Vassilis Aidinis Research Group

Thieno[3,4-c]pyrazol-3-yl acetamides as autotaxin inhibitors.

PCT International Application WO 2022/003377 A1; Inventors: Vassilios Aidinis and Alexios Matralis; Owners: B.S.R.C. "Alexander Fleming" and Uni-Pharma Kleon Tsetis Pharmaceutical Laboratories S.A.
Priority 2020-07-02  Filing 2021-07-02 Publication 2022-01-07

A pharmaceutical compound or pharmaceutically acceptable salt thereof, for use in the treatment of pulmonary fibrosis, pulmonary allograft fibrosis, hepatic fibrosis, renal fibrosis, cardiac fibrosis, pneumonia, Covid-19 disease, bacterial infection, rheumatoid arthritis, neurodegenerative diseases, diseases related to metabolic syndrome and cancer, due to autotaxin inhibition, having the chemical formula (A), wherein: -R1 is selected from a heterocyclic group, or a heteroaromatic group, or an aromatic group which is selected from 4-bromophenyl, 4-carboxyphenyl- or 4-nitrophenyl-groups, R2 is independently selected from an alkyl carbon chain or from a cyclic hydrocarbon or from one or more heterocyclic, aromatic, heteroaromatic rings, wherein each ring may carry one of more substituents selected from hydrogen, halogen, nitro-, methoxy-, and carboxylic-group or from a group -CR3R4Ar wherein R3 and R4 are selected from hydrogen, (C1-6)alkyl, trifluoromethyl- , methoxy- or (C3-7)cycloalkane and Ar is an aromatic or heteroaromatic ring.

Autotaxin pathway modulation and uses thereof.

EP US WO Application WO2011151461A2 Vassilios Aidinis B.S.R.C. "Alexander Fleming" 
Priority 2010-06-04 • Filing 2011-06-03 • Publication 2011-12-08

Disclosed are methods for preventing, treating, or reducing symptoms of a disorder involving the autotaxin (ATX) pathway. In one embodiment, the method features administering to a mammal a sufficient amount of an autotaxin (ATX) or lysophosphatidic acid (LPA) signaling inhibitor, to prevent, treat or reduce symptoms of an inflammatory disorder, autoimmune disorder, fibrosis or malignancy of the lung. Further disclosed are methods for diagnosing an autotaxin-related disorder as well as kits for performing the methods of the invention.

Deregulated Genes and/or Processes in Inflammatory Arthritis.

EP JP US WO Application US20080311185A1  Georgios Kollias,  Vassilios Aidinis, Yoshishide Hayashizaki,  Piero Carninci
Priority 2005-10-19 • Filing 2006-10-19 • Publication 2008-12-18

The invention provides means and methods for determining whether a sample is derived from an individual suffering from inflammatory arthritis or from an individual at risk of suffering there from, said method comprising measuring in said sample the level of expression of at least one gene product of a gene of table A, table B or and comparing said expression level with a reference value. Further provided is a non-human animal model comprising an altered expression of a gene of table A, table B or when compared to a reference non-human animal, and use of this model as or in an arthritis model. Further provided is an in vitro assay for screening compounds for effect on a phenotype of synovial fibroblasts. The synovial fibroblast are preferably derived from a human or non-human animal suffering from inflammatory arthritis.