ECSP18094769A - Moduladores alostéricos positivos del receptor muscarínico de acetilcolina m4 - Google Patents
Moduladores alostéricos positivos del receptor muscarínico de acetilcolina m4Info
- Publication number
- ECSP18094769A ECSP18094769A ECSENADI201894769A ECDI201894769A ECSP18094769A EC SP18094769 A ECSP18094769 A EC SP18094769A EC SENADI201894769 A ECSENADI201894769 A EC SENADI201894769A EC DI201894769 A ECDI201894769 A EC DI201894769A EC SP18094769 A ECSP18094769 A EC SP18094769A
- Authority
- EC
- Ecuador
- Prior art keywords
- amine
- compounds
- muscarinic acetylcholine
- positive allosteric
- allosteric modulators
- Prior art date
Links
- 230000003281 allosteric effect Effects 0.000 title abstract 2
- OIPILFWXSMYKGL-UHFFFAOYSA-N acetylcholine Chemical compound CC(=O)OCC[N+](C)(C)C OIPILFWXSMYKGL-UHFFFAOYSA-N 0.000 title 1
- 229960004373 acetylcholine Drugs 0.000 title 1
- 230000003551 muscarinic effect Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- YOJZNEVXQGTIHY-UHFFFAOYSA-N 8-oxa-3,5,10,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaen-6-amine Chemical compound N1=NC=CC2=C1OC1=C2N=CN=C1N YOJZNEVXQGTIHY-UHFFFAOYSA-N 0.000 abstract 1
- VOTWWJBOLAGEDB-UHFFFAOYSA-N 8-thia-3,5,10,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaen-6-amine Chemical compound N1=NC=CC2=C1SC1=C2N=CN=C1N VOTWWJBOLAGEDB-UHFFFAOYSA-N 0.000 abstract 1
- 102000014415 Muscarinic acetylcholine receptor Human genes 0.000 abstract 1
- 108050003473 Muscarinic acetylcholine receptor Proteins 0.000 abstract 1
- 102000000413 Muscarinic acetylcholine receptor M4 Human genes 0.000 abstract 1
- 108050008897 Muscarinic acetylcholine receptor M4 Proteins 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- HVWJATXZZQPVEL-UHFFFAOYSA-N furo[3,2-d]pyrimidin-4-amine Chemical compound NC1=NC=NC2=C1OC=C2 HVWJATXZZQPVEL-UHFFFAOYSA-N 0.000 abstract 1
- 230000007257 malfunction Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000000926 neurological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- OYRRZWATULMEPF-UHFFFAOYSA-N pyrimidin-4-amine Chemical compound NC1=CC=NC=N1 OYRRZWATULMEPF-UHFFFAOYSA-N 0.000 abstract 1
- QIZMFTNGJPBSBT-UHFFFAOYSA-N thieno[3,2-d]pyrimidin-4-amine Chemical compound NC1=NC=NC2=C1SC=C2 QIZMFTNGJPBSBT-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- 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
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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
-
- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Anesthesiology (AREA)
- Psychology (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)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Liquid Crystal Substances (AREA)
- Control Of El Displays (AREA)
- Electrochromic Elements, Electrophoresis, Or Variable Reflection Or Absorption Elements (AREA)
Abstract
En este documento se divulgan compuestos tricíclicos, incluyendo los compuestos pirimido[4',5':4,5]tieno[2,3-c]piridazin-8-amina, pirido[3',2':4,5]tieno[3,2-d]pirimidin-4-amina, pirazino[2',3':4,5]tieno[3,2-d]pirimidin-4-amina, pirido[3',2':4,5]furo[3,2-d]pirimidin-4-amina y pirimido[4',5':4,5]furo[2,3-c]piridazin-8-amina, que pueden ser útiles como moduladores alostéricos positivos del receptor muscarínico de acetilcolina M4 (mAChR M4). En este documento también se divulgan métodos de preparación de los compuestos, composiciones farmacéuticas que comprenden los compuestos y métodos de tratamiento de trastornos neurológicos y psiquiátricos asociados con el mal funcionamiento del receptor muscarínico de acetilcolina usando los compuestos y composiciones.
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 |
|---|---|
| ECSP18094769A true ECSP18094769A (es) | 2019-01-31 |
Family
ID=60675830
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSENADI201894769A ECSP18094769A (es) | 2016-06-22 | 2018-12-20 | Moduladores alostéricos positivos del receptor muscarínico de acetilcolina m4 |
Country Status (30)
| Country | Link |
|---|---|
| US (5) | US10239887B2 (es) |
| EP (2) | EP3474846B1 (es) |
| JP (1) | JP7038414B2 (es) |
| KR (1) | KR102474326B1 (es) |
| CN (2) | CN116178391A (es) |
| AU (1) | AU2017281228B2 (es) |
| BR (1) | BR112018003417B1 (es) |
| CL (1) | CL2018003669A1 (es) |
| CO (1) | CO2018013600A2 (es) |
| CR (1) | CR20180598A (es) |
| DK (1) | DK3474846T3 (es) |
| DO (1) | DOP2018000263A (es) |
| EC (1) | ECSP18094769A (es) |
| ES (1) | ES2936827T3 (es) |
| FI (1) | FI3474846T3 (es) |
| GE (2) | GEP20207167B (es) |
| IL (1) | IL263500B (es) |
| JO (1) | JOP20180114B1 (es) |
| MA (1) | MA45463A (es) |
| MX (1) | MX385384B (es) |
| NI (1) | NI201800141A (es) |
| PE (1) | PE20190446A1 (es) |
| PH (1) | PH12018502638B1 (es) |
| RU (1) | RU2750935C2 (es) |
| SG (1) | SG11201810794VA (es) |
| SV (1) | SV2018005800A (es) |
| TN (1) | TN2018000416A1 (es) |
| UA (1) | UA125874C2 (es) |
| WO (1) | WO2017223290A1 (es) |
| ZA (1) | ZA201808219B (es) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017112719A1 (en) | 2015-12-23 | 2017-06-29 | Merck Sharp & Dohme Corp. | 6,7-dihydro-5h-pyrrolo[3,4-b]pyridin-5-one allosteric modulators of the m4 muscarinic acetylcholine receptor |
| 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 |
| ES2936827T3 (es) * | 2016-06-22 | 2023-03-22 | Univ Vanderbilt | Moduladores alostéricos positivos del receptor muscarínico de acetilcolina M4 |
| WO2018085813A1 (en) * | 2016-11-07 | 2018-05-11 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
| MA47126A (fr) | 2016-11-07 | 2019-10-30 | Univ Vanderbilt | Modulateurs allostériques positifs du récepteur muscarinique à l'acétylcholine m4 |
| EP3534901B1 (en) | 2016-11-07 | 2022-06-22 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
| 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 |
| 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 |
| WO2018112843A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine 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 |
| 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 |
| 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 |
| WO2019113174A1 (en) | 2017-12-05 | 2019-06-13 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
| 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 |
| EP4100410A1 (en) * | 2020-02-05 | 2022-12-14 | Neurocrine Biosciences, Inc. | Muscarinic receptor 4 antagonists and methods of use |
| 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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