AR031345A1 - Derivados de benzodiazepina como moduladores receptores gaba a - Google Patents
Derivados de benzodiazepina como moduladores receptores gaba aInfo
- Publication number
- AR031345A1 AR031345A1 ARP010105323A ARP010105323A AR031345A1 AR 031345 A1 AR031345 A1 AR 031345A1 AR P010105323 A ARP010105323 A AR P010105323A AR P010105323 A ARP010105323 A AR P010105323A AR 031345 A1 AR031345 A1 AR 031345A1
- Authority
- AR
- Argentina
- Prior art keywords
- imidazo
- benzodiazepine
- triazolo
- lower alkyl
- oxadiazol
- 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
Compuestos de formula en donde R1 es hidrogeno, halogeno, alquilo inferior, alcoxilo inferior, hidroxilo, ciano, trifluorometilo, trifluorometoxilo o alquiltio inferior; R2 es -C(O)O-alquilo inferior, isoxazol, 1,2,4-oxadiazol-3-ilo o 1,2,4-oxadiazol-5-ilo, cuyos anillos pueden estar sustituidos por alquilo inferior, trifluorometilo o cicloalquilo; R3 es hidrogeno, alquilo inferior, -(CH2)n-cicloalquilo, -(CH2)n-halogeno, -(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, halogeno, -SO2CH3, fenilo, OCF3, nitro, CF3, -NR2, o es -(CH2)n-indolilo, opcionalmente sustituido por alquilo inferior o alcoxilo inferior, o es pirrolidinil-5-oxo, -C(O)-NR2, -(CH2)n -OH, -(CH2)n-NR2 o -(CH2)n-benzo[1,3]dioxol; R es hidrogeno o alquilo inferior; y n es 0, 1, 2,o 3; y sus sales de adicion ácida farmacéuticamente aceptables, con la excepcion de los siguientes compuestos: Etil-9H-imidazo[1,5-a][1,2,4]triazolo[3,4-d][1,4]benzo-diazepina-10-carboxilato, 10-(3-ciclopropil-1,2,4-oxadiazol-5-il)-9H-imidazo[1,5-a][1,2,4]triazolo[4,3-d][1.4]-benzodiazepina, etil 3-fluoro-9H-imidazo[1,5-a][1,2,4]triazolo[4,3-d][1,4]-benzodiazepina-10-carboxilato, 10-(3-ciclopropil-1,2,4-oxadiazol-5-il)-3-fluoro-9H-imidazo[1,5-a][1,2,4]triazolo[4,3-d][1,4]benzodiazepina, etil-3-cloro-9H-imidazo[1,5-a][1,2,4]triazolo[4,3-d][1,4]benzodiazepina, etil-3-cloro-9H-imidazo[1,5-a][1,2,4]triazolo[4,3-d][1,4]-benzodiazepina-10-carboxilato y 3-cloro-10-(3-ciclopropil-1,2,4-oxadiazol-5-il)-9H-imidazo [1,5-a][1.2.4]triazol[4,3-d][1,4]benzodiazepina. Estos compuestos presentan una buena afinidad para el receptor GABA A a 5 y por consiguiente son utiles 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 |
|---|---|
| AR031345A1 true AR031345A1 (es) | 2003-09-17 |
Family
ID=8170315
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010105323A AR031345A1 (es) | 2000-11-16 | 2001-11-15 | Derivados de benzodiazepina como moduladores receptores 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) | AU2002217007B2 (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 |
| US7626029B2 (en) * | 2003-06-19 | 2009-12-01 | Daiichi Pharmaceutical Co., Ltd. | Method of selectively introducing amino substituent |
| WO2005060968A1 (en) | 2003-12-11 | 2005-07-07 | Sepracor Inc. | Combination of a sedative and a neurotransmitter modulator, and methods for improving sleep quality and treating depression |
| WO2006020959A2 (en) | 2004-08-13 | 2006-02-23 | Amgen Inc. | Substituted benzofused heterocycles |
| RU2007112675A (ru) * | 2004-10-12 | 2008-11-20 | Ф.Хоффманн-Ля Рош Аг (Ch) | ПРОИЗВОДНЫЕ ИМИДАЗО[1,5-a]ТРИАЗОЛО[1,5-d]БЕНЗОДИАЗЕПИНА ДЛЯ ЛЕЧЕНИЯ КОГНИТИВНЫХ РАССТРОЙСТВ |
| WO2006045429A1 (en) * | 2004-10-20 | 2006-05-04 | F. Hoffmann-La Roche Ag | Halogen substituted benzodiazepine derivatives |
| 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 |
| JP4783380B2 (ja) | 2004-12-14 | 2011-09-28 | エフ．ホフマン−ラ ロシュ アーゲー | Ｇａｂａレセプタ調節物質としての四環系イミダゾ−ベンゾジアゼピン類 |
| US8510055B2 (en) | 2005-08-03 | 2013-08-13 | The Johns Hopkins University | Methods for characterizing and treating cognitive impairment in aging and disease |
| EP1924712B1 (en) * | 2005-08-03 | 2018-10-03 | The Johns Hopkins University | Methods for characterizing and treating cognitive impairment in aging and disease |
| BRPI0617204A2 (pt) * | 2005-10-11 | 2011-07-19 | Hoffmann La Roche | derivados de imidazo benzodiazepina |
| WO2007053596A1 (en) * | 2005-10-31 | 2007-05-10 | Braincells, Inc. | Gaba receptor mediated modulation of neurogenesis |
| US9156836B2 (en) * | 2008-05-16 | 2015-10-13 | Synta Pharmaceuticals Corp. | Tricyclic triazole compounds that modulate HSP90 activity |
| CN102216304B (zh) | 2008-11-18 | 2014-07-09 | 弗·哈夫曼-拉罗切有限公司 | 二氢四氮杂苯并薁的烷基环己基醚 |
| JP5452608B2 (ja) * | 2008-11-28 | 2014-03-26 | エフ．ホフマン−ラ ロシュ アーゲー | バソプレシン介在受容体アンタゴニストとしての使用のためのジヒドロテトラアザベンゾアズレンのアリールシクロヘキシルエーテル |
| CU20090172A6 (es) | 2009-10-09 | 2011-10-05 | Facultad De Quimica Universidad De La Habana | Sistemas tricíclicos y tetracíclicos con actividad sobre el sistema nervioso central y vascular |
| US9145372B2 (en) | 2010-11-15 | 2015-09-29 | Agenebio, Inc. | Pyridazine derivatives, compositions and methods for treating cognitive impairment |
| US20150374705A1 (en) | 2012-02-14 | 2015-12-31 | Shanghai Institues for Biological Sciences | Substances for treatment or relief of pain |
| JP2015529254A (ja) * | 2012-09-21 | 2015-10-05 | ユーダブリューエム・リサーチ・ファウンデーション，インコーポレーテッド | 喘息における気道の過敏症及び炎症を制御するための新規なｇａｂａａアゴニスト及び使用方法 |
| CA3123897C (en) | 2013-12-20 | 2024-02-06 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| CA2990004C (en) * | 2015-06-19 | 2024-04-23 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating 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 |
| JP2021528427A (ja) * | 2018-06-19 | 2021-10-21 | エージンバイオ， インコーポレイテッド | 認知障害を処置するためのベンゾジアゼピン誘導体、組成物および方法 |
| 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 JP JP2002543495A patent/JP4088151B2/ja not_active Expired - Fee Related
- 2001-11-08 US US10/007,883 patent/US6743789B2/en not_active Expired - Fee Related
- 2001-11-08 DE DE60103776T patent/DE60103776T2/de not_active Expired - Lifetime
- 2001-11-08 WO PCT/EP2001/012887 patent/WO2002040487A2/en active IP Right Grant
- 2001-11-08 AU AU2002217007A patent/AU2002217007B2/en not_active Ceased
- 2001-11-08 PT PT01996541T patent/PT1337535E/pt unknown
- 2001-11-08 EP EP01996541A patent/EP1337535B1/en not_active Expired - Lifetime
- 2001-11-08 ES ES01996541T patent/ES2220831T3/es not_active Expired - Lifetime
- 2001-11-08 MX MXPA03004251A patent/MXPA03004251A/es active IP Right Grant
- 2001-11-08 HU HU0303281A patent/HUP0303281A3/hu unknown
- 2001-11-08 BR BR0115393-5A patent/BR0115393A/pt not_active IP Right Cessation
- 2001-11-08 SK SK723-2003A patent/SK7232003A3/sk unknown
- 2001-11-08 CA CA002427576A patent/CA2427576C/en not_active Expired - Fee Related
- 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 IL IL15581301A patent/IL155813A0/xx unknown
- 2001-11-08 YU YU35603A patent/YU35603A/sh unknown
- 2001-11-08 AT AT01996541T patent/ATE268776T1/de not_active IP Right Cessation
- 2001-11-08 CZ CZ20031597A patent/CZ295256B6/cs not_active IP Right Cessation
- 2001-11-08 RU RU2003116895/04A patent/RU2278865C2/ru not_active IP Right Cessation
- 2001-11-08 PL PL01362925A patent/PL362925A1/xx not_active Application Discontinuation
- 2001-11-08 DK DK01996541T patent/DK1337535T3/da active
- 2001-11-08 NZ NZ525413A patent/NZ525413A/en unknown
- 2001-11-08 CN CNB018189415A patent/CN1191255C/zh not_active Expired - Fee Related
- 2001-11-08 AU AU1700702A patent/AU1700702A/xx active Pending
- 2001-11-08 TR TR2004/02073T patent/TR200402073T4/xx 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 MY MYPI20015253A patent/MY141675A/en unknown
- 2001-11-15 GT GT200100230A patent/GT200100230A/es unknown
- 2001-11-15 UY UY27026A patent/UY27026A1/es not_active Application Discontinuation
- 2001-11-15 AR ARP010105323A patent/AR031345A1/es not_active Application Discontinuation
- 2001-11-15 PA PA20018532401A patent/PA8532401A1/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 BG BG107817A patent/BG107817A/bg unknown
- 2003-05-16 MA MA27163A patent/MA26962A1/fr unknown
-
2004
- 2004-07-21 HK HK04105348A patent/HK1062442A1/xx not_active IP Right Cessation
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |