AR071729A1 - Inhibidores de quinasas simil polo (plk) - Google Patents

Inhibidores de quinasas simil polo (plk)

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Publication number
AR071729A1
AR071729A1 ARP080104179A ARP080104179A AR071729A1 AR 071729 A1 AR071729 A1 AR 071729A1 AR P080104179 A ARP080104179 A AR P080104179A AR P080104179 A ARP080104179 A AR P080104179A AR 071729 A1 AR071729 A1 AR 071729A1
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AR
Argentina
Prior art keywords
alkyl
cycloalkyl
heterocycloalkyl
heterobicycloaryl
bicycloaryl
Prior art date
Application number
ARP080104179A
Other languages
English (en)
Inventor
Benjamin Jones
Stephen W Kaldor
Victoria Feher
Sheldon X Cao
Takashi Ichikawa
Betty Lam
Yan Liu
Andre A Kiryanov
Christopher Mcbrid
Original Assignee
Takeda Pharmaceutical
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40219644&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR071729(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Takeda Pharmaceutical filed Critical Takeda Pharmaceutical
Publication of AR071729A1 publication Critical patent/AR071729A1/es

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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
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  • Health & Medical Sciences (AREA)
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  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Dermatology (AREA)
  • Neurosurgery (AREA)
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  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychiatry (AREA)
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  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)

Abstract

Tambien se proveen composiciones farmaceuticas, kits y art¡culos de fabricacion que comprenden tales compuestos; metodos e intermediarios de utilidad para preparar los compuestos; y metodos de uso de dichos compuestos. Reivindicacion 1: Un compuesto de la formula (1) y sus sales farmaceuticamente aceptables, caracterizado porque W est  seleccionado del grupo que consiste en CR8 y N; Y es -(CR9R10)n-; n est  seleccionado del grupo que consiste en 1, 2, 3 y 4; L est  ausente o es un ligador que provee 1, 2, 3, 4, 5 o 6 separaciones de  tomos entre R7 y el nitrogeno al que L est  unido, en donde los  tomos del ligador que proveen la separacion est n seleccionados del grupo que consiste en carbono, ox¡geno, nitrogeno y azufre; R1 est  seleccionado del grupo que consiste en hidrogeno, ciano, tio, hidroxi, carboniloxi, alcoxi, ariloxi, heteroariloxi, carbonilo, oxicarbonilo, amido, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-3, tiocarbonilalquilo C1-3, sulfonilalquilo C1-3, sulfinilalquilo C1-3, azaalquilo C1-10, iminoalquilo C1-3, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-5, arilalquilo C1-10, heteroarilalquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R2 est  seleccionado del grupo que consiste en hidrogeno, carbonilo, oxicarbonilsulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, carbonilalquilo C1-3, tiocarbonilalquilo C1-3, sulfonilalquilo C1-3, sulfinilalquilo C1-3, azaalquilo C1-10, iminoalquilo C1-3, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-5, arilalquilo C1-10, heteroarilalquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido o R2 y R1 o R14 se toman juntos para formar un anillo sustituido o no sustituido; R3 es hidrogeno o un sustituyente convertible en vivo en hidrogeno; R4 es halo; R5 est  seleccionado del grupo que consiste en hidrogeno, halo, nitro, ciano, tio, oxi, hidroxi, carboniloxi, alcoxi C1-10, aril C4-12-oxi, heteroaril C1-10-oxi, carbonilo, oxicarbonilo, amido, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, iminoalquilo C1-10, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-10, arilalquilo C1-10, heteroaril C1-10-alquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R6 est  seleccionado del grupo que consiste en hidrogeno, carbonilo, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, carbonilalquilo C1-3, tiocarbonilalquilo C1-3, sulfonilalquilo C1-3, sulfinilalquilo C1-3, azaalquilo C1-10, iminoalquilo C1-3, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-5, arilalquilo C1-10, heteroarilalquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R7 est  seleccionado del grupo que consiste en cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R8 est  seleccionado del grupo que consiste en hidrogeno, halo, nitro, ciano, tio, oxi, hidroxi, carboniloxi, alcoxi, ariloxi, heteroariloxi, carbonilo, oxicarbonilo, amido, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-3, tiocarbonilalquilo C1-3, sulfonilalquilo C1-3, sulfinilalquilo C1-3, azaalquilo C1-10, iminoalquilo C1-3, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-5, arilalquilo C1-10, heteroarilalquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R9 y R10 est n seleccionados cada uno, de modo independiente, del grupo que consiste en hidrogeno, halo, nitro, ciano, tio, oxi, hidroxi, carboniloxi, alcoxi C1-10, aril C4-2-oxi, heteroaril C1-10-oxi, carbonilo, oxicarbonilo, amido, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, iminoalquilo C1-10, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-10, arilalquilo C1-10, heteroaril C1-10-alquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido o R9 y R10 se toman juntos con el carbono al que est n unidos para formar C=O, C=S, C=NR11 o C=CR12R13; R11 est  seleccionado del grupo que consiste en hidrogeno, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, iminoalquilo C1-10, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-10, arilalquilo C1-10, heteroaril C1-10-alquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, heteroalquilo C1-10, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R12 y R13 est n seleccionados cada uno, de modo independiente, del grupo que consiste en hidrogeno, halo, nitro, ciano, oxicarbonilo, amido, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, oxaalquilo C1-10, oxoalquilo C1-10, iminoalquilo C1-10, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-10, arilalquilo C1-10, heteroaril C1-10-alquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, heteroalquilo C1-10, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R14 est  seleccionado del grupo que consiste en alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, iminoalquilo C1-10, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-10, arilalquilo C1-10, heteroaril C1-10-alquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, heteroalquilo C1-10, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R32 y R33 se toman juntos para formar X o R32 y R33 est n seleccionados cada uno, de modo independiente, del grupo que consiste en hidrogeno, halo, nitro, ciano, tio, oxi, hidroxi, carboniloxi, alcoxi C1-10, aril C4-12-oxi, heteroaril C1-10-oxi, carbonilo, oxicarbonilo, amido, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, oxaalquilo C1-10, oxoalquilo C1-10, iminoalquilo C1-10, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-10, arilalquilo C1-10, heteroaril C1-10-alquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, heteroalquilo C1-10, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; y X est  seleccionado del grupo que consiste en NR14, O y S, o dos R2, R5, R6, R9, R10 R32 y R33 cualesquiera se toman juntos para formar un anillo sustituido o no sustituido; p est  seleccionado del grupo que consiste en 0 y 1; R34 est  seleccionado del grupo que consiste en -CONJ34-, -NJ34CO-, -NJ34-, -SO2NJ34-, -NJ34SO2-, J34 est  seleccionado del grupo que consiste en hidrogeno y alquilo C1-4; R35 est  seleccionado del grupo que consiste en amino, arilo C4-12, heteroarilo C1-10, cicloalquilo C3-8, heterocicloalquilo C3-6, bicicloalquilo C7-12, heterobicicloalquilo C3-12, cada uno sustituido o no sustituido; q est  seleccionado del grupo que consiste en 0 y 1; R36 est  seleccionado del grupo que consiste en alquilo C1-4, azaalquilo C1-4, cicloalquilo C3-8, heterocicloalquilo C3-8, cada uno sustituido o no sustituido; r est  seleccionado del grupo que consiste en 0 y 1; R37 es cicloalquilo C3-8 opcionalmente s
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