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1. WO2011036284 - BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE

Publication Number WO/2011/036284
Publication Date 31.03.2011
International Application No. PCT/EP2010/064222
International Filing Date 27.09.2010
Chapter 2 Demand Filed 03.06.2011
IPC
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
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
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
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
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
38
having sulfur as a ring hetero atom
381
having five-membered 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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425
Thiazoles
429
condensed with heterocyclic ring systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
C07D 495/04 (2006.01)
C07D 495/14 (2006.01)
C07D 513/04 (2006.01)
C07D 513/14 (2006.01)
A61K 31/381 (2006.01)
A61K 31/429 (2006.01)
CPC
A61K 31/381
A61K 31/41
A61K 31/4196
A61K 31/4245
A61K 31/429
A61K 31/4365
Applicants
  • F. HOFFMANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124 CH-4070 Basel, CH (AllExceptUS)
  • BLAQUIERE, Nicole [CA/US]; US (UsOnly)
  • DO, Steven [US/US]; US (UsOnly)
  • DUDLEY, Danette [US/US]; US (UsOnly)
  • FOLKES, Adrian, J. [GB/GB]; GB (UsOnly)
  • GOLDSMITH, Richard, A. [US/US]; US (UsOnly)
  • HEALD, Robert [GB/GB]; GB (UsOnly)
  • HEFFRON, Tim [US/US]; US (UsOnly)
  • KOLESNIKOV, Aleksandr [US/US]; US (UsOnly)
  • NDUBAKU, Chudi [US/US]; US (UsOnly)
  • OLIVERO, Alan, G. [US/US]; US (UsOnly)
  • PRICE, Stephen [GB/GB]; GB (UsOnly)
  • STABEN, Steven [US/US]; US (UsOnly)
  • WEI, BinQing [CN/US]; US (UsOnly)
Inventors
  • BLAQUIERE, Nicole; US
  • DO, Steven; US
  • DUDLEY, Danette; US
  • FOLKES, Adrian, J.; GB
  • GOLDSMITH, Richard, A.; US
  • HEALD, Robert; GB
  • HEFFRON, Tim; US
  • KOLESNIKOV, Aleksandr; US
  • NDUBAKU, Chudi; US
  • OLIVERO, Alan, G.; US
  • PRICE, Stephen; GB
  • STABEN, Steven; US
  • WEI, BinQing; US
Agents
  • SAUER, Frank; Grenzacherstrasse 124 CH-4070 Basel, CH
Priority Data
61/246,38628.09.2009US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
(FR) COMPOSÉS DE BENZOXÉPINE INHIBITEURS DE PI3K ET LEURS PROCÉDÉS D'UTILISATION
Abstract
(EN)
Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. 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 porte sur des composés de benzoxépine de formule I, y compris les stéréoisomères, isomères géométriques, tautomères, solvates, métabolites et sels pharmaceutiquement acceptables de ceux-ci, dans laquelle formule : Z1 représente CR1 ou N; Z2 représente CR2 ou N; Z3 représente CR3 ou N; Z4 représente CR4 ou N; et dans laquelle (i) X1 représente N et X2 représente S, (ii) X1 représente S et X2 représente N, (iii) X1 représente CR7 et X2 représente S, (iv) X1 représente S et X2 représente CR7; (v) X1 représente NR8 et X2 représente N, (vi) X1 représente N et X2 représente NR8, (vii) X1 représente CR7 et X2 représente O, (viii) X1 représente O et X2 représente CR7, (ix) X1 représente CR7 et X2 représente C(R7)2, (x) X1 représente C(R7)2 et X2 représente CR7; (xi) X1 représente N et X2 représente O ou (xii) X1 représente O et X2 représente N, lesquels sont utiles pour l'inhibition de lipide-kinases, dont la p110-alpha et d'autres isoformes de PI3K, et pour le traitement de troubles tels qu'un cancer à médiation par des lipide-kinases. L'invention porte également sur des procédés d'utilisation de composés de formule I pour le diagnostic in vitro, in situ et in vivo, la prévention ou le traitement de tels troubles dans des cellules de mammifère, ou d'états pathologiques associés.
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