Abstract: 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.
Abstract: The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein: R1 is alkyl, Cl, F or Br; R2 is H or F; R3 is selected from H and alkyl; R4 is selected from H and C(O)R6; R5 is H; or R4 and R5 are linked to form a heterocyclic group which is optionally substituted with one or more R10 groups; R6 is selected from R7, OR7 and NR8R9; R7, R8 and R9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocyclyl and aryl, each of which is optionally substituted with one or more R10 groups; each R10 is independently selected from halogen, OH, CN, NO2, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy; X and Z are each independently CR11, and Y is selected from CR11 and N; and R11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.
Type:
Grant
Filed:
November 25, 2019
Date of Patent:
March 23, 2021
Assignees:
United Kingdom Research and Innovation, Inflectis Bioscience
Abstract: 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.
Abstract: 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.
Abstract: 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.
Abstract: The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein R1 is alkyl, Cl, F or Br, R2 is H or F; R3 is selected from H and alkyl; R4 is selected from H and C(O)R6; R5 is H or R4 and R5 are linked to form a heterocyclic group which is optionally substituted with one or more R10 groups R6 is selected from R7, OR7 and NR8R6; R7R8 and R9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocycyl and aryl, each of which is optionally substituted with one or more R10 groups; each R10 is independently selected from halogen, OH, CN NO1, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy, X and Z are each independently CR11 and Y is selected from CR11 and N and R11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.
Type:
Grant
Filed:
August 31, 2018
Date of Patent:
January 7, 2020
Assignees:
InFlectis BioScience, United Kingdom Research and Innovation
Abstract: The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein: R1 is alkyl, Cl, F or Br; R2 is H or F; R3 is selected from H and alkyl; R4 is selected from H and C(O)R6; R5 is H; or R4 and R5 are linked to form a heterocyclic group which is optionally substituted with one or more R10 groups; R6 is selected from R7, OR7 and NR8R9; R7, R8 and R9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocyclyl and aryl, each of which is optionally substituted with one or more R10 groups; each R10 is independently selected from halogen, OH, CN, NO2, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy; X and Z are each independently CR11, and Y is selected from CR11 and N; and R11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.
Type:
Grant
Filed:
March 23, 2017
Date of Patent:
October 16, 2018
Assignees:
United Kingdom Research and Innovation, InFlectis BioScience
Abstract: The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein: R1 is alkyl, Cl, F or Br; R2 is H or F; R3 is selected from H and alkyl; R4 is selected from H and C(O)R6; R5 is H; or R4 and R5 are linked to form a heterocyclic group which is optionally substituted with one or more R10 groups; R6 is selected from R7, OR7 and NR8R9; R7, R8 and R9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocyclyl and aryl, each of which is optionally substituted with one or more R10 groups; each R10 is independently selected from halogen, OH, CN, NO2, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy; X and Z are each independently CR11, and Y is selected from CR11 and N; and R11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.
Type:
Grant
Filed:
January 10, 2014
Date of Patent:
June 20, 2017
Assignees:
MEDICAL RESEARCH COUNCIL, INFLECTIS BIOSCIENCE