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1. WO2017216279 - HETEROARYL ESTROGEN RECEPTOR MODULATORS AND USES THEREOF

Publication Number WO/2017/216279
Publication Date 21.12.2017
International Application No. PCT/EP2017/064650
International Filing Date 15.06.2017
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
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
12
in which the condensed system contains three hetero rings
14
Ortho-condensed systems
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
12
in which the condensed system contains three hetero rings
20
Spiro-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
495
Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur 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
70
Carbohydrates; Sugars; Derivatives thereof
7042
Compounds having saccharide radicals and heterocyclic rings
7052
having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
7056
containing five-membered rings with nitrogen as a ring hetero atom
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)
C07D 471/14 (2006.01)
C07D 471/20 (2006.01)
C07D 487/04 (2006.01)
C07D 491/04 (2006.01)
C07D 495/04 (2006.01)
CPC
C07D 471/04
C07D 471/14
C07D 471/20
C07D 487/04
C07D 491/04
C07D 495/04
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, DJ, 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, KH, KM, KN, KP, KR, KW, 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
  • LI, Jun; US
  • LIANG, Jun; US
  • LIAO, Jiangpeng; CN
  • ORTWINE, Daniel Fred; US
  • RAY, Nicholas Charles; GB
  • WANG, Xiaojing; US
  • ZBIEG, Jason; US
  • ZHANG, Birong; US
Agents
  • SALUD, Carlos; CH
Priority Data
62/350,88516.06.2016US
PCT/CN2017/08724106.06.2017CN
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) HETEROARYL ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
(FR) MODULATEURS DES RÉCEPTEURS DES ŒSTROGÈNES HÉTÉROARYLES ET LEURS UTILISATIONS
Abstract
(EN)
Described herein are heteroaryl compounds with estrogen receptor modulation activity or function having the Formula (I), (II), and (III) structures: 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, II, and III 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 hétéroaryles présentant une activité ou une fonction de modulation des récepteurs des œstrogènes, ces composés ayant les structures représentées par les formules (I), (II) et (III), ainsi que des stéréo-isomères, des tautomères ou des sels pharmaceutiquement acceptables de ceux-ci, et leurs substituants et caractéristiques structurales. La présente invention concerne également des compositions pharmaceutiques et des médicaments qui comprennent les composés représentés par les formules (I), (II) et (III), ainsi que des procédés d'utilisation de ces modulateurs des récepteurs des œstrogènes, seuls ou en association avec d'autres agents thérapeutiques, pour le traitement de maladies ou d'affections médiées par les récepteurs des œstrogènes ou qui en dépendent.
Also published as
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