59 results about "HDAC6" patented technology

The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I:

where R, L, X¹, X², X³, X⁴, Y¹, Y², Y³, and Y⁴ are described herein.

The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I:

where R, L, X¹, X², X³, X⁴, Y¹, Y², Y³, and Y⁴ are described herein.

The invention relates to histone deacetylase (HDAC) biomarkers in multiple myeloma. Specifically, the biomarkers are drug specific, histone deacetylase (HDAC) or HDAC6 biomarker RNAs for multiple myeloma. The invention also relates to a kit for determining the treatment efficiency of a HDAC6 inhibitor, and a kit for identifying a histone deacetylase 6 (HDAC6) inhibitor. The invention further relates to a method for monitoring treatment efficiency of an HDAC inhibitor in a subject.

The present invention is directed to substituted 5-trifluoromethyl oxadiazole compounds of generic formula (I) or a pharmaceutically acceptable salt thereof. In particular, the invention is directed to a class of aryl and heteroaryl substituted 5-trifluoromethyl oxadiazole compounds of formula I which may be useful as HDAC6 inhibitors for treating cellular proliferative diseases, including cancer, neurodegenerative diseases, such as schizophrenia and stroke, as well as other diseases.

Provided are compounds having HDAC6 modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by HDAC6.

The invention provides an application of inhibitor of histone deacetylase HDAC 6 in preparing drugs for preventing and treating acute kidney injury. Furthermore, the histone deacetylase HDAC 6 is Tubastatin A. The selective inhibitor of HDAC 6 can lighten the renal pathology damage of acute kidney injury induced by cis-platinum and improve the kidney function. The HDAC6 inhibitor TA can lower the release of inflammatory factors and lighten the oxidative stress reaction through regulating an AKT signal access, an NF-KB inflammation access, an autophagy level and an E-cadherin expression; thus the apoptosis of kidney tubule cell and necrosis of tubule expansion are reduced, the renal pathology damage and kidney function are improved; the inhibitor can protect the kidney structure and function in the acute kidney injury. Therefore, HDAC6 is likely to be an important target point to prevent and treat the acute kidney injury.

The invention relates to the field of medical chemistry, in particular to a hydroxamic acid compound containing substituted 2-phenylthiazole-5-formamide or 2-phenylimidazole-5-formamide and application of the hydroxamic acid compound, the compound has a structure as shown in a formula (I), can selectively act on HDAC6, inhibit cancer cell proliferation and enhance tumor immunity, and can be used for preparing an HDAC6 drug or an HDAC6 drug or an HDAC6 drug or an HDAC6 drug or an HDAC6 drug or an HDAC6 drug or an HDAC6 drug. The compound has efficient anti-cancer activity. Therefore, the compound can be used for preparing histone deacetylase inhibitors and drugs for treating and/or preventing cancers.

The invention relates to biomarkers for determining the prognosis of cancer patients. By determining the level of the biomarker HR23B in the cell or patient, and optionally determining the levels of one or more of the biomarkers HDAC6, LC3 and HSP90, the invention provides a method for determining the susceptibility of a cell or a patient of interest to entering an autophagocytic state upon treatment with a drug. The invention also provides a method of determining susceptibility of a cell or patient to treatment with a drug. Entering an autophagocytic state is thought to be a tumour cell survival mechanism, whereby the tumour cell avoids apoptosis. The methods of the invention may therefore be helpful for determining whether a patient should be treated and for determining the prognosis upon drug treatment.

The present invention relates to novel compounds having histone deacetylase 6 (HDAC6) inhibitory activity, isomers thereof, or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions comprising the same, a method of treating disease using the composition, and methods for preparing the novel compounds. The novel compounds according to the present invention have histone deacetylase 6 (HDAC6) inhibitory activity, and are effective for the prevention or treatment of HDAC6-associated diseases, including cancer, inflammatory diseases, autoimmune diseases, neurological diseases and neurodegenerative disorders.

The invention relates to compounds of Formula (I) as described herein, useful as histone deacetylase 6 (HDAC6) inhibitors. The invention also relates to pharmaceutical compositions comprising these compounds and to their use in therapy.

The invention discloses a double-target inhibitor as well as a preparation method and application thereof. The double-target inhibitor has a structure shown as a formula (I), wherein R1 is H, an electron-withdrawing group or an electron-donating group; R is alkyl; n is equal to 1 to 5. The double-target inhibitor provided by the invention can be used for selectively inhibiting HDAC6 and IC50 values on HDAC1 and HDAC8 are greater than 20 muM; the double-target inhibitor is used as a prodrug to be subjected to hydrolysis reaction in cells, and tubulin and an HDAC double-target inhibitor can be released; the inhibition activity of histone deacetylase on solid tumors is improved; the double-target inhibitor has a relatively good inhibition effect on tumor cells. The formula (I) is shown in thedescription.

The present invention provides compositions and methods for increasing the transfer of nucleic acids into cells. In particular, the present invention provides for the use of inhibitors of HDAC6, a cytoplasmic histone deacetylase present in mammalian cells by, for example, small molecules or siRNA treatment, in increasing gene transfer and/or expression in cells in vitro and in vivo for research and gene therapy applications.

The invention discloses a tricyclic compound and application thereof. The invention specifically discloses a compound as shown in a formula I or pharmaceutically acceptable salt thereof. The tricyclic compound disclosed by the invention has a very good inhibition effect on HDAC (histone deacetylase), especially HDAC6, has relatively good selectivity and can be used for inhibiting proliferation of various tumor cells.

The present application provides a method for treating a neurodegenerative disease in a subject characterised in that a therapeutically effective amount of a modulator of HDAC6 administered to said subject.

The invention provides application of histone deacetylase 6 in preparation of a marker for evaluating kidney function progress of an IgA nephrotic patient. According to the invention, the situation ofrenal function progress is evaluated through the change of the content of HDAC6, the expression of HDAC6 in the renal tissue of an IgA nephrotic patient is high, the prognosis of the renal function progress is estimated quickly, and positive treatment and rigorous follow-up visit should be given to the patient. According to the invention, the kidney biopsy specimen is subjected to pinus massoniana staining and immunohistochemical staining; software is used for quantitatively detecting the content of HDAC6, the correlation between HDAC6 and clinical indexes of IgA nephropathy patients is discussed, it is proved that histone deacetylase HDAC6 has correlation with the kidney function progress of IgA nephropathy patients, and a new theoretical basis is provided for clinically evaluating the kidney function progress of IgA nephropathy patients.