ECSP034851A - Derivados imidazo[1,5-a]pirimido[5,4-d]benzazepina como moduladores del receptor gaba a - Google Patents
Derivados imidazo[1,5-a]pirimido[5,4-d]benzazepina como moduladores del receptor gaba aInfo
- Publication number
- ECSP034851A ECSP034851A EC2003004851A ECSP034851A ECSP034851A EC SP034851 A ECSP034851 A EC SP034851A EC 2003004851 A EC2003004851 A EC 2003004851A EC SP034851 A ECSP034851 A EC SP034851A EC SP034851 A ECSP034851 A EC SP034851A
- Authority
- EC
- Ecuador
- Prior art keywords
- lower alkyl
- gaba
- benzazepina
- pyrimid
- cycloalkyl
- 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
- 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
La presente invención se refiere a compuestos de fórmula 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(0) O-alquilo inferior, -C(0) OH, o un grupo heteroaromático de cinco miembros, cuyos anillos pueden estar sustituidos por alquilo inferior o cicloalquilo; n es 0, 1 ó 2; m es 0, 1 ó 2; y sus sales de adición ácida farmacéuticamente aceptables. Se ha descubierto que esta clase de compuestos muestran una elevada afinidad y selectividad para los sitios de unión del receptor a5 de GABA A y pueden ser útiles para el tratamiento de mejoras cognitivas o de 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 |
|---|---|
| ECSP034851A true ECSP034851A (es) | 2003-12-24 |
Family
ID=8177471
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2003004851A ECSP034851A (es) | 2001-05-18 | 2003-11-17 | Derivados imidazo[1,5-a]pirimido[5,4-d]benzazepina como moduladores del receptor gaba a |
Country Status (38)
| 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) |
| HK (1) | HK1066544A1 (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) | NO20035104L (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 (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20120091275A (ko) | 2004-05-14 | 2012-08-17 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 아우로라 키나아제의 억제에 의해 유사분열 진행을 억제하기 위한 화합물 및 그 방법 |
| EP1799684B1 (en) * | 2004-10-04 | 2014-12-03 | Millennium Pharmaceuticals, Inc. | Lactam compounds useful as protein kinase inhibitors |
| MX2007004640A (es) * | 2004-10-20 | 2007-06-08 | Hoffmann La Roche | Derivados de benzodiazepina sustituidos con halogeno. |
| MX2007004639A (es) * | 2004-10-20 | 2007-06-08 | Hoffmann La Roche | Derivados de imidazo-benzodiazepina. |
| 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. |
| CL2008003749A1 (es) | 2007-12-17 | 2010-01-15 | Janssen Pharmaceutica Nv | Compuestos derivados de imidazol, oxazol, y tiazol pirimidina, moduladores de trpv1, proceso de preparacion, composicion farmaceutica y su uso en el tratamiento de enfermedades, trastornos o condicion de dolor, prurito, artritis, tos, asma, trastorno del oido interno y enfermedad inflamatoria intestinal, entre otras. |
| 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 |
| JP5684719B2 (ja) * | 2008-12-05 | 2015-03-18 | 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． | Ｐｌｋ阻害剤としての５，７−ジヒドロ−６ｈ−ピリミド［５、−４ｄ］［１］ベンゾアゼピン−６−チオン |
| EP2376082B1 (en) | 2008-12-22 | 2014-03-05 | Millennium Pharmaceuticals, Inc. | Combination of aurora kinase inhibitors and anti-cd20 antibodies |
| JO3635B1 (ar) | 2009-05-18 | 2020-08-27 | Millennium Pharm Inc | مركبات صيدلانية صلبة وطرق لانتاجها |
| JP2013520424A (ja) | 2010-02-19 | 2013-06-06 | 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 | ナトリウム４−｛［９−クロロ−７−（２−フルオロ−６−メトキシフェニル）−５Ｈ−ピリミド［５，４−ｄ］［２］ベンゾアゼピン−２−イル］アミノ｝−２−メトキシベンゾエートの結晶形 |
| 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 |
| CN105209042B (zh) | 2013-03-22 | 2019-03-08 | 米伦纽姆医药公司 | 催化性mtorc 1/2抑制剂与选择性极光a激酶抑制剂的组合 |
| AU2014368961B2 (en) | 2013-12-20 | 2019-10-17 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| WO2016205739A1 (en) | 2015-06-19 | 2016-12-22 | Belew Mekonnen | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| EP3324976A4 (en) | 2015-07-21 | 2019-03-27 | Millennium Pharmaceuticals, Inc. | ADMINISTRATION OF KINASE AURORA INHIBITOR AND CHEMOTHERAPEUTIC AGENTS |
| US11505555B2 (en) | 2016-12-19 | 2022-11-22 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| WO2019246300A1 (en) | 2018-06-19 | 2019-12-26 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| 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 (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201311B (es) | 1991-06-17 | 1993-03-01 | Hoffmann La Roche | |
| 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 |
| US6511987B1 (en) | 1999-11-12 | 2003-01-28 | Neurogen Corporation | Bicyclic and tricyclic heteroaromatic compounds |
| TWI239333B (en) | 2000-11-16 | 2005-09-11 | Hoffmann La Roche | Benzodiazepine derivatives as GABA A receptor modulators |
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2002
- 2002-04-09 US US10/118,584 patent/US6686352B2/en not_active Expired - Fee Related
- 2002-05-08 NZ NZ529097A patent/NZ529097A/en unknown
- 2002-05-08 BR BR0209859-8A patent/BR0209859A/pt not_active IP Right Cessation
- 2002-05-08 ES ES02771640T patent/ES2232778T3/es not_active Expired - Lifetime
- 2002-05-08 DK DK02771640T patent/DK1399448T3/da active
- 2002-05-08 AU AU2002338898A patent/AU2002338898B2/en not_active Ceased
- 2002-05-08 CZ CZ20033355A patent/CZ20033355A3/cs unknown
- 2002-05-08 EP EP02771640A patent/EP1399448B1/en not_active Expired - Lifetime
- 2002-05-08 AT AT02771640T patent/ATE283857T1/de not_active IP Right Cessation
- 2002-05-08 CN CNB028101774A patent/CN1230436C/zh not_active Expired - Fee Related
- 2002-05-08 KR KR10-2003-7015036A patent/KR100533406B1/ko not_active IP Right Cessation
- 2002-05-08 DE DE60202147T patent/DE60202147T2/de not_active Expired - Lifetime
- 2002-05-08 SK SK1525-2003A patent/SK15252003A3/sk unknown
- 2002-05-08 JP JP2002591507A patent/JP4068466B2/ja not_active Expired - Fee Related
- 2002-05-08 IL IL15857202A patent/IL158572A0/xx unknown
- 2002-05-08 SI SI200230055T patent/SI1399448T1/xx unknown
- 2002-05-08 PT PT02771640T patent/PT1399448E/pt unknown
- 2002-05-08 YU YU90003A patent/YU90003A/sh unknown
- 2002-05-08 RU RU2003136078/04A patent/RU2287531C2/ru not_active IP Right Cessation
- 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 WO PCT/EP2002/005121 patent/WO2002094834A1/en active IP Right Grant
- 2002-05-08 HU HU0400743A patent/HUP0400743A3/hu unknown
- 2002-05-08 PL PL02366846A patent/PL366846A1/xx not_active Application Discontinuation
- 2002-05-14 JO JO200243A patent/JO2297B1/en active
- 2002-05-15 PA PA20028545201A patent/PA8545201A1/es unknown
- 2002-05-15 TW TW091110162A patent/TWI251489B/zh not_active IP Right Cessation
- 2002-05-16 AR ARP020101805A patent/AR033753A1/es not_active Application Discontinuation
- 2002-05-16 GT GT200200087A patent/GT200200087A/es unknown
- 2002-05-16 PE PE2002000413A patent/PE20030041A1/es not_active Application Discontinuation
- 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
- 2003-11-04 HR HR20030890A patent/HRP20030890A2/xx not_active Application Discontinuation
- 2003-11-14 MA MA27398A patent/MA27024A1/fr unknown
- 2003-11-17 NO NO20035104A patent/NO20035104L/no not_active Application Discontinuation
- 2003-11-17 EC EC2003004851A patent/ECSP034851A/es unknown
- 2003-11-18 BG BG108369A patent/BG108369A/bg unknown
-
2004
- 2004-12-01 HK HK04109492A patent/HK1066544A1/xx not_active IP Right Cessation
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