56results about "Cyclosporins" patented technology

The present invention relates to solid state forms of lenicortafusp (RCF), pharmaceutical compositions comprising the solid state forms and methods of manufacturing pharmaceutical dosage forms utilizing the solid state forms.

This disclosure provides methods and reagents useful for analyzing protein-protein interfaces, such as the interface between a presenter protein (e.g., a member of the FKBP family, a member of the cyclophyllin family, or PIN1) and a target protein. [Solution] In some embodiments, the target and / or presenter protein is an intracellular protein. In some embodiments, the target and / or presenter protein is a mammalian protein.

The present invention belongs to the technical field of drug synthesis. In particular, the present invention relates to a method for preparing salts of isocyclosporin A, in particular a method for preparing salts of isocyclosporin A by transesterification of cyclosporin A.

Compositions are disclosed that include acridinium esters of cyclosporin A or C. Kits containing same, as well as methods of making and using same, are also disclosed.

The present disclosure provides compounds defined by Formulae 1-6 and their use as cyclophilin inhibitors for the prevention or treatment of a disease or disorder, such as a cyclophilin-mediated disease or disorder, in particular a cyclophilin A-mediated disease or disorder.

To provide a new molecular modality capable of modulating the function of an undruggable target.SOLUTION: A compound (e.g., a macrocyclic compound comprising 14 to 40 ring atoms as shown below) capable of modulating a biological process by binding to presenter proteins (e.g., members of the FKBP family, members of the cyclophilin family, or PIN1) and target proteins (e.g., eukaryotic target proteins such as mammalian target proteins or fungal target proteins or prokaryotic target proteins such as bacterial target proteins).SELECTED DRAWING: None

The present disclosure relates to solid state forms of Voclosporin and salts thereof, processes for preparation thereof and pharmaceutical compositions thereof.

A method of treating or preventing a Coronaviridae infection in a subject comprising administrating a therapeutically effective amount of a compound of Formula (I) or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and the Coronaviridae comprises at least one selected from 2019-nCov virus, HCov 229E virus, SARS virus, MERS virus, (I).

Provided herein is Compound I or a pharmaceutically acceptable salt thereof for use in the prevention and / or treatment of a kidney condition or disease in a subject exposed to a nephrotoxin capable of inducing said kidney condition or disease.

This invention relates to the field of insect control, specifically to the Paecilomyces lilacinus strain XI-5, and the extraction and identification of crude toxins produced by secondary metabolites of Paecilomyces lilacinus strain XI-5. This invention confirms that the secondary metabolites of Paecilomyces lilacinus strain XI-5 produce cyclosporine C. Cyclosporine C has a stomach poison effect on adult whiteflies. Twenty-four hours after application, the LC50 concentration of cyclosporine C against adult whiteflies was 31.75 µg / ml; compared to the control group, the LC30 concentration of cyclosporine C resulted in a decrease in oviposition / fertility in female whiteflies.

Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.

Compounds defined by Formula 4 are used as cyclophilin inhibitors for the prevention or treatment of diseases or disorders, in particular diseases or conditions associated with cellular injury or cell death, such as organ injury or organ failure, which can be caused by a number of different reasons, such as ischemia or ischemia reperfusion injury, toxins, infection or mechanical trauma.

Disclosed herein are particles including a position 3-substituted cyclosporine derivative and a biodegradable polymer, a controlled-release composition for topical injection including the same, and use of the same for prevention of hair loss and promotion of hair growth.

This article discloses cyclosporine compounds and methods for treating or preventing neutrophil-mediated inflammation, wherein the compounds inhibit the activity of MRP2 and FPR1.

The invention relates to a process for the preparation of an intermediate useful for the synthesis of voclosporin, an immunosuppressant active ingredient inhibitor of calcineurin.

Compounds defined by Formula 4 are used as cyclophilin inhibitors for the prevention or treatment of diseases or disorders, such as organ injury or organ failure.

This invention relates to solid state forms of Rencofilstat (RCF), pharmaceutical compositions comprising the same, and methods of manufacturing pharmaceutical dosage forms utilizing the same.

Disclosed herein are cyclosporine compounds and methods for use in the treatment or prevention of neutrophil-mediated inflammation, wherein the compounds inhibit the activity of MRP2 and FPRL.

The invention relates to a method for preparing a cyclised peptide from a modified peptide comprising an acyl azide group; the use of the method to prepare a library of two or more cyclised peptides; and to a library of cyclised peptides prepared using the method.

Compounds as defined by Formulas 1-6 and uses thereof for as cyclophilin inhibitors, for the prevention or treatment of diseases or conditions such as cyclophilin-mediated diseases or conditions, in particular, cyclophilin A-mediated diseases or conditions.

An objective of the present invention is to provide methods of producing a cyclic organic compound using a continuous stirred tank reactor(s) (CSTR), the methods being capable of achieving excellent impurity-suppressing effects (quality improvement), reduction in reaction-tank size, continuous production, and such. The present inventors conducted studies on cyclization reactions using a CSTR(s), which had not been conventionally used for cyclization reactions for cyclic compounds. As a result, the inventors have found that the present methods can achieve excellent impurity-suppressing effects (quality improvement), reduction in reaction-tank size, continuous production, and such, as compared with conventional cyclization methods. Furthermore, the present inventors have also found that the above-mentioned improvement effects can efficiently be achieved even in the production of cyclic peptides and heterocyclic compounds by applying simulation methods that had been conventionally used mainly at the fine chemicals plant level to the cyclization reactions of the present invention, thereby experimentally predicting the reaction rate of a cyclization reaction, and setting the flow volume (residence time), the concentrations of precursor and cyclic organic compound, and the temperature for the cyclization reaction and such which affect these conditions, in the cyclization reaction using a CSTR(s).

The invention provides for Compound I or a pharmaceutically acceptable salt thereoffor use in the prevention and / or treatment of a kidney condition or disease in a subject exposed to a nephrotoxin capable of inducing said kidney condition or disease.

The present invention belongs to the technical field of drug synthesis. In particular, the present invention relates to a method for preparing salts of isocyclosporin A, in particular a method for preparing salts of isocyclosporin A by transesterification of cyclosporin A.

Provided herein is Compound I or a pharmaceutically acceptable salt thereof for use in the prevention and / or treatment of a kidney condition or disease in a subject exposed to a nephrotoxin capable of inducing said kidney condition or disease.

The invention features compounds (e.g., macrocyclic compounds) capable of modulating biological processes, for example through binding to a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein (e.g., a eukaryotic target protein such as a mammalian target protein or a fungal target protein or a prokaryotic target protein such as a bacterial target protein). These compounds bind endogenous intracellular presenter proteins, such as the FKBPs or cyclophilins, and the resulting binary complexes selectively bind and modulate the activity of intracellular target proteins . Formation of a tripartite complex among the presenter protein, the compound, and the target protein is driven by both protein-compound and protein-protein interactions, and both are required for modulation of the targeted protein's activity. In some embodiments, the compounds of the invention "re-program" the binding of the presenter proteins to protein targets that either do not normally bind to the presenter protein (e.g., do not show detectable binding in mammalian cells absent the compound). In some embodiments, provided compounds "re-program" presenter protein binding to greatly enhance interaction with a particular target with which it may have some interaction absent the compound. Interactions achieved through such reprogramming result in an ability to modulate the activity of these new targets.