1263430-76-7

Upstream product

• 80441-55-0 6-(S-tritylmercapto)hexanoic acid 
• 107-15-3 ethylenediamine 
• 14470-28-1 mono-4-methoxytrityl chloride 
• 109938-55-8 mono-m-methoxytrityl chloride 
• 924273-15-4 6-(S-tritylsulfanyl)-hexaneamine 
• 114729-69-0 N¹-((4-methoxyphenyl)diphenylmethyl)ethane-1,2-diamine 

Downstream Products

• 1263430-78-9 C₅₂H₅₈N₂O₃S 

Relevant academic research and scientific papers

BIODEGRADABLE POLYETHYLENE GLYCOL BASED WATER-INSOLUBLE HYDROGELS

The invention relates to a process for the preparation of a hydrogel prodrug, comprising the steps of (a) providing a reactive biodegradable hydrogel, wherein said hydrogel comprises backbone moieties which are linked together through crosslinker moieties, each crosslinker moiety being terminated by at least two hydrolytically degradable bonds, and wherein from a branching core 3 to 16 linear PEG-based polymeric chains extend and wherein one terminus of said polymeric chains is connected to the branching core and the other to a hyperbranched dendritic moiety; wherein each said hyperbranched dendritic moiety has at least 3 branchings and at least 4 reactive functional groups; (b) conjugating a prodrug linker to a biologically active moiety, resulting in a biologically active moiety-prodrug linker conjugate; and (c) reacting the biologically active moiety-prodrug linker conjugate from step (b) with the reactive functional groups of the hydrogel of step (a). The invention further relates to a hydrogel prodrug obtainable from the process.

PRODRUGS COMPRISING AN EXENDIN LINKER CONJUGATE

The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising an exendin linker conjugate D-L, wherein D represents an exendin moiety; and -L is a non-biologically active linker moiety -L 1 represented by formula (I), wherein the dashed line indicates the attachment to one of the amino groups of the exendin moiety by forming an amide bond. The invention further relates to pharmaceutical compositions comprising said prodrugs as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by exendin.

CONJUGATES COMPRISING AN GLP-1/GLUCAGON/GIP TRIPLE RECEPTOR AGONIST, A LINKER AND HYALURONIC ACID

The present invention relates to a conjugate or a pharmaceutically acceptable salt thereof comprising an GLP-1/Glucagon/GIP triple receptor agonist, a linker and a hyaluronic acid hydrogel bearing - L1 -L2 - L - Y - R20 groups, wherein Y represents an GLP-1/Glucagon/GIP triple receptor agonist moiety; and -L is a linker moiety - by formula (la), wherein the dashed line indicates the attachment to one of the amino groups of the GLP-1/Glucagon/GIP triple receptor agonist moiety by forming an amide bond. The invention further relates to pharmaceutical compositions comprising said conjugates as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by GLP-1/Glucagon/GIP triple receptor agonist.

CONJUGATES COMPRISING AN GLP-1/GLUCAGON DUAL AGONIST, A LINKER AND HYALURONIC ACID

The present invention relates to a conjugate or a pharmaceutically acceptable salt thereof comprising an GLP-1/Glucagon receptor agonist, a linker and a hyaluronic acid hydrogel bearing -L1-L2-L-Y—R20 groups, wherein Y represents an GLP-1/Glucagon receptor agonist moiety; and -L is a linker moiety—by formula (la), wherein the dashed line indicates the attachment to one of the amino groups of the GLP-1/Glucagon receptor agonist moiety by forming an amide bond. The invention further relates to pharmaceutical compositions comprising said conjugates as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by GLP-1/Glucagon receptor agonist.

DOSAGE REGIMEN FOR A CONTROLLED-RELEASE PTH COMPOUND

The present invention relates to a pharmaceutical composition comprising at least one controlled-release PTH compound or a pharmaceutically acceptable salt, hydrate or solvate thereof, for use in the treatment, control, delay or prevention of a condition

PTH COMPOUNDS WITH LOW PEAK-TO-TROUGH RATIOS

The present invention relates to a pharmaceutical composition comprising a PTH compound, wherein after subcutaneous administration the pharmacokinetic profile of the PTH compound exhibits a peak to trough ratio of less than 4 within one injection interval

INCREMENTAL DOSE FINDING IN CONTROLLED-RELEASE PTH COMPOUNDS

The present invention relates to pharmaceutical compositions comprising a controlled-release PTH compound or a pharmaceutically acceptable salt, hydrate, or solvate thereof, for use in a method of treating, controlling, delaying or preventing a condition

Sustained release composition of prostacyclin

The present invention relates to sustained release compositions of prostacyclin, as well as uses thereof, in particular for the prevention and/or treatment of pulmonary arterial hypertension.

PTH PRODRUGS

The present invention relates to PTH prodrugs, pharmaceutical compositions comprising such PTH prodrugs and their uses.

Carrier-linked treprostinil prodrugs

The present invention relates to prodrugs or a pharmaceutically acceptable salt thereof comprising a covalent treprostinil carrier conjugate as well as pharmaceutical composition comprising said compounds. The compounds may be used as medicaments, especially for diseases or disorders which can be treated by treprostinil, such as pulmonary arterial hypertension (PAH).