1316216-06-4

Upstream product

• 591-50-4 iodobenzene 
• 1316216-05-3 C₁₉H₁₇N₃O₂ 
• 95928-49-7 2-hydroxy-pyrimidine-5-carboxylic acid ethyl ester 
• 864172-93-0 ethyl 2-(phenylamino)pyrimidine-5-carboxylate 
• 62-53-3 aniline 
• 89793-12-4 ethyl 2-chloropyrimidine-5-carboxylate 

Downstream Products

• 1316216-07-5 C₂₅H₂₈N₄O₃ 
• 1316214-52-4 N-[7-(hydroxyamino)-7-oxo-heptyl]-2-(N-phenylanilino)pyrimidine-5-carboxamide 

Relevant academic research and scientific papers

Mercapto compounds as histone deacetylase inhibitors and uses thereof

Experimental results show, that the compound shown by the invention has high blood-brain barrier permeability, on normal cytotoxic low, potential cardiac toxicity, and higher blood-brain barrier permeability of, on a cell model as a compound shown, or a pharmaceutically acceptable salt, ester or a prodrug, of the compound as a high-efficiency low-toxicity anti-tumor or neurodegenerative disease therapeutic agent shown in the invention. The compound has high blood-brain barrier permeability . The compound of the present invention has higher blood-brain barrier permeability as shown in the development prospect (I) of, a: therapeutic agent for high-efficiency and low-toxicity antitumor or neurodegenerative diseases.

PHARMACEUTICAL COMBINATIONS COMPRISING A HISTONE DEACETYLASE INHIBITOR AND EPOTHILONE AND METHODS OF USE THEREOF

The present disclosure relates to a pharmaceutical combination comprising (a) a histone deacetylase 6 inhibitor and (b) an epothilone, including combined preparations and pharmaceutical compositions thereof; uses of such combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.

PHARMACEUTICAL COMBINATIONS COMPRISING A HISTONE DEACETYLASE INHIBITOR AND A PROGRAMMED DEATH-LIGAND 1 (PD-L1) INHIBITOR AND METHODS OF USE THEREOF

The present disclosure relates to a pharmaceutical combination comprising (a) a histone deacetylase 6 inhibitor and (b) a programmed death ligand 1 (PD-L1) inhibitor, including combined preparations and pharmaceutical compositions thereof; uses of such combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.

PHARMACEUTICAL COMBINATIONS COMPRISING A HISTONE DEACETYLASE INHIBITOR AND A BCL-2 INHIBITOR AND METHODS OF USE THEREOF

The present disclosure relates to a pharmaceutical combination comprising (a) a histone deacetylase 6 inhibitor and (b) a BCL-2 inhibitor, including combined preparations and pharmaceutical compositions thereof; uses of such combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.

PHARMACEUTICAL COMBINATIONS COMPRISING A HISTONE DEACETYLASE INHIBITOR AND AN AURORA KINASE INHIBITOR AND METHODS OF USE THEREOF

The present disclosure relates to a pharmaceutical combination comprising (a) a histone deacetylase 6 inhibitor and (b) an aurora kinase inhibitor, including combined preparations and pharmaceutical compositions thereof; uses of such combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.

PHARMACEUTICAL COMBINATIONS COMPRISING A HISTONE DEACETYLASE INHIBITOR AND A CD38 INHIBITOR AND METHODS OF USE THEREOF

The present disclosure relates to a pharmaceutical combination comprising (a) a histone deacetylase inhibitor and (b) a CD38 inhibitor, including combined preparations and pharmaceutical compositions thereof; uses of such combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.

USE OF HDAC6 INHIBITORS FOR PREVENTING AND TREATING RENAL CYSTOGENESIS, RENAL CELL CARCINOMA, AND RENAL CILIOPATHIES

The present disclosure is directed to the use of HDAC6 inhibitors for the treatment of renal diseases and disorders, including ciliopathy, Von Hippel-Lindau (VHL) disease, renal cystogenesis, renal cell carcinoma, and Tuberous Sclerosis Complex (TSC), and the like. In some embodiments, the HDAC6 inhibitor is a direct inhibitor of HDAC6. In a further embodiment, the HDAC6 signaling inhibitor is ACY-1215 or a pharmaceutically acceptable salt thereof. In some embodiments, the HDAC6 inhibitor is combined with an AURKA inhibitor.

Biomarkers to identify patients that will respond to treatment and treating such patients

The invention relates to methods for using biomarkers to identify cancer patients that will or are likely to respond to treatment. Specifically, the invention relates to the use of one or more of three association studies of cancer types, gene mutations, or gene expression levels in order to identify cancer patients that will or are likely to respond to treatment with a histone deacetylase (HDAC) inhibitor, alone or in combination with another cancer treatment. The methods may, optionally, further include treating such patient with an HDAC inhibitor, alone or in combination with another cancer treatment.

HDAC INHIBITORS FOR THE TREATMENT OF DIABETIC PERIPHERAL NEUROPATHY

The invention relates to HDAC inhibitors for use in the treatment of diabetic peripheral neuropathy in a subject in need thereof. Also provided herein are methods for treating diabetic peripheral neuropathy in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor.

INCREASING EXPRESSION OF INTERFERON REGULATED GENES WITH COMBINATONS OF HISTONE DEACETYLASE INHIBITORS AND IMMUNOMODULATORY DRUGS

Provided herein is a combination comprising an HDAC inhibitor and an IMiD for increasing interferon regulated gene expression or decreasing c-MYC gene expression in a cancer cell or tumor in a subject in need thereof. Increasing interferon regulated gene expression may result in increased recognition of tumors by innate or adaptive immune system and an increase in programmed cell death (apoptosis) gene expression, increasing apoptosis in cancer cells and tumors. The cells can be multiple myeloma cells or diffuse large B-cell lymphoma cells. Also provided are methods for treating myelodysplastic syndromes/acute myeloid leukemia (MDS/AML) or pathogen infections in a subject in need thereof comprising administering to the subject an effective amount of HDAC inhibitor and an IMiD. The HDAC inhibitor can be an HDAC6-selective inhibitor.