758721-57-2

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 
• 758721-54-9 3-methyl-6-propyl-5H-[1,2]thiazolo[4,5-e]pyrimidin-4-one 
• 162702-38-7 5-(butanoylamino)-3-methyl-1,2-thiazole-4-carboxamide 
• 162702-06-9 N-(4-cyano-3-methyl-1,2-thiazol-5-yl)butanamide 
• 758721-55-0 5-benzyl-3-methyl-6-propyl-[1,2]thiazolo[4,5-e]pyrimidin-4-one 

Downstream Products

• 758721-59-4 tert-butyl N-[3-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)propylamino]propyl]carbamate 
• 876306-71-7 tert-butyl N-[3-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)propyl-(4-methylbenzoyl)amino]propyl]carbamate 
• 876306-81-9 tert-butyl N-[3-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)propyl-(3-fluoro-4-methylbenzoyl)amino]propyl]carbamate 
• 758721-70-9 tert-butyl N-[3-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)propyl-(4-bromobenzoyl)amino]propyl]carbamate 
• 799296-01-8 6-(1-amino-propyl)-5-benzyl-3-methyl-5H-isothiazolo[5,4-d]pyrimidin-4-one 

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.

NOVEL FUSED HETEROCYCLES AND USES THEREOF

This invention relates to novel compounds having the formula (I) (a chemical formula should be inserted here - please see paper copy enclosed herewith) m = 0, 1, 2 n = 0, 1 (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the specification and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.

Bicyclicpyrimidones and their use to treat diseases

The present invention is directed to dihydropyrimidones having formula I or II and methods of using them to induce mitotic arrest, thereby making them useful as anti-cancer agents and other diseases that can be treated by inducing mitotic arrest.