556053-94-2

Upstream product

• 556053-93-1 3-(5-benzyloxypentyl)pentanedioic acid diethyl ester 
• 111-29-5 1 ,5-pentanediol 
• 1014-93-3 1-(benzyloxy)-5-bromopentane 
• 4541-15-5 5-(benzyloxy)-1-pentanol 
• 100-44-7 benzyl chloride 
• 84885-76-7 (((5-iodopentyl)oxy)methyl)benzene 
• 186374-96-9 5-(benzyloxy)pentyl methanesulfonate 

Downstream Products

• 556053-95-3 methanesulfonic acid 7-benzyloxy-2-(methanesulfonyloxymethyl)heptyl ester 
• 556054-36-5 4-(5-benzyloxypentyl)[1,2]dithiolane 

Relevant academic research and scientific papers

LEPTIN mRNA COMPOSITIONS AND FORMULATIONS

A formulation comprising a modified synthetic messenger RNA and a delivery agent. The modified synthetic messenger RNA encodes a leptin protein, is non-replicating and is translation-ready. The formulation can be delivered to a subject with congenital leptin deficiency, lipodystrophy or other condition where circulating leptin level is low.

LIPIDS AND LIPID COMPOSITIONS FOR THE DELIVERY OF ACTIVE AGENTS

This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, n and p are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

LIPIDS AND LIPID COMPOSITIONS FOR THE DELIVERY OF ACTIVE AGENTS

This invention provides for a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R3, n, p, L1 and L2 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

Synthesis and pharmacological evaluation of new 1,2-dithiolane based antioxidants

Molecules containing a dithiolane moiety are widely investigated due to their antioxidant properties. The archetypal representative of this class of compounds is lipoic acid and indeed the lipoic acid-dihydrolipoic acid couple is part of the antioxidant defence system of the cell. In the course of a program aiming to find improved antioxidants effective in vivo, we designed, synthesised and pharmacologically investigated new lipoic acid analogs. The salient feature of these structures is the connection, via a thioamide or a thiocarbamate, of a 1,2-dithiolane moiety bearing a carbon chain and a N-alkyl-substituted morpholine ring. It was expected that the antioxidant and chelating properties of these functional groups combined with the basicity of the morpholine ring will impact on the antioxidant as well as on the partition and solubility characteristics of the compounds. Indeed in vitro and in vivo pharmacological investigation showed that these new molecules and especially those containing a thiocarbamate linker possess superior antioxidant properties compared with α-lipoic acid and to the amide or carbamate linker analogs. In particular, some of these compounds efficiently cross the blood brain barrier (BBB) thus providing efficient protection from lethality in a situation of induced oxidative stress. Moreover the absence of the 1,2-dithiolane moiety does not completely abolish antioxidant effects thus demonstrating that these compounds are distinct new chemical entities and not merely lipoic acid prodrugs. The chemical and pharmacological features of these new antioxidants are presented and discussed in the following paper.

Synthesis of extremely simplified compounds possessing the key pharmacophore units of taxol, phenylisoserine and oxetane moieties

Straight chain compounds having a phenylisoserine unit and an oxetane ring at the α- and ω- position, respectively as extremely simplified analogues of taxol were prepared. None of these compounds showed promising tubulin inhibitory activity.