GEP20207167B - Positive allosteric modulators of the muscarinic acetylcholine receptor m4 - Google Patents
Positive allosteric modulators of the muscarinic acetylcholine receptor m4Info
- Publication number
- GEP20207167B GEP20207167B GEAP201714954A GEAP2017014954A GEP20207167B GE P20207167 B GEP20207167 B GE P20207167B GE AP201714954 A GEAP201714954 A GE AP201714954A GE AP2017014954 A GEAP2017014954 A GE AP2017014954A GE P20207167 B GEP20207167 B GE P20207167B
- Authority
- GE
- Georgia
- Prior art keywords
- acetylcholine receptor
- muscarinic acetylcholine
- positive allosteric
- allosteric modulators
- muscarinic
- Prior art date
Links
- 102000000413 Muscarinic acetylcholine receptor M4 Human genes 0.000 title 1
- 108050008897 Muscarinic acetylcholine receptor M4 Proteins 0.000 title 1
- 230000003281 allosteric effect Effects 0.000 title 1
- 102000014415 Muscarinic acetylcholine receptor Human genes 0.000 abstract 1
- 108050003473 Muscarinic acetylcholine receptor Proteins 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000004064 dysfunction Effects 0.000 abstract 1
- 230000000926 neurological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
Classifications
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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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic 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
- C07D495/14—Ortho-condensed systems
-
- 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
- A61K31/495—Heterocyclic 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K31/495—Heterocyclic 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic 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
- C07D491/12—Heterocyclic 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
- C07D491/14—Ortho-condensed systems
- C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/12—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains three hetero rings
- C07D493/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic 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
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- 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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662353447P | 2016-06-22 | 2016-06-22 | |
| US201662418638P | 2016-11-07 | 2016-11-07 | |
| US201762471281P | 2017-03-14 | 2017-03-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| GEP20207167B true GEP20207167B (en) | 2020-10-12 |
Family
ID=60675830
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GEAP201714954A GEP20207167B (en) | 2016-06-22 | 2017-06-22 | Positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
Country Status (30)
| Country | Link |
|---|---|
| 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) |
| MX (1) | MX385384B (enExample) |
| 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) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201726675A (zh) | 2015-12-23 | 2017-08-01 | 默沙東藥廠 | M4毒蕈鹼乙醯膽鹼受體之異位調節劑6,7-二氫-5h-吡咯并[3,4-b]吡啶-5-酮 |
| 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 |
| 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 |
| WO2018112843A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor |
| WO2018112840A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | 6, 5-fused heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor |
| WO2019000236A1 (en) | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
| WO2019000237A1 (en) | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
| WO2019000238A1 (en) | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | 5- (PYRIDIN-3-YL) OXAZOLE ALLOSTERIC MODULATORS OF M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
| MA51036A (fr) | 2017-12-05 | 2021-03-17 | Univ Vanderbilt | Modulateurs allostériques positifs du récepteur muscarinique de l'acétylcholine m4 |
| TW201930311A (zh) | 2017-12-05 | 2019-08-01 | 泛德比爾特大學 | 蕈毒鹼型乙醯膽鹼受體m4之正向別構調節劑 |
| CN110950774B (zh) * | 2019-11-04 | 2021-04-13 | 北京大学 | 蛋白质定量标记试剂及其制备方法与应用 |
| EP4069367B1 (en) | 2019-12-06 | 2024-05-15 | Neurocrine Biosciences, Inc. | Muscarinic receptor 4 antagonists and methods of use |
| JP7707176B2 (ja) * | 2020-02-05 | 2025-07-14 | ニューロクライン バイオサイエンシーズ，インコーポレイテッド | ムスカリン性受容体４アンタゴニストおよび使用方法 |
| 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 |
| WO2022226078A1 (en) * | 2021-04-20 | 2022-10-27 | The Regents Of The University Of California | Therapy for alcohol-related liver disease |
| EP4447953A1 (en) | 2021-12-13 | 2024-10-23 | Sage Therapeutics, Inc. | Combination of muscarinic receptor positive modulators and nmda positive allosteric modulators |
| WO2025129082A1 (en) * | 2023-12-14 | 2025-06-19 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
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| PE20060526A1 (es) | 2004-06-15 | 2006-07-13 | Schering Corp | Compuestos triciclicos como antagonistas de mglur1 |
| EP1619196A1 (de) | 2004-07-23 | 2006-01-25 | Curacyte Discovery GmbH | Substituierte Pyrido[3',2':4,5]thieno[3,2-d]pyrimidine und Pyrido[3',2':4,5]furo[3,2-d]-pyrimidine zur Verwendung als Inhibitoren der PDA-4 und/oder TNF-alpha Freisetzung |
| ATE455777T1 (de) | 2004-07-23 | 2010-02-15 | Medicines Co Leipzig Gmbh | Substituierte pyridoä3',2':4,5üthienoä3,2- düpyrimidine und pyridoä3',2':4,5üfuroä3,2-dü- pyrimidine zur verwendung als inhibitoren der pda-4 und/oder tnf-alpha freisetzung |
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| US20080021063A1 (en) * | 2006-07-18 | 2008-01-24 | Kazantsev Aleksey G | Compositions and methods for modulating sirtuin activity |
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| WO2012131297A1 (en) | 2011-03-28 | 2012-10-04 | Jonathan Bayldon Baell | Pyrido [3',2' :4,5] thieno [3, 2-d] pyrimidin- 4 - ylamine derivatives and their therapeutical use |
| WO2013040534A1 (en) * | 2011-09-16 | 2013-03-21 | Vanderbilt University | Substituted 1h-pyrazolo[3',4',4,5]thieno[2,3-b]pyridin-3-amine analogs as positive allosteric modulatiors of the muscarinic acetycholine receptor m4 |
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| WO2013126856A1 (en) | 2012-02-23 | 2013-08-29 | Vanderbilt University | Substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
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| US9637498B2 (en) | 2013-08-23 | 2017-05-02 | Vanderbilt University | Substituted thieno[2,3-C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4 |
| WO2015027204A1 (en) | 2013-08-23 | 2015-02-26 | Vanderbilt University | Substituted thieno[2,3-b]pyridine-2-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
| US9981920B2 (en) * | 2014-06-26 | 2018-05-29 | Rodin Therapeutics, Inc. | Inhibitors of histone deacetylase |
| GEP20207167B (en) | 2016-06-22 | 2020-10-12 | Univ Vanderbilt | 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 |
| 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 |
| MA51036A (fr) * | 2017-12-05 | 2021-03-17 | Univ Vanderbilt | Modulateurs allostériques positifs du récepteur muscarinique de l'acétylcholine m4 |
-
2017
- 2017-06-22 GE GEAP201714954A patent/GEP20207167B/en unknown
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