Universiteit Leiden

National Institutes of Health, a Component of the US Dept. of Health & Human Services

Gruenenthal Gmbh

Leiden University

Adriaan Pieter Ijzerman

Johannes Brussee

Bernd Sundermann

Kenneth Alan Jacobson

Zhan-Guo Gao

Matthias Gerlach

Corinna Sundermann

Utz-Peter Jagusch

Claudia Katharina Puetz

Reynier Tromp

Anikó Göblyös

Aniko Goblyos

Lisa Chung Wai Chang

Jacobien Von Frijtag Drabbe Kuenzel

Corrinna Sundermann

Martin Fuhr

Miriam Dissen-De Groote

The claimed subject matter relates to allosteric modulation of Aadenosine receptor (AAR) and provides for the use of an Aadenosine receptor modulator (ARM), for the preparation of pharmaceutical compositions for modulating the AAR in a subject, as well as pharmaceutical compositions including the same and therapeutic methods including administering to a subject an amount of an ARM, the amount being effective to modulate AAR activity. The ARM according to claimed subject matter are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives. Also provided are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives.

A3 adenosine receptor allosteric modulators

The present invention relates to allosteric modulation of Aadenosine receptor (AAR) and provides for the use of an Aadenosine receptor modulator (ARM), for the preparation of pharmaceutical compositions for modulating the AAR in a subject, as well as pharmaceutical compositions comprising the same and therapeutic methods comprising administering to a subject an amount of an ARM, the amount being effective to modulate AAR activity. The ARM according to the invention are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives. The invention also provides some of such novel 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives.

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The invention provides a compound of formula (I) wherein R and R' are selected from hydrogen, alkyl, alkenyl, alkynyl, or aryl; R&#x2033; and R&#x2032;&#x2033; are selected from hydrogen, acyl, thio-acyl, seleno-acyl, alkyl, alkenyl, alkynyl, or aryl; or a pharmaceutically acceptable salt thereof, to interact with the adenosine receptors in the beneficial treatment and/or prevention of a (dis)order arising from the said receptors. The invention further provides pharmaceutical compositions comprising said compounds. The invention also relates to the use of said compositions for treating an/or preventing a variety of diseases. 

Substituted pyrimidines as ligands of adenosine receptors

Analogs or derivatives of nitrobenzylthioinosine compounds. The use of these new analogs of nitrobenzylthioinosine and methods for the treatment of pain and various other indications using these analogs of nitrobenzylthioinosine as well as pharmaceutical compositions including analogs of nitrobenzylthioinosine.

Analogs of nitrobenzylthioinosine

Substituted pyrazolopyrimidines and thiazolopyrimidines, specifically, compounds corresponding to the structure (I A), (I B) or (II) processes for their preparation, substance libraries containing them, pharmaceutical formulations containing these compounds, the use of these compounds for the production of medicaments for the treatment and/or prophylaxis of pain and related treatment methods are provided.

Substituted pyrazolopyrimidines and thiazolopyrimidines

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Haarlem, Netherlands

Adriaan Pieter Ijzerman