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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 A

Info

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
Application number
PE2002000413A
Other languages
English (en)
Inventor
Raffaello Masciadri
Andrew William Thomas
Juergen Wichmann
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 PE20030041A1 publication Critical patent/PE20030041A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic 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
    • C07D487/14Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs 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
PE2002000413A 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 PE20030041A1 (es)

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 (38)

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)
HK (1) HK1066544A1 (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) NO20035104L (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)

* Cited by examiner, † Cited by third party
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KR101748290B1 (ko) 2004-05-14 2017-06-16 밀레니엄 파머슈티컬스 인코퍼레이티드 아우로라 키나아제의 억제에 의해 유사분열 진행을 억제하기 위한 화합물 및 그 방법
CN101068815B (zh) * 2004-10-04 2012-09-05 千禧药品公司 有效作为蛋白激酶抑制剂的内酰胺化合物
KR100915469B1 (ko) * 2004-10-20 2009-09-03 에프. 호프만-라 로슈 아게 할로겐 치환된 벤조다이아제핀 유도체
NZ554439A (en) * 2004-10-20 2009-09-25 Hoffmann La Roche Imidazo-benzodiazepine derivatives
CA2625611A1 (en) * 2005-10-11 2007-04-19 F. Hoffman-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.
EP2376082B1 (en) 2008-12-22 2014-03-05 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
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
CN105209042B (zh) 2013-03-22 2019-03-08 米伦纽姆医药公司 催化性mtorc 1/2抑制剂与选择性极光a激酶抑制剂的组合
CN106068256B (zh) 2013-12-20 2020-10-23 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*衍生物、组合物和方法
IL256354B (en) 2015-06-19 2022-09-01 Agenebio Inc Benzodiazepine derivatives, compositions, and uses thereof for treating cognitive impairment
US20180207173A1 (en) 2015-07-21 2018-07-26 Millennium Pharmaceuticals, Inc. Administration of aurora kinase inhibitor and chemotherapeutic agents
US11505555B2 (en) 2016-12-19 2022-11-22 Agenebio, Inc. Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment
MX2020013927A (es) 2018-06-19 2021-03-02 Agenebio Inc Derivados de benzodiazepina, composiciones y metodos para tratar el deterioro cognitivo.
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201311B (es) 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
ES2195943T3 (es) 1999-11-12 2003-12-16 Neurogen Corp Compuestos heteroaromaticos biciclicos y triciclicos.
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
SI1399448T1 (en) 2005-02-28
BG108369A (bg) 2005-01-31
PA8545201A1 (es) 2003-02-28
YU90003A (sh) 2006-08-17
JP4068466B2 (ja) 2008-03-26
ZA200308544B (en) 2005-01-31
KR100533406B1 (ko) 2005-12-02
PT1399448E (pt) 2005-03-31
MA27024A1 (fr) 2004-12-20
NO20035104D0 (no) 2003-11-17
AU2002338898B2 (en) 2007-03-15
US20030055042A1 (en) 2003-03-20
CZ20033355A3 (en) 2004-07-14
DK1399448T3 (da) 2005-04-11
GT200200087A (es) 2003-06-19
AR033753A1 (es) 2004-01-07
BR0209859A (pt) 2004-06-15
IL158572A0 (en) 2004-05-12
US6686352B2 (en) 2004-02-03
CA2446903C (en) 2008-12-30
CN1509289A (zh) 2004-06-30
EP1399448A1 (en) 2004-03-24
NO20035104L (no) 2003-11-17
TWI251489B (en) 2006-03-21
IL158572A (en) 2010-02-17
HUP0400743A2 (hu) 2004-07-28
PL366846A1 (en) 2005-02-07
DE60202147D1 (de) 2005-01-05
HRP20030890A2 (en) 2005-08-31
AU2002338898B8 (en) 2002-12-03
MXPA03010529A (es) 2004-03-02
NZ529097A (en) 2005-04-29
SK15252003A3 (sk) 2004-08-03
MY127570A (en) 2006-12-29
ATE283857T1 (de) 2004-12-15
ES2232778T3 (es) 2005-06-01
EP1399448B1 (en) 2004-12-01
CA2446903A1 (en) 2002-11-28
HK1066544A1 (en) 2005-03-24
DE60202147T2 (de) 2005-12-01
JP2004531563A (ja) 2004-10-14
WO2002094834A1 (en) 2002-11-28
KR20040002975A (ko) 2004-01-07
HUP0400743A3 (en) 2007-09-28
RU2003136078A (ru) 2005-05-27
JO2297B1 (en) 2005-09-12
RU2287531C2 (ru) 2006-11-20
CN1230436C (zh) 2005-12-07
ECSP034851A (es) 2003-12-24

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