AR033753A1 - Derivados de imidazo[1,5-a]pirimido[5,4-d]benzazepina - Google Patents
Derivados de imidazo[1,5-a]pirimido[5,4-d]benzazepinaInfo
- Publication number
- AR033753A1 AR033753A1 ARP020101805A ARP020101805A AR033753A1 AR 033753 A1 AR033753 A1 AR 033753A1 AR P020101805 A ARP020101805 A AR P020101805A AR P020101805 A ARP020101805 A AR P020101805A AR 033753 A1 AR033753 A1 AR 033753A1
- Authority
- AR
- Argentina
- Prior art keywords
- lower alkyl
- cycloalkyl
- substituted
- benzazepina
- pyrimid
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 230000007370 cognitive improvement Effects 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
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 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
- 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)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (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)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
Compuestos de fórmula I en donde R1 es halógeno o alquilo inferior; R2 es hidrógeno; alquilo inferior, cicloalquilo -(CH2)m-fenilo, en donde el anillo fenilo puede estar sustituido por alcoxilo inferior, o es -(CH2)m-indolilo; R3 es -C(O)O-alquilo inferior, -C(O)OH, o un grupo heteroaromático de cinco miembros, cuyos anillos pueden estar sustituidos por alquilo inferior o cicloalquilo; n es 0, 1 o 2; m es 0, 1 o 2; y sus sales de adición ácida farmacéuticamente aceptables. Se ha descubierto que esta clase de compuestos muestra una elevada afinidad y selectividad para los sitios de reunión del receptor alfa 5 de GABA A y pueden ser útiles para el tratamiento de mejoras cognitivas o trastornos cognitivos como la enfermedad de Alzheimer.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01112222 | 2001-05-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR033753A1 true AR033753A1 (es) | 2004-01-07 |
Family
ID=8177471
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020101805A AR033753A1 (es) | 2001-05-18 | 2002-05-16 | Derivados de imidazo[1,5-a]pirimido[5,4-d]benzazepina |
Country Status (37)
| Country | Link |
|---|---|
| US (1) | US6686352B2 (es) |
| EP (1) | EP1399448B1 (es) |
| JP (1) | JP4068466B2 (es) |
| KR (1) | KR100533406B1 (es) |
| CN (1) | CN1230436C (es) |
| AR (1) | AR033753A1 (es) |
| AT (1) | ATE283857T1 (es) |
| AU (1) | AU2002338898B2 (es) |
| BG (1) | BG108369A (es) |
| BR (1) | BR0209859A (es) |
| CA (1) | CA2446903C (es) |
| CZ (1) | CZ20033355A3 (es) |
| DE (1) | DE60202147T2 (es) |
| DK (1) | DK1399448T3 (es) |
| EC (1) | ECSP034851A (es) |
| ES (1) | ES2232778T3 (es) |
| GT (1) | GT200200087A (es) |
| HR (1) | HRP20030890A2 (es) |
| HU (1) | HUP0400743A3 (es) |
| IL (2) | IL158572A0 (es) |
| JO (1) | JO2297B1 (es) |
| MA (1) | MA27024A1 (es) |
| MX (1) | MXPA03010529A (es) |
| MY (1) | MY127570A (es) |
| NO (1) | NO20035104D0 (es) |
| NZ (1) | NZ529097A (es) |
| PA (1) | PA8545201A1 (es) |
| PE (1) | PE20030041A1 (es) |
| PL (1) | PL366846A1 (es) |
| PT (1) | PT1399448E (es) |
| RU (1) | RU2287531C2 (es) |
| SI (1) | SI1399448T1 (es) |
| SK (1) | SK15252003A3 (es) |
| TW (1) | TWI251489B (es) |
| WO (1) | WO2002094834A1 (es) |
| YU (1) | YU90003A (es) |
| ZA (1) | ZA200308544B (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS50568B8 (sr) | 2004-05-14 | 2019-08-30 | Millennium Pharm Inc | Jedinjenja i postupci za inhibiciju mitotičke progresije inhibiranjem aurora kinaze |
| CA2582235A1 (en) * | 2004-10-04 | 2006-04-20 | Millennium Pharmaceuticals, Inc. | Lactam compounds useful as protein kinase inhibitors |
| 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 |
| NZ554439A (en) * | 2004-10-20 | 2009-09-25 | Hoffmann La Roche | Imidazo-benzodiazepine derivatives |
| AU2006301377B2 (en) * | 2005-10-11 | 2012-03-08 | F. Hoffmann-La Roche Ag | Imidazo benzodiazepine derivatives |
| PE20080145A1 (es) * | 2006-03-21 | 2008-02-11 | Janssen Pharmaceutica Nv | Tetrahidro-pirimidoazepinas como moduladores de trpv1 |
| CL2007003244A1 (es) | 2006-11-16 | 2008-04-04 | Millennium Pharm Inc | Compuestos derivados de pirimido[5,4-d][2]benzazepina; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento del cancer. |
| JP5562865B2 (ja) | 2007-12-17 | 2014-07-30 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Trpv1のイミダゾロ−、オキサゾロ−、及びチアゾロピリミジン・モジュレーター |
| CN101735211B (zh) * | 2008-11-04 | 2012-11-14 | 复旦大学 | 2,3-二氢[1,5]苯并噻氮杂*类化合物或其盐在制备GSK-3β抑制剂中的用途 |
| US7998952B2 (en) | 2008-12-05 | 2011-08-16 | Millennium Pharmaceuticals, Inc. | Thiolactams and uses thereof |
| MX2011006725A (es) | 2008-12-22 | 2011-09-15 | Millennium Pharm Inc | Combinacion de inhibidores de aurora cinasa y anticuerpos anti-cd20. |
| JO3635B1 (ar) | 2009-05-18 | 2020-08-27 | Millennium Pharm Inc | مركبات صيدلانية صلبة وطرق لانتاجها |
| CN102770024A (zh) | 2010-02-19 | 2012-11-07 | 米伦纽姆医药公司 | 4-{[9-氯-7-(2-氟-6-甲氧基苯基)-5h-嘧啶并[5,4-d][2]苯并氮杂卓-2基]氨基}-2-甲氧基苯甲酸钠的结晶形式 |
| 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 |
| CN102424670A (zh) * | 2011-10-31 | 2012-04-25 | 江苏阿尔法药业有限公司 | 一种合成3-(3-氯丙基)-1,3,4,5-四氢-7,8-二甲氧基-2h-3-苯并氮杂卓-2-酮的方法 |
| US20150374705A1 (en) | 2012-02-14 | 2015-12-31 | Shanghai Institues for Biological Sciences | Substances for treatment or relief of pain |
| US20130303519A1 (en) | 2012-03-20 | 2013-11-14 | Millennium Pharmaceuticals, Inc. | Methods of treating cancer using aurora kinase inhibitors |
| WO2014153509A1 (en) | 2013-03-22 | 2014-09-25 | Millennium Pharmaceuticals, Inc. | Combination of catalytic mtorc 1/2 inhibitors and selective inhibitors of aurora a kinase |
| AU2014368961B2 (en) | 2013-12-20 | 2019-10-17 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| EP3310785B1 (en) | 2015-06-19 | 2024-11-20 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| JP2018524292A (ja) | 2015-07-21 | 2018-08-30 | ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. | オーロラキナーゼインヒビターと化学療法剤の投与 |
| 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 |
| MX2020013927A (es) | 2018-06-19 | 2021-03-02 | Agenebio Inc | Derivados de benzodiazepina, composiciones y metodos para tratar el deterioro cognitivo. |
| CN110452172B (zh) * | 2019-08-21 | 2021-03-26 | 爱斯特(成都)生物制药股份有限公司 | 一种苯并己内酰胺的合成方法 |
| CN112159411A (zh) * | 2020-10-15 | 2021-01-01 | 南京工业大学 | 一种三氟甲基取代嘧啶并[1,3]二氮杂*化合物及其制备方法 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2607503B1 (fr) * | 1986-12-02 | 1989-02-24 | Rhone Poulenc Sante | Nouveaux derives de l'isoindolinone, leur preparation et les compositions pharmaceutiques qui les contiennent |
| TW201311B (es) | 1991-06-17 | 1993-03-01 | Hoffmann La Roche | |
| RU2119496C1 (ru) * | 1992-04-14 | 1998-09-27 | Научно-исследовательский институт фармакологии Российской академии медицинских наук | Производные n-ацилпролилдипептидов |
| FR2728902B1 (fr) * | 1994-12-29 | 1997-01-31 | Synthelabo | Derives d'acide 8-oxo-5,8-dihydro-6h-dibenzo(a,g)quinolizine-13-propanoique, leur preparation et leur application en therapeutique |
| WO1999043682A1 (en) * | 1998-02-26 | 1999-09-02 | Neurogen Corporation | 2-(het-)aryl-4-(cyclic amino substituted) heteroaryl fused pyridine derivatives, their preparation and their use as (ant-)agonists for gaba (a) brain receptors |
| US6177569B1 (en) * | 1998-08-25 | 2001-01-23 | Neurogen Corporation | Oxo-pyridoimidazole-carboxamides: GABA brain receptor ligands |
| FR2783828B1 (fr) | 1998-09-29 | 2000-11-10 | Synthelabo | Derives d'acide 5,6-dihydro-4h-imidazo[1,2-a][1] benzazepine -1-acetique, leur preparation et leur application en therapeutique |
| ES2195943T3 (es) | 1999-11-12 | 2003-12-16 | Neurogen Corp | Compuestos heteroaromaticos biciclicos y triciclicos. |
| TWI239333B (en) | 2000-11-16 | 2005-09-11 | Hoffmann La Roche | Benzodiazepine derivatives as GABA A receptor modulators |
-
2002
- 2002-04-09 US US10/118,584 patent/US6686352B2/en not_active Expired - Fee Related
- 2002-05-08 BR BR0209859-8A patent/BR0209859A/pt not_active IP Right Cessation
- 2002-05-08 YU YU90003A patent/YU90003A/sh unknown
- 2002-05-08 CN CNB028101774A patent/CN1230436C/zh not_active Expired - Fee Related
- 2002-05-08 WO PCT/EP2002/005121 patent/WO2002094834A1/en not_active Ceased
- 2002-05-08 ES ES02771640T patent/ES2232778T3/es not_active Expired - Lifetime
- 2002-05-08 HR HR20030890A patent/HRP20030890A2/xx not_active Application Discontinuation
- 2002-05-08 NZ NZ529097A patent/NZ529097A/en unknown
- 2002-05-08 SK SK1525-2003A patent/SK15252003A3/sk unknown
- 2002-05-08 RU RU2003136078/04A patent/RU2287531C2/ru not_active IP Right Cessation
- 2002-05-08 DK DK02771640T patent/DK1399448T3/da active
- 2002-05-08 PL PL02366846A patent/PL366846A1/xx not_active Application Discontinuation
- 2002-05-08 KR KR10-2003-7015036A patent/KR100533406B1/ko not_active Expired - Fee Related
- 2002-05-08 IL IL15857202A patent/IL158572A0/xx unknown
- 2002-05-08 MX MXPA03010529A patent/MXPA03010529A/es active IP Right Grant
- 2002-05-08 CA CA002446903A patent/CA2446903C/en not_active Expired - Fee Related
- 2002-05-08 JP JP2002591507A patent/JP4068466B2/ja not_active Expired - Fee Related
- 2002-05-08 SI SI200230055T patent/SI1399448T1/xx unknown
- 2002-05-08 AT AT02771640T patent/ATE283857T1/de not_active IP Right Cessation
- 2002-05-08 EP EP02771640A patent/EP1399448B1/en not_active Expired - Lifetime
- 2002-05-08 AU AU2002338898A patent/AU2002338898B2/en not_active Ceased
- 2002-05-08 DE DE60202147T patent/DE60202147T2/de not_active Expired - Lifetime
- 2002-05-08 CZ CZ20033355A patent/CZ20033355A3/cs unknown
- 2002-05-08 HU HU0400743A patent/HUP0400743A3/hu unknown
- 2002-05-08 PT PT02771640T patent/PT1399448E/pt unknown
- 2002-05-14 JO JO200243A patent/JO2297B1/en active
- 2002-05-15 TW TW091110162A patent/TWI251489B/zh not_active IP Right Cessation
- 2002-05-15 PA PA20028545201A patent/PA8545201A1/es unknown
- 2002-05-16 PE PE2002000413A patent/PE20030041A1/es not_active Application Discontinuation
- 2002-05-16 AR ARP020101805A patent/AR033753A1/es not_active Application Discontinuation
- 2002-05-16 GT GT200200087A patent/GT200200087A/es unknown
- 2002-05-17 MY MYPI20021808A patent/MY127570A/en unknown
-
2003
- 2003-10-23 IL IL158572A patent/IL158572A/en not_active IP Right Cessation
- 2003-10-31 ZA ZA200308544A patent/ZA200308544B/en unknown
- 2003-11-14 MA MA27398A patent/MA27024A1/fr unknown
- 2003-11-17 EC EC2003004851A patent/ECSP034851A/es unknown
- 2003-11-17 NO NO20035104A patent/NO20035104D0/no not_active Application Discontinuation
- 2003-11-18 BG BG108369A patent/BG108369A/bg unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |