AR086791A1 - POSITIVE ALLOSTERIC MODULATORS OF NICOTINIC ACETILCOLINE RECEIVER - Google Patents
POSITIVE ALLOSTERIC MODULATORS OF NICOTINIC ACETILCOLINE RECEIVERInfo
- Publication number
- AR086791A1 AR086791A1 ARP120102330A ARP120102330A AR086791A1 AR 086791 A1 AR086791 A1 AR 086791A1 AR P120102330 A ARP120102330 A AR P120102330A AR P120102330 A ARP120102330 A AR P120102330A AR 086791 A1 AR086791 A1 AR 086791A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- compounds
- alkynyl
- cyano
- alkenyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic 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
- C07D471/02—Heterocyclic 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
- C07D471/04—Ortho-condensed systems
-
- 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
- A61P25/28—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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente se refiere a compuestos útiles en terapia, a composiciones que comprenden dichos compuestos, y a métodos de tratamiento de enfermedades, que comprenden la administración de dichos compuestos. Los compuestos referidos son moduladores alostéricos positivos (PAM) del receptor de acetilcolina nicotínico a7. Los compuestos son útiles para el tratamiento de la enfermedad de Alzheimer, demencia senil y otras, epilepsia, amnesia postraumática. Reivindicación 1: Un compuesto de acuerdo con la fórmula (1), donde A⁴ es C-R⁴ o N, A⁵ es C-R⁵ o N, y A⁶ es C-R⁶ o N, siempre que por lo menos uno de A⁴, A⁵ o A⁶ sea N, y no más de dos de A⁴, A⁵ y A⁶ sean N; R¹ es fenilo o heteroarilo; donde dicho fenilo o heteroarilo está opcionalmente sustituido con uno o más sustituyentes R¹¹, donde cada R¹¹ es individualmente seleccionado de alquilo C₁₋₆, halógeno, hidroxi, haloalquilo C₁₋₆, alcoxi C₁₋₆, haloalcoxi C₁₋₆, ciano, alquil C₁₋₆sulfonilo, -S(O)₂NH₂ y -NR¹²R¹³, donde R¹² y R¹³ representan, de manera independiente, hidrógeno o alquilo C₁₋₆; R² se selecciona de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, alcoxi C₁₋₆, halógeno y ciano; R³, R⁴, R⁵, R⁶ y R⁷ se seleccionan, de manera independiente entre sí, de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, alcoxi C₁₋₆, halógeno, ciano y -NR⁹R¹⁰, donde R⁹ y R¹⁰ representan, de manera independiente, hidrógeno, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆ o fenilo; R⁸ se selecciona de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, alcoxi C₁₋₆, halógeno, ciano y fenilo; y una de sus sales farmacéuticamente aceptables.This refers to compounds useful in therapy, to compositions comprising said compounds, and to methods of treatment of diseases, which comprise the administration of said compounds. The referred compounds are positive allosteric modulators (PAM) of the nicotinic acetylcholine a7 receptor. The compounds are useful for the treatment of Alzheimer's disease, senile dementia and others, epilepsy, posttraumatic amnesia. Claim 1: A compound according to formula (1), wherein A⁴ is C-R⁴ or N, A⁵ is C-R⁵ or N, and A⁶ is C-R⁶ or N, provided that at least one of A⁴, A⁵ or A⁶ be N, and no more than two of A⁴, A⁵ and A⁶ are N; R¹ is phenyl or heteroaryl; wherein said phenyl or heteroaryl is optionally substituted with one or more R¹¹ substituents, where each R¹¹ is individually selected from C₁₋₆ alkyl, halogen, hydroxy, C₁₋₆ haloalkyl, C₁₋₆ alkoxy, C₁₋₆ haloalkoxy, cyano, C₁ alkyl Ulfsulfonyl, -S (O) ₂NH₂ and -NR¹²R¹³, where R¹² and R¹³ independently represent hydrogen or C₁₋₆ alkyl; R² is selected from H, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ alkoxy, halogen and cyano; R³, R⁴, R⁵, R⁶ and R⁷ are independently selected from H, C alquilo alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ alkoxy, halogen, cyano and -NR⁹R¹⁰, where R⁹ and R¹⁰ independently represent hydrogen, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl or phenyl; R⁸ is selected from H, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ alkoxy, halogen, cyano and phenyl; and one of its pharmaceutically acceptable salts.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201100498 | 2011-07-01 | ||
| DKPA201100514 | 2011-07-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR086791A1 true AR086791A1 (en) | 2014-01-22 |
Family
ID=46456582
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120102330A AR086791A1 (en) | 2011-07-01 | 2012-06-28 | POSITIVE ALLOSTERIC MODULATORS OF NICOTINIC ACETILCOLINE RECEIVER |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR086791A1 (en) |
| TW (1) | TW201315731A (en) |
| WO (1) | WO2013004617A1 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201801193QA (en) * | 2015-08-19 | 2018-03-28 | Astellas Pharma Inc | Tetrahydrooxepinopyridine compound |
| JP2019006680A (en) * | 2015-11-13 | 2019-01-17 | 国立大学法人大阪大学 | Pyrazolo pyridine derivatives and use thereof |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9903997D0 (en) | 1999-11-03 | 1999-11-03 | Astra Ab | New compounds |
| CA2622677A1 (en) * | 2005-09-23 | 2007-04-05 | Richard Schumacher | Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof |
| US8536221B2 (en) | 2008-02-07 | 2013-09-17 | Abbvie Inc. | Amide derivatives as positive allosteric modulators and methods of use thereof |
-
2012
- 2012-06-28 AR ARP120102330A patent/AR086791A1/en not_active Application Discontinuation
- 2012-06-29 TW TW101123404A patent/TW201315731A/en unknown
- 2012-06-29 WO PCT/EP2012/062703 patent/WO2013004617A1/en active Application Filing
Also Published As
| Publication number | Publication date |
|---|---|
| TW201315731A (en) | 2013-04-16 |
| WO2013004617A1 (en) | 2013-01-10 |
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| FA | Abandonment or withdrawal |