KR20230004722A - Nrf2 활성제로서의 테트라히드로이소퀴놀린 화합물 - Google Patents
Nrf2 활성제로서의 테트라히드로이소퀴놀린 화합물 Download PDFInfo
- Publication number
- KR20230004722A KR20230004722A KR1020227040564A KR20227040564A KR20230004722A KR 20230004722 A KR20230004722 A KR 20230004722A KR 1020227040564 A KR1020227040564 A KR 1020227040564A KR 20227040564 A KR20227040564 A KR 20227040564A KR 20230004722 A KR20230004722 A KR 20230004722A
- Authority
- KR
- South Korea
- Prior art keywords
- methyl
- alkyl
- carbonyl
- tetrahydroisoquinoline
- carboxamide
- 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.)
- Pending
Links
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- C07D401/14—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 three or more hetero 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D405/14—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 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
- C07D413/14—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
- C07D417/14—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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Neurosurgery (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Neurology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB2005852.5 | 2020-04-22 | ||
| GBGB2005852.5A GB202005852D0 (en) | 2020-04-22 | 2020-04-22 | Therapeutic compounds |
| PCT/GB2021/050975 WO2021214472A1 (en) | 2020-04-22 | 2021-04-22 | Tetrahydroisoquinoline compounds as nrf2 activators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20230004722A true KR20230004722A (ko) | 2023-01-06 |
Family
ID=70859963
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020227040564A Pending KR20230004722A (ko) | 2020-04-22 | 2021-04-22 | Nrf2 활성제로서의 테트라히드로이소퀴놀린 화합물 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US20230159511A1 (https=) |
| EP (1) | EP4139295B1 (https=) |
| JP (1) | JP7751165B2 (https=) |
| KR (1) | KR20230004722A (https=) |
| CN (1) | CN115667242B (https=) |
| AR (1) | AR121913A1 (https=) |
| AU (1) | AU2021258539A1 (https=) |
| BR (1) | BR112022021370A2 (https=) |
| CA (1) | CA3174360A1 (https=) |
| ES (1) | ES3031970T3 (https=) |
| GB (1) | GB202005852D0 (https=) |
| IL (1) | IL297440A (https=) |
| MX (1) | MX2022013396A (https=) |
| PH (1) | PH12022552773A1 (https=) |
| WO (1) | WO2021214472A1 (https=) |
| ZA (1) | ZA202211464B (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2021004566A (es) | 2018-10-22 | 2021-06-08 | C4X Discovery Ltd | Compuestos terapeuticos. |
| US20240424112A1 (en) | 2021-10-25 | 2024-12-26 | C4X Discovery Limited | Tetrahydroisoquinoline compounds that are keap1 binders. |
| PE20241779A1 (es) * | 2022-01-07 | 2024-09-03 | Chugai Pharmaceutical Co Ltd | Compuesto heterociclico que contiene nitrogeno que tiene un efecto de activacion del nrf2 |
| WO2024130411A1 (en) * | 2022-12-21 | 2024-06-27 | Variational Ai Inc. | Protease inhibitors and methods of using same |
| WO2024262491A1 (ja) * | 2023-06-19 | 2024-12-26 | 中外製薬株式会社 | Ｎｒｆ２活性化作用を有する含窒素複素環化合物の結晶 |
| EP4596534A1 (en) * | 2024-01-31 | 2025-08-06 | University of Copenhagen | Noncovalent small-molecule inhibitors of the keap1-nrf2 interaction |
| WO2025237912A1 (en) | 2024-05-13 | 2025-11-20 | Astrazeneca Ab | Keap1 inhibitors for use in the treatment of bronchiectasis |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140256767A1 (en) * | 2011-10-31 | 2014-09-11 | The Broad Institute, Inc. | Direct inhibitors of keap1-nrf2 interaction as antioxidant inflammation modulators |
| CA2988373A1 (en) * | 2015-06-15 | 2016-12-22 | Glaxosmithkline Intellectual Property Development Limited | Nrf2 regulators |
| JP2020097526A (ja) * | 2017-03-28 | 2020-06-25 | 武田薬品工業株式会社 | 複素環化合物 |
| MX2021004566A (es) | 2018-10-22 | 2021-06-08 | C4X Discovery Ltd | Compuestos terapeuticos. |
-
2020
- 2020-04-22 GB GBGB2005852.5A patent/GB202005852D0/en not_active Ceased
-
2021
- 2021-04-22 BR BR112022021370A patent/BR112022021370A2/pt unknown
- 2021-04-22 ES ES21724005T patent/ES3031970T3/es active Active
- 2021-04-22 KR KR1020227040564A patent/KR20230004722A/ko active Pending
- 2021-04-22 US US17/920,244 patent/US20230159511A1/en active Pending
- 2021-04-22 JP JP2022564532A patent/JP7751165B2/ja active Active
- 2021-04-22 MX MX2022013396A patent/MX2022013396A/es unknown
- 2021-04-22 WO PCT/GB2021/050975 patent/WO2021214472A1/en not_active Ceased
- 2021-04-22 AR ARP210101081A patent/AR121913A1/es unknown
- 2021-04-22 PH PH1/2022/552773A patent/PH12022552773A1/en unknown
- 2021-04-22 AU AU2021258539A patent/AU2021258539A1/en active Pending
- 2021-04-22 CA CA3174360A patent/CA3174360A1/en active Pending
- 2021-04-22 CN CN202180030434.4A patent/CN115667242B/zh active Active
- 2021-04-22 IL IL297440A patent/IL297440A/en unknown
- 2021-04-22 EP EP21724005.0A patent/EP4139295B1/en active Active
-
2022
- 2022-10-19 ZA ZA2022/11464A patent/ZA202211464B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ES3031970T3 (en) | 2025-07-14 |
| EP4139295B1 (en) | 2025-04-09 |
| JP2023524207A (ja) | 2023-06-09 |
| ZA202211464B (en) | 2025-05-28 |
| AU2021258539A1 (en) | 2022-11-10 |
| GB202005852D0 (en) | 2020-06-03 |
| IL297440A (en) | 2022-12-01 |
| WO2021214472A1 (en) | 2021-10-28 |
| MX2022013396A (es) | 2022-12-13 |
| JP7751165B2 (ja) | 2025-10-08 |
| EP4139295A1 (en) | 2023-03-01 |
| US20230159511A1 (en) | 2023-05-25 |
| CA3174360A1 (en) | 2021-10-28 |
| PH12022552773A1 (en) | 2024-03-25 |
| CN115667242A (zh) | 2023-01-31 |
| BR112022021370A2 (pt) | 2022-12-06 |
| CN115667242B (zh) | 2025-02-28 |
| AR121913A1 (es) | 2022-07-20 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
St.27 status event code: A-0-1-A10-A15-nap-PA0105 |
|
| PG1501 | Laying open of application |
St.27 status event code: A-1-1-Q10-Q12-nap-PG1501 |
|
| A201 | Request for examination | ||
| E13-X000 | Pre-grant limitation requested |
St.27 status event code: A-2-3-E10-E13-lim-X000 |
|
| P11-X000 | Amendment of application requested |
St.27 status event code: A-2-2-P10-P11-nap-X000 |
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| P13-X000 | Application amended |
St.27 status event code: A-2-2-P10-P13-nap-X000 |
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| PA0201 | Request for examination |
St.27 status event code: A-1-2-D10-D11-exm-PA0201 |
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| R18-X000 | Changes to party contact information recorded |
St.27 status event code: A-3-3-R10-R18-oth-X000 |
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| D21 | Rejection of application intended |
Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D21-EXM-PE0902 (AS PROVIDED BY THE NATIONAL OFFICE) |
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| PE0902 | Notice of grounds for rejection |
St.27 status event code: A-1-2-D10-D21-exm-PE0902 |