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PE20181893A1 - Nuevos compuestos de 6,7-dihidro-5h-benzo[7]anuleno sustituidos, procesos para su preparacion y usos terapeuticos de los mismos - Google Patents

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

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Publication number
PE20181893A1
PE20181893A1 PE2018001528A PE2018001528A PE20181893A1 PE 20181893 A1 PE20181893 A1 PE 20181893A1 PE 2018001528 A PE2018001528 A PE 2018001528A PE 2018001528 A PE2018001528 A PE 2018001528A PE 20181893 A1 PE20181893 A1 PE 20181893A1
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PE
Peru
Prior art keywords
compounds
hydrogen
benzo
dihydro
preparation
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PE2018001528A
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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 Sa
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Publication of PE20181893A1 publication Critical patent/PE20181893A1/es

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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/4025Heterocyclic 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
    • AHUMAN NECESSITIES
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/4015Heterocyclic 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
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    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract

Referido a compuestos 6,7-dihidro-5H-benzo[7]anuleno sustituidos de formula (I), en donde: R1 y R2 son, independientemente, hidrogeno o deuterio, R3 es hidrogeno, -COOH, -OH o -OPO(OH)2; R4 es hidrogeno o fluor; R5 es hidrogeno o -OH; en donde: al menos uno de R3 o R5 es diferente de hidrogeno; cuando R3 es -COOH, -OH u -OPO(OH)2, entonces R5 es hidrogeno; cuando R5 es -OH, entonces R3 y R4 son, cada uno, hidrogeno y R6 se selecciona entre fenilo, heteroarilo, cicloalquilo o heterocicloalquilo opcionalmente sustituidos. Dichos compuestos son inhibidores y degradadores de los receptores de estrogeno. Tambien refiere a un proceso de preparacion y el uso estos compuestos en el tratamiento del cancer.
PE2018001528A 2016-02-15 2017-02-14 Nuevos compuestos de 6,7-dihidro-5h-benzo[7]anuleno sustituidos, procesos para su preparacion y usos terapeuticos de los mismos PE20181893A1 (es)

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EP16305174 2016-02-15

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PE20181893A1 true PE20181893A1 (es) 2018-12-11

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US (6) US9714221B1 (es)
EP (2) EP3524600B1 (es)
JP (4) JP6425852B1 (es)
KR (2) KR102813741B1 (es)
CN (2) CN112979524B (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)
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DK (2) DK3416962T3 (es)
DO (1) DOP2018000184A (es)
EA (2) EA038639B1 (es)
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HU (2) HUE057892T2 (es)
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LT (1) LT3416962T (es)
MA (2) MA44226B1 (es)
MX (2) MX386677B (es)
MY (2) 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)
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TW (3) TWI737681B (es)
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ZA (1) ZA201805137B (es)

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PE20181893A1 (es) 2016-02-15 2018-12-11 Sanofi Sa Nuevos compuestos de 6,7-dihidro-5h-benzo[7]anuleno sustituidos, procesos para su preparacion y usos terapeuticos de los mismos
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
TW201835064A (zh) 2017-02-10 2018-10-01 美商G1治療公司 苯并噻吩雌激素受體調節劑
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
EP3749654B1 (en) * 2018-02-06 2025-04-23 The Board of Trustees of the University of Illinois Substituted benzothiophene analogs as selective estrogen receptor degraders
CN113490850B (zh) 2018-08-17 2024-12-06 基因泰克公司 用于治疗乳腺癌的诊断和治疗方法
AR116300A1 (es) 2018-09-07 2021-04-21 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
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
EP4037768B1 (en) * 2019-10-01 2023-10-11 Sanofi Novel substituted 6,7-dihydro-5h-benzo[7]annulene compounds, processes for their preparation and therapeutic uses thereof
KR20220113695A (ko) * 2019-12-09 2022-08-16 사노피 7h-벤조[7]아눌렌-2-카르복실산 유도체의 결정질 형태
TW202146007A (zh) 2020-02-27 2021-12-16 法商賽諾菲公司 包含阿培利司(alpelisib)與6-(2,4-二氯苯基)-5-[4-[(3s)-1-(3-氟丙基)吡咯啶-3-基]氧苯基]-8,9-二氫-7h-苯并[7]輪烯-2-羧酸之組合
CN113896669B (zh) * 2020-06-22 2024-12-17 海南先声再明医药股份有限公司 雌激素受体调节剂及其用途
US12415799B2 (en) 2020-06-28 2025-09-16 Zhejiang Yangli Pharmaceutical Technology Co., Ltd. Indazole-fused cyclic compound
EP4228758B1 (en) 2020-10-19 2024-07-24 Sanofi Substituted 6,7-dihydro-5h-benzo[7]annulene compounds and their derivatives, processes for their preparation and therapeutic uses thereof
EP4228757B1 (en) * 2020-10-19 2024-08-14 Sanofi Substituted 6,7-dihydro-5h-benzo[7]annulene compounds and their derivatives, processes for their preparation and therapeutic uses thereof
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