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AR090633A1 - Compuestos de indol e indazol que activan la ampk - Google Patents

Compuestos de indol e indazol que activan la ampk

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Publication number
AR090633A1
AR090633A1 ARP130101147A ARP130101147A AR090633A1 AR 090633 A1 AR090633 A1 AR 090633A1 AR P130101147 A ARP130101147 A AR P130101147A AR P130101147 A ARP130101147 A AR P130101147A AR 090633 A1 AR090633 A1 AR 090633A1
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AR
Argentina
Prior art keywords
alkyl
carbonyl
alkoxy
nrmrn
independently
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ARP130101147A
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English (en)
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Pfizer
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Publication of AR090633A1 publication Critical patent/AR090633A1/es

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    • 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
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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
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61K31/403—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 condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • 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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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/14—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 three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • 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
    • C07D403/10—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 carbon chain containing aromatic rings
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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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
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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
    • C07D405/10—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 carbon chain containing aromatic rings
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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
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    • C07D405/14—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 three or more hetero rings
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    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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Abstract

La presente se refiere a compuestos de indol e indazol que activan proteína quinasa activada por 5 adenosina monofosfato (AMPK). También comprende composiciones farmacéuticas que contienen estos compuestos y métodos para tratar o prevenir enfermedades, condiciones o trastornos mejorados por activación de AMPK, como enfermedad renal crónica, nefropatìa diabética, lesión renal, diabetes tipo II, dislipidemia u obesidad. Reivindicación 1: Un compuesto de la fórmula (1) o una de sus sales farmacéuticamente aceptables, en donde X es N o CH; R¹ es -C(O)ORA, -C(O)NRBRC, -S(O₂)ORA, -S(O₂)NHC(O)RD, 5-oxo-4,5-dihidro-1,2,4-oxadiazol-3-ilo o 1H-tetrazol-5-ilo; RA es H o alquilo C₁₋₆; RB y RC son, de modo independiente, H, alquilo C₁₋₆ o -S(O₂)RD; RD es alquilo C₁₋₆, -CF₃ o fenilo, en donde el fenilo está opcionalmente sustituido con 1, 2, 3, 4 ó 5 sustituyentes que son, de modo independiente, alcoxi C₁₋₆, alquilo C₁₋₆, ciano, halógeno, haloalcoxi C₁₋₆, haloalquilo C₁₋₆, hidroxi, mercapto, nitro o NRERF; RE y RF son, de modo independiente, H o alquilo C₁₋₆; R², R³ y R⁴ son, de modo independiente, H, alcoxi C₁₋₆, alquilo C₁₋₆, alquil C₁₋₆-tio, carboxi, ciano, halógeno, haloalcoxi C₁₋₆, haloalquilo C₁₋₆, hidroxi, hidroxialquilo C₁₋₈, mercapto, nitro, -NRGRH o (NRGRH)carbonilo; RG y RH son, de modo independiente, H, alquilo C₁₋₆ o alquil C₁₋₆-carbonilo; R⁵ es H o alquilo C₁₋₆; L es un enlace, O, S, NRA, alquileno C₁₋₆, alquenileno C₂₋₆ o alquinileno C₂₋₆; A es fenilo, 2,3-dihidrobenzo[b][1,4]dioxinilo, 2,3-dihidrobenzofuranilo, 2,3-dihidro-1H-indenilo, imidazolilo, pirazinilo, pirazolilo, piridinilo, pirimidinilo o tiazolilo, en donde cada uno está opcionalmente sustituido con 1, 2, 3, 4 ó 5 sustituyentes que son, de modo independiente, alcoxi C₁₋₆, alcoxi C₁₋₆-alcoxi C₁₋₆, alcoxi C₁₋₆-alquilo C₁₋₆, alcoxi C₁₋₆-carbonilo, alquilo C₁₋₆, alquil C₁₋₆-carbonilo, alquil C₁₋₆-tio, arilo, arilalcoxi C₁₋₆, arilalquilo C₁₋₆, arilcarbonilo, ariloxi, carboxi, carboxialcoxi C₁₋₆, carboxialquilo C₁₋₆, ciano, cicloalquilo C₃₋₈, cicloalquil C₃₋₈-alcoxi C₁₋₆, cicloalquil C₃₋₈-alquilo C₁₋₆, cicloalquil C₃₋₈-carbonilo, cicloalquil C₃₋₈-oxi, halógeno, haloalcoxi C₁₋₆, haloalquilo C₁₋₆, heteroarilo, heteroarilalcoxi C₁₋₆, heteroarilalquilo C₁₋₆, heteroarilcarbonilo, heteroariloxi, heterociclo C₃₋₇, heterociclo C₃₋₇-alcoxi C₁₋₆, heterociclo C₃₋₇-alquilo C₁₋₆, heterociclo C₃₋₇-carbonilo, heterociclo C₃₋₇-carbonilalquilo C₁₋₆, heterociclo C₃₋₇-oxi, hidroxi, hidroxialcoxi C₁₋₆, hidroxialquilo C₁₋₆, mercapto, nitro, -NRJRK, (NRJRK)carbonilo, -NRMRN, -NRMRN-alcoxi C₁₋₆, (NRMRN)carbonilo, (NRMRN)carbonilalquilo C₁₋₆ o (NRMRN)carbonilalcoxi C₁₋₆; en donde el arilo, arilalcoxi C₁₋₆, arilalquilo C₁₋₆, arilcarbonilo y ariloxi están opcionalmente sustituidos con 1, 2, 3, 4 ó 5 sustituyentes que son, de modo independiente, alcoxi C₁₋₆, alcoxi C₁₋₆-carbonilo, alquilo C₁₋₆, alquil C₁₋₆-carbonilo, alquil C₁₋₆-tio, carboxi, ciano, halógeno, haloalcoxi C₁₋₆, haloalquilo C₁₋₆, hidroxi, hidroxialquilo C₁₋₆, mercapto, nitro, -NRMRN o (NRMRN)carbonilo; en donde el haloalquilo C₁₋₆ está opcionalmente sustituido con 1 ó 2 grupos hidroxi; en donde el cicloalquilo C₃₋₈, cicloalquil C₃₋₈-alcoxi C₁₋₆, cicloalquil C₃₋₈-alquilo C₁₋₆, cicloalquil C₃₋₈-carbonilo y cicloalquil C₃₋₈-oxi están opcionalmente sustituidos con 1, 2 ó 3 sustituyentes que son, de modo independiente, alcoxi C₁₋₆, alcoxi C₁₋₆-carbonilo, alquilo C₁₋₆, alquil C₁₋₆-carbonilo, alquil C₁₋₆-tio, carboxi, ciano, halógeno, haloalcoxi C₁₋₆, haloalquilo C₁₋₆, hidroxi, hidroxialquilo C₁₋₆, mercapto, nitro, -NRMRN o (NRMRN)carbonilo; en donde el heteroarilo, heteroarilalcoxi C₁₋₆, heteroarilalquilo C₁₋₆, heteroarilcarbonilo y heteroariloxi están opcionalmente sustituidos con 1, 2 ó 3 sustituyentes que son, de modo independiente, alcoxi C₁₋₆, alcoxi C₁₋₆- carbonilo, alquilo C₁₋₆, alquil C₁₋₆-carbonilo, alquil C₁₋₆-tio, carboxi, ciano, halógeno, haloalcoxi C₁₋₆, haloalquilo C₁₋₆, hidroxi, hidroxialquilo C₁₋₆, mercapto, nitro, -NRMRN o (NRMRN)carbonilo; y en donde el heterociclo C₃₋₇, heterociclo C₃₋₇-alcoxi C₁₋₆, heterociclo C₃₋₇-alquilo C₁₋₆, heterociclo C₃₋₇-carbonilo, heterociclo C₃₋₇-carbonilalquilo C₁₋₆ y heterociclo C₃₋₇-oxi, están opcionalmente sustituidos con 1, 2 ó 3 sustituyentes que son, de modo independiente, alcoxi C₁₋₆, alcoxi C₁₋₆-carbonilo, alcoxi C₁₋₆-sulfonilo, alquilo C₁₋₆, alquil C₁₋₆-carbonilo, alquil C₁₋₆-sulfonilo, alquil C₁₋₆-tio, carboxi, ciano, halógeno, haloalcoxi C₁₋₆, haloalquilo C₁₋₆, hidroxi, hidroxialquilo C₁₋₆, mercapto, nitro, -NRMRN, (NRMRN)carbonilo u oxo; RJ y RK son, de modo independiente, H o alquilo C₁₋₆; y RM y RN son, de modo independiente, H, alquilo C₁₋₆ o alquil C₁₋₆-carbonilo; o RM y RN junto con el nitrógeno al que están unidos forman un anillo de 3 a 8 miembros; siempre que la fórmula (1) no comprenda 5-(4-bromofenil)-1H-indol-3-carboxamida; 5-(2,6-dihidroxi-[1,1-bifenil]-4-il)-1H-indol-3-carboxamida; y 5-(2,6-dimetoxi-[1,1]bifenil]-4-il)-1H-indol-3-carboxamida.
ARP130101147A 2012-04-10 2013-04-09 Compuestos de indol e indazol que activan la ampk AR090633A1 (es)

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