KR100533406B1 - Ｇａｂａ ａ 수용체 조절제로서의이미다조[1,5-ａ]피리미도[5,4-ｄ]벤즈아제핀 유도체 - Google Patents

Ｇａｂａ ａ 수용체 조절제로서의이미다조[1,5-ａ]피리미도[5,4-ｄ]벤즈아제핀 유도체 Download PDF

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Publication number
KR100533406B1
KR100533406B1 KR10-2003-7015036A KR20037015036A KR100533406B1 KR 100533406 B1 KR100533406 B1 KR 100533406B1 KR 20037015036 A KR20037015036 A KR 20037015036A KR 100533406 B1 KR100533406 B1 KR 100533406B1
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South Korea
Prior art keywords
benzazin
pyrimido
formula
ethyl ester
acid ethyl
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Korean (ko)
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KR20040002975A (ko
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마스시아드리라파엘로
토마스앤드류윌리암
비흐만유에르겐
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에프. 호프만-라 로슈 아게
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    • 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

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  • 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)
KR10-2003-7015036A 2001-05-18 2002-05-08 Ｇａｂａ ａ 수용체 조절제로서의이미다조[1,5-ａ]피리미도[5,4-ｄ]벤즈아제핀 유도체 Expired - Fee Related KR100533406B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP01112222 2001-05-18
EP01112222.3 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 (2)

Publication Number Publication Date
KR20040002975A KR20040002975A (ko) 2004-01-07
KR100533406B1 true KR100533406B1 (ko) 2005-12-02

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KR10-2003-7015036A Expired - Fee Related KR100533406B1 (ko) 2001-05-18 2002-05-08 Ｇａｂａ ａ 수용체 조절제로서의이미다조[1,5-ａ]피리미도[5,4-ｄ]벤즈아제핀 유도체

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US (1) US6686352B2 (https=)
EP (1) EP1399448B1 (https=)
JP (1) JP4068466B2 (https=)
KR (1) KR100533406B1 (https=)
CN (1) CN1230436C (https=)
AR (1) AR033753A1 (https=)
AT (1) ATE283857T1 (https=)
AU (1) AU2002338898B2 (https=)
BG (1) BG108369A (https=)
BR (1) BR0209859A (https=)
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DE (1) DE60202147T2 (https=)
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IL (2) IL158572A0 (https=)
JO (1) JO2297B1 (https=)
MA (1) MA27024A1 (https=)
MX (1) MXPA03010529A (https=)
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SK (1) SK15252003A3 (https=)
TW (1) TWI251489B (https=)
WO (1) WO2002094834A1 (https=)
YU (1) YU90003A (https=)
ZA (1) ZA200308544B (https=)

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AU2005243175B2 (en) 2004-05-14 2011-12-01 Millennium Pharmaceuticals, Inc. Compounds and methods for inhibiting mitotic progression by inhibition 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
AU2005299031B2 (en) 2004-10-20 2011-11-10 F. Hoffmann-La Roche Ag Halogen substituted benzodiazepine derivatives
MX2007004639A (es) * 2004-10-20 2007-06-08 Hoffmann La Roche Derivados de imidazo-benzodiazepina.
BRPI0617204A2 (pt) 2005-10-11 2011-07-19 Hoffmann La Roche derivados de imidazo benzodiazepina
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
JP5684719B2 (ja) * 2008-12-05 2015-03-18 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． Ｐｌｋ阻害剤としての５，７−ジヒドロ−６ｈ−ピリミド［５、−４ｄ］［１］ベンゾアゼピン−６−チオン
RU2535032C2 (ru) 2008-12-22 2014-12-10 Милленниум Фармасьютикалз, Инк. Сочетание ингибиторов аврора киназы и анти-cd 20 антител
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
WO2014153509A1 (en) 2013-03-22 2014-09-25 Millennium Pharmaceuticals, Inc. Combination of catalytic mtorc 1/2 inhibitors and selective inhibitors of aurora a kinase
NZ760341A (en) * 2013-12-20 2021-12-24 Agenebio Inc Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment
MX392119B (es) 2015-06-19 2025-03-11 Agenebio Inc Derivados de benzodiazepina, composiciones y metodos para tratar deterioro cognitivo
WO2017015316A1 (en) 2015-07-21 2017-01-26 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
US20180170941A1 (en) 2016-12-19 2018-06-21 Agenebio, Inc. Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment
CN112601749B (zh) 2018-06-19 2024-03-26 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
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

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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 (https=) 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
CA2388593A1 (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

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Publication number Publication date
DE60202147D1 (de) 2005-01-05
HRP20030890A2 (en) 2005-08-31
WO2002094834A1 (en) 2002-11-28
PL366846A1 (en) 2005-02-07
EP1399448B1 (en) 2004-12-01
JP4068466B2 (ja) 2008-03-26
RU2003136078A (ru) 2005-05-27
CN1509289A (zh) 2004-06-30
ECSP034851A (es) 2003-12-24
ZA200308544B (en) 2005-01-31
MXPA03010529A (es) 2004-03-02
NZ529097A (en) 2005-04-29
SK15252003A3 (sk) 2004-08-03
ATE283857T1 (de) 2004-12-15
PE20030041A1 (es) 2003-02-07
PA8545201A1 (es) 2003-02-28
NO20035104D0 (no) 2003-11-17
HK1066544A1 (en) 2005-03-24
BG108369A (bg) 2005-01-31
IL158572A0 (en) 2004-05-12
AR033753A1 (es) 2004-01-07
CZ20033355A3 (en) 2004-07-14
PT1399448E (pt) 2005-03-31
HUP0400743A2 (hu) 2004-07-28
BR0209859A (pt) 2004-06-15
US6686352B2 (en) 2004-02-03
US20030055042A1 (en) 2003-03-20
DK1399448T3 (da) 2005-04-11
GT200200087A (es) 2003-06-19
AU2002338898B8 (en) 2002-12-03
ES2232778T3 (es) 2005-06-01
EP1399448A1 (en) 2004-03-24
SI1399448T1 (en) 2005-02-28
KR20040002975A (ko) 2004-01-07
YU90003A (sh) 2006-08-17
NO20035104L (no) 2003-11-17
AU2002338898B2 (en) 2007-03-15
DE60202147T2 (de) 2005-12-01
CA2446903A1 (en) 2002-11-28
JO2297B1 (en) 2005-09-12
CN1230436C (zh) 2005-12-07
RU2287531C2 (ru) 2006-11-20
CA2446903C (en) 2008-12-30
JP2004531563A (ja) 2004-10-14
IL158572A (en) 2010-02-17
HUP0400743A3 (en) 2007-09-28
TWI251489B (en) 2006-03-21
MY127570A (en) 2006-12-29
MA27024A1 (fr) 2004-12-20

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