JP6847093B2 - ムスカリン様アゴニスト - Google Patents
ムスカリン様アゴニスト Download PDFInfo
- Publication number
- JP6847093B2 JP6847093B2 JP2018504993A JP2018504993A JP6847093B2 JP 6847093 B2 JP6847093 B2 JP 6847093B2 JP 2018504993 A JP2018504993 A JP 2018504993A JP 2018504993 A JP2018504993 A JP 2018504993A JP 6847093 B2 JP6847093 B2 JP 6847093B2
- Authority
- JP
- Japan
- Prior art keywords
- piperidine
- compound according
- hydrogen
- azaspiro
- salt
- 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.)
- Active
Links
- 0 CC(C(C)C(C1)(CN1C(OC*)=O)C1)C1N(CC1)*CC1/C(/N*(*)/C=C(\*)/C1)=N\C1(C)I Chemical compound CC(C(C)C(C1)(CN1C(OC*)=O)C1)C1N(CC1)*CC1/C(/N*(*)/C=C(\*)/C1)=N\C1(C)I 0.000 description 3
- GINABUAPACIWCA-UHFFFAOYSA-N CC(C)NC1CCNCC1 Chemical compound CC(C)NC1CCNCC1 GINABUAPACIWCA-UHFFFAOYSA-N 0.000 description 1
- XFHXZLONBKDICT-UHFFFAOYSA-N CC(CCC1)N1C(NC)=O Chemical compound CC(CCC1)N1C(NC)=O XFHXZLONBKDICT-UHFFFAOYSA-N 0.000 description 1
- MWGHJHUULCXBKO-UHFFFAOYSA-N CCC(C1)C1C(N1CC(C2)(CC2N(CC2)CCC2NC(C)C)C1)=O Chemical compound CCC(C1)C1C(N1CC(C2)(CC2N(CC2)CCC2NC(C)C)C1)=O MWGHJHUULCXBKO-UHFFFAOYSA-N 0.000 description 1
- LUBGFMZTGFXIIN-UHFFFAOYSA-N CCOC(N(CC1)CCC1=O)=O Chemical compound CCOC(N(CC1)CCC1=O)=O LUBGFMZTGFXIIN-UHFFFAOYSA-N 0.000 description 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1513740.9A GB201513740D0 (en) | 2015-08-03 | 2015-08-03 | Muscarinic agonist |
| GB1513740.9 | 2015-08-03 | ||
| PCT/GB2016/052384 WO2017021728A1 (en) | 2015-08-03 | 2016-08-03 | Muscarinic agonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018522034A JP2018522034A (ja) | 2018-08-09 |
| JP2018522034A5 JP2018522034A5 (https=) | 2019-09-12 |
| JP6847093B2 true JP6847093B2 (ja) | 2021-03-24 |
Family
ID=54063147
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018504993A Active JP6847093B2 (ja) | 2015-08-03 | 2016-08-03 | ムスカリン様アゴニスト |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US10548884B2 (https=) |
| EP (1) | EP3331528B1 (https=) |
| JP (1) | JP6847093B2 (https=) |
| CN (1) | CN107949384B (https=) |
| AU (1) | AU2016302047B2 (https=) |
| CA (1) | CA2994143C (https=) |
| DK (1) | DK3331528T3 (https=) |
| ES (1) | ES2894855T3 (https=) |
| GB (1) | GB201513740D0 (https=) |
| WO (1) | WO2017021728A1 (https=) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2012338581B2 (en) | 2011-11-18 | 2016-12-08 | Nxera Pharma Uk Limited | Muscarinic M1 receptor agonists |
| GB201404922D0 (en) | 2014-03-19 | 2014-04-30 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201513740D0 (en) * | 2015-08-03 | 2015-09-16 | Heptares Therapeutics Ltd | Muscarinic agonist |
| GB201513743D0 (en) | 2015-08-03 | 2015-09-16 | Heptares Therapeutics Ltd | Muscarinic agonists |
| GB201519352D0 (en) | 2015-11-02 | 2015-12-16 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| WO2017107089A1 (en) | 2015-12-23 | 2017-06-29 | Merck Sharp & Dohme Corp. | 3- (1h-pyrazol-4-yl) pyridineallosteric modulators of the m4 muscarinic acetylcholine receptor |
| US10329289B2 (en) | 2015-12-23 | 2019-06-25 | Merck Sharp & Dohme Corp. | 6,7-dihydro-5H-pyrrolo[3,4-B]pyridin-5-one allosteric modulators of the M4 muscarinic acetylcholine receptor |
| GB201617454D0 (en) | 2016-10-14 | 2016-11-30 | Heptares Therapeutics Limited | Pharmaceutical compounds |
| WO2018112843A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor |
| WO2018112842A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | 6,6-fused heteroaryl piperidine ether allosteric modulators of m4 muscarinic acetylcholine receptor |
| US12600726B2 (en) | 2017-07-12 | 2026-04-14 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor M4 |
| IL310346A (en) | 2017-10-20 | 2024-03-01 | Univ Vanderbilt | Muscarinic acetylcholine M4 receptor antagonists |
| EP3732163A4 (en) * | 2017-12-20 | 2021-07-14 | Vanderbilt University | MUSCARIN M4 ACETYLCHOLIN RECEPTOR ANTAGONISTS |
| EP4219464A1 (en) | 2018-03-23 | 2023-08-02 | Pfizer Inc. | Piperazine azaspiro derivaves |
| GB201810239D0 (en) | 2018-06-22 | 2018-08-08 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201819960D0 (en) | 2018-12-07 | 2019-01-23 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201819961D0 (en) | 2018-12-07 | 2019-01-23 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB202020191D0 (en) | 2020-12-18 | 2021-02-03 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| IL291569B2 (en) * | 2019-09-25 | 2025-04-01 | Oncoarendi Therapeutics Sa | Process for the production of 5-(4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)piperidin-1-yl)-1H-4,2,1-triazol-3-amine |
| KR20220079921A (ko) * | 2019-10-09 | 2022-06-14 | 노파르티스 아게 | M4 작용제로서의 2-아자스피로[3.4]옥탄 유도체 |
| PE20221454A1 (es) * | 2019-10-09 | 2022-09-21 | Novartis Ag | Derivados de 2-azaespiro[3.4]octano como agonistas de m4 |
| EP4069367B1 (en) | 2019-12-06 | 2024-05-15 | Neurocrine Biosciences, Inc. | Muscarinic receptor 4 antagonists and methods of use |
| EP4100410B1 (en) * | 2020-02-05 | 2026-04-22 | Neurocrine Biosciences, Inc. | Muscarinic receptor 4 antagonists and methods of use |
| WO2023114224A1 (en) | 2021-12-13 | 2023-06-22 | Sage Therapeutics, Inc. | Combination of muscarinic receptor positive modulators and nmda positive allosteric modulators |
| WO2025030095A1 (en) * | 2023-08-03 | 2025-02-06 | Neurocrine Biosciences, Inc. | Methods of synthesis |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101426499A (zh) | 2006-02-22 | 2009-05-06 | 弗特克斯药品有限公司 | 毒蕈碱受体调节剂 |
| NZ570497A (en) * | 2006-02-22 | 2011-09-30 | Vertex Pharma | Spiro condensed 4,4'-quinilino-piperidines derivatives as modulators of muscarinic receptors |
| JP2012506883A (ja) | 2008-10-29 | 2012-03-22 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | 置換されたスピロアミン |
| FR2945531A1 (fr) | 2009-05-12 | 2010-11-19 | Sanofi Aventis | Derives de 7-aza-spiro°3,5!nonane-7-carboxylates, leur preparation et leur application en therapeutique |
| AU2012338581B2 (en) * | 2011-11-18 | 2016-12-08 | Nxera Pharma Uk Limited | Muscarinic M1 receptor agonists |
| BR112015006029B1 (pt) * | 2012-09-18 | 2022-01-25 | Heptares Therapeutics Limited | Compostos aza bicíclicos como agonistas de receptor m1 muscarínicos, composição farmacêutica compreendendo ditos compostos e uso dos mesmos para tratar um distúrbio cognitivo ou distúrbio psicótico ou para tratar ou reduzir a gravidade de dores agudas, crônicas, neuropáticas ou inflamatórias |
| WO2014122474A1 (en) * | 2013-02-07 | 2014-08-14 | Takeda Pharmaceutical Company Limited | Piperidin-1 -yl and azepin-1 -yl carboxylates as muscarinic m4 receptor agonists |
| KR102352388B1 (ko) * | 2014-02-06 | 2022-01-17 | 헵테얼즈 테라퓨틱스 리미티드 | 무스카린성 m1 수용체 및/또는 m4 수용체 작용제로서 바이사이클릭 아자 화합물 |
| GB201504675D0 (en) * | 2015-03-19 | 2015-05-06 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201513743D0 (en) | 2015-08-03 | 2015-09-16 | Heptares Therapeutics Ltd | Muscarinic agonists |
| GB201513740D0 (en) * | 2015-08-03 | 2015-09-16 | Heptares Therapeutics Ltd | Muscarinic agonist |
-
2015
- 2015-08-03 GB GBGB1513740.9A patent/GB201513740D0/en not_active Ceased
-
2016
- 2016-08-03 WO PCT/GB2016/052384 patent/WO2017021728A1/en not_active Ceased
- 2016-08-03 EP EP16750221.0A patent/EP3331528B1/en active Active
- 2016-08-03 CA CA2994143A patent/CA2994143C/en active Active
- 2016-08-03 CN CN201680045225.6A patent/CN107949384B/zh active Active
- 2016-08-03 ES ES16750221T patent/ES2894855T3/es active Active
- 2016-08-03 DK DK16750221.0T patent/DK3331528T3/da active
- 2016-08-03 AU AU2016302047A patent/AU2016302047B2/en active Active
- 2016-08-03 JP JP2018504993A patent/JP6847093B2/ja active Active
- 2016-08-03 US US15/749,743 patent/US10548884B2/en active Active
-
2019
- 2019-12-27 US US16/728,762 patent/US11324738B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| EP3331528A1 (en) | 2018-06-13 |
| JP2018522034A (ja) | 2018-08-09 |
| WO2017021728A9 (en) | 2017-04-27 |
| US20200129496A1 (en) | 2020-04-30 |
| WO2017021728A1 (en) | 2017-02-09 |
| ES2894855T3 (es) | 2022-02-16 |
| CA2994143A1 (en) | 2017-02-09 |
| US11324738B2 (en) | 2022-05-10 |
| AU2016302047B2 (en) | 2020-09-10 |
| EP3331528B1 (en) | 2021-09-29 |
| CN107949384A (zh) | 2018-04-20 |
| CA2994143C (en) | 2023-09-26 |
| US20180228791A1 (en) | 2018-08-16 |
| AU2016302047A8 (en) | 2018-03-08 |
| US10548884B2 (en) | 2020-02-04 |
| DK3331528T3 (da) | 2021-10-25 |
| GB201513740D0 (en) | 2015-09-16 |
| HK1250139A1 (en) | 2018-11-30 |
| CN107949384B (zh) | 2025-02-28 |
| AU2016302047A1 (en) | 2018-02-15 |
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