1194550-63-4

Upstream product

• 1194550-56-5 5,7-dichloro-2-trityl-1,2,3,4-tetrahydroisoquinoline-6-carboxylic acid 
• 10203-08-4 3,5-dichlorobenzaldehyde 
• 1289646-72-5 C₂₈H₂₃Cl₂N 
• 14046-52-7 N-(2-chloroethyl)-3,5-dichlorobenzylamine hydrochloride 
• 1194550-59-8 (2S)-2-amino-3-(3-(methanesulfonyl)phenyl)propionic acid benzyl ester hydrochloride 
• 1289646-78-1 (S)-benzyl 2-((tert-butoxycarbonyl)amino)-3-((3-methylsulfonyl)phenyl)propionate 
• 1289646-76-9 (S)-2-((tert-butoxycarbonyl)amino)-3-((3-methylsulfonyl)phenyl)propanol 
• 82278-73-7 (2S)-3-(3-bromophenyl)-2-[(tert-butoxycarbonyl)amino]propanoic acid 
• 73075-47-5 5,7-dichloro-1,2,3,4-tetrahydroisoquinoline hydrochloride 
• 73075-58-8 5,7-dichloro isoquinoline 
• 1000210-73-0 (3,5-dichloro-benzylidene)-(2,2-diethoxy-ethyl)-amine 
• 82311-69-1 (S)-2-amino-3-(3-bromophenyl)propanoic acid 
• 89315-56-0 5,7-dichloro-1,2,3,4-tetrahydroisoquinoline 

Downstream Products

• 1194550-65-6 benzyl (S)-2-(5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-[3-(methylsulfonyl)phenyl]propanoate hydrochloride 
• 1194550-67-8 ((S)-benzyl 2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-methylsulfonyl)phenyl)propanoate 
• 1025967-78-5 (S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid 
• 851785-70-1 (S)-2-(5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid 

Relevant academic research and scientific papers

PROCESSES FOR PREPARATION OF LIFITEGRAST AND INTERMEDIATES THEREOF

The present invention provides process for preparation of lifitegrast, amine salts of lifitegrast, process for preparation of amine salts of lifitegrast and their use in purification of lifitegrast, and also provided are process for preparation of amorphous lifitegrast and pharmaceutical compositions comprising lifitegrast prepared by the processes of the present invention.

LFA-1 INHIBITOR AND POLYMORPH THEREOF

Methods of preparation and purification of a compound, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA -1 mediated diseases are also disclosed.

Discovery and development of potent LFA-1/ICAM-1 antagonist SAR 1118 as an ophthalmic solution for treating dry eye

LFA-1/ICAM-1 interaction is essential in support of inflammatory and specific T-cell regulated immune responses by mediating cell adhesion, leukocyte extravasation, migration, antigen presentation, formation of immunological synapse, and augmentation of T-cell receptor signaling. The increase of ICAM-1 expression levels in conjunctival epithelial cells and acinar cells was observed in animal models and patients diagnosed with dry eye. Therefore, it has been hypothesized that small molecule LFA-1/ICAM-1 antagonists could be an effective topical treatment for dry eye. In this letter, we describe the discovery of a potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonist (SAR 1118) and its development as an ophthalmic solution for treating dry eye.