Publication number: 20240150293
Abstract: Compounds of Formula (I): wherein R1, R3, R11, R12, X, Y1, Y2, Y3, Y4 and are as defined in the description. Medicinal products containing the same which are useful in treating conditions requiring anti-apoptotic inhibitors.
Type:
Application
Filed:
January 11, 2022
Publication date:
May 9, 2024
Inventors:
Stephen STOKES, Simon BEDFORD, l-Jen CHEN, James Edward Paul DAVIDSON, Nicholas DAVIES, Christopher John GRAHAM, Sean Martin MCKENNA, Johannes W.G. MEISSNER, James Brooke MURRAY, Rachel Jane PARSONS, Stuart RAY, Emma SANDERS, Claire Louise WALMSLEY, Paul Andrew BROUGH, András KOTSCHY, Ágnes PROSZENYÁK, Ádám SINAI, Balázs Károly BÁLINT, Márton CSÉKEI, Márton ZWILLINGER, Rita GARAMVÖLGYI, Szabolcs SIPOS, Vilibald KUN, Zoltán SZABÓ, Maïa CHANRION, Francesca ROCCHETTI, Frédéric COLLAND, Ana Leticia MARAGNO, Laura BRESSON
Publication number: 20090181989
Abstract: Compounds of formula (I) are inhibitors of HSP90, and of utility in the treatment of, for example, cancers: wherein ring A is an aryl or heteroaryl ring or ring system; R1 is hydrogen, fluoro, chloro, bromo, or a radical of formula (IA): —X-Alk1-(Z)m-(Alk2)n-Q (IA) wherein X is a bond, —O—, —S— —S(O)—, —SO2—, or —NH—, Z is —O—, —S—, —(C?O)—, —(C?S)—, —S(O)—, —SO2—, —NRA, or, in either orientation —C(?O)O—, —C(?O)NRA, —C(?S)NRA—, —SO2NRA—, —NRAC(?O)—, or —NRASO2— wherein RA is hydrogen or C1-C6 alkyl in which one or more hydrogens is optionally substituted by fluorine; Alk1 and Alk2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m and n are independently 0 or 1, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is cyano (—CN), fluoro, chloro, bromo, methyl, ethyl, —OH, —CH2OH, —C(?O)NH2, —C(?O)H, —C(?O)CH3, or —NH2; R3 and R4 are independently selected from hydrogen, fluoro, chloro, bromo, cyano (—CN), C1-C3alkyl optionally substituted
Type:
Application
Filed:
February 27, 2009
Publication date:
July 16, 2009
Applicants:
VERNALIS ( R & D) LTD., CANCER RESEARCH TECHNOLOGY LTD, THE INSTITUTE OF CANCER
Inventors:
Paul Andrew BROUGH, Martin DRYSDALE, Xavier BARRIL-ALONSO
Publication number: 20090163490
Abstract: Compounds of formula (I) have HSP90 inhibitory activity and are therefore useful in the treatment of, inter alia, cancer: Formula (I) wherein Ri is hydrogen, fluoro, chloro, bromo, or a radical of formula -X-Alk1-(Z)m-(Alk2)n-Q wherein X is —O—, —S— —S(O)—, SO2—, or —NH—, Z is —O—, —S—, —(C?O)—, —(C?S)—, —S(O)—, —SO2—, —NRA—, or, in either orientation —C(?O)O—, —C(?O)NRA—, —C(?S)NRA—, —SO2NRA—, —NRAC(?O)—, or —NRASO2— wherein RA is hydrogen or C1-C6 alkyl AIk1 and AIk2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, n and p are independently 0 or 1, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is a radical of formula —(Ar1)p-(Alk1)q-(Z)r-(Alk2)s-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1, Alk2, Z, and Q are as defined above, and p, q, r and s are independently 0 or 1; and R3 is cyano (—CN), fluoro, chloro, bromo, methyl in which in which one or more hydrogen atoms are optionally replaced by fluorine
Type:
Application
Filed:
March 9, 2007
Publication date:
June 25, 2009
Applicant:
VERNALIS (R&D) LTD.
Inventors:
Paul Andrew Brough, Martin James Drysdale, Nicholas Gareth Davies, Nicolas Noel Foloppe, Stephen Stokes
Publication number: 20090069336
Abstract: Compounds of formula (I) are inhibitors of HSP90, and useful in the treatment of, for example, cancers: wherein R2 is a group of formula (IA): -(Ar1)m-(Alk1)p-(Z)r-(Alk2)s-Q??(IA) wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C?O)—, —(C?S)—, —SO2—, —C(?O)O—, —C(?O)NRA—, —C(?S)NRA—, —SO2NRA—, —NRAC(?O)—, —NRASO2— or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is (i) hydrogen, a —CN group, a nitro group —NO2, or a —C(?NOH)(NH2) group, or (ii) an optionally substituted C1-C6alkyl, aryl, heterocyclic, aryl(C1-C6alkyl)-, or heterocyclic(C1-C6alkyl)- group, or (iii) a group of formula —C(?O)R5 wherein R5 is
Type:
Application
Filed:
July 18, 2005
Publication date:
March 12, 2009
Applicants:
VERNALIS (CAMBRIDGE) LIMITED., CANCER RESEARCH TECHNOLOGY LTD., THE INSTITUTE OF CANCER RESEARCH
Inventors:
Xavier Barril-Alonso, Paul Andrew Brough, Martin James Drysdale, Paul Webb
Publication number: 20090054421
Abstract: Compounds of formula (I) are HSP90 inhibitors, of utility in the treatment of, for example, cancers: wherein R1 is -(Alk1)p-(Z)r(Alk2)-Q wherein AIk1 and AIk2 are optionally substituted divalent C1C3 alkylene or C2-C3 alkenylene radicals, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C?O)—, —(C?S)—, —SO2—, —C(?O)O—, —C(?O)NRA, —C(?S)NRA-, —SO2NRA—NRAC(?O)—, —NRASO2— or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is optionally substituted aryl or heteroaryl; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C-6)alkyl, aryl or heteroaryl radical; and R4 is (i) a carboxylic ester, carboxamide or sulfonamide group, or (ii) a —CN group, or (iii) an optionally substituted C1-C6alkyl, aryl, heteroaryl, aryl(C1-C6alkyl)-, or heteroaryl(C1-C6alkyl)- group, or (iv) a group of formula —C(?O)R5 wherein R5 is hydroxyl, optionally substituted C1-C6alkyl, C1-C6alkyoxy, aryl, aryloxy, heteroaryl, heteroaryl
Type:
Application
Filed:
January 23, 2006
Publication date:
February 26, 2009
Applicants:
Vernalis R & D Limited, Cancer Research Technology LTD, THE INSTITUTE OF CANCER RESEARCH
Inventors:
Thomas Peter Matthews, Kwai Ming Cheung, Ian Collins, Edward McDonald, Paul Andrew Brough, Martin James Drysdale