AR110990A1 - Compuestos moduladores del receptor de hidrocarburos de arilo (ahr) - Google Patents
Compuestos moduladores del receptor de hidrocarburos de arilo (ahr)Info
- 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
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 239000004215 Carbon black (E152) Substances 0.000 title 1
- 229930195733 hydrocarbon Natural products 0.000 title 1
- 150000002430 hydrocarbons Chemical class 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 17
- 125000001424 substituent group Chemical group 0.000 abstract 8
- 229910052736 halogen Inorganic materials 0.000 abstract 7
- 150000002367 halogens Chemical group 0.000 abstract 7
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000005842 heteroatom Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000002950 monocyclic group Chemical group 0.000 abstract 4
- 229910052760 oxygen Inorganic materials 0.000 abstract 4
- 229910052717 sulfur Inorganic materials 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 125000001054 5 membered carbocyclic group Chemical group 0.000 abstract 2
- 125000001960 7 membered carbocyclic group Chemical group 0.000 abstract 2
- 101150073096 NRAS gene Proteins 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000002837 carbocyclic group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic 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
- A61K31/403—Heterocyclic 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
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic 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
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic 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
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/02—Heterocyclic 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
- C07D401/12—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic 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
- C07D403/12—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic 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
- C07D405/02—Heterocyclic 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
- C07D405/12—Heterocyclic 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyridine Compounds (AREA)
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.
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)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180100396A AR110990A1 (es) | 2017-02-21 | 2018-02-20 | Compuestos moduladores del receptor de hidrocarburos de arilo (ahr) |
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) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN111587249A (zh) | 2017-11-20 | 2020-08-25 | 阿里根公司 | 吲哚化合物及其用途 |
| ES2946632T7 (es) | 2018-02-06 | 2025-03-04 | Ideaya Biosciences Inc | Moduladores de AhR |
| WO2020021024A1 (en) * | 2018-07-26 | 2020-01-30 | Phenex Pharmaceuticals Ag | Substituted bicyclic compounds as modulators of the aryl hydrocarbon receptor (ahr) |
| EP3843853A1 (en) * | 2018-08-31 | 2021-07-07 | Jaguahr Therapeutics Pte Ltd | Heterocyclic compounds as ahr modulators |
| AU2020258394A1 (en) | 2019-04-15 | 2021-10-28 | 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) |
| EP4110778A1 (en) | 2020-02-26 | 2023-01-04 | 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 |
| CN115572282B (zh) * | 2021-07-05 | 2024-07-09 | 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 |
| EP4644386A1 (en) * | 2023-08-09 | 2025-11-05 | Daewoong Pharmaceutical Co., Ltd. | Novel compound, and pharmaceutical composition for prevention or treatment of cancer or tumors comprising same |
| CN117447402A (zh) * | 2023-10-18 | 2024-01-26 | 德明药泰生物技术（深圳）有限公司 | 芳香烃受体调节剂类化合物及其制备方法和应用 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1992002500A1 (fr) * | 1990-07-31 | 1992-02-20 | Teikoku Hormone Mfg. Co., Ltd. | Derive de 2-phenylindole |
| AU2003270426A1 (en) * | 2002-09-12 | 2004-04-30 | Avanir Pharmaceuticals | PHENYL-INDOLE COMPOUNDS FOR MODULATING IgE AND INHIBITING CELLULAR PROLIFERATION |
| US20050032869A1 (en) * | 2003-07-08 | 2005-02-10 | Pharmacia Italia S.P.A. | Pyrazolyl-indole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| KR101804588B1 (ko) * | 2009-10-13 | 2017-12-04 | 리간드 파마슈티칼스 인코포레이티드 | 조혈 성장 인자 모방체 소분자 화합물 및 이의 용도 |
| CN103179968B (zh) | 2010-07-27 | 2017-10-03 | 波士顿大学管理委员会 | 作为癌症疗法的芳烃受体(AhR)调节剂 |
| HK1207379A1 (en) * | 2012-10-17 | 2016-01-29 | 霍夫曼-拉罗奇有限公司 | 6-aminoindole derivatives as trp channel antagonists |
-
2018
- 2018-02-14 TW TW107105512A patent/TW201835070A/zh unknown
- 2018-02-20 UY UY0001037610A patent/UY37610A/es unknown
- 2018-02-20 AR ARP180100396A patent/AR110990A1/es unknown
- 2018-02-21 EA EA201991598A patent/EA201991598A1/ru unknown
- 2018-02-21 JP JP2019544924A patent/JP2020508311A/ja not_active Withdrawn
- 2018-02-21 CN CN201880013058.6A patent/CN110325532A/zh not_active Withdrawn
- 2018-02-21 US US16/483,981 patent/US20200031805A1/en not_active Abandoned
- 2018-02-21 BR BR112019015720-4A patent/BR112019015720A2/pt not_active Application Discontinuation
- 2018-02-21 EP EP18706506.5A patent/EP3585780A1/en not_active Withdrawn
- 2018-02-21 CA CA3051645A patent/CA3051645A1/en not_active Withdrawn
- 2018-02-21 WO PCT/EP2018/054234 patent/WO2018153893A1/en not_active Ceased
- 2018-02-21 AU AU2018224166A patent/AU2018224166A1/en not_active Withdrawn
- 2018-02-21 KR KR1020197027573A patent/KR20190120293A/ko not_active Withdrawn
- 2018-02-21 MA MA047585A patent/MA47585A/fr unknown
- 2018-02-21 MX MX2019009836A patent/MX2019009836A/es unknown
-
2019
- 2019-07-28 IL IL268300A patent/IL268300A/en unknown
- 2019-08-13 PH PH12019550155A patent/PH12019550155A1/en unknown
- 2019-08-16 CL CL2019002314A patent/CL2019002314A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP3585780A1 (en) | 2020-01-01 |
| UY37610A (es) | 2018-03-23 |
| EA201991598A1 (ru) | 2020-03-10 |
| PH12019550155A1 (en) | 2020-03-16 |
| US20200031805A1 (en) | 2020-01-30 |
| JP2020508311A (ja) | 2020-03-19 |
| CL2019002314A1 (es) | 2019-12-20 |
| CN110325532A (zh) | 2019-10-11 |
| BR112019015720A2 (pt) | 2020-03-24 |
| AU2018224166A1 (en) | 2019-08-01 |
| KR20190120293A (ko) | 2019-10-23 |
| WO2018153893A1 (en) | 2018-08-30 |
| CA3051645A1 (en) | 2018-08-30 |
| TW201835070A (zh) | 2018-10-01 |
| MA47585A (fr) | 2020-01-01 |
| MX2019009836A (es) | 2019-10-04 |
| IL268300A (en) | 2019-09-26 |
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