AR093308A1 - Derivados triciclicos fusionados de tiofeno como inhibidores de jak - Google Patents

Derivados triciclicos fusionados de tiofeno como inhibidores de jak

Info

Publication number
AR093308A1
AR093308A1 ARP130103980A ARP130103980A AR093308A1 AR 093308 A1 AR093308 A1 AR 093308A1 AR P130103980 A ARP130103980 A AR P130103980A AR P130103980 A ARP130103980 A AR P130103980A AR 093308 A1 AR093308 A1 AR 093308A1
Authority
AR
Argentina
Prior art keywords
nrcrd
nrcc
nrcs
ora
nre
Prior art date
Application number
ARP130103980A
Other languages
English (en)
Original Assignee
Incyte Corp
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=49578588&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR093308(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of AR093308A1 publication Critical patent/AR093308A1/es

Links

Classifications

    • 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
    • C07D495/12—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 three hetero 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
    • A61K31/435—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • 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
    • 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
    • A61P19/02—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
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • 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
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • 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
    • C07D495/12—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 three hetero rings
    • C07D495/14—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Transplantation (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Estos compuestos modulan la actividad de la cinasa Janus (JAK) y son útiles para el tratamiento de enfermedades relacionadas con la actividad de JAK incluyendo, por ejemplo, trastornos inflamatorios, trastornos autoinmunitarios, cáncer y otras enfermedades. Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable de este, donde: el sistema de anillo de la fórmula (2) es aromático; cada ⁻ ⁻ ⁻ se selecciona independientemente de un enlace simple y un enlace doble; Y es N o CR⁴; X¹ se selecciona de CR¹, CR¹R¹ᵃ, C(=O), N, NR¹, O y S; X² se selecciona de CR², C(=O), N, NR² y C(=NR²ᵃ); X³ se selecciona de CR³ y NR³; X⁴ se selecciona de C y N; y X⁵ es C; o X⁴ es C; y X⁵ se selecciona de C y N; siempre que: (i) las selecciones para cada uno de X¹, X², X³, X⁴, X⁵ y ⁻ ⁻ ⁻ mantienen la valencia adecuada; (ii) cuando X¹ es O ó S, X² no es NR² y X²⁻ ⁻ ⁻X³ no es -C(=O)-CR³-; (iii) cuando X¹ es NR¹, X²⁻ ⁻ ⁻X³ no es -NR²-NR³-; (iv) cuando X⁴ es N, X¹⁻ ⁻ ⁻X²⁻ ⁻ ⁻X³ no es =N-NR²-NR³-; y (v) cuando X⁵ es N, X¹⁻ ⁻ ⁻X² no es -NR¹-NR²- y X¹⁻ ⁻ ⁻X²⁻ ⁻ ⁻X³ no es -CR¹R¹ᵃ-NR²-CR³=; R¹ se selecciona de H, halo, CN, NH₂, alquilo C₁₋₃, alcoxi C₁₋₃ y haloalquilo C₁₋₃; R¹ᵃ se selecciona de H, halo, CN, NH₂, alquilo C₁₋₃ y haloalquilo C₁₋₃; R²ᵃ se selecciona de CN, OH, OCH₃ y NO₂; R² se selecciona de H, halo, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆, alquilo C₁₋₆-S-, CN, C(=O)Rᵇ, C(=O)NRᶜRᵈ, C(=O)ORᵃ, OC(=O)Rᵇ, OC(=O)NRᶜRᵈ, NRᶜRᵈ, NRᶜC(=O)Rᵇ, NRᶜC(=O)ORᵃ, NRᶜC(=O)NRᶜRᵈ, C(=NRᵉ)Rᵇ, C(=NRᵉ)NRᶜRᵈ, NRᶜC(=NRᵉ)NRᶜRᵈ, NRᶜS(=O)Rᵇ, NRᶜS(=O)₂Rᵇ, NRᶜS(=O)₂NRᶜRᵈ, S(=O)Rᵇ, S(=O)NRᶜRᵈ, S(=O)₂Rᵇ y S(=O)₂NRᶜRᵈ; donde cada uno de dichos alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, alcoxi C₁₋₆ y alquilo C₁₋₆-S- está opcionalmente sustituido con 1, 2 ó 3 sustituyentes que se seleccionan independientemente de Cy², halo, CN, NO₂, ORᵃ, SRᵃ, C(=O)Rᵇ, C(=O)NRᶜRᵈ, C(=O)ORᵃ, OC(=O)Rᵇ, OC(=O)NRᶜRᵈ, C(=NRᵉ)NRᶜRᵈ, NRᶜC(=NRᵉ)NRᶜRᵈ, NRᶜRᵈ, NRᶜC(=O)Rᵇ, NRᶜC(=O)ORᵃ, NRᶜC(=O)NRᶜRᵈ, NRᶜS(=O)Rᵇ, NRᶜS(=O)₂Rᵇ, NRᶜS(=O)₂NRᶜRᵈ, S(=O)Rᵇ, S(=O)NRᶜRᵈ, S(=O)₂Rᵇ y S(=O)₂NRᶜRᵈ; de manera alternativa, R² se selecciona de arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros y heterocicloalquilo de 3 - 10 miembros, donde cada uno de dichos arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros y heterocicloalquilo de 3 - 10 miembros está opcionalmente sustituido con 1, 2, 3, 4 ó 5 sustituyentes que se seleccionan independientemente de halo, R²¹, Cy², CN, NO₂, ORᵃ, SRᵃ, C(=O)Rᵇ, C(=O)NRᶜRᵈ, C(=O)ORᵃ, OC(=O)Rᵇ, OC(=O)NRᶜRᵈ, C(=NRᵉ)NRᶜRᵈ, NRᶜC(=NRᵉ)NRᶜRᵈ, NRᶜRᵈ, NRᶜC(=O)Rᵇ, NRᶜC(=O)ORᵃ, NRᶜC(=O)NRᶜRᵈ, NRᶜS(=O)Rᵇ, NRᶜS(=O)₂Rᵇ, NRᶜS(=O)₂NRᶜRᵈ, S(=O)Rᵇ, S(=O)NRᶜRᵈ, S(=O)₂Rᵇ y S(=O)₂NRᶜRᵈ; con la condición de que cuando X¹⁻ ⁻ ⁻X²⁻ ⁻ ⁻X³ es -N=CR²-NR³-, X⁴ es C y X⁵ es C; y Cy⁴ es heterocicloalquileno saturado sustituido o no sustituido con 3 - 10 miembros que tienen uno o más átomos de nitrógeno o Cy⁴A es heterocicloalquileno saturado sustituido o no sustituido de 3 - 10 miembros que tiene uno o más átomos de nitrógeno, R² se selecciona de H, halo, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆, alquilo C₁₋₆-S-, CN, C(=O)Rᵇ, C(=O)NRᶜRᵈ, C(=O)ORᵃ, OC(=O)Rᵇ, OC(=O)NRᶜRᵈ, NRᶜRᵈ, NRᶜC(=O)Rᵇ, NRᶜC(=O)ORᵃ, NRᶜC(=O)NRᶜRᵈ, C(=NRᵉ)Rᵇ, C(=NRᵉ)NRᶜRᵈ, NRᶜC(=NRᵉ)NRᶜRᵈ, NRᶜS(=O)Rᵇ, NRᶜS(=O)₂Rᵇ, NRᶜS(=O)₂NRᶜRᵈ, S(=O)Rᵇ, S(=O)NRᶜRᵈ, S(=O)₂Rᵇ y S(=O)₂NRᶜRᵈ; donde cada uno de dichos alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, alcoxi C₁₋₆ y alquilo C₁₋₆-S- está opcionalmente sustituido con 1, 2 ó 3 sustituyentes que se seleccionan independientemente de Cy², halo, CN, NO₂, ORᵃ, SRᵃ, C(=O)Rᵇ, C(=O)NRᶜRᵈ, C(=O)ORᵃ, OC(=O)Rᵇ, OC(=O)NRᶜRᵈ, C(=NRᵉ)NRᶜRᵈ, NRᶜC(=NRᵉ)NRᶜRᵈ, NRᶜRᵈ, NRᶜC(=O)Rᵇ, NRᶜC(=O)ORᵃ, NRᶜC(=O)NRᶜRᵈ, NRᶜS(=O)Rᵇ, NRᶜS(=O)₂Rᵇ, NRᶜS(=O)₂NRᶜRᵈ, S(=O)Rᵇ, S(=O)NRᶜRᵈ, S(=O)₂Rᵇ y S(=O)₂NRᶜRᵈ; cada R²¹ se selecciona independientemente de alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆ y haloalquilo C₁₋₆, donde cada uno de dichos alquilo C₁₋₆, alquenilo C₂₋₆ y alquinilo C₂₋₆ está opcionalmente sustituido con 1, 2 ó 3 sustituyentes que se seleccionan independientemente de Cy², halo, CN, NO₂, ORᵃ, SRᵃ, C(=O)Rᵇ, C(=O)NRᶜRᵈ, C(=O)ORᵃ, OC(=O)Rᵇ, OC(=O)NRᶜRᵈ, C(=NRᵉ)NRᶜRᵈ, NRᶜC(=NRᵉ)NRᶜRᵈ, NRᶜRᵈ, NRᶜC(=O)Rᵇ, NRᶜC(=O)ORᵃ, NRCC(=O)NRᶜRᵈ, NRᶜS(=O)Rᵇ, NRᶜS(=O)₂Rᵇ, NRᶜS(=O)₂NRᶜRᵈ, S(=O)Rᵇ, S(=O)NRᶜRᵈ, S(=O)₂Rᵇ y S(=O)₂NRᶜRᵈ; de manera alternativa, cuando dos grupos R²¹ están unidos al mismo átomo de carbono, los dos grupos R²¹, junto con el átomo de carbono al que están unidos, forman un anillo de cicloalquilo de 3 - 7 miembros o un anillo de heterocicloalquilo de 3 - 7 miembros, donde 1 ó 2 miembros del anillo de dicho anillo de heterocicloalquilo se seleccionan independientemente de N, O y S; y donde cada uno de dicho anillo de cicloalquilo y anillo de heterocicloalquilo está opcionalmente sustituido con 1, 2 ó 3 sustituyentes que se seleccionan independientemente de halo, OH, CN, alquilo C₁₋₃, alcoxi C₁₋₃ y haloalquilo C₁₋₃; cada Cy² se selecciona independientemente de arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros y heterocicloalquilo de 3 - 10 miembros, donde cada uno de dichos arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros y heterocicloalquilo de 3 - 10 miembros está opcionalmente sustituido con 1, 2, 3, 4 ó 5 sustituyentes que se seleccionan independientemente de halo, R²², CN, NO₂, ORᵃ, SRᵃ, C(=O)Rᵇ, C(=O)NRᶜRᵈ, C(=O)ORᵃ, OC(=O)Rᵇ, OC(=O)NRᶜRᵈ, C(=NRᵉ)NRᶜRᵈ, NRᶜC(=NRᵉ)NRᶜRᵈ, NRᶜRᵈ, NRᶜC(=O)Rᵇ, NRᶜC(=O)ORᵃ, NRᶜC(=O)NRᶜRᵈ, NRᶜS(=O)Rᵇ, NRᶜS(=O)₂Rᵇ, NRᶜS(=O)₂NRᶜRᵈ, S(=O)Rᵇ, S(=O)NRᶜRᵈ, S(=O)₂Rᵇ y S(=O)₂NRᶜRᵈ; cada Rᵃ, Rᶜ y Rᵈ se selecciona independientemente de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros y heterocicloalquilo de 3 - 10 miembros, donde cada uno de dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros y heterocicloalquilo de 3 - 10 miembros está opcionalmente sustituido con 1, 2, 3, 4 ó 5 sustituyentes que se seleccionan independientemente de halo, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo
ARP130103980A 2012-11-01 2013-10-31 Derivados triciclicos fusionados de tiofeno como inhibidores de jak AR093308A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261721308P 2012-11-01 2012-11-01
US201361783850P 2013-03-14 2013-03-14

Publications (1)

Publication Number Publication Date
AR093308A1 true AR093308A1 (es) 2015-05-27

Family

ID=49578588

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130103980A AR093308A1 (es) 2012-11-01 2013-10-31 Derivados triciclicos fusionados de tiofeno como inhibidores de jak

Country Status (22)

Country Link
US (7) US9181271B2 (es)
EP (1) EP2917221A1 (es)
JP (2) JP6359546B2 (es)
KR (1) KR20150074193A (es)
CN (2) CN107936039A (es)
AR (1) AR093308A1 (es)
AU (2) AU2013337824B2 (es)
BR (1) BR112015009942A2 (es)
CA (1) CA2888816A1 (es)
CL (1) CL2015001160A1 (es)
CR (1) CR20150255A (es)
EA (1) EA031882B1 (es)
HK (1) HK1214823A1 (es)
IL (2) IL238410B (es)
MX (1) MX2015005428A (es)
NZ (1) NZ707495A (es)
PE (1) PE20151141A1 (es)
PH (1) PH12015500963B1 (es)
SG (2) SG11201503141TA (es)
TW (1) TWI646099B (es)
UA (1) UA117572C2 (es)
WO (1) WO2014071031A1 (es)

Families Citing this family (90)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2426129T3 (pl) 2005-12-13 2017-04-28 Incyte Holdings Corporation Podstawione heteroarylem pirolo[2,3-b]pirydyny i pirolo[2,3-b]pirymidyny jako inhibitory kinazy Janusowej
ME00960B (me) 2007-06-13 2012-06-20 Incyte Corp Soli inhibitora janus kinaze, (r)-3-(4-(7h-pirol[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropannitrila
LT2432472T (lt) 2009-05-22 2020-02-10 Incyte Holdings Corporation 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- arba heptan-nitrilas, kaip jak inhibitoriai
US8716303B2 (en) 2009-05-22 2014-05-06 Incyte Corporation N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EP2845856A1 (en) 2009-06-29 2015-03-11 Incyte Corporation Pyrimidinones as PI3K inhibitors
US9249145B2 (en) 2009-09-01 2016-02-02 Incyte Holdings Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
PL3050882T3 (pl) 2010-03-10 2018-08-31 Incyte Holdings Corporation Piperydyn-4-ylowe pochodne azetydyny jako inhibitory JAK1
BR112012029653B1 (pt) 2010-05-21 2021-01-12 Incyte Holdings Corporation formulação farmacêutica para aplicação tópica em pele e seu uso
CN103415515B (zh) 2010-11-19 2015-08-26 因塞特公司 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物
EP3660016A1 (en) 2010-12-20 2020-06-03 Incyte Holdings Corporation N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
CA2839767A1 (en) 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
SG11201400232WA (en) 2011-09-02 2014-03-28 Incyte Corp Heterocyclylamines as pi3k inhibitors
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
EP2917221A1 (en) * 2012-11-01 2015-09-16 Incyte Corporation Tricyclic fused thiophene derivatives as jak inhibitors
HUE055894T2 (hu) 2012-11-15 2021-12-28 Incyte Holdings Corp A ruxolitinib nyújtott felszabadulású dózisformái
EP2943485B1 (en) 2013-01-14 2017-09-20 Incyte Holdings Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
NZ749911A (en) 2013-01-15 2020-02-28 Incyte Holdings Corp Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors
BR112015021458B1 (pt) 2013-03-06 2022-06-07 Incyte Holdings Corporation "processos e intermediários para preparar {1-{1-[3-flúor2-(trifluormetil)isonicotinoil] piperidin-4-il}-3-[4-(7hpirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]azetidin-3-il}acetonitrila, útil no tratamento de doenças relacionadas com a atividade de janus quinases
TWI599567B (zh) 2013-03-14 2017-09-21 健生藥品公司 Ｐ２ｘ７調節劑
TWI627174B (zh) 2013-03-14 2018-06-21 比利時商健生藥品公司 Ｐ２ｘ７調控劑
US9604982B2 (en) 2013-03-14 2017-03-28 Janssen Pharmaceutica Nv P2X7 modulators
AP2015008601A0 (en) 2013-03-14 2015-07-31 Boehringer Ingelheim Int Substituted 2-aza-bicyclo[2.2.1] heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin C
WO2014152537A1 (en) 2013-03-14 2014-09-25 Janssen Pharmaceutica Nv P2x7 modulators
HUE043573T2 (hu) 2013-05-17 2019-08-28 Incyte Corp Bipirazol só, amely JAK-gátlóként alkalmazható
KR20160045081A (ko) 2013-08-07 2016-04-26 인사이트 코포레이션 Jak1 억제제용 지속 방출 복용 형태
SG11201601259YA (en) 2013-08-23 2016-03-30 Incyte Corp Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors
PL3110409T3 (pl) * 2014-02-28 2018-12-31 Incyte Corporation Inhibitory jak1 do leczenia zespołów mielodysplastycznych
PT3129021T (pt) 2014-04-08 2020-11-16 Incyte Corp Ratamento de doenças malignas das células b por uma associação de inibidores de jak e pi3k
CN106687462A (zh) * 2014-04-30 2017-05-17 因赛特公司 Jak1抑制剂的制备方法以及其新形式
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
US9822124B2 (en) 2014-07-14 2017-11-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
SG11201701633SA (en) 2014-09-12 2017-03-30 Boehringer Ingelheim Int Spirocyclic inhibitors of cathepsin c
JP6592510B2 (ja) 2014-09-12 2019-10-16 ヤンセン ファーマシューティカ エヌ．ベー． Ｐ２ｘ７調節因子
US9586949B2 (en) 2015-02-09 2017-03-07 Incyte Corporation Aza-heteroaryl compounds as PI3K-gamma inhibitors
EP3262046B1 (en) 2015-02-27 2020-11-04 Incyte Corporation Salts of pi3k inhibitor and processes for their preparation
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
WO2016183071A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Hetero-tricyclic compounds and their use for the treatment of cancer
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
WO2017027717A1 (en) 2015-08-12 2017-02-16 Incyte Corporation Bicyclic fused pyrimidine compounds as tam inhibitors
WO2017035366A1 (en) 2015-08-26 2017-03-02 Incyte Corporation Pyrrolopyrimidine derivatives as tam inhibitors
TWI734699B (zh) 2015-09-09 2021-08-01 美商英塞特公司 Ｐｉｍ激酶抑制劑之鹽
TW201718546A (zh) 2015-10-02 2017-06-01 英塞特公司 適用作pim激酶抑制劑之雜環化合物
EP4086259A1 (en) 2015-11-06 2022-11-09 Incyte Corporation Heterocyclic compounds as pi3k-gamma inhibitors
EP3400221B1 (en) 2016-01-05 2020-08-26 Incyte Corporation Pyrazol / imidazol substituted pyridines as pi3k-gamma inhibitors
CN114456175B (zh) 2016-03-28 2024-09-03 因赛特公司 作为tam抑制剂的吡咯并三嗪化合物
TW201803871A (zh) 2016-06-24 2018-02-01 英塞特公司 作為ＰＩ３Ｋ-γ抑制劑之雜環化合物
BR112019005969A2 (pt) * 2016-10-03 2019-06-18 Tll Pharmaceutical Llc inibidores seletivos de jak1 inovadores e usos dos mesmos
AU2018208516B2 (en) * 2017-01-11 2021-07-08 Aqilion Ab Novel amino-imidazopyridine derivatives as Janus kinase inhibitors and pharmaceutical use thereof
WO2019067594A1 (en) 2017-09-27 2019-04-04 Incyte Corporation SALTS OF PYRROLOTRIAZINE DERIVATIVES USEFUL AS TAM INHIBITORS
BR112020007593A2 (pt) 2017-10-18 2020-09-24 Incyte Corporation derivados de imidazol condensados substituídos por grupos hidróxi terciários como inibidores de pi3k-gama
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
TWI797242B (zh) 2018-01-30 2023-04-01 美商英塞特公司 製備ｊａｋ抑制劑之方法及中間物
CN118557580A (zh) 2018-02-16 2024-08-30 因赛特公司 用于治疗细胞因子相关的病症的jak1通路抑制剂
WO2019191679A1 (en) 2018-03-30 2019-10-03 Incyte Corporation Biomarkers for inflammatory skin disease
SG11202009441PA (en) * 2018-03-30 2020-10-29 Incyte Corp Treatment of hidradenitis suppurativa using jak inhibitors
KR20210018218A (ko) 2018-04-13 2021-02-17 인사이트 코포레이션 이식편대숙주질환용 바이오마커
MX2021000127A (es) 2018-06-29 2021-03-29 Incyte Corp Formulaciones de un inhibidor de axl/mer.
EP3818060B1 (en) 2018-07-06 2023-02-22 LEO Pharma A/S Novel amino-imidazopyrimidine derivatives as janus kinase inhibitors and pharmaceutical use thereof
IL309869A (en) 2018-09-05 2024-02-01 Incyte Corp Crystal forms of phosphoinositide 3-kinase inhibitor (PI3K)
WO2020065614A1 (en) 2018-09-28 2020-04-02 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
EA202190886A1 (ru) 2018-09-28 2021-09-07 Янссен Фармацевтика Нв Модуляторы моноацилглицерин-липазы
MX2021004946A (es) 2018-10-31 2021-07-15 Incyte Corp Terapia combinada para tratamiento de enfermedades hematológicas.
EP3897627A1 (en) 2018-12-19 2021-10-27 Incyte Corporation Jak1 pathway inhibitors for the treatment of gastrointestinal disease
CN114007621A (zh) 2019-03-05 2022-02-01 因赛特公司 用于治疗慢性肺同种异体移植物功能障碍的jak1途径抑制剂
EP3941474A2 (en) 2019-03-19 2022-01-26 Incyte Corporation Biomarkers for vitiligo
WO2020244348A1 (zh) * 2019-06-06 2020-12-10 广州高瓴制药有限公司 呋喃并咪唑并吡啶类化合物的合成方法、呋喃并咪唑并吡啶类化合物的晶型及其盐的晶型
BR112021024530A2 (pt) * 2019-06-06 2022-01-18 Highlightll Pharmaceutical Hainan Co Ltd Método para sintetizar composto de furoimidazopiridina, substância polimórfica e substância polimórfica de sal
EP4038070A1 (en) 2019-09-30 2022-08-10 Janssen Pharmaceutica NV Radiolabelled mgl pet ligands
EP4041204A1 (en) 2019-10-10 2022-08-17 Incyte Corporation Biomarkers for graft-versus-host disease
US20210123931A1 (en) 2019-10-10 2021-04-29 Incyte Corporation Biomarkers for graft-versus-host disease
JP7518900B2 (ja) * 2019-10-16 2024-07-18 インサイト・コーポレイション 皮膚エリテマトーデス及び扁平苔癬（ｌｐ）の治療のためのｊａｋ１阻害剤の使用
US11992490B2 (en) 2019-10-16 2024-05-28 Incyte Corporation Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP)
CN115210229A (zh) 2020-01-03 2022-10-18 博格有限责任公司 多环酰胺作为治疗癌症的ube2k调节剂
CN111297870B (zh) * 2020-03-20 2021-03-26 中国医学科学院医药生物技术研究所 硝基苯甲酸类化合物在制备治疗肿瘤的药物中的应用
KR20220157999A (ko) 2020-03-26 2022-11-29 얀센 파마슈티카 엔.브이. 모노아실글리세롤 리파아제 조절제
AR122505A1 (es) 2020-06-02 2022-09-14 Incyte Corp Procesos para preparar un inhibidor de jak1
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022120131A1 (en) 2020-12-04 2022-06-09 Incyte Corporation Jak inhibitor with a vitamin d analog for treatment of skin diseases
KR20230118118A (ko) 2020-12-08 2023-08-10 인사이트 코포레이션 백반증의 치료를 위한 jak1 경로 저해제
CA3207859A1 (en) 2021-01-11 2022-07-14 Incyte Corporation Combination therapy comprising jak pathway inhibitor and rock inhibitor
WO2022235613A1 (en) 2021-05-03 2022-11-10 Incyte Corporation Jak1 pathway inhibitors for the treatment of prurigo nodularis
US20240309095A1 (en) 2021-07-07 2024-09-19 Incyte Corporation Anti-b7-h4 antibodies and uses thereof
CA3241889A1 (en) 2021-12-08 2023-06-15 Incyte Corporation Anti-mutant calreticulin (calr) antibodies and uses thereof
WO2024030600A1 (en) 2022-08-05 2024-02-08 Incyte Corporation Treatment of urticaria using jak inhibitors

Family Cites Families (82)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1306260C (en) 1985-10-18 1992-08-11 Shionogi & Co., Ltd. Condensed imidazopyridine derivatives
JP2513001B2 (ja) 1988-11-01 1996-07-03 山川薬品工業株式会社 光学活性テトラヒドロフラン−２−カルボン酸のラセミ化方法
JPH02225463A (ja) 1989-02-27 1990-09-07 Nissan Chem Ind Ltd Ｎ―アセチル―インドリン―２―カルボン酸エステルのラセミ化法
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
FR2695126B1 (fr) * 1992-08-27 1994-11-10 Sanofi Elf Dérivés d'acide thiényl ou pyrrolyl carboxyliques, leur préparation et médicaments les contenant.
JP3178301B2 (ja) 1994-08-08 2001-06-18 東レ株式会社 ラセミ脂肪族ヘテロ環カルボン酸エステルの製造方法
EP0727217A3 (en) 1995-02-10 1997-01-15 Suntory Ltd Pharmaceutical and cosmetic compositions containing God-type ellagitannin as an active ingredient
US6025366A (en) * 1998-04-02 2000-02-15 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
ES2342240T3 (es) 1998-08-11 2010-07-02 Novartis Ag Derivados de isoquinolina con actividad que inhibe la angiogenia.
JP2000119271A (ja) * 1998-08-12 2000-04-25 Hokuriku Seiyaku Co Ltd １ｈ―イミダゾピリジン誘導体
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
AU2002215608B2 (en) 2000-06-28 2004-12-09 Smithkline Beecham P.L.C. Wet milling process
JP2003002890A (ja) 2000-08-22 2003-01-08 Hokuriku Seiyaku Co Ltd １ｈ−イミダゾピリジン誘導体
WO2002016370A1 (fr) * 2000-08-22 2002-02-28 Hokuriku Seiyaku Co., Ltd. Derives de 1h-imidazopyridine
CA2466243A1 (en) 2001-09-19 2003-03-27 Aventis Pharma S.A. Indolizines as kinase protein inhibitors
HU230798B1 (hu) 2001-10-30 2018-06-28 Novartis Ag Staurosporin-származékok mint az FLT3 receptor tirozin-kináz aktivitás inhibitorai
PE20040522A1 (es) 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
JP4374222B2 (ja) 2003-09-01 2009-12-02 Ｈｏｙａ株式会社 変倍光学系
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
WO2005105814A1 (en) 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
AR049511A1 (es) 2004-06-10 2006-08-09 Irm Llc Compuestos y composiciones como inhibidores de quinasa de proteina
KR20070085433A (ko) 2004-11-24 2007-08-27 노파르티스 아게 Ｊａｋ 저해제들과 ｂｃｒ-ａｂｌ, ｆｌｔ-3, ｆａｋ 또는ｒａｆ 키나제 저해제들 중 하나 이상의 조합물
AR054416A1 (es) 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
US7683171B2 (en) * 2005-02-04 2010-03-23 Bristol-Myers Squibb Company 1H-imidazo[4,5-d]thieno[3,2-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
US20070149506A1 (en) 2005-09-22 2007-06-28 Arvanitis Argyrios G Azepine inhibitors of Janus kinases
US20130137681A1 (en) 2005-12-13 2013-05-30 Incyte Corporation HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS
PL2426129T3 (pl) 2005-12-13 2017-04-28 Incyte Holdings Corporation Podstawione heteroarylem pirolo[2,3-b]pirydyny i pirolo[2,3-b]pirymidyny jako inhibitory kinazy Janusowej
WO2008011190A1 (en) * 2006-07-21 2008-01-24 Vertex Pharmaceuticals Incorporated Cgrp receptor antagonists
MX2009006543A (es) * 2006-12-20 2009-06-26 Amgen Inc Compuestos heterociclicos y su uso en el tratamiento de la inflamacion, angiogenesis y cancer.
CA2673038C (en) 2006-12-22 2015-12-15 Incyte Corporation Substituted tricyclic heteroaryl compounds as janus kinase inhibitors
ME00960B (me) 2007-06-13 2012-06-20 Incyte Corp Soli inhibitora janus kinaze, (r)-3-(4-(7h-pirol[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropannitrila
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
UA104849C2 (uk) 2007-11-16 2014-03-25 Інсайт Корпорейшн 4-піразоліл-n-арилпіримідин-2-аміни і 4-піразоліл-n-гетероарилпіримідин-2-аміни як інгібітори кіназ janus
BRPI0909040B8 (pt) 2008-03-11 2021-05-25 Incyte Holdings Corp derivados de azetidina e ciclobutano, seus usos, e composição
CA2727928A1 (en) * 2008-06-18 2009-12-23 Merck Sharp & Dohme Corp. Inhibitors of janus kinases
SG178812A1 (en) * 2008-06-20 2012-03-29 Genentech Inc Triazolopyridine jak inhibitor compounds and methods
CL2009001884A1 (es) 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
JOP20190230A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
LT2432472T (lt) 2009-05-22 2020-02-10 Incyte Holdings Corporation 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- arba heptan-nitrilas, kaip jak inhibitoriai
US8716303B2 (en) 2009-05-22 2014-05-06 Incyte Corporation N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
CN102574857B (zh) 2009-07-08 2015-06-10 利奥制药有限公司 作为jak受体和蛋白酪氨酸激酶抑制剂的杂环化合物
US9249145B2 (en) 2009-09-01 2016-02-02 Incyte Holdings Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
MX2012004180A (es) 2009-10-09 2012-07-17 Incyte Corp Derivados de hidroxil, ceto y glucuronido de 3-(4-7h-pirrolo[2,3-d ]pirimidin-a-il)-1h-pirazol-1-il)-3-ciclopentilpropanonitrilo.
KR20140015162A (ko) * 2010-01-12 2014-02-06 에프. 호프만-라 로슈 아게 트라이사이클릭 헤테로사이클릭 화합물, 조성물 및 이의 사용 방법
EP2536729A1 (en) 2010-02-18 2012-12-26 Incyte Corporation Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors
PL3050882T3 (pl) 2010-03-10 2018-08-31 Incyte Holdings Corporation Piperydyn-4-ylowe pochodne azetydyny jako inhibitory JAK1
BR112012029653B1 (pt) 2010-05-21 2021-01-12 Incyte Holdings Corporation formulação farmacêutica para aplicação tópica em pele e seu uso
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
CN103415515B (zh) 2010-11-19 2015-08-26 因塞特公司 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物
ES2547916T3 (es) 2011-02-18 2015-10-09 Novartis Pharma Ag Terapia de combinación de inhibidores de mTOR/JAK
ES2666870T3 (es) 2011-03-10 2018-05-08 Daiichi Sankyo Company, Limited Derivado de dispiropirrolidina
CA2839767A1 (en) 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
WO2013007768A1 (en) * 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Tricyclic heterocyclic compounds, compositions and methods of use thereof as jak inhibitors
WO2013007765A1 (en) 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Fused tricyclic compounds for use as inhibitors of janus kinases
EP2741747A1 (en) 2011-08-10 2014-06-18 Novartis Pharma AG JAK P13K/mTOR COMBINATION THERAPY
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
EP2917221A1 (en) * 2012-11-01 2015-09-16 Incyte Corporation Tricyclic fused thiophene derivatives as jak inhibitors
HUE055894T2 (hu) 2012-11-15 2021-12-28 Incyte Holdings Corp A ruxolitinib nyújtott felszabadulású dózisformái
BR112015021458B1 (pt) 2013-03-06 2022-06-07 Incyte Holdings Corporation "processos e intermediários para preparar {1-{1-[3-flúor2-(trifluormetil)isonicotinoil] piperidin-4-il}-3-[4-(7hpirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]azetidin-3-il}acetonitrila, útil no tratamento de doenças relacionadas com a atividade de janus quinases
HUE043573T2 (hu) 2013-05-17 2019-08-28 Incyte Corp Bipirazol só, amely JAK-gátlóként alkalmazható
KR20160045081A (ko) 2013-08-07 2016-04-26 인사이트 코포레이션 Jak1 억제제용 지속 방출 복용 형태
CN105555313A (zh) * 2013-08-20 2016-05-04 因赛特公司 在c-反应蛋白水平较高的实体肿瘤患者中的存活益处
PL3110409T3 (pl) 2014-02-28 2018-12-31 Incyte Corporation Inhibitory jak1 do leczenia zespołów mielodysplastycznych
PT3129021T (pt) * 2014-04-08 2020-11-16 Incyte Corp Ratamento de doenças malignas das células b por uma associação de inibidores de jak e pi3k
CN106687462A (zh) 2014-04-30 2017-05-17 因赛特公司 Jak1抑制剂的制备方法以及其新形式
US9498467B2 (en) * 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
WO2015191677A1 (en) * 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
WO2017035366A1 (en) * 2015-08-26 2017-03-02 Incyte Corporation Pyrrolopyrimidine derivatives as tam inhibitors
CN118557580A (zh) * 2018-02-16 2024-08-30 因赛特公司 用于治疗细胞因子相关的病症的jak1通路抑制剂
SG11202009441PA (en) * 2018-03-30 2020-10-29 Incyte Corp Treatment of hidradenitis suppurativa using jak inhibitors
WO2019191679A1 (en) * 2018-03-30 2019-10-03 Incyte Corporation Biomarkers for inflammatory skin disease
KR20210018218A (ko) * 2018-04-13 2021-02-17 인사이트 코포레이션 이식편대숙주질환용 바이오마커
MX2021004946A (es) * 2018-10-31 2021-07-15 Incyte Corp Terapia combinada para tratamiento de enfermedades hematológicas.
EP3941474A2 (en) * 2019-03-19 2022-01-26 Incyte Corporation Biomarkers for vitiligo

Also Published As

Publication number Publication date
US10370387B2 (en) 2019-08-06
CN107936039A (zh) 2018-04-20
US20200040002A1 (en) 2020-02-06
PE20151141A1 (es) 2015-08-06
CR20150255A (es) 2015-09-09
US20160024109A1 (en) 2016-01-28
US11851442B2 (en) 2023-12-26
SG11201503141TA (en) 2015-06-29
US20240228508A1 (en) 2024-07-11
BR112015009942A2 (pt) 2017-07-11
US20160015695A1 (en) 2016-01-21
US9777017B2 (en) 2017-10-03
US9908895B2 (en) 2018-03-06
JP6359546B2 (ja) 2018-07-18
US20140121198A1 (en) 2014-05-01
HK1214823A1 (zh) 2016-08-05
US20210387998A1 (en) 2021-12-16
TW201422624A (zh) 2014-06-16
IL238410A0 (en) 2015-06-30
SG10201703533VA (en) 2017-06-29
EP2917221A1 (en) 2015-09-16
AU2013337824A1 (en) 2015-05-14
PH12015500963A1 (en) 2015-08-17
US20180148460A1 (en) 2018-05-31
WO2014071031A1 (en) 2014-05-08
IL238410B (en) 2018-02-28
TWI646099B (zh) 2019-01-01
US9181271B2 (en) 2015-11-10
JP2015535288A (ja) 2015-12-10
PH12015500963B1 (en) 2015-08-17
MX2015005428A (es) 2015-07-21
CN104918945A (zh) 2015-09-16
JP2018141020A (ja) 2018-09-13
CL2015001160A1 (es) 2015-08-28
CA2888816A1 (en) 2014-05-08
AU2013337824B2 (en) 2018-03-08
CN104918945B (zh) 2018-01-05
EA031882B1 (ru) 2019-03-29
AU2018204090A1 (en) 2018-06-28
EA201590850A1 (ru) 2015-09-30
KR20150074193A (ko) 2015-07-01
UA117572C2 (uk) 2018-08-27
NZ707495A (en) 2019-01-25
US11161855B2 (en) 2021-11-02
IL257066A (en) 2018-03-29

Similar Documents

Publication Publication Date Title
AR093308A1 (es) Derivados triciclicos fusionados de tiofeno como inhibidores de jak
AR124916A2 (es) Piridinas sustituidas con heteroarilo y métodos de uso
AR106605A1 (es) Oxadiazoles sustituidos para combatir hongos fitopatógenos
AR095326A1 (es) Heterociclos tricíclicos como inhibidores de la proteína bet
AR106763A1 (es) Oxadiazoles sustituidos para combatir hongos fitopatógenos
AR106595A1 (es) COMPUESTOS HETEROCÍCLICOS COMO INHIBIDORES DE PI3K-g
AR094174A1 (es) Lactamas fusionadas de arilo y heteroarilo
AR098136A1 (es) Compuestos de heteroarilo como inhibidores de btk y usos de los mismos
AR094313A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR100442A1 (es) Derivados de pirido[1,2-a]pirimidin-4-ona para tratar atrofia muscular espinal
AR107032A1 (es) Inhibidores bicíclicos de pad4
AR096837A1 (es) Heterociclos tricíclicos como inhibidores de proteínas bet
AR092742A1 (es) Piridinonas antifibroticas
AR088781A1 (es) Compuestos antimicrobianos y metodos para prepararlos y utilizarlos
AR088423A1 (es) Ligadores p1 ciclicos como inhibidores del factor xia
AR085004A1 (es) Inhibidores selectivos de glicosidasas y usos de los mismos
AR093505A1 (es) Derivados de 5-fluoro-n-(piridin-2-il)piridin-2-amina que contienen un grupo sulfoximina
AR089527A1 (es) Inhibidores de bromodominios
AR100810A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR117900A1 (es) Pirazolopiridinas y triazolopiridinas como inhibidores de a2a / a2b
AR098776A1 (es) Derivados del isocromeno como inhibidores de las fosfoinositido-3 quinasas
AR096721A1 (es) Compuestos de tetrahidrocarbazol y carbazol carboxamida sustituidos
AR098492A1 (es) Derivados de purina
AR097436A1 (es) Bis-amidopiridinas
AR088320A1 (es) Derivados de isoindolinona y pirrolopiridinona como inhibidores de akt

Legal Events

Date Code Title Description
FB Suspension of granting procedure