ECSP18069466A - Nuevos compuestos de 6,7-dihidro-5h-benzo[7]anuleno sustituidos, procesos para su preparación y usos terapéuticos de los mismos - Google Patents

Nuevos compuestos de 6,7-dihidro-5h-benzo[7]anuleno sustituidos, procesos para su preparación y usos terapéuticos de los mismos

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Publication number
ECSP18069466A
ECSP18069466A ECSENADI201869466A ECDI201869466A ECSP18069466A EC SP18069466 A ECSP18069466 A EC SP18069466A EC SENADI201869466 A ECSENADI201869466 A EC SENADI201869466A EC DI201869466 A ECDI201869466 A EC DI201869466A EC SP18069466 A ECSP18069466 A EC SP18069466A
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EC
Ecuador
Prior art keywords
compounds
group
preparation
hydrogen atom
therapeutic uses
Prior art date
Application number
ECSENADI201869466A
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English (en)
Inventor
Laurent Schio
Bruno Filoche-Romme
Michel Tabart
Maurice Brollo
Monsif Bouaboula
Fabienne Thompson
Gary Mccort
Victor Certal
Corinne Terrier
Youssef El-Ahmad
Frank Halley
Original Assignee
Sanofi Sa
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Publication date
Application filed by Sanofi Sa filed Critical Sanofi Sa
Publication of ECSP18069466A publication Critical patent/ECSP18069466A/es

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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
    • A—HUMAN NECESSITIES
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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
    • A61K31/4015—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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    • A61K31/395—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/495—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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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P35/00—Antineoplastic agents
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    • 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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    • 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
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    • 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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    • 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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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
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    • 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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    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • 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
    • C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
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  • Animal Behavior & Ethology (AREA)
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  • Epidemiology (AREA)
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  • Diabetes (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
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  • Biochemistry (AREA)
  • 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 presente invención se refiere a compuestos de fórmula (I): en donde R1 y R2 representan átomos de hidrógeno o deuterio; R3 representa un átomo de hidrógeno o un grupo -COOH, -OH u -OPO(OH)2; R4 representa un átomo de hidrógeno o un átomo de flúor; R5 representa un átomo de hidrógeno o un grupo -OH; en donde al menos uno de R3 o R5 es diferente de un átomo de hidrógeno; cuando R3 representa un grupo –COOH, OH u OPO(OH)2, entonces R5 representa un átomo de hidrógeno; cuando R5 representa un grupo -OH, entonces R3 y R4 representan átomos de hidrógeno; y R6 se selecciona entre un grupo fenilo, heteroarilo, cicloalquilo o heterocicloalquilo opcionalmente sustituido. La invención se refiere también a la preparación y a los usos terapéuticos de los compuestos de fórmula (I) como inhibidores y degradadores de los receptores de estrógeno, útiles especialmente en el tratamiento del cáncer.
ECSENADI201869466A 2016-02-15 2018-09-13 Nuevos compuestos de 6,7-dihidro-5h-benzo[7]anuleno sustituidos, procesos para su preparación y usos terapéuticos de los mismos ECSP18069466A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP16305174 2016-02-15

Publications (1)

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ECSP18069466A true ECSP18069466A (es) 2018-09-30

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ECSENADI201869466A ECSP18069466A (es) 2016-02-15 2018-09-13 Nuevos compuestos de 6,7-dihidro-5h-benzo[7]anuleno sustituidos, procesos para su preparación y usos terapéuticos de los mismos

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US (6) US9714221B1 (es)
EP (2) EP3524600B1 (es)
JP (4) JP6425852B1 (es)
KR (2) KR20180105759A (es)
CN (2) CN108884079B (es)
AR (1) AR107616A1 (es)
AU (2) AU2017221083B2 (es)
BR (1) BR112018016490A2 (es)
CA (1) CA3014424A1 (es)
CL (1) CL2018002290A1 (es)
CO (1) CO2018009534A2 (es)
CR (1) CR20180442A (es)
CY (1) CY1125165T1 (es)
DK (2) DK3524600T3 (es)
DO (1) DOP2018000184A (es)
EA (2) EA038639B1 (es)
EC (1) ECSP18069466A (es)
ES (2) ES2906208T3 (es)
HR (1) HRP20211043T1 (es)
HU (2) HUE055107T2 (es)
IL (2) IL261099B (es)
LT (1) LT3416962T (es)
MA (2) MA46479A (es)
MX (2) MX2018009908A (es)
MY (1) MY196486A (es)
PE (1) PE20181893A1 (es)
PH (1) PH12018501679A1 (es)
PL (1) PL3416962T3 (es)
PT (1) PT3416962T (es)
RS (1) RS62132B1 (es)
SG (2) SG10202106024XA (es)
SI (1) SI3416962T1 (es)
TN (1) TN2018000285A1 (es)
TW (3) TWI737681B (es)
UY (1) UY37124A (es)
WO (1) WO2017140669A1 (es)
ZA (1) ZA201805137B (es)

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AR107616A1 (es) 2016-02-15 2018-05-16 Sanofi Sa Compuestos de 6,7-dihidro-5h-benzo[7]anuleno sustituidos, procesos para su preparación y usos terapéuticos de los mismos
MX2019005777A (es) * 2016-11-17 2019-08-12 Sanofi Sa Compuestos de n-(3fluoropropil)-pirrolidina sustituidos novedosos, procesos para su preparacion y usos terapeuticos de los mismos.
AU2018217809A1 (en) 2017-02-10 2019-08-22 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
JP7348665B2 (ja) 2018-02-06 2023-09-21 ザ ボード オブ トラスティーズ オブ ザ ユニヴァーシティ オブ イリノイ 選択的エストロゲン受容体分解剤としての置換ベンゾチオフェン類似体
JP2021533787A (ja) 2018-08-17 2021-12-09 ジェネンテック， インコーポレイテッド 乳がんの処置のための診断的および治療的方法
EP3847156B1 (en) 2018-09-07 2022-05-04 Sanofi Salts 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 and preparation process thereof
EP3699167A1 (en) 2019-02-22 2020-08-26 Sanofi Process for preparing methyl 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
US20230115865A1 (en) * 2019-10-01 2023-04-13 Sanofi Novel Substituted 6,7-Dihydro-5H-Benzo[7]Annulene Compounds, Processes for Their Preparation and Therapeutic Uses Thereof
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