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Warner-Lambert Company

Novel quinolone and naphthyridine antibacterial agents are herein described having improved in vivo activity both orally and subcutaneously where the 7-side chain of such compounds contain an alpha-amino acid; also described are its corresponding optical isomers, methods of preparation as well as compositions and methods of treating infections diseases.

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Reference£º
1,702-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N696 – PubChem

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Bayer Aktiengesellschaft

The invention relates to new quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by a tricyclic amine radical, their salts, processes for their preparation and antibacterial compositions comprising these compounds.

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1,698-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N692 – PubChem

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2-Aminomethyl-1-azetidinyl, -1-pyrrolidinyl, and -1-piperidinyl groups were designed as novel C-7 substituents for potential antibacterial quinolone agents. Of the three substituents, the 2-aminomethyl-1-azetidinyl group (compound 12a) was found to be the most favorable for enhancing the activity of the 6,8-difluoroquinoline molecule 12. Therefore the 2-aminomethyl-1- azetidinyl group was introduced into a variety of quinolines (giving 24 – 26a, and 28a) and naphthyridines (giving 31a and 32a). Through optical resolution of 1-benzylazetidine-2-carboxamide (19) and chiral synthesis of its R-isomer, both enantiomers of 2-aminomethyl-1-azetidinyl quinolines 12a and 24 – 26a were also prepared. The most active of all the compounds was 5- amino-6,8-difluoroquinoline (R)-26a. The activity of (R)-26a was more potent than those of the corresponding 1-piperazinyl derivative (3) and sparfloxacin (1), and was comparable to those of the corresponding 3-amino-1-pyrrolidinyl (4), 3-aminomethyl-1-pyrrolidinyl (5), and 3-amino-1-azetidinyl (6) derivatives.

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1,721-Naphthyridine – Wikipedia,
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The TRAF2 and NCK interacting kinase (TNIK) has been proposed to play a role in cytoskeletal organization and synaptic plasticity and has been linked, among others, to neurological disorders. However, target validation efforts for TNIK have been hampered by the limited kinase selectivity of small molecule probes and possible functional compensation in mouse models. Both issues are at least in part due to its close homology to the kinases MINK1 (or MAP4K6) and MAP4K4 (or HGK). As part of our interest in validating TNIK as a therapeutic target for neurological diseases, we set up a panel of biochemical and cellular assays, which are described herein. We then examined the activity of known amino-pyridine-based TNIK inhibitors (1, 3) and prepared structurally very close analogs that lack the ability to inhibit the target. We also developed a structurally orthogonal, naphthyridine-based TNIK inhibitor (9) and an inactive control molecule of the same chemical series. These validated small-molecule probes will enable dissection of the function of TNIK family in the context of human disease biology.

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1,579-Naphthyridine – Wikipedia,
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A series of non-basic building blocks was synthesized and introduced to the C7 position of the quinolone nucleus 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid to afford the corresponding fluoroquinolones in 46-85% yield. The antibacterial activity of these new fluoroquinolones was evaluated using a standard broth microdilution technique. The sulfur-containing quinolone, 7-(2-thia-5-azabicyclo[2.2.1]heptan-5-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid exhibited a superior antibacterial activity against quinolone-susceptible and multidrug-resistant strains in comparison with the clinically used fluoroquinolones ciprofloxacin and vancomycin, especially to the Streptococcus pneumonia and multidrug-resistant S. pneumonia clinical isolates. Crown Copyright

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1,728-Naphthyridine – Wikipedia,
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DONG WHA PHARM. CO., LTD.; CHOI, Dong-Rack; LIM, Jae-Kyung; CHOI, Jung-Uk; SHIN, Dong-Hyuk; KIM, Seung-Hwan; WON, Dae-Yeon; KIM, Jung-Hwan

The present invention provides an improved method of manufacturing Zabofloxacin D-aspartate. The present invention provides a novel method of manufacturing 8-methoxyimino-2,6-diaza-spiro[3,4]octane-2-carboxylic acid t-butyl ester succinate (TBDCS) or 2-(2,2,2-trifluoro-acetyl)-2,6-diaza-spiro[3,4]octan-8-one O-methyloxime methanesulfonate (TDMOS), which are separately the starting materials for manufacturing Zabofloxacin D-aspartate. The manufacturing method according to the present invention is suitable for mass production of Zabofloxacin D-aspartate for it enables manufacturing in high yield and high quality (HPLC purity ? 99.5%) as well as reducing the unit cost of production by using only 1.0~1.1 equivalents of TBDCS or TDMOS in a substitution reaction.

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1,662-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N656 – PubChem

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Actelion Pharmaceuticals Ltd.

The invention relates to novel chimeric antibiotics of formula I wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; A represents N or CR6; R3 represents H or fluorine; R4 is H, (C1-C3) alkyl, or cycloalkyl; R5 is the residue of a naturally occurring amino acid, of the enantiomer of a naturally occurring amino acid or of dimethylaminoglycine; R6 represents H, alkoxy or halogen; and n is 0 or 1; and to salts (in particular pharmaceutically acceptable salts) of compounds of formula I. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).

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1,664-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N658 – PubChem

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Aeterna Zentaris GmbH

The present invention relates to kinase modulators of the naphthyridine type and to the preparation and use thereof as medicaments for the modulation of misdirected cellular signal transduction processes, in particular for influencing the function of tyrosine and serine/threonine kinases and for the treatment of malignant or benign tumours and other disorders based on pathological cell proliferation, such as, for example, restenosis,psoriasis, arteriosclerosis and cirrhosis of the liver.

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1,655-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N649 – PubChem

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Novel tricyclic fluoroquinolones, [1,2,4]triazolo[3,4-h][1,8]naphthyridine-8-one-7-carboxylic acid derivatives 4a-4h bearing carrying a functional Mannich-base moiety at the C-8 position, were synthesized and evaluated for their antimicrobial activity. The results showed that some compounds with a piperazine side chain exhibited comparable or better antibacterial activity than comparator cirprofloxacin. Furthermore, the targeted compounds also displayed a broad spectrum of activity against resistant strains including both Gram-negative and Gram-positive bacteria. In particular, compound 4h showed an MIC of 0.25 mug/mL in antibacterial assay against multiple drug-resistant Escherichia coli, which represents an about 30-fold increase of potency compared to ciprofloxacin. Thus, their excellent antibacterial activity against resistant strains suggests that triazole-fused fluoroquinolones warrant further optimization as novel anti-infective chemotherapies.

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1,722-Naphthyridine – Wikipedia,
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Application of 54569-28-7, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 54569-28-7, 4-Bromo-1,8-naphthyridine, introducing its new discovery.

Shanxi Laite Optoelectric Materials Co., Ltd.; Ma Tiantian; Yang Min; Nan Peng

The present disclosure provides a nitrogen-containing compound, electronic element and an electronic device, and relates to the technical field, of organic materials, wherein I is selected from the group consisting of deuterium, nitro, X hydroxy ;R alkyl, cycloalkyl ;L alkyl, alkenyl, alkyl ;R alkoxyl, alkoxyl-alkyl-alkenylsilyl.arylsilyl. alpha.aryl,heterocyclyl,cycloalkyl,heteroarylthio,cycloalkyl-alkynylmethylsilylone-containing nitrogen compound, as shown in Formula, The, present disclosure provides, a, nitrogen, compound- containing, compound. Alkyl,L-heteroarylalkyl or alkylsilyl, alkoxy, heterocyclyl, alkyl or alkylsilylone-containing compound is disclosed in the present. disclosure. (by machine translation)

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1,602-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N596 – PubChem