Category: 60122-51-2

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Fibroblast activation protein (FAP) is a serine protease related to dipeptidyl peptidase IV (DPPIV). It has been convincingly linked to multiple disease states involving remodeling of the extracellular matrix. FAP inhibition is investigated as a therapeutic option for several of these diseases, with most attention so far devoted to oncology applications. We previously discovered the N-4-quinolinoyl-Gly-(2S)-cyanoPro scaffold as a possible entry to highly potent and selective FAP inhibitors. In the present study, we explore in detail the structure-activity relationship around this core scaffold. We report extensively optimized compounds that display low nanomolar inhibitory potency and high selectivity against the related dipeptidyl peptidases (DPPs) DPPIV, DPP9, DPPII, and prolyl oligopeptidase (PREP) the log D values, plasma stabilities, and microsomal stabilities of selected compounds were found to be highly satisfactory. Pharmacokinetic evaluation in mice of selected inhibitors demonstrated high oral bioavailability, plasma half-life, and the potential to selectively and completely inhibit FAP in vivo.

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Reference£º
1,442-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N436 – PubChem

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MERCK SHARP & DOHME CORP.; COBURN, Craig, A.; MALETIC, Milana, M.; LUO, Yunfu; QI, Zhiqi; LI, Chun Sing; YU, Tingting

The present invention relates to aryl linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhbiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.

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Reference£º
1,439-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N433 – PubChem

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A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 60122-51-2

Synthetic Route of 60122-51-2, 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.60122-51-2, Name is 1,7-Naphthyridin-4(1H)-one, molecular formula is C8H6N2O. In a article£¬once mentioned of 60122-51-2

MERCK SHARP & DOHME CORP.; COBURN, Craig; MALETIC, Milana; LUO, Yunfu; QI, Zhiqi; LI, Chun Sing; YU, Tingting

The present invention relates to aryl linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhbiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.

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Reference£º
1,440-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N434 – PubChem

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Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Synthetic Route of 60122-51-2. In my other articles, you can also check out more blogs about 60122-51-2

Synthetic Route of 60122-51-2, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 60122-51-2, Name is 1,7-Naphthyridin-4(1H)-one, molecular formula is C8H6N2O. In a Article£¬once mentioned of 60122-51-2

This paper describes the different strategies devised and applied to overcome the selectivity issues in the syntheses of 6,7-disubstituted-1H-quinolin-4-one, 7-substituted-1H-1,6-naphthyridin-4-one and 6-substituted-1H-1,7-naphthyridin-4-one derivatives. They allowed us to improve the overall yields and the scaling-up feasibility. Several examples illustrate these strategies with their advantages and drawbacks.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Synthetic Route of 60122-51-2. In my other articles, you can also check out more blogs about 60122-51-2

Reference£º
1,443-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N437 – PubChem

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A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 60122-51-2

Application of 60122-51-2, 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.60122-51-2, Name is 1,7-Naphthyridin-4(1H)-one, molecular formula is C8H6N2O. In a article£¬once mentioned of 60122-51-2

ASTRAZENECA AB; ASTRAZENECA UK LIMITED

The invention concerns naphthyridine derivatives of Formula (Ia) or (Ib) or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, G1, G2, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders or disease states associated with angiogenesis and/or vascular permeability.

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Reference£º
1,441-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N435 – PubChem