934344-61-3

Upstream product

• 5699-40-1 acetylguanidine 
• 1177369-31-1 (R,E)-6-(2-bromo-4-fluorophenyl)-3-(1-hydroxyethylidene)piperidine-2,4-dione 
• 1177369-29-7 (R)-ethyl 3-(2-bromo-4-fluorophenyl)-3-(3-oxobutanamido)propanoate 
• 934346-18-6 (β-R)-ethyl β-amino-2-bromo-4-fluorobenzenepropanoate hydrochloride 
• 934346-17-5 (β-R)-ethyl 2-bromo-β-[[(S)-(1,1-dimethylethyl)sulfinyl]amino]-4-fluorobenzenepropanoate 
• 1039750-61-2 (S,E)-N-(2-bromo-4-fluorobenzylidene)-2-methylpropane-2-sulfinamide 
• 934346-16-4 (6R)-3-acetyl-6-(2-bromo-4-fluorophenyl)piperidine-2,4-dione 
• 59142-68-6 2-bromo-4-fluorobenzaldehyde 
• 50-01-1 guanidine hydrochloride 

Downstream Products

• 1177370-48-7 (R)-5-(1H-benzo[d][1,2,3]triazol-1-yl)-7-(2-bromo-4-fluorophenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidine-2-amine 
• 1177369-34-4 (R)-2-amino-7-(2-bromo-4-fluoro-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidine-5-thione 
• 934343-74-5 (R)-2-amino-7-[4-fluoro-2-(6-methyloxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one 
• 1177369-45-7 (R)-2-amino-7-(5-fluoro-3'-((4-(trifluoromethoxy)phenoxy)methyl)biphenyl-2-yl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one 

Relevant academic research and scientific papers

Design, structure-activity relationship, and in vivo characterization of the development candidate NVP-HSP990

Utilizing structure-based drug design, a novel dihydropyridopyrimidinone series which exhibited potent Hsp90 inhibition, good pharmacokinetics upon oral administration, and an excellent pharmacokinetic/pharmacodynamic relationship in vivo was developed from a commercial hit. The exploration of this series led to the selection of NVP-HSP990 as a development candidate.

OXIM DERIVATIVES AS HSP90 INHIBITORS

The invention relates to HSP90 inhibiting compounds consisting of the formula: (I) wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

2-AMINO-7,8-DIHYDRO-6H-PYRIDO[4,3-D] PYRIMIDIN-5-ONES

Disclosed are 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, their stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Disclosed also are methods of using the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative, viral, autoimmune, cardiovascular, and central nevous system diseases.