AR110789A1 - Compuestos moduladores del receptor de hidrocarburos de arilo (ahr) - Google Patents
Compuestos moduladores del receptor de hidrocarburos de arilo (ahr)Info
- Publication number
- AR110789A1 AR110789A1 ARP180100227A ARP180100227A AR110789A1 AR 110789 A1 AR110789 A1 AR 110789A1 AR P180100227 A ARP180100227 A AR P180100227A AR P180100227 A ARP180100227 A AR P180100227A AR 110789 A1 AR110789 A1 AR 110789A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- independently selected
- halogen
- heteroaryl
- halo
- 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 10
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical group 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000002837 carbocyclic group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- 125000002950 monocyclic group Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 101150073096 NRAS gene Proteins 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 239000012453 solvate Substances 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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- 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
- A61K31/41—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
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not 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
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not 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
- A61K31/435—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
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- C07D471/00—Heterocyclic 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
- C07D471/02—Heterocyclic 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
- C07D471/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Reivindicación 1: Un compuesto representado por la fórmula (1), un enantiómero, diastereómero, tautómero, solvato, prodroga o sal farmacéuticamente aceptable del mismo, en donde A y B están independientemente seleccionados a partir de arilo mono- o bicíclico de 6 a 10 miembros y heteroarilo mono- o bicíclico de 5 a 10 miembros que contiene 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 que están unidos pueden formar un anillo carbocíclico o anillo 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 el anillo 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 están cada uno independientemente seleccionados a partir de hidrógeno, halógeno, C₁₋₃-alquilo, halo-C₁₋₃-alquilo, OH, O-C₁₋₃-alquilo, y CN; Rᵃ es hidrógeno o C₁₋₆-alquilo; y Rᵇ es hidrógeno o C₁₋₆-alquilo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17000158 | 2017-02-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR110789A1 true AR110789A1 (es) | 2019-05-02 |
Family
ID=57960223
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180100227A AR110789A1 (es) | 2017-02-01 | 2018-01-31 | Compuestos moduladores del receptor de hidrocarburos de arilo (ahr) |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US10981908B2 (es) |
| EP (1) | EP3577112B1 (es) |
| JP (1) | JP6849823B2 (es) |
| KR (1) | KR102320516B1 (es) |
| CN (1) | CN110248940B (es) |
| AR (1) | AR110789A1 (es) |
| AU (1) | AU2018216957B2 (es) |
| BR (1) | BR112019015716A2 (es) |
| CA (1) | CA3050827C (es) |
| CL (1) | CL2019002108A1 (es) |
| CO (1) | CO2019007881A2 (es) |
| CR (1) | CR20190392A (es) |
| CU (1) | CU20190069A7 (es) |
| EA (1) | EA038318B1 (es) |
| EC (1) | ECSP19055169A (es) |
| ES (1) | ES2858329T3 (es) |
| IL (1) | IL268080B (es) |
| MX (1) | MX2019008994A (es) |
| MY (1) | MY196831A (es) |
| NI (1) | NI201900076A (es) |
| PE (1) | PE20191478A1 (es) |
| PH (1) | PH12019550135A1 (es) |
| SG (1) | SG11201906958TA (es) |
| TW (1) | TWI752155B (es) |
| UA (1) | UA122745C2 (es) |
| UY (1) | UY37589A (es) |
| WO (1) | WO2018141857A1 (es) |
| ZA (1) | ZA201904771B (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| 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) |
| US20230028680A1 (en) * | 2018-11-30 | 2023-01-26 | Celularity Inc. | Expansion of natural killer cells and ilc3 cells with novel aromatic compounds |
| US20230108408A1 (en) * | 2020-01-23 | 2023-04-06 | Phenex Pharmaceuticals Ag | Oxalamide substituted heterocyclic compounds as modulators of the aryl hydrocarbon receptor (ahr) |
| KR20220153595A (ko) | 2020-02-26 | 2022-11-18 | 재규어 테라퓨틱스 피티이 리미티드 | AhR 신호전달의 조절에 유용한 피리도피리미딘 유도체 |
| US20230234967A1 (en) * | 2020-05-28 | 2023-07-27 | Senda Biosciences, Inc. | Fused Azole Heterocycles as AHR Antagonists |
| 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 |
| CN114835687B (zh) * | 2021-04-02 | 2023-09-05 | 北京华森英诺生物科技有限公司 | AhR抑制剂 |
| 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 |
| WO2024076300A1 (en) | 2022-10-03 | 2024-04-11 | Jaguahr Therapeutics Pte Ltd | Compounds useful in modulation of ahr signalling |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO1992002500A1 (en) | 1990-07-31 | 1992-02-20 | Teikoku Hormone Mfg. Co., Ltd. | 2-phenylindole derivative |
| HUP9903330A2 (hu) | 1996-11-19 | 2000-03-28 | Amgen Inc. | Gyulladásgátló hatású, aril- és heteroaril csoporttal szubsztituált kondenzált pirrolszármazékok, valamint ezeket tartalmazó gyógyászati készítmények |
| 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 |
| KR101007489B1 (ko) | 2005-11-18 | 2011-01-12 | 에프. 호프만-라 로슈 아게 | 아자인돌-2-카복스아마이드 유도체 |
| US8563573B2 (en) * | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
| AU2010307006B2 (en) | 2009-10-13 | 2016-08-11 | Ligand Pharmaceuticals Inc. | Hematopoietic growth factor mimetic small molecule compounds and their uses |
| CN106588908A (zh) * | 2009-11-02 | 2017-04-26 | 宋嘉声 | 用于介入治疗和根除癌症的ite |
| US20130338201A1 (en) * | 2009-11-02 | 2013-12-19 | Ahr Pharmaceuticals, Inc. | Method of Cancer Treatment with 2-(1H-Indole-3-Carbonyl)-Thiazole-4-Carboxylic Acid Methyl Ester |
| CN102834393B (zh) | 2010-02-03 | 2015-07-22 | 武田药品工业株式会社 | 细胞凋亡信号调节激酶1抑制剂 |
| US8410117B2 (en) * | 2010-03-26 | 2013-04-02 | Hoffmann-La Roche Inc. | Imidazopyrimidine derivatives |
| TWI510487B (zh) | 2010-04-21 | 2015-12-01 | Plexxikon Inc | 用於激酶調節的化合物和方法及其適應症 |
| US10314810B2 (en) | 2010-07-27 | 2019-06-11 | Trustees Of Boston University | Aryl hydrocarbon receptor (AhR) modifiers as novel cancer therapeutics |
| GB201104267D0 (en) | 2011-03-14 | 2011-04-27 | Cancer Rec Tech Ltd | Pyrrolopyridineamino derivatives |
| CN104755461A (zh) | 2012-10-17 | 2015-07-01 | 霍夫曼-拉罗奇有限公司 | 作为trp通道拮抗剂的6-氨基吲哚衍生物 |
| LT2935248T (lt) | 2012-12-21 | 2018-04-10 | Plexxikon Inc. | Kinazės moduliavimo junginiai ir būdai bei indikacijos |
| 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 |
| 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 |
| TW201835070A (zh) | 2017-02-21 | 2018-10-01 | 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 |
-
2018
- 2018-01-26 TW TW107102803A patent/TWI752155B/zh not_active IP Right Cessation
- 2018-01-31 UY UY0001037589A patent/UY37589A/es not_active Application Discontinuation
- 2018-01-31 AR ARP180100227A patent/AR110789A1/es not_active Application Discontinuation
- 2018-02-01 JP JP2019561370A patent/JP6849823B2/ja active Active
- 2018-02-01 CR CR20190392A patent/CR20190392A/es unknown
- 2018-02-01 KR KR1020197023990A patent/KR102320516B1/ko active IP Right Grant
- 2018-02-01 EA EA201991599A patent/EA038318B1/ru unknown
- 2018-02-01 CN CN201880009354.9A patent/CN110248940B/zh active Active
- 2018-02-01 CU CU2019000069A patent/CU20190069A7/es unknown
- 2018-02-01 CA CA3050827A patent/CA3050827C/en active Active
- 2018-02-01 MX MX2019008994A patent/MX2019008994A/es unknown
- 2018-02-01 PE PE2019001482A patent/PE20191478A1/es unknown
- 2018-02-01 AU AU2018216957A patent/AU2018216957B2/en not_active Ceased
- 2018-02-01 BR BR112019015716-6A patent/BR112019015716A2/pt not_active IP Right Cessation
- 2018-02-01 MY MYPI2019004031A patent/MY196831A/en unknown
- 2018-02-01 EP EP18701774.4A patent/EP3577112B1/en active Active
- 2018-02-01 ES ES18701774T patent/ES2858329T3/es active Active
- 2018-02-01 WO PCT/EP2018/052542 patent/WO2018141857A1/en active Application Filing
- 2018-02-01 SG SG11201906958TA patent/SG11201906958TA/en unknown
- 2018-02-01 US US16/479,130 patent/US10981908B2/en active Active
- 2018-02-01 UA UAA201908353A patent/UA122745C2/uk unknown
-
2019
- 2019-07-15 IL IL268080A patent/IL268080B/en unknown
- 2019-07-15 NI NI201900076A patent/NI201900076A/es unknown
- 2019-07-19 ZA ZA2019/04771A patent/ZA201904771B/en unknown
- 2019-07-23 CO CONC2019/0007881A patent/CO2019007881A2/es unknown
- 2019-07-24 PH PH12019550135A patent/PH12019550135A1/en unknown
- 2019-07-29 CL CL2019002108A patent/CL2019002108A1/es unknown
- 2019-07-31 EC ECSENADI201955169A patent/ECSP19055169A/es unknown
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