AU2017281228B2 - Positive allosteric modulators of the muscarinic acetylcholine receptor M4 - Google Patents

Positive allosteric modulators of the muscarinic acetylcholine receptor M4 Download PDF

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AU2017281228B2
AU2017281228B2 AU2017281228A AU2017281228A AU2017281228B2 AU 2017281228 B2 AU2017281228 B2 AU 2017281228B2 AU 2017281228 A AU2017281228 A AU 2017281228A AU 2017281228 A AU2017281228 A AU 2017281228A AU 2017281228 B2 AU2017281228 B2 AU 2017281228B2
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thieno
pyridazin
methyl
amine
dimethyl
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AU2017281228A1 (en
Inventor
Sean BOLLINGER
Thomas M. Bridges
P. Jeffrey Conn
Darren W. Engers
Julie L. Engers
Craig W. Lindsley
Madeline LONG
Paul Spearing
James C. Tarr
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Vanderbilt University
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Vanderbilt University
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    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14Ortho-condensed systems
    • 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
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
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    • 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
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14Ortho-condensed systems
    • C07D491/147Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/12Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains three hetero rings
    • C07D493/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Anesthesiology (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Liquid Crystal Substances (AREA)
  • Control Of El Displays (AREA)
  • Electrochromic Elements, Electrophoresis, Or Variable Reflection Or Absorption Elements (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2017281228A 2016-06-22 2017-06-22 Positive allosteric modulators of the muscarinic acetylcholine receptor M4 Active AU2017281228B2 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201662353447P 2016-06-22 2016-06-22
US62/353,447 2016-06-22
US201662418638P 2016-11-07 2016-11-07
US62/418,638 2016-11-07
US201762471281P 2017-03-14 2017-03-14
US62/471,281 2017-03-14
PCT/US2017/038711 WO2017223290A1 (en) 2016-06-22 2017-06-22 Positive allosteric modulators of the muscarinic acetylcholine receptor m4

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AU2017281228A1 AU2017281228A1 (en) 2018-12-20
AU2017281228B2 true AU2017281228B2 (en) 2021-02-18

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US (5) US10239887B2 (enExample)
EP (2) EP4186910A1 (enExample)
JP (1) JP7038414B2 (enExample)
KR (1) KR102474326B1 (enExample)
CN (2) CN116178391A (enExample)
AU (1) AU2017281228B2 (enExample)
BR (1) BR112018003417B1 (enExample)
CL (1) CL2018003669A1 (enExample)
CO (1) CO2018013600A2 (enExample)
CR (1) CR20180598A (enExample)
DK (1) DK3474846T3 (enExample)
DO (1) DOP2018000263A (enExample)
EC (1) ECSP18094769A (enExample)
ES (1) ES2936827T3 (enExample)
FI (1) FI3474846T3 (enExample)
GE (1) GEP20207167B (enExample)
IL (1) IL263500B (enExample)
JO (1) JOP20180114B1 (enExample)
MA (1) MA45463A (enExample)
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NI (1) NI201800141A (enExample)
PE (1) PE20190446A1 (enExample)
PH (1) PH12018502638B1 (enExample)
RU (1) RU2750935C2 (enExample)
SG (1) SG11201810794VA (enExample)
SV (1) SV2018005800A (enExample)
TN (1) TN2018000416A1 (enExample)
UA (1) UA125874C2 (enExample)
WO (1) WO2017223290A1 (enExample)
ZA (1) ZA201808219B (enExample)

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GEP20207167B (en) 2016-06-22 2020-10-12 Univ Vanderbilt Positive allosteric modulators of the muscarinic acetylcholine receptor m4
CN109863139B (zh) 2016-11-07 2023-02-17 范德比尔特大学 毒蕈碱型乙酰胆碱受体m4的正向别构调节剂
US11008335B2 (en) 2016-11-07 2021-05-18 Vanderbilt University Positive allosteric modulators of the muscarinic acetylcholine receptor M4
CN109862893B (zh) 2016-11-07 2023-02-17 范德比尔特大学 毒蕈碱型乙酰胆碱受体m4的正向别构调节剂
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
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AU2017281228A1 (en) 2018-12-20
TN2018000416A1 (en) 2020-06-15
EP3474846A1 (en) 2019-05-01
DK3474846T3 (da) 2023-02-06
US10239887B2 (en) 2019-03-26
RU2018142987A3 (enExample) 2020-07-24
EP4186910A1 (en) 2023-05-31
JP2019523233A (ja) 2019-08-22
CO2018013600A2 (es) 2018-12-28
BR112018003417B1 (pt) 2023-10-24
WO2017223290A1 (en) 2017-12-28
ECSP18094769A (es) 2019-01-31
CA3026578A1 (en) 2017-12-28
JOP20180114B1 (ar) 2022-09-15
MX385384B (es) 2025-03-18
UA125874C2 (uk) 2022-06-29
US20170369505A1 (en) 2017-12-28
MA45463A (fr) 2019-05-01
JP7038414B2 (ja) 2022-03-18
RU2018142987A (ru) 2020-07-22
PH12018502638B1 (en) 2023-03-24
CR20180598A (es) 2019-11-20
CL2018003669A1 (es) 2019-02-01
EP3474846B1 (en) 2022-11-30
PH12018502638A1 (en) 2019-10-21
BR112018003417A2 (enExample) 2018-10-02
US20230348490A1 (en) 2023-11-02
CN109310668A (zh) 2019-02-05
SG11201810794VA (en) 2019-01-30
KR20190018645A (ko) 2019-02-25
ZA201808219B (en) 2020-05-27
RU2750935C2 (ru) 2021-07-06
PE20190446A1 (es) 2019-03-29
ES2936827T3 (es) 2023-03-22
NI201800141A (es) 2020-07-22
DOP2018000263A (es) 2019-03-31
IL263500B (en) 2021-09-30
EP3474846A4 (en) 2019-12-04
CN116178391A (zh) 2023-05-30
US20190161498A1 (en) 2019-05-30
IL263500A (en) 2019-01-31
NZ748982A (en) 2024-11-29
JOP20180114A1 (ar) 2019-01-30
MX2018015878A (es) 2019-05-27
KR102474326B1 (ko) 2022-12-05
US20250026764A1 (en) 2025-01-23
US20230014109A1 (en) 2023-01-19
FI3474846T3 (fi) 2023-02-16
SV2018005800A (es) 2019-02-13
US11142532B2 (en) 2021-10-12
CN109310668B (zh) 2023-01-24
GEP20207167B (en) 2020-10-12

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