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CY1125165T1 - Διεργασιες και ενδιαμεσα για την παρασκευη νεων υποκατεστημενων ενωσεων 6,7-διυδρο-5η-βενζο[7] αννουλενιου - Google Patents

Διεργασιες και ενδιαμεσα για την παρασκευη νεων υποκατεστημενων ενωσεων 6,7-διυδρο-5η-βενζο[7] αννουλενιου

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Publication number
CY1125165T1
CY1125165T1 CY20221100140T CY221100140T CY1125165T1 CY 1125165 T1 CY1125165 T1 CY 1125165T1 CY 20221100140 T CY20221100140 T CY 20221100140T CY 221100140 T CY221100140 T CY 221100140T CY 1125165 T1 CY1125165 T1 CY 1125165T1
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CY
Cyprus
Prior art keywords
intermediates
processes
preparation
group
hydrogen atom
Prior art date
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CY20221100140T
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English (en)
Inventor
Monsif Bouaboula
Maurice Brollo
Victor Certal
Youssef El-Ahmad
Bruno Filoche-Romme
Frank Halley
Gary Mccort
Laurent Schio
Michel Tabart
Corinne Terrier
Fabienne Thompson
Original Assignee
Sanofi
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Application filed by Sanofi filed Critical Sanofi
Publication of CY1125165T1 publication Critical patent/CY1125165T1/el

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/12—Oxygen or sulfur atoms
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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    • A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
    • A—HUMAN NECESSITIES
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • C07D209/04—Indoles; Hydrogenated indoles
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyrrole Compounds (AREA)
  • Steroid Compounds (AREA)
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Abstract

Η παρούσα εφεύρεση αφορά σε διεργασίες και ενδιάμεσα για την παρασκευή των ενώσεων του τύπου (Ι): όπου τα R1 και R2 αντιπροσωπεύουν υδρογόνο και άτομα δευτερίου∙ το R3 αντιπροσωπεύει ένα άτομο υδρογόνου ή μια ομάδα -COOH, ή -ΟΗ ή -ΟΡΟ(ΟΗ)2∙ το R4 αντιπροσωπεύει ένα άτομο υδρογόνου ή ένα άτομο φθορίου· το R5 αντιπροσωπεύει ένα άτομο υδρογόνου ή μια ομάδα -ΟΗ∙ όπου τουλάχιστον ένα εκ των R3 ή R5 είναι διαφορετικό από ένα άτομο υδρογόνου∙ όταν το R3 αντιπροσωπεύει μια ομάδα -COOH, -ΟΗ ή -ΟΡΟ(ΟΗ)2, τότε το R5 αντιπροσωπεύει ένα άτομο υδρογόνου∙ όταν το R5 αντιπροσωπεύει μια ομάδα -ΟΗ, τότε τα R3 και R4 αντιπροσωπεύουν άτομα υδρογόνου∙ και το R6 επιλέγεται από μια προαιρετικά υποκατεστημένη ομάδα φαινυλίου, ετεροαρυλίου, κυκλοαλκυλίου ή ετεροκυκλοαλκυλίου.
CY20221100140T 2016-02-15 2022-02-16 Διεργασιες και ενδιαμεσα για την παρασκευη νεων υποκατεστημενων ενωσεων 6,7-διυδρο-5η-βενζο[7] αννουλενιου CY1125165T1 (el)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP16305174 2016-02-15
EP17705842.7A EP3416962B1 (en) 2016-02-15 2017-02-14 6,7-dihydro-5h-benzo[7]annulene derivatives as estrogen receptor modulators
PCT/EP2017/053282 WO2017140669A1 (en) 2016-02-15 2017-02-14 6,7-dihydro-5h-benzo[7]annulene derivatives as estrogen receptor modulators

Publications (1)

Publication Number Publication Date
CY1125165T1 true CY1125165T1 (el) 2023-06-09

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Country Status (37)

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US (6) US9714221B1 (el)
EP (2) EP3416962B1 (el)
JP (4) JP6425852B1 (el)
KR (2) KR20180105759A (el)
CN (2) CN112979524B (el)
AR (1) AR107616A1 (el)
AU (2) AU2017221083B2 (el)
BR (1) BR112018016490A2 (el)
CA (1) CA3014424A1 (el)
CL (1) CL2018002290A1 (el)
CO (1) CO2018009534A2 (el)
CR (1) CR20180442A (el)
CY (1) CY1125165T1 (el)
DK (2) DK3524600T3 (el)
DO (1) DOP2018000184A (el)
EA (2) EA034994B1 (el)
EC (1) ECSP18069466A (el)
ES (2) ES2881508T3 (el)
HR (1) HRP20211043T1 (el)
HU (2) HUE057892T2 (el)
IL (2) IL261099B (el)
LT (1) LT3416962T (el)
MA (2) MA44226B1 (el)
MX (2) MX2018009908A (el)
MY (1) MY196486A (el)
PE (1) PE20181893A1 (el)
PH (1) PH12018501679A1 (el)
PL (1) PL3416962T3 (el)
PT (1) PT3416962T (el)
RS (1) RS62132B1 (el)
SG (2) SG10202106024XA (el)
SI (1) SI3416962T1 (el)
TN (1) TN2018000285A1 (el)
TW (3) TWI779620B (el)
UY (1) UY37124A (el)
WO (1) WO2017140669A1 (el)
ZA (1) ZA201805137B (el)

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* Cited by examiner, † Cited by third party
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MX2018009908A (es) 2016-02-15 2018-09-07 Sanofi Sa Derivados de 6,7-dihidro-5h-benzo[7]anuleno como moduladores de receptores de estrogenos.
JP6946430B2 (ja) * 2016-11-17 2021-10-06 サノフイＳａｎｏｆｉ 新規の置換ｎ−（３−フルオロプロピル）−ピロリジン化合物、それを製造するための方法、およびその治療的使用
WO2018148576A1 (en) 2017-02-10 2018-08-16 G1 Therapeutics, Inc. Benzothiophene estrogen receptor modulators
EP3434272A1 (en) * 2017-07-25 2019-01-30 Sanofi Combination comprising palbociclib and 6-(2,4-dichlorophenyl)-5-[4-[(3s)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulene-2-carboxylic acid
US11759450B2 (en) 2018-02-06 2023-09-19 The Board Of Trustees Of The University Of Illinois Substituted benzothiophene analogs as selective estrogen receptor degraders
EP3837548A2 (en) 2018-08-17 2021-06-23 F. Hoffmann-La Roche AG Diagnostic and therapeutic methods for the treatment of breast cancer
SG11202102057SA (en) 2018-09-07 2021-03-30 Sanofi Sa Process for the preparation of methyl 6-(2,4-dichlorophenyl)-5-[4-[(3s)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulene-2-carboxylate
EP3699167A1 (en) * 2019-02-22 2020-08-26 Sanofi Process for preparing methyl 1-benzosuberone-7-carboxylate
SG11202111979SA (en) 2019-05-09 2021-11-29 Sanofi Sa 6-(2,4-dichlorophenyl)-5-[4-[(3s)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulene-2-carboxylic acid for use in metastatic or advanced breast cancer patients
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