AR110990A1 - Compuestos moduladores del receptor de hidrocarburos de arilo (ahr) - Google Patents

Compuestos moduladores del receptor de hidrocarburos de arilo (ahr)

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Publication number
AR110990A1
AR110990A1 ARP180100396A ARP180100396A AR110990A1 AR 110990 A1 AR110990 A1 AR 110990A1 AR P180100396 A ARP180100396 A AR P180100396A AR P180100396 A ARP180100396 A AR P180100396A AR 110990 A1 AR110990 A1 AR 110990A1
Authority
AR
Argentina
Prior art keywords
alkyl
independently selected
halogen
substituted
group
Prior art date
Application number
ARP180100396A
Other languages
English (en)
Inventor
Thomas Hoffmann
Michael Albers
Christoph Steeneck
Ulrich Deuschle
Original Assignee
Phenex Pharmaceuticals Ag
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Filing date
Publication date
Application filed by Phenex Pharmaceuticals Ag filed Critical Phenex Pharmaceuticals Ag
Publication of AR110990A1 publication Critical patent/AR110990A1/es

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    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • 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
    • A61K31/41551,2-Diazoles non condensed and containing further 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
    • A61K31/41Heterocyclic 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
    • A61K31/41961,2,4-Triazoles
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/08Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • 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
    • 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
    • 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

Reivindicación 1: Un compuesto representado por la fórmula (1), en donde A está seleccionado a partir de arilo mono- o bicíclico de 6 a 10 miembros y heteroarilo mono- o bicíclico de 5 a 10 miembros que contienen 1 a 4 heteroátomos independientemente seleccionados a partir de N, O y S, en donde arilo y heteroarilo están no sustituidos o sustituidos con 1 a 7 sustituyentes independientemente seleccionados a partir del grupo que consiste en halógeno, OH, CN, C₁₋₆-alquilo, O-C₁₋₆-alquilo, C(O)ORᵃ, OC(O)Rᵃ, S(O)-C₁₋₆-alquilo, S(O)₂-C₁₋₆-alquilo, N(Rᵃ)₂, C(O)N(Rᵃ)₂, NRᵃC(O)-C₁₋₆-alquilo, S(O)₂N(Rᵃ)₂, NRᵃS(O)₂-C₁₋₆-alquilo y C₃₋₆-cicloalquilo, en donde el alquilo y el cicloalquilo están no sustituidos o sustituidos con 1 a 3 sustituyentes independientemente seleccionados a partir del grupo que consiste en halógeno, C₁₋₃-alquilo, halo-C₁₋₃-alquilo, OH, CN y oxo; o en donde dos sustituyentes en el grupo arilo o heteroarilo junto con los átomos a los cuales están unidos pueden formar un anillo carbocíclico o heterocíclico de 5 a 7 miembros, saturado o parcialmente insaturado, que contiene 1 a 3 heteroátomos independientemente seleccionados a partir de O, N y S, en donde el anillo carbocíclico o heterocíclico está no sustituido o sustituido con 1 a 5 sustituyentes independientemente seleccionados a partir del grupo que consiste en halógeno, C₁₋₆-alquilo y halo-C₁₋₆-alquilo; B está seleccionado a partir de arilo mono- o bicíclico de 6 a 10 miembros y heteroarilo mono- o bicíclico de 5 a 10 miembros que contienen 1 a 4 heteroátomos independientemente seleccionados a partir de N, O y S, en donde arilo y heteroarilo están no sustituidos o sustituidos con 1 a 7 sustituyentes independientemente seleccionados a partir del grupo que consiste en halógeno, OH, CN, C₁₋₆-alquilo, O-C₁₋₆-alquilo, C(O)ORᵃ, OC(O)Rᵃ, S(O)-C₁₋₆-alquilo, S(O)₂-C₁₋₆-alquilo, N(Rᵃ)₂, C(O)N(Rᵃ)₂, NRᵃC(O)-C₁₋₆-alquilo, S(O)₂N(Rᵃ)₂, NRᵃS(O)₂-C₁₋₆-alquilo y C₃₋₆-cicloalquilo, en donde el alquilo y el cicloalquilo están no sustituidos o sustituidos con 1 a 3 sustituyentes independientemente seleccionados a partir del grupo que consiste en halógeno, C₁₋₃-alquilo, halo-C₁₋₃-alquilo, OH, CN y oxo; o en donde dos sustituyentes en el grupo arilo o heteroarilo junto con los átomos a los cuales están unidos pueden formar un anillo carbocíclico o heterocíclico de 5 a 7 miembros, saturado o parcialmente insaturado, que contiene 1 a 3 heteroátomos independientemente seleccionados a partir de O, N y S, en donde el anillo carbocíclico o heterocíclico está no sustituido o sustituido con 1 a 5 sustituyentes independientemente seleccionados a partir del grupo que consiste en halógeno, C₁₋₆-alquilo y halo-C₁₋₆-alquilo; R¹, R², R³ y R⁴ están cada uno independientemente seleccionados a partir de hidrógeno, halógeno, C₁₋₄-alquilo, halo-C₁₋₃-alquilo, OH, O-C₁₋₃-alquilo, y CN; Rᵃ es independientemente hidrógeno o C₁₋₆-alquilo, y Rᵇ es independientemente hidrógeno o C₁₋₆-alquilo.
ARP180100396A 2017-02-21 2018-02-20 Compuestos moduladores del receptor de hidrocarburos de arilo (ahr) AR110990A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP17000276 2017-02-21

Publications (1)

Publication Number Publication Date
AR110990A1 true AR110990A1 (es) 2019-05-22

Family

ID=58108394

Family Applications (1)

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Country Status (18)

Country Link
US (1) US20200031805A1 (es)
EP (1) EP3585780A1 (es)
JP (1) JP2020508311A (es)
KR (1) KR20190120293A (es)
CN (1) CN110325532A (es)
AR (1) AR110990A1 (es)
AU (1) AU2018224166A1 (es)
BR (1) BR112019015720A2 (es)
CA (1) CA3051645A1 (es)
CL (1) CL2019002314A1 (es)
EA (1) EA201991598A1 (es)
IL (1) IL268300A (es)
MA (1) MA47585A (es)
MX (1) MX2019009836A (es)
PH (1) PH12019550155A1 (es)
TW (1) TW201835070A (es)
UY (1) UY37610A (es)
WO (1) WO2018153893A1 (es)

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CN108239083B (zh) 2016-12-26 2021-08-17 阿里根公司 芳香烃受体调节剂
TWI752155B (zh) 2017-02-01 2022-01-11 德商菲尼克斯製藥股份有限公司 芳香烴受體(AhR)調節劑化合物
TWI674260B (zh) 2017-02-01 2019-10-11 德商菲尼克斯製藥股份有限公司 芳基烴受體(AhR)調節劑化合物
WO2019099977A2 (en) 2017-11-20 2019-05-23 Ariagen, Inc. Indole compounds and their use
EP4219495A1 (en) 2018-02-06 2023-08-02 Ideaya Biosciences, Inc. Ahr modulators
WO2020021024A1 (en) * 2018-07-26 2020-01-30 Phenex Pharmaceuticals Ag Substituted bicyclic compounds as modulators of the aryl hydrocarbon receptor (ahr)
SG11202101499UA (en) * 2018-08-31 2021-03-30 Jaguahr Therapeutics Pte Ltd Heterocyclic compounds as ahr modulators
EP3956327A1 (en) 2019-04-15 2022-02-23 Ariagen, Inc. Chiral indole compounds and their use
WO2021148628A1 (en) * 2020-01-23 2021-07-29 Phenex Pharmaceuticals Ag Oxalamide substituted heterocyclic compounds as modulators of the aryl hydrocarbon receptor (ahr)
WO2021173082A1 (en) 2020-02-26 2021-09-02 Jaguahr Therapeutics Pte Ltd Pyridopyrimidine derivatives useful in modulation of ahr signalling
CN114181212B (zh) * 2020-09-15 2023-06-06 山东轩竹医药科技有限公司 哒嗪酮类AhR抑制剂
WO2022078356A1 (zh) * 2020-10-15 2022-04-21 山东轩竹医药科技有限公司 杂芳环类AhR抑制剂
CN115215720B (zh) * 2021-04-19 2023-08-22 中国科学院化学研究所 含薁单元的石墨烯纳米片段分子—薁并玉红省及其合成方法与应用
CN115572282A (zh) * 2021-07-05 2023-01-06 华东理工大学 含芳杂环结构的吡唑酰胺类化合物及其制备方法和应用
CN115093400B (zh) * 2021-09-18 2023-09-05 北京华森英诺生物科技有限公司 AhR抑制剂及其用途和制备方法
WO2023088435A1 (zh) * 2021-11-19 2023-05-25 成都奥睿药业有限公司 三取代吡啶衍生物的制备及作为芳香烃受体调节物的应用
WO2024076300A1 (en) 2022-10-03 2024-04-11 Jaguahr Therapeutics Pte Ltd Compounds useful in modulation of ahr signalling

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Publication number Publication date
BR112019015720A2 (pt) 2020-03-24
IL268300A (en) 2019-09-26
CA3051645A1 (en) 2018-08-30
JP2020508311A (ja) 2020-03-19
KR20190120293A (ko) 2019-10-23
EA201991598A1 (ru) 2020-03-10
MA47585A (fr) 2020-01-01
UY37610A (es) 2018-03-23
MX2019009836A (es) 2019-10-04
TW201835070A (zh) 2018-10-01
PH12019550155A1 (en) 2020-03-16
CN110325532A (zh) 2019-10-11
US20200031805A1 (en) 2020-01-30
CL2019002314A1 (es) 2019-12-20
EP3585780A1 (en) 2020-01-01
WO2018153893A1 (en) 2018-08-30
AU2018224166A1 (en) 2019-08-01

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