YU90003A - Derivati imidazo/1,5-a/pirimido/5,4-d//1/benzazepina kao modulatori gaba a raceptora - Google Patents
Derivati imidazo/1,5-a/pirimido/5,4-d//1/benzazepina kao modulatori gaba a raceptoraInfo
- Publication number
- YU90003A YU90003A YU90003A YUP90003A YU90003A YU 90003 A YU90003 A YU 90003A YU 90003 A YU90003 A YU 90003A YU P90003 A YUP90003 A YU P90003A YU 90003 A YU90003 A YU 90003A
- Authority
- YU
- Yugoslavia
- Prior art keywords
- lower alkyl
- gaba
- pyrimido
- imidazo
- receptor modulators
- Prior art date
Links
- 102000004300 GABA-A Receptors Human genes 0.000 title 1
- 108090000839 GABA-A Receptors Proteins 0.000 title 1
- 150000008038 benzoazepines Chemical class 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
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 239000002475 cognitive enhancer Substances 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 group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 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
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
Predmetni pronalazak se odnosi na jedinjenja formule (I), naznačena time što R1 predstavlja halogen ili niži alkil; R2 je vodonik, niži alkil, cikloalkil, -(CH2)m-fenil, pri čemu fenilni prsten može biti supstituisan nižom alkoksi grupom ili je -(CH2)m-indolil; R3 je C(O)O-niži alkil, -C(O)OH, ili neka petočlana heteroaromatična grupa, čiji prstenovi mogu biti supstituisani nižom alkil ili cikloalkil grupom; n je 0, 1 ili 2; m je 0, 1 ili 2; i na njihove farmaceutski prihvatljive adicione soli. Utvrdjeno da je ova klasa jedinjenja pokazuje visok afinitet i selektivnost prema GABA A α5 receptornim vezujućim mestima i da se može primeniti u terapiji kognitivnih poremećaja kao što je Alchajmerova bolest.[The present invention relates to compounds of formula (I) wherein R1 is halogen or lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, -(CH2)m-phenyl, wherein the phenyl ring may be substituted by lower alkoxy, or is (CH2)m-indolyl; R3 is C(O)O-lower alkyl, -C(O)OH, or a five membered heteroaromatic group, which rings may be substituted by lower alkyl or cycloalkyl; n is 0, 1 or 2 ; m is 0, 1 or 2 ; and their pharmaceutically acceptable acid addition salts. It has been found that this class of compounds show high affinity and selectivity for GABA A α5 receptor binding sites and might be useful for the treatment of cognitive enhancer or of cognitive disorders like Alzheimer's disease.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01112222 | 2001-05-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| YU90003A true YU90003A (sh) | 2006-08-17 |
Family
ID=8177471
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| YU90003A YU90003A (sh) | 2001-05-18 | 2002-05-08 | Derivati imidazo/1,5-a/pirimido/5,4-d//1/benzazepina kao modulatori gaba a raceptora |
Country Status (37)
| Country | Link |
|---|---|
| US (1) | US6686352B2 (sh) |
| EP (1) | EP1399448B1 (sh) |
| JP (1) | JP4068466B2 (sh) |
| KR (1) | KR100533406B1 (sh) |
| CN (1) | CN1230436C (sh) |
| AR (1) | AR033753A1 (sh) |
| AT (1) | ATE283857T1 (sh) |
| AU (1) | AU2002338898B2 (sh) |
| BG (1) | BG108369A (sh) |
| BR (1) | BR0209859A (sh) |
| CA (1) | CA2446903C (sh) |
| CZ (1) | CZ20033355A3 (sh) |
| DE (1) | DE60202147T2 (sh) |
| DK (1) | DK1399448T3 (sh) |
| EC (1) | ECSP034851A (sh) |
| ES (1) | ES2232778T3 (sh) |
| GT (1) | GT200200087A (sh) |
| HR (1) | HRP20030890A2 (sh) |
| HU (1) | HUP0400743A3 (sh) |
| IL (2) | IL158572A0 (sh) |
| JO (1) | JO2297B1 (sh) |
| MA (1) | MA27024A1 (sh) |
| MX (1) | MXPA03010529A (sh) |
| MY (1) | MY127570A (sh) |
| NO (1) | NO20035104D0 (sh) |
| NZ (1) | NZ529097A (sh) |
| PA (1) | PA8545201A1 (sh) |
| PE (1) | PE20030041A1 (sh) |
| PL (1) | PL366846A1 (sh) |
| PT (1) | PT1399448E (sh) |
| RU (1) | RU2287531C2 (sh) |
| SI (1) | SI1399448T1 (sh) |
| SK (1) | SK15252003A3 (sh) |
| TW (1) | TWI251489B (sh) |
| WO (1) | WO2002094834A1 (sh) |
| YU (1) | YU90003A (sh) |
| ZA (1) | ZA200308544B (sh) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1905773E (pt) | 2004-05-14 | 2012-10-25 | Millennium Pharm Inc | Compostos e métodos para inibir a progressão mitótica por inibição da quinase aurora |
| JP5002460B2 (ja) * | 2004-10-04 | 2012-08-15 | 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 | タンパク質キナーゼインヒビターとして有用なラクタム化合物 |
| NZ554439A (en) * | 2004-10-20 | 2009-09-25 | Hoffmann La Roche | Imidazo-benzodiazepine derivatives |
| AU2005299031B2 (en) * | 2004-10-20 | 2011-11-10 | F. Hoffmann-La Roche Ag | Halogen substituted benzodiazepine derivatives |
| ATE477255T1 (de) | 2005-10-11 | 2010-08-15 | Hoffmann La Roche | Imidazobenzdiazepinderivate |
| 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. |
| PE20091102A1 (es) | 2007-12-17 | 2009-07-25 | Janssen Pharmaceutica Nv | Moduladores imidazolo-, oxazolo-, y tiazolopirimidina del 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 |
| US7998952B2 (en) | 2008-12-05 | 2011-08-16 | Millennium Pharmaceuticals, Inc. | Thiolactams and uses thereof |
| KR101741168B1 (ko) | 2008-12-22 | 2017-05-29 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 오로라 키나아제 억제제 및 항ｃｄ 항체의 병용 |
| JO3635B1 (ar) | 2009-05-18 | 2020-08-27 | Millennium Pharm Inc | مركبات صيدلانية صلبة وطرق لانتاجها |
| CN104031049A (zh) | 2010-02-19 | 2014-09-10 | 米伦纽姆医药公司 | 极光激酶抑制剂的结晶形式 |
| 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 |
| US9724354B2 (en) | 2013-03-22 | 2017-08-08 | Millennium Pharmaceuticals, Inc. | Combination of catalytic mTORC1/2 inhibitors and selective inhibitors of Aurora A kinase |
| MX391314B (es) * | 2013-12-20 | 2025-03-21 | Agenebio Inc | Derivados de benzodiazepina, composiciones, y metodos para tratar el deterioro cognitivo. |
| MX392119B (es) | 2015-06-19 | 2025-03-11 | Agenebio Inc | Derivados de benzodiazepina, composiciones y metodos para tratar deterioro cognitivo |
| 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 |
| 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 (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 (sh) | 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 |
| AU1481701A (en) | 1999-11-12 | 2001-06-06 | 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 |
-
2002
- 2002-04-09 US US10/118,584 patent/US6686352B2/en not_active Expired - Fee Related
- 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 IL IL15857202A patent/IL158572A0/xx unknown
- 2002-05-08 DE DE60202147T patent/DE60202147T2/de not_active Expired - Lifetime
- 2002-05-08 WO PCT/EP2002/005121 patent/WO2002094834A1/en active IP Right Grant
- 2002-05-08 EP EP02771640A patent/EP1399448B1/en not_active Expired - Lifetime
- 2002-05-08 ES ES02771640T patent/ES2232778T3/es not_active Expired - Lifetime
- 2002-05-08 MX MXPA03010529A patent/MXPA03010529A/es active IP Right Grant
- 2002-05-08 KR KR10-2003-7015036A patent/KR100533406B1/ko not_active Expired - Fee Related
- 2002-05-08 PL PL02366846A patent/PL366846A1/xx not_active Application Discontinuation
- 2002-05-08 CN CNB028101774A patent/CN1230436C/zh not_active Expired - Fee Related
- 2002-05-08 NZ NZ529097A patent/NZ529097A/en unknown
- 2002-05-08 HR HR20030890A patent/HRP20030890A2/xx not_active Application Discontinuation
- 2002-05-08 CZ CZ20033355A patent/CZ20033355A3/cs unknown
- 2002-05-08 PT PT02771640T patent/PT1399448E/pt unknown
- 2002-05-08 DK DK02771640T patent/DK1399448T3/da active
- 2002-05-08 SK SK1525-2003A patent/SK15252003A3/sk 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 SI SI200230055T patent/SI1399448T1/xx unknown
- 2002-05-08 RU RU2003136078/04A patent/RU2287531C2/ru not_active IP Right Cessation
- 2002-05-08 HU HU0400743A patent/HUP0400743A3/hu unknown
- 2002-05-08 BR BR0209859-8A patent/BR0209859A/pt not_active IP Right Cessation
- 2002-05-08 AT AT02771640T patent/ATE283857T1/de not_active IP Right Cessation
- 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 GT GT200200087A patent/GT200200087A/es unknown
- 2002-05-16 AR ARP020101805A patent/AR033753A1/es not_active Application Discontinuation
- 2002-05-16 PE PE2002000413A patent/PE20030041A1/es not_active Application Discontinuation
- 2002-05-17 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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