Sanofi

Thomas Olpp

Dieter Kadereit

Pradeep K Dhal

Michael Wagner

Andreas Evers

James E Stefano

Martin Bossart

Nino Meyer

Paul Konowicz

Klaus Wirth

Herman Schreuder

Christian Buning

Sven Ruf

Thorsten Sadowski

Georg Horstick

Nils Poth

Peyman Sakhaii

Josef Pernerstorfer

Torsten Haack

Katrin Lorenz

Kai Rossen

Bodo Scheiper

Volker Kraft

Gerhard Kretzschmar

Magnus Besev

Robert Miller

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 -L-L-L-L-Y&#x2014;Rgroups, wherein Y represents an GLP-1/Glucagon receptor agonist moiety; and -L is a linker moiety&#x2014;by formula (Ia), 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 the conjugate or the pharmaceutically acceptable salt thereof 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.

Conjugates comprising an GLP-1/Glucagon dual agonist, a linker and hyaluronic acid

The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising an GLP-1/Glucagon agonist linker conjugate Z-L-L-L-Y&#x2014;R, wherein Y represents an GLP-1/Glucagon agonist moiety; and -L is a linker moiety&#x2014;by formula (Ia), wherein the dashed line indicates the attachment to one of the amino groups of the GLP-1/Glucagon agonist 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 GLP-1/Glucagon agonist. 

Prodrugs comprising an GLP-1/glucagon dual agonist linker hyaluronic acid conjugate

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&#x2014;R20 groups, wherein Y represents an GLP-1/Glucagon receptor agonist moiety; and -L is a linker moiety&#x2014;by formula (Ia), 

Conjugates comprising an GLP-1/glucagon dual agonist, a linker and hyaluronic acid

The present invention relates to compounds of the formula I, wherein A, D, E, G, R, R, R, R, Rand Rhave the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Amino-substituted 3-heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals

A process for the production of 2-alkyl-3-aroyl-5-nitrobenzofurans by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-aryl-ethanones and subsequent treatment of the esters with combinations of bases and proton acids or Lewis acids. This process can be used for the production of Dronedarone. Furthermore, novel intermediates for the manufacture of Dronedarone are provided.

Process for the production of benzofurans

The present invention relates to compounds of the formula I, wherein A, D, E, G, R, R, R, Rand Rhave the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them. 

Oxygen-substituted 3-heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals

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Frankfurt am Main, Germany

Thomas Olpp