KR20210021019A - GABA A α5 PAM으로서의 이속사졸릴 에테르 유도체 - Google Patents
GABA A α5 PAM으로서의 이속사졸릴 에테르 유도체 Download PDFInfo
- Publication number
- KR20210021019A KR20210021019A KR1020217000958A KR20217000958A KR20210021019A KR 20210021019 A KR20210021019 A KR 20210021019A KR 1020217000958 A KR1020217000958 A KR 1020217000958A KR 20217000958 A KR20217000958 A KR 20217000958A KR 20210021019 A KR20210021019 A KR 20210021019A
- Authority
- KR
- South Korea
- Prior art keywords
- methyl
- isoxazol
- methylpyridin
- pyridazin
- pyridazine
- 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.)
- Ceased
Links
Classifications
-
- 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
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K31/537—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 spiro-condensed or forming part of bridged ring systems
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- C07D413/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- 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
- C07D487/08—Bridged 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
- C07D487/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- 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
-
- 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
- C07D498/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP18177522.2 | 2018-06-13 | ||
| EP18177522 | 2018-06-13 | ||
| EP18177825 | 2018-06-14 | ||
| EP18177825.9 | 2018-06-14 | ||
| PCT/EP2019/065129 WO2019238633A1 (en) | 2018-06-13 | 2019-06-11 | New isoxazolyl ether derivatives as gaba a alpha5 pam |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20210021019A true KR20210021019A (ko) | 2021-02-24 |
Family
ID=66776367
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020217000958A Ceased KR20210021019A (ko) | 2018-06-13 | 2019-06-11 | GABA A α5 PAM으로서의 이속사졸릴 에테르 유도체 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US11840528B2 (https=) |
| EP (1) | EP3807269A1 (https=) |
| JP (1) | JP7478676B2 (https=) |
| KR (1) | KR20210021019A (https=) |
| CN (1) | CN112424196A (https=) |
| AU (1) | AU2019286312B2 (https=) |
| BR (1) | BR112020025355A2 (https=) |
| CA (1) | CA3102101A1 (https=) |
| CL (1) | CL2020003214A1 (https=) |
| CR (1) | CR20200610A (https=) |
| IL (1) | IL279266B2 (https=) |
| MA (1) | MA52868A (https=) |
| MX (1) | MX2020013518A (https=) |
| PE (1) | PE20210555A1 (https=) |
| PH (1) | PH12020500674A1 (https=) |
| SG (1) | SG11202012200QA (https=) |
| TW (1) | TWI816812B (https=) |
| WO (1) | WO2019238633A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI901650B (zh) | 2020-03-26 | 2025-10-21 | 匈牙利商羅特格登公司 | 啶及吡啶并〔３，４－ｃ〕嗒衍生物 |
| EP4149933B1 (en) * | 2020-05-13 | 2024-06-12 | F. Hoffmann-La Roche AG | New triazolyl derivatives as gaba a alpha5 pam |
| HU231691B1 (hu) | 2021-09-29 | 2025-10-28 | Richter Gedeon Nyrt | GABAA ALFA5 receptor modulátor hatású biciklusos aminszármazékok |
| WO2026009854A1 (ja) * | 2024-07-01 | 2026-01-08 | 日本たばこ産業株式会社 | ピリダジノン化合物及びその医薬用途 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2682301A1 (en) * | 2007-04-18 | 2008-10-30 | Astrazeneca Ab | Xanthine compounds having a positive allosteric gabab receptor modulator effect |
| KR101237576B1 (ko) | 2007-12-04 | 2013-03-04 | 에프. 호프만-라 로슈 아게 | 아이속사졸로-피리딘 유도체 |
| US7943619B2 (en) * | 2007-12-04 | 2011-05-17 | Hoffmann-La Roche Inc. | Isoxazolo-pyridazine derivatives |
| CA2724842A1 (en) * | 2008-05-19 | 2009-11-26 | Sunovion Pharmaceuticals Inc. | Imidazo[1,2-a]pyridine compounds |
| JP5460858B2 (ja) * | 2009-05-05 | 2014-04-02 | エフ．ホフマン−ラ ロシュ アーゲー | イソオキサゾール−ピラゾール誘導体 |
| US8604062B2 (en) | 2011-10-20 | 2013-12-10 | Hoffman-La Roche Inc. | Process for the preparation of isoxazolyl-methoxy nicotinic acids |
| US8785435B2 (en) | 2011-10-20 | 2014-07-22 | Hoffmann-La Roche Inc. | Solid forms |
| BR112019006571A2 (pt) | 2016-12-08 | 2019-07-02 | F. Hoffmann-La Roche Ag | derivados de éter de isoxazolila como gaba a alfa5 pam |
-
2019
- 2019-06-11 WO PCT/EP2019/065129 patent/WO2019238633A1/en not_active Ceased
- 2019-06-11 EP EP19729015.8A patent/EP3807269A1/en active Pending
- 2019-06-11 BR BR112020025355-3A patent/BR112020025355A2/pt not_active IP Right Cessation
- 2019-06-11 SG SG11202012200QA patent/SG11202012200QA/en unknown
- 2019-06-11 IL IL279266A patent/IL279266B2/en unknown
- 2019-06-11 MA MA052868A patent/MA52868A/fr unknown
- 2019-06-11 CR CR20200610A patent/CR20200610A/es unknown
- 2019-06-11 CN CN201980046146.0A patent/CN112424196A/zh active Pending
- 2019-06-11 PE PE2020001963A patent/PE20210555A1/es unknown
- 2019-06-11 AU AU2019286312A patent/AU2019286312B2/en not_active Ceased
- 2019-06-11 CA CA3102101A patent/CA3102101A1/en active Pending
- 2019-06-11 JP JP2020569188A patent/JP7478676B2/ja active Active
- 2019-06-11 KR KR1020217000958A patent/KR20210021019A/ko not_active Ceased
- 2019-06-11 MX MX2020013518A patent/MX2020013518A/es unknown
- 2019-06-12 TW TW108120285A patent/TWI816812B/zh not_active IP Right Cessation
-
2020
- 2020-12-10 CL CL2020003214A patent/CL2020003214A1/es unknown
- 2020-12-10 PH PH12020500674A patent/PH12020500674A1/en unknown
- 2020-12-11 US US17/119,977 patent/US11840528B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| JP2021527099A (ja) | 2021-10-11 |
| BR112020025355A2 (pt) | 2021-03-09 |
| CA3102101A1 (en) | 2019-12-19 |
| CL2020003214A1 (es) | 2021-05-07 |
| SG11202012200QA (en) | 2021-01-28 |
| US11840528B2 (en) | 2023-12-12 |
| AU2019286312A1 (en) | 2021-01-07 |
| MX2020013518A (es) | 2021-02-26 |
| JP7478676B2 (ja) | 2024-05-07 |
| MA52868A (fr) | 2021-04-21 |
| PE20210555A1 (es) | 2021-03-17 |
| PH12020500674A1 (en) | 2021-06-07 |
| WO2019238633A1 (en) | 2019-12-19 |
| AU2019286312B2 (en) | 2023-08-17 |
| TWI816812B (zh) | 2023-10-01 |
| TW202016106A (zh) | 2020-05-01 |
| IL279266B2 (en) | 2024-03-01 |
| US20210094945A1 (en) | 2021-04-01 |
| EP3807269A1 (en) | 2021-04-21 |
| CR20200610A (es) | 2021-02-05 |
| IL279266B1 (en) | 2023-11-01 |
| IL279266A (en) | 2021-01-31 |
| CN112424196A (zh) | 2021-02-26 |
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| EP4149933B1 (en) | New triazolyl derivatives as gaba a alpha5 pam | |
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| HK40041196A (en) | New isoxazolyl ether derivatives as gaba a alpha5 pam | |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
Patent event date: 20210112 Patent event code: PA01051R01D Comment text: International Patent Application |
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| PG1501 | Laying open of application | ||
| A201 | Request for examination | ||
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Patent event code: PA02012R01D Patent event date: 20220610 Comment text: Request for Examination of Application |
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Comment text: Notification of reason for refusal Patent event date: 20240801 Patent event code: PE09021S01D |
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| PE0601 | Decision on rejection of patent |
Patent event date: 20241007 Comment text: Decision to Refuse Application Patent event code: PE06012S01D |