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=***_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

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 (6) US9181271B2 (es)
EP (1) EP2917221A1 (es)
JP (2) JP6359546B2 (es)
KR (1) KR20150074193A (es)
CN (2) CN104918945B (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) SG10201703533VA (es)
TW (1) TWI646099B (es)
UA (1) UA117572C2 (es)
WO (1) WO2014071031A1 (es)

Families Citing this family (89)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2348023B9 (en) 2005-12-13 2017-03-08 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
CN101932582B (zh) 2007-06-13 2013-09-25 因塞特公司 詹纳斯激酶抑制剂(R)-3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的盐
SG176111A1 (en) 2009-05-22 2011-12-29 Incyte Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
CN102458581B (zh) 2009-05-22 2016-03-30 因塞特控股公司 作为JANUS激酶抑制剂的吡唑-4-基-吡咯并[2，3-d]嘧啶和吡咯-3-基-吡咯并[2，3-d]嘧啶的N-(杂)芳基-吡咯烷衍生物
ME01838B (me) 2009-06-29 2014-12-20 Lncyte Holdings Corp Pirimidinoni kao inhibitori pi3k
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
ME02386B (me) 2010-03-10 2016-09-20 Incyte Holdings Corp Derivati piperidin-4-il azetidina kao inhibitori jak1
KR102303885B1 (ko) 2010-05-21 2021-09-24 인사이트 홀딩스 코포레이션 Ｊａｋ 저해제에 대한 국소 제형
EP2640723A1 (en) 2010-11-19 2013-09-25 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
EP2655374B1 (en) 2010-12-20 2019-10-23 Incyte Holdings Corporation N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
US8691807B2 (en) 2011-06-20 2014-04-08 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
MX2020004502A (es) 2011-09-02 2022-01-20 Incyte Holdings Corp Heterociclilaminas como inhibidores de fosfoinositida 3-cinasas (pi3k).
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
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
PE20151141A1 (es) * 2012-11-01 2015-08-06 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de jak
EA201590930A1 (ru) 2012-11-15 2015-08-31 Инсайт Корпорейшн Лекарственные формы руксолитиниба с замедленным высвобождением
WO2014110574A1 (en) 2013-01-14 2014-07-17 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
SG11201505347VA (en) 2013-01-15 2015-08-28 Incyte Corp Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors
JP6397831B2 (ja) 2013-03-06 2018-09-26 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｋ阻害剤の製造方法及びその中間体
JP6294953B2 (ja) 2013-03-14 2018-03-14 ヤンセン ファーマシューティカ エヌ．ベー． Ｐ２ｘ７調節物質
US10053463B2 (en) 2013-03-14 2018-08-21 Janssen Pharmaceutica Nv Substituted [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
TWI627174B (zh) 2013-03-14 2018-06-21 比利時商健生藥品公司 Ｐ２ｘ７調控劑
UY35391A (es) 2013-03-14 2014-09-30 Boehringer Ingelheim Int Acido 2-aza-biciclo[2.2.1]heptano-3-carboxilico (bencil-cianometil)-amidas sustituidas inhibidores de catepsina c
TWI599567B (zh) 2013-03-14 2017-09-21 健生藥品公司 Ｐ２ｘ７調節劑
ME02763B (me) 2013-05-17 2018-01-20 Incyte Corp Derivati bipirazola kao inhibitori jak
MY195091A (en) 2013-08-07 2023-01-10 Incyte Corp Sustained Release Dosage Forms for a JAK1 Inhibitor
US9556197B2 (en) 2013-08-23 2017-01-31 Incyte Corporation Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors
SI3110409T1 (sl) * 2014-02-28 2018-11-30 Incyte Corporation Inhibitorji JAK1 za zdravljenje mielodisplastičnih sindromov
KR20230044320A (ko) 2014-04-08 2023-04-03 인사이트 코포레이션 Ｊａｋ 및 ｐｉ3ｋ 억제제 조합에 의한 ｂ-세포 악성종양의 치료
SG10201809518QA (en) * 2014-04-30 2018-11-29 Incyte Corp Processes of preparing a jak1 inhibitor and new forms thereto
WO2015184305A1 (en) * 2014-05-30 2015-12-03 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
WO2016010897A1 (en) 2014-07-14 2016-01-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors
EA034015B1 (ru) 2014-09-12 2019-12-19 Янссен Фармацевтика Нв Модуляторы р2х7
HUE047208T2 (hu) 2014-09-12 2020-04-28 Boehringer Ingelheim Int A katepszin-C spirociklikus inhibitorai
US9586949B2 (en) 2015-02-09 2017-03-07 Incyte Corporation Aza-heteroaryl compounds as PI3K-gamma inhibitors
CR20170389A (es) 2015-02-27 2018-01-26 Incyte Corp Sales de inhibidor de p13k y procesos de preparación
WO2016183071A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Hetero-tricyclic compounds and their use for the treatment of cancer
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
US9540347B2 (en) 2015-05-29 2017-01-10 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
US10053465B2 (en) 2015-08-26 2018-08-21 Incyte Corporation Pyrrolopyrimidine derivatives as TAM inhibitors
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
WO2017059251A1 (en) 2015-10-02 2017-04-06 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
MD3371190T2 (ro) 2015-11-06 2022-09-30 Incyte Corp Compuși heterociclici ca inhibitori PI3K-gamma
EP3400221B1 (en) 2016-01-05 2020-08-26 Incyte Corporation Pyrazol / imidazol substituted pyridines as pi3k-gamma inhibitors
KR20230111268A (ko) 2016-03-28 2023-07-25 인사이트 코포레이션 Tam 억제제로서 피롤로트리아진 화합물
AR108875A1 (es) 2016-06-24 2018-10-03 Incyte Corp COMPUESTOS HETEROCÍCLICOS COMO INHIBIDORES DE PI3K-g
ES2901216T3 (es) * 2016-10-03 2022-03-21 Highlightll Pharmaceutical Hainan Co Ltd Nuevos inhibidores selectivos de Jak1 y usos de los mismos
RU2019125177A (ru) 2017-01-11 2021-02-15 Лео Фарма А/С Новые производные амино-имидазопиридина в качестве ингибиторов янус-киназы и их фармацевтическое применение
EP3988552A1 (en) 2017-09-27 2022-04-27 Incyte Corporation Salts of pyrrolotriazine derivatives useful as tam inhibitors
PE20210169A1 (es) 2017-10-18 2021-01-29 Incyte Corp Derivados de imidazol condensados sustituidos por grupos de hidroxia terciaria como inhibidores de pi3k-y gamma
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
CR20200379A (es) 2018-01-30 2021-03-05 Incyte Corp Procesos e intermedio para elaborar un inhibidor de jak campo técnico
KR20200128043A (ko) 2018-02-16 2020-11-11 인사이트 코포레이션 사이토카인-관련 장애의 치료를 위한 jak1 경로 억제제
CA3095487A1 (en) 2018-03-30 2019-10-03 Incyte Corporation Treatment of hidradenitis suppurativa using jak inhibitors
MA52655A (fr) 2018-03-30 2021-02-17 Incyte Corp Biomarqueurs pour maladie cutanée inflammatoire
WO2019200030A1 (en) 2018-04-13 2019-10-17 Incyte Corporation Biomarkers for graft-versus-host disease
AR117600A1 (es) 2018-06-29 2021-08-18 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
DK3847175T3 (da) 2018-09-05 2024-03-18 Incyte Corp Krystallinske former af en phosphoinositid-3-kinase- (pi3k) inhibitor
BR112021005936A2 (pt) 2018-09-28 2021-06-29 Janssen Pharmaceutica Nv moduladores de monoacilglicerol lipase
TW202028198A (zh) 2018-09-28 2020-08-01 比利時商健生藥品公司 單醯基丙三醇脂酶調節劑
MX2021004946A (es) 2018-10-31 2021-07-15 Incyte Corp Terapia combinada para tratamiento de enfermedades hematológicas.
CN113692278A (zh) 2018-12-19 2021-11-23 因赛特公司 用于治疗胃肠道疾病的jak1途径抑制剂
SG11202109563WA (en) 2019-03-05 2021-09-29 Incyte Corp Jak1 pathway inhibitors for the treatment of chronic lung allograft dysfunction
US11624751B2 (en) 2019-03-19 2023-04-11 Incyte Corporation Biomarkers for vitiligo
KR20220017990A (ko) * 2019-06-06 2022-02-14 하이라이트ll 파머슈티컬 (하이난) 컴퍼니, 리미티드 푸로이미다조피리딘 화합물의 합성 방법, 다형성 물질 및 염의 다형성 물질
AU2020289149B2 (en) * 2019-06-06 2023-05-11 Hangzhou Highlightll Pharmaceutical Co., Ltd. Synthesis method of furoimidazopyridine compound, crystal form of furoimidazopyridine compound, and crystal form of salt thereof
MX2022003819A (es) 2019-09-30 2022-05-11 Janssen Pharmaceutica Nv Ligandos de pet de mgl radiomarcados.
US20210123931A1 (en) 2019-10-10 2021-04-29 Incyte Corporation Biomarkers for graft-versus-host disease
CA3157499A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
JP2023506118A (ja) * 2019-10-16 2023-02-15 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
WO2021138540A1 (en) 2020-01-03 2021-07-08 Berg Llc Polycyclic amides as ube2k modulators for treating cancer
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***的药物中的应用
EP4126860A1 (en) 2020-03-26 2023-02-08 Janssen Pharmaceutica NV Monoacylglycerol lipase modulators
EP4157831A1 (en) 2020-06-02 2023-04-05 Incyte Corporation Processes of preparing a jak1 inhibitor
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
TW202237125A (zh) 2020-12-04 2022-10-01 美商英塞特公司 用於治療皮膚疾病之jak抑制劑與維生素d類似物
CA3204374A1 (en) 2020-12-08 2022-06-16 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
KR20230157307A (ko) 2021-01-11 2023-11-16 인사이트 코포레이션 Jak 경로 억제제 및 rock 억제제를 포함하는 병용 요법
JP2024516302A (ja) 2021-05-03 2024-04-12 インサイト・コーポレイション 結節性痒疹を治療するためのｊａｋ１経路阻害薬
WO2023283345A1 (en) 2021-07-07 2023-01-12 Incyte Corporation Anti-b7-h4 antibodies and uses thereof
TW202330623A (zh) 2021-12-08 2023-08-01 美商英塞特公司 抗突變鈣網伴護蛋（ｃａｌｒ））抗體及其用途
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
CN1152031C (zh) 1998-08-11 2004-06-02 诺瓦提斯公司 具有血管生成抑制活性的异喹啉衍生物
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
CA2413330A1 (en) 2000-06-28 2002-01-03 Smithkline Beecham P.L.C. Wet milling process
AU2001278790A1 (en) 2000-08-22 2002-03-04 Hokuriku Seiyaku Co. Ltd 1h-imidazopyridine derivatives
JP2003002890A (ja) 2000-08-22 2003-01-08 Hokuriku Seiyaku Co Ltd １ｈ−イミダゾピリジン誘導体
AU2002337142B2 (en) 2001-09-19 2007-10-11 Aventis Pharma S.A. Indolizines as kinase protein inhibitors
CA2462657C (en) 2001-10-30 2011-04-26 Novartis Ag Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity
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
PE20050952A1 (es) 2003-09-24 2005-12-19 Novartis Ag Derivados de isoquinolina como inhibidores de b-raf
US20060106020A1 (en) 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
MXPA06014247A (es) 2004-06-10 2007-03-12 Irm Llc Compuestos y composiciones como inhibidores de la proteina quinasa.
CN101106983A (zh) 2004-11-24 2008-01-16 诺瓦提斯公司 JAK抑制剂与至少一种Bcr-Abl、Flt-3、FAK或RAF激酶抑制剂的组合
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
WO2007038215A1 (en) 2005-09-22 2007-04-05 Incyte Corporation Tetracyclic 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
EP2348023B9 (en) 2005-12-13 2017-03-08 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
CA2658573A1 (en) * 2006-07-21 2008-01-24 Vertex Pharmaceuticals Incorporated Cgrp receptor antagonists
CA2672903C (en) * 2006-12-20 2012-10-23 Amgen Inc. Heterocyclic compounds and their use in treating inflammation, angiogenesis and cancer
JP5492565B2 (ja) 2006-12-22 2014-05-14 インサイト・コーポレイション Ｊａｎｕｓキナーゼ阻害剤としての置換複素環
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.
CN101932582B (zh) 2007-06-13 2013-09-25 因塞特公司 詹纳斯激酶抑制剂(R)-3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的盐
EP2220068B1 (en) 2007-11-16 2016-01-27 Incyte Holdings Corporation 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors
UA101493C2 (ru) 2008-03-11 2013-04-10 Инсайт Корпорейшн Производные азетидина и циклобутана как ингибиторы jak
CA2727928A1 (en) * 2008-06-18 2009-12-23 Merck Sharp & Dohme Corp. Inhibitors of janus kinases
MX2010014005A (es) * 2008-06-20 2011-02-15 Genentech Inc Compuestos de triazolopiridina inhibidores de jak y los metodos.
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.
JOP20190231A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
SG176111A1 (en) 2009-05-22 2011-12-29 Incyte Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
CN102458581B (zh) 2009-05-22 2016-03-30 因塞特控股公司 作为JANUS激酶抑制剂的吡唑-4-基-吡咯并[2，3-d]嘧啶和吡咯-3-基-吡咯并[2，3-d]嘧啶的N-(杂)芳基-吡咯烷衍生物
TW201105674A (en) * 2009-07-08 2011-02-16 Leo Pharma As Novel JAK receptor and protein tyrosine kinase inhibitors and pharmaceutical use thereof
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
KR20180126619A (ko) 2009-10-09 2018-11-27 인사이트 홀딩스 코포레이션 3-（4-（7Ｈ-피롤로〔2,3-ｄ〕피리미딘-4-일）-1Ｈ-피라졸-1-일）-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체
RU2012132278A (ru) * 2010-01-12 2014-02-20 Ф. Хоффманн-Ля Рош Аг Трициклические гетероциклические соединения, содержащие их композиции и способы их применения
BR112012020693B1 (pt) 2010-02-18 2020-05-12 Incyte Holdings Corporation Derivados de ciclobutano e metilciclobutano como inibidores de janus quinase e composição que os compreende
ME02386B (me) 2010-03-10 2016-09-20 Incyte Holdings Corp Derivati piperidin-4-il azetidina kao inhibitori jak1
KR102303885B1 (ko) 2010-05-21 2021-09-24 인사이트 홀딩스 코포레이션 Ｊａｋ 저해제에 대한 국소 제형
EP2640723A1 (en) 2010-11-19 2013-09-25 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
CA2827673C (en) 2011-02-18 2020-10-27 Novartis Pharma Ag Mtor/jak inhibitor combination therapy
JP5792279B2 (ja) 2011-03-10 2015-10-07 第一三共株式会社 ジスピロピロリジン誘導体
US8691807B2 (en) 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives 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
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
CA2844507A1 (en) 2011-08-10 2013-02-14 Novartis Pharma Ag Jak pi3k/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
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
PE20151141A1 (es) 2012-11-01 2015-08-06 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de jak
EA201590930A1 (ru) 2012-11-15 2015-08-31 Инсайт Корпорейшн Лекарственные формы руксолитиниба с замедленным высвобождением
JP6397831B2 (ja) 2013-03-06 2018-09-26 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｋ阻害剤の製造方法及びその中間体
ME02763B (me) 2013-05-17 2018-01-20 Incyte Corp Derivati bipirazola kao inhibitori jak
MY195091A (en) 2013-08-07 2023-01-10 Incyte Corp Sustained Release Dosage Forms for a JAK1 Inhibitor
JP2016528288A (ja) * 2013-08-20 2016-09-15 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ 上昇したｃ反応性タンパク質レベルを有する固形腫瘍の患者における延命効果
SI3110409T1 (sl) 2014-02-28 2018-11-30 Incyte Corporation Inhibitorji JAK1 za zdravljenje mielodisplastičnih sindromov
KR20230044320A (ko) * 2014-04-08 2023-04-03 인사이트 코포레이션 Ｊａｋ 및 ｐｉ3ｋ 억제제 조합에 의한 ｂ-세포 악성종양의 치료
SG10201809518QA (en) 2014-04-30 2018-11-29 Incyte Corp Processes of preparing a jak1 inhibitor and new forms thereto
WO2015184305A1 (en) * 2014-05-30 2015-12-03 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
US10053465B2 (en) * 2015-08-26 2018-08-21 Incyte Corporation Pyrrolopyrimidine derivatives as TAM inhibitors
KR20200128043A (ko) * 2018-02-16 2020-11-11 인사이트 코포레이션 사이토카인-관련 장애의 치료를 위한 jak1 경로 억제제
CA3095487A1 (en) * 2018-03-30 2019-10-03 Incyte Corporation Treatment of hidradenitis suppurativa using jak inhibitors
MA52655A (fr) * 2018-03-30 2021-02-17 Incyte Corp Biomarqueurs pour maladie cutanée inflammatoire
WO2019200030A1 (en) * 2018-04-13 2019-10-17 Incyte Corporation Biomarkers for graft-versus-host disease
MX2021004946A (es) * 2018-10-31 2021-07-15 Incyte Corp Terapia combinada para tratamiento de enfermedades hematológicas.
US11624751B2 (en) * 2019-03-19 2023-04-11 Incyte Corporation Biomarkers for vitiligo

Also Published As

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

Similar Documents

Publication Publication Date Title
AR093308A1 (es) Derivados triciclicos fusionados de tiofeno como inhibidores de jak
AR108396A1 (es) Compuestos heterocíclicos como inmunomoduladores
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
AR109595A1 (es) Compuestos de pirazolopirimidina y usos de estos como inhibidores de hpk1
AR106595A1 (es) COMPUESTOS HETEROCÍCLICOS COMO INHIBIDORES DE PI3K-g
AR098136A1 (es) Compuestos de heteroarilo como inhibidores de btk y usos de los mismos
AR094174A1 (es) Lactamas fusionadas de arilo y heteroarilo
AR094313A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR100442A1 (es) Derivados de pirido[1,2-a]pirimidin-4-ona para tratar atrofia muscular espinal
AR096837A1 (es) Heterociclos tricíclicos como inhibidores de proteínas bet
AR107032A1 (es) Inhibidores bicíclicos de pad4
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
AR117102A1 (es) Inhibidores de arg1 y/o arg2
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

Legal Events

Date Code Title Description
FB Suspension of granting procedure