907572-18-3

Upstream product

• 100-46-9 benzylamine 
• 83863-72-3 (-)-ethyl 3-methoxy-4-oxo-1-piperidine-carboxylate 
• 83898-43-5 ethyl 3-hydroxy-4,4-dimethoxy-1-piperidinecarboxylate 
• 83863-71-2 ethyl (3RS,4SR)-4-amino-3-methoxypiperidine-1-carboxylic acid hydrochloride Salt 
• 83863-73-4 (-)-ethyl 3,4,4-trimethoxy-1-piperidinecarboxylate 
• 29976-53-2 N-ethoxycarbonyl-4-piperidone 
• 907543-86-6 ethyl (3S,4R)-4-(benzylamino)-3-methoxypiperidine-1-carboxylate 

Downstream Products

• 1351866-22-2 C₁₈H₂₆N₂O₅ 
• 1351865-90-1 C₂₄H₂₇F₃N₆O₂ 
• 1351866-25-5 C₁₆H₂₂N₆O₂ 
• 1351866-24-4 C₁₉H₂₆N₆O₄ 
• 907543-86-6 ethyl (3S,4R)-4-(benzylamino)-3-methoxypiperidine-1-carboxylate 

Relevant academic research and scientific papers

Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099)

AZD5099 (compound 63) is an antibacterial agent that entered phase 1 clinical trials targeting infections caused by Gram-positive and fastidious Gram-negative bacteria. It was derived from previously reported pyrrolamide antibacterials and a fragment-based approach targeting the ATP binding site of bacterial type II topoisomerases. The program described herein varied a 3-piperidine substituent and incorporated 4-thiazole substituents that form a seven-membered ring intramolecular hydrogen bond with a 5-position carboxylic acid. Improved antibacterial activity and lower in vivo clearances were achieved. The lower clearances were attributed, in part, to reduced recognition by the multidrug resistant transporter Mrp2. Compound 63 showed notable efficacy in a mouse neutropenic Staphylococcus aureus infection model. Resistance frequency versus the drug was low, and reports of clinical resistance due to alteration of the target are few. Hence, 63 could offer a novel treatment for serious issues of resistance to currently used antibacterials.

DIMETHYLBENZOFURAN AND DIMETHYLBENZOPYRAN DERIVATIVES AND THEIR USE AS 5-HT3 ANTAGONISTS

Method of treating 5-HT 3-mediated disorders, which comprises systemic administration of an effective amount of a compound of formula (I) STR1 the pharmaceutically acceptable acid addition salt forms and the stereochemically isomeric forms thereof, wherein R 1 and R 2 represent hydrogen, or R 1 and R 2 taken together form a bivalent radical of formula--CH=CH--CH=CH--(a),--CH=C(Cl)--CH= CH--(b) or--CH=CH--C(Cl)=CH--(c); n represents 2, 3 or 4; R. sup.3 represents hydrogen or methoxy; m represents 1 or 2; R 4 represents hydrogen, amino or C 1-3-alkylcarbonylamino; and R 5 represents hydrogen or halo; novel compounds; compositions; processes for preparing novel compounds and intermediates.

Novel N-(3-hydroxy-4-piperidinyl)benzamide derivatives

Novel N-(3-hydroxy-4-piperidinyl)benzamides and derivatives thereof, said compounds being useful as stimulators of the motility of the gastro-intestinal system.