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1. WO2011036280 - BENZOXAZEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE

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Publication Number WO/2011/036280
Publication Date 31.03.2011
International Application No. PCT/EP2010/064208
International Filing Date 27.09.2010
Chapter 2 Demand Filed 03.06.2011
IPC
C07D 498/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 498/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
C07D 519/00 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
519Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/ or C07D455/257
A61K 31/4162 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
4151,2-Diazoles
4162condensed with heterocyclic ring systems
A61K 31/4188 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
41641,3-Diazoles
4188condensed with heterocyclic ring systems, e.g. biotin, sorbinil
A61K 31/4196 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
41961,2,4-Triazoles
CPC
A61K 31/4162
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
4151,2-Diazoles
4162condensed with heterocyclic ring systems
A61K 31/4188
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
41641,3-Diazoles
4188condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
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 31/553
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
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
553having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 1/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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)
  • HEALD, Robert [GB]/[GB] (UsOnly)
  • HEFFRON, Timothy [US]/[US] (UsOnly)
  • JONES, Mark [GB]/[GB] (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)
  • WANG, Lan [CA]/[US] (UsOnly)
Inventors
  • BLAQUIERE, Nicole
  • DO, Steven
  • DUDLEY, Danette
  • FOLKES, Adrian J.
  • HEALD, Robert
  • HEFFRON, Timothy
  • JONES, Mark
  • KOLESNIKOV, Aleksandr
  • NDUBAKU, Chudi
  • OLIVERO, Alan G.
  • PRICE, Stephen
  • STABEN, Steven
  • WANG, Lan
Agents
  • SAUER, Frank
Priority Data
61/246,38128.09.2009US
61/330,68503.05.2010US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) BENZOXAZEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
(FR) COMPOSÉS DE BENZOXAZÉPINE INHIBITEURS DE PI3K ET LEURS PROCÉDÉS D'UTILISATION
front page image
Abstract
(EN) The invention relates to benzoxazepin compounds of Formula (I) including stereoisomers, geometric isomers, tautomers, or 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 B is a pyrazolyl, imidazolyl, or triazolyl ring which compounds have anti-cancer activity, and more specifically, inhibit PI3 kinase activity.
(FR) L'invention porte sur des composés de benzoxazépine de formule (I) y compris les stéréoisomères, isomères géométriques, tautomères ou 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 B représente un noyau pyrazolyle, imidazolyle ou triazolyle, lesquels composés ont une activité anticancéreuse et, plus spécifiquement, inhibent l'activité de la PI3-kinase.
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