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AR087591A1 - Derivados de ciclohexil azetidina como inhibidores de jak - Google Patents

Derivados de ciclohexil azetidina como inhibidores de jak

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Publication number
AR087591A1
AR087591A1 ARP120103038A ARP120103038A AR087591A1 AR 087591 A1 AR087591 A1 AR 087591A1 AR P120103038 A ARP120103038 A AR P120103038A AR P120103038 A ARP120103038 A AR P120103038A AR 087591 A1 AR087591 A1 AR 087591A1
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alkyl
independently selected
membered monocyclic
optionally substituted
groups
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Incyte Corp
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
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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]
    • A—HUMAN NECESSITIES
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
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    • A—HUMAN NECESSITIES
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
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  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
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  • Pulmonology (AREA)
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  • Transplantation (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Composiciones farmacéuticas que los contienen, que modulan la actividad de Janus Quinasa (JAK)y son útiles en el tratamiento de enfermedades relacionadas con la actividad de JAK, incluyendo por ejemplo, trastornos inflamatorios, trastornos autoinmunes, cáncer, y otras enfermedades. Reivindicación 1: Un compuesto de fórmula (1) o una sal aceptable para uso farmacéutico del mismo, en donde: X es CR¹ o N; Y es CR² o N; W es CR³ o N; Z es CR⁴ o N; V es CR⁵ o N; en donde el anillo aromático de 6 miembros formado por átomo de carbono, X, Y, W, Z, y V tiene 0, 1, ó 2 miembros de anillo de nitrógeno; R¹, R², R³, R⁴, y R⁵ cada uno se selecciona independientemente de H, halo, CN, NO₂, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, Cy, -alquileno C₁₋₃-Cy, ORᵃ, NRᵉRᶠ, SRᵇ, S(=O)₂Rᵇ, S(=O)₂NRᵉRᶠ, C(=O)Rᵇ, C(=O)ORᵃ, C(=O)NRᵉRᶠ, OC(=O)Rᵇ, OC(=O)NRᵉRᶠ, NRᶜC(=O)Rᵈ, NRᶜC(=O)ORᵈ, NRᶜS(=O)₂Rᵈ, NRᶜS(=O)₂NRᵉRᶠ; y CRᵒRᵖORᵃ¹, y CRᵒRᵖNRᵉ¹Rᶠ¹; en donde dicho alquilo C₁₋₆ está opcionalmente sustituido por 1, 2, ó 3 grupos Rˣ independientemente seleccionados; R⁶ es F, metilo, -OH, o -OCH₃; cada Cy se selecciona independientemente de cicloalquilo monocíclico de 3 - 6 miembros, heterocicloalquilo monocíclico de 4 - 6 miembros, fenilo, y heteroarilo monocíclico de 5 - 6 miembros, que está cada uno opcionalmente sustituido por 1, 2, ó 3 grupos Rᵍ independientemente seleccionados; cada Rᵃ, Rᶜ, Rᵈ, Rᵉ, y Rᶠ se selecciona independientemente de H, alquilo C₁₋₆, haloalquilo C₁₋₆, Cy¹, y -alquileno C₁₋₃-Cy¹; en donde dicho alquilo C₁₋₆ está opcionalmente sustituido con 1, 2, ó 3 grupos Rʰ independientemente seleccionados; o cada Rᵉ y Rᶠ, junto con el átomo de nitrógeno al que están unidos, forman un anillo heterocicloalquilo monocíclico de 4 - 6 miembros; que está opcionalmente sustituido con 1, 2, ó 3 grupos Rᵍ independientemente seleccionados; cada Rᵇ se selecciona independientemente de alquilo C₁₋₆, haloalquilo C₁₋₆, Cy¹, y -alquileno C₁₋₃-Cy¹; en donde dicho alquilo C₁₋₆ está opcionalmente sustituido con 1, 2, ó 3 grupos Rʰ independientemente seleccionados; Rᵒ y Rᵖ, tomados junto con el átomo de carbono al que están unidos, forman un anillo cicloalquilo monocíclico de 3 - 4 miembros; cada Cy¹ se selecciona independientemente de cicloalquilo monocíclico de 3 - 6 miembros, heterocicloalquilo monocíclico de 4 - 6 miembros, fenilo, y heteroarilo monocíclico de 5 - 6 miembros, que está cada uno opcionalmente sustituido por 1, 2, ó 3 grupos Rᵍ independientemente seleccionados; cada Rᵍ se selecciona independientemente de halo, CN, hidroxi, alquilo C₁₋₄, haloalquilo C₁₋₄, alcoxi C₁₋₄, haloalcoxi C₁₋₄, hidroxil-alquilo C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, ciano-alquilo C₁₋₄, amino, alquilamino C₁₋₄, di-alquilamino C₁₋₄, carbamilo, alquilcarbamilo C₁₋₄, di(alquil C₁₋₄)carbamilo, alquilcarbonilo C₁₋₄, alcoxicarbonilo C₁₋₄, alquilcarboniloxi C₁₋₄, alquilsulfonilo C₁₋₄, alquilcarbonilamino C₁₋₄, alquilsulfonilamino C₁₋₄, aminosulfonilo, alquilaminosulfonilo C₁₋₄, di-alquilaminosulfonilo C₁₋₄, aminosulfonilamino, alquilaminosulfonilamino C₁₋₄, y di-alquilaminosulfonilamino C₁₋₄; cada Rʰ se selecciona independientemente de halo, CN, hidroxi, alcoxi C₁₋₄, haloalcoxi C₁₋₄, hidroxil-alquilo C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, ciano-alquilo C₁₋₄, amino, alquilamino C₁₋₄, di-alquilamino C₁₋₄, carbamilo, alquilcarbamilo C₁₋₄, di(alquil C₁₋₄)carbamilo, alquilcarbonilo C₁₋₄, alcoxicarbonilo C₁₋₄, alquilcarboniloxi C₁₋₄, alquilcarbonilamino C₁₋₄, alquilsulfonilamino C₁₋₄, aminosulfonilo, alquilaminosulfonilo C₁₋₄, di-alquilaminosulfonilo C₁₋₄, aminosulfonilamino, alquilaminosulfonilamino C₁₋₄, y di-alquilaminosulfonilamino C₁₋₄; cada grupo Rˣ se selecciona independientemente de halo, CN, NO₂, ORᵃ¹, NRᵉ¹Rᶠ¹, SRᵇ¹, S(=O)₂NRᵇ¹, S(=O)₂NRᵉ¹Rᶠ¹, C(=O)Rᵈ¹, C(=O)ORᵃ¹, C(=O)NRᵉ¹Rᶠ¹, OC(=O)Rᵇ¹, OC(=O)NRᵉ¹Rᶠ¹, NRᶜ¹C(=O)Rᵈ¹, NRᶜ¹C(=O)ORᵈ¹, NRᶜ¹S(=O)₂Rᵈ¹, NRᶜ¹S(=O)₂NRᵉ¹Rᶠ¹; cada Rᵃ¹, Rᶜ¹, Rᵈ¹, Rᵉ¹, y Rᶠ¹ se selecciona independientemente de H, alquilo C₁₋₆, haloalquilo C₁₋₆, Cy², y -alquileno C₁₋₃-Cy²; en donde dicho alquilo C₁₋₆ está opcionalmente sustituido por 1, 2, ó 3 grupos Rᵏ seleccionados independientemente; o cada Rᵉ¹ y Rᶠ¹, junto con el átomo de nitrógeno al que están unidos, forma un anillo heterocicloalquilo monocíclico de 4 - 6 miembros; que está opcionalmente sustituido con 1, 2, ó 3 grupos Rᵐ seleccionados independientemente; cada Rᵇ¹ se selecciona independientemente de alquilo C₁₋₆, haloalquilo C₁₋₆, Cy², y -alquileno C₁₋₃-Cy²; en donde dicho alquilo C₁₋₆ está opcionalmente sustituido por 1, 2, ó 3 grupos Rᵏ seleccionados independientemente; cada Cy² se selecciona independientemente de cicloalquilo monocíclico de 3 - 6 miembros, heterocicloalquilo monocíclico de 4 - 6 miembros, fenilo, y heteroarilo monocíclico de 5 - 6 miembros, que está cada uno opcionalmente sustituido por 1, 2, ó 3 grupos Rᵐ seleccionados independientemente; cada Rᵏ se selecciona independientemente de halo, CN, hidroxi, alcoxi C₁₋₄, haloalcoxi C₁₋₄, hidroxil-alquilo C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, ciano-alquilo C₁₋₄, amino, alquilamino C₁₋₄, di-alquilamino C₁₋₄, carbamilo, alquilcarbamilo C₁₋₄, di(alquil C₁₋₄)carbamilo, alquilcarbonilo C₁₋₄, alcoxicarbonilo C₁₋₄, alquilcarboniloxi C₁₋₄, alquilcarbonilamino C₁₋₄, alquilsulfonilo C₁₋₄, alquilsulfonilamino C₁₋₄, aminosulfonilo, alquilaminosulfonilo C₁₋₄, di-alquilaminosulfonilo C₁₋₄, aminosulfonilamino, alquilaminosulfonilamino C₁₋₄, y di-alquilaminosulfonilamino C₁₋₄; cada Rᵐ se selecciona independientemente de halo, CN, hidroxi, alquilo C₁₋₄, haloalquilo C₁₋₄, alcoxi C₁₋₄, haloalcoxi C₁₋₄, hidroxil-alquilo C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, ciano-alquilo C₁₋₄, amino, alquilamino C₁₋₄, di-alquilamino C₁₋₄, carbamilo, alquilcarbamilo C₁₋₄, di(alquil C₁₋₄)carbamilo, alquilcarbonilo C₁₋₄, alcoxicarbonilo C₁₋₄, alquilcarboniloxi C₁₋₄, alquilsulfonilo C₁₋₄, alquilcarbonilamino C₁₋₄, alquilsulfonilamino C₁₋₄, aminosulfonilo, alquilaminosulfonilo C₁₋₄, di-alquilaminosulfonilo C₁₋₄, aminosulfonilamino, alquilaminosulfonilamino C₁₋₄, y di-alquilaminosulfonilamino C₁₋₄; y n es 0, 1, ó 2.
ARP120103038A 2011-08-18 2012-08-17 Derivados de ciclohexil azetidina como inhibidores de jak AR087591A1 (es)

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US201161525081P 2011-08-18 2011-08-18
US201261674694P 2012-07-23 2012-07-23

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TW (1) TW201313721A (es)
WO (1) WO2013026025A1 (es)

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