AU2012338581B2 - Muscarinic M1 receptor agonists - Google Patents

Muscarinic M1 receptor agonists Download PDF

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Publication number
AU2012338581B2
AU2012338581B2 AU2012338581A AU2012338581A AU2012338581B2 AU 2012338581 B2 AU2012338581 B2 AU 2012338581B2 AU 2012338581 A AU2012338581 A AU 2012338581A AU 2012338581 A AU2012338581 A AU 2012338581A AU 2012338581 B2 AU2012338581 B2 AU 2012338581B2
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AU
Australia
Prior art keywords
carboxylate
azepane
ethyl
piperidin
carbamoyl
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Active
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AU2012338581A
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AU2012338581A1 (en
Inventor
Giles Brown
Julie CANSFIELD
Miles Congreve
Benjamin TEHAN
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Nxera Pharma UK Ltd
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Nxera Pharma UK Ltd
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Publication of AU2012338581B2 publication Critical patent/AU2012338581B2/en
Priority to AU2017201505A priority Critical patent/AU2017201505B2/en
Priority to AU2018236871A priority patent/AU2018236871B2/en
Assigned to NXERA PHARMA UK LIMITED reassignment NXERA PHARMA UK LIMITED Request to Amend Deed and Register Assignors: HEPTARES THERAPEUTICS LIMITED
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    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • 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
    • A61K31/4545—Non 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
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2012338581A 2011-11-18 2012-11-16 Muscarinic M1 receptor agonists Active AU2012338581B2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2017201505A AU2017201505B2 (en) 2011-11-18 2017-03-06 Muscarinic M1 receptor agonists
AU2018236871A AU2018236871B2 (en) 2011-11-18 2018-09-28 Muscarinic M1 receptor agonists

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161632813P 2011-11-18 2011-11-18
US61/632,813 2011-11-18
PCT/GB2012/052857 WO2013072705A1 (en) 2011-11-18 2012-11-16 Muscarinic m1 receptor agonists

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2017201505A Division AU2017201505B2 (en) 2011-11-18 2017-03-06 Muscarinic M1 receptor agonists

Publications (2)

Publication Number Publication Date
AU2012338581A1 AU2012338581A1 (en) 2014-06-05
AU2012338581B2 true AU2012338581B2 (en) 2016-12-08

Family

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Family Applications (3)

Application Number Title Priority Date Filing Date
AU2012338581A Active AU2012338581B2 (en) 2011-11-18 2012-11-16 Muscarinic M1 receptor agonists
AU2017201505A Active AU2017201505B2 (en) 2011-11-18 2017-03-06 Muscarinic M1 receptor agonists
AU2018236871A Active AU2018236871B2 (en) 2011-11-18 2018-09-28 Muscarinic M1 receptor agonists

Family Applications After (2)

Application Number Title Priority Date Filing Date
AU2017201505A Active AU2017201505B2 (en) 2011-11-18 2017-03-06 Muscarinic M1 receptor agonists
AU2018236871A Active AU2018236871B2 (en) 2011-11-18 2018-09-28 Muscarinic M1 receptor agonists

Country Status (16)

Country Link
US (6) US9187451B2 (OSRAM)
EP (1) EP2780015B1 (OSRAM)
JP (2) JP6083818B2 (OSRAM)
CN (2) CN104039321B (OSRAM)
AU (3) AU2012338581B2 (OSRAM)
BR (1) BR112014012056B1 (OSRAM)
CA (1) CA2856076C (OSRAM)
DK (1) DK2780015T3 (OSRAM)
ES (1) ES2619829T3 (OSRAM)
GB (1) GB2511685A (OSRAM)
HU (1) HUE033114T2 (OSRAM)
IN (1) IN2014KN01075A (OSRAM)
PL (1) PL2780015T3 (OSRAM)
PT (1) PT2780015T (OSRAM)
SG (1) SG11201402405QA (OSRAM)
WO (1) WO2013072705A1 (OSRAM)

Families Citing this family (20)

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BR112014012056B1 (pt) 2011-11-18 2021-12-14 Heptares Therapeutics Limited Compostos agonistas do receptor m1 muscarínico, composição farmacêutica compreendendo os ditos compostos e uso dos mesmos para tratar um distúrbio cognitivo ou psicótico ou para tratamento ou diminuição da severidade da dor aguda, crônica, neuropática ou inflamatória
CA2883210C (en) 2012-09-18 2021-06-15 Heptares Therapeutics Limited Bicyclic aza compounds as muscarinic m1 receptor agonists
GB2519470A (en) * 2013-09-18 2015-04-22 Heptares Therapeutics Ltd Bicyclic aza compounds as muscarinic M1 receptor agonists
MX393637B (es) * 2014-02-06 2025-03-11 Heptares Therapeutics Ltd Compuestos aza biciclicos como agonistas del receptor muscarinico m1.
GB201404922D0 (en) * 2014-03-19 2014-04-30 Heptares Therapeutics Ltd Pharmaceutical compounds
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
GB201513742D0 (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
CN108226319A (zh) * 2016-12-22 2018-06-29 亚宝药业集团股份有限公司 一种检测卡巴拉汀贴剂中光学异构体的方法
TW201922758A (zh) 2017-10-24 2019-06-16 美商歐樂根公司 烯胺及烯胺的非鏡像選擇性還原
JP6691928B2 (ja) * 2018-02-07 2020-05-13 株式会社ジンズホールディングス アイウエアセット及び信号処理ユニット
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
CN113121495A (zh) * 2020-01-10 2021-07-16 深圳市九明药业有限公司 一种地氯雷他定的制备方法
WO2025167860A1 (zh) * 2024-02-06 2025-08-14 南京迈诺威医药科技有限公司 一种含有占诺美林或其盐的药物组合物

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