929904-84-7

Upstream product

• 51549-34-9 3’-O-tert-butyldimethylsilyl-2’-deoxyguanosine 
• 51549-35-0 3',5'-bis-O-(tert-butyldimethylsilyl)-2'-deoxyguanosine 
• 961-07-9 2'-Deoxyguanosine 
• 73602-61-6 triethylamine tris(hydrogen fluoride) 
• 121-44-8 triethylamine 
• 2353-33-5 5-aza-2'-deoxycytidine 
• 929904-85-8 guadecitabine sodium salt 
• 5204-74-0 triethylammonium acetate 
• 929904-98-3 C₄₆H₅₃N₆O₉P 

Downstream Products

• 929904-85-8 guadecitabine sodium salt 

Relevant academic research and scientific papers

IMPROVED PROCESSES FOR THE PREPARATION OF GUADECITABINE AND INTERMEDIATES THEREOF

Described are procedures and intermediates for the preparation of guadecitabine, and guadecitabine salts and solid state forms thereof.

COMBINATION OF ISOINDOLINONE DERIVATIVES WITH SGI-110

The invention provides a combination comprising: (i) a compound of formula (Io) : (Io) or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims; and (ii) a compound which is SGI-110 (SGI-110) or a tautomer or a solvate or a pharmaceutically acceptable salt thereof. Also provided are pharmaceutical compositions containing the combinations and medical uses of the combinations.

LYOPHILIZED PHARMACEUTICAL COMPOSITIONS

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.

Oligonucleotide analogues incorporating 5-aza-cytosine therein

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.