PE20030041A1 - DERIVADOS DE IMIDAZO [1,5-a]PIRIMIDO[5,4-d]BENZAZEPINA COMO LIGANDOS DE RECEPTORES SUBUNIDAD O5 DE GABA A - Google Patents
DERIVADOS DE IMIDAZO [1,5-a]PIRIMIDO[5,4-d]BENZAZEPINA COMO LIGANDOS DE RECEPTORES SUBUNIDAD O5 DE GABA AInfo
- Publication number
- PE20030041A1 PE20030041A1 PE2002000413A PE2002000413A PE20030041A1 PE 20030041 A1 PE20030041 A1 PE 20030041A1 PE 2002000413 A PE2002000413 A PE 2002000413A PE 2002000413 A PE2002000413 A PE 2002000413A PE 20030041 A1 PE20030041 A1 PE 20030041A1
- Authority
- PE
- Peru
- Prior art keywords
- imidazo
- benzazepine
- ethyl ester
- carboxyl acid
- alkyl
- Prior art date
Links
- DQFQCHIDRBIESA-UHFFFAOYSA-N 1-benzazepine Chemical compound N1C=CC=CC2=CC=CC=C12 DQFQCHIDRBIESA-UHFFFAOYSA-N 0.000 title 1
- 229960003692 gamma aminobutyric acid Drugs 0.000 title 1
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 title 1
- 239000003446 ligand Substances 0.000 title 1
- 239000002253 acid Substances 0.000 abstract 5
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical class CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 abstract 4
- -1 COMPOUNDS ETHYL ESTER Chemical class 0.000 abstract 2
- 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 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 230000007370 cognitive improvement Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- 125000000896 monocarboxylic acid group Chemical group 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
SE REFIERE A DERIVADOS DE IMIDAZO [1,5-a]PIRIMIDO[5,4-d]BENZAZEPINA DE FORMULA I DONDE R1 ES HALOGENO, ALQUILO; R2 ES H, ALQUILO, CICLOALQUILO, -(CH2)m-FENILO, -(CH2)m-INDOLILO; R3 ES COO-ALQUILO, COOH, GRUPO HETEROAROMATICO DE 5 MIEMBROS OPCIONALMENTE SUSTITUIDOS CON ALQUILO, CICLOALQUILO; n Y m SON 0-2; SON COMPUESTOS PREFERIDOS ESTER ETILICO DEL ACIDO 9H-IMIDAZO[1,5-a]PIRIMIDO[5,4-d][1]BENZAZEPINA-10-CARBOXILICO; ESTER ETILICO DEL ACIDO 6-PROPIL-9H-IMIDAZO[1,5-a]PIRIMIDO[5,4-d][1]-BENZAZEPINA-10-CARBOXILICO; ESTER ETILICO DEL ACIDO 6-(1-METILETIL)-9H-IMIDAZO[1,5-a]PIRIMIDO[5,4-d][1]BENZAZEPIN-10-CARBOXILICO; ESTER ETILICO DEL ACIDO 6-CICLOPROPIL-9H-IMIDAZO[1,5-a]PIRIMIDO[5,4-d][1]BENZAZEPINA-10-CARBOXILICO; ESTER ETILICO DEL ACIDO 6-[(4-METOXIFENIL)METIL]-9H-IMIDAZO[1,5-a]PIRIMIDO[5,4-d][1]BENZAZEPINA-10-CARBOXILICO; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCESO PARA LA PREPARACION. LOS COMPUESTOS SON AGONISTAS DE LOS RECEPTORES SUBUNIDAD O5 DE GABA A Y PUEDEN SER UTILES PARA MEJORA COGNITIVA Y TRATAMIENTO DE ENFERMEDAD DE ALZHEIMER
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01112222 | 2001-05-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20030041A1 true PE20030041A1 (es) | 2003-02-07 |
Family
ID=8177471
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2002000413A PE20030041A1 (es) | 2001-05-18 | 2002-05-16 | DERIVADOS DE IMIDAZO [1,5-a]PIRIMIDO[5,4-d]BENZAZEPINA COMO LIGANDOS DE RECEPTORES SUBUNIDAD O5 DE GABA A |
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 |
|---|---|---|---|---|
| NZ551370A (en) | 2004-05-14 | 2009-08-28 | Millennium Pharm Inc | Compounds and methods for inhibiting mitotic progression by inhibiting of aurora kinase |
| CN102766142A (zh) * | 2004-10-04 | 2012-11-07 | 千禧药品公司 | 有效作为蛋白激酶抑制剂的内酰胺化合物 |
| MX2007004640A (es) * | 2004-10-20 | 2007-06-08 | Hoffmann La Roche | Derivados de benzodiazepina sustituidos con halogeno. |
| BRPI0519991A2 (pt) * | 2004-10-20 | 2009-04-07 | Hoffmann La Roche | derivados de imidazo-benzodiazepina |
| WO2007042421A1 (en) | 2005-10-11 | 2007-04-19 | 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 |
| AR074487A1 (es) | 2008-12-05 | 2011-01-19 | Millennium Pharm Inc | Tiolactamas inhibidoras de proteinquinasas plk, composiciones farmaceuticas que las contienen y usos de las mismas para el tratamiento de trastornos proliferativos e inflamatorios, en particular cancer. |
| CA2747326C (en) | 2008-12-22 | 2017-05-16 | 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 |
| BR112012020557A8 (pt) | 2010-02-19 | 2018-01-02 | Millennium Pharm Inc | formas cristalinas de 4-{[9-cloro-7-(2-flúor-6-metoifenil)-5h-pirimido[5,4-d][2]benzazepin-2-il]amino}-2-metoxibenzoato de sódio |
| 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 |
| CA2907726A1 (en) | 2013-03-22 | 2014-09-25 | Millennium Pharmaceuticals, Inc. | Combination of catalytic mtorc1/2 inhibitors and selective inhibitors of aurora a kinase |
| MX381561B (es) * | 2013-12-20 | 2025-03-12 | Agenebio Inc | Derivados de benzodiazepina, composiciones, y métodos para tratar el deterioro cognitivo. |
| CN113264939A (zh) | 2015-06-19 | 2021-08-17 | 艾吉因生物股份有限公司 | 用于治疗认知损害的苯并二氮杂环庚三烯衍生物、组合物和方法 |
| US20180207173A1 (en) | 2015-07-21 | 2018-07-26 | Millennium Pharmaceuticals, Inc. | Administration of aurora kinase inhibitor and chemotherapeutic agents |
| BR112019012821A2 (pt) | 2016-12-19 | 2019-11-26 | Agenebio, Inc. | derivados de benzodiazepina, composições e métodos para o tratamento do comprometimento cognitivo |
| US20180170941A1 (en) | 2016-12-19 | 2018-06-21 | 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 (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 |
| WO2001034603A2 (en) | 1999-11-12 | 2001-05-17 | 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 DK DK02771640T patent/DK1399448T3/da active
- 2002-05-08 AU AU2002338898A patent/AU2002338898B2/en not_active Ceased
- 2002-05-08 PL PL02366846A patent/PL366846A1/xx not_active Application Discontinuation
- 2002-05-08 NZ NZ529097A patent/NZ529097A/en unknown
- 2002-05-08 CN CNB028101774A patent/CN1230436C/zh not_active Expired - Fee Related
- 2002-05-08 YU YU90003A patent/YU90003A/sh unknown
- 2002-05-08 PT PT02771640T patent/PT1399448E/pt unknown
- 2002-05-08 WO PCT/EP2002/005121 patent/WO2002094834A1/en not_active Ceased
- 2002-05-08 IL IL15857202A patent/IL158572A0/xx unknown
- 2002-05-08 CA CA002446903A patent/CA2446903C/en not_active Expired - Fee Related
- 2002-05-08 MX MXPA03010529A patent/MXPA03010529A/es active IP Right Grant
- 2002-05-08 BR BR0209859-8A patent/BR0209859A/pt not_active IP Right Cessation
- 2002-05-08 JP JP2002591507A patent/JP4068466B2/ja not_active Expired - Fee Related
- 2002-05-08 HU HU0400743A patent/HUP0400743A3/hu unknown
- 2002-05-08 SK SK1525-2003A patent/SK15252003A3/sk unknown
- 2002-05-08 EP EP02771640A patent/EP1399448B1/en not_active Expired - Lifetime
- 2002-05-08 SI SI200230055T patent/SI1399448T1/xx unknown
- 2002-05-08 CZ CZ20033355A patent/CZ20033355A3/cs unknown
- 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 HR HR20030890A patent/HRP20030890A2/xx not_active Application Discontinuation
- 2002-05-08 DE DE60202147T patent/DE60202147T2/de not_active Expired - Lifetime
- 2002-05-08 KR KR10-2003-7015036A patent/KR100533406B1/ko not_active Expired - Fee Related
- 2002-05-08 ES ES02771640T patent/ES2232778T3/es not_active Expired - Lifetime
- 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 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
- 2003-11-14 MA MA27398A patent/MA27024A1/fr unknown
- 2003-11-17 NO NO20035104A patent/NO20035104D0/no not_active Application Discontinuation
- 2003-11-17 EC EC2003004851A patent/ECSP034851A/es unknown
- 2003-11-18 BG BG108369A patent/BG108369A/bg unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |