WO2011041989A3 - Sistemas tricíclicos y tetracíclicos con actividad sobre el sistema nervioso central y vascular - Google Patents

Sistemas tricíclicos y tetracíclicos con actividad sobre el sistema nervioso central y vascular Download PDF

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Publication number
WO2011041989A3
WO2011041989A3 PCT/CU2010/000004 CU2010000004W WO2011041989A3 WO 2011041989 A3 WO2011041989 A3 WO 2011041989A3 CU 2010000004 W CU2010000004 W CU 2010000004W WO 2011041989 A3 WO2011041989 A3 WO 2011041989A3
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WO
WIPO (PCT)
Prior art keywords
tricyclic
derivatives
ortho
systems
dihydropyridine
Prior art date
Application number
PCT/CU2010/000004
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English (en)
French (fr)
Other versions
WO2011041989A2 (es
Inventor
Yamila Verdecia Reyes
Estael OCHOA RODRÍGUEZ
Alberto Ruiz Reyes
Yanier NUÑEZ FIGUEREDO
Carmen CARILLO DOMÍNGUEZ
Juan Enrique Tacoronte Morales
Livan Lázaro ALBA GUTIÉRREZ
Gilberto Lázaro PARDO ANDREU
Original Assignee
Centro de Investigación y Desarrollo de Medicamentos (CIDEM)
Laboratorio De Síntesis Orgánica De La Facultad De Química De La Universidad De La Habana
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Centro de Investigación y Desarrollo de Medicamentos (CIDEM), Laboratorio De Síntesis Orgánica De La Facultad De Química De La Universidad De La Habana filed Critical Centro de Investigación y Desarrollo de Medicamentos (CIDEM)
Priority to CA2777209A priority Critical patent/CA2777209C/en
Priority to EP10821598.9A priority patent/EP2487174A4/en
Priority to US13/500,983 priority patent/US9315497B2/en
Priority to CN2010800556597A priority patent/CN102656171A/zh
Priority to JP2012532450A priority patent/JP2013507329A/ja
Publication of WO2011041989A2 publication Critical patent/WO2011041989A2/es
Publication of WO2011041989A3 publication Critical patent/WO2011041989A3/es
Priority to ZA2012/03295A priority patent/ZA201203295B/en
Priority to US14/282,111 priority patent/US10138231B2/en
Priority to US16/171,046 priority patent/US20190092769A1/en

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    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/28—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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • 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
    • C07D471/22—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 systems contains four or more hetero rings
    • 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
    • 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
    • C07D491/22—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 four or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente invención se relaciona con la Química, la Farmacéutica y en particular con la obtención de nuevas entidades moleculares, derivados tricíclicos y tetracíclicos del tipo benzodiazepinas, piridodiazepinas y pirimidodiazepinas fusionadas a derivados de 1,4-dihidropiridinas. con acción sobre el Sistema Nervioso Central y Vascular. A partir de derivados que contienen un anillo de dihidropiridina, mediante reacciones con compuestos del tipo orto- fenilendiaminas, orto-diaminopiridinas y orto-diaminopirimidinas, así como posteriores transformaciones a algunos de ellos, se obtienen derivados tricíclicos y tetracíclicos de fórmula general I-XI I que contienen un núcleo de diazepina o diazepinona fusionadas a un núcleo de 1,4-dihidropiridina, donde el ciclo A, es un anillo de benceno, piridina o pirimidina sustituido o no. Estas entidades moleculares presentan acción GABAérgica y moduladora de los canales de calcio, utilizables en el tratamiento de las enfermedades cardiovasculares, cerebrovasculares, neurodegenerativas, neuropsiquiátricas y neurológicas.
PCT/CU2010/000004 2009-10-09 2010-10-08 Sistemas tricíclicos y tetracíclicos con actividad sobre el sistema nervioso central y vascular WO2011041989A2 (es)

Priority Applications (8)

Application Number Priority Date Filing Date Title
CA2777209A CA2777209C (en) 2009-10-09 2010-10-08 Tricyclic and tetracyclic systems with activity on the central-nervous and vascular systems
EP10821598.9A EP2487174A4 (en) 2009-10-09 2010-10-08 TRICYCLIC AND TETRACYCLIC SYSTEMS WITH EFFECT ON THE CENTRAL NERVOUS AND VACUUM SYSTEM
US13/500,983 US9315497B2 (en) 2009-10-09 2010-10-08 Tricyclic and tetracyclic systems with activity on the central nervous and vascular systems
CN2010800556597A CN102656171A (zh) 2009-10-09 2010-10-08 对血管系统和中枢神经系统起作用的三环和四环系统
JP2012532450A JP2013507329A (ja) 2009-10-09 2010-10-08 脈管系および中枢神経系に作用する三環系化合物および四環系化合物
ZA2012/03295A ZA201203295B (en) 2009-10-09 2012-05-07 Tricyclic and tetracyclic systems with activity on the central-nervous and vascular systems
US14/282,111 US10138231B2 (en) 2009-10-09 2014-05-20 Tricyclic and tetracyclic systems acting upon the vascular and central nervous systems
US16/171,046 US20190092769A1 (en) 2009-10-09 2018-10-25 Tricyclic and tetracyclic systems acting upon the vascular and central nervous systems

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CUP2009000172A CU20090172A7 (es) 2009-10-09 2009-10-09 Sistemas tricíclicos y tetracíclicos con actividad sobre el sistema nervioso central y vascular
CUPCT/CU2009/000172 2009-10-09

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US13/500,983 A-371-Of-International US9315497B2 (en) 2009-10-09 2010-10-08 Tricyclic and tetracyclic systems with activity on the central nervous and vascular systems
US14/282,111 Continuation-In-Part US10138231B2 (en) 2009-10-09 2014-05-20 Tricyclic and tetracyclic systems acting upon the vascular and central nervous systems

Publications (2)

Publication Number Publication Date
WO2011041989A2 WO2011041989A2 (es) 2011-04-14
WO2011041989A3 true WO2011041989A3 (es) 2011-09-15

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PCT/CU2010/000004 WO2011041989A2 (es) 2009-10-09 2010-10-08 Sistemas tricíclicos y tetracíclicos con actividad sobre el sistema nervioso central y vascular

Country Status (9)

Country Link
US (3) US9315497B2 (es)
EP (1) EP2487174A4 (es)
JP (1) JP2013507329A (es)
KR (1) KR20120093940A (es)
CN (1) CN102656171A (es)
CA (1) CA2777209C (es)
CU (1) CU20090172A7 (es)
WO (1) WO2011041989A2 (es)
ZA (1) ZA201203295B (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201215033D0 (en) 2012-08-23 2012-10-10 Novartis Ag Diazepinone derivatives
GB201510010D0 (en) 2015-06-09 2015-07-22 King S College London PDD and BPD compounds
US20180339985A1 (en) 2015-08-21 2018-11-29 Femtogenix Limited Pdd compounds
GB201514928D0 (en) 2015-08-21 2015-10-07 King S College London PDD compounds
CU20160058A7 (es) 2016-05-04 2017-12-08 Centro De Investigación Y Desarrollo De Medicamentos (Cidem) Organizacion Superior De Desarrollo Emp Derivado de benzodiazepina con actividad sobre el sistema nervioso central y vascular
CU20190114A7 (es) 2019-12-26 2021-08-06 Centro De Investig Y Desarrollo De Medicamentos Cidem Combinación para simultáneamente incrementar la eficacia analgésica de la morfina y reducir su dependencia física
WO2022055168A1 (ko) * 2020-09-09 2022-03-17 서울대학교산학협력단 신규 피리미도디아제핀 유도체 및 이의 용도

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US3780047A (en) * 1972-07-05 1973-12-18 Squibb & Sons Inc Derivatives of pyrazolo(3',4'-2,3)pyrido(4,5-e)b-benzo-1,5-diazepines
US4012373A (en) * 1972-09-22 1977-03-15 E. R. Squibb & Sons, Inc. Pyrazolo[3',4'-2,3]pyrido[4,5-e]b-benzo-1,5-diazepinones
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EP0498290A1 (en) * 1991-02-07 1992-08-12 Boehringer Ingelheim Pharmaceuticals Inc. Pyridobenzodiazepines, dipyrido [3,2-b:2',3'-e] [1,4]diazepines and their use in the prevention or treatment of HIV infection

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Also Published As

Publication number Publication date
JP2013507329A (ja) 2013-03-04
CU20090172A6 (es) 2011-10-05
CA2777209A1 (en) 2011-04-14
CU20090172A7 (es) 2011-10-05
US9315497B2 (en) 2016-04-19
US20190092769A1 (en) 2019-03-28
CU23879B1 (es) 2013-04-19
KR20120093940A (ko) 2012-08-23
ZA201203295B (en) 2014-10-29
WO2011041989A2 (es) 2011-04-14
CN102656171A (zh) 2012-09-05
CA2777209C (en) 2016-11-22
EP2487174A2 (en) 2012-08-15
EP2487174A4 (en) 2013-05-08
US20140275042A1 (en) 2014-09-18
US20120202791A1 (en) 2012-08-09
US10138231B2 (en) 2018-11-27

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