911716-00-2Relevant academic research and scientific papers
Substituted 7-amino-5-thio-thiazolo[4,5- d ]pyrimidines as potent and selective antagonists of the fractalkine receptor (CX3CR1)
Karlstr?m, Sofia,Nordvall, Gunnar,Sohn, Daniel,Hettman, Andreas,Turek, Dominika,?hlin, Kristofer,Kers, Annika,Claesson, Martina,Slivo, Can,Lo-Alfredsson, Yvonne,Petersson, Carl,Bessidskaia, Galina,Svensson, Per H.,Rein, Tobias,Jerning, Eva,Malmberg, ?sa,Ahlgen, Charlotte,Ray, Colin,Vares, Lauri,Ivanov, Vladimir,Johansson, Rolf
supporting information, p. 3177 - 3190 (2013/06/05)
We have developed two parallel series, A and B, of CX3CR1 antagonists for the treatment of multiple sclerosis. By modifying the substituents on the 7-amino-5-thio-thiazolo[4,5-d]pyrimidine core structure, we were able to achieve compounds with high selectivity for CX3CR1 over the closely related CXCR2 receptor. The structure-activity relationships showed that a leucinol moiety attached to the core-structure in the 7-position together with α-methyl branched benzyl derivatives in the 5-position displayed promising affinity, and selectivity as well as physicochemical properties, as exemplified by compounds 18a and 24h. We show the preparation of the first potent and selective orally available CX3CR1 antagonists.
NOVEL 5-SUBSTITUTED 7-AMINO-[1,3]THIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES
-
Page/Page column 22-23, (2010/11/24)
There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the specification, and pharmaceutically accept
NOVEL 5,7-DISUBSTITUTED [1,3]THIAZOLO[4,5-D]PYRIMIDIN-2(3H)-ONE DERIVATIVES
-
Page/Page column 46; 49-50, (2008/06/13)
There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) [Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, R3, R4 and R5 are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.
