TWI868079B - 作為ｇａｂａａ ａ５受體調節子的雙環衍生物 - Google Patents
作為ｇａｂａａ ａ５受體調節子的雙環衍生物 Download PDFInfo
- Publication number
- TWI868079B TWI868079B TW108135172A TW108135172A TWI868079B TW I868079 B TWI868079 B TW I868079B TW 108135172 A TW108135172 A TW 108135172A TW 108135172 A TW108135172 A TW 108135172A TW I868079 B TWI868079 B TW I868079B
- Authority
- TW
- Taiwan
- Prior art keywords
- methyl
- methoxy
- fluorophenyl
- tetrahydro
- triazol
- Prior art date
Links
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
-
- 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
- A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- A61K31/4192—1,2,3-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
- A61K31/435—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
- A61K31/435—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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other 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
- 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)
- 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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HUP1800333 | 2018-09-28 | ||
| HU1800333A HU231223B1 (hu) | 2018-09-28 | 2018-09-28 | GABAA A5 receptor modulátor hatású biciklusos vegyületek |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW202035403A TW202035403A (zh) | 2020-10-01 |
| TWI868079B true TWI868079B (zh) | 2025-01-01 |
Family
ID=89992765
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW108135172A TWI868079B (zh) | 2018-09-28 | 2019-09-27 | 作為ｇａｂａａ ａ５受體調節子的雙環衍生物 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US12370182B2 (https=) |
| EP (1) | EP3856342B1 (https=) |
| JP (1) | JP7480128B2 (https=) |
| KR (1) | KR20210086631A (https=) |
| CN (1) | CN112805063B (https=) |
| AR (1) | AR116549A1 (https=) |
| AU (1) | AU2019346147B2 (https=) |
| BR (1) | BR112021005837A2 (https=) |
| CA (1) | CA3113072A1 (https=) |
| EA (1) | EA202190857A1 (https=) |
| HU (1) | HU231223B1 (https=) |
| MX (1) | MX2021003670A (https=) |
| TW (1) | TWI868079B (https=) |
| UA (1) | UA130217C2 (https=) |
| WO (1) | WO2020065597A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20240043418A1 (en) * | 2020-03-26 | 2024-02-08 | Richter Gedeon Nyrt. | 1,3-dihydro-2h-pyrrolo[3,4-c]pyridine derivatives as gabaa a5 receptor modulators |
| 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 |
| HU231691B1 (hu) * | 2021-09-29 | 2025-10-28 | Richter Gedeon Nyrt | GABAA ALFA5 receptor modulátor hatású biciklusos aminszármazékok |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009071464A1 (en) * | 2007-12-04 | 2009-06-11 | F. Hoffmann-La Roche Ag | Isoxazolo-pyrazine derivatives |
| WO2012062687A1 (en) * | 2010-11-09 | 2012-05-18 | F. Hoffmann-La Roche Ag | Triazole derivatives and their use for neurological disorders |
| WO2014001278A1 (en) * | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1237793B (it) * | 1989-12-21 | 1993-06-17 | Zambon Spa | Composti attivi come inibitori dell'enzima hmg-coa reduttasi |
| EP0986562B1 (en) | 1997-05-08 | 2002-08-07 | MERCK SHARP & DOHME LTD. | Substituted 1,2,4-triazolo 3,4-a]phthalazine derivatives as gaba alpha 5 ligands |
| GB9813576D0 (en) | 1998-06-24 | 1998-08-19 | Merck Sharp & Dohme | Therapeutic agents |
| GB0017518D0 (en) | 2000-07-17 | 2000-08-30 | Merck Sharp & Dohme | Therapeutic agents |
| JP4148672B2 (ja) | 2000-11-17 | 2008-09-10 | 武田薬品工業株式会社 | イソオキサゾール誘導体 |
| JP2003261545A (ja) | 2001-12-28 | 2003-09-19 | Takeda Chem Ind Ltd | 神経栄養因子産生・分泌促進剤 |
| EP1888594A2 (en) | 2005-05-16 | 2008-02-20 | Wisys Technology Foundation, Inc. | Gabaergic agents to treat memory deficits |
| US7790745B2 (en) | 2005-10-21 | 2010-09-07 | Bristol-Myers Squibb Company | Tetrahydroisoquinoline LXR Modulators |
| TW200812982A (en) | 2006-05-24 | 2008-03-16 | Lilly Co Eli | Compounds and methods for modulating FXR |
| KR20100038102A (ko) | 2007-06-13 | 2010-04-12 | 글락소스미스클라인 엘엘씨 | 파네소이드 ｘ 수용체 작용제 |
| 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 |
| US8389550B2 (en) * | 2009-02-25 | 2013-03-05 | Hoffmann-La Roche Inc. | Isoxazoles / O-pyridines with ethyl and ethenyl linker |
| US8222246B2 (en) | 2009-04-02 | 2012-07-17 | Hoffmann-La Roche Inc. | Substituted isoxazoles |
| 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 |
| BRPI1013766A2 (pt) | 2009-05-07 | 2016-04-05 | Hoffmann La Roche | "derivados de isoxazol-piridina como moduladores de gaba" |
| GB2474120B (en) | 2009-10-01 | 2011-12-21 | Amira Pharmaceuticals Inc | Compounds as Lysophosphatidic acid receptor antagonists |
| GB201016088D0 (en) | 2010-09-24 | 2010-11-10 | Phase Focus Ltd | Improvements in imaging |
| MX341471B (es) | 2010-11-05 | 2016-08-22 | Hoffmann La Roche | Uso de compuestos farmaceuticos activos para el tratamiento de estados patologicos del sistema nervioso central. |
| KR20130100348A (ko) | 2010-11-09 | 2013-09-10 | 에프. 호프만-라 로슈 아게 | Gaba 수용체에 대한 리간드로서의 트라이아졸 유도체 |
| AU2011329233A1 (en) | 2010-11-15 | 2013-05-23 | Abbvie Deutschland Gmbh & Co Kg | NAMPT and ROCK inhibitors |
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| US8604062B2 (en) | 2011-10-20 | 2013-12-10 | Hoffman-La Roche Inc. | Process for the preparation of isoxazolyl-methoxy nicotinic acids |
| BR112014013136B1 (pt) | 2011-11-30 | 2020-05-26 | F. Hoffmann-La Roche Ag | Novos derivados de dihidroisoquinolina-1-ona biciclicos |
| WO2014001281A1 (en) | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
| WO2016107832A1 (en) | 2014-12-30 | 2016-07-07 | F. Hoffmann-La Roche Ag | Novel tetrahydropyridopyrimidines and tetrahydropyridopyridines for the treatment and prophylaxis of hepatitis b virus infection |
| WO2017133521A1 (zh) | 2016-02-01 | 2017-08-10 | 山东轩竹医药科技有限公司 | Fxr受体激动剂 |
| BR112019006571A2 (pt) | 2016-12-08 | 2019-07-02 | F. Hoffmann-La Roche Ag | derivados de éter de isoxazolila como gaba a alfa5 pam |
-
2018
- 2018-09-28 HU HU1800333A patent/HU231223B1/hu unknown
-
2019
- 2019-09-27 TW TW108135172A patent/TWI868079B/zh active
- 2019-09-27 US US17/279,654 patent/US12370182B2/en active Active
- 2019-09-27 EP EP19779613.9A patent/EP3856342B1/en active Active
- 2019-09-27 CN CN201980063431.3A patent/CN112805063B/zh active Active
- 2019-09-27 BR BR112021005837-0A patent/BR112021005837A2/pt unknown
- 2019-09-27 WO PCT/IB2019/058208 patent/WO2020065597A1/en not_active Ceased
- 2019-09-27 EA EA202190857A patent/EA202190857A1/ru unknown
- 2019-09-27 MX MX2021003670A patent/MX2021003670A/es unknown
- 2019-09-27 KR KR1020217012783A patent/KR20210086631A/ko not_active Ceased
- 2019-09-27 CA CA3113072A patent/CA3113072A1/en active Pending
- 2019-09-27 AU AU2019346147A patent/AU2019346147B2/en active Active
- 2019-09-27 AR ARP190102762A patent/AR116549A1/es unknown
- 2019-09-27 UA UAA202102250A patent/UA130217C2/uk unknown
- 2019-09-27 JP JP2021516369A patent/JP7480128B2/ja active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009071464A1 (en) * | 2007-12-04 | 2009-06-11 | F. Hoffmann-La Roche Ag | Isoxazolo-pyrazine derivatives |
| WO2012062687A1 (en) * | 2010-11-09 | 2012-05-18 | F. Hoffmann-La Roche Ag | Triazole derivatives and their use for neurological disorders |
| WO2014001278A1 (en) * | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
Also Published As
| Publication number | Publication date |
|---|---|
| US12370182B2 (en) | 2025-07-29 |
| KR20210086631A (ko) | 2021-07-08 |
| JP7480128B2 (ja) | 2024-05-09 |
| HUP1800333A2 (hu) | 2020-04-28 |
| EP3856342C0 (en) | 2025-12-10 |
| CN112805063B (zh) | 2024-02-23 |
| JP2022502366A (ja) | 2022-01-11 |
| AU2019346147A1 (en) | 2021-05-20 |
| US20210386718A1 (en) | 2021-12-16 |
| EP3856342A1 (en) | 2021-08-04 |
| UA130217C2 (uk) | 2025-12-24 |
| CA3113072A1 (en) | 2020-04-02 |
| MX2021003670A (es) | 2021-08-19 |
| CN112805063A (zh) | 2021-05-14 |
| WO2020065597A1 (en) | 2020-04-02 |
| EA202190857A1 (ru) | 2021-06-23 |
| HU231223B1 (hu) | 2022-01-28 |
| AR116549A1 (es) | 2021-05-19 |
| AU2019346147B2 (en) | 2025-01-09 |
| BR112021005837A2 (pt) | 2021-07-27 |
| TW202035403A (zh) | 2020-10-01 |
| EP3856342B1 (en) | 2025-12-10 |
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