8 results about "Aurora kinase" patented technology

The present invention relates to compositions, methods, uses and kits for the treatment of renal cystogenesis. In particular, the compositions, methods, uses and kits are particularly useful, but not limited to, the treatment or prevention of Polycystic Kidney Disease. In one aspect, the prevent invention provides a method of minimising or delaying renal cystogenesis in a subject in need thereof, the method comprising inhibiting AKT in the subject, or reducing the level of Aurora kinase in the subject, thereby minimising or delaying renal cystogenesis.

Compounds (I), compositions, and methods for use in degrading Aurora kinase are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo. Also disclosed are pharmaceutical compositions comprising Aurora kinase degraders, as well as methods for treating cancer using Aurora kinase degraders.

The invention discloses a screening method of an aurora kinase AURKA inhibitor, and the preparation method is characterized by having the following general formula: the invention provides a virtual screening method of the aurora kinase AURKA inhibitor, which comprises the following steps: (1) an AURKA model: obtaining an AURKA crystal structure, preprocessing crystal data, defining the crystal data as a counter acceptor, and determining a binding site; (2) a small molecule compound library: pretreating small molecule structures; (3) performing rigid docking based on shape matching on the constructed AURKA crystal data and the small molecular structure, and selecting the structure in the front sequence to perform next optimization; (4) carrying out more accurate semi-flexible butt joint on the small molecular structure subjected to primary screening, and taking the binding energy as the standard of secondary screening; and (5) integrating two times of docking scoring to obtain the aurora kinase AURKA inhibitor.

To provide forms of Compound A, which is a potent Aurora A, B, and C, and FLT3 kinase inhibitor, that are stable and have a certain degree of inherent water solubility.SOLUTION: Provided are a fumarate salt and polymorphic forms of Compound A (6-chloro-7-(4-(4-chlorobenzyl)piperazin-1-yl)-2-(1,3-dimethyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine). The present invention also provides processes for preparation of salts and polymorphic forms of Compound A, pharmaceutical compositions comprising them, and their use in treatment of proliferative disorders such as cancer, and other diseases or conditions in which Aurora kinase and / or FLT3 activity is implicated.SELECTED DRAWING: None

Disclosed herein inter alia are compositions and methods useful in the treatment of cancer and for modulating the activity of Aurora A kinase and / or a Myc family protein.

The diagnostic markers that provide novel diagnostic criteria to blastic plasmacytoid dendritic cell neoplasm (BPDCN) has been searched, and the presence of immunoblastoid cytomorphology, 8q24 rearrangement, and MYC expression were established as novel markers for subtyping BPDCN. It has been further found that the inhibitors which directly or indirectly inhibit the expression, functions, or signaling pathways of MYC, such as BET bromodomain-selective inhibitors or aurora kinase inhibitors, are effective in MYC-positive BPDCN, and HDAC inhibitors or BCL2 family protein inhibitors are effective as therapeutic drugs for BPDCN.

The present invention relates to salts and polymorphic forms of Compound A (6-chloro-7-(4-(4-chlorobenzyl)piperazin-1-yl)-2-(1,3-dimethyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine), an inhibitor of Aurora kinase and FMS-like tyrosine kinase 3 (FLT3) activity. The present invention also relates to processes for the preparation of the salts and polymorphic forms of the compound, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which Aurora kinase and / or FLT3 activity is implicated.

The invention belongs to the field of drug delivery, and discloses a nano-liposome delivery system targeting PLK1 / Aurora kinase and an application of the nano-liposome delivery system in oral squamous cell carcinoma treatment, the system jointly loads Volasertib and Alisertib in DOPE / CHEMS pH sensitive liposome, is coupled with GE11 targeting EGFR, realizes accurate delivery through active targeting and pH response drug release, induces mitosis disasters synergistically through double targets, and the inhibition rate exceeds 80%.