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1. WO2012126901 - BENZOXAZEPIN COMPOUNDS SELECTIVE FOR PI3K P110 DELTA AND METHODS OF USE

Publication Number WO/2012/126901
Publication Date 27.09.2012
International Application No. PCT/EP2012/054849
International Filing Date 20.03.2012
IPC
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
02
in which the condensed system contains two hetero rings
04
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
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
519
Heterocyclic 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
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
55
having seven-membered rings, e.g. azelastine, pentylenetetrazole
553
having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37
Drugs for immunological or allergic disorders
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19
Drugs for skeletal disorders
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12
Antivirals
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5
Drugs for disorders of the endocrine system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
C07D 498/04 (2006.01)
C07D 498/14 (2006.01)
C07D 519/00 (2006.01)
A61K 31/553 (2006.01)
A61P 35/00 (2006.01)
A61P 37/00 (2006.01)
CPC
C07D 498/04
C07D 498/14
C07D 519/00
Applicants
  • F. HOFFMANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124 CH-4070 Basel, CH (AllExceptUS)
  • ELLIOTT, Richard [GB/GB]; GB (UsOnly)
  • GANCIA, Emanuela [GB/GB]; GB (UsOnly)
  • HEALD, Robert [GB/GB]; GB (UsOnly)
  • HEFFRON, Timothy [US/US]; US (UsOnly)
  • SAFINA, Brian [US/US]; US (UsOnly)
  • SEWARD, Eileen, M. [IE/GB]; GB (UsOnly)
  • STABEN, Steven [US/US]; US (UsOnly)
  • SUTHERLIN, Daniel, P. [US/US]; US (UsOnly)
  • WASZKOWYCZ, Bohdan [GB/GB]; GB (UsOnly)
  • WEI, BinQing [CN/US]; US (UsOnly)
Inventors
  • ELLIOTT, Richard; GB
  • GANCIA, Emanuela; GB
  • HEALD, Robert; GB
  • HEFFRON, Timothy; US
  • SAFINA, Brian; US
  • SEWARD, Eileen, M.; GB
  • STABEN, Steven; US
  • SUTHERLIN, Daniel, P.; US
  • WASZKOWYCZ, Bohdan; GB
  • WEI, BinQing; US
Agents
  • SAUER, Frank; Grenzacherstrasse 124 CH-4070 Basel, CH
Priority Data
61/454,67221.03.2011US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) BENZOXAZEPIN COMPOUNDS SELECTIVE FOR PI3K P110 DELTA AND METHODS OF USE
(FR) COMPOSÉS DE BENZOXAZÉPINE SÉLECTIFS POUR PI3K P110 DELTA ET LEURS MÉTHODES D'UTILISATION
Abstract
(EN)
Benzoxazepin Formula (I) compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, 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)
La présente invention concerne des composés de benzoxazépine de formule (I), y compris leurs stéréo-isomères, leurs isomères géométriques, leurs tautomères, leurs métabolites et des sels pharmaceutiquement acceptables de ceux-ci, qui peuvent être utilisés en vue de l'inhibition de l'isoforme delta de PI3K et du traitement d'affections à médiation par les lipides-kinases comme l'inflammation, les affections immunologiques et le cancer. L'invention concerne des méthodes d'utilisation des composés de formule (I) en vue du diagnostic in vitro, in situ et in vivo, de la prévention ou du traitement, dans des cellules de mammifère, desdites affections ou de pathologies associées.
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