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
- SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical class N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 title 1
- 102000005915 GABA Receptors Human genes 0.000 title 1
- 108010005551 GABA Receptors Proteins 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000004505 1,2,4-oxadiazol-5-yl group Chemical group O1N=CN=C1* 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
- 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 1
- 102000004300 GABA-A Receptors Human genes 0.000 abstract 1
- 108090000839 GABA-A Receptors Proteins 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 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
- 125000001424 substituent 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
- 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)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (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 (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) | 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) |
| 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 |
| PL1691811T3 (pl) | 2003-12-11 | 2014-12-31 | Sunovion Pharmaceuticals Inc | Skojarzenie leku uspokajającego i modulatora neuroprzekaźnikowego oraz sposoby poprawy jakości snu i leczenia depresji |
| US7572783B2 (en) | 2004-08-13 | 2009-08-11 | Amgen Inc. | Substituted benzofused heterocycles |
| BRPI0517412A (pt) * | 2004-10-12 | 2008-10-07 | Hoffmann La Roche | derivados de benzodiazepina substituìdos |
| 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 |
| EP1805184B1 (en) * | 2004-10-20 | 2013-01-09 | F. Hoffmann-La Roche AG | Imidazo-benzodiazepine derivatives |
| KR100923393B1 (ko) * | 2004-12-14 | 2009-10-23 | 에프. 호프만-라 로슈 아게 | Ｇａｂａ 수용체 조절제로서 테트라사이클릭이미다조-벤조다이아제핀 |
| US8510055B2 (en) | 2005-08-03 | 2013-08-13 | The Johns Hopkins University | Methods for characterizing and treating cognitive impairment in aging and disease |
| WO2007019312A2 (en) * | 2005-08-03 | 2007-02-15 | 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 |
| 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 |
| WO2010057795A1 (en) * | 2008-11-18 | 2010-05-27 | F. Hoffmann-La Roche Ag | Alkylcyclohexylethers of dihydrotetraazabenzoazulenes |
| PL2370441T3 (pl) * | 2008-11-28 | 2014-02-28 | Hoffmann La Roche | Arylocykloheksyloetery dihydrotetraazabenzoazulenów do stosowania jako antagoniści receptora v1a wazopresyny |
| 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 |
| NO3034079T3 (es) | 2010-11-15 | 2018-06-09 | ||
| US20150374705A1 (en) | 2012-02-14 | 2015-12-31 | Shanghai Institues for Biological Sciences | Substances for treatment or relief of pain |
| CA2885148A1 (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 |
| US10329301B2 (en) * | 2013-12-20 | 2019-06-25 | 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 |
| 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 |
| 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 |
| 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 |
| EP4572852A1 (en) | 2022-08-19 | 2025-06-25 | 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 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 AU AU2002217007A patent/AU2002217007B2/en not_active Ceased
- 2001-11-08 IL IL15581301A patent/IL155813A0/xx unknown
- 2001-11-08 WO PCT/EP2001/012887 patent/WO2002040487A2/en not_active Ceased
- 2001-11-08 CN CNB018189415A patent/CN1191255C/zh not_active Expired - Fee Related
- 2001-11-08 HR HR20030360A patent/HRP20030360A2/hr not_active Application Discontinuation
- 2001-11-08 BR BR0115393-5A patent/BR0115393A/pt not_active IP Right Cessation
- 2001-11-08 NZ NZ525413A patent/NZ525413A/en unknown
- 2001-11-08 SK SK723-2003A patent/SK7232003A3/sk unknown
- 2001-11-08 EP EP01996541A patent/EP1337535B1/en not_active Expired - Lifetime
- 2001-11-08 PT PT01996541T patent/PT1337535E/pt unknown
- 2001-11-08 RU RU2003116895/04A patent/RU2278865C2/ru not_active IP Right Cessation
- 2001-11-08 SI SI200130125T patent/SI1337535T1/xx unknown
- 2001-11-08 TR TR2004/02073T patent/TR200402073T4/xx unknown
- 2001-11-08 AU AU1700702A patent/AU1700702A/xx active Pending
- 2001-11-08 ES ES01996541T patent/ES2220831T3/es not_active Expired - Lifetime
- 2001-11-08 CZ CZ20031597A patent/CZ295256B6/cs not_active IP Right Cessation
- 2001-11-08 KR KR10-2003-7006609A patent/KR100504300B1/ko not_active Expired - Fee Related
- 2001-11-08 PL PL01362925A patent/PL362925A1/xx not_active Application Discontinuation
- 2001-11-08 DK DK01996541T patent/DK1337535T3/da active
- 2001-11-08 AT AT01996541T patent/ATE268776T1/de not_active IP Right Cessation
- 2001-11-08 YU YU35603A patent/YU35603A/sh unknown
- 2001-11-08 DE DE60103776T patent/DE60103776T2/de not_active Expired - Lifetime
- 2001-11-08 CA CA002427576A patent/CA2427576C/en not_active Expired - Fee Related
- 2001-11-08 HU HU0303281A patent/HUP0303281A3/hu unknown
- 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 GT GT200100230A patent/GT200100230A/es unknown
- 2001-11-15 PA PA20018532401A patent/PA8532401A1/es unknown
- 2001-11-15 AR ARP010105323A patent/AR031345A1/es not_active Application Discontinuation
-
2003
- 2003-05-05 ZA ZA200303435A patent/ZA200303435B/en unknown
- 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
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ECSP034607A (es) | Derivados de benzodiazepina como modulares del receptor gaba a | |
| ES2525763T3 (es) | Derivados del ácido fenilalcanoico sustituido y sus usos para el tratamiento de enfermedades respiratorias | |
| PE20040832A1 (es) | Derivados de indolil pirazinona | |
| AR037489A1 (es) | Quinolinas sustituidas y proceso para su preparacion | |
| ECSP034431A (es) | N-oxidos como profarmacos antagonistas del receptor nk1 de derivados de 4-fenil-piridina | |
| NZ512731A (en) | Tricyclic inhibitors of poly(ADP-ribose) polymerases | |
| PA8517101A1 (es) | Derivados de tropano ùtiles en terapia | |
| AR034553A1 (es) | Triazolopirimidinas sustituidas, medicamento que los contienen, composiciones farmaceuticas y el uso de dichos derivados para la fabricacion de medicamentos como agentes anticancerosos | |
| AR038341A1 (es) | Compuestos que son agonistas de receptores alfa-1 preferentemente agonistas de receptores alfa-1a/l | |
| AR045180A1 (es) | Derivados 3-amino cromado y 2-amino tetralina y composiciones que contienen a dichos compuestos | |
| AR036032A1 (es) | Compuesto derivado de quinolina, composicion que lo comprende; uso del mismo en la fabricacion de medicamentos, proceso para prepararlo, y metodo para detectar y seleccionar un agente que module la actividad del mif | |
| MX2009007502A (es) | Derivados de espirocromanona sustituidos. | |
| YU18999A (sh) | Supstituisani tricikli | |
| UY24532A1 (es) | Derivados del indazol sustituidos y compuestos relacionados | |
| BG104287A (en) | Halogensubstituted tetracyclic derivatives of tetrahydrofuran | |
| AR042002A1 (es) | Benzoxazinonas sustituidas, proceso de obtencion y usos para tratamiento de enfermedades del sistema nervioso central. | |
| CO4940485A1 (es) | Nuevos derivados de triazole, procedimiento para su preparacion y composiciones farmaceuticas que los contienen | |
| DK1204662T3 (da) | Azaindoler med serotoninreceptoraffinitet | |
| ATE355843T1 (de) | N-biphenylcarbonyl- und n-phenylpyridylcarbonyl substituierte bi- and tricyclische azepine und diazepine als vasopressin-agonisten | |
| ATE337827T1 (de) | N-aryl-4,5-diaminopyrazole und diese verbindungen enthaltende färbemittel | |
| AR036735A1 (es) | Derivados de 5-metoxi-8-aril-[1,2,4]triazolo[1,5-a]piridina | |
| DK1583752T3 (da) | Cykliseringsfremgangsmåde til substituerede benzothiazolderivater | |
| MY139070A (en) | (indol-3-yl)-hetero cycle derivatives | |
| CA2431617A1 (en) | 7-heterocyclyl quinoline and thieno[2,3-b]pyridine derivatives useful as antagonists of gonadotropin releasing hormone | |
| AR035718A1 (es) | Derivados de quinolina, procedimientos para su preparacion, composiciones farmaceuticas que lo comprenden, y el uso de tales compuestos en la fabricacion de medicamentos |