Patent classifications
C07J5/0076
MONOMERIC AND OLIGOMERIC COMPOUND EMBODIMENTS AS CONTRACEPTIVES AND THERAPIES AND METHODS OF MAKING AND USING THE SAME
Disclosed herein are monomeric and oligomeric compound embodiments for use as contraceptive agents. Monomeric compound embodiments disclosed herein comprise substituents that facilitate the ability of the compounds to exhibit progestogenic, androgenic, and estrogenic activity, which can prevent or inhibit bone density loss in subjects. Oligomeric compound embodiments disclosed herein provide the ability to control receptor activation and/or treatment by incorporating a tunable linker group which couples steroidal-based compounds to one another or with therapeutic agents and facilitates selective cleavage of the monomeric components of the oligomeric compound.
CRYSTALLINE FORMS OF VAMOROLONE
Provided are certain polymorphic forms of vamorolone as well as pharmaceutical compositions and methods for their use.
Method for preparing 6-alkylated steroidal derivatives and corresponding alkylated 5,6,7,8-tetrahydronaphthalene-2(4 alpha.H)-ones
The present invention concerns a method for preparing certain steroidal derivatives alkylated in position 6, comprising a step of alkylating the corresponding compound halogenated in position 6 with an organometallic alkylating agent.
Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof
The present invention further provides method of preparing nanocrystals or microcrystals of a hydrophobic therapeutic agent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).
LIPID CONJUGATE PREPARED FROM SCAFFOLD MOIETY
The application relates to a lipid conjugate of formula M-X1-L wherein M is a molecule of interest such as a drug moiety; X1 is a linker group such as ester, ether or carbamate; and L is a lipid scaffold represented by formula (IId): -L1-[L2(H)(X2R)]n-L3-[L4(H)(X2R)]p-L5-L6 and wherein L comprises 5 to 40 carbon atoms and 0 to 2 carbon-carbon double bonds. The lipid conjugate can p be formulated in a drug delivery vehicle such as a lipid nanoparticle (LNP).
HETERODIMER COMPOSITIONS AND METHODS FOR THE TREATMENT OF OCULAR DISORDERS
Described herein are processable compositions comprising at least one moiety that is processable in its free form. Also described herein are compositions and methods for the treatment of ocular diseases or disorders including glaucoma, blepharitis, ocular inflammation, diabetic macular edema, posterior inflammation, anterior inflammation, macular degeneration (e.g., wet macular degeneration (AMD) or dry AMD), post-cataract surgery, and retinal vein occlusion. Said compositions and methods comprise steroids and prostaglandins which demonstrate anti-inflammatory activity, intraocular pressure (IOP) lowering, and/or other desirable activities. Injection of said compositions in the eye provides therapeutic benefit to patients suffering from ocular disorders.
DIMER COMBINATIONS AND USES THEREOF
The present invention is directed towards articles comprising a steroid material comprising a steroid dimer and at least one therapeutic agent distributed throughout the steroid material and the use of such articles in sustained release delivery systems. Said article may be fibers, fiber meshes, woven fabrics, non-woven fabrics, films, pellets, cylinders, microparticles, nanoparticles, shaped articles or coatings on a substrate (such as an implant). Control of the release profile of the at least one therapeutic agent can be achieved via selection of the steroids within the steroid dimer, the linker conjugating the steroids within the dimer, the linkage groups between the steroids and the linker, the surface area of the article, the location of the at least one therapeutic agent within the article and the amount of the at least one therapeutic agent within the article.
CRYSTALLINE FORMS OF DEXAMETHASONE DIMERS AND USES THEREOF
The disclosure features polymorphs of a prodrug dimer of dexamethasone linked at the 21-C and 21′-C carbons via a carbonate-triethylene glycol-carbonate linker. Also disclosed are pharmaceutical compositions and articles comprising said polymorphs, and the use thereof in the treatment of a disease or condition, e.g. via the extended or controlled release of dexamethasone from said articles.
HETERODIMER COMPOSITIONS AND METHODS FOR THE TREATMENT OF OCULAR DISORDERS
Described herein are processable compositions comprising at least one moiety that is processable in its free form. Also described herein are compositions and methods for the treatment of ocular diseases or disorders including glaucoma, blepharitis, ocular inflammation, diabetic macular edema, posterior inflammation, anterior inflammation, macular degeneration (e.g., wet macular degeneration (AMD) or dry AMD), post-cataract surgery, and retinal vein occlusion. Said compositions and methods comprise steroids and prostaglandins which demonstrate anti-inflammatory activity, intraocular pressure (IOP) lowering, and/or other desirable activities. Injection of said compositions in the eye provides therapeutic benefit to patients suffering from ocular disorders.
Heterodimer compositions and methods for the treatment of ocular disorders
Described herein are processable compositions comprising at least one moiety that is processable in its free form. Also described herein are compositions and methods for the treatment of ocular diseases or disorders including glaucoma, blepharitis, ocular inflammation, diabetic macular edema, posterior inflammation, anterior inflammation, macular degeneration (e.g., wet macular degeneration (AMD) or dry AMD), post-cataract surgery, and retinal vein occlusion. Said compositions and methods comprise steroids and prostaglandins which demonstrate anti-inflammatory activity, intraocular pressure (IOP) lowering, and/or other desirable activities. Injection of said compositions in the eye provides therapeutic benefit to patients suffering from ocular disorders.