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)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Neurology (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (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 (enExample) | 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 (enExample) |
| EP (1) | EP3331528B1 (enExample) |
| JP (1) | JP6847093B2 (enExample) |
| CN (1) | CN107949384B (enExample) |
| AU (1) | AU2016302047B2 (enExample) |
| CA (1) | CA2994143C (enExample) |
| DK (1) | DK3331528T3 (enExample) |
| ES (1) | ES2894855T3 (enExample) |
| GB (1) | GB201513740D0 (enExample) |
| WO (1) | WO2017021728A1 (enExample) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2780015B1 (en) | 2011-11-18 | 2017-01-04 | Heptares Therapeutics Limited | Muscarinic m1 receptor agonists |
| GB201404922D0 (en) | 2014-03-19 | 2014-04-30 | 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 |
| 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 |
| TW201726675A (zh) | 2015-12-23 | 2017-08-01 | 默沙東藥廠 | M4毒蕈鹼乙醯膽鹼受體之異位調節劑6,7-二氫-5h-吡咯并[3,4-b]吡啶-5-酮 |
| GB201617454D0 (en) | 2016-10-14 | 2016-11-30 | Heptares Therapeutics Limited | Pharmaceutical compounds |
| 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 |
| WO2018112843A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor |
| AU2018300980A1 (en) | 2017-07-12 | 2020-01-02 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor M4 |
| IL273924B2 (en) | 2017-10-20 | 2024-07-01 | Univ Vanderbilt | Antagonists of the muscarinic acetylcholine receptor m4 |
| WO2019126559A1 (en) | 2017-12-20 | 2019-06-27 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor m4 |
| PT3768669T (pt) * | 2018-03-23 | 2023-04-24 | Pfizer | Derivados de piperazina azaspiro |
| 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 |
| MX2022002881A (es) * | 2019-09-25 | 2022-06-08 | Oncoarendi Therapeutics Sa | Proceso para la produccion de 5-(4-((2s,5s)-5-(4-clorobencil)-2-me tilmorfolino)piperidin-1-il)-1h-1,2,4-triazol-3-amina. |
| WO2021070090A1 (en) * | 2019-10-09 | 2021-04-15 | Novartis Ag | 2-azaspiro[3.4]octane derivatives as m4 agonists |
| CN119390705A (zh) * | 2019-10-09 | 2025-02-07 | 诺华股份有限公司 | 作为m4激动剂的5-氧杂-2-氮杂螺[3.4]辛烷衍生物 |
| US12486250B2 (en) | 2019-12-06 | 2025-12-02 | Neurocrine Biosciences, Inc. | Muscarinic receptor 4 antagonists and methods of use |
| JP7707176B2 (ja) * | 2020-02-05 | 2025-07-14 | ニューロクライン バイオサイエンシーズ,インコーポレイテッド | ムスカリン性受容体4アンタゴニストおよび使用方法 |
| 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 |
|---|---|---|---|---|
| KR20080098070A (ko) * | 2006-02-22 | 2008-11-06 | 버텍스 파마슈티칼스 인코포레이티드 | 무스카린성 수용체의 조절제로서의 스피로 축합된 피페리딘 |
| AU2007221214A1 (en) | 2006-02-22 | 2007-09-07 | Vertex Pharmaceuticals Incorporated | Modulators of muscarinic receptors |
| MX2011004340A (es) | 2008-10-29 | 2011-05-23 | Gruenenthal Gmbh | Espiroaminas sustituidas. |
| 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 |
| EP2780015B1 (en) * | 2011-11-18 | 2017-01-04 | Heptares Therapeutics Limited | Muscarinic m1 receptor agonists |
| CN107098899B (zh) * | 2012-09-18 | 2019-09-06 | 赫普泰雅治疗有限公司 | 作为毒蕈碱的m1受体激动剂的二环氮杂化合物 |
| JP6478923B2 (ja) * | 2013-02-07 | 2019-03-06 | ヘプタレス セラピューティクス リミテッドHeptares Therapeutics Limited | ムスカリンm4受容体アゴニストとしてのピペリジン−1−イル及びアゼピン−1−イルカルボキシレート |
| SG11201606269WA (en) * | 2014-02-06 | 2016-09-29 | Heptares Therapeutics Ltd | Bicyclic aza compounds as muscarinic m1 receptor and/or m4 receptor agonists |
| GB201504675D0 (en) * | 2015-03-19 | 2015-05-06 | 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 |
-
2015
- 2015-08-03 GB GBGB1513740.9A patent/GB201513740D0/en not_active Ceased
-
2016
- 2016-08-03 ES ES16750221T patent/ES2894855T3/es active Active
- 2016-08-03 AU AU2016302047A patent/AU2016302047B2/en active Active
- 2016-08-03 WO PCT/GB2016/052384 patent/WO2017021728A1/en not_active Ceased
- 2016-08-03 DK DK16750221.0T patent/DK3331528T3/da active
- 2016-08-03 CA CA2994143A patent/CA2994143C/en active Active
- 2016-08-03 EP EP16750221.0A patent/EP3331528B1/en active Active
- 2016-08-03 JP JP2018504993A patent/JP6847093B2/ja active Active
- 2016-08-03 CN CN201680045225.6A patent/CN107949384B/zh 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 |
|---|---|
| ES2894855T3 (es) | 2022-02-16 |
| JP2018522034A (ja) | 2018-08-09 |
| HK1250139A1 (en) | 2018-11-30 |
| US20180228791A1 (en) | 2018-08-16 |
| DK3331528T3 (da) | 2021-10-25 |
| CN107949384A (zh) | 2018-04-20 |
| CA2994143A1 (en) | 2017-02-09 |
| US20200129496A1 (en) | 2020-04-30 |
| WO2017021728A1 (en) | 2017-02-09 |
| AU2016302047A8 (en) | 2018-03-08 |
| AU2016302047A1 (en) | 2018-02-15 |
| US11324738B2 (en) | 2022-05-10 |
| CA2994143C (en) | 2023-09-26 |
| EP3331528A1 (en) | 2018-06-13 |
| EP3331528B1 (en) | 2021-09-29 |
| CN107949384B (zh) | 2025-02-28 |
| US10548884B2 (en) | 2020-02-04 |
| WO2017021728A9 (en) | 2017-04-27 |
| GB201513740D0 (en) | 2015-09-16 |
| AU2016302047B2 (en) | 2020-09-10 |
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