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1. WO2016097071 - ESTROGEN RECEPTOR MODULATORS AND USES THEREOF

Publication Number WO/2016/097071
Publication Date 23.06.2016
International Application No. PCT/EP2015/080118
International Filing Date 17.12.2015
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14
containing three or more hetero rings
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
397
having four-membered rings, e.g. azetidine
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
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
4025
not condensed and containing further heterocyclic rings, e.g. cromakalim
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
205
Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
02
not condensed with other rings
04
having no double bonds between ring members or between ring members and non-ring members
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04
having no double bonds between ring members or between ring members and non-ring members
08
with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
493
Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
411
Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
C07D 401/14 (2006.01)
A61K 31/397 (2006.01)
A61K 31/4025 (2006.01)
C07D 403/02 (2006.01)
C07D 403/14 (2006.01)
C07D 409/02 (2006.01)
CPC
A61K 31/381
A61K 31/397
A61K 31/40
A61K 31/4025
A61K 31/404
A61K 31/416
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
  • SMITH, Nicholas D.; US
  • LIANG, Jun; US
  • ORTWINE, Daniel Fred; US
  • WANG, Xiaojing; US
  • KAHRAMAN, Mehmet; US
  • NAGASAWA, Johnny Y.; US
  • GOODACRE, Simon Charles; GB
  • RAY, Nicholas Charles; GB
  • GOVEK, Steven P.; US
Agents
  • HAEFELE RACIN, Thomas; CH
Priority Data
62/093,92918.12.2014US
62/110,99802.02.2015US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
(FR) MODULATEURS DU RÉCEPTEUR DES ŒSTROGÈNES ET LEURS UTILISATIONS
Abstract
(EN)
Described herein are compounds that are estrogen receptor modulators of Formula (I) and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein SERMF is a selective estrogen receptor modulator fragment and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
(FR)
L'invention concerne des composés qui sont des modulateurs du récepteur des œstrogènes de formule (I) ainsi que des stéréo-isomères, des tautomères, ou des sels pharmaceutiquement acceptables de ceux-ci, SERMF désignant un fragment de modulateur sélectif des récepteurs des œstrogènes et présentant les substituants et les caractéristiques suivants : L'invention concerne également des compositions pharmaceutiques et des médicaments contenant lesdits composés, ainsi que des méthodes d'utilisation desdits modulateurs du récepteur des œstrogènes, seuls ou en association avec d'autres composés, pour traiter des maladies ou des troubles qui sont médiés par des récepteurs des œstrogènes ou qui en dépendent.
Also published as
Latest bibliographic data on file with the International Bureau