876191-30-9

Upstream product

• 41808-35-9 5-amino-4-cyano-3-methylisothiazole 
• 5417-82-3 (1-ethoxyethylidene)malononitrile 
• 116595-42-7 (2E)-2-cyano-3-ethoxybut-2-enethioamide 
• 758721-53-8 (2E)-3-amino-2-cyanobut-2-enethioamide 
• 758722-00-8 3-methyl-6-(2-methylpropyl)-5H-[1,2]thiazolo[4,5-e]pyrimidin-4-one 
• 456-41-7 1-(Bromomethyl)-3-fluorobenzene 
• 162702-36-5 3-methyl-5-(3-methylbutanoylamino)-1,2-thiazole-4-carboxamide 
• 162702-04-7 N-(4-cyano-3-methyl-1,2-thiazol-5-yl)-3-methylbutanamide 

Downstream Products

• 876191-31-0 6-(1-bromo-2-methylpropyl)-5-[(3-fluorophenyl)methyl]-3-methyl-[1,2]thiazolo[4,5-e]pyrimidin-4-one 
• 876191-32-1 6-(1-azido-2-methylpropyl)-5-[(3-fluorophenyl)methyl]-3-methyl-[1,2]thiazolo[4,5-e]pyrimidin-4-one 
• 876191-33-2 6-(1-amino-2-methylpropyl)-5-[(3-fluorophenyl)methyl]-3-methyl-[1,2]thiazolo[4,5-e]pyrimidin-4-one 
• 876191-35-4 tert-butyl N-[3-[[1-[5-[(3-fluorophenyl)methyl]-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl]-2-methylpropyl]amino]propyl]carbamate 
• 876191-38-7 tert-butyl N-[3-[[1-[5-[(3-fluorophenyl)methyl]-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl]-2-methylpropyl]-(4-methylbenzoyl)amino]propyl]carbamate 

Relevant academic research and scientific papers

Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2] thiazolo[5,4- d ]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent

Structure-activity relationship analysis identified (+)-N-(3-aminopropyl)- N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl) -2-methylpropyl]-4-methylbenzamide (AZD4877), from a series of novel kinesin spindle protein (KSP) inhibitors, as exhibiting both excellent biochemical potency and pharmaceutical properties suitable for clinical development. The selected compound arrested cells in mitosis leading to the formation of the monopolar spindle phenotype characteristic of KSP inhibition and induction of cellular death. A favorable pharmacokinetic profile and notable in vivo efficacy supported the selection of this compound as a clinical candidate for the treatment of cancer.

Selected fused heterocyclics and uses thereof

This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.