MXPA03010529A - Derivados de imidazol [1,5a]pirimido[5,4-d]benzazepina, como moduladores del receptor gaba a. - Google Patents
Derivados de imidazol [1,5a]pirimido[5,4-d]benzazepina, como moduladores del receptor gaba a.Info
- Publication number
- MXPA03010529A MXPA03010529A MXPA03010529A MXPA03010529A MXPA03010529A MX PA03010529 A MXPA03010529 A MX PA03010529A MX PA03010529 A MXPA03010529 A MX PA03010529A MX PA03010529 A MXPA03010529 A MX PA03010529A MX PA03010529 A MXPA03010529 A MX PA03010529A
- Authority
- MX
- Mexico
- Prior art keywords
- lower alkyl
- gaba
- pyrimido
- imidazo
- receptor modulators
- 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
- 102000004300 GABA-A Receptors Human genes 0.000 title 1
- 108090000839 GABA-A Receptors Proteins 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
La presente invencion se refiere a compuestos de formula (ver formula). en donde R1 es halogeno o alquilo inferior; R2 es hidrogeno, alquilo inferior, cicloalquilo, - (CH2)m fenilo, en donde el anillo fenilo puede estar sustituido con alcoxilo-inferior, o es - (CH2) ,-indolilo; R3 es -C(O)O-alquilo inferior, -C(O)OH, o un grupo heteroaromatico de cinco miembros, cuyos anillos pueden estar sustituidos con alquilo inferior o cicloalquilo; n es 0, 1 o 2; m es 0, 1 o 2; y sus sales de adicion acida farmaceuticamente aceptables. Se ha descubierto que esta clase de compuestos muestran una elevada afinidad y selectividad para los sitios de union del receptor (5 de GABA A y pueden ser utiles para el tratamiento de mejoras cognitivas o de trastornos cognitivos como la enfermedad 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 |
|---|---|
| MXPA03010529A true MXPA03010529A (es) | 2004-03-02 |
Family
ID=8177471
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MXPA03010529A MXPA03010529A (es) | 2001-05-18 | 2002-05-08 | Derivados de imidazol [1,5a]pirimido[5,4-d]benzazepina, como moduladores del receptor 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 (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4467616B2 (ja) | 2004-05-14 | 2010-05-26 | 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 | Ａｕｒｏｒａキナーゼの阻害により有糸分裂の進行を阻止するための化合物および方法 |
| CA2582235A1 (en) * | 2004-10-04 | 2006-04-20 | Millennium Pharmaceuticals, Inc. | Lactam compounds useful as protein kinase inhibitors |
| ES2399439T3 (es) * | 2004-10-20 | 2013-04-01 | F. Hoffmann-La Roche Ag | Derivados de imidazo-benzodiazepina |
| RU2007114763A (ru) * | 2004-10-20 | 2008-11-27 | Ф.Хоффманн-Ля Рош Аг (Ch) | Галогенозамещенные производные бензодиазепинов |
| 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. |
| WO2009078999A1 (en) | 2007-12-17 | 2009-06-25 | Janssen Pharmaceutica N.V. | 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 |
| WO2010065134A1 (en) * | 2008-12-05 | 2010-06-10 | Millennium Pharmaceuticals, Inc. | 5, 7-dihydro- 6h-pyrimido [ 5, 4-d] [ 1 ] benzazepin-6-thiones as plk inhibitors |
| BRPI0923579A2 (pt) | 2008-12-22 | 2020-01-14 | Millennium Pharm Inc | combinação de inibidores de aurora quinase e anticorpos anti-cd20 |
| JO3635B1 (ar) | 2009-05-18 | 2020-08-27 | Millennium Pharm Inc | مركبات صيدلانية صلبة وطرق لانتاجها |
| WO2011103089A1 (en) | 2010-02-19 | 2011-08-25 | Millennium Pharmaceuticals, Inc. | Crystalline forms of sodium 4-{[9-chloro-7-(2-fluoro-6--methoxyphenyl)-5h -pyrimido[5,4-d][2]benzazepin-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 |
| CA2907726A1 (en) | 2013-03-22 | 2014-09-25 | Millennium Pharmaceuticals, Inc. | Combination of catalytic mtorc1/2 inhibitors and selective inhibitors of aurora a kinase |
| CA3123897C (en) | 2013-12-20 | 2024-02-06 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| CN108026107B (zh) | 2015-06-19 | 2021-07-30 | 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 |
| 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 |
| BR112019012821A2 (pt) | 2016-12-19 | 2019-11-26 | Agenebio Inc | derivados de benzodiazepina, composições e métodos para o tratamento do comprometimento cognitivo |
| 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 (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 |
| US6166203A (en) * | 1998-02-26 | 2000-12-26 | Neurogen Corporation | Heterocyclic amino substituted heteroaryl fused pyridines; GABA brain receptor ligands |
| 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 |
| MXPA02004735A (es) | 1999-11-12 | 2003-01-28 | Orive Javier Uhthoff | Compuestos heteroaromaticos, biciclicos y triciclicos. |
| 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 SI SI200230055T patent/SI1399448T1/xx unknown
- 2002-05-08 DK DK02771640T patent/DK1399448T3/da active
- 2002-05-08 AT AT02771640T patent/ATE283857T1/de not_active IP Right Cessation
- 2002-05-08 CZ CZ20033355A patent/CZ20033355A3/cs unknown
- 2002-05-08 HR HR20030890A patent/HRP20030890A2/xx not_active Application Discontinuation
- 2002-05-08 AU AU2002338898A patent/AU2002338898B2/en not_active Ceased
- 2002-05-08 BR BR0209859-8A patent/BR0209859A/pt not_active IP Right Cessation
- 2002-05-08 CA CA002446903A patent/CA2446903C/en not_active Expired - Fee Related
- 2002-05-08 WO PCT/EP2002/005121 patent/WO2002094834A1/en not_active Ceased
- 2002-05-08 HU HU0400743A patent/HUP0400743A3/hu unknown
- 2002-05-08 JP JP2002591507A patent/JP4068466B2/ja not_active Expired - Fee Related
- 2002-05-08 KR KR10-2003-7015036A patent/KR100533406B1/ko not_active Expired - Fee Related
- 2002-05-08 PT PT02771640T patent/PT1399448E/pt unknown
- 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 EP EP02771640A patent/EP1399448B1/en not_active Expired - Lifetime
- 2002-05-08 IL IL15857202A patent/IL158572A0/xx unknown
- 2002-05-08 RU RU2003136078/04A patent/RU2287531C2/ru not_active IP Right Cessation
- 2002-05-08 DE DE60202147T patent/DE60202147T2/de not_active Expired - Lifetime
- 2002-05-08 NZ NZ529097A patent/NZ529097A/en unknown
- 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 YU YU90003A patent/YU90003A/sh unknown
- 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 PE PE2002000413A patent/PE20030041A1/es not_active Application Discontinuation
- 2002-05-16 GT GT200200087A patent/GT200200087A/es unknown
- 2002-05-16 AR ARP020101805A patent/AR033753A1/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
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| MXPA03010529A (es) | Derivados de imidazol [1,5a]pirimido[5,4-d]benzazepina, como moduladores del receptor gaba a. | |
| CA2401229A1 (en) | Aryl fused azapolycyclic compounds | |
| GC0000375A (en) | Benzodiazepine derivatives as gaba a receptor modulators | |
| CA2520898A1 (en) | Non-cross-linking pyrrolo(2,1-c)(1,4)benzodiazepines as potential antitumour agents and process thereof | |
| BG107120A (bg) | Нови бавнодействащи бетамиметици, метод за тяхното получаване и приложението им като лекарствени средства | |
| WO2005113536A3 (en) | Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands | |
| MX2007000044A (es) | Compuestos, composiciones y metodos de tetrahidroquinazolin-4(3h)- ona-relacionados y tetrahidropirido [2,3-d] pirimidin-4(3h)-ona- relacionados para su uso. | |
| CA2375670A1 (en) | 5-phenyl-pyrimidine derivatives | |
| IL190398A0 (en) | Imidazo benzodiazepine derivatives | |
| TW200630372A (en) | Imidazo-benzodiazepine derivatives | |
| TW200734328A (en) | Aryl-isoxazolo-4-yl-imidazo [1,5-a] pyridine derivatives | |
| DE602005008633D1 (de) | Imidazoä1,5aütriazoloä1,5dübenzodiazepin-derivative zur behandlung kognitiver störungen | |
| TW200631953A (en) | Tetracyclic imidazo-benzodiazepines | |
| WO2007054444A3 (en) | 3-aryl-isoxazole-4-carbonyl-benzofuran derivatives | |
| MX2007004640A (es) | Derivados de benzodiazepina sustituidos con halogeno. | |
| WO2003045940A3 (en) | Benzazepine derivatives and their use as 5-ht ligands | |
| TW200500365A (en) | Preparation of substituted quinoxalines | |
| WO2005007630A3 (en) | Aryl fused azapolycyclic compounds | |
| GB2425309A (en) | C2-fluoro pyrrolo[2,1-c][1,4]benzodiazepine dimers | |
| SE0400440D0 (sv) | Novel Cinnamic Amides | |
| SE0100297D0 (sv) | New compounds | |
| MXPA06000774A (es) | E3-nitro-pirazolo[1,5-a]pirimidinas 7-sustituidas y composiciones y metodos relacionados. | |
| SE0100295D0 (sv) | New compounds | |
| TNSN05324A1 (en) | 7-substituted 3-nitro-pyrazolo `1,5-a! pyrimidines | |
| TNSN05325A1 (en) | N-[3-(3-SUBSTITUTED-PYRAZOLO[1,5-a]PYRIMIDIN-7-YL)PHENYL]-SULFONAMIDES, AND COMPOSITIONS, AND METHODS RELATED THERETO |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |