Processing

Please wait...

Settings

Settings

Goto Application

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
C07D 487/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 495/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
495Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 513/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
513Heterocyclic 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
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/519 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61K 31/52 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
52Purines, e.g. adenine
A61P 37/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
CPC
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
A61P 3/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
A61P 31/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 37/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
Applicants
  • F. HOFFMANN-LA ROCHE AG [CH]/[CH] (AllExceptUS)
  • CASTANEDO, Georgette [US]/[US] (UsOnly)
  • GOLDSTEIN, David, Michael [US]/[US] (UsOnly)
  • KONDRU, Rama, K. [IN]/[US] (UsOnly)
  • LUCAS, Matthew, C. [GB]/[US] (UsOnly)
  • PALMER, Wylie, Solang [US]/[US] (UsOnly)
  • PRICE, Stephen [GB]/[GB] (UsOnly)
  • SAFINA, Brian [US]/[US] (UsOnly)
  • SAVY, Pascal, Pierre, Alexandre [FR]/[GB] (UsOnly)
  • SEWARD, Eileen, Mary [IE]/[GB] (UsOnly)
  • SUTHERLIN, Daniel, P. [US]/[US] (UsOnly)
  • SWEENEY, Zachary, Kevin [US]/[US] (UsOnly)
Inventors
  • CASTANEDO, Georgette
  • GOLDSTEIN, David, Michael
  • KONDRU, Rama, K.
  • LUCAS, Matthew, C.
  • PALMER, Wylie, Solang
  • PRICE, Stephen
  • SAFINA, Brian
  • SAVY, Pascal, Pierre, Alexandre
  • SEWARD, Eileen, Mary
  • SUTHERLIN, Daniel, P.
  • SWEENEY, Zachary, Kevin
Agents
  • HEIROTH, Ulrike
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.
Related patent documents
Latest bibliographic data on file with the International Bureau