PE20020583A1 - Derivados de benzodiazepina como moduladores del receptor gaba a - Google Patents
Derivados de benzodiazepina como moduladores del receptor gaba aInfo
- Publication number
- PE20020583A1 PE20020583A1 PE2001001135A PE2001001135A PE20020583A1 PE 20020583 A1 PE20020583 A1 PE 20020583A1 PE 2001001135 A PE2001001135 A PE 2001001135A PE 2001001135 A PE2001001135 A PE 2001001135A PE 20020583 A1 PE20020583 A1 PE 20020583A1
- Authority
- PE
- Peru
- Prior art keywords
- benzodiazepine
- triazolo
- imidazo
- alkyl
- oxadiazol
- Prior art date
Links
- 102000004300 GABA-A Receptors Human genes 0.000 title 1
- 108090000839 GABA-A Receptors Proteins 0.000 title 1
- 229940053197 benzodiazepine derivative antiepileptics Drugs 0.000 title 1
- 150000001557 benzodiazepines Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- NZTCFMPWFGWRBN-UHFFFAOYSA-N 3H-[1,2,4]triazolo[4,3-d][1,4]benzodiazepine-10-carboxylic acid Chemical compound N1=NCN2C=CN=C3C(=C21)C=C(C=C3)C(=O)O NZTCFMPWFGWRBN-UHFFFAOYSA-N 0.000 abstract 2
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical class F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 abstract 2
- LZOISVDTQDUWEU-UHFFFAOYSA-N 2,4,8,10,11-pentazatetracyclo[11.4.0.02,6.08,12]heptadeca-1(17),4,6,9,11,13,15-heptaene Chemical class C=1N2C=NN=C2C2=CC=CC=C2N2CN=CC2=1 LZOISVDTQDUWEU-UHFFFAOYSA-N 0.000 abstract 1
- NKWDDGCMDWGDLU-UHFFFAOYSA-N 3H-[1,2,4]triazolo[4,3-d][1,4]benzodiazepine Chemical compound N1=NCN2C=CN=C3C(=C21)C=CC=C3 NKWDDGCMDWGDLU-UHFFFAOYSA-N 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- SFPHNARDXIEZPB-UHFFFAOYSA-N C1=NNN2C=CN=C3C(=C21)C=C(C=C3)C(=O)O Chemical compound C1=NNN2C=CN=C3C(=C21)C=C(C=C3)C(=O)O SFPHNARDXIEZPB-UHFFFAOYSA-N 0.000 abstract 1
- -1 CYANE Chemical class 0.000 abstract 1
- 102000005915 GABA Receptors Human genes 0.000 abstract 1
- 108010005551 GABA Receptors Proteins 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- TUJKJAMUKRIRHC-UHFFFAOYSA-N hydroxyl Chemical class [OH] TUJKJAMUKRIRHC-UHFFFAOYSA-N 0.000 abstract 1
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 abstract 1
- 238000000034 method Methods 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
- 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)
- Neurology (AREA)
- Neurosurgery (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
SE REFIERE A DERIVADOS SUSTITUIDOS DE IMIDAZO[1,5-a][1,2,4]TRIAZOLO[4,3-d][1,4]BENZODIAZEPINA; DONDE: R1 ES H, HALOGENO, ALQUILO, ALCOXILO, HIDROXILO, CIANO, TRIFLUOROMETILO, TRIFLUOROMETOXILO, ALQUILTIO; R2 ES COO-ALQUILO, ISOXAZOL, 1,2,4-OXADIAZOL-3-IL, 1,2,4-OXADIAZOL-5-ILO OPCIONALMENTE SUSTITUIDO POR ALQUILO, TRIFLUOROMETILO, CICLOALQUILO; R3 ES H, ALQUILO, (CH2)n-CICLOALQUILO, (CH2)nHALOGENO, (CH2)n-PIRIDN-4-ILO, (CH2)nFENILO; R ES H, ALQUILO; n ES 0-3; EXCEPTO LOS COMPUESOS ETIL-9H-IMIDAZO[1,5-a][1,2,4]TRIAZOLO[3,4-d][1,4]BENZODIAZEPINA-10-CARBOXILATO, ENTRE OTROS; SON COMPUESTOS PREFERIDOS ETIL-3-METOXI-9H-IMIDAZO[1,5-a][1,2,4]TRIAZOLO[4,3-d][1,4]-BENZODIAZEPINA-10-CARBOXILATO; ETIL-3-METOXI-7-METIL-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-METOXI-9H-IMIDAZO[1,5a][1,2,4]TRIAZOLO[4,3-d][1,4]BENZODIAZEPINA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS TIENEN AFINIDAD Y SELECTIVIDAD PARA LOS SITIOS DE UNION DEL RECEPTOR GABA A SUBUNIDAD O5 Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE TRASTORNOS COGNITIVOS COMO LA ENFERMEDAD DE ALZHEIMER
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP00124332 | 2000-11-16 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20020583A1 true PE20020583A1 (es) | 2002-07-06 |
Family
ID=8170315
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2001001135A PE20020583A1 (es) | 2000-11-16 | 2001-11-14 | Derivados de benzodiazepina como moduladores del receptor gaba a |
Country Status (40)
| 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) |
| 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 |
| WO2004113321A1 (ja) * | 2003-06-19 | 2004-12-29 | Daiichi Pharmaceutical Co., Ltd. | 選択的なアミノ置換基導入法 |
| JP5646126B2 (ja) | 2003-12-11 | 2014-12-24 | サノビオン ファーマシューティカルズ インクＳｕｎｏｖｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃ． | 鎮静剤と神経伝達物質調節剤の併用、および睡眠の質の向上方法および鬱の治療方法 |
| 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 |
| MX2007004640A (es) * | 2004-10-20 | 2007-06-08 | Hoffmann La Roche | Derivados de benzodiazepina sustituidos con halogeno. |
| 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 |
| BRPI0515800A (pt) | 2004-12-14 | 2008-08-05 | Hoffmann La Roche | imidazo-benzodiazepinas tetracìclicas como moduladores de receptores de gaba |
| 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 |
| ATE477255T1 (de) * | 2005-10-11 | 2010-08-15 | Hoffmann La Roche | Imidazobenzdiazepinderivate |
| EP1942879A1 (en) | 2005-10-31 | 2008-07-16 | 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 |
| AU2009317386B2 (en) * | 2008-11-18 | 2013-07-25 | F. Hoffmann-La Roche Ag | Alkylcyclohexylethers of dihydrotetraazabenzoazulenes |
| CN102227428B (zh) * | 2008-11-28 | 2015-03-25 | 弗·哈夫曼-拉罗切有限公司 | 用作加压素via受体拮抗剂的二氢四氮杂苯并薁的芳基环己基醚 |
| 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 |
| WO2012068161A1 (en) | 2010-11-15 | 2012-05-24 | 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 |
| MA42624A (fr) | 2015-06-19 | 2021-04-28 | Agenebio Inc | Dérivés de benzodiazépine, compositions et méthodes de traitement de la déficience cognitive |
| 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 |
| 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 |
| 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 |
| JP2025529834A (ja) | 2022-08-19 | 2025-09-09 | 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アゼピン誘導体、組成物および方法 |
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 PL PL01362925A patent/PL362925A1/xx not_active Application Discontinuation
- 2001-11-08 AU AU1700702A patent/AU1700702A/xx active Pending
- 2001-11-08 IL IL15581301A patent/IL155813A0/xx unknown
- 2001-11-08 HU HU0303281A patent/HUP0303281A3/hu 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 PT PT01996541T patent/PT1337535E/pt unknown
- 2001-11-08 EP EP01996541A patent/EP1337535B1/en not_active Expired - Lifetime
- 2001-11-08 SI SI200130125T patent/SI1337535T1/xx unknown
- 2001-11-08 CN CNB018189415A patent/CN1191255C/zh not_active Expired - Fee Related
- 2001-11-08 KR KR10-2003-7006609A patent/KR100504300B1/ko not_active Expired - Fee Related
- 2001-11-08 YU YU35603A patent/YU35603A/sh unknown
- 2001-11-08 HR HR20030360A patent/HRP20030360A2/hr not_active Application Discontinuation
- 2001-11-08 ES ES01996541T patent/ES2220831T3/es not_active Expired - Lifetime
- 2001-11-08 AU AU2002217007A patent/AU2002217007B2/en not_active Ceased
- 2001-11-08 NZ NZ525413A patent/NZ525413A/en unknown
- 2001-11-08 MX MXPA03004251A patent/MXPA03004251A/es active IP Right Grant
- 2001-11-08 WO PCT/EP2001/012887 patent/WO2002040487A2/en not_active Ceased
- 2001-11-08 TR TR2004/02073T patent/TR200402073T4/xx unknown
- 2001-11-08 DE DE60103776T patent/DE60103776T2/de not_active Expired - Lifetime
- 2001-11-08 DK DK01996541T patent/DK1337535T3/da active
- 2001-11-08 BR BR0115393-5A patent/BR0115393A/pt not_active IP Right Cessation
- 2001-11-08 RU RU2003116895/04A patent/RU2278865C2/ru not_active IP Right Cessation
- 2001-11-08 CA CA002427576A patent/CA2427576C/en not_active Expired - Fee Related
- 2001-11-08 US US10/007,883 patent/US6743789B2/en not_active Expired - Fee Related
- 2001-11-08 AT AT01996541T patent/ATE268776T1/de not_active IP Right Cessation
- 2001-11-08 JP JP2002543495A patent/JP4088151B2/ja not_active Expired - Fee Related
- 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 UY UY27026A patent/UY27026A1/es not_active Application Discontinuation
- 2001-11-15 MY MYPI20015253A patent/MY141675A/en unknown
- 2001-11-15 PA PA20018532401A patent/PA8532401A1/es unknown
- 2001-11-15 AR ARP010105323A patent/AR031345A1/es not_active Application Discontinuation
- 2001-11-15 GT GT200100230A patent/GT200100230A/es unknown
-
2003
- 2003-05-05 ZA ZA200303435A patent/ZA200303435B/en unknown
- 2003-05-15 NO NO20032208A patent/NO324706B1/no unknown
- 2003-05-15 EC EC2003004607A patent/ECSP034607A/es unknown
- 2003-05-16 MA MA27163A patent/MA26962A1/fr unknown
- 2003-05-16 BG BG107817A patent/BG107817A/bg unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |