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

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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)
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 (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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

Also Published As

Publication number Publication date
EP3331528A1 (en) 2018-06-13
JP2018522034A (ja) 2018-08-09
JP6847093B2 (ja) 2021-03-24
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
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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