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Recently, four subtypes of the human phosphodiesterase type 4 (PDE4A-D) enzyme have been described. So far, only very few PDE4 subtype-selective inhibitors are known. Herein, we describe the synthesis of 6,8-disubstituted 1,7-naphthyridines and their characterization as potent and selective inhibitors of PDE4D which suppress the oxidative burst in human eosinophils with IC50 values as low as 0.7 nM. SAR development and the extended use of palladium-catalyzed cross-coupling reactions led to compound 11 which inhibited human PDE4D with an IC50 value of 1 nM. Thus, compound 11 was 55, 175, and 1000 times more potent in inhibiting PDE4D over PDE4B, PDE4A, and PDE4C. In a Brown Norway rat model of allergic asthma, compound 11 when given by the oral route (1 mg/kg) reduced by more than 50% the influx of eosinophils, T-cells, and neutrophils into bronchoalveolar lavage fluid (BALF) samples obtained from antigen-challenged animals. Thus, PDE4D- selective inhibitors of the 1,7-naphthyridine class have the potential as an oral therapy for treating asthma.

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1,630-Naphthyridine – Wikipedia,
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Beijing Huilinsi Biological Technology Co., Ltd.; He Lei; Quan Qizhe; Lin Hu; Xu Ming; Huang Rongtao; Li Junye

The present invention provides a method for preparing the binding […], the preparation method comprises: shown in formula I of formula II ring chelate compound shown in side chain in the non-protonic solvent after the reaction, removing a chelating moiety, as shown in formula III intermediate, as shown in formula III intermediate get rid of protecting group, generating […] method, the present invention provides a process route prepared […] do not require further purification, high yield, high purity, is suitable for industrial production. (by machine translation)

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64874-38-0, Name is 6-Bromo-1,8-naphthyridin-2-amine, belongs to naphthyridine compound, is a common compound. 64874-38-0In an article, authors is Bahman Jahromi, Enayatollah, once mentioned the new application about 64874-38-0.

Some new substituted 1,8- naphthyridines 2a, 2b, 2c, 2d, 2e, 2f, 2g have been synthesized by treating various 2-substituted vinamidinium salts 1a, 1b, 1c, 1d, 1e, 1f, 1g with 2,6-diaminopyridine. The structures of the synthesized compounds have been established on the basis of elemental analysis and spectroscopic data (1H-NMR, 13C-NMR, IR, UV/VIS, and mass).

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Warner-Lambert Company

Novel naphthyridine-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections.

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SB Pharmco Puerto Rico Inc. of the United States Corporation Company

Chemical intermediates which are of use in the production of quinolone carboxylic acid derivatives having antibacterial activity.

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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 Article, the author is Frigola and a compound is mentioned, 100361-18-0, 7-Chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic Acid, introducing its new discovery. 100361-18-0

A series of 7-(2,3-disubstituted-1-azetidinyl)-1,4-dihydro-6-fluoro-4- oxoquinoline- and -1,8-naphthyridine-3-carboxylic acids, with varied substituents at the 1-, 5-, and 8-positions, was prepared to study the effects on potency and physicochemical properties of the substituent at position 2 of the azetidine moiety. The activity of the title compounds was determined in vitro against Gram-positive and Gram-negative bacteria, and the in vivo efficacy of selected derivatives was determined using a mouse infection model. The X-ray crystal structures of 6b, 6c, and 6d were found to be in reasonable agreement with the corresponding AM1 calculated geometries. Correlations between antibacterial potency of all the synthesized 7- azetidinylquinolones and naphthyridines and their calculated electronic properties and experimental capacity factors were established. Antibacterial efficacy and pharmacokinetic and physicochemical properties of selected derivatives were compared to the relevant 7-(3-amino-1-azetidinyl) and 7-(3- amino-3-methyl-1-azetidinyl) analogues (for Part 1, see: J. Med. Chem. 1993, 36, 801-810). A combination of a cyclopropyl or a substituted phenyl group at N-1 and a trans-3-amino-2-methyl-1-azetidinyl group at C-7 conferred the best overall antibacterial, pharmacokinetic, and physicochemical properties to the azetidinylquinolones studied.

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1,720-Naphthyridine – Wikipedia,
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AFFINIUM PHARMACEUTICALS, INC.

In part, the present invention is directed to antibacterial compounds

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Shandong Joint Pesticide Co., Ltd.; Tang Jianfeng; Chi Huiwei; Wu Jianting; Han Jun

The invention discloses a quinolone compound and application, in particular to an agriculturally acceptable salt thereof. The quinolone compound has good prevention and treatment effects on various bacterial pathogens in the agricultural field, and can be used for preparing a fungicide, in particular for crops or plants, and has good activity in improving the growth and development of the crops, and can be used for preventing and treating bacterial harmful organisms in agricultural field, and can be used for preparing the bactericidal agent for crops or plants at a low dosage. (by machine translation)

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100361-18-0, In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 100361-18-0, name is 7-Chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic Acid, introducing its new discovery.

Warner-Lambert Co.

Novel naphthyridine-, quinoline- and benzoxazine-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.

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BOEHRINGER INGELHEIM INTERNATIONAL GMBH; FADER, Lee; LEPAGE, Olivier; BAILEY, Murray; BEAULIEU, Pierre Louis; BILODEAU, Francois; CARSON, Rebekah; GIROUX, Andre; GODBOUT, Cedrickx; MOREAU, Benoit; NAUD, Julie; PARISIEN, Mathieu; POIRIER, Martin; POIRIER, Maude; SURPRENANT, Simon; THIBEAULT, Carl

Compounds of Formula (I) wherein n, m, R1, R2, R3, R4, R5 and R6 are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.

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