53241-92-2

Upstream product

• 53241-90-0 diethyl {[(6-methoxypyridin-3-yl)amino]methylidene}propanedioate 
• 6628-77-9 6-methoxy-pyridin-3-ylamine 
• 87-13-8 diethyl 2-ethoxymethylenemalonate 
• 13049-86-0 diethyl 2-(ethoxycarbonylmethylene)malonate 

Downstream Products

• 1345868-84-9 C₂₇H₂₆N₄O₄ 
• 1345868-86-1 C₂₇H₂₃F₃N₄O₄ 
• 1345868-88-3 C₂₆H₂₃ClN₄O₄ 
• 724788-65-2 4-bromo-6-methoxy-1,5-naphthyridine-3-carboxylic acid 
• 724788-66-3 4-bromo-6-(methyloxy)-1,5-naphthyridin-3-amine 
• 724788-70-9 8-bromo-7-fluoro-2-methoxy-1,5-naphthyridine 
• 1417551-48-4 t-butyl 4-bromo-6-methoxy-1,5-naphthyridine-3-yl-carbamate 
• 724788-64-1 ethyl 4-bromo-6-methoxy-1,5-naphthyridine-3-carboxylate 
• 1415415-01-8 7-fluoro-2-methoxy-8-methyl-1,5-naphthyridine 
• 1616409-89-2 t-butyl 1-(2-(3-fluoro-6-methoxy-1,5-naphthyridin-4-yl)-1-hydroxyethyl)-2-oxabicyclo[2.2.2]octan-4-ylcarbamate 
• 1616409-88-1 t-butyl 1-(2-(3-fluoro-6-methoxy-1,5-naphthyridin-4-yl)-1-hydroxyethyl)-2-oxabicyclo[2.2.2]octan-4-ylcarbamate 
• 1345868-80-5 C₂₆H₂₄N₄O₄ 
• 1345868-78-1 C₂₅H₂₁F₂N₃O₆ 
• 1345868-76-9 C₂₄H₁₉F₂N₃O₅ 

Relevant academic research and scientific papers

ANTIBACTERIAL COMPOUNDS HAVING BROAD SPECTRUM OF ACTIVITY

The present invention relates to novel antibacterial compounds, pharmaceutical compositions containing them and their use as antimicrobials.

Oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad spectrum antibacterial agents

Bacterial resistance is eroding the clinical utility of existing antibiotics necessitating the discovery of new agents. Bacterial type II topoisomerase is a clinically validated, highly effective, and proven drug target. This target is amenable to inhibit

Synthesis and structure-activity relationship studies of dihydronaphthyridinediones as a novel structural class of potent and selective PDE7 inhibitors

The synthesis and SAR studies of a series of structurally novel inhibitors of PDE7 are discussed. The best compounds from the series display low nanomolar inhibitory activity and are selective versus other PDE isoenzymes.

Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases

We have identified a series of amino-piperidine antibacterials with a good broad spectrum potency. We report the investigation of various subunits in this series and advanced studies on compound 8. Compound 8 possesses good pharmacokinetics, broad spectrum antibacterial activity and demonstrates oral efficacy in a rat lung infection model.

NOVEL BICYCLIC ANTIBIOTICS

Compounds of formula (I) wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C-H, C-(C1-C6alkyl), C-(C1-C6alkoxy), C-halogen, C-COOH; X5 represents C-H or C-(C1-C6alkyl), C-halogen; R1 and R2, independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, carboxy, amino, C1-C6alkylamino, di(C1-C6alkyl)amino, mercapto, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylamino- carbonyloxy, C2-C6alkenyl, C2-C6alkynyl, C1-C6alkylcarbonyloxy, C1-C6alkyl- sulfonyloxy, C1 -C6heteroalkylcarbonyloxy, C5-C6heterocyclylcarbonyloxy, C1-C6heteroalkyl, C1-C6heteroalkoxy, wherein heteroalkyl, heteroalkoxy groups or heterocyclyl comprise 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, in which substituents the alkyl moieties are unsubstituted or further substituted by halogeno, cyano, hydroxy, C1-C4alkoxy, C1-C4alkylcarbonyl, C1-C4alkoxycarbonyl, unsubstituted or substituted phenoxy or phenylcarbonyl, unsubstituted or substituted C5-C6heterocyclyl or carboxy; A1 represents a divalent group of one of the formulae -O-(CH2)m-(CH2)-, -S-(CH2)m-(CH2)- or -(C=O)O-(CH2)m-(CH2)-, wherein the (CH2)m moiety is optionally substituted by C1-C4alkyl, C2-C4alkenyl, C3-C6cycloalkyl, C3-C6cycloalkylmethyl, morpholinomethyl, halogen, carboxy, hydroxy, C1-C4alkoxy; C1 -C4alkoxyC1 -C4alkyl, C1 -C4alkoxy(C1 -C4alkylenoxy)C1 -C4alkyl, benzyloxyC1 - C4alkyl, amino, mono- or di-(C1-C4alkyl)amino or acylamino, in which substituents the alkyl moieties can be further substituted by 1 or more fluoro atoms m is 0, 1 or 2, provided that the number of atoms in the direct chain between the two terminal valencies of A1 is at least 3, which group A1 is linked to A2 via the terminal (CH2)-moiety; A2 is a group selected from C3-C8cycloalkylene; saturated and unsaturated 4 to 8- membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, which group A2 is unsubstituted or substituted; R4 represents hydrogen or C1 -C4alkyl; A3 represents C1-C4alkylene, C2-C4alkenylene, >C=O, -C(O)C1-C3alkylene-, -C(=O)NH-, or a group selected from -C2H4NH-, -C2H4O-, and -C2H4S- being linked to the adjacent NR4-group via the carbon atom; and G represents aryl or heteroaryl, which is unsubstituted or substituted and n is 0, 1 or 2; or a pharmaceutically acceptable salts, hydrates or solvates thereof are valuable antibacterial agents.

SUBSTITUTED 1-METHYL-1H-QUINOLIN-2-ONES AND 1-METHYL-1H-1,5-NAPHTHYRIDIN-2-ONES AS ANTIBACTERIALS

Bicyclic nitrogen containing compounds of formula (I) and their use as antibacterials.

Antibacterial Agents

Naphthalene, quinoline, quinoaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.

ANTIBACTERIAL AGENTS

Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.

ANTIBACTERIAL AGENTS

Naphthyridine and related derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.

ANTIBACTERIAL AGENTS

Naphthyridine and quinoline derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.