220880-36-4

Upstream product

• 219496-61-4 (S)-2-tert-butoxycarbonylamino-3-[4-(2,6-dichloro-benzoylamino)-phenyl]-propionic acid methyl ester 
• 65615-90-9 (S)-methyl 3-(4-aminophenyl)-2-((tert-butoxycarbonyl)amino)propanoate 
• 65615-89-6 methyl (S)-2-((tert-butoxycarbonyl)amino)-3-(4-nitrophenyl)propanoate 
• 33305-77-0 Boc-Phe(p-NO₂)-OH 
• 103724-64-7 1-(2-bromoethyl)cyclopentane carboxylic acid methyl ester 
• 220875-87-6 1-(2-azido-ethyl)-cyclopentanecarboxylic acid 

Downstream Products

• 1448718-98-6 (S)-2-{[1-(2-amino-ethyl)-cyclopentanecarbonyl]-amino}-3-[4-(2,6-dichloro-benzoylamino)-phenyl]-propionic acid tert-butyl ester 
• 1448718-97-5 (S)-2-[[1-(2-azido-ethyl)-cyclopentanecarbonyl]-amino]-3-[4-(2,6-dichloro-benzoylamino)-phenyl]-propionic acid tert-butyl ester 
• 220877-86-1 (S)-2-[[[1-(2-amino ethyl)cyclopentyl]carbonyl]amino]-3-[4-(2,6-dichlorobenzoylamino)phenyl]propionic acid methyl ester 

Relevant academic research and scientific papers

Lipid Compounds Targeting VLA-4

The invention relates to the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein n, G, W, X, Y, and R1 are defined in the detailed description and claims. The compounds of formula I bind to or associate with VLA-4 and can be used in delivery formulations to deliver drugs, nucleic acids, or other therapeutic compounds to tissues or cells expressing VLA-4.

INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING VLA-4

The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to VLA-4 integrin antagonists to target cells expressing VLA-4.

CHITOSAN COVALENTLY LINKED WITH SMALL MOLECULE INTEGRIN ANTAGONIST FOR TARGETED DELIVERY

The invention relates to the chitosan polymer derivatives of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Y, X1, X4, R1, R2, and n are defined in the detailed description and claims. The chitosan polymer derivatives of formula I bind to or associate with alpha-4-beta-1 (α4β1) and alpha-V-beta-3 (αVβ3) integrin dimers and can be used in delivery formulations to deliver drugs, nucleic acids, or other therapeutic compounds to tissues or cells expressing such integrins.

N-Cycloalkanoyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.

A systematic structure-activity relationship investigation of the lead compound 1 resulted the identification of several N-[(substituted alkyl)cycloalkanoyl]-4-[((2,6-dichlorophenyl)carbonyl)amino]-L-phenylalanine derivatives as potent VCAM/VLA-4 antagonists. The data are consistent with a model of these compounds in which these alkanoylphenylalanines reside in a compact gauche (-) bioactive conformation.