BRPI0515800A - imidazo-benzodiazepinas tetracìclicas como moduladores de receptores de gaba - Google Patents
imidazo-benzodiazepinas tetracìclicas como moduladores de receptores de gabaInfo
- Publication number
- BRPI0515800A BRPI0515800A BRPI0515800-1A BRPI0515800A BRPI0515800A BR PI0515800 A BRPI0515800 A BR PI0515800A BR PI0515800 A BRPI0515800 A BR PI0515800A BR PI0515800 A BRPI0515800 A BR PI0515800A
- Authority
- BR
- Brazil
- Prior art keywords
- lower alkyl
- substituted
- halogen
- cycloalkyl
- hydrogen
- Prior art date
Links
- 102000005915 GABA Receptors Human genes 0.000 title abstract 2
- 108010005551 GABA Receptors Proteins 0.000 title abstract 2
- 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
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 150000002431 hydrogen Chemical group 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
- 208000028698 Cognitive impairment Diseases 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 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
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 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
"IMIDAZO-BENZODIAZEPINAS TETRACìCLICAS COMO MODULADORES DE RECEPTORES DE GABA". A presente invenção refere-se a derivados de imidazo¢1,5-a!¢1,2,4!triazol¢1,5-d!¢1,4!benzodiazepina substituìdos da seguinte fórmula (I) em que R é hidrogênio, halogênio, alquila inferior, alquila inferior substituída por halogênio, alcóxi inferior, alcóxi inferior substituído por halogênio, nitro, cicloalquila, -O(CH~ 2~)~ m~O(CH~ 2~)~ m~OH ou -C<154>C-R'; R é hidrogênio ou metila; R é alquila inferior, alquila inferior substituída por halogênio, alquenila inferior, alquenila inferior substituída por halogênio, alquinila inferior, -(CH~ 2~)~ n~-cicloalquila, -(CR'R")~ m~- CH~ 3~, ou é fenila, não-substituída ou substituída por halogênio, ou é piridinila ou tienila, não-substituída ou substituída por alquila inferior, ou é -(CH~ 2~)~ n~-NH-cicloalquila, alquenil-cicloalquila inferior, alquinil-(CR'R")~ m~OH inferior, ou é alquenil-fenila inferior, em que o anel de fenila é substituída ou não-substituída por halogênio, CF~ 3~, alquila inferior ou alcóxi inferior; R' é hidrogênio ou alquila inferior; R" é hidrogênio, hidróxi ou alquila inferior; n é 0, 1 ou 2; m é 1, 2 ou 3; o é 1 ou 2; e com o seus sais de adição de ácido farmaceuticamente aceitáveis. Foi descoberto que esta classe de compostos apresenta alta afinidade e seletividade com relação aos sítios de ligação de receptor GABA A <244>5 e pode ser útil como realçador cognitivo ou para o tratamento de distúrbio cognitivo como doença 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 |
|---|---|
| BRPI0515800A true BRPI0515800A (pt) | 2008-08-05 |
Family
ID=36129290
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0515800-1A BRPI0515800A (pt) | 2004-12-14 | 2005-12-05 | imidazo-benzodiazepinas tetracìclicas como moduladores de receptores de gaba |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US7432256B2 (pt) |
| EP (1) | EP1828194B1 (pt) |
| JP (1) | JP4783380B2 (pt) |
| KR (1) | KR100923393B1 (pt) |
| CN (1) | CN101115756B (pt) |
| AR (1) | AR055005A1 (pt) |
| AT (1) | ATE396998T1 (pt) |
| AU (1) | AU2005315913B2 (pt) |
| BR (1) | BRPI0515800A (pt) |
| CA (1) | CA2590333C (pt) |
| DE (1) | DE602005007265D1 (pt) |
| ES (1) | ES2307230T3 (pt) |
| MX (1) | MX2007007115A (pt) |
| PL (1) | PL1828194T3 (pt) |
| RU (1) | RU2393161C2 (pt) |
| TW (1) | TW200631953A (pt) |
| WO (1) | WO2006063708A1 (pt) |
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 |
| US20130150351A1 (en) * | 2010-06-03 | 2013-06-13 | Stanley T. Carmichael | Methods and compositions for treating a subject for central nervous system (cns) injury |
| US20150374705A1 (en) | 2012-02-14 | 2015-12-31 | Shanghai Institues for Biological Sciences | Substances for treatment or relief of pain |
| CN112409363B (zh) * | 2013-12-20 | 2023-11-14 | 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䓬衍生物、组合物和方法 |
| WO2016205739A1 (en) | 2015-06-19 | 2016-12-22 | Belew Mekonnen | 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 |
| US20180170941A1 (en) * | 2016-12-19 | 2018-06-21 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| BR112020026062B1 (pt) | 2018-06-19 | 2023-04-04 | Agenebio, Inc | Compostos derivados de benzodiazepina ou um sal farmaceuticamente aceitavel, isômero ou combinação dos mesmos, composição farmacêutica compreendendo os mesmos e usos dos mesmos para o tratamento de comprometimento cognitivo, câncer cerebral e psicose da doença de parkinson |
| 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 |
| EP0150040B1 (de) | 1984-01-19 | 1994-08-31 | F. Hoffmann-La Roche Ag | Imidazodiazepin-Derivate |
| 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 (pt) * | 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 |
| JP4783375B2 (ja) * | 2004-10-20 | 2011-09-28 | エフ．ホフマン−ラ ロシュ アーゲー | イミダゾベンゾジゼピン誘導体 |
-
2005
- 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 BR BRPI0515800-1A patent/BRPI0515800A/pt not_active IP Right Cessation
- 2005-12-05 PL PL05825935T patent/PL1828194T3/pl unknown
- 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 EP EP05825935A patent/EP1828194B1/en not_active Expired - Lifetime
- 2005-12-05 JP JP2007545890A patent/JP4783380B2/ja not_active Expired - Fee Related
- 2005-12-05 RU RU2007121767/04A patent/RU2393161C2/ru not_active IP Right Cessation
- 2005-12-05 MX MX2007007115A patent/MX2007007115A/es active IP Right Grant
- 2005-12-05 WO PCT/EP2005/012993 patent/WO2006063708A1/en not_active Ceased
- 2005-12-05 AT AT05825935T patent/ATE396998T1/de active
- 2005-12-05 AU AU2005315913A patent/AU2005315913B2/en not_active Ceased
- 2005-12-05 CN CN2005800479250A patent/CN101115756B/zh not_active Expired - Fee Related
- 2005-12-08 US US11/297,691 patent/US7432256B2/en not_active Expired - Fee Related
- 2005-12-12 TW TW094143881A patent/TW200631953A/zh unknown
- 2005-12-12 AR ARP050105181A patent/AR055005A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| JP2008523125A (ja) | 2008-07-03 |
| US7432256B2 (en) | 2008-10-07 |
| RU2007121767A (ru) | 2009-01-27 |
| DE602005007265D1 (de) | 2008-07-10 |
| KR20070089227A (ko) | 2007-08-30 |
| RU2393161C2 (ru) | 2010-06-27 |
| CA2590333C (en) | 2013-01-08 |
| EP1828194B1 (en) | 2008-05-28 |
| WO2006063708A1 (en) | 2006-06-22 |
| CN101115756B (zh) | 2010-06-16 |
| AU2005315913A1 (en) | 2006-06-22 |
| CN101115756A (zh) | 2008-01-30 |
| ES2307230T3 (es) | 2008-11-16 |
| JP4783380B2 (ja) | 2011-09-28 |
| AR055005A1 (es) | 2007-08-01 |
| CA2590333A1 (en) | 2006-06-22 |
| EP1828194A1 (en) | 2007-09-05 |
| US20060128691A1 (en) | 2006-06-15 |
| KR100923393B1 (ko) | 2009-10-23 |
| PL1828194T3 (pl) | 2008-11-28 |
| TW200631953A (en) | 2006-09-16 |
| MX2007007115A (es) | 2007-07-11 |
| AU2005315913B2 (en) | 2011-11-24 |
| ATE396998T1 (de) | 2008-06-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 9A ANUIDADE. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2283 DE 07/10/2014. |