Cambridge, United Kingdom
Cambridge, United Kingdom

Astex Therapeutics was a biotechnology company focused on the discovery and development of drugs in oncology and other areas. Astex was founded in 1999 by Sir Tom Blundell, Chris Abell & Harren Jhoti, and is located in Cambridge, England.The company's research efforts focus on utilization of a proprietary "drug discovery engine" dubbed Pyramid. Astex has also solved the structure of two key cytochrome P450 isoenzymes involved in drug metabolism, 2C9 & 3A4, which the company hopes will help in optimizing the pharmacokinetic properties and safety of their lead compounds.Astex Therapeutic's first drug candidate, a cell cycle inhibitor, entered Phase I clinical trials in 2005. Since that time they have created eight drugs that have progressed into the clinical stage of development. Wikipedia.


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Oligonucleotide analogues are provided that incorporate 5-aza-cytosine in the oligonucleotide sequence, e.g., in the form of 5-aza-2-deoxycytidine (decitabine) or 5-aza-cytidine. In particular, oligonucleotide analogues rich in decitabine-deoxyguanosine islets (DpG and GpD) are provided to target the CpG islets in the human genome, especially in the promoter regions of genes susceptible to aberrant hypermethylation. Such analogues can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position. Methods for synthesizing these oligonucleotide analogues and for modulating nucleic acid methylation are provided. Also provided are phosphoramidite building blocks for synthesizing the oligonucleotide analogues, methods for synthesizing, formulating and administering these compounds or compositions to treat conditions, such as cancer and hematological disorders.


Tickle I.J.,Astex
Acta Crystallographica Section D: Biological Crystallography | Year: 2012

The commonly used validation metrics for the local agreement of a structure model with the observed electron density, namely the real-space R (RSR) and the real-space correlation coefficient (RSCC), are reviewed. It is argued that the primary goal of all validation techniques is to verify the accuracy of the model, since precision is an inherent property of the crystal and the data. It is demonstrated that the principal weakness of both of the above metrics is their inability to distinguish the accuracy of the model from its precision. Furthermore, neither of these metrics in their usual implementation indicate the statistical significance of the result. The statistical properties of electron-density maps are reviewed and an improved alternative likelihood-based metric is suggested. This leads naturally to a χ2 significance test of the difference density using the real-space difference density Z score (RSZD). This is a metric purely of the local model accuracy, as required for effective model validation and structure optimization by practising crystallographers prior to submission of a structure model to the PDB. A new real-space observed density Z score (RSZO) is also proposed; this is a metric purely of the model precision, as a substitute for other precision metrics such as the B factor. © International Union of Crystallography 2012.


Patent
Astex | Date: 2016-01-19

The invention relates to new pyridopyrazine and naphthyridine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.


Patent
Astex | Date: 2016-07-01

The invention provides a method of preparing a lyophilized pharmaceutical composition containing a compound described herein or a pharmaceutically-acceptable salt thereof. The process comprises dissolving the compound in a solvent comprising dimethylsulfoxide and optionally one or more co-solvents to form a solution, and then removing the solvent and any co-solvents by a freeze-drying process. Also provided by the invention are lyophilized pharmaceutical compositions and their use in medicine and in particular in the treatment of cancer.


Patent
Astex | Date: 2016-07-08

The invention relates to new quinoline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.


Patent
Astex | Date: 2016-07-06

The invention relates to new pteridine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.


Patent
Astex | Date: 2016-02-03

The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.


The invention relates to new pyridopyrazine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.


Patent
Astex | Date: 2016-06-06

The invention provides derivatives of decitabine with superior chemical stability and shelf life, with similar physiological activity. The derivatives are provided in a non-aqueous formulation, which further stabilizes the derivatives. Methods of treating one or more myelodysplastic syndromes, leukemia, or solid tumours using the formulations are described.


Patent
Astex, The Institute Of Cancer Research Royal Cancer Hospital and Cancer Research Technology Ltd | Date: 2016-01-29

The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R^(1 )and NR^(2)R^(3 )and a maximum chain length of 4 atoms extending between E and NR^(2)R^(3), wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom with respect to the NR^(2)R^(3 )group and provided that the oxo group when present is located at a carbon atom with respect to the NR^(2)R^(3 )group;E is a monocyclic or bicyclic carbocyclic or heterocyclic group;R^(1 )is an aryl or heteroaryl group; andR^(2), R^(3), R^(4 )and R^(5 )are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.

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