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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
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 495/14 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
12in which the condensed system contains three hetero rings
14Ortho-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
C07D 513/14 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
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
A61K 31/381 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
38having sulfur as a ring hetero atom
381having five-membered rings
A61K 31/429 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425Thiazoles
429condensed with heterocyclic ring systems
CPC
A61K 31/381
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
38having sulfur as a ring hetero atom
381having five-membered rings
A61K 31/41
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
A61K 31/4196
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41961,2,4-Triazoles
A61K 31/4245
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
4245Oxadiazoles
A61K 31/429
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
425Thiazoles
429condensed with heterocyclic ring systems
A61K 31/4365
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
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
4365the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
Applicants
  • F. HOFFMANN-LA ROCHE AG [CH]/[CH] (AllExceptUS)
  • BLAQUIERE, Nicole [CA]/[US] (UsOnly)
  • DO, Steven [US]/[US] (UsOnly)
  • DUDLEY, Danette [US]/[US] (UsOnly)
  • FOLKES, Adrian, J. [GB]/[GB] (UsOnly)
  • GOLDSMITH, Richard, A. [US]/[US] (UsOnly)
  • HEALD, Robert [GB]/[GB] (UsOnly)
  • HEFFRON, Tim [US]/[US] (UsOnly)
  • KOLESNIKOV, Aleksandr [US]/[US] (UsOnly)
  • NDUBAKU, Chudi [US]/[US] (UsOnly)
  • OLIVERO, Alan, G. [US]/[US] (UsOnly)
  • PRICE, Stephen [GB]/[GB] (UsOnly)
  • STABEN, Steven [US]/[US] (UsOnly)
  • WEI, BinQing [CN]/[US] (UsOnly)
Inventors
  • BLAQUIERE, Nicole
  • DO, Steven
  • DUDLEY, Danette
  • FOLKES, Adrian, J.
  • GOLDSMITH, Richard, A.
  • HEALD, Robert
  • HEFFRON, Tim
  • KOLESNIKOV, Aleksandr
  • NDUBAKU, Chudi
  • OLIVERO, Alan, G.
  • PRICE, Stephen
  • STABEN, Steven
  • WEI, BinQing
Agents
  • SAUER, Frank
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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