324781-26-2

Upstream product

• 451-46-7 4-fluorobenzoic acid ethyl ester 
• 25437-94-9 ethyl 4-(4-hydroxypiperidin-1-yl)benzoate 
• 247034-87-3 ethyl 4-(4-phthalimidopiperidin-1-yl)benzoate 
• 247034-89-5 ethyl 4-{4-(pyrimidin-2-ylamino)piperidin-1-yl}benzoate 
• 5382-16-1 4-HYDROXYPIPERIDINE 
• 247034-90-8 4-{4-(Pyrimidin-2-ylamino)piperidin-1-yl}benzoic acid 
• 247034-88-4 ethyl 4-(4-aminopiperidin-1-yl)benzoate 
• 324781-24-0 t-butyl (2S)-hydroxy-3-[4-{4-(pyrimidin-2-ylamino)-piperidin-1-yl}benzoylamino]propionate 

Relevant academic research and scientific papers

Tricyclic pharmacophore-based molecules as novel integrin αvβ3 antagonists. Part 2: Synthesis of potent αvβ3/αIIbβ3 dual antagonists

We synthesized 4-aminopiperidine derivatives of our prototype integrin αvβ3 antagonist 1 in an attempt to increase the activity and water solubility. Introduction of one or two hydrophilic moieties into the central aromatic ring and/or the benzene ring at the C-terminus of 1 increased water solubility and enhanced inhibition of cell adhesion. The results of a structure-activity relationships (SAR) study indicated that the torsion angle between the central aromatic ring and the piperidine ring, and the acidity at the sulfonamide moiety, might be important for αvβ 3 receptor binding activity. Some of these compounds are novel and potent αvβ3/αIIbβ 3 dual antagonists with acceptable water solubility and a satisfactory early absorption, distribution, metabolism, excretion, and toxicity (ADMET) profile.

OMEGA-AMINO-ALPHA-HYDROXYCARBOXYLIC ACID DERIVATIVES HAVING INTEGRIN ALPHA V BETA 3 ANTAGONISM

An objective of the present invention is to provide highly water-soluble compounds having integrin ανβ3 antagonistic activity. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutic