligand binding domain of the human oestrogen receptor ?, with a synthetic ligand that does not interfere with oestrogen signalling. In particular, the present invention concerns a method for generating tightly temporally-controlled targeted somatic mutations in a vertebrate, preferably a mouse, by inducing the activity of a fusion protein comprising a site-specific recombinase protein and an ERM polypeptide, with a synthetic ligand devoid of oestrogenic and anti-oestrogenic activities.

Abstract: The present invention relates to a new process for identifying novel anti-inflammatory molecules with reduced direct transrepression of genes induced by glucocorticoids. The inventors have discovered that GCs-mediated transrepression can be mediated not only via the tethering indirect pathway, but also through direct binding of GR to “simple” negative GREs (nGRE), which belongs to a novel family of evolutionary-conserved cis-acting negative response elements (IR nGREs), and are found in numerous GC-repressed genes.

Abstract: The present invention relates to a method for tightly temporally controlling the biological activity of a protein of interest in a vertebrate, upon induction of the activity of a fusion protein comprising said protein of interest and an ERM polypeptide containing a mutated ligand binding domain of the human oestrogen receptor ?, with a synthetic ligand that does not interfere with oestrogen signalling. In particular, the present invention concerns a method for generating tightly temporally-controlled targeted somatic mutations in a vertebrate, preferably a mouse, by inducing the activity of a fusion protein comprising a site-specific recombinase protein and an ERM polypeptide, with a synthetic ligand devoid of oestrogenic and anti-oestrogenic activities.

Abstract: The present invention concerns a method for generating a human atopic disease-like phenotype, preferably an atopic dermatitis (AD)-like phenotype in a mammal comprising administering to said mammal at least one compound selected in the group comprising the physiologically active vitamin D3 (1?,25(OH)2D3) and agonistic analogs thereof. The present invention also concerns a method for treating and/or preventing an atopic disease in a patient in a patent comprising administrating to said patient an effective amount of at least one vitamin D3 antagonist.

Abstract: The invention relates to a microparticulate form of 1-[2-(2-naphthyl)-ethyl]-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine hydrochloride consisting of particles for which at least 55% of the population have a diameter below 50 micrometers, and to pharmaceutical compositions in which it is present.

Abstract: Process for the production of a superhydrophobic fibrous substrate. The process involves preparing hydrophobic core-shell microparticles, the microparticles having a core of polyurethane and a shell of polydimethylsiloxane or of polybutadiene, then depositing a liquid suspension of the microparticles on the fibrous substrate. Superhydrophobic fibrous substrates of this kind are useful for the manufacture of textiles intended for apparel, or of coatings for printing.

Abstract: The invention relates to a microparticulate form of 1-[2-(2-naphthyl)-ethyl]-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine hydrochloride consisting of particles for which at least 55% of the population have a diameter below 50 micrometers, and to pharmaceutical compositions in which it is present.