Archives for Chemistry Experiments of 6-Amino-8-bromo-1,7-naphthyridine

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Figure Presented. A survey of PDE4 inhibitors reveals that some compounds trigger intracellular aggregation of PDE4A4 into accretion foci through association with the ubiquitin-binding scaffold protein p62 (SQSTM1). We show that this effect is driven by inhibitor occupancy of the catalytic pocket and stabilization of a capped state in which a sequence within the enzymes upstream conserved region 2 (UCR2) module folds across the catalytic pocket. Only certain inhibitors cause PDE4A4 foci formation, and the structural features responsible for driving the process are defined. Switching to the UCR2-capped state induces conformational transition in the enzymes regulatory N-terminal portion, facilitating protein association events responsible for reversible aggregate assembly. PDE4-selective inhibitors able to trigger relocalization of PDE4A4 into foci can therefore be expected to exert actions on cells that extend beyond simple inhibition of PDE4 catalytic activity and that may arise from reconfiguring the enzymes protein association partnerships.

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1,629-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N623 – PubChem

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Novartis AG

Novel 8-aryl-1,7-naphthyridines, in free or salt form, are PDE IV inhibitors and are thus useful as pharmaceuticals, e.g. for asthma therapy. Preferred compounds include compounds of formulae (I and II) wherein the R groups are as defined. Pharmaceutical compositions comprising the compounds, processes for preparation of the compounds and novel intermediates for use in the processes are disclosed.

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1,626-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N620 – PubChem

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Eisai Co., Ltd.

The present provides a condensed pyridine compound (I) represented by the following formula: (wherein, R2 represents ring A represents benzene ring, pyridine ring, thiophene ring or furan ring; andB represents its pharmaceutically acceptable salt or hydrates thereof, which is a clinically useful medicament having a serotonin antagonism, in particular, that for treating, ameliorating or preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.

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1,627-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N621 – PubChem

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The phosphoinositide 3-kinase (PI3K) family catalyzes the ATP-dependent phosphorylation of the 3?-hydroxyl group of phosphatidylinositols and plays an important role in cell growth and survival. There is abundant evidence demonstrating that PI3K signaling is dysregulated in many human cancers, suggesting that therapeutics targeting the PI3K pathway may have utility for the treatment of cancer. Our efforts to identify potent, efficacious, and orally available PI3K/mammalian target of rapamycin (mTOR) dual inhibitors resulted in the discovery of a series of substituted quinolines and quinoxalines derivatives. In this report, we describe the structure-activity relationships, selectivity, and pharmacokinetic data of this series and illustrate the in vivo pharmacodynamic and efficacy data for a representative compound.

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1,634-Naphthyridine – Wikipedia,
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A six-step synthesis of a 4-[8-(3-fluorophenyl)[1,7]naphthyridin-6-yl]- trans-cyclohexanecarboxylic acid with an overall yield of 27% starting from 2-cyano-3-methylpyridine, cyclohexane-1,4-dicarboxylic acid dimethyl ester, and 3-fluorophenylboronic acid is described. The trans stereochemistry in the cyclohexane moiety was achieved through a series of equilibration steps at different stages of the synthesis.

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1,633-Naphthyridine – Wikipedia,
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SS Pharmaceutical Co., Ltd.

Certain 1,7-naphthyridine derivatives and their acid addition salts have strong antiarrhythmic effects, cardiotonic effects, diuretic effects, bronchodilation effects, anti-acetylcholine effects, anti-inflammatory effects, analgesic effects and the like and are hence useful for various diseases such as heart diseases, hypertension, asthma, arthritis, lumbago, toothache, etc.

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1,628-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N622 – PubChem

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AMGEN INC.

The present invention relates to compounds of Formula (I), or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein Q, X1, X2, R1 and Z are as defined herein.

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1,624-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N618 – PubChem

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Electric Literature of 5912-35-6, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.5912-35-6, Name is 6-Amino-8-bromo-1,7-naphthyridine, molecular formula is C8H6BrN3. In a article£¬once mentioned of 5912-35-6

NOVARTIS AG; NOVARTIS PHARMA GMBH

Compounds of Formula (I) in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by of phosphodiesterase type 4 or the down-regulation or inhibition of TNF-alpha release, particularly obstructive or inflammatory airways diseases. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

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1,625-Naphthyridine – Wikipedia,
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5912-35-6, Name is 6-Amino-8-bromo-1,7-naphthyridine, belongs to naphthyridine compound, is a common compound. HPLC of Formula: C8H6BrN3In an article, once mentioned the new application about 5912-35-6.

The synthesis of a 6,8-disubstituted 1,7-naphthyridine 1 and its characterization as a potent and selective phosphodiesterase type 4D inhibitor (IC50=1.5nM) are described. The compound inhibited TNFalpha-release from human peripheral blood mononuclear cells and was orally active in a model of adjuvant-induced arthritis in rats.

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1,631-Naphthyridine – Wikipedia,
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Quinuclidine-containing spirooxazolines, as described in the previous report in this series, were demonstrated to have utility as alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) partial agonists. In this work, the SAR of this chemotype was expanded to include an array of diazine heterocyclic substitutions. Many of the heterocyclic analogs were potent partial agonists of the alpha7 receptor, selective against other nicotinic receptors and the serotinergic 5HT3A receptor. (1?S,3?R,4?S)-N-(6-phenylpyrimidin-4-yl)-4H-1?-azaspiro[oxazole-5,3?-bicyclo[2.2.2]octan]-2-amine, a potent and selective alpha7 nAChR partial agonist, was demonstrated to improve cognition in the mouse novel object recognition (NOR) model of episodic memory.

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1,632-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N626 – PubChem