MA44226B1 - Dérivés de 6,7-dihydro-5h-benzo[7]annulène comme modulateurs de récepteurs d' oestrogènes - Google Patents

Dérivés de 6,7-dihydro-5h-benzo[7]annulène comme modulateurs de récepteurs d' oestrogènes

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Publication number
MA44226B1
MA44226B1 MA44226A MA44226A MA44226B1 MA 44226 B1 MA44226 B1 MA 44226B1 MA 44226 A MA44226 A MA 44226A MA 44226 A MA44226 A MA 44226A MA 44226 B1 MA44226 B1 MA 44226B1
Authority
MA
Morocco
Prior art keywords
group
hydrogen atom
benzo
dihydro
estrogen receptor
Prior art date
Application number
MA44226A
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English (en)
Inventor
Gary Mccort
Youssef El-Ahmad
Laurent Schio
Monsif Bouaboula
Maurice Brollo
Victor Certal
Bruno Filoche-Rommé
Frank Halley
Michel Tabart
Corinne Terrier
Fabienne Thompson
Original Assignee
Sanofi Sa
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sanofi Sa filed Critical Sanofi Sa
Publication of MA44226B1 publication Critical patent/MA44226B1/fr

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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • 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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    • C07—ORGANIC CHEMISTRY
    • 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
    • A61K31/4015—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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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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 containing two hetero rings
    • C07D401/12—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 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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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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    • C07D417/00—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 C07D415/00
    • C07D417/02—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 C07D415/00 containing two hetero rings
    • C07D417/12—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 C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D471/02—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 C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
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    • C07F9/572—Five-membered rings
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  • Diabetes (AREA)
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  • Pregnancy & Childbirth (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyrrole Compounds (AREA)
  • Steroid Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

La présente invention concerne des composés de formule (i) : r1 et r2 représentent des atomes d'hydrogène ou de deutérium; r3 représente un atome d'hydrogène ou un groupe -cooh, -oh ou -opo(oh)2; r4 représente un atome d'hydrogène ou un atome de fluor; r5 représente un atome d'hydrogène ou un groupe -oh; au moins l'un de r3 ou r5 étant différent d'un atome d'hydrogène; quand r3 représente un groupe -cooh, -oh ou -opo(oh)2, alors r5 représente un atome d'hydrogène; quand r5 représente un groupe -oh, alors r3 et r4 représentent des atomes d'hydrogène; et r6 est choisi parmi un groupe phényle, hétéroaryle, cycloalkyle ou hétérocycloalkyle éventuellement substitué. L'invention concerne également la préparation et les utilisations thérapeutiques des composés de formule (i) en tant qu'inhibiteurs et agents de dégradation de récepteurs des œstrogènes, utilisés en particulier pour le traitement du cancer.
MA44226A 2016-02-15 2017-02-14 Dérivés de 6,7-dihydro-5h-benzo[7]annulène comme modulateurs de récepteurs d' oestrogènes MA44226B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP16305174 2016-02-15
PCT/EP2017/053282 WO2017140669A1 (fr) 2016-02-15 2017-02-14 Dérivés de 6,7-dihydro-5h-benzo[7]annulène utilisés en tant que modulateurs de récepteurs des oestrogènes

Publications (1)

Publication Number Publication Date
MA44226B1 true MA44226B1 (fr) 2021-07-29

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ID=55398242

Family Applications (2)

Application Number Title Priority Date Filing Date
MA046479A MA46479A (fr) 2016-02-15 2017-02-14 Procédés et intermédiaires pour la préparation de nouveaux composés substitués de 6,7-dihydro-5h-benzo[7]annulène
MA44226A MA44226B1 (fr) 2016-02-15 2017-02-14 Dérivés de 6,7-dihydro-5h-benzo[7]annulène comme modulateurs de récepteurs d' oestrogènes

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Application Number Title Priority Date Filing Date
MA046479A MA46479A (fr) 2016-02-15 2017-02-14 Procédés et intermédiaires pour la préparation de nouveaux composés substitués de 6,7-dihydro-5h-benzo[7]annulène

Country Status (37)

Country Link
US (6) US9714221B1 (fr)
EP (2) EP3524600B1 (fr)
JP (4) JP6425852B1 (fr)
KR (2) KR20220098057A (fr)
CN (2) CN112979524A (fr)
AR (1) AR107616A1 (fr)
AU (2) AU2017221083B2 (fr)
BR (1) BR112018016490A2 (fr)
CA (1) CA3014424A1 (fr)
CL (1) CL2018002290A1 (fr)
CO (1) CO2018009534A2 (fr)
CR (1) CR20180442A (fr)
CY (1) CY1125165T1 (fr)
DK (2) DK3524600T3 (fr)
DO (1) DOP2018000184A (fr)
EA (2) EA038639B1 (fr)
EC (1) ECSP18069466A (fr)
ES (2) ES2906208T3 (fr)
HR (1) HRP20211043T1 (fr)
HU (2) HUE055107T2 (fr)
IL (2) IL261099B (fr)
LT (1) LT3416962T (fr)
MA (2) MA46479A (fr)
MX (2) MX2020011469A (fr)
MY (1) MY196486A (fr)
PE (1) PE20181893A1 (fr)
PH (1) PH12018501679A1 (fr)
PL (1) PL3416962T3 (fr)
PT (1) PT3416962T (fr)
RS (1) RS62132B1 (fr)
SG (2) SG11201806829TA (fr)
SI (1) SI3416962T1 (fr)
TN (1) TN2018000285A1 (fr)
TW (3) TWI737681B (fr)
UY (1) UY37124A (fr)
WO (1) WO2017140669A1 (fr)
ZA (1) ZA201805137B (fr)

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JP6425852B1 (ja) * 2016-02-15 2018-11-21 サノフイＳａｎｏｆｉ エストロゲン受容体調節剤としての６，７−ジヒドロ−５ｈ−ベンゾ［７］アヌレン誘導体
WO2018091153A1 (fr) * 2016-11-17 2018-05-24 Sanofi Nouveaux composés n-(3-fluoropropyl)-pyrrolidine substitués, leurs procédés de préparation et leurs utilisations thérapeutiques
AU2018217809A1 (en) 2017-02-10 2019-08-22 G1 Therapeutics, Inc. Benzothiophene estrogen receptor modulators
EP3434272A1 (fr) 2017-07-25 2019-01-30 Sanofi Combinaison comprenant du palbociclib et 6-(2,4-dichlorophényl)-5-[4-[(3s)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulène-2-acide carboxylique
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
AU2019321588A1 (en) 2018-08-17 2021-03-04 Genentech, Inc. Diagnostic and therapeutic methods for the treatment of breast cancer
MX2021002666A (es) * 2018-09-07 2021-07-16 Sanofi Sa Proceso para la preparacion de 6-(2,4-diclorofenil)-5-[4-[(3s)-1-( 3-fluoropropil)pirrolidin-3-il]oxifenil]-8,9-dihidro-7h-benzo[7]a nulen-2-carboxilato de metilo.
EP3699167A1 (fr) * 2019-02-22 2020-08-26 Sanofi Procédé de préparation de méthyl 1-benzosuberone-7-carboxylate
JP2022531898A (ja) 2019-05-09 2022-07-12 サノフイ 転移性または進行性乳房がん患者において使用するための６－（２，４－ジクロロフェニル）－５－［４－［（３ｓ）－１－（３－フルオロプロピル）ピロリジン－３－イル］オキシフェニル］－８，９－ジヒドロ－７ｈ－ベンゾ［７］アヌレン－２－カルボン酸
KR102058384B1 (ko) * 2019-09-06 2019-12-24 강원대학교산학협력단 2h-벤조[7]에눌렌 화합물 및 이의 제조방법
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