Inflectis Bioscience

United Kingdom Research and Innovation

Hybrigenics S.a.

Merck Patent Gmbh

Medical Research Council

Philippe Guedat

Anne Bertolotti

Jean-Christophe Rain

Frédéric Colland

Etienne Formstecher

Xavier Jacq

Laurent Daviet

Rémi Delansorne

Olivier Chevreuil

Guillaume Boissy

Matteo Colombo

Catherine Borg-Capra

Francois Collonges

Thierry Convard

Stéphane Yvon

Hervé Dumas

Peter Kane

Marie Noelle Denault

Julia Lainton

Avril Robertson

Pierre Miniou

Bernd Wendt

Stefania Vallese

Ilaria Peretto

Stefano Vignando

The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof,  and its uses to treat a disorder associated with protein misfolding stress and in particular with an accumulation of misfolded proteins.

O-alkyl-benzylideneguanidine derivatives and therapeutic use for the treatment of disorders associated with an accumulation of misfolded proteins

The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein: Ris alkyl, Cl, F or Br; Ris H or F; Ris selected from H and alkyl; Ris selected from H and C(O)R; Ris H; or Rand Rare linked to form a heterocyclic group which is optionally substituted with one or more Rgroups; Ris selected from R, ORand NRR; R, Rand Rare each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocyclyl and aryl, each of which is optionally substituted with one or more Rgroups; each Ris independently selected from halogen, OH, CN, NO, COO-alkyl, aralkyl, SO-alkyl, SO-aryl, COOH, CO-alkyl, CO-aryl, NH, NH-alkyl, N(alkyl), CF, alkyl and alkoxy; X and Z are each independently CR, and Y is selected from CRand N; and Ris H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.

Benzylideneguanidine derivatives and therapeutic use for the treatment of protein misfolding diseases

The present invention relates to novel uses of a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, in treating a disorder associated with the PPP1R15A pathway and associated with protein misfolding stress and in particular with accumulation of misfolded proteins selected in the group of tauopathies, synucleinopathies, polyglutamine and polyalanine diseases, leukodystrophies, cystic fibrosis, multiple sclerosis, lysosomal storage disorders, amyloidosis diseases, inflammation, metabolic disorders, cardio-vascular disorders, osteoporosis, nervous system trauma, ischemia. 

Therapeutic uses of benzylideneguanidine derivatives for the treatment of proteopathies

The present invention relates to a composition for use in treating a glioma or ameliorating the effects of a glioma, particularly glioblastoma, wherein said composition comprises a first active agent selected from the group consisting of a compound of formula (I), or a pharmaceutically acceptable salt thereof, (I) and a second active agent, which is temozolomide, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier. 

Method of treating cancer with a combination of benzylideneguanidine derivatives and chemotherapeutic agent

The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof Formula (I), and its uses to treat a disorder associated with protein misfolding stress and in particular with an accumulation of misfolded proteins. 

O-alkyl-benzylideneguanidine derivatives and therapeutic use for the treatment of disorders associated an accumulation of misfolded proteins

The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein Ris alkyl, Cl, F or Br, Ris H or F; Ris selected from H and alkyl; Ris selected from H and C(O)R; Ris H or Rand Rare linked to form a heterocyclic group which is optionally substituted with one or more Rgroups Ris selected from R, ORand NRR; RRand Rare each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocycyl and aryl, each of which is optionally substituted with one or more Rgroups; each Ris independently selected from halogen, OH, CN NO, COO-alkyl, aralkyl, SO-alkyl, SO-aryl, COOH, CO-alkyl, CO-aryl, NH, NH-alkyl, N(alkyl), CF, alkyl and alkoxy, X and Z are each independently CRand Y is selected from CRand N and Ris H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins. 

The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein: Ris alkyl, Cl, F or Br; Ris H or F; Ris selected from H and alkyl; Ris selected from H and C(O)R; Ris H; or Rand Rare linked to form a heterocyclic group which is optionally substituted with one or more Rgroups; Ris selected from R, ORand NRR; R, Rand Rare each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocyclyl and aryl, each of which is optionally substituted with one or more Rgroups; each Ris independently selected from halogen, OH, CN, NO, COO-alkyl, aralkyl, SO-alkyl, SO-aryl, COOH, CO-alkyl, CO-aryl, NH, NH-alkyl, N(alkyl), CF, alkyl and alkoxy; X and Z are each independently CR, and Y is selected from CRand N; and Ris H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins. 

The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use.

Cysteine protease inhibitors and their therapeutic applications

The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use wherein R3, R4, R5, R6, Y, Het1, T, U, V, W, X, Ru, Rv and Rw are as defined in claim

Tetracyclic inhibitors of cysteine proteases, the pharmaceutical compositions thereof and their therapeutic applications

The present invention relates to thiazolylimidazole derivatives of the general formula (I) in which: G represents a bond or a divalent radical chosen from the groups g1, g2 and g3; and R, R, R, R, R, R, Y and Z are as defined in the description. Application of the compounds of the formula (I) to the treatment of hypertriglyceridaemia, hypercholesterolaemia and dyslipidaemia. 

Thiazolylimidazole derivatives and their use as inhibitors of microsomal triglyceride transfer protein

The present invention relates to derivatives of aroyl-O-piperidine structure of the general formula (I): in which R, R, Rand Rare as defined in the description. Application of the compounds of the formula (I) to the treatment of hyper-triglyceridaemia, hypercholesterolaemia and dyslipidaemia, and to the prevention or treatment of obesity. 

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Montenois, France

Philippe Guedat