We started our SAR (Structure Activity Relationship) study with a micromolar active hit identified by our client. Within 12-month, we succeeded to prepare a series of orally available anti-cancer drug candidates with single digit nanomolar potency. The compounds are active also against resistant carcinomas. Several analogs issued from this series have also proven active in vivo in the nanomolar range. The most advanced of them has completed Phase I and will enter in Phase II clinical trials. Additional research chemistry yielded a backup candidate with improved ADME-Tox and cardiovascular profile that is currently in pre-clinical trial.
Patents issued by this collaboration: WO2004041817, WO2005108398; two more patents have been filed.
Our client provided Prestwick’s chemists with several families of weakly selective tyrosine-kinase inhibitors. After a short period of hit selection, we designed and synthesized selective and original c-kit tyrosine-kinase inhibitors. The compounds act at nanomolar concentrations and present favorable ADME and toxicity profiles. Our client subsequently developed one of the compounds prepared through positive preclinical studies and Phase I clinical studies. It will enter in Phase III clinical trial in S2 2007 for the treatment of mastocytoses.
Corresponding patents: WO 2004014903, WO 2005073225, WO 2005040139
Starting from a validated PDE 10 inhibitor with anti-tumor activity, we succeeded to synthesize in less than 2 years a series of original and highly selective analogues with improved pharmacodynamic profile. Several candidates are available for pre-clinical development. Such compounds may also treat some neurological disorders.
Corresponding patents: WO2005003130, WO2005003129, WO2006075012, WO2006089815
Within 6 months, we were able to transform a weakly active and patented positive ionic channel modulator into a full agonist with an improved potency (x 300). We then significantly improved the family’s chemical pathway and synthetized sufficient additional compounds for patent exemplification. The compound is patentable and is presently developed as a new and original candidate for the treatment of depression.
Patents filed in 2006. Not yet published.
Starting from a quinolone antibiotic patented several years ago by Roche and in only 18 months, we succeeded in preparing several molecules satisfying the selection criteria:
Most of these compounds do not fall under any known patent in a very congested IP environment. One molecule is presently in pre-clinical development.
Patent will be filed in 2008.
Following an initial SAR study of only 5 months, we designed and synthesized a new structurally original prototype relevant as calcium receptor antagonist. Such compounds may be clinically useful in osteoporosis prevention.
Corresponding patent: WO2006066070