Patent number: 9611223
Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2/-/-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.
Type:
Grant
Filed:
September 11, 2014
Date of Patent:
April 4, 2017
Assignee:
INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)
Inventors:
Alan Ashworth, Christopher James Lord, Richard James Rowland Elliott, Dan Niculescu-Duvaz, Roderick Alan Porter, Rehan Aqil, Raymond John Boffey, Melanie Jayne Bayford, Stuart Firth-Clark, Anna Hopkins, Ashley Nicholas Jarvis, Trevor Robert Perrior, Philip Alan Skone, Rebekah Elisabeth Key
Publication number: 20160221953
Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2/-/-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.
Type:
Application
Filed:
September 11, 2014
Publication date:
August 4, 2016
Applicant:
Institute of Cancer Research Royal Cancer Hospital (THE)
Inventors:
Alan ASHWORTH, Christopher James LORD, Richard James Rowland ELLIOT, Dan NICULESCU-DUVAZ, Roderick Alan PORTER, Rehan AQIL, Raymond John BOFFEY, Melanie Jayne BAYFORD, Stuart FIRTH-CLARK, Anna HOPKINS, Ashley Nicholas JARVIS, Trevor Robert PERRIOR, Philip Alan SKONE, Rebekah Elisabeth KEY
Publication number: 20110166136
Abstract: Compounds of formula (1), salts and pro-drugs wherein: R1, R2, R3 and R4 are hydrogen, alkyl, hydroxyalkyl, halogen, haloalkyl, alkoxy, haloalkoxy, alkoxycarbonyl, carboxyl, hydroxyl, nitro, amino, monalkylamino, dialkylamino, acylamino, alkoxycarbonylamino, alkylsulphonyl, arylsulphonyl, alkylsulphonylamino, arylsulphonylamino, aminosulphonyl or cyano, or any two of R1 to R4 that are adjacent on the ring may together represent the moiety āOā(CH2)nāOā wherein n is 1 to 3; R5 is hydrogen or alkyl; R6 is hydrogen or alkyl; and X is selected from the group consisting of: (a) groups of formula OR7 wherein R7 is hydrogen or alkyl which is optionally substituted with a substituent selected from alkylsulfonylalkyl, saturated or partially unsaturated heterocyclic, alkoxy, carboxyl, nitro, amino, monalkylamino, dialkylamino, halogen, and alkoxycarbonyl, provided that when R7 is hydrogen or ethyl, then R1, R2, R3 and R4 cannot be selected from hydrogen, halogen and alkyl; and (b) groups of formula NR8R9 wherein R8
Type:
Application
Filed:
July 3, 2009
Publication date:
July 7, 2011
Applicant:
LECTUS THERAPEUTICS LIMITED
Inventors:
Nawaz Mohammed Khan, Svenja Burckhardt, Julie Elaine Cansfield, Ngoc-Tri Vo, Richard Edward Armer, Raymond John Boffey