KR20200051646A - Ahr 억제제 및 이의 용도 - Google Patents
Ahr 억제제 및 이의 용도 Download PDFInfo
- Publication number
- KR20200051646A KR20200051646A KR1020207007714A KR20207007714A KR20200051646A KR 20200051646 A KR20200051646 A KR 20200051646A KR 1020207007714 A KR1020207007714 A KR 1020207007714A KR 20207007714 A KR20207007714 A KR 20207007714A KR 20200051646 A KR20200051646 A KR 20200051646A
- Authority
- KR
- South Korea
- Prior art keywords
- methyl
- compound
- μmol
- mmol
- mixture
- Prior art date
- Legal status (The legal status 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 status listed.)
- Abandoned
Links
- 0 CC=C1C=CC(C)=*C(C=C2)=C*2=*C1 Chemical compound CC=C1C=CC(C)=*C(C=C2)=C*2=*C1 0.000 description 19
- IMBTXCDBJDERIW-KYQOHRQGSA-N CC(C)/C(/C[C@@H]1[IH][IH]C1C1N=C1C(N(C)/N=C\C)=C)=C\C1N=CC(c2ccccc2OC)=C[C@H]1C Chemical compound CC(C)/C(/C[C@@H]1[IH][IH]C1C1N=C1C(N(C)/N=C\C)=C)=C\C1N=CC(c2ccccc2OC)=C[C@H]1C IMBTXCDBJDERIW-KYQOHRQGSA-N 0.000 description 1
- WRFYIYOXJWKONR-UHFFFAOYSA-N COc1cc(Br)ccc1N Chemical compound COc1cc(Br)ccc1N WRFYIYOXJWKONR-UHFFFAOYSA-N 0.000 description 1
- UQOAAKGOFKYUTN-UHFFFAOYSA-N C[n]1nccc1C(C1C(Cc(ccc2c3)cc2ncc3-c(cc2)ccc2N2CC[U]CC2)C1)=O Chemical compound C[n]1nccc1C(C1C(Cc(ccc2c3)cc2ncc3-c(cc2)ccc2N2CC[U]CC2)C1)=O UQOAAKGOFKYUTN-UHFFFAOYSA-N 0.000 description 1
- RRRJGYHSHOOOKF-UHFFFAOYSA-N C[n]1nccc1C(Nc1cc(N=CC(C2)C3CCCCC3)c2cc1)=O Chemical compound C[n]1nccc1C(Nc1cc(N=CC(C2)C3CCCCC3)c2cc1)=O RRRJGYHSHOOOKF-UHFFFAOYSA-N 0.000 description 1
- RHURJWMRIIMJJK-UHFFFAOYSA-N Cc(cc(cc1)C#CC2CCNCC2)c1NC(c1ccn[n]1C)=O Chemical compound Cc(cc(cc1)C#CC2CCNCC2)c1NC(c1ccn[n]1C)=O RHURJWMRIIMJJK-UHFFFAOYSA-N 0.000 description 1
Classifications
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- 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
-
- 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
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/38—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic 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
- C07D413/12—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Physiology (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Quinoline Compounds (AREA)
- Pyridine Compounds (AREA)
- Polysaccharides And Polysaccharide Derivatives (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762546757P | 2017-08-17 | 2017-08-17 | |
| US62/546,757 | 2017-08-17 | ||
| US201862613141P | 2018-01-03 | 2018-01-03 | |
| US62/613,141 | 2018-01-03 | ||
| PCT/US2018/046957 WO2019036657A1 (en) | 2017-08-17 | 2018-08-17 | AHR INHIBITORS AND USES THEREOF |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20200051646A true KR20200051646A (ko) | 2020-05-13 |
Family
ID=65360285
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020207007714A Abandoned KR20200051646A (ko) | 2017-08-17 | 2018-08-17 | Ahr 억제제 및 이의 용도 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US10696650B2 (enExample) |
| EP (1) | EP3668496A4 (enExample) |
| JP (1) | JP7269917B2 (enExample) |
| KR (1) | KR20200051646A (enExample) |
| CN (1) | CN111163766A (enExample) |
| AU (1) | AU2018319016B2 (enExample) |
| BR (1) | BR112020003116A2 (enExample) |
| CA (1) | CA3073051A1 (enExample) |
| IL (1) | IL272649B2 (enExample) |
| MX (1) | MX2020001793A (enExample) |
| SG (1) | SG11202001310SA (enExample) |
| WO (1) | WO2019036657A1 (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2018300150A1 (en) | 2017-07-11 | 2020-01-30 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| CN111163766A (zh) | 2017-08-17 | 2020-05-15 | 医肯纳肿瘤学公司 | Ahr抑制剂和其用途 |
| WO2020146682A1 (en) | 2019-01-10 | 2020-07-16 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| WO2020146612A1 (en) | 2019-01-10 | 2020-07-16 | Vertex Pharmaceuticals Incorporated | Esters and carbamates as modulators of sodium channels |
| KR20220044753A (ko) * | 2019-07-25 | 2022-04-11 | 큐라데브 파마 프라이버트 리미티드 | 아세틸 조효소 a 신테타제 단쇄 2(acss2)의 소분자 억제제 |
| WO2021080015A1 (en) * | 2019-10-24 | 2021-04-29 | Ono Pharmaceutical Co., Ltd. | Modulators of trek (twik related k+ channels) channel function |
| PH12022551379A1 (en) | 2019-12-06 | 2023-05-03 | Vertex Pharma | Substituted tetrahydrofurans as modulators of sodium channels |
| BR112022013673A2 (pt) | 2020-01-10 | 2022-09-13 | Ikena Oncology Inc | Inibidores de ahr e seus usos |
| IL296790B1 (en) | 2020-03-30 | 2026-07-01 | Hutchmed Ltd | Amide compounds and their uses |
| WO2021236717A1 (en) | 2020-05-20 | 2021-11-25 | Senda Biosciences, Inc. | Fused imidazole derivatives 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 |
| SI4347031T1 (sl) | 2021-06-04 | 2026-01-30 | Vertex Pharmaceuticals Incorporated | N-(hidroksialkil (hetero)aril) tetrahidrofuran karboksamidi kot modulatorji natrijevih kanalčkov |
| 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 |
| CN116135850A (zh) * | 2021-11-16 | 2023-05-19 | 深圳湾实验室 | 抗鼻咽癌的小分子抑制剂、化合物的制备方法及其应用 |
| CN119707643A (zh) * | 2023-09-28 | 2025-03-28 | 德明药泰生物技术（深圳）有限公司 | AhR调节剂及其应用 |
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| CA3073051A1 (en) | 2019-02-21 |
| AU2018319016B2 (en) | 2023-08-31 |
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| SG11202001310SA (en) | 2020-03-30 |
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| MX2020001793A (es) | 2020-07-22 |
| EP3668496A4 (en) | 2021-07-14 |
| WO2019036657A1 (en) | 2019-02-21 |
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| JP7269917B2 (ja) | 2023-05-09 |
| IL272649A (en) | 2020-03-31 |
| US20210017153A1 (en) | 2021-01-21 |
| IL272649B2 (en) | 2023-02-01 |
| IL272649B (en) | 2022-10-01 |
| US10696650B2 (en) | 2020-06-30 |
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