KR102833588B1 - 무스카린성 m1 및/또는 m4 수용체의 작용제로서의 옥사디아졸 - Google Patents

무스카린성 m1 및/또는 m4 수용체의 작용제로서의 옥사디아졸

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KR102833588B1
KR102833588B1 KR1020217001748A KR20217001748A KR102833588B1 KR 102833588 B1 KR102833588 B1 KR 102833588B1 KR 1020217001748 A KR1020217001748 A KR 1020217001748A KR 20217001748 A KR20217001748 A KR 20217001748A KR 102833588 B1 KR102833588 B1 KR 102833588B1
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methyl
oxadiazol
azabicyclo
octan
diazaspiro
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KR20210024036A (ko
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길스 앨버트 브라운
배리 존 테오발드
벤자민 제랄드 테한
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넥세라 파마 유케이 리미티드
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    • C07ORGANIC CHEMISTRY
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    • 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
    • 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
    • A61K31/439Heterocyclic 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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
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    • 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
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/14Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
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    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
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    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
KR1020217001748A 2018-06-22 2019-06-24 무스카린성 m1 및/또는 m4 수용체의 작용제로서의 옥사디아졸 Active KR102833588B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1810245.9A GB201810245D0 (en) 2018-06-22 2018-06-22 Pharmaceutical compounds
GB1810245.9 2018-06-22
PCT/GB2019/051778 WO2019243850A1 (en) 2018-06-22 2019-06-24 Oxadiazoles as agonists of the muscarinic m1 and/or m4 receptor

Publications (2)

Publication Number Publication Date
KR20210024036A KR20210024036A (ko) 2021-03-04
KR102833588B1 true KR102833588B1 (ko) 2025-07-16

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US (2) US10858352B2 (enExample)
EP (1) EP3810607A1 (enExample)
JP (3) JP7389762B2 (enExample)
KR (1) KR102833588B1 (enExample)
CN (2) CN119039284A (enExample)
AU (1) AU2019289216B2 (enExample)
BR (1) BR112020026437A2 (enExample)
CA (1) CA3104085A1 (enExample)
GB (1) GB201810245D0 (enExample)
MX (1) MX2020014156A (enExample)
SG (1) SG11202012570TA (enExample)
TW (1) TWI872024B (enExample)
WO (1) WO2019243850A1 (enExample)
ZA (1) ZA202007986B (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
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
GB201519352D0 (en) 2015-11-02 2015-12-16 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201617454D0 (en) 2016-10-14 2016-11-30 Heptares Therapeutics Limited Pharmaceutical compounds
GB201810239D0 (en) 2018-06-22 2018-08-08 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201810245D0 (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
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

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WO2017021730A1 (en) 2015-08-03 2017-02-09 Heptares Therapeutics Limited Muscarinic agonists
WO2018069732A1 (en) 2016-10-14 2018-04-19 Heptares Therapeutics Limited Heterocyclic compounds having activity as modulators of muscarinic m1 and/or m4 receptors in the treatment of cns diseases and pains.

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US7786141B2 (en) 2004-08-19 2010-08-31 Vertex Pharmaceuticals Incorporated Dihydrospiroindene modulators of muscarinic receptors
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KR20080098070A (ko) 2006-02-22 2008-11-06 버텍스 파마슈티칼스 인코포레이티드 무스카린성 수용체의 조절제로서의 스피로 축합된 피페리딘
AU2007284548A1 (en) 2006-08-15 2008-02-21 Vertex Pharmaceuticals Incorporated Modulators of muscarinic receptors
WO2008117229A1 (en) * 2007-03-23 2008-10-02 Ranbaxy Laboratories Limited Muscarinic receptor antagonists
EP2616074A1 (en) * 2010-09-17 2013-07-24 Array Biopharma, Inc. Piperidinyl-substituted lactams as gpr119 modulators
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
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
GB201810245D0 (en) * 2018-06-22 2018-08-08 Heptares Therapeutics Ltd Pharmaceutical compounds

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WO2017021730A1 (en) 2015-08-03 2017-02-09 Heptares Therapeutics Limited Muscarinic agonists
WO2018069732A1 (en) 2016-10-14 2018-04-19 Heptares Therapeutics Limited Heterocyclic compounds having activity as modulators of muscarinic m1 and/or m4 receptors in the treatment of cns diseases and pains.

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US20190389849A1 (en) 2019-12-26
AU2019289216A1 (en) 2021-01-14
CA3104085A1 (en) 2019-12-26
AU2019289216B2 (en) 2023-04-06
GB201810245D0 (en) 2018-08-08
US20210101893A1 (en) 2021-04-08
CN112585135A (zh) 2021-03-30
US10858352B2 (en) 2020-12-08
CN112585135B (zh) 2024-08-02
CN119039284A (zh) 2024-11-29
ZA202007986B (en) 2021-10-27
WO2019243850A1 (en) 2019-12-26
BR112020026437A2 (pt) 2021-03-23
KR20210024036A (ko) 2021-03-04
EP3810607A1 (en) 2021-04-28
TW202019918A (zh) 2020-06-01
JP2026002915A (ja) 2026-01-08
JP7389762B2 (ja) 2023-11-30
US11319312B2 (en) 2022-05-03
TWI872024B (zh) 2025-02-11
MX2020014156A (es) 2021-03-09
JP2021528447A (ja) 2021-10-21
SG11202012570TA (en) 2021-01-28
JP2023164721A (ja) 2023-11-10

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