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The solubility-driven optimization of a series of 1,7-napthyridine phosphodiesterase-4 inhibitors is described. Directed structural changes resulted in increased aqueous solubility, enabling superior pharmacokinetic properties with retention of PDE4 inhibition. A range of potent and orally bioavailable compounds with good in vivo efficacy in animal models of inflammation and reduced emetic potential compared to previously described drugs were synthesized. Compound 2d was taken forward as a clinical candidate for the treatment of COPD.

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1,635-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N629 – PubChem

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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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Name is 6-Amino-8-bromo-1,7-naphthyridine, as a common heterocyclic compound, it belongs to naphthyridine compound, and cas is 5912-35-6, its synthesis route is as follows.,5912-35-6

To a stirred solution of 6-amino-8-bromo-1, 7-naphthyridine (0.5 g) in a mixture of toluene (2.5 ml), DMF (4 ml) and aqueous KZCOS (0.68 g in 2 ml water) is added bis (dibenzylideneacetone) palladium (51 mg), triphenylphosphine (47 mg) and 3- fluorophenylboronic acid (0.33 g). The mixture is stirred for 4 hours at 100C. The mixture is diluted with ethyl acetate, then filtered through a CeliteTM filter. The ethyl acetate solution is washed with 2 N NAOH and water, dried over magnesium sulphate, then concentrated to afford the title compound. MS: APCI 240.0 MH+.

With the complex challenges of chemical substances, we look forward to future research findings about 6-Amino-8-bromo-1,7-naphthyridine

Reference£º
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2004/55013; (2004); A1;,
1,8-Naphthyridine – Wikipedia
1,8-Naphthyridine | C8H6N2 – PubChem

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As a common heterocyclic compound, it belongs to naphthyridine compound, name is 6-Amino-8-bromo-1,7-naphthyridine, and cas is 5912-35-6, its synthesis route is as follows.,5912-35-6

To a stirred solution of 8-BROMO- [1, 7] naphthyridin-6-ylamine (1.70 g) in a mixture of toluene (7 ml), DMF (11 ml) and aqueous K2CO3 (2.31 g in 5 ml water) is added bis (dibenzylideneacetone) palladium (174 mg), triphenylphosphine (158 mg) and 5-fluoro-2- methoxyphenylboronic acid (1.38 g). The mixture is stirred for 3.5 hours at 100C, then diluted with ethyl acetate and filtered through Celite. The ethyl acetate solution is washed with 2N NAOH and water, dried over magnesium sulphate, then concentrated to afford the title compound. MS: APCI 270.0 MH+.

With the complex challenges of chemical substances, we look forward to future research findings about 5912-35-6,belong naphthyridine compound

Reference£º
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2004/55013; (2004); A1;,
1,8-Naphthyridine – Wikipedia
1,8-Naphthyridine | C8H6N2 – PubChem

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5912-35-6, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,5912-35-6 ,6-Amino-8-bromo-1,7-naphthyridine, other downstream synthetic routes, hurry up and to see

It is a common heterocyclic compound, the naphthyridine compound, 6-Amino-8-bromo-1,7-naphthyridine, cas is 5912-35-6 its synthesis route is as follows.

To a stirred solution of 6-amino-8-bromo-1, 7-naphthyridine (0.5 g) in a mixture of toluene (2.5 ml), DMF (4 ml) and aqueous KZCOS (0.68 g in 2 ml water) is added bis (dibenzylideneacetone) palladium (51 mg), triphenylphosphine (47 mg) and 3- fluorophenylboronic acid (0.33 g). The mixture is stirred for 4 hours at 100C. The mixture is diluted with ethyl acetate, then filtered through a CeliteTM filter. The ethyl acetate solution is washed with 2 N NAOH and water, dried over magnesium sulphate, then concentrated to afford the title compound. MS: APCI 240.0 MH+.

5912-35-6, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,5912-35-6 ,6-Amino-8-bromo-1,7-naphthyridine, other downstream synthetic routes, hurry up and to see

Reference£º
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2004/55013; (2004); A1;,
1,8-Naphthyridine – Wikipedia
1,8-Naphthyridine | C8H6N2 – PubChem

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5912-35-6, 6-Amino-8-bromo-1,7-naphthyridine is a naphthyridine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5912-35-6, To a stirred solution of 8-BROMO- [1, 7] naphthyridin-6-ylamine (1.70 g) in a mixture of toluene (7 ml), DMF (11 ml) and aqueous K2CO3 (2.31 g in 5 ml water) is added bis (dibenzylideneacetone) palladium (174 mg), triphenylphosphine (158 mg) and 5-fluoro-2- methoxyphenylboronic acid (1.38 g). The mixture is stirred for 3.5 hours at 100C, then diluted with ethyl acetate and filtered through Celite. The ethyl acetate solution is washed with 2N NAOH and water, dried over magnesium sulphate, then concentrated to afford the title compound. MS: APCI 270.0 MH+.

As the paragraph descriping shows that 5912-35-6 is playing an increasingly important role.

Reference£º
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2004/55013; (2004); A1;,
1,8-Naphthyridine – Wikipedia
1,8-Naphthyridine | C8H6N2 – PubChem

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5912-35-6 6-Amino-8-bromo-1,7-naphthyridine 10704335, anaphthyridine compound, is more and more widely used in various.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5912-35-6,6-Amino-8-bromo-1,7-naphthyridine,as a common compound, the synthetic route is as follows.,5912-35-6

To a stirred solution of 6-amino-8-bromo-1, 7-naphthyridine (0.5 g) in a mixture of toluene (2.5 ml), DMF (4 ml) and aqueous KZCOS (0.68 g in 2 ml water) is added bis (dibenzylideneacetone) palladium (51 mg), triphenylphosphine (47 mg) and 3- fluorophenylboronic acid (0.33 g). The mixture is stirred for 4 hours at 100C. The mixture is diluted with ethyl acetate, then filtered through a CeliteTM filter. The ethyl acetate solution is washed with 2 N NAOH and water, dried over magnesium sulphate, then concentrated to afford the title compound. MS: APCI 240.0 MH+.

5912-35-6 6-Amino-8-bromo-1,7-naphthyridine 10704335, anaphthyridine compound, is more and more widely used in various.

Reference£º
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2004/55013; (2004); A1;,
1,8-Naphthyridine – Wikipedia
1,8-Naphthyridine | C8H6N2 – PubChem