CA2994143C - Muscarinic agonists - Google Patents

Muscarinic agonists Download PDF

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Publication number
CA2994143C
CA2994143C CA2994143A CA2994143A CA2994143C CA 2994143 C CA2994143 C CA 2994143C CA 2994143 A CA2994143 A CA 2994143A CA 2994143 A CA2994143 A CA 2994143A CA 2994143 C CA2994143 C CA 2994143C
Authority
CA
Canada
Prior art keywords
carboxylate
ethyl
azaspiro
compound according
piperidin
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
Application number
CA2994143A
Other languages
English (en)
French (fr)
Other versions
CA2994143A1 (en
Inventor
Giles Albert Brown
Miles Stuart Congreve
Mark PICKWORTH
Mark David RACKHAM
Benjamin Gerald TEHAN
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Nxera Pharma UK Ltd
Original Assignee
Heptares Therapeutics Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Heptares Therapeutics Ltd filed Critical Heptares Therapeutics Ltd
Publication of CA2994143A1 publication Critical patent/CA2994143A1/en
Application granted granted Critical
Publication of CA2994143C publication Critical patent/CA2994143C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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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)
CA2994143A 2015-08-03 2016-08-03 Muscarinic agonists Active CA2994143C (en)

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 (2)

Publication Number Publication Date
CA2994143A1 CA2994143A1 (en) 2017-02-09
CA2994143C true CA2994143C (en) 2023-09-26

Family

ID=54063147

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2994143A Active CA2994143C (en) 2015-08-03 2016-08-03 Muscarinic agonists

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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2619829T3 (es) 2011-11-18 2017-06-27 Heptares Therapeutics Limited Agonistas del receptor muscarínico M1
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
EP3394061B1 (en) 2015-12-23 2020-03-11 Merck Sharp & Dohme Corp. 6,7-dihydro-5h-pyrrolo[3,4-b]pyridin-5-one allosteric modulators of the m4 muscarinic acetylcholine receptor
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
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
EP3651762B1 (en) 2017-07-12 2024-07-03 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
JP7270989B2 (ja) 2017-10-20 2023-05-11 ヴァンダービルト ユニバーシティー ムスカリン性アセチルコリン受容体m4のアンタゴニスト
EP3732163A4 (en) * 2017-12-20 2021-07-14 Vanderbilt University MUSCARIN M4 ACETYLCHOLIN RECEPTOR ANTAGONISTS
EP3768669B1 (en) * 2018-03-23 2023-01-25 Pfizer Inc. Piperazine azaspiro derivaves
GB201810239D0 (en) 2018-06-22 2018-08-08 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201819961D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201819960D0 (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
JP7697933B2 (ja) * 2019-09-25 2025-06-24 オンコアレンディ セラピューティクス エス.エー. 5-(4-((2s,5s)-5-(4-クロロベンジル)-2-メチルモルホリノ)ピペリジン-1-イル)-1h-1,2,4-トリアゾール-3-アミンの製造プロセス
UY38906A (es) * 2019-10-09 2021-05-31 Novartis Ag Compuestos 2- derivados de azaspiro[3,4]octano como agonistas de m4 y composiciones de los mismos
PH12022550860A1 (en) * 2019-10-09 2023-06-14 Novartis Ag 5-oxa-2-azaspiro[3.4]octane derivatives as m4 agonists
US12486250B2 (en) 2019-12-06 2025-12-02 Neurocrine Biosciences, Inc. Muscarinic receptor 4 antagonists and methods of use
TWI889751B (zh) * 2020-02-05 2025-07-11 美商紐羅克里生物科學有限公司 蕈毒受體4拮抗劑及使用方法
US20250064833A1 (en) 2021-12-13 2025-02-27 Sage Therapeutics, Inc. Combination of muscarinic receptor positive modulators and nmda positive allosteric modulators
KR20260046441A (ko) * 2023-08-03 2026-04-07 뉴로크린 바이오사이언시즈 인코퍼레이티드 합성 방법

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2008137583A (ru) 2006-02-22 2010-03-27 Вертекс Фармасьютикалз Инкорпорейшн (Us) Спиропиперидины в качестве модуляторов мускариновых рецепторов
US8003660B2 (en) 2006-02-22 2011-08-23 Vertex Pharmaceuticals Incorporated Modulators of muscarinic receptors
AU2009309988A1 (en) 2008-10-29 2010-05-06 Grunenthal Gmbh Substituted spiroamines
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
ES2619829T3 (es) 2011-11-18 2017-06-27 Heptares Therapeutics Limited Agonistas del receptor muscarínico M1
EP2897948B1 (en) * 2012-09-18 2016-08-31 Heptares Therapeutics Limited Bicyclic aza compounds as muscarinic m1 receptor agonists
US9593106B2 (en) * 2013-02-07 2017-03-14 Heptares Therapeutics Limited Piperidin-1-yl and azepin-1-yl carboxylates as muscarinic M4 receptor agonists
RU2685230C2 (ru) * 2014-02-06 2019-04-17 Хептарес Терапьютикс Лимитед Бициклические азотсодержащие соединения как агонисты М1 мускариновых рецепторов
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

Also Published As

Publication number Publication date
US20200129496A1 (en) 2020-04-30
WO2017021728A1 (en) 2017-02-09
AU2016302047A1 (en) 2018-02-15
US10548884B2 (en) 2020-02-04
CN107949384B (zh) 2025-02-28
CA2994143A1 (en) 2017-02-09
WO2017021728A9 (en) 2017-04-27
EP3331528B1 (en) 2021-09-29
US11324738B2 (en) 2022-05-10
EP3331528A1 (en) 2018-06-13
JP2018522034A (ja) 2018-08-09
JP6847093B2 (ja) 2021-03-24
ES2894855T3 (es) 2022-02-16
AU2016302047B2 (en) 2020-09-10
US20180228791A1 (en) 2018-08-16
CN107949384A (zh) 2018-04-20
GB201513740D0 (en) 2015-09-16
DK3331528T3 (da) 2021-10-25
HK1250139A1 (en) 2018-11-30
AU2016302047A8 (en) 2018-03-08

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