929904-85-8

Usage

Uses

Used in Oncology:
S-110 is used as a DNA methylation inhibitor for its potential to reduce tumor growth in various types of cancer. It has been shown to be effective and well-tolerated in tumor-free mice, indicating its potential as a promising therapeutic agent in oncology.
Used in Drug Development:
S-110 can be used in the development of novel drug delivery systems to enhance its applications and efficacy against cancer cells. By employing various organic and metallic nanoparticles as carriers for S-110 delivery, researchers can improve its delivery, bioavailability, and therapeutic outcomes, making it a valuable component in drug development for cancer treatment.

Upstream product

• 2353-33-5 5-aza-2'-deoxycytidine 
• 961-07-9 2'-Deoxyguanosine 
• 51549-35-0 3',5'-bis-O-(tert-butyldimethylsilyl)-2'-deoxyguanosine 
• 51549-34-9 3’-O-tert-butyldimethylsilyl-2’-deoxyguanosine 
• 929904-84-7 guadecitabine triethylammonium salt 

Downstream Products

• 929904-84-7 guadecitabine triethylammonium salt 

Relevant academic research and scientific papers

A process for preparing [...] gemcitabine and intermediates thereof (by machine translation)

The invention discloses a method for preparing [...] gemcitabine and intermediates thereof. The invention to isobutene N - acyl - 3 '- [1 - (1 - fluoro - 1, 1 - diisopropyl siloxy) - 1, 1 - diisopropyl silyloxy] - 2' - deoxy guanosine and 5 - aza - 4 - (N, N - dimethylamino methylene base) amino - 5 '- (4, 4' - dimethoxy trityl) - 2' - deoxycytidine as raw materials, through the phosphorus reagent under the action of the corresponding catalyst connected, followed by removing acid-sensitive protecting group, silicon protecting group and alkali sensitive protecting group to obtain the target product. The connection of the two raw materials "one-pot" the completion of the reaction, the operation is simple, mild condition, high yield good repeatability; various deprotection step reaction time is short, the selectivity is high, less by-products. The present invention provides a preparation method of the process is simple, low cost, easy to control mild reaction conditions, the production process is safe and reliable, and is suitable for industrial production. (by machine translation)

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.

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.

DRUG COMBINATIONS

The invention provides combinations of derivatives of decitabine and other active agents, including T-cell activating agents, cancer vaccines, and adjuvants. Some derivatives of decitabine exhibit superior chemical stability and shelf life, with similar physiological activity. Methods of treating one or more myelodysplasia syndromes, cancers, haematological disorders, or diseases associated with abnormal haemoglobin synthesis using the combinations are described.

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.