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1. WO2012082997 - TRICYCLIC PI3K INHIBITOR COMPOUNDS AND METHODS OF USE

Publication Number WO/2012/082997
Publication Date 21.06.2012
International Application No. PCT/US2011/065101
International Filing Date 15.12.2011
Chapter 2 Demand Filed 11.10.2012
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
12
in which the condensed system contains three hetero rings
14
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
12
in which the condensed system contains three hetero rings
14
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
12
in which the condensed system contains three hetero rings
14
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
498
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12
in which the condensed system contains three hetero rings
14
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 487/14 (2006.01)
C07D 491/14 (2006.01)
C07D 495/14 (2006.01)
C07D 498/14 (2006.01)
A61K 31/519 (2006.01)
A61P 35/00 (2006.01)
CPC
A61K 2039/505
A61K 31/5377
A61K 31/5383
A61K 31/5386
A61K 39/3955
C07D 471/14
Applicants
  • F. HOFFMANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124 CH-4070 Basel, CH (AllExceptUS)
  • DOTSON, Jennafer [US/US]; US (UsOnly)
  • HEALD, Robert Andrew [GB/GB]; GB (UsOnly)
  • HEFFRON, Timothy [US/US]; US (UsOnly)
  • JONES, Graham Elgin [GB/GB]; GB (UsOnly)
  • KRINTEL, Sussie Lerche [DK/GB]; GB (UsOnly)
  • MCLEAN, Neville James [GB/GB]; GB (UsOnly)
  • NDUBAKU, Chudi [US/US]; US (UsOnly)
  • OLIVERO, Alan G. [US/US]; US (UsOnly)
  • SALPHATI, Laurent [FR/US]; US (UsOnly)
  • WANG, Lan [CA/US]; US (UsOnly)
  • WEI, BinQing [CN/US]; US (UsOnly)
Inventors
  • DOTSON, Jennafer; US
  • HEALD, Robert Andrew; GB
  • HEFFRON, Timothy; US
  • JONES, Graham Elgin; GB
  • KRINTEL, Sussie Lerche; GB
  • MCLEAN, Neville James; GB
  • NDUBAKU, Chudi; US
  • OLIVERO, Alan G.; US
  • SALPHATI, Laurent; US
  • WANG, Lan; US
  • WEI, BinQing; US
Agents
  • HARRIS, Robert, J.; Viksnins Harris & Padys PLLP 7900 International Drive Suite 670 Bloomington, MN 55425, US
Priority Data
61/423,69416.12.2010US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) TRICYCLIC PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
(FR) COMPOSÉS TRICYCLIQUES INHIBITEURS DE PI3K ET PROCÉDÉS D'UTILISATION
Abstract
(EN)
Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti- inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.
(FR)
L'invention concerne des composés tricycliques inhibiteurs de PI3K de Formule I ayant une activité anticancéreuse, une activité anti- inflammatoire, ou des propriétés immunorégulatrices et plus spécifiquement ayant une activité modulant ou inhibant la PI3 kinase. L'invention concerne des procédés pour l'utilisation des composés tricycliques inhibiteurs de PI3K de Formule I pour le diagnostic ou le traitement in vitro, in situ, et in vivo de cellules mammaliennes, d'organismes, ou de conditions pathologiques associées. Les composés de Formule I incluent les stéréoisomères, les isomères géométriques, les tautomères, et les sels pharmaceutiquement acceptables de ceux-ci. Les lignes en pointillés indiquent une double liaison facultative, et au moins une ligne en pointillés est une double liaison. Les substituants sont tels que décrits.
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