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1. WO2010136491 - BICYCLIC INDOLE-PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE

Publication Number WO/2010/136491
Publication Date 02.12.2010
International Application No. PCT/EP2010/057244
International Filing Date 26.05.2010
Chapter 2 Demand Filed 21.12.2010
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
495
Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
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
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
52
Purines, e.g. adenine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37
Drugs for immunological or allergic disorders
C07D 487/04 (2006.01)
C07D 495/04 (2006.01)
C07D 513/04 (2006.01)
A61K 31/519 (2006.01)
A61K 31/52 (2006.01)
A61P 37/00 (2006.01)
CPC
C07D 487/04
C07D 495/04
C07D 513/04
Applicants
  • F. HOFFMANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124 CH-4070 Basel, CH (AllExceptUS)
  • CASTANEDO, Georgette [US/US]; US (UsOnly)
  • GOLDSTEIN, David, Michael [US/US]; US (UsOnly)
  • KONDRU, Rama, K. [IN/US]; US (UsOnly)
  • LUCAS, Matthew, C. [GB/US]; US (UsOnly)
  • PALMER, Wylie, Solang [US/US]; US (UsOnly)
  • PRICE, Stephen [GB/GB]; GB (UsOnly)
  • SAFINA, Brian [US/US]; US (UsOnly)
  • SAVY, Pascal, Pierre, Alexandre [FR/GB]; GB (UsOnly)
  • SEWARD, Eileen, Mary [IE/GB]; GB (UsOnly)
  • SUTHERLIN, Daniel, P. [US/US]; US (UsOnly)
  • SWEENEY, Zachary, Kevin [US/US]; US (UsOnly)
Inventors
  • CASTANEDO, Georgette; US
  • GOLDSTEIN, David, Michael; US
  • KONDRU, Rama, K.; US
  • LUCAS, Matthew, C.; US
  • PALMER, Wylie, Solang; US
  • PRICE, Stephen; GB
  • SAFINA, Brian; US
  • SAVY, Pascal, Pierre, Alexandre; GB
  • SEWARD, Eileen, Mary; GB
  • SUTHERLIN, Daniel, P.; US
  • SWEENEY, Zachary, Kevin; US
Agents
  • HEIROTH, Ulrike; Grenzacherstrasse 124 CH-4070 Basel, CH
Priority Data
61/181,45827.05.2009US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) BICYCLIC INDOLE-PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE
(FR) COMPOSÉS BICYCLIQUES INDOLE-PYRIMIDINE INHIBITEURS DE PI3K SÉLECTIFS POUR P110 DELTA ET LEURS PROCÉDÉS D'UTILISATION
Abstract
(EN)
Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, (iv) X1 is CR7 and X2 is O, or (v) X1 is CR7 and X2 is NR2, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PBK, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
(FR)
L'invention concerne des composés de formule I (Ia et Ib) dans laquelle (i) X1 est N et X2 est S, (ii) X1 est CR7 et X2 est S, (iii) X1 est N et X2 est NR2, (iv) X1 est CR7 et X2 est O, ou (v) X1 est CR7 et X2 est NR2, y compris leurs stéréoisomères, tautomères, métabolites et sels pharmaceutiquement acceptables, qui sont utiles pour inhiber l'isoforme delta de PBK et pour traiter les troubles médiés par les kinases lipidiques, tels que l'inflammation, les troubles immunologiques et le cancer. L'invention concerne également des procédés d'utilisation de composés de formule I pour le diagnostic, la prévention et le traitement in vitro, in situ et in vivo de tels troubles dans des cellules mammaliennes, ou d'états pathologiques associés.
Also published as
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