859855-38-2

Upstream product

• 67-56-1 methanol 
• 859855-37-1 (3S,4S)-4-((S)-1-phenylethylamino)piperidine-1,3-dicarboxylic acid 1-tert-butyl ester 3-methyl ester 

Downstream Products

• 859855-39-3 (3S,4S)-1-tert-butyl 3-methyl 4-(benzyloxycarbonylamino)piperidine-1,3-dicarboxylate 

Relevant academic research and scientific papers

Discovery of the Potent, Selective, Orally Available CXCR7 Antagonist ACT-1004-1239

The chemokine receptor CXCR7, also known as ACKR3, is a seven-transmembrane G-protein-coupled receptor (GPCR) involved in various pathologies such as neurological diseases, autoimmune diseases, and cancers. By binding and scavenging the chemokines CXCL11 and CXCL12, CXCR7 regulates their extracellular levels. From an original high-throughput screening campaign emerged hit 3 among others. The hit-to-lead optimization led to the discovery of a novel chemotype series exemplified by the trans racemic compound 11i. This series provided CXCR7 antagonists that block CXCL11- and CXCL12-induced ?-arrestin recruitment. Further structural modifications on the trisubstituted piperidine scaffold of 11i yielded compounds with high CXCR7 antagonistic activities and balanced ADMET properties. The effort described herein culminated in the discovery of ACT-1004-1239 (28f). Biological characterization of ACT-1004-1239 demonstrated that it is a potent, insurmountable antagonist. Oral administration of ACT-1004-1239 in mice up to 100 mg/kg led to a dose-dependent increase of plasma CXCL12 concentration.

PIPERIDINE CXCR7 RECEPTOR MODULATORS

The present invention relates to piperidine derivatives of formula (I) wherein Ar1, Ar2, RAr1, R1, R2, and R3 are as described in the description, their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.

PYRROLOTRIAZINE COMPOUNDS AS KINASE INHIBITORS

The present invention provides compounds of formula (I); and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula (I) compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.