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1. WO2017042182 - TRICYCLIC PI3K INHIBITOR COMPOUNDS AND METHODS OF USE

Publication Number WO/2017/042182
Publication Date 16.03.2017
International Application No. PCT/EP2016/071015
International Filing Date 07.09.2016
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
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
535
having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5365
ortho- or peri-condensed with heterocyclic ring 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
55
having seven-membered rings, e.g. azelastine, pentylenetetrazole
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
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
C07D 498/04 (2006.01)
A61K 31/5365 (2006.01)
A61K 31/55 (2006.01)
C07D 519/00 (2006.01)
A61P 35/00 (2006.01)
CPC
A61K 31/4188
A61K 31/4196
A61K 31/423
A61K 31/428
A61K 31/4439
A61K 31/498
Applicants
  • F. HOFFMANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124 4070 Basel, CH (AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BE, BF, BG, BH, BJ, BN, BR, BW, BY, BZ, CA, CF, CG, CH, CI, CL, CM, CN, CO, CR, CU, CY, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GT, GW, HN, HR, HU, ID, IE, IL, IN, IR, IS, IT, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MC, MD, ME, MG, MK, ML, MN, MR, MT, MW, MX, MY, MZ, NA, NE, NG, NI, NL, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SI, SK, SL, SM, SN, ST, SV, SY, SZ, TD, TG, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, ZA, ZM, ZW)
  • GENENTECH, INC. [US/US]; 1 DNA Way South San Francisco, California 94080, US (US)
Inventors
  • BRAUN, Marie-Gabrielle; US
  • GARLAND, Keira; US
  • HANAN, Emily; US
  • PURKEY, Hans; US
  • STABEN, Steven T.; US
  • HEALD, Robert Andrew; GB
  • KNIGHT, Jamie; GB
  • MACLEOD, Calum; GB
  • LU, Aijun; CN
  • WU, Guosheng; CN
Agents
  • SAUER, Frank; CH
Priority Data
PCT/CN2015/08912108.09.2015CN
PCT/CN2016/07612611.03.2016CN
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)
Described herein are tricyclic compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.
(FR)
L'invention concerne des composés tricycliques ayant une activité ou une fonction de modulation de la phosphoinositide 3-kinase (PI3K) ayant une structure de Formule (I) : ou les stéréoisomères, tautomères ou sels pharmaceutiquement acceptables de ceux-ci, et avec les substituants et caractéristiques structurales décrits dans la présente description. La présente invention concerne en outre des compositions pharmaceutiques et des médicaments qui comprennent les composés de Formule I, ainsi que des procédés d'utilisation desdits modulateurs de PI3K, seuls ou en association avec d'autres agents thérapeutiques, dans le traitement de maladies ou d'affections qui sont médiées par une dérégulation de PI3K ou qui en dépendent.
Also published as
Latest bibliographic data on file with the International Bureau