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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
Application number
MXPA03010529A
Other languages
English (en)
Inventor
Masciadri Raffaello
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MXPA03010529A publication Critical patent/MXPA03010529A/es

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

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.
MXPA03010529A 2001-05-18 2002-05-08 Derivados de imidazol [1,5a]pirimido[5,4-d]benzazepina, como moduladores del receptor gaba a. MXPA03010529A (es)

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)

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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)

* Cited by examiner, † Cited by third party
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

Also Published As

Publication number Publication date
RU2003136078A (ru) 2005-05-27
BR0209859A (pt) 2004-06-15
AR033753A1 (es) 2004-01-07
KR100533406B1 (ko) 2005-12-02
YU90003A (sh) 2006-08-17
ECSP034851A (es) 2003-12-24
JP2004531563A (ja) 2004-10-14
TWI251489B (en) 2006-03-21
EP1399448A1 (en) 2004-03-24
AU2002338898B8 (en) 2002-12-03
IL158572A (en) 2010-02-17
CZ20033355A3 (en) 2004-07-14
IL158572A0 (en) 2004-05-12
HUP0400743A3 (en) 2007-09-28
JO2297B1 (en) 2005-09-12
PA8545201A1 (es) 2003-02-28
DE60202147D1 (de) 2005-01-05
HRP20030890A2 (en) 2005-08-31
WO2002094834A1 (en) 2002-11-28
MY127570A (en) 2006-12-29
DE60202147T2 (de) 2005-12-01
MA27024A1 (fr) 2004-12-20
GT200200087A (es) 2003-06-19
SI1399448T1 (en) 2005-02-28
AU2002338898B2 (en) 2007-03-15
HK1066544A1 (en) 2005-03-24
NO20035104L (no) 2003-11-17
HUP0400743A2 (hu) 2004-07-28
CN1509289A (zh) 2004-06-30
PE20030041A1 (es) 2003-02-07
PT1399448E (pt) 2005-03-31
NZ529097A (en) 2005-04-29
US20030055042A1 (en) 2003-03-20
NO20035104D0 (no) 2003-11-17
CA2446903A1 (en) 2002-11-28
ATE283857T1 (de) 2004-12-15
KR20040002975A (ko) 2004-01-07
ES2232778T3 (es) 2005-06-01
PL366846A1 (en) 2005-02-07
CN1230436C (zh) 2005-12-07
DK1399448T3 (da) 2005-04-11
ZA200308544B (en) 2005-01-31
RU2287531C2 (ru) 2006-11-20
BG108369A (bg) 2005-01-31
US6686352B2 (en) 2004-02-03
EP1399448B1 (en) 2004-12-01
JP4068466B2 (ja) 2008-03-26
CA2446903C (en) 2008-12-30
SK15252003A3 (sk) 2004-08-03

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