AR103081A1 - Tetrahidro-pirido[3,4-b]indoles moduladores de receptores de estrógenos y usos de los mismos - Google Patents

Tetrahidro-pirido[3,4-b]indoles moduladores de receptores de estrógenos y usos de los mismos

Info

Publication number
AR103081A1
AR103081A1 ARP150104155A ARP150104155A AR103081A1 AR 103081 A1 AR103081 A1 AR 103081A1 AR P150104155 A ARP150104155 A AR P150104155A AR P150104155 A ARP150104155 A AR P150104155A AR 103081 A1 AR103081 A1 AR 103081A1
Authority
AR
Argentina
Prior art keywords
2conh2
alkyldiyl
coch3
nra
methanone
Prior art date
Application number
ARP150104155A
Other languages
English (en)
Original Assignee
Hoffmann La Roche
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.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR103081A1 publication Critical patent/AR103081A1/es

Links

Classifications

    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Reivindicación 1: Un compuesto elegido entre la fórmula (1), y estereoisómeros, tautómeros o sales farmacéuticamente aceptables del mismo, en el que: Y¹ es CRᵇ o N; Y² es -(CH₂)-, -(CH₂CH₂)- o NRᵃ; Y³ es NRᵃ o C(Rᵇ)₂; en los que uno de Y¹, Y² e Y³ es N o NRᵃ; Rᵃ se elige entre H, alquilo C₁₋₆, alquenilo C₂₋₈, propargilo, cicloalquilo C₃₋₆ y heterociclilo C₃₋₆, opcionalmente sustituido con uno o más grupos elegidos con independencia entre F, Cl, Br, I, CN, OH, OCH₃ y SO₂CH₃; Rᵇ se elige con independencia entre H, -O(alquilo C₁₋₃), alquilo C₁₋₆, alquenilo C₂₋₈, propargilo, -(alquildiil C₁₋₆)-(cicloalquilo C₃₋₆), cicloalquilo C₃₋₆ y heterociclilo C₃₋₆, opcionalmente sustituido con uno o más grupos elegidos con independencia entre F, Cl, Br, I, CN, -CH₂F, -CHF₂, -CF₃, -CH₂CF₃, -CH₂CHF₂, -CH₂CH₂F, OH, OCH₃ y SO₂CH₃, Rᶜ se elige entre H, alquilo C₁₋₆, alilo, propargilo, opcionalmente sustituido con uno o más grupos elegidos con independencia entre F, Cl, Br, I, CN, OH, OCH₃ y SO₄CH₃; Z¹ se elige entre CRᵃRᵇ, C(O) y un enlace; Cy se elige entre arildiilo C₆₋₂₀, carbociclildiilo C₃₋₁₂, heterociclildiilo C₂₋₂₀ y heteroarildiilo C₁₋₂₀; Z² se elige entre O, S, NRᵃ, alquildiilo C₁₋₆, fluoralquildiilo C₁₋₆, O-(alquildiilo C₁₋₆), O-(fluoralquildiilo C₁₋₆), C(O) y un enlace; R¹, R², R³ y R⁴ se eligen con independencia entre H, F, Cl, Br, I, -CN, -CH₃, -CH₂CH₃, -CH(CH₃)₂, -CH₂CH(CH₃)₂, -CH₂OH, -CH₂OCH₃, -CH₂CH₂OH, -C(CH₃)₂OH, -CH(OH)CH(CH₃)₂, -C(CH₃)₂CH₂OH, -CH₂CH₂SO₂CH₃, -CH₂OP(O)(OH)₂, -CH₂F, -CHF₂, -CH₂NH₂, -CH₂NHSO₂CH₃, -CH₂NHCH₃, -CH₂N(CH₃)₂, -CF₃, -CH₂CF₃, -CH₂CHF₂, -CH(CH₃)CN, -C(CH₃)₂CN, -CH₂CN, -CO₂H, -COCH₃, -CO₂CH₃, -CO₂C(CH₃)₃, -COCH(OH)CH₃, -CONH₂, -CONHCH₃, -CONHCH₂CH₃, -CONHCH(CH₃)₂, -CON(CH₃)₂, -C(CH₃)₂CONH₂, -NH₂, -NHCH₃, -N(CH₃)₂, -NHCOCH₃, -N(CH₃)COCH₃, -NHS(O)₂CH₃, -N(CH₃)C(CH₃)₂CONH₂, -N(CH₃)CH₂CH₂S(O)₂CH₃, -NO₂, =O, -OH, -OCH₃, -OCH₂CH₃, -OCH₂CH₂OCH₃, -OCH₂CH₂OH, -OCH₂CH₂N(CH₃)₂, -OP(O)(OH)₂, -S(O)₂N(CH₃)₂, -SCH₃, -S(O)₂CH₃, -S(O)₃H, ciclopropilo, ciclopropilamida, ciclobutilo, oxetanilo, azetidinilo, 1-metilazetidin-3-il)oxi, N-metil-N-oxetan-3-ilamino, azetidin-1-ilmetilo, benciloxifenilo, pirrolidin-1-ilo, pirrolidin-1-il-metanona, piperazin-1-ilo, morfolinometilo, morfolino-metanona y morfolino; R⁵ se elige entre H, alquilo C₁₋₉, cicloalquilo C₃₋₉, heterociclo C₃₋₉, arilo C₆₋₉, heteroarilo C₆₋₉, -(alquildiil C₁₋₆)-(cicloalquilo C₃₋₉), -(alquildiil C₁₋₆)-(heterociclo C₃₋₉), C(O)Rᵇ, C(O)NRᵃ, SO₂Rᵃ y SO₂NRᵃ, opcionalmente sustituido con uno o más de halógeno, CN, ORᵃ, N(Rᵃ)₂, alquilo C₁₋₉, cicloalquilo C₃₋₉, heterociclo C₃₋₉, arilo C₃₋₉, heteroarilo C₆₋₉, C₍O₎Rᵇ, C(O)NRᵃ, SO₂Rᵃ y SO₂NRᵃ; R⁶ se elige entre F, Cl, Br, I, -CN, -CH₃, -CH₂CH₃, -CH(CH₃)₂, -CH₂CH(CH₃)₂, -CH₂OH, -CH₂OCH₃, -CH₂CH₂OH, -C(CH₃)₂OH, -CH(OH)CH(CH₃)₂, -C(CH₃)₂CH₂OH, -CH₂CH₂SO₂CH₃, -CH₂OP(O)(OH)₂, -CH₂F, -CHF₂, -CH₂NH₂, -CH₂NHSO₂CH₃, -CH₂NHCH₃, -CH₂N(CH₃)₂, -CF₃, -CH₂CF₃, -CH₂CHF₂, -CH₂CH₂F, -CH(CH₃)CN, -C(CH₃)₂CN, -CH₂CN, -CO₂H, -COCH₃, -CO₂CH₃, -CO₂C(CH₃)₂, -COCH(OH)CH₃, -CONH₂, -CONHCH₃, -CONHCH₂CH₃, -CONHCH(CH₃)₂, -CON(CH₃)₂, -C(CH₃)₂CONH₂, -NH₂, -NHCH₃, -N(CH₃)₂, -NHCOCH₃, -N(CH₃)COCH₃, -NHS(O)₂CH₃, -N(CH₃)C(CH₃)₂CONH₂, -N(CH₃)CH₂CH₂S(O)₂CH₃, -NO₂, =O, -OH, -OCH₃, -OCH₂CH₃, -OCH₂CH₂OCH₃, -OCH₂CH₂OH, -OCH₂CH₂N(CH₃)₂, -OP(O)(OH)₂, -S(O)₂N(CH₃)₂, -SCH₃, -S(O)₂CH₃, -S(O)₃H, ciclopropilo, ciclopropilamida, ciclobutilo, oxetanilo, azetidinilo, 1-metilazetidin-3-il)oxi, N-metil-N-oxetan-3-ilamino, azetidin-1-ilmetilo, benciloxifenilo, pirrolidin-1-ilo, pirrolidin-1-il-metanona, piperazin-1-ilo, morfolinometilo, morfolino-metanona y morfolino; y m se elige entre 0, 1, 2, 3 y 4; dichos alquildiilo, fluoralquildiilo, arildiilo, carbociclildiilo, heterociclildiilo y heteroarildiilo están opcionalmente sustituidos por uno o más grupos elegidos con independencia entre F, Cl, Br, I, -CN, -CH₃, -CH₂CH₃, -CH(CH₃)₂, -CH₂CH(CH₃)₂, -CH₂OH, -CH₂OCH₃, -CH₂CH₂OH, -C(CH₃)₂OH, -CH(OH)CH(CH₃)₂, -C(CH₃)₂CH₂OH, -CH₂CH₂SO₂CH₃, -CH₂OP(O)(OH)₂, -CH₂F, -CHF₂, -CF₃, -CH₂CF₃, -CH₂CHF₂, -CH₂CH₂F, -CH(CH₃)CN, -C(CH₃)₂CN, -CH₂CN, -CH₂NH₂, -CH₂NHSO₂CH₃, -CH₂NHCH₃, -CH₂N(CH₃)₂, -CO₂H, -COCH₃, -CO₂CH₃, -CO₂C(CH₃)₃, -COCH(OH)CH₃, -CONH₂, -CONHCH₃, -CON(CH₃)₂, -C(CH₃)₂CONH₂, -NH₂, -NHCH₃, -N(CH₃)₂, -NHCOCH₃, -N(CH₃)COCH₃, -NHS(O)₂CH₃, -N(CH₃)C(CH₃)₂CONH₂, -N(CH₃)CH₂CH₂S(O)₂CH₃, -NO₂, =O, -OH, -OCH₃, -OCH₂CH₃, -OCH₂CH₂OCH₃, -OCH₂CH₂OH, -OCH₂CH₂N(CH₃)₂, -OP(O)(OH)₂, -S(O)₂N(CH₃)₂, -SCH₃, -S(O)₂CH₃, -S(O)₃H, ciclopropilo, ciclopropilamida, ciclobutilo, oxetanilo, azetidinilo, 1-metilazetidin-3-il)oxi, N-metil-N-oxetan-3-ilamino, azetidin- 1-ilmetilo, benciloxifenilo, pirrolidin-l-ilo, pirrolidin-1-il-metanona, piperazin-1-ilo, morfolinometilo, morfolino-metanona y morfolino.
ARP150104155A 2014-12-18 2015-12-17 Tetrahidro-pirido[3,4-b]indoles moduladores de receptores de estrógenos y usos de los mismos AR103081A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462093929P 2014-12-18 2014-12-18

Publications (1)

Publication Number Publication Date
AR103081A1 true AR103081A1 (es) 2017-04-12

Family

ID=58672209

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP150104155A AR103081A1 (es) 2014-12-18 2015-12-17 Tetrahidro-pirido[3,4-b]indoles moduladores de receptores de estrógenos y usos de los mismos
ARP210101150A AR122456A2 (es) 2014-12-18 2021-04-28 Tetrahidro-pirido[3,4-b]indoles moduladores de receptores de estrógenos y usos de los mismos

Family Applications After (1)

Application Number Title Priority Date Filing Date
ARP210101150A AR122456A2 (es) 2014-12-18 2021-04-28 Tetrahidro-pirido[3,4-b]indoles moduladores de receptores de estrógenos y usos de los mismos

Country Status (2)

Country Link
AR (2) AR103081A1 (es)
MA (1) MA41172B1 (es)

Also Published As

Publication number Publication date
MA41172B1 (fr) 2020-09-30
AR122456A2 (es) 2022-09-14

Similar Documents

Publication Publication Date Title
AR085683A1 (es) Compuestos de piridona y aza-piridona y metodos de uso
AR088061A1 (es) Compuestos de pirazol-4-il-heterociclil-carboxamida y metodos de uso
AR120338A1 (es) Piridazinonas como inhibidores de parp7
AR088643A1 (es) Compuestos de 8-fluoroftalazin-1(2h)-ona
AR121016A2 (es) Sales de fenotiazindiaminio y su uso
AR110400A1 (es) Compuestos de amino-triazolopiridina y su uso en el tratamiento del cáncer
AR089671A1 (es) 1,4-dihidropirimidinas 4,4-disustituidas y su uso como medicamentos para el tratamiento de la hepatitis b
AR106963A2 (es) Compuestos de isoindolina y composiciones farmacéuticas de los mismos
AR094197A1 (es) Compuestos del tipo de las carbamilpiridonas policiclicas y su uso farmaceutico
AR081058A1 (es) Derivados de arilmetoxi isoindolina, composiciones que los comprenden y su uso en el tratamiento del cancer.
AR081859A1 (es) Pirimidinas 2,4,6-trisustituidas, composiciones farmaceuticas que las comprenden y su uso en el tratamiento de tumores sensibles a la inhibicion de la cinasa atr
NI201500032A (es) Métodos para el tratamiento de cáncer de mamas localmente avanzado
EA201591781A1 (ru) Химические соединения
AR092869A1 (es) Alcoxipirazoles como activadores de guanilato ciclasa soluble
PE20170664A1 (es) Agonistas del receptor de apelina(apj) y usos de los mismos
AR105575A1 (es) COMPUESTOS DE QUINOLINA COMO MODULADORES DE TNFa
AR094537A1 (es) COMPUESTOS DE PIRIDILO SUSTITUIDOS CON ALQUILAMIDA ÚTILES COMO MODULADORES DE LAS RESPUESTAS DE IL-12, IL-23 Y/O IFNa
AR091156A1 (es) Nucleosidos de espirooxetano de uracilo
AR089768A1 (es) Compuestos terapeuticamente activos y sus metodos de uso
AR093840A1 (es) Derivados de bencimidazol como antagonistas de ep4
AR092670A1 (es) Derivados de quinazolinona
AR106865A1 (es) Piridinas sustituidas y métodos de uso
CY1122313T1 (el) Ορβεπιταντη για την αγωγη του χρονιου κνησμου
AR118084A1 (es) Inhibidores de enzimas
AR093143A1 (es) Compuestos de 2-aminopiridina