AR112348A1 - Compuestos bicíclicos de pirazolo y triazolo como inhibidores de quinasas jak - Google Patents

Compuestos bicíclicos de pirazolo y triazolo como inhibidores de quinasas jak

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Publication number
AR112348A1
AR112348A1 ARP180102151A AR112348A1 AR 112348 A1 AR112348 A1 AR 112348A1 AR P180102151 A ARP180102151 A AR P180102151A AR 112348 A1 AR112348 A1 AR 112348A1
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Argentina
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group
alkyl
independently selected
optionally
alkoxy
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Miroslav Rapta
Venkat R Thalladi
Marta Dabros
Jerry Nzerem
Breena Fraga
Diana Jin Wang
Anthony Francesco Palermo
Robert Murray Mkinnell
Mandy Loo
Tom M Lam
Erik Fenster
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Theravance Biopharma R&D Ip Llc
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Publication of AR112348A1 publication Critical patent/AR112348A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/4161,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde: X¹ y X² se seleccionan, cada uno independientemente, entre N y CH; X³ se selecciona entre el grupo que consiste en N, CH, C-CH₃, C-CF₃, C-CHF₂, C-CH₂-O-CH₃, C-SMe, C-NMe₂, C-NH-CH₃, C-Cl, C-CN, y C-OMe; el resto de fórmula (2) se selecciona entre el grupo que consiste en los compuestos del grupo de fórmulas (3); Rᵃ, Rᵇ, Rᶜ, y Rᶠ se seleccionan, cada uno independientemente, entre el grupo que consiste en H y alquilo C₁₋₃; Rᵈ, Rᵉ, Rᵍ, Rʰ, Rⁱ, Rʲ, Rˡ, Rᵐ, Rⁿ y Rᵒ se seleccionan, cada uno independientemente, entre el grupo que consiste en H y alquilo C₁₋₃, en donde el grupo alquilo C₁₋₃ puede estar opcionalmente sustituido con 1 a 3 halógenos; opcionalmente, Rᵈ y Rᵉ pueden unirse para formar un anillo de ciclopropilo; A se selecciona entre el grupo que consiste en: (a) un grupo heterocíclico monocíclico de 4 a 10 miembros que contiene un átomo de nitrógeno y que opcionalmente contiene un heteroátomo adicional seleccionado entre N, S, S(O)₂ y O, y (b) un grupo heterocíclico multicíclico de 6 a 10 miembros que contiene un átomo de nitrógeno y que opcionalmente contiene un heteroátomo adicional seleccionado entre N, S, y O, en donde L está ligado a un átomo de carbono en A, y A está opcionalmente sustituido con 1 a 3 grupos Rᵏ; cada Rᵏ se selecciona independientemente entre el grupo que consiste en F, CN, alcoxi C₁₋₃, ciclopropilo, y alquilo C₁₋₃, en donde el grupo alquilo C₁₋₃ puede estar opcionalmente sustituido con OH, OMe o 1 a 3 halógenos; R¹ se selecciona entre el grupo que consiste en los compuestos del grupo de fórmulas (4), en donde Rᵖ y Rq se seleccionan, cada uno independientemente, entre el grupo que consiste en H, cicloalquilo C₃₋₅ y alquilo C₁₋₆, en donde el grupo alquilo C₁₋₆ puede estar opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados entre el grupo que consiste en alcoxi C₁₋₃ y -S-alquilo C₁₋₃, o Rᵖ y Rq forman un grupo heterocíclico monocíclico de 4 a 6 miembros que contiene un átomo de nitrógeno y que opcionalmente contiene un heteroátomo adicional seleccionado entre N, S, y O, en donde el grupo heterocíclico monocíclico de 4 a 6 miembros está opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados entre el grupo que consiste en alquilo C₁₋₆, alcoxi C₁₋₃, -S-alquilo C₁₋₃ y alquilo C₁₋₃-alcoxi C₁₋₃; R² se selecciona entre el grupo que consiste en H, Cl, OMe, Me y F; R³ se selecciona entre el grupo que consiste en H y F; R⁴ se selecciona entre el grupo que consiste en H y F; y R⁵ se selecciona entre el grupo que consiste en H, Me y F.
ARP180102151 2017-08-01 2018-07-31 Compuestos bicíclicos de pirazolo y triazolo como inhibidores de quinasas jak AR112348A1 (es)

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US201762539642P 2017-08-01 2017-08-01

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US (4) US10392368B2 (es)
EP (1) EP3652169A1 (es)
JP (2) JP7098716B2 (es)
KR (1) KR20200036004A (es)
CN (1) CN111032646B (es)
AR (1) AR112348A1 (es)
AU (1) AU2018312349A1 (es)
BR (1) BR112020002265A2 (es)
CA (1) CA3069990A1 (es)
CL (1) CL2020000283A1 (es)
CO (1) CO2020001469A2 (es)
EA (1) EA038912B1 (es)
IL (1) IL272031A (es)
MA (1) MA49570A (es)
MX (1) MX2020001170A (es)
MY (1) MY200629A (es)
PE (1) PE20201028A1 (es)
PH (1) PH12020500201A1 (es)
SG (1) SG11202000602YA (es)
TW (1) TW201920150A (es)
UA (1) UA125318C2 (es)
WO (1) WO2019027960A1 (es)
ZA (1) ZA202000561B (es)

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