MX2007007115A - Imidazo-benzodiazepinas tetraciclicas como moduladoras del receptor del acido gamma-aminobutirico (gaba). - Google Patents
Imidazo-benzodiazepinas tetraciclicas como moduladoras del receptor del acido gamma-aminobutirico (gaba).Info
- Publication number
- MX2007007115A MX2007007115A MX2007007115A MX2007007115A MX2007007115A MX 2007007115 A MX2007007115 A MX 2007007115A MX 2007007115 A MX2007007115 A MX 2007007115A MX 2007007115 A MX2007007115 A MX 2007007115A MX 2007007115 A MX2007007115 A MX 2007007115A
- Authority
- MX
- Mexico
- Prior art keywords
- substituted
- halogen
- lower alkyl
- cycloalkyl
- hydrogen
- Prior art date
Links
- 102000005915 GABA Receptors Human genes 0.000 title 1
- 108010005551 GABA Receptors Proteins 0.000 title 1
- KLNFAMGHSZQYHR-UHFFFAOYSA-N imidazo[4,5-i][1,2]benzodiazepine Chemical class C1=CC=NN=C2C3=NC=NC3=CC=C21 KLNFAMGHSZQYHR-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 8
- 229910052736 halogen Inorganic materials 0.000 abstract 7
- 150000002367 halogens Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 239000002475 cognitive enhancer Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 229960003692 gamma aminobutyric acid Drugs 0.000 abstract 1
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- MEYXEJCDZRDIFZ-UHFFFAOYSA-N imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine Chemical class C=1N2N=CN=C2C2=CC=CC=C2N2CN=CC2=1 MEYXEJCDZRDIFZ-UHFFFAOYSA-N 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/14—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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
-
- 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
-
- 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
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente invencion se refiere a derivados de imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepina sustituida de la formula siguiente (ver formula I) en la que R1 es hidrogeno, halogeno, alquilo inferior, alquilo inferior sustituido por halogeno, alcoxi inferior, alcoxi inferior sustituido por halogeno, nitro, cicloalquilo, - O(CH2)mO(CH2)mOH o -C=C-R'; R2 es hidrogeno o metilo; R3 es alquilo inferior, alquilo inferior sustituido por halogeno, alquenilo inferior, alquenilo inferior sustituido por halogeno, alquinilo inferior, -(CH2)n-cicloalquilo, -(CR'R'')m-CH3, o es fenilo, sin sustituir o sustituido por halogeno, o es piridinilo o tienilo, sin sustituir o sustituidos por alquilo inferior, o es -(CH2)n-NH-cicloalquilo, (alquenilo inferior)-cicloalquilo, (alquinilo inferior)-(R'R'')mOH, o es (alquinilo inferior)-fenilo, en el que el anillo fenilo esta sin sustituir o sustituido por halogeno, CF3, alquilo inferior o alcoxi inferior; R' es hidrogeno o alquilo inferior, R'' es hidrogeno, hidroxi o alquilo inferior; n es 0, 1 o 2; m es 1, 2 o 3; o es 1 o 2; y a sus sales de adicion de acido farmaceuticamente aceptables. Se ha encontrado que los compuestos de este grupo presentan una gran afinidad y selectividad para los sitio de fijacion del receptor GABA A a5 y que pueden ser utiles como mejoradores cognitivos o para el tratamiento de trastornos cognitivos, tales como la enfermedad de Alzheimer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04106556 | 2004-12-14 | ||
| PCT/EP2005/012993 WO2006063708A1 (en) | 2004-12-14 | 2005-12-05 | Tetracyclic imidazo-benzodiazepines as gaba receptors modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2007007115A true MX2007007115A (es) | 2007-07-11 |
Family
ID=36129290
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2007007115A MX2007007115A (es) | 2004-12-14 | 2005-12-05 | Imidazo-benzodiazepinas tetraciclicas como moduladoras del receptor del acido gamma-aminobutirico (gaba). |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US7432256B2 (es) |
| EP (1) | EP1828194B1 (es) |
| JP (1) | JP4783380B2 (es) |
| KR (1) | KR100923393B1 (es) |
| CN (1) | CN101115756B (es) |
| AR (1) | AR055005A1 (es) |
| AT (1) | ATE396998T1 (es) |
| AU (1) | AU2005315913B2 (es) |
| BR (1) | BRPI0515800A (es) |
| CA (1) | CA2590333C (es) |
| DE (1) | DE602005007265D1 (es) |
| ES (1) | ES2307230T3 (es) |
| MX (1) | MX2007007115A (es) |
| PL (1) | PL1828194T3 (es) |
| RU (1) | RU2393161C2 (es) |
| TW (1) | TW200631953A (es) |
| WO (1) | WO2006063708A1 (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008064318A2 (en) * | 2006-11-22 | 2008-05-29 | University Of Medicine And Dentistry Of New Jersey | Peripheral opioid receptor active compounds |
| US10206921B2 (en) | 2009-06-03 | 2019-02-19 | The Regents Of The University Of California | Methods and compositions for treating a subject for central nervous system (CNS) injury |
| CN101891706B (zh) * | 2010-04-09 | 2013-05-29 | 复旦大学 | 3,4-二氢苯并[f][1,4]噻氮杂*类化合物或其盐及其药物用途 |
| EP2575455A4 (en) * | 2010-06-03 | 2014-01-15 | Univ California | METHOD AND COMPOSITIONS FOR TREATING PATIENTS WITH INJURIES OF THE CENTRAL NERVOUS SYSTEM |
| US20150374705A1 (en) | 2012-02-14 | 2015-12-31 | Shanghai Institues for Biological Sciences | Substances for treatment or relief of pain |
| NZ722077A (en) | 2013-12-20 | 2021-12-24 | Agenebio Inc | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| CN108026107B (zh) | 2015-06-19 | 2021-07-30 | 艾吉因生物股份有限公司 | 用于治疗认知损害的苯并二氮杂环庚三烯衍生物、组合物和方法 |
| US20180170941A1 (en) * | 2016-12-19 | 2018-06-21 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| US11505555B2 (en) | 2016-12-19 | 2022-11-22 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| IL279530B1 (en) | 2018-06-19 | 2025-09-01 | Agenebio Inc | Benzodiazepine history, preparations, and methods for treating cognitive disorder |
| WO2023174374A1 (zh) | 2022-03-16 | 2023-09-21 | 江苏恒瑞医药股份有限公司 | 稠杂环类化合物、其制备方法及其在医药上的应用 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA1143728A (en) | 1979-10-04 | 1983-03-29 | Max Gerecke | Imidazodiazepine derivatives |
| NZ210850A (en) | 1984-01-19 | 1988-10-28 | Hoffmann La Roche | Imidazodiazepine derivatives and pharmaceutical compositions |
| DK174086D0 (da) | 1986-04-16 | 1986-04-16 | Ferrosan As | Nye benzodiazepinderivater samt fremgangsmaade til fremstilling af samme |
| US4897392A (en) | 1989-07-03 | 1990-01-30 | Hoechst-Roussel Pharmaceuticals, Inc. | 4H-indolo(1,2-d)(1,2,4)triazolo(4,3-A)(1,4)benzodiazepines |
| TW201311B (es) | 1991-06-17 | 1993-03-01 | Hoffmann La Roche | |
| TWI239333B (en) * | 2000-11-16 | 2005-09-11 | Hoffmann La Roche | Benzodiazepine derivatives as GABA A receptor modulators |
| EP1805184B1 (en) * | 2004-10-20 | 2013-01-09 | F. Hoffmann-La Roche AG | Imidazo-benzodiazepine derivatives |
-
2005
- 2005-12-05 AT AT05825935T patent/ATE396998T1/de active
- 2005-12-05 JP JP2007545890A patent/JP4783380B2/ja not_active Expired - Fee Related
- 2005-12-05 CN CN2005800479250A patent/CN101115756B/zh not_active Expired - Fee Related
- 2005-12-05 MX MX2007007115A patent/MX2007007115A/es active IP Right Grant
- 2005-12-05 EP EP05825935A patent/EP1828194B1/en not_active Expired - Lifetime
- 2005-12-05 BR BRPI0515800-1A patent/BRPI0515800A/pt not_active IP Right Cessation
- 2005-12-05 AU AU2005315913A patent/AU2005315913B2/en not_active Ceased
- 2005-12-05 CA CA2590333A patent/CA2590333C/en not_active Expired - Fee Related
- 2005-12-05 KR KR1020077015973A patent/KR100923393B1/ko not_active Expired - Fee Related
- 2005-12-05 RU RU2007121767/04A patent/RU2393161C2/ru not_active IP Right Cessation
- 2005-12-05 ES ES05825935T patent/ES2307230T3/es not_active Expired - Lifetime
- 2005-12-05 DE DE602005007265T patent/DE602005007265D1/de not_active Expired - Lifetime
- 2005-12-05 PL PL05825935T patent/PL1828194T3/pl unknown
- 2005-12-05 WO PCT/EP2005/012993 patent/WO2006063708A1/en not_active Ceased
- 2005-12-08 US US11/297,691 patent/US7432256B2/en not_active Expired - Fee Related
- 2005-12-12 AR ARP050105181A patent/AR055005A1/es not_active Application Discontinuation
- 2005-12-12 TW TW094143881A patent/TW200631953A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN101115756A (zh) | 2008-01-30 |
| BRPI0515800A (pt) | 2008-08-05 |
| WO2006063708A1 (en) | 2006-06-22 |
| JP2008523125A (ja) | 2008-07-03 |
| AR055005A1 (es) | 2007-08-01 |
| AU2005315913B2 (en) | 2011-11-24 |
| EP1828194A1 (en) | 2007-09-05 |
| KR100923393B1 (ko) | 2009-10-23 |
| ES2307230T3 (es) | 2008-11-16 |
| CN101115756B (zh) | 2010-06-16 |
| PL1828194T3 (pl) | 2008-11-28 |
| EP1828194B1 (en) | 2008-05-28 |
| JP4783380B2 (ja) | 2011-09-28 |
| RU2007121767A (ru) | 2009-01-27 |
| RU2393161C2 (ru) | 2010-06-27 |
| DE602005007265D1 (de) | 2008-07-10 |
| CA2590333C (en) | 2013-01-08 |
| US20060128691A1 (en) | 2006-06-15 |
| AU2005315913A1 (en) | 2006-06-22 |
| US7432256B2 (en) | 2008-10-07 |
| TW200631953A (en) | 2006-09-16 |
| ATE396998T1 (de) | 2008-06-15 |
| KR20070089227A (ko) | 2007-08-30 |
| CA2590333A1 (en) | 2006-06-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |