ECSP034607A - Derivados de benzodiazepina como modulares del receptor gaba a - Google Patents
Derivados de benzodiazepina como modulares del receptor gaba aInfo
- Publication number
- ECSP034607A ECSP034607A EC2003004607A ECSP034607A ECSP034607A EC SP034607 A ECSP034607 A EC SP034607A EC 2003004607 A EC2003004607 A EC 2003004607A EC SP034607 A ECSP034607 A EC SP034607A EC SP034607 A ECSP034607 A EC SP034607A
- Authority
- EC
- Ecuador
- Prior art keywords
- lower alkyl
- triazolo
- halogen
- hydrogen
- phenyl
- Prior art date
Links
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
- 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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención describe los compuestos de la fórmula en donde (Gráfico) R1 es hidrógeno, halógeno, alquilo inferior, alcoxilo inferior, hidroxilo, ciano, trifluorometilo, triufluorometoxilo o alquilo inferior; R2 es-C(0) 0- alquilo inferior, isoxasol, 1, 2, 4-oxidiazol-3-ilo o 1, 2, 4-oxadiazol-5-ilo, cuyos anillos pueden ser sustituidos por alquilo inferior, trifluorometilo o cicloalquilo; R3 es hidrógeno, alquilo inferior, -(CH2)n-cicloalquilo, -(CH2)n-halógeno, -(CH2)n-piridin-4-ilo, o-(CH2)n-fenilo, en donde el anillo fenilo puede estar sustituido por uno o más sustituyentes seleccionados del grupo consistente en alcoxilo inferior, halógeno, -SO2CH3,fenilo OCF3, nitro, CF3-NR2, o es-(CH2)n-indolilo, opcionalmente sustituido por alquilo inferior o alcoxio inferior, o es pirrolidinil-5-oxo, -C (0) -NR2, -(CH2)n-OH, -(CH2)n-NR2 o (CH2)n-benzo[1, 3]dioxol; R es hidrógeno o alquilo inferior; y n es o, 1, 2 o 3; y sus sales de adición ácida farmacéutica mente aceptables, con la excepción de los siguientes compuestos: Etil-9H - imidazo [1, S-a] [1, 2, 4]triazolo [3, 4-d] [1, 4] benzo-diazepina-10-carboxilato, 10-(3-ciclopropil-1, 2, 4-oxadizol1-S-i1)-9H-imidazol [1, S-a][1, 2, 4]triazolo [4, 3-d][1, 4]-benzodiazepina, etil 3-fluoro-9H-imidazol[1, S-a][1, 2, 4]triazolo[4, 3-d][1, 4]-benzodiazepina-10-carboxilato, 10-(3-ciclopropil-1, 2, 4-oxidiazol1-S-i1)-3 fluoro-9H.Estos compuestos, presentan una buena afinidad para el receptor GABA A as y por consiguiente son útiles durante el tratamiento de enfermedades relacionadas con este receptor.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP00124332 | 2000-11-16 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP034607A true ECSP034607A (es) | 2003-06-25 |
Family
ID=8170315
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2003004607A ECSP034607A (es) | 2000-11-16 | 2003-05-15 | Derivados de benzodiazepina como modulares del receptor gaba a |
Country Status (41)
| Country | Link |
|---|---|
| US (1) | US6743789B2 (es) |
| EP (1) | EP1337535B1 (es) |
| JP (1) | JP4088151B2 (es) |
| KR (1) | KR100504300B1 (es) |
| CN (1) | CN1191255C (es) |
| AR (1) | AR031345A1 (es) |
| AT (1) | ATE268776T1 (es) |
| AU (2) | AU1700702A (es) |
| BG (1) | BG107817A (es) |
| BR (1) | BR0115393A (es) |
| CA (1) | CA2427576C (es) |
| CZ (1) | CZ295256B6 (es) |
| DE (1) | DE60103776T2 (es) |
| DK (1) | DK1337535T3 (es) |
| EC (1) | ECSP034607A (es) |
| ES (1) | ES2220831T3 (es) |
| GC (1) | GC0000375A (es) |
| GT (1) | GT200100230A (es) |
| HK (1) | HK1062442A1 (es) |
| HR (1) | HRP20030360A2 (es) |
| HU (1) | HUP0303281A3 (es) |
| IL (1) | IL155813A0 (es) |
| JO (1) | JO2359B1 (es) |
| MA (1) | MA26962A1 (es) |
| MX (1) | MXPA03004251A (es) |
| MY (1) | MY141675A (es) |
| NO (1) | NO324706B1 (es) |
| NZ (1) | NZ525413A (es) |
| PA (1) | PA8532401A1 (es) |
| PE (1) | PE20020583A1 (es) |
| PL (1) | PL362925A1 (es) |
| PT (1) | PT1337535E (es) |
| RU (1) | RU2278865C2 (es) |
| SI (1) | SI1337535T1 (es) |
| SK (1) | SK7232003A3 (es) |
| TR (1) | TR200402073T4 (es) |
| TW (1) | TWI239333B (es) |
| UY (1) | UY27026A1 (es) |
| WO (1) | WO2002040487A2 (es) |
| YU (1) | YU35603A (es) |
| ZA (1) | ZA200303435B (es) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6686352B2 (en) | 2001-05-18 | 2004-02-03 | Hoffmann-La Roche Inc. | Substituted imidazo [1,5-a] pyrimido [5,4-d] [1] benzazepine derivatives |
| JP4616770B2 (ja) * | 2003-06-19 | 2011-01-19 | 第一三共株式会社 | 選択的なアミノ置換基導入法 |
| EP2343073A3 (en) | 2003-12-11 | 2011-10-12 | Sepracor Inc. | Combination of a sedative and a neurotransmitter modulator, and methods for improving sleep quality and treating depression |
| AU2005272627A1 (en) | 2004-08-13 | 2006-02-23 | Amgen Inc. | Substituted benzofused heterocycles |
| EP1809297B1 (en) * | 2004-10-12 | 2008-07-30 | F. Hoffmann-Roche AG | Imidazo[1,5a]triazolo[1,5d]benzodiazepine derivatives for the treatment of cognitive disorders |
| RU2007112940A (ru) * | 2004-10-20 | 2008-11-27 | Ф.Хоффманн-Ля Рош Аг (Ch) | Производные имидазобензодиазепина |
| JP4751398B2 (ja) * | 2004-10-20 | 2011-08-17 | エフ．ホフマン−ラ ロシュ アーゲー | ハロゲン置換ベンゾジアゼピン誘導体 |
| RU2393161C2 (ru) | 2004-12-14 | 2010-06-27 | Ф. Хоффманн-Ля Рош Аг | Тетрациклические имидазо-бензодиазепины в качестве модуляторов гамк-рецепторов |
| US8510055B2 (en) | 2005-08-03 | 2013-08-13 | The Johns Hopkins University | Methods for characterizing and treating cognitive impairment in aging and disease |
| EP2682481A3 (en) * | 2005-08-03 | 2014-09-17 | The Johns-Hopkins University | Methods for characterizing and treating cognitive impairment in aging and disease |
| EP1937688B1 (en) | 2005-10-11 | 2010-08-11 | F. Hoffmann-La Roche AG | Imidazo benzodiazepine derivatives |
| CA2625210A1 (en) * | 2005-10-31 | 2007-05-10 | Braincells, Inc. | Gaba receptor mediated modulation of neurogenesis |
| WO2009139916A1 (en) * | 2008-05-16 | 2009-11-19 | Synta Pharmaceuticals Corp. | Tricyclic triazole compounds that modulate hsp90 activity |
| EP2358714B1 (en) | 2008-11-18 | 2012-08-01 | F. Hoffmann-La Roche AG | Alkylcyclohexylethers of dihydrotetraazabenzoazulenes |
| BRPI0922303B1 (pt) * | 2008-11-28 | 2019-11-12 | Hoffmann La Roche | arilciclo-hexiléteres de di-hidrotetra-azabenzoazulenos, seu processo de preparação, composição farmacêutica que os compreende e uso |
| CU20090172A7 (es) | 2009-10-09 | 2011-10-05 | Ct De Investigación Y Desarrollo De Medicamentos | Sistemas tricíclicos y tetracíclicos con actividad sobre el sistema nervioso central y vascular |
| CN103313712B (zh) | 2010-11-15 | 2016-10-26 | 艾吉因生物股份有限公司 | 用于治疗认知障碍的哒嗪衍生物、组合物和方法 |
| US20150374705A1 (en) | 2012-02-14 | 2015-12-31 | Shanghai Institues for Biological Sciences | Substances for treatment or relief of pain |
| WO2014047413A1 (en) * | 2012-09-21 | 2014-03-27 | Uwm Research Foundation, Inc. | Novel gabaa agonists and methods of using to control airway hyperresponsiveness and inflammation in asthma |
| JP6883988B2 (ja) * | 2013-12-20 | 2021-06-09 | エージンバイオ， インコーポレイテッド | ベンゾジアゼピン誘導体、組成物、および認知障害を処置するための方法 |
| IL256354B (en) * | 2015-06-19 | 2022-09-01 | Agenebio Inc | History of benzodiazepines, preparations and their use for the treatment of cognitive impairment |
| US10059718B2 (en) | 2016-01-04 | 2018-08-28 | Tabomedex Biosciences, LLC | Fused quadracyclic compounds, compositions and uses thereof |
| US10973479B2 (en) | 2016-05-16 | 2021-04-13 | Canon Medical Systems Corporation | X-ray diagnosis apparatus, X-ray diagnosis apparatus controlling method, and X-ray diagnosis system |
| 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 |
| KR102512548B1 (ko) | 2017-12-22 | 2023-03-22 | 삼성디스플레이 주식회사 | 유기 전계 발광 소자 및 유기 전계 발광 소자용 함질소 화합물 |
| EA202190076A1 (ru) * | 2018-06-19 | 2021-09-22 | Эйджинбайо, Инк. | Производные бензодиазепина, композиции и способы лечения когнитивных нарушений |
| KR102151969B1 (ko) * | 2019-12-11 | 2020-09-04 | 주식회사 지투비 | 투과도 가변창의 제조방법 및 그에 의해 제조된 투과도 가변창 |
| CN112979658B (zh) * | 2021-02-22 | 2022-05-31 | 南湖实验室 | 一种氟马西尼的制备方法 |
| WO2024039886A1 (en) | 2022-08-19 | 2024-02-22 | Agenebio, Inc. | Benzazepine derivatives, compositions, and methods for treating cognitive impairment |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK174086D0 (da) | 1986-04-16 | 1986-04-16 | Ferrosan As | Nye benzodiazepinderivater samt fremgangsmaade til fremstilling af samme |
| TW201311B (es) | 1991-06-17 | 1993-03-01 | Hoffmann La Roche |
-
2001
- 2001-11-07 TW TW090127658A patent/TWI239333B/zh not_active IP Right Cessation
- 2001-11-08 NZ NZ525413A patent/NZ525413A/en unknown
- 2001-11-08 ES ES01996541T patent/ES2220831T3/es not_active Expired - Lifetime
- 2001-11-08 PL PL01362925A patent/PL362925A1/xx not_active Application Discontinuation
- 2001-11-08 BR BR0115393-5A patent/BR0115393A/pt not_active IP Right Cessation
- 2001-11-08 YU YU35603A patent/YU35603A/sh unknown
- 2001-11-08 JP JP2002543495A patent/JP4088151B2/ja not_active Expired - Fee Related
- 2001-11-08 TR TR2004/02073T patent/TR200402073T4/xx unknown
- 2001-11-08 US US10/007,883 patent/US6743789B2/en not_active Expired - Fee Related
- 2001-11-08 MX MXPA03004251A patent/MXPA03004251A/es active IP Right Grant
- 2001-11-08 EP EP01996541A patent/EP1337535B1/en not_active Expired - Lifetime
- 2001-11-08 PT PT01996541T patent/PT1337535E/pt unknown
- 2001-11-08 KR KR10-2003-7006609A patent/KR100504300B1/ko not_active IP Right Cessation
- 2001-11-08 SI SI200130125T patent/SI1337535T1/xx unknown
- 2001-11-08 DE DE60103776T patent/DE60103776T2/de not_active Expired - Lifetime
- 2001-11-08 CN CNB018189415A patent/CN1191255C/zh not_active Expired - Fee Related
- 2001-11-08 IL IL15581301A patent/IL155813A0/xx unknown
- 2001-11-08 CZ CZ20031597A patent/CZ295256B6/cs not_active IP Right Cessation
- 2001-11-08 SK SK723-2003A patent/SK7232003A3/sk unknown
- 2001-11-08 DK DK01996541T patent/DK1337535T3/da active
- 2001-11-08 AU AU1700702A patent/AU1700702A/xx active Pending
- 2001-11-08 AU AU2002217007A patent/AU2002217007B2/en not_active Ceased
- 2001-11-08 WO PCT/EP2001/012887 patent/WO2002040487A2/en active IP Right Grant
- 2001-11-08 RU RU2003116895/04A patent/RU2278865C2/ru not_active IP Right Cessation
- 2001-11-08 AT AT01996541T patent/ATE268776T1/de not_active IP Right Cessation
- 2001-11-08 CA CA002427576A patent/CA2427576C/en not_active Expired - Fee Related
- 2001-11-08 HU HU0303281A patent/HUP0303281A3/hu unknown
- 2001-11-12 JO JO2001183A patent/JO2359B1/en active
- 2001-11-13 GC GCP20011724 patent/GC0000375A/en active
- 2001-11-14 PE PE2001001135A patent/PE20020583A1/es not_active Application Discontinuation
- 2001-11-15 AR ARP010105323A patent/AR031345A1/es not_active Application Discontinuation
- 2001-11-15 MY MYPI20015253A patent/MY141675A/en unknown
- 2001-11-15 UY UY27026A patent/UY27026A1/es not_active Application Discontinuation
- 2001-11-15 PA PA20018532401A patent/PA8532401A1/es unknown
- 2001-11-15 GT GT200100230A patent/GT200100230A/es unknown
-
2003
- 2003-05-05 ZA ZA200303435A patent/ZA200303435B/en unknown
- 2003-05-07 HR HR20030360A patent/HRP20030360A2/hr not_active Application Discontinuation
- 2003-05-15 EC EC2003004607A patent/ECSP034607A/es unknown
- 2003-05-15 NO NO20032208A patent/NO324706B1/no unknown
- 2003-05-16 MA MA27163A patent/MA26962A1/fr unknown
- 2003-05-16 BG BG107817A patent/BG107817A/bg unknown
-
2004
- 2004-07-21 HK HK04105348A patent/HK1062442A1/xx not_active IP Right Cessation
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