Universiteit Leiden

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

Schwarz Pharma Ag

Johannes Brussee

Adriaan Pieter Ijzerman

Kenneth Alan Jacobson

Zhan-Guo Gao

Johanna Aaltje Bouwstra

Klaus Sandrock

Anikó Göblyös

Aniko Goblyos

Lisa Chung Wai Chang

Ferdinand Spies

Maria Hel&egrave;ne Ponec

Henri Ernest Bodd&eacute;

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.

[object Object]

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

The invention relates to pharmaceutical compositions for topical application containing at least one physiologically active agent and an effective amount of 1-oleylazacycloheptan-2-one as the human or animal epithelial membrane permeability enhancer, to the application of such pharmaceutical compositions by means of locally contacting the skin or other membrane of the human or animal with the above composition and to the 1-oleylazacycloheptan-2-one compound per se.

Pharmaceutical compositions containing 1-oleylazacycloheptan-2-one as enhancing agent of transport across biological membranes

Growing community of inventors

Rijnsburg, Netherlands

Johannes Brussee