CR20180442A - 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
CR20180442A
CR20180442A CR20180442A CR20180442A CR20180442A CR 20180442 A CR20180442 A CR 20180442A CR 20180442 A CR20180442 A CR 20180442A CR 20180442 A CR20180442 A CR 20180442A CR 20180442 A CR20180442 A CR 20180442A
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CR
Costa Rica
Prior art keywords
preparation
group
hydrogen atom
therapeutic uses
benzo
Prior art date
Application number
CR20180442A
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English (en)
Inventor
Corinne; Terrier
Laurent; Schio
Monsif; Bouaboula
Youssef; El-Ahmad
Michel; Tabart
Fabienne; Thompson
Victor; Certal
Gary Mccort
Maurice; Brollo
Bruno; Filoche-Rommé
Frank; Halley
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.)
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Publication date
Application filed by Sanofi Sa filed Critical Sanofi Sa
Publication of CR20180442A publication Critical patent/CR20180442A/es

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    • 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
    • A61K31/4025—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
    • 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
    • A61K31/40—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
    • 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
    • A61K31/435—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
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    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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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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    • 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
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    • C07D209/04—Indoles; Hydrogenated indoles
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    • 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
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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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    • C07D417/12—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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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyrrole Compounds (AREA)
  • Steroid Compounds (AREA)
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Abstract

Nuevos compuestos de 6,7-dihidro-5h-benzo[7]anuleno sustituidos, procesos para su preparación y usos terapéuticos de los mismos. 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.
CR20180442A 2016-02-15 2017-02-14 Nuevos compuestos de 6,7-dihidro-5h-benzo[7]anuleno sustituidos, procesos para su preparación y usos terapéuticos de los mismos CR20180442A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP16305174 2016-02-15
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
CR20180442A true CR20180442A (es) 2018-12-21

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CR20180442A CR20180442A (es) 2016-02-15 2017-02-14 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) KR20220098057A (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) DK3416962T3 (es)
DO (1) DOP2018000184A (es)
EA (2) EA038639B1 (es)
EC (1) ECSP18069466A (es)
ES (2) ES2906208T3 (es)
HR (1) HRP20211043T1 (es)
HU (2) HUE057892T2 (es)
IL (2) IL261099B (es)
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MA (2) MA46479A (es)
MX (2) MX2020011469A (es)
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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)
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TW (3) TWI779621B (es)
UY (1) UY37124A (es)
WO (1) WO2017140669A1 (es)
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CN108884079B (zh) 2016-02-15 2021-03-05 赛诺菲 作为雌激素受体调节剂的6，7-二氢-5h-苯并[7]轮烯衍生物
SG11201903908PA (en) * 2016-11-17 2019-05-30 Sanofi Sa Novel substituted n-(3-fluoropropyl)-pyrrolidine compounds, processes for their preparation and therapeutic uses thereof
JP2020507566A (ja) 2017-02-10 2020-03-12 ジー１ セラピューティクス， インコーポレイテッド ベンゾチオフェンエストロゲン受容体モジュレーター
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
CA3109090A1 (en) 2018-08-17 2020-02-20 F. Hoffmann-La Roche Ag Diagnostic and therapeutic methods for the treatment of breast cancer
ES2924738T3 (es) 2018-09-07 2022-10-10 Sanofi Sa Proceso para la preparación de 6-(2,4-diclorofenil)-5-[4-[(3S)-1-(3-fluoropropil)pirrolidin-3-il]oxifenil]-8,9-dihidro-7H-benzo[7]anuleno-2-carboxilato de metilo y una sal del mismo
EP3699167A1 (en) 2019-02-22 2020-08-26 Sanofi Process for preparing methyl 1-benzosuberone-7-carboxylate
MX2021013711A (es) 2019-05-09 2021-12-10 Sanofi Sa Acido 6-(2,4-diclorofenil)-5-[4-[(3s)-1-(3-fluoropropil)pirrolidin -3-il]oxifenil]-8,9-dihidro-7h-benzo[7]anuleno-2-carboxilico para su uso en pacientes con cancer de mama metastasico o avanzado.
KR102058384B1 (ko) * 2019-09-06 2019-12-24 강원대학교산학협력단 2h-벤조[7]에눌렌 화합물 및 이의 제조방법
CN114502562A (zh) * 2019-10-01 2022-05-13 赛诺菲 新颖的经取代的6,7-二氢-5h-苯并[7]轮烯化合物、其制备方法以及其治疗用途
CA3160897A1 (en) 2019-12-09 2021-06-17 Sanofi Crystalline form of a 7h-benzo[7]annulene-2-carboxylic acid derivative
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