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1. WO2016097072 - TETRAHYDRO-PYRIDO[3,4-b]INDOLE ESTROGEN RECEPTOR MODULATORS AND USES THEREOF

Publication Number WO/2016/097072
Publication Date 23.06.2016
International Application No. PCT/EP2015/080119
International Filing Date 17.12.2015
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
4353
ortho- or peri-condensed with heterocyclic ring systems
437
the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
C07D 471/04 (2006.01)
A61K 31/437 (2006.01)
A61P 35/00 (2006.01)
CPC
A61K 31/138
A61K 31/437
A61K 31/4545
A61K 31/497
A61K 31/506
A61K 31/565
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
  • GOODACRE, Simon Charles; GB
  • LABADIE, Sharada; US
  • LIANG, Jun; US
  • ORTWINE, Daniel Fred; US
  • RAY, Nicholas Charles; GB
  • WANG, Xiaojing; US
  • ZBIEG, Jason; US
  • ZHANG, Birong; US
Agents
  • HAEFELE RACIN, Thomas; CH
Priority Data
62/093,92918.12.2014US
62/110,99802.02.2015US
62/142,07702.04.2015US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) TETRAHYDRO-PYRIDO[3,4-b]INDOLE ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
(FR) MODULATEURS DES RÉCEPTEURS DES OESTROGÈNES TÉTRAHYDRO-PYRIDO[3,4-B]INDOLE ET UTILISATIONS ASSOCIÉES
Abstract
(EN)
Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula (I) structure and 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 estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
(FR)
L'invention concerne des composés de tétrahydro-pyrido[3,4-b]indol-1-yl dotés d'une activité ou d'une fonction de modulation des récepteurs des œstrogènes, ces composés présentant une structure de Formule (I), ainsi que des stéréoisomères, des tautomères ou des sels pharmaceutiquement acceptables de ceux-ci, et leurs substituants et caractéristiques structurelles. La présente invention concerne également des compositions pharmaceutiques et des médicaments contenant lesdits composés de Formule (I), ainsi que des méthodes d'utilisation desdits modulateurs des récepteurs des œstrogènes, seuls ou en association avec d'autres agents thérapeutiques, dans le traitement de maladies ou d'affections induites par les récepteurs des oestrogènes ou qui en dépendent.
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