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AR102258A1 - QUINOLINE AND QUINAZOLINE COMPOUNDS - Google Patents

QUINOLINE AND QUINAZOLINE COMPOUNDS

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Publication number
AR102258A1
AR102258A1 ARP150103310A ARP150103310A AR102258A1 AR 102258 A1 AR102258 A1 AR 102258A1 AR P150103310 A ARP150103310 A AR P150103310A AR P150103310 A ARP150103310 A AR P150103310A AR 102258 A1 AR102258 A1 AR 102258A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
alkoxy
amino
heterocycloalkyl
Prior art date
Application number
ARP150103310A
Other languages
Spanish (es)
Original Assignee
Acerta Pharma Bv
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
Application filed by Acerta Pharma Bv filed Critical Acerta Pharma Bv
Publication of AR102258A1 publication Critical patent/AR102258A1/en

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Classifications

    • 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
    • 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
    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicación 1: Un compuesto de la fórmula (1) o una sal farmacéuticamente aceptable del mismo, en donde: A es CH o N, con la condición de que si B es N, A sea CH; B es CH o N, con la condición de que si A es N, B sea CH; T es CH o N; U es CH o N; V es NR⁵, O, S, SO o SO₂; W es CH, N, O ó S; X es C(R⁶), N, O ó S; Y es CH, N o enlace; Z es CH o N; con la condición de que: 0 a 2 átomos de W, X, Y puedan ser simultáneamente un heteroátomo; cuando un átomo seleccionado de entre W, X, Y es O ó S, entonces otro átomo seleccionado entre W, X, Y no puede ser O ó S; cuando Y es CH o N, entonces X es C(R⁶) o N y W es CH o N; R¹ es H, alquilo C₁₋₄ opcionalmente sustituido con R⁷ o C(O)R⁷, o alcoxi C₁₋₅ opcionalmente sustituido con R⁷ o C(O)R⁷, u O-heterocicloalquilo C₂₋₆ opcionalmente sustituido con hidroxilo o alquilo C₁₋₄; R³ es H, alquilo C₁₋₃ opcionalmente sustituido con R⁷, o cicloalquilo C₃₋₇ opcionalmente sustituido con R⁷; R⁴ es H, R¹¹C(O), R¹²S(O), R¹³SO₂, o alquilo C₁₋₆ opcionalmente sustituido con R¹⁴; R¹ y R³ juntos pueden formar un heterocicloalquilo C₂₋₆; R⁵ es H o alquilo C₁₋₃; R² es H, halógeno, ciano, alquilo C₁₋₄, alquenilo C₂₋₄, alquinilo C₂₋₄, alcoxi C₁₋₃, cicloalquilo C₃₋₆; todos los grupos alquilo de R² están opcionalmente sustituidos con uno o más halógenos; o R² es arilo C₆₋₁₀ o heterocicloalquilo C₂₋₆; R⁶ es H o alquilo C₁₋₃; o R² y R⁶ juntos pueden formar un cicloalquenilo C₃₋₇, o heterocicloalquenilo C₂₋₆; cada uno opcionalmente sustituido con alquilo C₁₋₃, o uno o más halógenos; R⁷ es H, alcoxi C₁₋₃, o un heterocicloalquilo C₂₋₆; (uno o más) hidroxilo, [alquilo C₁₋₄]amino, di[alquilo C₁₋₄]amino, cicloalcoxi C₃₋₇; R¹¹ se selecciona independientemente del grupo que consiste en alquilo C₁₋₆, alquenilo C₂₋₆ y alquinilo C₂₋₆ donde cada alquilo, alquenilo o alquinilo está opcionalmente sustituido con uno o más grupos seleccionados entre hidroxilo, alquilo C₁₋₄, cicloalquilo C₃₋₇, alcoxi C₁₋₃, cicloalcoxi C₃₋₇, [alquilo C₁₋₄]amino opcionalmente sustituido con hidroxilo, halógeno, o alcoxi C₁₋₃, di[alquilo C₁₋₄]amino opcionalmente sustituido con hidroxilo, halógeno, o alcoxi C₁₋₃, arilo C₆₋₁₀ o heterocicloalquilo C₃₋₇, o R¹¹ es heteroarilo C₁₋₅ opcionalmente sustituido con uno o más grupos seleccionados de halógeno o ciano; R¹² y R¹³ se seleccionan independientemente entre el grupo constituido por alquenilo C₂₋₆ o alquinilo C₂₋₆ ambos opcionalmente sustituidos con uno o más grupos seleccionados de hidroxilo, alquilo C₁₋₄, cicloalquilo C₃₋₇, [alquilo C₁₋₄]amino, di[alquilo C₁₋₄]amino, alcoxi C₁₋₃, cicloalcoxi C₃₋₇, arilo C₆₋₁₀, o heterocicloalquilo C₃₋₇; o heteroarilo C₁₋₅ opcionalmente sustituido con uno o más grupos seleccionados de halógeno o ciano; R¹⁴ se selecciona independientemente del grupo que consiste en halógeno, ciano o alquenilo C₂₋₆ o alquinilo C₂₋₆ ambos opcionalmente sustituidos con uno o más grupos seleccionados entre hidroxilo, alquilo C₁₋₄, cicloalquilo C₃₋₇, [alquilo C₁₋₄]amino, di[alquilo C₁₋₄]amino, alcoxi C₁₋₃, cicloalcoxi C₃₋₇, arilo C₆₋₁₀, heteroarilo C₁₋₅ o heterocicloalquilo C₃₋₇.Claim 1: A compound of the formula (1) or a pharmaceutically acceptable salt thereof, wherein: A is CH or N, provided that if B is N, A is CH; B is CH or N, with the proviso that if A is N, B is CH; T is CH or N; U is CH or N; V is NR⁵, O, S, SO or SO₂; W is CH, N, O or S; X is C (R⁶), N, O or S; Y is CH, N or link; Z is CH or N; with the proviso that: 0 to 2 atoms of W, X, Y can simultaneously be a heteroatom; when an atom selected from W, X, Y is O or S, then another atom selected from W, X, Y cannot be O or S; when Y is CH or N, then X is C (R⁶) or N and W is CH or N; R¹ is H, C₁₋₄ alkyl optionally substituted with R⁷ or C (O) R⁷, or C₁₋₅ alkoxy optionally substituted with R⁷ or C (O) R⁷, or C₂₋₆ O-heterocycloalkyl optionally substituted with hydroxyl or C₁₋ alkyl ₄; R³ is H, C₁₋₃ alkyl optionally substituted with R⁷, or C₃₋₇ cycloalkyl optionally substituted with R⁷; R⁴ is H, R¹¹C (O), R¹²S (O), R¹³SO₂, or C₁₋₆ alkyl optionally substituted with R¹⁴; R¹ and R³ together can form a C₂₋₆ heterocycloalkyl; R⁵ is H or C₁₋₃ alkyl; R² is H, halogen, cyano, C₁₋₄ alkyl, C₂₋₄ alkenyl, C₂₋₄ alkynyl, C₁₋₃ alkoxy, C₃₋₆ cycloalkyl; all R² alkyl groups are optionally substituted with one or more halogens; or R² is C₆₋₁₀ aryl or C₂₋₆ heterocycloalkyl; R⁶ is H or C₁₋₃ alkyl; or R² and R⁶ together can form a C₃₋₇ cycloalkenyl, or C₂₋₆ heterocycloalkenyl; each optionally substituted with C₁₋₃ alkyl, or one or more halogens; R⁷ is H, C₁₋₃ alkoxy, or a C₂₋₆ heterocycloalkyl; (one or more) hydroxyl, [C₁₋₄ alkyl] amino, di [C₁₋₄ alkyl] amino, C₃₋₇ cycloalkoxy; R¹¹ is independently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆ alkenyl and C₂₋₆ alkynyl where each alkyl, alkenyl or alkynyl is optionally substituted with one or more groups selected from hydroxyl, C₁₋₄ alkyl, C₃₋ cycloalkyl ₇, C₁₋₃ alkoxy, C₃₋₇ cycloalkoxy, [C₁₋₄ alkyl] amino optionally substituted with hydroxyl, halogen, or C₁₋₃ alkoxy, di [C₁₋₄ alkyl] amino optionally substituted with hydroxyl, halogen, or C₁ alkoxy ₋₃, C₆₋₁₀ aryl or C₃₋₇ heterocycloalkyl, or R¹¹ is C₁₋₅ heteroaryl optionally substituted with one or more groups selected from halogen or cyano; R¹² and R¹³ are independently selected from the group consisting of C₂₋₆ alkenyl or C₂₋₆ alkynyl both optionally substituted with one or more groups selected from hydroxyl, C₁₋₄ alkyl, C₃₋₇ cycloalkyl, [C₁₋₄ alkyl] amino, di [C₁₋₄ alkyl] amino, C₁₋₃ alkoxy, C₃₋₇ cycloalkoxy, C₆₋₁₀ aryl, or C₃₋₇ heterocycloalkyl; or C₁₋₅ heteroaryl optionally substituted with one or more groups selected from halogen or cyano; R¹⁴ is independently selected from the group consisting of halogen, cyano or C₂₋₆ alkenyl or C₂₋₆ alkynyl both optionally substituted with one or more groups selected from hydroxyl, C₁₋₄ alkyl, C₃₋₇ cycloalkyl, [C₁₋₄ alkyl] amino, di [C₁₋₄ alkyl] amino, C₁₋₃ alkoxy, C₃₋₇ cycloalkoxy, C₆₋₁₀ aryl, C₁₋₅ heteroaryl or C₃₋₇ heterocycloalkyl.

ARP150103310A 2014-10-10 2015-10-13 QUINOLINE AND QUINAZOLINE COMPOUNDS AR102258A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462062823P 2014-10-10 2014-10-10

Publications (1)

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AR102258A1 true AR102258A1 (en) 2017-02-15

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AR (1) AR102258A1 (en)
TW (1) TW201629036A (en)
WO (1) WO2016055982A1 (en)

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WO2018026877A1 (en) 2016-08-05 2018-02-08 Calitor Sciences, Llc Process for preparing substituted quinolin-4-ol compounds
IL266003B (en) * 2016-11-28 2022-08-01 Eisai R&D Man Co Ltd Salts of indazole derivatives and their crystals
MX2021003517A (en) 2018-09-25 2021-08-16 Black Diamond Therapeutics Inc Quinazoline derivatives as tyrosine kinase inhibitor, compositions, methods of making them and their use.
MX2022001467A (en) * 2019-08-08 2022-05-06 B C I Pharma QUINOLINE DERIVATIVES AS PROTEIN KINASE INHIBITORS.
AU2020328598A1 (en) 2019-08-15 2022-03-03 Black Diamond Therapeutics, Inc. Alkynyl quinazoline compounds
US20230339865A1 (en) * 2020-06-05 2023-10-26 Dana-Farber Cancer Institute, Inc. Quinazoline-derived hck inhibitors for use in the treatment of myd88 mutated diseases
CN115197135B (en) * 2022-08-30 2023-09-19 鲁东大学 A zinc-catalyzed method for preparing multi-substituted quinoline compounds
WO2025151487A2 (en) * 2024-01-08 2025-07-17 Regents Of The University Of Michigan Small-molecule inhibitors of adar1

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WO2016055982A1 (en) 2016-04-14
TW201629036A (en) 2016-08-16

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