[go: up one dir, main page]

AR054416A1 - 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. - Google Patents

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.

Info

Publication number
AR054416A1
AR054416A1 ARP050105384A ARP050105384A AR054416A1 AR 054416 A1 AR054416 A1 AR 054416A1 AR P050105384 A ARP050105384 A AR P050105384A AR P050105384 A ARP050105384 A AR P050105384A AR 054416 A1 AR054416 A1 AR 054416A1
Authority
AR
Argentina
Prior art keywords
alkyl
nrc
ora
alkynyl
cycloalkyl
Prior art date
Application number
ARP050105384A
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=36602272&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR054416(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 AR054416A1 publication Critical patent/AR054416A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • 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
    • 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
    • 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
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biotechnology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Reivindicacion 1:Un compuesto de la formula (1) o una prodroga o sal farmacéuticamente aceptable del mismo, donde: R1, R2 y R3 son cada uno, independientemente, H, halogeno, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, haloalquilo C1-4, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rd, NRcC(O)Ora, S(O)Rb, S(O) NRcRd, S(O)2Rb o S(O)2NRcRd; R4 es H, alquilo C1-4, alquenilo C2-4, alquenilo C2-4, alquinilo C2-4, S(O)2R9, SOR9, cicloalquilo o heterocicloalquilo, donde dichos alquilo C1-4, alquenilo C2-4, alquinilo C2-4, cicloalquilo, heterocicloalquilo están, cada uno opcionalmente sustituidos con 1, 2 o 3 sustituyentes seleccionados a partir de halogeno, alquilo C1-4 alquenilo C2-4, alquinilo C2-4, haloalquilo C1-4, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, Ora, SRa, C(O)Rb, C(O)NRcRd, C(O)Ora, OC(O)Rb. OC(O)NRcRd, NRcC(O)Rd, NRcC(O)Ora, S(O)Rb, S(O)NRcRd, S(O)2Rb y S(O)2NRcRd; R5 es cicloalquilo de 3 a 8 miembros, heterocicloalquilo de 3 a 8 miembros, -L-(cicloalquilo de 3 a 8 miembros), -L-(heterocicloalquilo de 3 a 8 miembros), cada uno sustituido con un R6y O, 1 o 2 R7; L es alquileno C1-4, alquenilenilo C4, alquinilenilo C2-4, O, S, NR14, CO, COO, OCO, NR14C(O)=, CONR14, SO, SO2, SONR14, SO2NR14 o NR14CONR14; R6 es -W1-W2-W3-W4-W5- W6-R13; W1 está ausente o es alquilenilo C1-4, alquenilenilo C2-4, alquinilenilo C2-4, arilo, heteroarilo, cicloalquilo o heterocicloalquilo, cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados a partir de halogeno, CH, NO2, ON, =NH, =NOH, =NO-(alquilo C1-4), haloalquilo C1-4, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4 o dialquilamino C2-8; W2 está ausente o es alquilenilo C1-4, alquenilenilo C2-4, alquinilenilo C2-4, O, S, NR12, CO, COO, OCO, C(S), C(S)NR12, -C(=N-CH)-, NR12C(O)O, CONE12, SO, SO2SONR12, SO2NR12 o NR12CONR12, donde dichos alquilenilo C1-4, alquenilenilo C2-4, alquinilenilo C2-4, están cada uno opcionalmente sustituidos con 1, 2 o 3 sustituyentes seleccionados a partir de halogeno, OH, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4 o dialquilamino C2-8; W3 está ausente o es alquilenilo C1-4, alquenilenilo C2-4, alquinilenilo C2-4, arilo, cicloalquilo, heteroarilo o heterocicloalquilo, donde cada uno de dichos alquilenilo C1-4, alquenilenilo C2-4, alquinilenilo C2-4, arilo, cicloalquilo, heteroarilo o heterocicloalquilo está opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados a partir de halogeno, CH, NO2, OH, =NH, =NOH, =NO-(alquilo C1-4), haloalquilo C1-4, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4 o dialquilamino C2-8; W4 está ausente o es alquinilenilo C1-4, alquenilenilo C2-4, alquinilenilo C2-4, O, S, NR12, CO, COO, OCO, -C(=N-CN)-, NR12C(O)O, CONR12, SO, SO2, SONR12, SO2NR12 o NR12CONR12, donde dichos alquinilenilo C1-4, alquinilenilo C2-4, alquenilenilo C2-4, alquinilenilo C2- 4 están, cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados a partir de halogeno CN, NO2, OH, =NH, =NOH, =NO-(alquilo C1-4), haloalquilo C1-4 alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4 o dialquilamino C2-8; W5 está ausente o es C1-4 alquilenilo, C2-4alquenilenilo, C2-4alquinilenilo, arilo, cicloalquilo, heteroarilo o heterocicloalquilo, donde dicho C1-4alquilenilo, C2-4 alquenilenilo, C2-4alquinilenilo, arilo, cicloalquilo, heteroarilo o heterocicloalquilo está opcionalmente sustituido con 1, 2 o 3 sustituyentes halogeno, CN, NO2, OH, =NH, =NOH, =NO-(C1-4 alquilo), C1-4haloalquilo, C1-4 alcoxi, C1-4, haloalcoxi, amino, C1-4 alquilamino o C2-8dialquilamino; W6 está ausente o es alquilo C1-4, alquenilo C2-4, alquinilo C2-4, O, S, NR12, CO, COO, OCO, -C(=N-CN)-, NR12C(O)O, CONR12, SO, SO2, SONR12, SO2NR12 o NR12CONR12, donde dichos alquilo C1-4, alquenilo C2-4, alquinilo C2-4 están, cada uno, opcionalmente sustituidos con 1, 2 o 3 sustituyentes seleccionados a partir de CN, NO2, OH, =NH, =NOH, =NO-(alquilo C1-4), haloalquilo C1-4, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4 o dialquilamino C2-8; Rx es halogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, cicloalquilalquilo, heteroarilalquilo, heterocicloalquilalquilo, CN, NO2, ORa'', SRa'', C(O)Rb'', C(O)NRc''Rd'', C(O)ORa'', OC(O)Rb'', OC(O)NRc''Rd'', NRc''Rd'', NRc''C(O)Rd'', NRc''C(O)ORa'', S(O)Rb'', S(O) NRc''Rd'', S(O)2Rb'', S(O)2NRc''Rd'', -(alquil C1-6)-CN, -(alquil C1-6)-NO2, -(alquil C1-6)-ORa'', -(alquil C1-6)-SRa'', -(alquil C1-6)-C(O)Rb'', -(alquil C1-6)-C(O)Rb'', -(alquil C1-6)-C(O)NRc''Rd'', - (alquil C1-6)-C(O)ORa'', -(alquil C1-6)-OC(O)Rb'', -(alquil C1-6)-OC(O)NRc''Rd'', -(alquil C1-6)-NRc''Rd'', (alquil C1-6)-NRc''C(O)Rd'', (alquil C1-6)-NRc''C(O)ORA'', -(alquil C1-6)-S(O)Rb'', -(alquil C1-6)-S(O)NRc''Rd'', -(alquil C1-6)- S(O)2Rb''o - (alquil C16)-S(O)2NRc''Rd''; R9 es alquilo C1-4, arilo, heteroarilo, cicloalquilo o heterocicloalquilo, cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados a partir de halogeno, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, haloalquilo C1-4, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa', C8O9NRc'Rd', C(O)ORa', OC(O)Rb', OC(O)NRc'Rd', NRc'Rd', NRc'C(O)Rd', NRc'C(O) ORa', S(O)Rb', S(O)NRcRd', S(O)2Rb' y S(O)2NRc'Rd'; R10 es halogeno, CN, NO2, OH, =NH, =NOH, =NO-(alquilo C1-4), haloalquilo C1-4, alcoxi C1-4, haloalcoxi C1-4amino, alquilamino C1-4 o dialquilamino C2-8 o alquilo C1-6 donde dicho alquilo C1-6 está opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados a partir de halogeno, CN NO2, OH, amino, (alquil C1-4)amino, (dialquil C2-8)amino, haloalquilo C1-6, acilo C1-6, aciloxi C1-6, acilamino C1-6 -(alquil C1-6)-CN y -(alquil C1-6)-NO2; R12 y R14 son cada uno independientemente H o alquilo C1-6opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados a partir de OH, CN NO2, amino, (alquil C1-4)amino, (dialquil C2-8)amino, haloalquilo C1-6, aciloxi C1-6, acilamino C1-6, -(alquil C1-6)-CN y -(alquil C1-6)-NO2; R13 es halogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, cicloalquilalquilo, heteroarilalquilo, heterocicloalquilalquilo, CN, NO2, ORa'', SRa'', C(O)RB'', C(O)NRc''Rd'', C(O)ORa'', OC(O)Rb'', OC(O)NRc''Rd'', NRc''Rd'', NRc''C(O)Rd'', NRc''C(O)ORa'', S(O)Rb'', S(O) NRc''Rd'', S(O)2Rb'', S(O)2NRc''Rd'', -(alquil C1-6)-CN, -(alquil C1-6)-ORa'', -(alquil C1-6)-SRa'', -(alquil C1-6)-C(O)Rb'', -(alquil C1-6)-C(O) NRc''Rd'', -(alquil C1-6)-C(O)ORa'', -(alquil C1-6)-OC(O)Rb'', -(alquil C1-6)-OC(O)NRc''Rd'', -(alquil C1-6)-NRc''Rd'', -(alquil C1-6)-NRc''C(O)Rd'', -(alquil C1-6)-NRc''C(O)ORa'',-(alquil C1-06)-S(O)R'', -(alquil C1-6)-S(O)NRc''Rd'', -(alquil C1-6)-S(O)2Rb'' o - (alquil C1-6)-S(O)2NRc''Rd'', donde cada uno de dichos alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, cicloalquilalquilo, heteoarilalquilo o heterocicloalquilalquilo está opcionalmente sustituido con 1, 2, 3 4 o 5 sustituyentes independientemente seleccionados a partir de: alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, cicloalquilalquilo, heteroarilalquilo, heterocicloalquilalquilo, halogeno, CN, NO2, ORa'', SRa'', C(O)Rb'', C(O) NRc''Rd'', C(O)ORa'', OC(O)Rb'', OC(O)NRc''Rd'', NRc''Rd'', NRc''Rd'', NRc''C(O)ORa'', S(O)Rb'', S(O)NRc''Rd'', S(O)2Rb'', S(O)2Rc''Rd'', -(alquil C1-6)-CN, -(alquil C1-6)-NO2, -(alquil C1-6)-ORa'', -(alquil C1-6)-SRa'', -(alquil C1-6)-C(O)Rb'', -(alquil C1-6)-C(O)NRc''Rd'', -(alquil C1-6)-C(O) ORa'', -(alquil C1-6)-OC(O)Rb'', -(alquil C1-6)-OC(O)NRc''Rd'', -(alquil C1-6)-NRc''Rd'', - (alquil C1-6)-NRc''C(O)Rd'', -(alquil C1-6)-NRc''C(O) ORa'', -(alquil C1-6)-S(O)Rb'', -alquil C1-6)-S(O)NRc''Rd'', -(alquil C1-6)-S(O)2Rb'' y -(alquil C1-6)- S(O)2NRc''Rd''; Ra, Ra' y Ra'' son cada uno independientemente, H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo o heterocicloalquilo; Rb, Rb'y Rb''son cada uno, independientemente, H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo o heterocicloalquilo; Rb, Rb' y Rb'' son cada uno, independientemente, H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo o heterocicloalquilo; Rc y Rd son cada uno, independientemente, H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, arilalquilo o cicloalquilalquilo; o Rc y Rd junto con el átomo de N atom con el cual están unidos forman un grupo heterocicloalquilo de 4-5-6 o 7 miembros; Rc' y Rd' son cada uno, independientemente, H, alquilo C1-6, haloalquilo C16, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, arilalquilo o cicloalquilalquilo; o Rc' y Rd' junto con el átomo de N atom con el cual están unidos forman un grupo heterocicloalquilo de 4-, 5-, 6-, o 7 miembros; y Rc'' y Rd'' son cada uno, independientemente, h, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, arilalquilo o cicloalquilalquilo; o Rc'' y Rd'' junto con el átomo de N atom con el cual están unidos forman un grupo heterocicloalquilo de 4-, 5-, 6- o 7 miembros.
ARP050105384A 2004-12-22 2005-12-20 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. AR054416A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US63847404P 2004-12-22 2004-12-22
US72628905P 2005-10-13 2005-10-13

Publications (1)

Publication Number Publication Date
AR054416A1 true AR054416A1 (es) 2007-06-27

Family

ID=36602272

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050105384A AR054416A1 (es) 2004-12-22 2005-12-20 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.

Country Status (18)

Country Link
US (7) US7335667B2 (es)
EP (2) EP2671882B1 (es)
JP (2) JP5048514B2 (es)
AR (1) AR054416A1 (es)
CA (1) CA2592119C (es)
CY (1) CY1120257T1 (es)
DK (1) DK2671882T3 (es)
ES (2) ES2536331T3 (es)
HR (1) HRP20180578T1 (es)
HU (1) HUE037435T2 (es)
LT (1) LT2671882T (es)
ME (1) ME03017B (es)
PL (1) PL2671882T3 (es)
PT (1) PT2671882T (es)
RS (1) RS57302B1 (es)
SI (1) SI2671882T1 (es)
TW (2) TW201414732A (es)
WO (1) WO2006069080A2 (es)

Families Citing this family (132)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005105814A1 (en) * 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
JP2008508358A (ja) 2004-08-02 2008-03-21 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド アリール−アミノ置換ピロロピリミジンマルチキナーゼ阻害化合物
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.
US7884109B2 (en) 2005-04-05 2011-02-08 Wyeth Llc Purine and imidazopyridine derivatives for immunosuppression
ZA200710379B (en) * 2005-05-20 2009-05-27 Vertex Pharma Pyrrolopyridines useful as inhibitors of protein kinase
US8163767B2 (en) 2005-07-14 2012-04-24 Astellas Pharma Inc. Heterocyclic Janus Kinase 3 inhibitors
EP2251341A1 (en) * 2005-07-14 2010-11-17 Astellas Pharma Inc. Heterocyclic Janus kinase 3 inhibitors
US20070149506A1 (en) 2005-09-22 2007-06-28 Arvanitis Argyrios G Azepine inhibitors of Janus kinases
SI3184526T1 (sl) 2005-12-13 2019-03-29 Incyte Holdings Corporation Derivati pirolo(2,3-D)pirimidina kot inhibitorji Janus kinaze
US7989459B2 (en) 2006-02-17 2011-08-02 Pharmacopeia, Llc Purinones and 1H-imidazopyridinones as PKC-theta inhibitors
US7919490B2 (en) 2006-10-04 2011-04-05 Wyeth Llc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
US7902187B2 (en) 2006-10-04 2011-03-08 Wyeth Llc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
WO2008043019A1 (en) 2006-10-04 2008-04-10 Pharmacopeia, Inc 8-substituted 2-(benzimidazolyl) purine derivatives for immunosuppression
WO2008060301A1 (en) * 2006-11-16 2008-05-22 Pharmacopeia , Llc 7-substituted purine derivatives for immunosuppression
JP2010510227A (ja) 2006-11-20 2010-04-02 プレジデント アンド フェロウズ オブ ハーバード カレッジ 痛みおよび痒みの治療方法、組成物およびキット
US8071779B2 (en) * 2006-12-18 2011-12-06 Inspire Pharmaceuticals, Inc. Cytoskeletal active rho kinase inhibitor compounds, composition and use
US20100022517A1 (en) * 2006-12-18 2010-01-28 Richards Lori A Ophthalmic formulation of rho kinase inhibitor compound
EP2121692B1 (en) 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
CA2673683C (en) 2007-01-11 2014-07-29 Critical Outcome Technologies, Inc. Compounds and method for treatment of cancer
CA2675288A1 (en) * 2007-01-12 2008-07-17 Astellas Pharma Inc. Condensed pyridine compound
US8063094B2 (en) 2007-02-08 2011-11-22 Boehringer Ingelheim International Gmbh Anti-cytokine heterocyclic compounds
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.
MX2009013402A (es) 2007-06-13 2010-02-24 Incyte Corp Sales de inhibidor de janus cinasa (r)-3-(4-(7h-pirrolo[2,3-d]piri midin-4-il)-1h-pirazol-1-il)-3-ciclopentilpropanitrilo.
DE102007027800A1 (de) * 2007-06-16 2008-12-18 Bayer Healthcare Ag Substituierte bicyclische Heteroaryl-Verbindungen und ihre Verwendung
US8309718B2 (en) * 2007-11-16 2012-11-13 Incyte Corporation 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines as janus kinase inhibitors
EP2225226B1 (en) 2007-12-26 2016-08-17 Critical Outcome Technologies, Inc. Compounds and their use in a method for treatment of cancer
CN102026999B (zh) * 2008-03-11 2014-03-05 因塞特公司 作为jak抑制剂的氮杂环丁烷和环丁烷衍生物
PE20110063A1 (es) * 2008-06-20 2011-02-16 Genentech Inc DERIVADOS DE [1, 2, 4]TRIAZOLO[1, 5-a]PIRIDINA COMO INHIBIDORES DE JAK
CA2727036C (en) * 2008-06-20 2017-03-21 Genentech, Inc. Triazolopyridine jak inhibitor compounds and methods
WO2010006438A1 (en) 2008-07-17 2010-01-21 Critical Outcome Technologies Inc. Thiosemicarbazone inhibitor compounds and cancer treatment methods
BRPI0916931A2 (pt) * 2008-08-01 2015-11-24 Biocryst Pharm Inc agentes terapêuticos
HRP20140395T1 (hr) 2008-08-20 2014-06-06 Zoetis Llc SPOJEVI PIROLO[2,3-d]PIRIMIDINA
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
WO2010093808A1 (en) * 2009-02-11 2010-08-19 Reaction Biology Corp. Selective kinase inhibitors
AU2010237859A1 (en) * 2009-04-14 2011-11-03 Astellas Pharma Inc. Fused pyrrolopyridine derivative
WO2010135650A1 (en) * 2009-05-22 2010-11-25 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
WO2010135621A1 (en) 2009-05-22 2010-11-25 Incyte Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak 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
EP2451944A4 (en) 2009-07-10 2012-11-28 Harvard College PERMANENTLY CHARGED SODIUM AND CALCIUM CHANNEL BLOCKERS AS ANTI-INFLAMMATORY AGENTS
TWI466885B (zh) * 2009-07-31 2015-01-01 Japan Tobacco Inc 含氮螺環化合物及其醫藥用途
CN102066372B (zh) 2009-08-24 2014-09-17 苏州爱斯鹏药物研发有限责任公司 含脲基的5，6元杂芳双环化合物作为激酶抑制剂
TW201113285A (en) * 2009-09-01 2011-04-16 Incyte Corp 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.
CN102574860A (zh) * 2009-10-15 2012-07-11 辉瑞大药厂 吡咯并[2,3-d]嘧啶化合物
EP2519525A4 (en) 2009-12-30 2013-06-12 Arqule Inc SUBSTITUTED PYRROLO-AMINOPYRIMIDINE COMPOUNDS
AU2011217961B2 (en) 2010-02-18 2016-05-05 Incyte Holdings Corporation Cyclobutane and methylcyclobutane derivatives as Janus kinase inhibitors
WO2011109217A2 (en) * 2010-03-02 2011-09-09 Immunodiagnostics, Inc. Methods of treating or preventing rna polymerase dependent viral disorders by administration of jak2 kinase inhibitors
PE20130038A1 (es) 2010-03-10 2013-01-28 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de jak1
CA2794952C (en) 2010-04-01 2018-05-15 Critical Outcome Technologies Inc. Compounds and method for treatment of hiv
SG10201503983QA (en) 2010-05-21 2015-06-29 Incyte Corp Topical Formulation for a JAK Inhibitor
WO2012054364A2 (en) * 2010-10-22 2012-04-26 Merck Sharp & Dohme Corp. Bicyclic diamines as janus kinase inhibitors
BR112013012502A2 (pt) 2010-11-19 2019-03-06 Incyte Corporation pirrolopiridina ciclobutil substituída e derivados de pirrolopirimidina derivativos como inibidores de jak
EP2640725B1 (en) 2010-11-19 2015-01-07 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
MX2013007792A (es) * 2011-01-07 2013-07-30 Leo Pharma As Nuevos derivados de sulfamida piperazina como inhibidores de proteina tirosina cinasa y uso farmaceutico de los mismos.
CA2827673C (en) 2011-02-18 2020-10-27 Novartis Pharma Ag Mtor/jak inhibitor combination therapy
AU2012241018B2 (en) * 2011-04-08 2015-11-12 Pfizer Inc. Crystalline and non- crystalline forms of tofacitinib, and a pharmaceutical composition comprising tofacitinib and a penetration enhancer
EP2721028B1 (en) 2011-06-20 2015-11-04 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
WO2013023119A1 (en) 2011-08-10 2013-02-14 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
MX2014006479A (es) 2011-11-30 2015-01-22 Univ Emory Inhibidores antivirales de la janus cinasa utiles en el tratamiento o prevencion de infecciones retrovirales y otras infecciones virales.
ES2682755T3 (es) * 2011-12-21 2018-09-21 Jiangsu Hengrui Medicine Co. Ltd. Derivado del anillo heteroarilo de seis miembros de pirrol, método de preparación del mismo y sus usos medicinales
AR091079A1 (es) 2012-05-18 2014-12-30 Incyte Corp Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak
CA2880896C (en) 2012-06-26 2021-11-16 Del Mar Pharmaceuticals Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof
WO2014071031A1 (en) 2012-11-01 2014-05-08 Incyte Corporation Tricyclic fused thiophene derivatives as jak inhibitors
PL2919766T3 (pl) 2012-11-15 2021-10-04 Incyte Holdings Corporation Postacie dawkowania ruksolitynibu o przedłużonym uwalnianiu
US10130632B2 (en) 2012-11-27 2018-11-20 Beth Israel Deaconess Medical Center, Inc. Methods for treating renal disease
US9260426B2 (en) 2012-12-14 2016-02-16 Arrien Pharmaceuticals Llc Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
CN103896946B (zh) * 2012-12-28 2018-04-03 浙江导明医药科技有限公司 用于预防及治疗多种自身免疫疾病的新化合物
WO2014113303A1 (en) * 2013-01-16 2014-07-24 Merck Sharp & Dohme Corp. 4-fluoropiperidine orexin receptor antagonists
PE20151764A1 (es) 2013-02-22 2015-12-03 Pfizer Derivados de pirrolo[2,3-d]pirimidina
EP3489239B1 (en) 2013-03-06 2021-09-15 Incyte Holdings Corporation Processes and intermediates for making a jak inhibitor
LT3030227T (lt) 2013-08-07 2020-06-10 Incyte Corporation Prailginto atpalaidavimo jak1 inhibitoriaus dozavimo formos
WO2015027090A1 (en) * 2013-08-22 2015-02-26 Genentech, Inc. Intermediates and processes for preparing compounds
WO2015027092A1 (en) * 2013-08-22 2015-02-26 Genentech, Inc. Process for preparing a compound
EP3318565B1 (en) * 2013-12-05 2021-04-14 Pfizer Inc. Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides
EP2924026A1 (en) 2014-03-28 2015-09-30 Novartis Tiergesundheit AG Aminosulfonylmethylcyclohexanes as JAK inhibitors
SG10201809518QA (en) 2014-04-30 2018-11-29 Incyte Corp Processes of preparing a jak1 inhibitor and new forms thereto
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
ES2750655T3 (es) 2014-08-12 2020-03-26 Pfizer Derivados de pirrolo[2,3-d]pirimidina útiles para inhibir la Janus cinasa
KR20180069782A (ko) 2015-08-03 2018-06-25 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 하전 이온 채널 블록커 및 이용 방법
KR101771219B1 (ko) 2015-08-21 2017-09-05 양지화학 주식회사 야누스 키나제 1 선택적 억제제 및 그 의약 용도
US10045981B2 (en) 2015-11-24 2018-08-14 Jakpharm, Llc Selective kinase inhibitors
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
JP2019530650A (ja) 2016-08-24 2019-10-24 アークル インコーポレイテッド アミノ−ピロロピリミジノン化合物およびその使用方法
EP3528816A4 (en) * 2016-10-21 2020-04-08 Nimbus Lakshmi, Inc. TYK2 INHIBITORS AND USES THEREOF
US10851116B2 (en) * 2017-01-20 2020-12-01 Leo Pharma A/S Bicyclic amines as novel JAK kinase inhibitors
JP2020509004A (ja) * 2017-02-27 2020-03-26 ヤンセン ファーマシューティカ エヌ．ベー． Ｏｇａ阻害剤としての、ピペリジン、モルホリンまたはピペラジンで置換されている［１，２，４］−トリアゾロ［１，５−ａ］−ピリミジニル誘導体
MX2020004946A (es) 2017-11-03 2020-09-25 Aclaris Therapeutics Inc Inhibidores jak de pirrolopiridina sustituidos y metodos para producir y utilizar los mismos.
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
MX2020007973A (es) 2018-01-30 2020-12-07 Incyte Corp Procesos para preparar (1-(3-fluoro-2-(trifluorometil)isonicotinil )piperidin-4-ona).
KR20240157777A (ko) 2018-02-16 2024-11-01 인사이트 코포레이션 사이토카인-관련 장애의 치료를 위한 jak1 경로 억제제
SI3773593T1 (sl) 2018-03-30 2024-08-30 Incyte Corporation Zdravljenje hidradenitisa suppurative z zaviralci jak
MA52655A (fr) 2018-03-30 2021-02-17 Incyte Corp Biomarqueurs pour maladie cutanée inflammatoire
MA52208A (fr) 2018-04-13 2021-02-17 Incyte Corp Biomarqueurs pour une maladie du greffon contre l'hôte
JP7591500B2 (ja) 2018-08-10 2024-11-28 アクラリス セラピューティクス，インコーポレイテッド ピロロピリミジンｉｔｋ阻害剤
EA202191170A1 (ru) 2018-10-31 2021-07-27 Инсайт Корпорейшн Комбинированная терапия для лечения гематологических заболеваний
US11168093B2 (en) 2018-12-21 2021-11-09 Celgene Corporation Thienopyridine inhibitors of RIPK2
NL2022471B1 (en) 2019-01-29 2020-08-18 Vationpharma B V Solid state forms of oclacitinib
US10786485B1 (en) 2019-03-11 2020-09-29 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
SG11202109720WA (en) 2019-03-11 2021-10-28 Nocion Therapeutics Inc Charged ion channel blockers and methods for use
US10780083B1 (en) 2019-03-11 2020-09-22 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
MA55320A (fr) 2019-03-11 2022-01-19 Nocion Therapeutics Inc Bloqueurs de canaux ioniques substitués par un ester et méthodes d'utilisation
CN113811305A (zh) 2019-03-11 2021-12-17 诺西恩医疗公司 带电的离子通道阻滞剂及其使用方法
EP3942045A1 (en) 2019-03-21 2022-01-26 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
PH12021552036A1 (en) 2019-05-02 2022-05-23 Aclaris Therapeutics Inc Substituted pyrrolopyridines as jak inhibitors
US20220235043A1 (en) * 2019-07-31 2022-07-28 Aclaris Therapeutics, Inc. Substituted sulfonamide pyrrolopyridines as jak inhibitors
WO2021062163A1 (en) 2019-09-27 2021-04-01 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
US12203942B2 (en) 2019-10-10 2025-01-21 Incyte Corporation Biomarkers for graft-versus-host disease
US12360120B2 (en) 2019-10-10 2025-07-15 Incyte Corporation Biomarkers for graft-versus-host disease
US10933055B1 (en) 2019-11-06 2021-03-02 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
JP7628539B2 (ja) 2019-11-06 2025-02-10 ノシオン セラピューティクス，インコーポレイテッド 荷電したイオンチャンネル遮断薬および使用方法
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
AU2020388638A1 (en) 2019-11-22 2022-06-30 Incyte Corporation Combination therapy comprising an ALK2 inhibitor and a JAK2 inhibitor
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
US11332446B2 (en) 2020-03-11 2022-05-17 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
US12162851B2 (en) 2020-03-11 2024-12-10 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
CA3177830A1 (en) 2020-05-13 2021-11-18 Maria BECONI Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
EP4200300A1 (en) 2020-08-18 2023-06-28 Incyte Corporation Process and intermediates for preparing a jak inhibitor
AR123268A1 (es) 2020-08-18 2022-11-16 Incyte Corp Proceso e intermediarios para preparar un inhibidor de jak1
CA3191607A1 (en) * 2020-09-08 2022-03-17 Gilles Ouvry Novel jak inhibitor compounds, method for synthesizing same and use thereof
AU2021341899A1 (en) * 2020-09-11 2023-05-25 Galderma Holding SA Novel jak inhibitor compounds, method for synthesizing same and use thereof
EP4259131A1 (en) 2020-12-08 2023-10-18 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
US20240166651A1 (en) * 2021-03-15 2024-05-23 Chiesi Farmaceutici S.P.A. Heterocyclic derivatives as janus kinase inhibitors
TW202308610A (zh) 2021-05-03 2023-03-01 美商英塞特公司 用於治療結節性癢疹之ｊａｋ１途徑抑制劑
US20240309095A1 (en) 2021-07-07 2024-09-19 Incyte Corporation Anti-b7-h4 antibodies and uses thereof
EP4370504A1 (en) 2021-07-12 2024-05-22 Incyte Corporation Process and intermediates for preparing baricitinib
CR20240277A (es) 2021-12-08 2024-08-07 Incyte Corp Anticuerpos anti-calreticulina (calr) mutante y usos de estos
WO2024186610A1 (en) 2023-03-06 2024-09-12 Zoetis Services Llc Topical compositions containing a janus kinase inhibitor
WO2025096716A1 (en) 2023-11-01 2025-05-08 Incyte Corporation Anti-mutant calreticulin (calr) antibody-drug conjugates and uses thereof

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3036390A1 (de) * 1980-09-26 1982-05-13 Troponwerke GmbH & Co KG, 5000 Köln Neue pyrrolo-pyrimidine, verfahren zu ihrer herstellung und ihre verwendung bei der herstellung von biologischen wirkstoffen
KR0133372B1 (ko) * 1991-09-06 1998-04-23 고야 다다시 4-아미노(알킬)시클로헥산-1-카르복사미드 화합물 및 그 용도
IL128456A0 (en) * 1996-08-12 2000-01-31 Yoshitomi Pharmaceutical Compositions containing a Rho kinase inhibitor
JPH11130751A (ja) * 1997-10-30 1999-05-18 Yoshitomi Pharmaceut Ind Ltd アミド化合物およびそれらの酸付加塩の標識化合物
KR20010052570A (ko) 1998-06-04 2001-06-25 스티븐 에프. 웨인스톡 세포 유착을 억제하는 소염성 화합물
US6232320B1 (en) 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
TW505646B (en) * 1998-06-19 2002-10-11 Pfizer Prod Inc Pyrrolo [2,3-d] pyrimidine compounds
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
US6080747A (en) 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
PT1382339E (pt) * 1999-12-10 2008-02-06 Pfizer Prod Inc Composições que contêm derivados de pirrolo[2,3-d]- pirimidina
HK1050191B (en) 1999-12-24 2011-04-29 Aventis Pharma Limited Azaindoles
US6335342B1 (en) * 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
DE60141963D1 (de) * 2000-06-23 2010-06-10 Mitsubishi Tanabe Pharma Corp Antitumoreffekt-verstärker
ES2257410T3 (es) * 2000-06-26 2006-08-01 Pfizer Products Inc. Compuestos de pirrolo(2,3-d)pirimidina como agentes inmunosupresores.
CA2436487A1 (en) 2001-01-30 2002-08-08 Cytopia Pty Ltd. Methods of inhibiting kinases
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
GB0115109D0 (en) * 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
GT200200234A (es) 2001-12-06 2003-06-27 Compuestos cristalinos novedosos
WO2003099796A1 (en) 2002-05-23 2003-12-04 Cytopia Pty Ltd Protein kinase inhibitors
KR20050086784A (ko) 2002-11-26 2005-08-30 화이자 프로덕츠 인크. 이식 거부반응의 치료 방법
SE0301372D0 (sv) * 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301373D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
CA2545192A1 (en) 2003-11-25 2005-06-09 Pfizer Products Inc. Method of treatment of atherosclerosis
WO2005060972A2 (en) 2003-12-17 2005-07-07 Pfizer Products Inc. Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection
WO2005069865A2 (en) * 2004-01-13 2005-08-04 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
WO2005105814A1 (en) 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
JP2007536310A (ja) 2004-05-03 2007-12-13 ノバルティス アクチエンゲゼルシャフト Ｓ１ｐ受容体アゴニストおよびｊａｋ３キナーゼ阻害剤を含む、組合せ剤
WO2006013114A1 (en) 2004-08-06 2006-02-09 Develogen Aktiengesellschaft Use of a timp-2 secreted protein product for preventing and treating pancreatic diseases and/or obesity and/or metabolic syndrome
MX2007006204A (es) 2004-11-24 2007-06-20 Novartis Ag Combinaciones que comprenden inhibidores de jak y cuando menos uno de entre inhibidores de bcr-abl, flt-3, fak o raf cinasa.
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.
SI3184526T1 (sl) 2005-12-13 2019-03-29 Incyte Holdings Corporation Derivati pirolo(2,3-D)pirimidina kot inhibitorji Janus kinaze

Also Published As

Publication number Publication date
JP5048514B2 (ja) 2012-10-17
ME03017B (me) 2018-10-20
CA2592119A1 (en) 2006-06-29
WO2006069080A3 (en) 2007-07-05
US20170349579A1 (en) 2017-12-07
TW201414732A (zh) 2014-04-16
US8053433B2 (en) 2011-11-08
JP2012140469A (ja) 2012-07-26
US20150315185A1 (en) 2015-11-05
ES2536331T3 (es) 2015-05-22
EP1828181B1 (en) 2015-02-18
EP2671882B1 (en) 2018-02-21
US20140228346A1 (en) 2014-08-14
JP5970676B2 (ja) 2016-08-17
US20110086835A1 (en) 2011-04-14
EP2671882A1 (en) 2013-12-11
DK2671882T3 (en) 2018-03-26
EP1828181A2 (en) 2007-09-05
ES2666819T3 (es) 2018-05-08
HUE037435T2 (hu) 2018-08-28
JP2008525463A (ja) 2008-07-17
HRP20180578T1 (hr) 2018-06-29
US8741895B2 (en) 2014-06-03
RS57302B1 (sr) 2018-08-31
SI2671882T1 (en) 2018-06-29
PL2671882T3 (pl) 2018-08-31
CY1120257T1 (el) 2019-07-10
US7335667B2 (en) 2008-02-26
TW200634010A (en) 2006-10-01
US20120014989A1 (en) 2012-01-19
US9879010B2 (en) 2018-01-30
WO2006069080A2 (en) 2006-06-29
US20130296299A1 (en) 2013-11-07
EP1828181A4 (en) 2010-08-25
US9090611B2 (en) 2015-07-28
LT2671882T (lt) 2018-06-25
TWI439459B (zh) 2014-06-01
US9580419B2 (en) 2017-02-28
CA2592119C (en) 2014-07-15
HK1108443A1 (en) 2008-05-09
PT2671882T (pt) 2018-04-20
US20060183906A1 (en) 2006-08-17
US8445488B2 (en) 2013-05-21

Similar Documents

Publication Publication Date Title
AR054416A1 (es) 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.
ES2561507T3 (es) Pirrolo[2,3-b]piridinas y pirrolo[2,3-b]pirimidinas sustituidas con heteroarilo como inhibidores de quinasas Janus
DE60043349D1 (de) Chinazolin-derivate und ihre verwendung als arzneimittel
CO5700725A2 (es) Derivados sustituidos de la ciclohexano-1,4-diamina
AR073530A1 (es) Inhibidores de janus quinasas para el tratamiento de ojo seco y otras enfermedades relacionadas con los ojos. inserto oftalmico
AR076052A1 (es) Derivados de pirimidinas sustituidas, composiciones farmaceuticas que los contienen y uso de los mismos en trastornos asociados con receptores de histamina h4, tales como trastornos inflamatorios, prurito y dolor.
CA2545427A1 (en) Selective kinase inhibitors
PE20030890A1 (es) Cumarinas utiles como biomarcadores
CO5080780A1 (es) Derivado de amida y antagonista de nociceptina
PE106499A1 (es) Antagonistas del receptor ccr-3
RU2009128591A (ru) Лиганды для визуализации иннервации сердца
PE20020976A1 (es) Pirido-pirimidinas 6-sustituidas como inhibidores de quinasas
EA200900934A1 (ru) НОВЫЕ ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ NF-κB
AR036093A1 (es) Compuestos derivados de tiazolidinilo, pirrolidinilo, oxazolidinilo, piperidilo, morfolinilo y tiomorfolinilo, su uso, composiciones farmaceuticas que los comprenden, y compuestos intermediarios
AR037816A1 (es) Fenil derivados sustituidos
ES2092316T3 (es) Agentes antianginosos de purinona.
AR057131A1 (es) Derivados de purina como inmunomodulador
AR049543A1 (es) Derivados de la 1-amino-ftalazina, su preparacion y su aplicacion en terapeutica
HRP20080493T3 (hr) Supstituirani kinolinski derivati kao mitotski inhibitori kinezina
AR037907A1 (es) Derivados de azaindolilalquilamina como ligandos de 5-hidroxitriptamina-6
CO6150178A2 (es) Derivados de pirazol como inhibidores de la citocromooxidasa p450
HRP20130918T1 (hr) Derivati 4-aminopirimidina kao receptori antagonista histamina h4
AR037906A1 (es) Derivados de indolilalquilamina como ligandos de 5-hidroxitriptamina-6
SE0101579D0 (sv) New compounds
AR039988A1 (es) Derivados de benzoxazina como moduladores de 5-ht6 y usos de los mismos

Legal Events

Date Code Title Description
FA Abandonment or withdrawal