36results about How to "Inhibit and reduce activity" patented technology

The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.

Biocompatible intraocular implants include a tyrosine kinase inhibitor and a biodegradable polymer that is effective to facilitate release of the tyrosine kinase inhibitor into the vitreous of an eye for an extended period of time. The therapeutic agents of the implants may be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The implants can be placed in an eye to treat or reduce the occurrence of one or more ocular conditions.

This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and / or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.

Isoform-binding molecules that specifically bind to one or more isoforms expressed and / or associated with oncogenic phenotypes in a hyperproliferative cell (e.g., a cancerous or tumor cell) are disclosed. The isoform-binding molecules can be used to treat, prevent and / or diagnose cancerous conditions and / or disorders. Methods of using the isoform-binding molecules to selectively detect oncogenic isoforms, to reduce the activity and / or induce the killing of a hyperproliferative cell expressing an oncogenic isoform in vitro, ex vivo or in vivo are also disclosed. Diagnostic and / or screening methods and kits for evaluating the function or expression of an oncogenic isoform are also disclosed.

The present invention relates to a method for screening and identifying compounds that modulate the activity of one or more components in the tRNA splicing pathway. In particular the invention relates to a method for screening and identifying compounds that modulate the activity tRNA splicing endonuclease and / or tRNA splicing ligase. The invention provides assays for the identification of compounds that inhibit animalia tRNA splicing endonuclease and / or animalia tRNA splicing ligase. The invention also provides assays for the identification of compounds that inhibit fungal tRNA splicing endonuclease and / or fungal tRNA splicing ligase. The methods of the present invention provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads useful for treating and / or preventing cancer and / or fungal infections.

The present invention relates to compositions comprising one or more viral interferon antagonists and methods of utilizing said compositions to modulate the cellular interferon immune response. In particular, the present invention relates to pharmaceutical compositions comprising one or more viral interferon antagonists and methods of utilizing said compositions to prevent, treat or ameliorate an immune disorder characterized by aberrant interferon expression and / or activity. The invention also relates to methods of treating, preventing or ameliorating the symptoms of an inflammatory disorder comprising administering to a subject in need thereof one or more viral interferon antagonist. The present invention also relates to compositions comprising fusion proteins comprising one or more viral interferon antagonists and a heterologous polypeptide, and methods of using said compositions to modulate the cellular interferon immune response. The present invention further relates to articles of manufacture comprising one or more viral interferon antagonists or fusion proteins.

The present invention relates to a method for screening and identifying compounds that modulate the activity of a fungal tRNA splicing endonuclease. In particular, the invention provides assays for the identification of compounds that inhibit or reduce the activity of a fungal tRNA splicing endonuclease. The methods of the present invention provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads useful for preventing, treating, managing and / or ameliorating a fungal infection or fungal infestation or one or more symptoms thereof.

The present invention relates to the treatment of nonalcoholic steatohepatitis (NASH), in particular to a compound that inhibits miR-21 expression for use in the treatment of nonalcoholic steatohepatitis.

The polypeptide Fortilin (also known as Translationally Controlled Tumor Protein, TCTP) specifically interacts with p53, a tumor suppressor involved in the induction of apoptosis and the normal growth regulation of a cell. Fortilin also specifically binds MCL1 (Myeloid Cell Leukemia 1). Fortilin has the ability to prevent apoptosis, which may be unregulated in hyperproliferative cells. The present invention is directed at compositions and methods involving a Fortilin modulator, which can induce apoptosis, for the prevention, treatment, or diagnosis of hyperproliferative diseases and conditions, including cancer and atherosclerosis. It is directed also at compositions and methods involving Fortilin, which can inhibit apoptosis, for the treatment of diseases and condition characterized by apoptosis, including certain vascular conditions.

This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula XVII which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and / or its interaction with its processivity factor. Formula XVII can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.

A pharmaceutical composition comprises: a) polymorphic form M or tromethamine salt of Compound (1) represented by the following structural formula:and b) a filler. A method of preparing a pharmaceutical composition comprises: providing a mixture of Compound (1) and a filler to form the composition of Compound (1). A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of the pharmaceutical composition.

Biocompatible intraocular implants include a tyrosine kinase inhibitor and a biodegradable polymer that is effective to facilitate release of the tyrosine kinase inhibitor into an eye for an extended period of time. The therapeutic agents of the implants may be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The implants may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions.

A method for enhancing or reducing photosynthetic activity, wherein non-toxic pigmented matter is applied to a photosynthetic organism. Depending on the composition of the pigmented matter, the method will have the effect of enhancing, reducing, or inhibiting photosynthetic activity.

The present disclosure generally relates to methods of treating hemolytic diseases such as sickle cell anemia using kinase inhibitors, for example, compounds that inhibit the spleen tyrosine kinase (SYK). In some embodiments a method is presented to prevent thrombosis in blood vessels of patients with a hemolytic disease comprising the step of: administrating to a patient having at least one hemolytic disease a therapeutically effective amount of at least one SYK inhibitor. In some embodiments the method includes repeatedly administering the SYK kinase inhibitor to a patient.

The present invention relates to a protein binder that binds to human iRhom2, and inhibits and / or reduces TACE / ADAM17 activity when bound to human iRhom2.

Cancer is a group of diseases involving abnormal cell growth with the potential to invade or spread to other parts of the body. In particular, hepatocellular carcinoma (HCC) has become the most common primary hepatic malignancy. Current therapies are now satisfying and there is therefore an important need for identifying new therapeutic avenues. IL-27 is a cytokine produced in liver microenvironment but its role in the pathogenesis of HCC has never been investigated. The inventors now show that IL-27 exerts anti-proliferative activities in HCC cell lines. However, the inventors show that in patients suffering from HCC that a decreased expression of WSX-1 (i.e. the IL-27 receptor) is associated with a worse prognosis and contributes to the tumor proliferation. The inventors then identified some microRNAs (miR) that are capable of repressing the expression of WSX-1 and show that overexpression of said miR are associated with a worse prognosis in patients. Finally, the inventors demonstrate that antagomirs restore the expression of WSX-1 that can thus restore the tumor cell sensitization to IL-27 properties. Accordingly, the present invention relates to methods for the treatment and prognosis of cancer, in particular hepatocellular carcinoma (HCC).

The present invention relates novel slice culture systems which provide a quick, simple, and effective tool for investigating pathological changes associated with AD. Also provided are methods of diagnosing AD and identifying potentially therapeutic compounds.

The invention relates to a transgenic non-human mammal whose cells express a constitutively active oncogenic mutant of the kinase-domain of the Raf-1 gene or a protein coded by a corresponding normal allele or derivative of the A, B, or c-Raf-1 gene.

The present invention relates to compositions and methods for regulating ROC-mediated death-associated protein kinase (DAPk) activity. The compositions and methods of the present invention are useful for treating or ameliorating cancer as well as pathologies associated with neuronal cell death, such as epilepsy and hypoxia / ischemia acute brain injury. The present invention further relates to screening methods for identifying agents that regulate ROC-mediated DAPk activation.

The present invention provides a novel inhibitor of FLT3 kinase, comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, ester, acid, metabolite or prodrug thereof. The present invention also provides a pharmaceutical composition comprising the compound of formula (I), as well as the use and method for preventing or treating FLT3-related conditions, especially conditions related to mutant FLT3 kinase (particularly, FLT3 / ITD mutant kinase).

The present invention relates to an isolated peptide, an anti-cancer medicinal composition including the same and a method of specifically reducing or inhibiting activities of cancer cells using the same. The isolated peptide including a TAT basic domain conjugated to a GABARAPL2 H2 domain can specifically reduce or inhibit an activity of cancer cells, thereby being applied to the anti-cancer medicinal composition and the method of specifically reducing or inhibiting activities of cancer cells using the same.

Polymorph Forms M, H, P, X, and ZA of Compound (1) represented by the following structural formula:are described. A method of preparing polymorph Form M of Compound (1) includes stirring a mixture of Compound (1) and a solvent system that includes isopropanol, ethyl acetate, n-butyl acetate, methyl acetate, acetone, 2-butanone (methylethylketone (MEK)), or heptane, or a combination thereof at a temperature in a range of 10° C. to 47° C. to form From M of Compound (1). A method of preparing polymorph Form H of Compound (1) includes stirring a solution of Compound (1) at a temperature in a range of 48° C. to 70° C. to form Form H of Compound (1). A method of preparing polymorph Form P of Compound (1) includes stirring a mixture of Compound (1) and a solvent system that includes a solvent selected from the group consisting of dichloromethane and tetrahydrofuran (THF), and a mixture thereof at room temperature to form Form P of Compound (1). A method of preparing polymorph Form X of Compound (1) includes removing ethyl acetate from ethylacetate solvate G of Compound (1). A method of preparing polymorph Form ZA of Compound (1) includes removing n-butyl acetate from n-butyl acetate solvate A of Compound (1).