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AR107616A1 - Compuestos de 6,7-dihidro-5h-benzo[7]anuleno sustituidos, procesos para su preparación y usos terapéuticos de los mismos - Google Patents

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
AR107616A1
AR107616A1 ARP170100360A ARP170100360A AR107616A1 AR 107616 A1 AR107616 A1 AR 107616A1 AR P170100360 A ARP170100360 A AR P170100360A AR P170100360 A ARP170100360 A AR P170100360A AR 107616 A1 AR107616 A1 AR 107616A1
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AR
Argentina
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group
substituted
unsubstituted
hydrogen atom
alkyl
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ARP170100360A
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Sanofi Sa
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Publication of AR107616A1 publication Critical patent/AR107616A1/es

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    • 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
    • A61K31/4025—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
    • A—HUMAN NECESSITIES
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    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32—Antioestrogens
    • C—CHEMISTRY; METALLURGY
    • 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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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • 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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    • C07—ORGANIC CHEMISTRY
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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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    • C07D403/02—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
    • 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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    • C07D405/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D413/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C07D471/04—Ortho-condensed systems
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    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
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    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
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    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • 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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    • C07B2200/07—Optical isomers

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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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Abstract

La presente solicitud se refiere a la preparación, a los usos terapéuticos y compuestos inhibidores y degradadores de los receptores de estrógeno, útiles especialmente en el tratamiento del cáncer. Reivindicación 1: Un compuesto de fórmula [1], en donde: R¹ y R² representan independientemente un átomo de hidrógeno o un átomo de deuterio; R³ representa un átomo de hidrógeno, un grupo -COOH, un grupo -OH o un grupo -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, un grupo -OH o un grupo -OPO(OH)₂, entonces R⁵ representa un átomo de hidrógeno; cuando R⁵ representa un grupo -OH, entonces R³ y R⁴ representan átomos de hidrógeno; R⁶ se selecciona entre: un grupo fenilo o un grupo heteroarilo que comprende 3 a 9 átomos de carbono y que comprende de 1 a 3 heteroátomos seleccionados independientemente entre oxígeno, nitrógeno y azufre, estando dichos grupos fenilo y heteroarilo sin sustituir o sustituidos con 1 a 3 sustituyentes seleccionados independientemente entre: un grupo alquilo C₁₋₆ sin sustituir o sustituido con uno o más átomos de flúor; un átomo de halógeno; un grupo -OH; un grupo alcoxi C₁₋₆ sin sustituir o sustituido con uno o más átomos de flúor; un grupo ciano; un grupo sulfuro sustituido con 5 átomos de flúor o grupos alquilo C₁₋₆ sustituidos con dos o más átomos de flúor; un grupo sulfonil-alquilo C₁₋₆ en donde dicho grupo alquilo C₁₋₆ está sin sustituir o sustituido con dos o más átomos de flúor; un grupo silano sustituido con 3 grupos alquilo C₁₋₆; un grupo amina sin sustituir o sustituido con uno o más grupos alquilo C₁₋₆; un grupo amida sin sustituir o sustituido con uno o más grupos alquilo C₁₋₆; un grupo heterocicloalquilo saturado o parcialmente saturado, que comprende 3 a 5 átomos de carbono y que comprende 1 ó 2 heteroátomos seleccionados independientemente entre oxígeno, nitrógeno o azufre, o un grupo heteroarilo que comprende 2 a 4 átomos de carbono y que comprende 1 a 3 heteroátomos seleccionados entre oxígeno, nitrógeno o azufre y que están sin sustituir o sustituidos con un grupo oxo; un grupo cicloalquilo o un grupo heterocicloalquilo que comprende 4 a 9 átomos de carbono y que comprende 1 ó 2 heteroátomos seleccionados independientemente entre oxígeno, nitrógeno o azufre, estando dichos grupos cicloalquilo o heterocicloalquilo saturados o parcialmente saturados y estando sin sustituir o sustituidos con 1 a 4 sustituyentes seleccionados independientemente entre: un átomo de flúor; un grupo -OH; un grupo alquilo C₁₋₆; un grupo -COOR⁷ en donde R⁷ es un grupo alquilo C₁₋₆; o un grupo oxo; o una sal farmacéuticamente aceptable del mismo. Reivindicación 6: Los compuestos seleccionados entre las fórmulas del grupo de fórmulas [2] en donde R¹, R², R³, R⁴, R⁵ y R⁶ son como se han definido en la formula [1] según cualquiera de las reivindicaciones 1 a 4.
ARP170100360A 2016-02-15 2017-02-14 Compuestos de 6,7-dihidro-5h-benzo[7]anuleno sustituidos, procesos para su preparación y usos terapéuticos de los mismos AR107616A1 (es)

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AR107616A1 true AR107616A1 (es) 2018-05-16

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US (6) US9714221B1 (es)
EP (2) EP3416962B1 (es)
JP (4) JP6425852B1 (es)
KR (2) KR20220098057A (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)
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CY (1) CY1125165T1 (es)
DK (2) DK3416962T3 (es)
DO (1) DOP2018000184A (es)
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ES (2) ES2906208T3 (es)
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TW (3) TWI737681B (es)
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CN112979524B (zh) * 2016-02-15 2024-09-10 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
EP3541809A1 (en) * 2016-11-17 2019-09-25 Sanofi Novel substituted n-(3-fluoropropyl)-pyrrolidine compounds, processes for their preparation and therapeutic uses thereof
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
CN112041307B (zh) * 2018-02-06 2024-02-09 伊利诺伊大学评议会 作为选择性雌激素受体降解剂的取代的苯并噻吩类似物
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