BR0209859A - Derivados de imidazo[1,5-a]pirimido[5-4-d][1]benzazepina como moduladores de receptores de gaba a - Google Patents
Derivados de imidazo[1,5-a]pirimido[5-4-d][1]benzazepina como moduladores de receptores de gaba aInfo
- Publication number
- BR0209859A BR0209859A BR0209859-8A BR0209859A BR0209859A BR 0209859 A BR0209859 A BR 0209859A BR 0209859 A BR0209859 A BR 0209859A BR 0209859 A BR0209859 A BR 0209859A
- Authority
- BR
- Brazil
- Prior art keywords
- gaba
- lower alkyl
- receptor modulators
- pyrimido
- imidazo
- 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
"DERIVADOS DE IMIDAZO[1,5-A]PIRIMIDO[5,4-D][1]BENZAZEPINA COMO MODULADORES DE RECEPTORES DE GABA A". A presente invenção refere-se a compostos de fórmula (I) onde R^ 1^ é halogênio ou alquila inferior; R^ 2^ é hidrogênio, alquila inferior, cicloalquila, -(CH~ 2~)~ m~-fenila, onde o anel fenila poderá ser substituído por alcóxi inferior, ou é -(CH~ 2~)~ m~-indolila; R^ 3^ é -C(O)O-alquila inferior, -C(O)OH ou um grupo heteroaromático de cinco membros, cujos anéis poderão ser substituídos por alquila inferior ou cicloalquila; n é 0, 1 ou 2; m é 0, 1 ou 2; e seus sais de adição de ácidos farmaceuticamente aceitáveis. Verificou-se que essa classe de compostos mostra alta afinidade e seletividade por sítios de ligação de receptores <244>5 de GABA A e poderia ser útil para o tratamento de aumento cognitivo ou de distúrbios cognitivos tal como doença de Alzheimer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01112222 | 2001-05-18 | ||
| PCT/EP2002/005121 WO2002094834A1 (en) | 2001-05-18 | 2002-05-08 | Imidazo [1,5-a] pyrimido [5,4-d] benzazepine derivatives as gaba a receptor modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0209859A true BR0209859A (pt) | 2004-06-15 |
Family
ID=8177471
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0209859-8A BR0209859A (pt) | 2001-05-18 | 2002-05-08 | Derivados de imidazo[1,5-a]pirimido[5-4-d][1]benzazepina como moduladores de receptores de gaba a |
Country Status (38)
| Country | Link |
|---|---|
| US (1) | US6686352B2 (pt) |
| EP (1) | EP1399448B1 (pt) |
| JP (1) | JP4068466B2 (pt) |
| KR (1) | KR100533406B1 (pt) |
| CN (1) | CN1230436C (pt) |
| AR (1) | AR033753A1 (pt) |
| AT (1) | ATE283857T1 (pt) |
| AU (1) | AU2002338898B2 (pt) |
| BG (1) | BG108369A (pt) |
| BR (1) | BR0209859A (pt) |
| CA (1) | CA2446903C (pt) |
| CZ (1) | CZ20033355A3 (pt) |
| DE (1) | DE60202147T2 (pt) |
| DK (1) | DK1399448T3 (pt) |
| EC (1) | ECSP034851A (pt) |
| ES (1) | ES2232778T3 (pt) |
| GT (1) | GT200200087A (pt) |
| HK (1) | HK1066544A1 (pt) |
| HR (1) | HRP20030890A2 (pt) |
| HU (1) | HUP0400743A3 (pt) |
| IL (2) | IL158572A0 (pt) |
| JO (1) | JO2297B1 (pt) |
| MA (1) | MA27024A1 (pt) |
| MX (1) | MXPA03010529A (pt) |
| MY (1) | MY127570A (pt) |
| NO (1) | NO20035104D0 (pt) |
| NZ (1) | NZ529097A (pt) |
| PA (1) | PA8545201A1 (pt) |
| PE (1) | PE20030041A1 (pt) |
| PL (1) | PL366846A1 (pt) |
| PT (1) | PT1399448E (pt) |
| RU (1) | RU2287531C2 (pt) |
| SI (1) | SI1399448T1 (pt) |
| SK (1) | SK15252003A3 (pt) |
| TW (1) | TWI251489B (pt) |
| WO (1) | WO2002094834A1 (pt) |
| YU (1) | YU90003A (pt) |
| ZA (1) | ZA200308544B (pt) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2540987T3 (es) | 2004-05-14 | 2015-07-15 | Millennium Pharmaceuticals, Inc. | Métodos para preparar inhibidores de la aurora cinasa |
| CA2582235A1 (en) * | 2004-10-04 | 2006-04-20 | Millennium Pharmaceuticals, Inc. | Lactam compounds useful as protein kinase inhibitors |
| EP1805184B1 (en) * | 2004-10-20 | 2013-01-09 | F. Hoffmann-La Roche AG | Imidazo-benzodiazepine derivatives |
| MX2007004640A (es) * | 2004-10-20 | 2007-06-08 | Hoffmann La Roche | Derivados de benzodiazepina sustituidos con halogeno. |
| EP1937688B1 (en) * | 2005-10-11 | 2010-08-11 | 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. |
| US8288397B2 (en) | 2007-12-17 | 2012-10-16 | Janssen Pharmaceutica Nv | Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of TRPV1 |
| 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 |
| 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 |
| RU2012140021A (ru) | 2010-02-19 | 2014-03-27 | Миллениум Фармасьютикалз, Инк. | КРИСТАЛЛИЧЕСКИЕ ФОРМЫ 4-{[9-ХЛОР-7-(2-ФТОР-6-МЕТОКСИФЕНИЛ)-5Н-ПИРИМИДО[5,4-d][2]БЕНЗАЗЕПИН-2-ИЛ]АМИНО}-2-МЕТОКСИБЕНЗОАТА НАТРИЯ |
| 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 |
| US9724354B2 (en) | 2013-03-22 | 2017-08-08 | Millennium Pharmaceuticals, Inc. | Combination of catalytic mTORC1/2 inhibitors and selective inhibitors of Aurora A kinase |
| EP3083569B1 (en) | 2013-12-20 | 2022-01-26 | 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 |
| 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 |
| US11505555B2 (en) | 2016-12-19 | 2022-11-22 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| EA202190076A1 (ru) | 2018-06-19 | 2021-09-22 | Эйджинбайо, Инк. | Производные бензодиазепина, композиции и способы лечения когнитивных нарушений |
| 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 (pt) | 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 |
| ATE236158T1 (de) | 1999-11-12 | 2003-04-15 | Neurogen Corp | Bicyclische und tricyclische heteroaromatische verbindungen |
| 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 ES ES02771640T patent/ES2232778T3/es not_active Expired - Lifetime
- 2002-05-08 BR BR0209859-8A patent/BR0209859A/pt not_active IP Right Cessation
- 2002-05-08 NZ NZ529097A patent/NZ529097A/en unknown
- 2002-05-08 PT PT02771640T patent/PT1399448E/pt unknown
- 2002-05-08 PL PL02366846A patent/PL366846A1/xx not_active Application Discontinuation
- 2002-05-08 CZ CZ20033355A patent/CZ20033355A3/cs unknown
- 2002-05-08 SI SI200230055T patent/SI1399448T1/xx unknown
- 2002-05-08 CN CNB028101774A patent/CN1230436C/zh not_active Expired - Fee Related
- 2002-05-08 CA CA002446903A patent/CA2446903C/en not_active Expired - Fee Related
- 2002-05-08 DE DE60202147T patent/DE60202147T2/de not_active Expired - Lifetime
- 2002-05-08 RU RU2003136078/04A patent/RU2287531C2/ru not_active IP Right Cessation
- 2002-05-08 AT AT02771640T patent/ATE283857T1/de not_active IP Right Cessation
- 2002-05-08 YU YU90003A patent/YU90003A/sh unknown
- 2002-05-08 MX MXPA03010529A patent/MXPA03010529A/es active IP Right Grant
- 2002-05-08 HU HU0400743A patent/HUP0400743A3/hu unknown
- 2002-05-08 KR KR10-2003-7015036A patent/KR100533406B1/ko not_active IP Right Cessation
- 2002-05-08 AU AU2002338898A patent/AU2002338898B2/en not_active Ceased
- 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 WO PCT/EP2002/005121 patent/WO2002094834A1/en active IP Right Grant
- 2002-05-08 SK SK1525-2003A patent/SK15252003A3/sk unknown
- 2002-05-08 DK DK02771640T patent/DK1399448T3/da active
- 2002-05-08 EP EP02771640A patent/EP1399448B1/en not_active Expired - Lifetime
- 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 PE PE2002000413A patent/PE20030041A1/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
- 2003-11-04 HR HR20030890A patent/HRP20030890A2/xx not_active Application Discontinuation
- 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
-
2004
- 2004-12-01 HK HK04109492A patent/HK1066544A1/xx not_active IP Right Cessation
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Legal Events
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| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 10A ANUI DADE. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: NAO APRESENTADA A GUIA DE CUMPRIMENTO DE EXIGENCIA. REFERENTE A 10A ANUIDADE. |