HUP0400743A2 - Imidazo[1,5-a]pirimido[5,4-d]benzazepin-származékok, eljárás előállításukra és az ezeket tartalmazó gyógyszerkészítmények - Google Patents
Imidazo[1,5-a]pirimido[5,4-d]benzazepin-származékok, eljárás előállításukra és az ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0400743A2 HUP0400743A2 HU0400743A HUP0400743A HUP0400743A2 HU P0400743 A2 HUP0400743 A2 HU P0400743A2 HU 0400743 A HU0400743 A HU 0400743A HU P0400743 A HUP0400743 A HU P0400743A HU P0400743 A2 HUP0400743 A2 HU P0400743A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- lower alkyl
- pyrimido
- imidazo
- preparation
- Prior art date
Links
- RZBORXKBSMHCCE-UHFFFAOYSA-N 2,4,10,12-tetrazatetracyclo[12.4.0.02,6.08,13]octadeca-1(18),4,6,8,10,12,14,16-octaene Chemical class C=1C2=CN=CN=C2C2=CC=CC=C2N2CN=CC2=1 RZBORXKBSMHCCE-UHFFFAOYSA-N 0.000 title 1
- 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
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 230000001149 cognitive effect 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
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 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
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000000021 stimulant Substances 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
A találmány az (I) általános képletű vegyületekre[mely képletben Rljelentése halogénatom vagy kis szénatomszámú alkilcsoport; R2jelentése hidrogénatom-, kis szénatomszámú alkilcsoport,cikloalkilcsoport, -(CH2)m-fenil-csoport - ahol a fenilgyűrű adottesetben kis szénatomszámú alkoxicsoporttal helyettesítve lehet - vagy-(CH2)m-indolil-csoport; R3 jelentése -C(O)O- kis szénatomszámú alkil,-C(O)-OH, vagy 5-tagú heteroaromás-csoport, amely gyűrű kisszénatomszámú alkil- vagy cikloalkil-csoporttal helyettesítve lehet; nértéke 0, 1 vagy 2; m értéke 0, 1 vagy 2] és gyógyászatilag alkalmassavaddíciós sóikra vonatkozik. Azt találták, hogy a találmány szerintivegyületek a GABA A a5 receptor kötődési helyekhez nagyfokú affinitástés szelektivitást mutatnak és ezért kognitív serkentőként vagykognitív rendellenességek (pl. Alzheimer-betegség) kezelésérealkalmazhatók. Ó
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 (2)
| Publication Number | Publication Date |
|---|---|
| HUP0400743A2 true HUP0400743A2 (hu) | 2004-07-28 |
| HUP0400743A3 HUP0400743A3 (en) | 2007-09-28 |
Family
ID=8177471
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0400743A HUP0400743A3 (en) | 2001-05-18 | 2002-05-08 | Imidazo[1,5-a]pyrimido[5,4-d]benzazepine derivatives, process for their preparation and pharmaceutical conpositions containing them |
Country Status (38)
| Country | Link |
|---|---|
| US (1) | US6686352B2 (hu) |
| EP (1) | EP1399448B1 (hu) |
| JP (1) | JP4068466B2 (hu) |
| KR (1) | KR100533406B1 (hu) |
| CN (1) | CN1230436C (hu) |
| AR (1) | AR033753A1 (hu) |
| AT (1) | ATE283857T1 (hu) |
| AU (1) | AU2002338898B2 (hu) |
| BG (1) | BG108369A (hu) |
| BR (1) | BR0209859A (hu) |
| CA (1) | CA2446903C (hu) |
| CZ (1) | CZ20033355A3 (hu) |
| DE (1) | DE60202147T2 (hu) |
| DK (1) | DK1399448T3 (hu) |
| EC (1) | ECSP034851A (hu) |
| ES (1) | ES2232778T3 (hu) |
| GT (1) | GT200200087A (hu) |
| HK (1) | HK1066544A1 (hu) |
| HR (1) | HRP20030890A2 (hu) |
| HU (1) | HUP0400743A3 (hu) |
| IL (2) | IL158572A0 (hu) |
| JO (1) | JO2297B1 (hu) |
| MA (1) | MA27024A1 (hu) |
| MX (1) | MXPA03010529A (hu) |
| MY (1) | MY127570A (hu) |
| NO (1) | NO20035104L (hu) |
| NZ (1) | NZ529097A (hu) |
| PA (1) | PA8545201A1 (hu) |
| PE (1) | PE20030041A1 (hu) |
| PL (1) | PL366846A1 (hu) |
| PT (1) | PT1399448E (hu) |
| RU (1) | RU2287531C2 (hu) |
| SI (1) | SI1399448T1 (hu) |
| SK (1) | SK15252003A3 (hu) |
| TW (1) | TWI251489B (hu) |
| WO (1) | WO2002094834A1 (hu) |
| YU (1) | YU90003A (hu) |
| ZA (1) | ZA200308544B (hu) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7572784B2 (en) | 2004-05-14 | 2009-08-11 | Millennium Pharmaceuticals, Inc. | Compounds and methods for inhibiting mitotic progression |
| CA2582235A1 (en) * | 2004-10-04 | 2006-04-20 | Millennium Pharmaceuticals, Inc. | Lactam compounds useful as protein kinase inhibitors |
| RU2007112940A (ru) * | 2004-10-20 | 2008-11-27 | Ф.Хоффманн-Ля Рош Аг (Ch) | Производные имидазобензодиазепина |
| 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 |
| 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. |
| 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 |
| TW201026703A (en) | 2008-12-05 | 2010-07-16 | Millennium Pharm Inc | Thiolactams and uses thereof |
| RU2535032C2 (ru) | 2008-12-22 | 2014-12-10 | Милленниум Фармасьютикалз, Инк. | Сочетание ингибиторов аврора киназы и анти-cd 20 антител |
| JO3635B1 (ar) | 2009-05-18 | 2020-08-27 | Millennium Pharm Inc | مركبات صيدلانية صلبة وطرق لانتاجها |
| EP2536279A4 (en) | 2010-02-19 | 2013-07-24 | Millennium Pharm Inc | CRYSTALLINE FORMS OF SODIUM 4 - {[9-CHLORO-7- (2-FLUORO-6-METHOXYPHENYL) -5H-PYRIMIDO [5,4-D] [2] BENZAZEPHIN-2YL] AMINO} -2-METHOXYBENZOATE |
| 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 |
| EP2976086B1 (en) | 2013-03-22 | 2020-10-14 | Millennium Pharmaceuticals, Inc. | Combination of catalytic mtorc 1/2 inhibitors and selective inhibitors of aurora a kinase |
| JP6883988B2 (ja) | 2013-12-20 | 2021-06-09 | エージンバイオ， インコーポレイテッド | ベンゾジアゼピン誘導体、組成物、および認知障害を処置するための方法 |
| IL256354B (en) | 2015-06-19 | 2022-09-01 | Agenebio Inc | History of benzodiazepines, preparations and their use for the treatment of cognitive impairment |
| 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 (hu) | 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 RU RU2003136078/04A patent/RU2287531C2/ru not_active IP Right Cessation
- 2002-05-08 ES ES02771640T patent/ES2232778T3/es not_active Expired - Lifetime
- 2002-05-08 SK SK1525-2003A patent/SK15252003A3/sk unknown
- 2002-05-08 MX MXPA03010529A patent/MXPA03010529A/es active IP Right Grant
- 2002-05-08 IL IL15857202A patent/IL158572A0/xx unknown
- 2002-05-08 EP EP02771640A patent/EP1399448B1/en not_active Expired - Lifetime
- 2002-05-08 PL PL02366846A patent/PL366846A1/xx not_active Application Discontinuation
- 2002-05-08 KR KR10-2003-7015036A patent/KR100533406B1/ko not_active IP Right Cessation
- 2002-05-08 JP JP2002591507A patent/JP4068466B2/ja not_active Expired - Fee Related
- 2002-05-08 YU YU90003A patent/YU90003A/sh unknown
- 2002-05-08 DK DK02771640T patent/DK1399448T3/da active
- 2002-05-08 HU HU0400743A patent/HUP0400743A3/hu unknown
- 2002-05-08 AT AT02771640T patent/ATE283857T1/de not_active IP Right Cessation
- 2002-05-08 DE DE60202147T patent/DE60202147T2/de 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 AU AU2002338898A patent/AU2002338898B2/en not_active Ceased
- 2002-05-08 CA CA002446903A patent/CA2446903C/en not_active Expired - Fee Related
- 2002-05-08 CZ CZ20033355A patent/CZ20033355A3/cs unknown
- 2002-05-08 WO PCT/EP2002/005121 patent/WO2002094834A1/en active IP Right Grant
- 2002-05-08 CN CNB028101774A patent/CN1230436C/zh not_active Expired - Fee Related
- 2002-05-08 SI SI200230055T patent/SI1399448T1/xx 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 GT GT200200087A patent/GT200200087A/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
- 2002-05-17 MY MYPI20021808A patent/MY127570A/en unknown
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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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| FD9A | Lapse of provisional protection due to non-payment of fees |