202195-67-3

Upstream product

• 177199-67-6 4-carbamoylmethoxy-3-nitro-benzoic acid methyl ester 
• 536-25-4 methyl 3-amino-4-hydroxybenzoate 
• 79-04-9 chloroacetyl chloride 
• 99-42-3 methyl (4-hydroxy-3-nitro)benzoate 
• 105-36-2 ethyl bromoacetate 
• 25253-99-0 4-carboxymethoxy-3-nitro-benzoic acid 
• 35005-30-2 methyl 4-(2-methoxy-2-oxoethoxyl)benzoate 
• 19360-67-9 4-carboxymethoxy-benzoic acid 
• 616-82-0 3-nitro-4-hydroxybenzoic acid 
• 83785-14-2 methyl 4-(2-methoxy-2-oxo-ethoxy)-3-nitrobenzoate 
• 82525-66-4 3-(2-chloro-acetylamino)-4-hydroxy-benzoic acid methyl ester 
• 177199-66-5 3-amino-4-carbamoylmethoxy-benzoic acid methyl ester 
• 67-56-1 methanol 
• 134997-87-8 6-Carboxy-2,3-dihydro-3-oxo-4H-1,4-benzoxazine 

Downstream Products

• 134997-87-8 6-Carboxy-2,3-dihydro-3-oxo-4H-1,4-benzoxazine 
• 615568-17-7 6-hydroxymethyl-4H-benzo[1,4]oxazin-3-one 
• 911210-32-7 benzyl 3-hydroxy-5-[4-(3-methoxypropyl)-3,4-dihydro-2H-benzo[1,4]oxazin-6-ylmethoxy]-4-(4-phenoxyphenyl)piperidine-1-carboxylate 
• 911210-34-9 (3R,4R,5S)-4-(4-hydroxy-phenyl)-3-[4-(3-methoxy-propyl)-3,4-dihydro-2H-benzo[1,4]oxazin-6-ylmethoxy]-5-triisopropylsilanyloxy-piperidine-1-carboxylic acid benzyl ester 
• 911210-35-0 (3R,4R,5S)-4-(4-hydroxy-phenyl)-3-[4-(3-methoxy-propyl)-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-6-ylmethoxy]-5-triisopropylsilanyloxy-piperidine-1-carboxylic acid benzyl ester 
• 911210-33-8 benzyl 3-[4-(3-methoxypropyl)-3,4-dihydro-2H-benzo[1,4]oxazin-6-ylmethoxy]-4-(4-phenoxy-phenyl)-5-triisopropylsilanyloxypiperidine-1-carboxylate 
• 911210-58-7 benzyl 3-[4-(3-methoxypropyl)-3,4-dihydro-2H-benzo[1,4]oxazin-6-ylmethoxy]-4-[4-(pyridin-2-yloxy)phenyl]-5-triisopropylsilanyloxypiperidine-1-carboxylate 
• 911210-36-1 (3R,4R,5S)-4-(4-allyloxy-phenyl)-3-[4-(3-methoxy-propyl)-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-6-ylmethoxy]-5-triisopropylsilanyloxy-piperidine-1-carboxylic acid benzyl ester 
• 1454807-85-2 methyl 3-oxo-4-phenyl-3,4-dihydro-2H-benzo[b][1,4]oxazine-6-carboxylate 

Relevant academic research and scientific papers

The discovery of potent small molecule activators of human STING

The adaptor protein STING plays a major role in innate immune sensing of cytosolic nucleic acids, by triggering a robust interferon response. Despite the importance of this protein as a potential therapeutic target for serious unmet medical conditions inc

QUINAZOLINE HETEROCYCLIC COMPOUND AS EGFR KINASE INHIBITOR AND PREPARATION AND APPLICATION THEREOF

The present invention relates to an N-substituted-phenyl-5-substituted-alkoxy-2,3-dihydro-[1,4]dioxane[2,3-f]quinazolin-10-amine (I) or 4-substituted-arylamino-6-substituted-alkyl-6H-[1,4]oxazino[3,2-g]quinazoline-7(8H)-one (II) type compounds, a preparation method thereof and an application thereof as an inhibitor for epidermal growth factor receptor (EGFR) (comprising some mutant forms of EGFR) to treat cancer. These compounds and salts thereof can be used to treat or prevent various cancer diseases.

Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors

A series of novel morpholin-3-one-fused quinazoline derivatives were designed, synthesized and evaluated as EGFR tyrosine kinase inhibitors. Nineteen compounds showed significant inhibitory activities against EGFRwtkinase (IC50?wt(IC50?=?53.1?nM). Compound a7 and a8 showed excellent inhibitory activities against mutant EGFRT790M/L858Rand strong antiproliferative activity against H358 and A549 cell lines. Finally, molecular docking studies were performed to predict the possible binding mode of the target compounds. It is believed that this work would be very useful for designing a new series of tyrosine kinase inhibitors targeting EGFR.

Exploring Left-Hand-Side substitutions in the benzoxazinone series of 4-amino-piperidine bacterial type IIa topoisomerase inhibitors

An SAR survey at the C-6 benzoxazinone position of a novel scaffold which inhibits bacterial type IIa topoisomerase demonstrates that a range of small electron donating groups (EDG) and electron withdrawing groups (EWG) are tolerated for antibacterial activity. Cyano was identified as a preferred substituent that affords good antibacterial potency while minimizing hERG cardiac channel activity.

POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS

Compounds of the following formula are provided for use in inhibiting Poly (ADP-ribose) Polymerase (PARP): wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds,

Pharmaceutical Compositions Comprising Nitrogen-Containing Fused Ring Coumpounds

[Problems] The present invention provides pharmaceutical composition which is effective for the prophylaxis or treatment of pathology showing involvement of uric acid (hyperuricemia, gouty tophus, acute gout arthritis, chronic gout arthritis, gouty kidney, urolithiasis, renal function disorder, coronary arterial disease, ischemic heart disease and the like) and the like, and is superior in the time-course stability and dissolution property (disintegration property). [Solving Means] The pharmaceutical composition of the present invention is a pharmaceutical composition comprising a nitrogen-containing fused ring compound represented by the following formula [1] or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable additives, wherein the nitrogen-containing fused ring compound or a pharmaceutically acceptable salt thereof is not in contact with a basic additive: wherein each symbol is as described in the specification.

Production Method of Nitrogen-Containing Fused Ring Compounds

[Problems] The present invention provides a superior production method and a superior purification method of compounds effective for the treatment or prophylaxis of pathology showing involvement of uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urolithiasis, renal function disorder, coronary artery disease, ischemic heart disease and the like. [Means] A compound represented by the following formula [2] or a pharmaceutically acceptable salt thereof can be produced by reacting a compound represented by the following formula [3] or a salt thereof with a compound represented by the following formula [4], a salt thereof or a reactive derivative thereof. Moreover, crystallization of a compound represented by the formula [2] can be performed with industrially superior workability, and high quality crystals of a compound represented by the formula [2] can be obtained. wherein each symbol is as defined in the description.

Nitrogen-containing fused ring compounds and use thereof

A URAT1 activity inhibitor containing a nitrogen-containing fused ring compound represented by the following formula [1]: wherein each symbol is as defined in the description. The present invention is useful for the prophylaxis or treatment of pathology showing involvement of uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urolithiasis, renal function disorder, coronary artery disease, ischemic heart disease and the like.

FUSED HETEROCYCLIC COMPOUND AND USE THEREOF

The present invention relates to wherein each symbol is as defined in the specification. The compound has a superior mineral corticoidreceptorantagonistic action and is useful as an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like, a compound having a fused heterocycle, or a prodrug thereof, or a salt thereof; and an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like.

Bicyclic pyrazole compounds as antibacterial agents

Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection.