185563-97-7

Upstream product

• 185563-96-6 N₂-(2,4,6-trimethylbenzenesulfonyl)-L-asparagine 
• 208446-28-0 N-(2,4,6-trimethylphenyl)sulfonyl-L-asparagine 
• 773-64-8 2-mesitylenesulphonyl chloride 

Downstream Products

• 185563-98-8 3S-3-amino-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid tert-butyl ester 
• 1187989-97-4 C₁₆H₂₄N₂O₅S 
• 1187990-00-6 C₁₉H₂₂N₂O₅S 
• 1187989-98-5 C₁₄H₂₀N₂O₆S 
• 214531-92-7 C₁₇H₂₆N₂O₆S 
• 1187989-96-3 C₁₄H₂₀N₂O₅S 
• 1187990-02-8 C₁₉H₂₄N₂O₄S 
• 1187989-99-6 C₁₃H₂₀N₂O₆S₂ 
• 185563-99-9 2-(2,4,6-trimethyl-benzenesulfonylamino)-3-({5-[4-(1-trityl-1H-imidazol-2-ylamino)-butyl]-4,5-dihydro-isoxazole-3-carbonyl}-amino)-propionic acid tert-butyl ester 
• 185564-00-5 2-(2,4,6-trimethyl-benzenesulfonylamino)-3-({5-[4-(1-trityl-1H-imidazol-2-ylamino)-butyl]-4,5-dihydro-isoxazole-3-carbonyl}-amino)-propionic acid 
• 258845-46-4 2-(2,4,6-trimethyl-benzenesulfonylamino)-3-({5-[2-(1-trityl-1H-imidazol-2-ylamino)-ethyl]-4,5-dihydro-isoxazole-3-carbonyl}-amino)-propionic acid 
• 258845-24-8 3-({5-[3-(2-acetylamino-3H-imidazol-4-yl)-propyl]-4,5-dihydro-isoxazole-3-carbonyl}-amino)-2-(2,4,6-trimethyl-benzenesulfonylamino)-propionic acid tert-butyl ester 
• 258845-36-2 3-[(5-{2-[3-(1H-imidazol-2-yl)-ureido]-ethyl}-4,5-dihydro-isoxazole-3-carbonyl)-amino]-2-(2,4,6-trimethyl-benzenesulfonylamino)-propionic acid tert-butyl ester 
• 258845-30-6 3-({5-[3-(1H-imidazol-2-ylcarbamoyl)-propyl]-4,5-dihydro-isoxazole-3-carbonyl}-amino)-2-(2,4,6-trimethyl-benzenesulfonylamino)-propionic acid tert-butyl ester 

Relevant academic research and scientific papers

Novel inhibitors of the αvβ3 integrin-lead identification strategy

A novel approach to inhibition of the αvβ3 integrin is described, which uses compounds designed to generate nM potency without using the arginine binding site.

Integrin antagonists

This invention relates to novel heterocycles which are useful as antagonists of the αvβ3 integrin, the α2bβ3 integrin, and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

Isoxazolines as potent antagonists of the integrin α(v)β3

Starting with lead compound 2, we sought to increase the selectivity for α(v)β3-mediated cell adhesion by examining the effects of structural changes in both the guanidine mimetic and the substituent α to the carboxylate. To prepare some of the desired aminoimidazoles, a novel reductive amination utilizing a trityl-protected aminoimidazole was developed. It was found that guanidine mimetics with a wide range of pK(a)'s were potent antagonists of α(v)β3. In general, it appeared that an acylated 2-aminoimidazole guanidine mimetic imparted excellent selectivity for α(v)β3-mediated adhesion versus α(IIb)β3-mediated platelet aggregation, with selectivity of approximately 3 orders of magnitude observed for compounds 3g and 3h. It was also found in this series that the α- substituent was required for potent activity and that 2,6-disubstituted arylsulfonamides were optimal. In addition, the selective α(v)β3 antagonist 3h was found to be a potent inhibitor of α(v)β3-mediated cell migration.

1,3,4-thiadiazoles and 1,3,4-Oxadiazoles as alpha v beta 3 antagonists

This invention relates to 1,3,4-thiadiazoles and 1,3,4-Oxadiazoles of Formula (I) which are useful as antagonists of alpha v beta 3 and related integrin receptors, to pharmaceutical compositions containing such compounds, alone or in combination with othe

Integrin receptor antagonists

This invention relates to novel heterocycles including 3-?1-?3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, which are useful as antagonists of the αv β3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.