ES2587137R1 - Use of the compounds derived from 3-alkyl-4-aryl-1,4,6,7,8,9-hexahydropyrazolo [4 ', 3': 5.6] pyran [2,3-b] quinolin-5- amine as dual inhibitors of GSK3B - AChE and Nrf2 inducers for the treatment of neurodegenerative diseases - Google Patents

Use of the compounds derived from 3-alkyl-4-aryl-1,4,6,7,8,9-hexahydropyrazolo [4 ', 3': 5.6] pyran [2,3-b] quinolin-5- amine as dual inhibitors of GSK3B - AChE and Nrf2 inducers for the treatment of neurodegenerative diseases Download PDF

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Publication number
ES2587137R1
ES2587137R1 ES201500274A ES201500274A ES2587137R1 ES 2587137 R1 ES2587137 R1 ES 2587137R1 ES 201500274 A ES201500274 A ES 201500274A ES 201500274 A ES201500274 A ES 201500274A ES 2587137 R1 ES2587137 R1 ES 2587137R1
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ES
Spain
Prior art keywords
hexahydropyrazolo
quinolin
pyran
aryl
amine
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
ES201500274A
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Spanish (es)
Other versions
ES2587137B1 (en
ES2587137A2 (en
Inventor
Sheila ABRIL COMESAÑA
Manuela García López
Maria Teresa RAMOS GARCÍA
José Carlos MENÉNDEZ RAMOS
Antonio Garcia Garcia
Rafael LEÓN MARTÍNEZ
Isabel GAMEIRO ROS
Giammarco TENTI
Patrycja MICHALSKA
Izaskun BUENDÍA ABAITUA
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Universidad Complutense de Madrid
Universidad Autonoma de Madrid
Fundacion para la Investigacion Biomedica del Hospital Universitario de la Princesa
Original Assignee
Universidad Complutense de Madrid
Universidad Autonoma de Madrid
Fundacion para la Investigacion Biomedica del Hospital Universitario de la Princesa
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Application filed by Universidad Complutense de Madrid, Universidad Autonoma de Madrid, Fundacion para la Investigacion Biomedica del Hospital Universitario de la Princesa filed Critical Universidad Complutense de Madrid
Priority to ES201500274A priority Critical patent/ES2587137B1/en
Publication of ES2587137A2 publication Critical patent/ES2587137A2/en
Publication of ES2587137R1 publication Critical patent/ES2587137R1/en
Application granted granted Critical
Publication of ES2587137B1 publication Critical patent/ES2587137B1/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presente invención se refiere al uso de derivados de 3-alquil-4-aril-1,4,6,7,8,9-hexahidropirazolo[4',3':5,6]pirano[2,3-b]quinolin-5-amina con actividad inhibidora dual de las enzimas glucógeno-sintasa-quinasa 3{be} y acetilcolinesterasa, capacidad inductora del factor de transcripción Nrf2, y capacidad neuroprotectora. Otro aspecto de la invención se refiere al uso de los derivados objeto de esta invención para el tratamiento de enfermedades en cuya patogénesis interviene la actividad anormal de estas enzimas en conjunto y/o el estrés oxidativo y/o enfermedades que cursen con desregulación de la actividad de genes de fase II activados por el factor Nrf2, como las enfermedades neurodegenerativas.The present invention relates to the use of 3-alkyl-4-aryl-1,4,6,7,8,9-hexahydropyrazolo [4 ', 3': 5,6] pyran [2,3-b] derivatives quinolin-5-amine with dual inhibitory activity of the enzymes glycogen synthase-kinase 3 {be} and acetylcholinesterase, inducing capacity of the transcription factor Nrf2, and neuroprotective capacity. Another aspect of the invention relates to the use of the derivatives object of this invention for the treatment of diseases whose pathogenesis involves the abnormal activity of these enzymes together and / or oxidative stress and / or diseases that occur with deregulation of the activity. of phase II genes activated by the Nrf2 factor, such as neurodegenerative diseases.

ES201500274A 2015-04-20 2015-04-20 Use of the compounds derived from 3-alkyl-4-aryl-1,4,6,7,8,9-hexahydropyrazolo [4 ', 3': 5.6] pyran [2,3-b] quinolin-5- amine as dual inhibitors of GSK3B - AChE and Nrf2 inducers for the treatment of neurodegenerative diseases Expired - Fee Related ES2587137B1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
ES201500274A ES2587137B1 (en) 2015-04-20 2015-04-20 Use of the compounds derived from 3-alkyl-4-aryl-1,4,6,7,8,9-hexahydropyrazolo [4 ', 3': 5.6] pyran [2,3-b] quinolin-5- amine as dual inhibitors of GSK3B - AChE and Nrf2 inducers for the treatment of neurodegenerative diseases

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
ES201500274A ES2587137B1 (en) 2015-04-20 2015-04-20 Use of the compounds derived from 3-alkyl-4-aryl-1,4,6,7,8,9-hexahydropyrazolo [4 ', 3': 5.6] pyran [2,3-b] quinolin-5- amine as dual inhibitors of GSK3B - AChE and Nrf2 inducers for the treatment of neurodegenerative diseases

Publications (3)

Publication Number Publication Date
ES2587137A2 ES2587137A2 (en) 2016-10-20
ES2587137R1 true ES2587137R1 (en) 2017-06-01
ES2587137B1 ES2587137B1 (en) 2018-03-16

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ES201500274A Expired - Fee Related ES2587137B1 (en) 2015-04-20 2015-04-20 Use of the compounds derived from 3-alkyl-4-aryl-1,4,6,7,8,9-hexahydropyrazolo [4 ', 3': 5.6] pyran [2,3-b] quinolin-5- amine as dual inhibitors of GSK3B - AChE and Nrf2 inducers for the treatment of neurodegenerative diseases

Country Status (1)

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ES (1) ES2587137B1 (en)

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050209297A1 (en) * 2000-08-31 2005-09-22 Pfizer Inc Pyrazole derivatives

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050209297A1 (en) * 2000-08-31 2005-09-22 Pfizer Inc Pyrazole derivatives

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Khoobi Mehdi et al. NEW TETRACYCLIC TACRINE ANALOGS CONTAINING PYRANO[2,3-C]PYRAZOLE: EFFICIENT SYNTHESIS, BIOLOGICAL ASSESSMENT AND DOCKING SIMULATION STUDY. European Journal of Medicinal Chemistry, 18/10/2014, Vol. 89, Páginas 296 - 303 [en línea][recuperado el 25/04/2017]. ISSN 0223-5234, (DOI: doi:10.1016/j.ejmech.2014.10.049) <p>Figura 1, tabla 1, compuestos 7a-l, página 299, conclusión,</p> *

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ES2587137B1 (en) 2018-03-16
ES2587137A2 (en) 2016-10-20

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