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1. WO2008152390 - THIAZOLIOPYRIMIDINES AND THEIR USE AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3 KINASE

Publication Number WO/2008/152390
Publication Date 18.12.2008
International Application No. PCT/GB2008/002014
International Filing Date 12.06.2008
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
513
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/, C07D477/232
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
C07D 513/04 (2006.01)
A61K 31/519 (2006.01)
A61P 35/00 (2006.01)
CPC
C07D 513/04
Applicants
  • F.HOFFMANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124 CH-4070 Basel, CH (AllExceptUS)
  • HANCOX, Timothy, Colin [GB/GB]; GB (UsOnly)
  • PEGG, Neil, Anthony [GB/GB]; GB (UsOnly)
  • BESWICK, Mandy, Christine [GB/GB]; GB (UsOnly)
  • BLENCH, Toby, Jonathan [GB/GB]; GB (UsOnly)
  • DECHAUX, Elsa, Amandine [FR/GB]; GB (UsOnly)
  • KULAGOWSKI, Janusz, Jozef [GB/GB]; GB (UsOnly)
  • NADIN, Alan, John [GB/GB]; GB (UsOnly)
  • PRICE, Stephen [GB/GB]; GB (UsOnly)
Inventors
  • HANCOX, Timothy, Colin; GB
  • PEGG, Neil, Anthony; GB
  • BESWICK, Mandy, Christine; GB
  • BLENCH, Toby, Jonathan; GB
  • DECHAUX, Elsa, Amandine; GB
  • KULAGOWSKI, Janusz, Jozef; GB
  • NADIN, Alan, John; GB
  • PRICE, Stephen; GB
Agents
  • KEEN, Celia, Mary ; J.A. Kemp & Co. 14 South Square Gray's Inn London WC1R 5JJ, GB
Priority Data
0711344.212.06.2007GB
0715677.110.08.2007GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) THIAZOLIOPYRIMIDINES AND THEIR USE AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3 KINASE
(FR) THIAZOLOPYRIMIDINES ET LEUR UTILISATION COMME INHIBITEURS DE LA PHOSPHATIDYLINOSITOL-3 KINASE (PI3K)
Abstract
(EN)
Thiazolopyrimidines of formula (I): wherein W represents a thiazole ring; R1 and R2 form, together with the N atom to which they are attached, a group of the following formula (IIa): in which A is a ring system; m is 0, 1 or 2; R3 is H or C1-C6 alkyl; and R4 is an indole group which is unsubstituted or substituted; and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110δ isoform, which is a class Ia PD kinase, over both other class Ia and class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
(FR)
La présente invention concerne des thiazolopyrimidines de formule (I) : dans laquelle W représente un cycle thiazole; R1 et R2 forment, conjointement avec l'atome d'N auquel ils sont liés, un groupe ayant la formule (Ha) : dans laquelle A représente : un système cyclique; m est égal à 0, 1 ou 2; R3 représente H ou alkyle en C1- C6; et R4 représente un groupe indole substitué ou non; et leurs sels pharmaceutiquement acceptables, qui sont des inhibiteurs de la PI3K et sont sélectifs de l'isoforme p110δ, qui est une PD kinase de classe Ia, par rapport aux deux autres kinases de classe Ia et Ib. Les composés peuvent être utilisés pour traiter des maladies et des troubles résultant d'une croissance, fonction ou comportement cellulaire anormaux associés à la PI3 kinase tels que cancer, troubles immunitaires, maladie cardiovasculaire, infection virale, inflammation, des troubles du métabolisme ou de la fonction endocrine et troubles neurologiques.
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