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AR050253A1 - Compuesto derivado de indazol carboxamida, composicion que lo comprende y su uso para la preparacion de un medicamento - Google Patents

Compuesto derivado de indazol carboxamida, composicion que lo comprende y su uso para la preparacion de un medicamento

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Publication number
AR050253A1
AR050253A1 ARP050102576A ARP050102576A AR050253A1 AR 050253 A1 AR050253 A1 AR 050253A1 AR P050102576 A ARP050102576 A AR P050102576A AR P050102576 A ARP050102576 A AR P050102576A AR 050253 A1 AR050253 A1 AR 050253A1
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AR
Argentina
Prior art keywords
optionally substituted
alkyl
group
cycloalkyl
heteroaryl
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Application number
ARP050102576A
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English (en)
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Smithkline Beecham Corp
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Publication of AR050253A1 publication Critical patent/AR050253A1/es

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    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D401/02—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
    • A—HUMAN NECESSITIES
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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
    • A61K31/435—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
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
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    • A61P11/00—Drugs for disorders of the respiratory system
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    • A61P11/16—Central respiratory analeptics
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P17/16—Emollients or protectives, e.g. against radiation
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P17/18—Antioxidants, e.g. antiradicals
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
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    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • 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]
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    • 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
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • 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
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D413/14—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

Compuesto derivado de indazol carboxamida que tienen la formula (1) en la cual Z es arilo opcionalmente sustituido o heteroarilo opcionalmente sustituido, estando dichos arilo y heteroarilo opcionalmente sustituidos con uno o más sustituyentes seleccionados, de manera independiente, del grupo consistente en : halo, alquilo C1-6 opcionalmente sustituido, haloalquilo C1-6 opcionalmente sustituido, heterocicloalquilo opcionalmetne sustituido, CN, N(Rb)SO2Re, N(Rb)C(O)Ra, C(O)NRaRb, C(O)NRaRb, C(O)NRxRy, SO2NRaRb, SO2NRxRy, ORc, N(Rb)C(O)NRaRb, N(Rb)C(0)NRxRy, N(Rb)C(O)ORd, estando dichos alquilo C1-6 y haloalquilo C1-6 opcionalmente sustituidos con uno o más sustituyentes seleccionados del grupo consistente en: NRaRb, cicloalquilo C3-6, ORc, fenilo y heterocicloalquilo opcionalmente sustituido con uno o dos grupos alquilo C1-6; R1 es H, halo, o -WX; W es un enlace o alquileno C1-6; X es arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, cicloalquilo C4-7 opcionalmente sustituido, cicloalquenilo C5-7 opcionalmente sustituido, N(Rb)SO2Re, N(Rb) C(O)Re, N(Rb)C(O)ORd, N(Rb)C(O)NRaRb, o N(Rb)C(o)NRxRy, estando dichos arilo, heteroarilo, heterocicloalquilo, cicloalquilo C4-7, y cicloalquenilo C5-7 opcionalmente sustituidos con uno o más sustituyentes seleccionados de manera independiente del grupo consistente en: halo, alquilo C1-6 opcionalmente sustituido, haloalquilo C1-6 opcionalmente sustituido, ORc, C(O)Rg, C(O)ORf, N(Rb)SO2Re, N(Rb)C(O)Ra, C(O)NRaRb, SO2NRaRb, SO2Re, y heterocicloalquilo, estando dichos alquilo C1-6 y haloalquilo C1-6 opcionalmente sustituidos con un grupo fenilo; cada Ra está seleccionado, de manera independiente, del grupo consistente en H, alquilo, C1-3 opcionalmente sustituido, fenilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, cicloalquilo C3-7 opcionalmente sustituido, y heterocicloalquilo opcionalemtne sustituido, estando dicho alquilo C1-3 opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo consistente en: halo, ORc, haloalquilo C1-6, fenilo y heteroarilo; y estando dichos fenilo, heteroarilo, cicloalquilo C3-7, y heterocicloalquilo opcionalmente sustituidos con uno o más sustituyentes seleccionados del grupo consistente en: halo, ORc, alquilo C1-6, y haloalquilo C1-6 cada Rb está seleccionado, de manera indendiente, del grupo consiste en: H y alquilo C1-3 opcionalemente sustituido, estando dicho alquilo C1-3 opcionalmente sustituido con uno o más grupos ORc; cada Rc está seleccionado, de manera independiente, del grupo consistente en: H, alquilo C1-6 opcionalmente sustituido, cicloalquilo C3-7 opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, y arilo opcionalmente sustituido, y arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, estando dichos alquilo C1-6 y haloalquilo C1-6 opcionalmente sustituidos con uno o más sustituyentes seleccionados del grupo consistente en: cicloalquilo C3-6, fenilo, heterocicloalquilo, y heteroarilo; y estando dichos arilo y heteroarilo opcionalmente sustituidos con uno o más sustituyentes seleccionados del grupo consistente en: halo, alquilo C1-3, haloalquilo C1-3 y OH; y estando dichos cicloalquilo C3-7 y heterocicloalquilo opcionalmente sustituidos con uno o más grupos alquilo C1-3; cara Rd es alquilo C1-3 opcionalmente sustituido de manera independiente, estando dicho alquilo C1-3 opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo consistente en: cicloalquilo C3-6, fenilo opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo consistente en: halo, alquilo C1-6, y cicloalquilo C3-6; y heteroarilo opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo consistente en: halo, alquilo C1-6, y cicloalquilo C3-6; cada Re está seleccionado, de manera independiente, del grupo consistente en: alquilo C1-6 opcionalmente sustituido, fenilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, cicloalquilo C5-7 opcionalmente sustituido, y heterocicloalquilo opcionalmente sustituido, estando dicho alquilo C1-6 opcionalmente sustituido con un sustituyente seleccionado del grupo consistente en: ORc, trifluorometilo, fenilo, heteroarilo, heterocicloalquilo opcionalmente sustituido con ORc o con heterocicloalquilo, NRaRb; estando dichos fenilo y heteroarilo opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo consistente en: halo, CN, alquilo C1-6, N(Rb)C(O)Ra, y ORh; y estando dichos cicloalquilo C5-7 y heterocicloalquilo opcionalmente sustituidos con uno o más sustituyentes seleccionados del grupo consistente en: halo, alquilo C1-6 opcionalmente sustituido con ORc, y cicloalquilo C3-6, cada Rf está seleccionado, de manera independiente, del grupo consistente en H y alquilo C1-4 opcionalmente sustituido, pudiendo estar dicho alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo consistente en: cicloalquilo C3-6; fenilo opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo consistente en: halo, alquilo C1-6, y heteroarilo opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo consistente en: halo, alquilo C1-6, y cicloalquilo C3-6; cada Rg está seleccionado, de manera independiente, del grupo consistente en: alquilo C1-3 opcionalmente sustituido, fenilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, cicloalquilo C3-7 opcionalmente sustituido y heterocicloalquilo opcionalmente sustituido, estando dicho alquilo C1-3 opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo consistente en: halo y haloalquilo C1-6; y estando dichos fenilo, heteroarilo, cicloalquilo C3-7, y heterocicloalquilo opcionalmente sustituidos con uno o más fenilo, heteroarilo, cicloalquilo C3-7, y heterocicloalquilo opcionalmente sustituidos con uno o más sustituyentes seleccionados del grupo consistente en: Halo, alquilo C1-6, y halolaquilo C1-6, cada Rh está seleccionado, de manera independiente, del grupo consistente en: H, alquilo C1-6, y haloalquilo C1-6; y Rx y Ry, tomados junto con el átomo de nitrogeno al cual están unidos, forman un anillo que tiene de 5 a 7 átomos miembros, conteniendo opcionalmente dicho anillo un heteroátomo adicional como átomo miembro siendo dicho anillo saturado o insaturado, pero no aromático, y estando dicho anillo opcionalmente sustituido con uno o dos sustituyentes alquilo C1-3; o una de sus sales faramcéuticamente aceptables. Composicion que lo comprende y su uso para la preparacion de un medicamento para tratar trastornos en los que interviene una actividad inadecuada de IKK2 ( denominado también IKKbeta), tales como la artritis reumatoide, el asma y la enfermedad pulmonar obstructiva cronica (EPOC, siglas inglesas COPD), transtornos inflamatorios, enfermedad de Alzheimer, SIDA, infarto, cáncer o caquexia.
ARP050102576A 2004-06-24 2005-06-22 Compuesto derivado de indazol carboxamida, composicion que lo comprende y su uso para la preparacion de un medicamento AR050253A1 (es)

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AR (1) AR050253A1 (es)
AT (1) ATE493396T1 (es)
AU (1) AU2005258332A1 (es)
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CA (1) CA2571712A1 (es)
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ATE493396T1 (de) 2011-01-15
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