AU2018351651B2 - Antagonists of the muscarinic acetylcholine receptor M4 - Google Patents

Antagonists of the muscarinic acetylcholine receptor M4 Download PDF

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AU2018351651B2
AU2018351651B2 AU2018351651A AU2018351651A AU2018351651B2 AU 2018351651 B2 AU2018351651 B2 AU 2018351651B2 AU 2018351651 A AU2018351651 A AU 2018351651A AU 2018351651 A AU2018351651 A AU 2018351651A AU 2018351651 B2 AU2018351651 B2 AU 2018351651B2
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hexahydro
cyclopenta
pyridazin
pyrrol
amine
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AU2018351651A1 (en
Inventor
Logan A. BAKER
Aaron M. Bender
P. Jeffrey Conn
Darren W. Engers
Julie L. Engers
Craig W. Lindsley
Kayla J. TEMPLE
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Vanderbilt University
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Vanderbilt University
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    • 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
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • 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
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    • C07B59/002Heterocyclic compounds
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
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    • 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
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    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
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    • C07ORGANIC CHEMISTRY
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    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D471/04Ortho-condensed systems
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
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    • C07D493/08Bridged systems
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    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
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    • C07B2200/07Optical isomers

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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Indole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AU2018351651A 2017-10-20 2018-10-20 Antagonists of the muscarinic acetylcholine receptor M4 Active AU2018351651B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2023202086A AU2023202086B2 (en) 2017-10-20 2023-04-04 Antagonists of the muscarinic acetylcholine receptor M4

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762574912P 2017-10-20 2017-10-20
US62/574,912 2017-10-20
PCT/US2018/056803 WO2019079783A1 (en) 2017-10-20 2018-10-20 ANTAGONISTS OF THE MUSCARINIC RECEPTOR OF ACETYLCHOLINE M4

Related Child Applications (1)

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AU2023202086A Division AU2023202086B2 (en) 2017-10-20 2023-04-04 Antagonists of the muscarinic acetylcholine receptor M4

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AU2018351651A1 AU2018351651A1 (en) 2020-06-04
AU2018351651B2 true AU2018351651B2 (en) 2023-01-05

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US (3) US11299481B2 (OSRAM)
EP (1) EP3697759A4 (OSRAM)
JP (1) JP7270989B2 (OSRAM)
KR (2) KR102776114B1 (OSRAM)
CN (2) CN118063442A (OSRAM)
AU (2) AU2018351651B2 (OSRAM)
CA (1) CA3079617A1 (OSRAM)
IL (2) IL273924B2 (OSRAM)
WO (1) WO2019079783A1 (OSRAM)

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WO2021067696A1 (en) 2019-10-04 2021-04-08 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
US20230122344A1 (en) * 2019-12-10 2023-04-20 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
US20230150986A1 (en) * 2019-12-10 2023-05-18 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
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EP4139303A1 (en) * 2020-04-24 2023-03-01 Vanderbilt University Condensed substituted hydropyrroles as antagonists of the muscarinic acetylcholine receptor m4
WO2021216949A1 (en) * 2020-04-24 2021-10-28 Vanderbilt University Condensed substituted hydropyrroles as antagonists of the muscarinic acetylcholine receptor m4
EP4196473B1 (en) * 2020-08-13 2024-10-02 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
WO2022109099A1 (en) * 2020-11-18 2022-05-27 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
CN116669737A (zh) * 2020-12-22 2023-08-29 范德堡大学 毒蕈碱型乙酰胆碱受体m4的拮抗剂
KR20230124608A (ko) * 2020-12-22 2023-08-25 반더빌트유니버시티 무스카린성 아세틸콜린 수용체 m4의 길항제
CN117120435A (zh) * 2021-04-01 2023-11-24 小野药品工业株式会社 Abhd6拮抗剂
US20240174655A1 (en) * 2021-04-02 2024-05-30 Vanderbilt University Indazole derivatives as antagonists of the muscarinic acetylcholine receptor m4
US20240228468A1 (en) * 2021-04-05 2024-07-11 Vanderbilt University N-(6-((octahydrocyclopenta[c]pyrrol-5-yi)amino)pyridazin-3-yl)phenyl)carboxamide and (6- ((octahydrocyclopenta[c]pyrrol-5-yl)amino)pyridazin-3-yl)benzamide derivatives as machr m4 antagonists for the treatment of neurodegenerative disorders
JP2024532729A (ja) * 2021-08-09 2024-09-10 シロナックス リミテッド. フェロトーシス調節物質、その調製及び使用
WO2023141511A1 (en) * 2022-01-19 2023-07-27 Vanderbilt University Positive allosteric modulators of the muscarinic acetylcholine receptor m4
JP2024052624A (ja) * 2022-09-30 2024-04-11 小野薬品工業株式会社 Abhd6アンタゴニストを含有する医薬組成物

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