BR112018013763A2 - moduladores alostéricos positivos do receptor muscarínico de acetilclona m4 - Google Patents
moduladores alostéricos positivos do receptor muscarínico de acetilclona m4Info
- Publication number
- BR112018013763A2 BR112018013763A2 BR112018013763-4A BR112018013763A BR112018013763A2 BR 112018013763 A2 BR112018013763 A2 BR 112018013763A2 BR 112018013763 A BR112018013763 A BR 112018013763A BR 112018013763 A2 BR112018013763 A2 BR 112018013763A2
- Authority
- BR
- Brazil
- Prior art keywords
- muscarinic
- positive allosteric
- allosteric modulators
- acetylclone
- compounds
- Prior art date
Links
- 230000003281 allosteric effect Effects 0.000 title abstract 2
- 230000003551 muscarinic effect Effects 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 3
- ZRZXSPXFHOKSLE-UHFFFAOYSA-N 8-thia-3,5,10,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaene Chemical class N1=NC=CC2=C1SC1=C2N=CN=C1 ZRZXSPXFHOKSLE-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
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- OIPILFWXSMYKGL-UHFFFAOYSA-N acetylcholine Chemical compound CC(=O)OCC[N+](C)(C)C OIPILFWXSMYKGL-UHFFFAOYSA-N 0.000 abstract 1
- 229960004373 acetylcholine Drugs 0.000 abstract 1
- 230000004064 dysfunction 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
- OHEQODPULDINCT-UHFFFAOYSA-N pyrido[4,5]thieno[1,2-b]pyrimidine Chemical compound N1=CN=C2C3=CC=CN=C3SC2=C1 OHEQODPULDINCT-UHFFFAOYSA-N 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
Classifications
-
- 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
- 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
- A61K31/505—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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662418663P | 2016-11-07 | 2016-11-07 | |
| US62/418,663 | 2016-11-07 | ||
| PCT/US2017/060324 WO2018085808A1 (en) | 2016-11-07 | 2017-11-07 | Positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112018013763A2 true BR112018013763A2 (pt) | 2018-12-11 |
Family
ID=62076580
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112018013763-4A BR112018013763A2 (pt) | 2016-11-07 | 2017-11-07 | moduladores alostéricos positivos do receptor muscarínico de acetilclona m4 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10961253B2 (https=) |
| EP (1) | EP3558309B1 (https=) |
| JP (1) | JP7099725B2 (https=) |
| CN (1) | CN109862893B (https=) |
| BR (1) | BR112018013763A2 (https=) |
| MA (1) | MA47126A (https=) |
| WO (1) | WO2018085808A1 (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX385384B (es) | 2016-06-22 | 2025-03-18 | Univ Vanderbilt | Moduladores alostericos positivos del receptor muscarinico de acetilcolina m4 |
| WO2018085813A1 (en) | 2016-11-07 | 2018-05-11 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
| WO2018085803A1 (en) | 2016-11-07 | 2018-05-11 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor 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 |
| EP4182316A1 (en) | 2020-07-15 | 2023-05-24 | Vanderbilt University | 7-(piperidin-1-yl)-4h-pyrimido[1,2-b]pyridazin-4-one derivatives as positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
| WO2023114224A1 (en) | 2021-12-13 | 2023-06-22 | Sage Therapeutics, Inc. | Combination of muscarinic receptor positive modulators and nmda positive allosteric modulators |
Family Cites Families (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5594001A (en) | 1993-04-08 | 1997-01-14 | The Dupont Merck Pharmaceutical Company | Polycyclic systems, and derivatives thereof, as neurotransmitter release enhancers useful in the treatment of cognitive disorders |
| IL112248A0 (en) * | 1994-01-25 | 1995-03-30 | Warner Lambert Co | Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them |
| US5679683A (en) | 1994-01-25 | 1997-10-21 | Warner-Lambert Company | Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family |
| US20020168761A1 (en) | 2000-01-24 | 2002-11-14 | Gour Barbara J. | Peptidomimetic modulators of cell adhesion |
| US6608053B2 (en) | 2000-04-27 | 2003-08-19 | Yamanouchi Pharmaceutical Co., Ltd. | Fused heteroaryl derivatives |
| US20040235809A1 (en) | 2000-07-27 | 2004-11-25 | Alexander John C | Epoxy steroidal aldosterone antagonist and beta-adremergic antagonist combination therepy for treatment of congestive heart failure |
| US7291733B2 (en) | 2003-10-10 | 2007-11-06 | Boehringer Ingelheim Pharmaceuticals, Inc. | Substituted tricyclic heterocycles and their uses |
| US20090099165A1 (en) | 2003-10-14 | 2009-04-16 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Protein Kinase Inhibitors |
| AU2004282179B2 (en) | 2003-10-14 | 2011-05-19 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Protein kinase inhibitors |
| AR049300A1 (es) | 2004-06-15 | 2006-07-12 | Schering Corp | Compuestos triciclicos antagonistas de mglur1 como agentes terapeuticos |
| DE502005008916D1 (de) | 2004-07-23 | 2010-03-11 | 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 |
| 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 |
| BRPI0517438A (pt) | 2004-10-25 | 2008-10-07 | Lilly Co Eli | composto, método para tratar a condição associada com atividade de receptor muscarìnico m4, uso do composto, e, composição farmacêutica |
| ES2259892B1 (es) | 2004-11-30 | 2007-11-01 | Laboratorios Almirall S.A. | Nuevos derivados de piridotienopirimidina. |
| ES2259891B1 (es) | 2004-11-30 | 2007-11-01 | Laboratorios Almirall S.A. | Nuevos derivados de piridotienopirimidina. |
| WO2006138418A2 (en) | 2005-06-14 | 2006-12-28 | President And Fellows Of Harvard College | Improvement of cognitive performance with sirtuin activators |
| AR059901A1 (es) | 2006-03-20 | 2008-05-07 | Bayer Pharmaceuticals Corp | Compuestos de tetrahidropiridotienopirimidina utiles para tratar o prevenir trastornos proliferativos celulares. |
| EP2043654A2 (en) * | 2006-06-12 | 2009-04-08 | Vertex Pharmaceuticals, Inc. | Thienopyrimidines useful as modulators of ion channels |
| US8153803B2 (en) * | 2006-07-18 | 2012-04-10 | The General Hospital Corporation | Compositions and methods for modulating sirtuin activity |
| US20080021063A1 (en) | 2006-07-18 | 2008-01-24 | Kazantsev Aleksey G | Compositions and methods for modulating sirtuin activity |
| US7547781B2 (en) | 2006-09-11 | 2009-06-16 | Curis, Inc. | Quinazoline based EGFR inhibitors containing a zinc binding moiety |
| EP2079736B1 (en) | 2006-12-29 | 2017-10-18 | Rigel Pharmaceuticals, Inc. | Substituted triazoles useful as axl inhibitors |
| US20090105240A1 (en) | 2007-10-17 | 2009-04-23 | Tomas Mustelin | Methods for treating leukemia and myelodysplastic syndrome, and methods for identifying agents for treating same |
| WO2009151569A2 (en) | 2008-06-09 | 2009-12-17 | Combinatorx, Incorporated | Beta adrenergic receptor agonists for the treatment of b-cell proliferative disorders |
| IN2012DN01325A (https=) | 2009-08-20 | 2015-06-05 | Karus Therapeutics Ltd | |
| US20110178107A1 (en) | 2010-01-20 | 2011-07-21 | Taigen Biotechnology Co., Ltd. | Hcv protease inhibitors |
| 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 |
| US9056876B2 (en) | 2011-09-16 | 2015-06-16 | Vanderbilt University | Substituted 1H-pyrazolo[3′,4′,4,5]thieno[2,3-b]pyridin-3-amine analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4 |
| US20130116241A1 (en) | 2011-11-09 | 2013-05-09 | Abbvie Inc. | Novel inhibitor compounds of phosphodiesterase type 10a |
| CA2859985C (en) | 2011-12-21 | 2020-11-03 | The Regents Of The University Of Colorado | Anti-cancer compounds targeting ral gtpases and methods of using the same |
| US8697888B2 (en) | 2012-01-06 | 2014-04-15 | Vanderbilt University | Substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs as antagonists of muscarinic acetylcholine M1 receptors |
| US9493481B2 (en) | 2012-02-23 | 2016-11-15 | Vanderbilt University | Substituted 5-aminothieno[2,3—C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4 |
| HK1210696A1 (en) | 2012-07-11 | 2016-05-06 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| US9056875B2 (en) | 2012-08-31 | 2015-06-16 | Vanderbilt University | Substituted pyrazolo[3′,4′:4,5]thieno[2,3-C]pyridazin-3-amine analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4 |
| 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 |
| MX385384B (es) * | 2016-06-22 | 2025-03-18 | Univ Vanderbilt | Moduladores alostericos positivos del receptor muscarinico de acetilcolina m4 |
| WO2018085803A1 (en) | 2016-11-07 | 2018-05-11 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
| WO2018085813A1 (en) | 2016-11-07 | 2018-05-11 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
-
2017
- 2017-11-07 US US16/347,450 patent/US10961253B2/en active Active
- 2017-11-07 EP EP17867920.5A patent/EP3558309B1/en active Active
- 2017-11-07 CN CN201780066090.6A patent/CN109862893B/zh active Active
- 2017-11-07 JP JP2019522981A patent/JP7099725B2/ja active Active
- 2017-11-07 BR BR112018013763-4A patent/BR112018013763A2/pt not_active Application Discontinuation
- 2017-11-07 MA MA047126A patent/MA47126A/fr unknown
- 2017-11-07 WO PCT/US2017/060324 patent/WO2018085808A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| EP3558309B1 (en) | 2023-07-26 |
| JP2019537590A (ja) | 2019-12-26 |
| JP7099725B2 (ja) | 2022-07-12 |
| WO2018085808A1 (en) | 2018-05-11 |
| MA47126A (fr) | 2019-10-30 |
| EP3558309A4 (en) | 2020-07-01 |
| CN109862893B (zh) | 2023-02-17 |
| EP3558309A1 (en) | 2019-10-30 |
| US10961253B2 (en) | 2021-03-30 |
| CN109862893A (zh) | 2019-06-07 |
| US20190330225A1 (en) | 2019-10-31 |
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