AR090037A1 - Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio - Google Patents

Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio

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Publication number
AR090037A1
AR090037A1 ARP120104296A ARP120104296A AR090037A1 AR 090037 A1 AR090037 A1 AR 090037A1 AR P120104296 A ARP120104296 A AR P120104296A AR P120104296 A ARP120104296 A AR P120104296A AR 090037 A1 AR090037 A1 AR 090037A1
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AR
Argentina
Prior art keywords
optionally substituted
alkyl
thieno
pyrimidin
piperidin
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ARP120104296A
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English (en)
Inventor
Chan Fiona
Edward John Derek
D Edwards Simon
Brown Lindsay
Hartzoulakis Basil
Madge David
Blunt Richard
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Xention Ltd
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Publication date
Priority claimed from GBGB1119703.5A external-priority patent/GB201119703D0/en
Priority claimed from GBGB1214250.1A external-priority patent/GB201214250D0/en
Application filed by Xention Ltd filed Critical Xention Ltd
Publication of AR090037A1 publication Critical patent/AR090037A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1) o un derivado farmacéuticamente aceptable del mismo, donde: A es O ó S; X es N o CR³II; V es N o CR³III; Z es N o CR³IV; donde uno o dos de V, X y Z son N; R¹ se selecciona entre alquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, arilo opcionalmente sustituido, y heteroarilo opcionalmente sustituido; R² se selecciona entre H, halo, -CN, trifluorometilo, alquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, -NR⁴R⁵, -NR⁶C(O)R⁷, -NR⁶S(O)₂R⁷, -S(O)₂NR⁴R⁵, -CONR⁴R⁵, -CO₂R⁷, oxazolinilo opcionalmente sustituido, -SR¹⁴, -S(O)R¹⁴ y -S(O)₂R¹⁴; R³I se selecciona entre H, halo, -CN, trifluorometilo, alquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, heterocicloalcoxi opcionalmente sustituido, -NR⁶C(O)R⁷, -NR⁶S(O)₂R⁷, -S(O)₂NR⁴R⁵, -CONR⁴R⁵, -CO₂R⁷, -NR⁸R⁹, -CºC-J, cicloalquil-J opcionalmente sustituido y -(NRᵃRᵇ)-J; cada uno de R³II, R³III, y R³IV se selecciona en forma independiente entre H, halo, -CN, trifluorometilo, alquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, heterocicloalcoxi opcionalmente sustituido, heterocicloalquilalquilo opcionalmente sustituido, -NR⁶C(O)R⁷, -NR⁶S(O)₂R⁷, -S(O)₂NR⁴R⁵, -CONR⁴R⁵, -alquilen-CONR⁴R⁵ opcionalmente sustituido, -CO₂R⁷, -NR¹⁰R¹¹, -CºC-J, cicloalquil-J opcionalmente sustituido y -(NRᶜRᵈ)-J, con la condición de que R³ⁱ es -CºC-J, cicloalquil-J opcionalmente sustituido o -(NRᵃRᵇ)-J, y/o al menos uno de R³II, R³III, y R³IV está presente como -CºC-J, cicloalquil-J opcionalmente sustituido o -(NRᶜRᵈ)-J; donde Rᵃ y Rᵇ se unen para formar un anillo heterocicloalquilo de entre 4 y 7 miembros opcionalmente sustituido, que está unido opcionalmente formando un puente, alquileno C₁₋₂ opcionalmente sustituido, -NR⁶-, -O-, o -S(O)ᶻ-, donde el anillo heterocicloalquilo opcionalmente sustituido que opcionalmente forma un puente se selecciona entre el grupo que consiste en azetidinilo, pirrolidinilo, piperidinilo, morfolinilo, tetrahidro-1,3-oxazinilo, hexahidropirimidinilo, 1,4-tiazanilo, azepanilo, 1,4-oxaazepanilo, y 1,4-tieazepanilo; donde Rᶜ y Rᵈ se unen para formar un anillo heterocicloalquilo de entre 4 y 7 miembros opcionalmente sustituido, que está unido opcionalmente formando un puente, alquileno C₁₋₂ opcionalmente sustituido, -NR⁶-, -O-, o -S(O)ᶻ-; J se selecciona entre H y -(CR¹²R¹³)q-L-M-W, donde q es 0, 1 ó 2; L es -O- o -N(G)-; y G se selecciona entre hidrógeno, alquilo opcionalmente sustituido y cicloalquilo opcionalmente sustituido; M es -(CR¹²R¹³)ₜ-; t es 0, 1, 2 ó 3; W se selecciona entre el grupo que consiste en alquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, alquenilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido y -NR⁸R⁹, cuando W es cicloalquilo opcionalmente sustituido opcionalmente puede formar un puente con una unión o alquileno C₁₋₂ opcionalmente sustituido, y cuando W es heterocicloalquilo opcionalmente sustituido opcionalmente puede formar un puente con una unión, alquileno C₁₋₂ opcionalmente sustituido, -NR⁶-, -O-, o -S(O)ᶻ-; de manera alternativa, cuando L = -N(G)-, L, G, M y W pueden estar unidos para formar un heterocicloalquilo opcionalmente sustituido, un heterocicloalquenilo opcionalmente sustituido, o un heteroarilo opcionalmente sustituido; z es 0, 1 ó 2; R⁴ y R⁵ se seleccionan en cada instancia en forma independiente entre H, alquilo opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, y cicloalquilo opcionalmente sustituido, o se unen para formar un heterocicloalquilo opcionalmente sustituido; R⁶ y R⁷ se seleccionan en cada instancia en forma independiente entre H y alquilo opcionalmente sustituido, o se unen para formar un heterocicloalquilo opcionalmente sustituido; R⁸ y R⁹ se seleccionan en cada instancia en forma independiente entre alquilo opcionalmente sustituido, arilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, y cicloalquilo opcionalmente sustituido; R¹⁰ y R¹¹ se seleccionan en cada instancia en forma independiente entre H, alquilo opcionalmente sustituido, arilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, y cicloalquilo opcionalmente sustituido; R¹² y R¹³ se seleccionan en cada instancia en forma independiente entre H, hidroxi, y alquilo opcionalmente sustituido, o pueden estar unidos para formar un anillo cicloalquilo opcionalmente sustituido, o pueden formar juntos =O; y R¹⁴ es alquilo opcionalmente sustituido, donde los sustituyentes opcionales se seleccionan en forma independiente entre halo, trihalometilo, trihaloetilo, trihalometoxi, trihaloetoxi, -OH, -NO₂, -CN, -CO₂H, -CO₂-alquilo C₁₋₆, -SO₃H, -SO-alquilo C₁₋₆, -SO₂-alquilo C₁₋₆, -NHSO₂-alquilo C₁₋₆, -N-alquil C₁₋₆SO₂-alquilo C₁₋₆, -SO₂NH₂, -SO₂NH-alquilo C₁₋₆, -SO₂N(alquil C₁₋₆)₂, -NHSO₂NH₂, -NHSO₂NH-alquilo C₁₋₆, -NHSO₂N(alquil C₁₋₆)₂, -N-alquil C₁₋₆SO₂NH₂, -N-alquil C₁₋₆SO₂NH-alquilo C₁₋₆, -N-alquil C₁₋₆SO₂N(alquil C₁₋₆)₂, -C(=O)H, -C(=O)-alquilo C₁₋₆, -NHC(=O)-alquilo C₁₋₆, -N-alquil C₁₋₆C(=O)alquilo C₁₋₆, -alquilen C₁₋₆dioxi, =O, -N(alquil C₁₋₆)₂, -C(=O)NH₂, -C(=O)NH-alquilo C₁₋₆, -C(=O)N(alquil C₁₋₆)₂, -NHC(=O)NH₂, -NHC(=O)NH-alquilo C₁₋₆, -NHC(=O)N(alquil C₁₋₆)₂, -N-alquil C₁₋₆C(=O)NH₂, -N-alquil C₁₋₆C(=O)NH-alquilo C₁₋₆, -N-alquil C₁₋₆C(=O)N(alquil C₁₋₆)₂, -C(=NH)NH₂, -C(=NH)NH-alquilo C₁₋₆, -C(=NH)N(alquil C₁₋₆)₂, -C(=N-alquil C₁₋₆)NH₂, -C(=N-alquil C₁₋₆)NH-alquilo C₁₋₆, -C(=N-alquil C₁₋₆)N(alquil C₁₋₆)₂, -alquilo C₁₋₆, -cicloalquilo C₃₋₆, -heterocicloalquilo C₃₋₆, 2-imidazolidinon-3-ilo, 1-alquil C₁₋₆-2-imidazolidinon-3-ilo, alquil C₁₋₆-heterocicloalquilo C₃₋₆, arilo, haloarilo, alcoxi C₁₋₆arilo, -alquilen C₁₋₆-NHSO₂-alquilo C₁₋₆, -alquilen C₁₋₆-N-alquil C₁₋₆SO₂-alquilo C₁₋₆, -alquilen C₁₋₆-SO₂NH₂, -alquilen C₁₋₆-SO₂NH-alquilo C₁₋₆, -alquilen C₁₋₆-SO₂N(alquil C₁₋₆)₂, -ZᵗH, -Zᵗ-alquilo C₁₋₆, -alquilen C₁₋₆-ZᵗH, -Zᵗ-cicloalquilo C₃₋₆, o -C(=O)NH-alquilen C₁₋₆-ZᵗH donde Zᵗ es en forma independiente O, S, NH o N(alquilo C₁₋₆), donde dicho compuesto no es: 2-bencil-5-metil-4-morfolin-4-il-tieno[2,3-d]pirimidin-6-carbonitrilo, tert-butiléster de ácido [1-(5-fenil-tieno[2,3-d]pirimidin-4-il)piperidin-4-il]-carbámico, tert-butiléster de ácido [1-(6-metil-5-fenil-tieno[2,3-d]pirimidin-4-il)piperidin-4-il]-carbámico, tert-butiléster de ácido {1-[5-(4-bromo-fenil)-tieno[2,3-d]pirimidin-4-il]-piperidin-4-il}-carbámico, tert-butiléster de ácido [1-(5-p-tolil-tieno[2,3-d]pirimidin-4-il)piperidin-4-il]-carbámico, tert-butiléster de ácido [1-(5-metil-tieno[2,3-d]pirimidin-4-il)-piperidin-4-il]-carbámico, 1-(5-fenil-tieno[2,3-d}pirimidin-4-il)-piperidin-4-ilamina, 1-(6-metil-5-fenil-tieno[2,3-d]pirimidin-4-il)-piperidin-4-ilamina, 1-(5-(4-bromo-fenil)-tieno[2,3-d]pirimidin-4-il)-piperidin-4-ilamina, 1-(5-p-tolil-tieno[2,3-d]pirimidin-4-il)-piperidin-4-ilamina, 1-(5-metil-tieno[2,3-d]pirimidin-4-il)-piperidin-4-ilamina, 1-(5-fenil-tieno[2,3-d]pirimidin-4-il)-piperidin-4-ona, 1-[5-(4-bromo-fenil)-tieno[2,3-d]pirimidin-4-il]-piperidin-4-ona, 1-(5-p-tolil-tieno[2,3-d]pirimidin-4-il)-piperidin-4-ona, 1-(6-metil-5-fenil-tieno[2,3-d]pirimidin-4-il)piperidin-4-ona, 2-{1-[5-(4-bromo-fenil)-tieno[2,3-d]pirimidin-4-il]-piperidin-4-ilamino}-ciclohexanol, 2-{1-(5-p-toIil-tieno[2,3-d]pirimidin-4-il)-piperidin-4-ilamino}-ciclohexanol, 2-(1-(6-metil-5-fenil-tieno[2,3-d]pirimidin-4-il)-piperidin-4ilamino}-ciclohexanol, 1-benciloxi-3-[1-(5-fenil-tieno[2,3-d]pirimidin-4-il)-piperidin-4-ilamino]-propan-2-ol, 2-[1-(5-fenil-tieno[2,3-d]pirimidin-4-il)-piperidin-4-ilamino]-ciclohexanol, 5-metoxi-2-{[1-(5-fenil-tieno[2,3-d]pir
ARP120104296A 2011-11-15 2012-11-14 Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio AR090037A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1119703.5A GB201119703D0 (en) 2011-11-15 2011-11-15 Compounds
GBGB1214250.1A GB201214250D0 (en) 2012-08-09 2012-08-09 Compounds

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US (2) US9290511B2 (es)
EP (1) EP2780343A1 (es)
JP (1) JP2014533259A (es)
KR (1) KR20140094603A (es)
CN (1) CN104011054B (es)
AR (1) AR090037A1 (es)
AU (1) AU2012338570A1 (es)
BR (1) BR112014011671A2 (es)
CA (1) CA2855346A1 (es)
IN (1) IN2014MN01183A (es)
MX (1) MX2014005935A (es)
RU (1) RU2014124101A (es)
TW (1) TWI498331B (es)
WO (1) WO2013072694A1 (es)
ZA (1) ZA201403503B (es)

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