227963-15-7

Usage

Uses

Used in Pharmaceutical Industry:
(S)-3-(6-methoxypyridin-3-yl)-3-(2-oxo-3-(3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl)imidazolidin-1-yl)propanoic acid is used as a potential pharmaceutical candidate for [application reason] due to its complex molecular structure and the presence of various functional groups that may interact with biological targets.
Used in Chemical Research:
In the field of chemical research, (S)-3-(6-methoxypyridin-3-yl)-3-(2-oxo-3-(3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl)imidazolidin-1-yl)propanoic acid serves as a subject for studying [application reason], such as its reactivity, stability, or potential to form new compounds with desired properties.

Upstream product

• 7521-41-7 2-Aminonicotinaldehyde 
• 204452-91-5 3(S)-(6-methoxypyridin-3-yl)-3-alanine tert-butyl ester p-toluenesulfonic acid 
• 227963-56-6 3(S)-(6-methoxypyridin-3-yl)-3-{2-oxo-[3-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)propyl]imidazolidin-1-yl}propionic acid ethyl ester 
• 339555-37-2 tert-butyl (2E)-3-(6-methoxypyridin-3-yl)prop-2-enoate 
• 37732-87-9 1-allyl-2-imidazolidone 
• 65873-72-5 6-methoxy-3-pyridinecarboxaldehyde 
• 339555-40-7 tert-butyl (3S)-3-{benzyl[(1R)-1-phenylethyl]amino}-3-(6-methoxypyridin-3-yl)propanoate 
• 13472-85-0 2-methoxy-5-bromopyridine 
• 227963-49-7 [(methoxy-methyl-carbamoyl)-methyl]-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-propyl]-carbamic acid tert-butyl ester 
• 227963-48-6 {tert-butoxycarbonyl-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)propyl]amino}acetic acid ethyl ester 
• 227752-09-2 N-benzyl-(R)-α-methylbenzyl-3(S)-(6-methoxypyridin-3-yl)-β-alanine ethyl ester 
• 227963-45-3 {tert-butoxycarbonyl-[3-(2-methyl-[1,3]dioxolan-2-yl)-propyl]-amino}-acetic acid ethyl ester 
• 227963-46-4 [tert-butoxycarbonyl-(4-oxopentyl)amino]acetic acid ethyl ester 
• 227963-44-2 [3-(2-methyl-[1,3]dioxolan-2-yl)-propylamino]-acetic acid ethyl ester 

Relevant academic research and scientific papers

Thermodynamic Understanding of an Aza-Michael Reaction Enables Five-Step Synthesis of the Potent Integrin Inhibitor MK-0429

We describe a general strategy for the aza-Michael addition of nucleophilic heterocycles into β-substituted acrylates using potassium tert-butoxide as catalyst. Demonstrating that the reaction is under thermodynamic control underpins optimization efforts and enables rapid exploration of the substrate scope, with yields ranging from 55% to 94%. We further leverage these lessons in a significantly shortened synthesis of MK-0429, a potent pan-integrin inhibitor previously taken into human clinical trials for the treatment of prostate cancer and osteoporosis.

COMPOSITION AND METHODS FOR TREATING CHRONIC KIDNEY DISEASE

This invention relates to the treatment of chronic kidney disease, including diabetic nephropathy, focal segmental glomerulosclerosis (FSGS), nephrotic syndrome, non-diabetic chronic kidney disease, renal fibrosis or acute kidney injury by the administrat

An efficient synthesis of an alphavbeta3 antagonist.

A practical preparation of an alpha(v)beta(3) antagonist is reported. The antagonist consists of three key components, a tetrahydronaphthyridine moiety, a beta-alanine moiety, and a central imidazolidone moiety. The tetrahydronaphthyridine component was p

Nonpeptide αvβ3 Antagonists. 8. In Vitro and in Vivo Evaluation of a Potent αvβ3 Antagonist for the Prevention and Treatment of Osteoporosis

3(S)-(6-Methoxypyridin-3-yl)-3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8] -naphthyridin-2-yl)propyl]-imidazolidin-1-yl}propionic acid 6 was identified as a potent and selective antagonist of the αvβ3 receptor. This compound has an excellent in vitro profile (IC50 = 0.08 nM), a significant unbound fraction in human plasma (12%), and good pharmacokinetics in rat, dog, and rhesus monkey. On the basis of the efficacy shown in three in vivo models of bone turnover, the compound was selected for clinical development. To support the ongoing metabolism and safety studies, a novel strategy was employed in which a series of oxidized derivatives of 6 were prepared by exposure of 6 (or the methyl ester) to chemical oxidizing agents. These products proved useful in the identification of active metabolites generated by either in vitro or in vivo metabolism.

Process and intermediates for the preparation of imidazolidinone αv integrin antagonists

A novel process is provided for the preparation of imidazolidinone αvβ3/αvβ5 integrin antagonists, and the useful intermediates obtained therein. These compounds are antagonists of αvβ3/αvβ5 integrin receptors and thus useful for inhibiting bone resorption and treating and preventing osteoporosis. Also disclosed is 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3(S)-(6-methoxy-pyridin-3-yl)-propionic acid in the form of a hemihydrate.

Integrin receptor antagonists

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors alpha v beta 3, alpha v beta 5 and/or alpha v beta 6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, and tumor growth and metastasis.