Abstract: Compounds of formula (I): wherein: W is O, N—H, N-alkyl, N-alkenyl, N-alkynyl, N-aryl, N-heteroaryl or S; each X is independently CH or N; R1 is formula (b) or R3 is H, alkyl, NH2, OH, =0 or halogen; each A and B are independently CH or N; D is NHR4; R4 is H, alkyl, —C(O)-alkyl.
Type:
Grant
Filed:
July 23, 2010
Date of Patent:
March 17, 2015
Assignee:
Karus Therapeutics Limited
Inventors:
Stephen Joseph Shuttleworth, Franck Alexandre Silva, Alexander Richard Liam Cecil, Thomas James Hill
Abstract: A compound of the general Structure (VII) or (VIII) including isoteres and pharmaceutically acceptable salts thereof, wherein R1, R2 (where X=—CONR6—), R3 and R7 are the same or different and each represents an amino-acid side chain moiety; R2 (where X=—CHZ—), R4 and R6 are the same or different and each represents hydrogen, C1-C6 alkyl, C2-C6 alkenyl, or C2-C6 alkynyl; K represents a linear or branched chain of carbon atoms and containing 1-10 atoms; L represents a moiety capable of chelating zinc in the active site of a histone deacetylase (HDAC) or of conversion to such a moiety in vivo (by hydrolysis or reduction, for example); M is a linear or branched chain of carbon or other atoms and containing 1-10 atoms, and capable of undergoing in vivo cleavage to give Structure (VII); and Z is a heteroatom bonded to the macrocycle by a single or double bond, and any other group bonded to Z is H or a protecting group.
Type:
Grant
Filed:
November 22, 2007
Date of Patent:
October 21, 2014
Assignee:
Karus Therapeutics Limited
Inventors:
Arasu Ganesan, Graham Keith Packham, Alexander Richard Liam Cecil
Abstract: Compounds of the invention are of the formula wherein: is a double bond and X is C; or is a single bond and X is N, CH or CQR1; and wherein: n is 1 to 10; R is H or QR1; each R? is independently selected from H and QR1; each Q is independently selected from a bond, CO, NH, S, SO, SO2 or O; each R1 is independently selected from C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, substituted or unsubstituted aryl or heteroaryl, acyl, C1-C10 cycloalkyl, halogen, C1-C10 alkylaryl or C1-C10 heterocycloalkyl; L is a nitrogen-containing heteroaryl; and W is a zinc-chelating residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in therapy.
Type:
Application
Filed:
April 30, 2014
Publication date:
August 21, 2014
Applicant:
Karus Therapeutics Limited
Inventors:
Stephen Joseph SHUTTLEWORTH, Cyrille Davy TOMASSI
Abstract: Compounds of the invention are of the formula (I); wherein: is a double bond and X is C; or is a single bond and X is N, CH or CQR1; and wherein: n is 1 to 10; R is H or QR1; each R? is independently selected from H and QR1; each Q is independently selected from a bond, CO, NH, S, SO, SO2 or O; each R1 is independently selected from C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, substituted or unsubstituted aryl or heteroaryl, acyl, C1-C10 cycloalkyl, halogen, C1-C10 alkylaryl or C1-C10 heterocycloalkyl; L is a nitrogen-containing heteroaryl; and W is a zinc-chelating residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in therapy.
Type:
Grant
Filed:
January 26, 2010
Date of Patent:
June 10, 2014
Assignee:
Karus Therapeutics Limited
Inventors:
Stephen Joseph Shuttleworth, Cyrille Davy Tomassi
Abstract: The subject application pertains to a compound of structure IX or X: or a pharmaceutically acceptable salt thereof, wherein: X is —C(?O)N(R10)— or —CH(OPr3) —; R7, R9 and R10 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid; Pr1 and Pr2 are the same or different and represent hydrogen or a thiol protecting group; Pr3 is hydrogen or an alcohol protecting group; R1, R2, R5 and R6 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid, or R1 and R2 and/or R5 and R6, taken together with the carbon atom to which they are attached, form a spirocyclic moiety, with the proviso that: each of R1 and R2 is not hydrogen, or each of R5 and R6 is not hydrogen.
Type:
Grant
Filed:
May 22, 2009
Date of Patent:
December 24, 2013
Assignee:
Karus Therapeutics Limited
Inventors:
Stephen Joseph Shuttleworth, Franck Alexandre Silva, Cyrille Davy Tomassi, Alexander Richard Liam Cecil, Thomas James Hill
Abstract: Compounds of formulae (I) and (II): or a pharmaceutically acceptable salt thereof, wherein: R1 is a nitrogen-containing 5 to 7-membered heteroaryl or heterocycle; R2 and R3 are each independently (LQ)mY, are described. The compounds are PI3K inhibitors and are useful for the treatment of cancer and immune-inflammatory diseases.
Type:
Application
Filed:
April 26, 2011
Publication date:
May 2, 2013
Applicant:
KARUS THERAPEUTICS LIMITED
Inventors:
Stephen Joseph Shuttleworth, Franck Alexandre Silva
Abstract: Compounds of formula (I): wherein: W is O, N—H, N-alkyl, N-alkenyl, N-alkynyl, N-aryl, N-heteroaryl or S; each X is independently CH or N; R1 is formula (b) or R3 is H, alkyl, NH2, OH, =0 or halogen; each A and B are independently CH or N; D is NHR4; R4 is H, alkyl, —C(O)— alkyl.
Type:
Application
Filed:
July 23, 2010
Publication date:
May 24, 2012
Applicant:
Karus Therapeutics Limited
Inventors:
Stephen Joseph Shuttleworth, Franck Alexandre Silva, Alexander Richard Liam Cecil, Thomas James Hill