AR081671A1 - Derivados de 6,7-dihidro-5h-benzo[7]anulenos, preparaciones farmaceuticas que los contienen y su uso para la preparacion de medicamentos - Google Patents

Derivados de 6,7-dihidro-5h-benzo[7]anulenos, preparaciones farmaceuticas que los contienen y su uso para la preparacion de medicamentos

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Publication number
AR081671A1
AR081671A1 ARP110102231A ARP110102231A AR081671A1 AR 081671 A1 AR081671 A1 AR 081671A1 AR P110102231 A ARP110102231 A AR P110102231A AR P110102231 A ARP110102231 A AR P110102231A AR 081671 A1 AR081671 A1 AR 081671A1
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AR
Argentina
Prior art keywords
alkyl
hydrogen
cycloalkyl
women
fluorine
Prior art date
Application number
ARP110102231A
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English (en)
Inventor
Tim Wintermantel
Carsten Moeller
Reinhard Nubbemeyer
Ludwig Zorn
Dirk Kosemund
Laak Antonius Ter
Rolf Bohlmann
Lars Wortmann
Ulrich Bothe
Donald Bierer
Original Assignee
Bayer Schering Pharma Ag
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44454656&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR081671(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of AR081671A1 publication Critical patent/AR081671A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/28—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
    • 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
    • A61K31/13—Amines
    • A61K31/145—Amines having sulfur, e.g. thiurams (>N—C(S)—S—C(S)—N< and >N—C(S)—S—S—C(S)—N<), Sulfinylamines (—N=SO), Sulfonylamines (—N=SO2)
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
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    • C07C323/23—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C323/24—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/25—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
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    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/12—One of the condensed rings being a six-membered aromatic ring the other ring being at least seven-membered

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Abstract

Reivindicación 1: Un compuesto, caracterizado porque es de la fórmula química general (1), en donde R1, R2, R3 y R4 son, de manera independiente entre sí, hidrógeno o flúor, en donde al menos un sustituyente seleccionado entre R1, R2, R3 y R4 es flúor; R5, R6 y R7 son, de manera independiente entre sí, hidrógeno, flúor, cloro, bromo, metilo, etilo, trifluorometilo o nitrilo; X se selecciona del grupo que comprende hidrógeno, -alquil C1-6-, -cicloalquil C3-8-, -alquenilo C2-6-, alquinilo C2-6-, -alquil C1-6-S(O)2, alquilcarbonil C1-6-, fenil-alquil C1-6, que opcionalmente puede estar mono, di o polisustituido con -OH, halógeno, -CN, -NR8R9, -C(O)NR10R11, -N(R10)C(O)NR10R11, -haloalcoxi C1-6-, alcoxi C1-6-, -C(O)OH, -C(O)O-alquilo C1-6 o -C(O)O-bencilo, opcionalmente también se pueden cambiar átomos de hidrógeno por átomos de deuterio; R8 y R9 son, alquilo C1-6, cicloalquilo C3-7, fenilo o bencilo opcionalmente sustituido con halógeno o deuterio; R10 y R11 son hidrógeno o alquilo C1-6, cicloalquilo C3-7, fenilo o bencilo opcionalmente sustituidos con halógeno o deuterio; Y es un -alquilo C1-4 perfluorado o parcialmente fluorado o un cicloalquilo C3-8 perfluorado o parcialmente fluorado; m es 4, 5, 6 ó 7; n es 2, 3, 4, 5 ó 6; p es 0, 1 ó 2; q es 0, 1, 2, 3, 4, 5 ó 6; y una sal, solvato o sal de solvato, incluyendo todas las modificaciones cristalinas, del mismo, del mismo.Reivindicación 10: Uso de un compuesto definido en cualquiera de las reivindicaciones 1 a 5, caracterizado porque es para preparar un medicamento para inducir la ovulación, para inhibir la maduración de esperma; para paliar los síntomas de la andropausia y menopausia, es decir, para la terapia de sustitución hormonal masculina y femenina, para la prevención o profilaxis y para el tratamiento de molestias que acompañan la dismenorrea, de sangrados uterinos disfuncionales, del acné, de enfermedades cardiovasculares, de la hipercolesterolemia, de la arterioesclerosis, de la proliferación de células de músculos lisos arteriales, del síndrome de dificultad respiratoria en el recién nacido, de la hipertensión sanguínea pulmonar primarias, de la osteoporosis, de la pérdida de hueso en mujeres posmenopáusicas, en mujeres con histerectomía o en mujeres que fueron tratadas con agonistas o antagonistas LHRH, de la artritis reumatoide, de la enfermedad de Alzheimer; de la endometriosis; de miomas; de tumores hormonodependientes (también en mujeres premenopáusicas), por ejemplo el carcinoma de mama o el carcinoma de endometrio, de la infertilidad, de enfermedades prostáticas, de enfermedades benignas de las mamas como por ejemplo la mastopatía, del ataque de apoplejía, de Alzheimer y otras enfermedades del sistema nervioso central que van acompañadas con la muerte celular de neuronas. Reivindicación 11: Medicamento que contiene un compuesto como el definido en cualquiera de las reivindicaciones 1 a 5, caracterizado porque se usa en combinación con otra sustancia activa, particularmente con análogos de LHRH, para el tratamiento de la endometriosis.
ARP110102231A 2010-06-25 2011-06-27 Derivados de 6,7-dihidro-5h-benzo[7]anulenos, preparaciones farmaceuticas que los contienen y su uso para la preparacion de medicamentos AR081671A1 (es)

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Application Number Priority Date Filing Date Title
DE102010030538A DE102010030538A1 (de) 2010-06-25 2010-06-25 6,7-Dihydro-5H-benzo[7]annulen-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln

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AR081671A1 true AR081671A1 (es) 2012-10-10

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US (1) US20130252890A1 (es)
EP (1) EP2585435A1 (es)
JP (1) JP5530031B2 (es)
KR (1) KR20130089238A (es)
CN (1) CN103080080B (es)
AR (1) AR081671A1 (es)
AU (1) AU2011269067B2 (es)
BR (1) BR112012032758A2 (es)
CA (1) CA2803690A1 (es)
CL (1) CL2012003648A1 (es)
CO (1) CO6660506A2 (es)
CR (1) CR20120657A (es)
CU (1) CU24106B1 (es)
DE (1) DE102010030538A1 (es)
DO (1) DOP2012000325A (es)
EA (1) EA022547B1 (es)
EC (1) ECSP12012355A (es)
GT (1) GT201200347A (es)
IL (1) IL223770A (es)
MA (1) MA34333B1 (es)
MX (1) MX2013000181A (es)
NZ (1) NZ605061A (es)
PE (1) PE20131196A1 (es)
SG (1) SG186437A1 (es)
TN (1) TN2012000618A1 (es)
TW (1) TW201204347A (es)
UA (1) UA108759C2 (es)
UY (1) UY33470A (es)
WO (1) WO2011161101A1 (es)

Families Citing this family (13)

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EP3205648A1 (en) 2010-06-10 2017-08-16 Seragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
DE102011087987A1 (de) * 2011-12-08 2013-06-13 Bayer Intellectual Property Gmbh 6,7-Dihydro-5H-benzo[7]annulen-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln
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