YU35603A - Derivati benzodiazepina kao modulatori gaba a receptora - Google Patents

Derivati benzodiazepina kao modulatori gaba a receptora

Info

Publication number
YU35603A
YU35603A YU35603A YUP35603A YU35603A YU 35603 A YU35603 A YU 35603A YU 35603 A YU35603 A YU 35603A YU P35603 A YUP35603 A YU P35603A YU 35603 A YU35603 A YU 35603A
Authority
YU
Yugoslavia
Prior art keywords
lower alkyl
halogen
gaba
hydrogen
phenyl
Prior art date
Application number
YU35603A
Other languages
English (en)
Inventor
Raffaello Masciadri
Andrew William Thomas
Juergen Wichmann
Original Assignee
F. Hoffmann-La Roche Ag.
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 F. Hoffmann-La Roche Ag. filed Critical F. Hoffmann-La Roche Ag.
Publication of YU35603A publication Critical patent/YU35603A/sh

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
    • 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Ovaj pronalazak se odnosi na jedinjenja formule (I) u kojoj R1 oznacava vodonik, halogen, nizi alkil, nizi alkoksi, hidroksi, cijan, trifluorometil, trifluorometoksi ili nizi alkiltio, R2 oznacava -C(O)O-nizi alkil, izoksazol, 1,2,4-oksadiazol-3-il ili 1,2,4-oksadiazol-5-il, koji prstenovi mogu biti supstituisani nizim alkilom, trifluormetilom ili cikloalkilom, R3 oznacava vodonik, nizi alkil, -(CH2)n-cikloalkil, -(CH2)n-halogen, -(CH2)n-piridin-4-il ili -(CH2)n-fenil, pri cemu fenil- prsten moze biti supstituisan sa jednim ili dva supstituenta koji su odabrani iz grupe koja se sastoji od nize alkoksi-grupe, halogena, -SO2CH3, fenila, -OCF3, nitro-grupe, -CF3, -NR2 ili oznacava -(CH2)n-indolil, koji je opciono supstituisan nizim alkilom ili nizom alkoksi-grupom, ili oznacava pirolidinil-5-okso, -C(O)-NR2, -(CH2)n-OH, -(CH2)n-NR2 ili -(CH2)n-benzo[1,3]dioksol, R oznacava vodonik ili nizi alkil i n je 0, 1, 2 ili 3, i na njihove farmaceutski prihvatljive kiselinske adicione soli uz izuzetak sledecih jedinjenja: etil-9H-imidazol[1,5-a][1,2,4]triazolo[3,4-d][1,4]enzodiazepin-10-karboksilata, 10-(3-ciklopropil-1,2,4-oksadiazol-5-il)-9H-imidazo[1,5-a][1,2,4]triazolo[4,3-d][1,4]benzodiazepina, etil-3-fluor-9H-imidazol[1,5-a][1,2,4]triazolo[3,4-d][1,4]benzodiazepin-10-karboksilata, 10-(3-ciklopropil-1,2,4-oksadiazol-5-il)-3-fluor-9H-imidazo[1,5-a][1,2,4]triazolo[3,4-d][1,4]benzodiazepina, etil-3-hlor-9H-imidazol[1,5-a][1,2,4]triazolo[3,4-d][1,4]benzodiazepin-10-karboksilata i 3-hlor-10-(3-ciklopriopil-1,2,4-oksadiazol-5-il)-9Himidazo[1,5-a][1,2,4]triazolo[3,4-d][1,4]benzodiazepina. Ova jedinjenja imaju dobar afinitet prema GABA α5 receptoru i ona su otuda korisna za lecenje bolesti koje su u vezi sa ovim receptorom.
YU35603A 2000-11-16 2001-11-08 Derivati benzodiazepina kao modulatori gaba a receptora YU35603A (sh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP00124332 2000-11-16

Publications (1)

Publication Number Publication Date
YU35603A true YU35603A (sh) 2006-05-25

Family

ID=8170315

Family Applications (1)

Application Number Title Priority Date Filing Date
YU35603A YU35603A (sh) 2000-11-16 2001-11-08 Derivati benzodiazepina kao modulatori gaba a receptora

Country Status (41)

Country Link
US (1) US6743789B2 (sh)
EP (1) EP1337535B1 (sh)
JP (1) JP4088151B2 (sh)
KR (1) KR100504300B1 (sh)
CN (1) CN1191255C (sh)
AR (1) AR031345A1 (sh)
AT (1) ATE268776T1 (sh)
AU (2) AU2002217007B2 (sh)
BG (1) BG107817A (sh)
BR (1) BR0115393A (sh)
CA (1) CA2427576C (sh)
CZ (1) CZ295256B6 (sh)
DE (1) DE60103776T2 (sh)
DK (1) DK1337535T3 (sh)
EC (1) ECSP034607A (sh)
ES (1) ES2220831T3 (sh)
GC (1) GC0000375A (sh)
GT (1) GT200100230A (sh)
HK (1) HK1062442A1 (sh)
HR (1) HRP20030360A2 (sh)
HU (1) HUP0303281A3 (sh)
IL (1) IL155813A0 (sh)
JO (1) JO2359B1 (sh)
MA (1) MA26962A1 (sh)
MX (1) MXPA03004251A (sh)
MY (1) MY141675A (sh)
NO (1) NO324706B1 (sh)
NZ (1) NZ525413A (sh)
PA (1) PA8532401A1 (sh)
PE (1) PE20020583A1 (sh)
PL (1) PL362925A1 (sh)
PT (1) PT1337535E (sh)
RU (1) RU2278865C2 (sh)
SI (1) SI1337535T1 (sh)
SK (1) SK7232003A3 (sh)
TR (1) TR200402073T4 (sh)
TW (1) TWI239333B (sh)
UY (1) UY27026A1 (sh)
WO (1) WO2002040487A2 (sh)
YU (1) YU35603A (sh)
ZA (1) ZA200303435B (sh)

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US6686352B2 (en) * 2001-05-18 2004-02-03 Hoffmann-La Roche Inc. Substituted imidazo [1,5-a] pyrimido [5,4-d] [1] benzazepine derivatives
WO2004113321A1 (ja) * 2003-06-19 2004-12-29 Daiichi Pharmaceutical Co., Ltd. 選択的なアミノ置換基導入法
PL1691811T3 (pl) 2003-12-11 2014-12-31 Sunovion Pharmaceuticals Inc Skojarzenie leku uspokajającego i modulatora neuroprzekaźnikowego oraz sposoby poprawy jakości snu i leczenia depresji
CA2577060A1 (en) 2004-08-13 2006-02-23 Amgen Inc. Substituted benzofused heterocycles
CN101039678B (zh) 2004-10-12 2011-06-15 弗·哈夫曼-拉罗切有限公司 用于治疗认知障碍的咪唑并[1,5-a]三唑并[1,5-d]苯并二氮杂䓬衍生物
CN101084220B (zh) * 2004-10-20 2010-12-15 弗·哈夫曼-拉罗切有限公司 卤素取代的苯并二氮杂*衍生物
RU2007112940A (ru) 2004-10-20 2008-11-27 Ф.Хоффманн-Ля Рош Аг (Ch) Производные имидазобензодиазепина
ES2307230T3 (es) 2004-12-14 2008-11-16 F. Hoffmann-La Roche Ag Imidazo-benzodiacepinas tetraciclicas como moduladores de los receptores gaba.
US8510055B2 (en) 2005-08-03 2013-08-13 The Johns Hopkins University Methods for characterizing and treating cognitive impairment in aging and disease
WO2007019312A2 (en) * 2005-08-03 2007-02-15 The Johns Hopkins University Methods for characterizing and treating cognitive impairment in aging and disease
ATE477255T1 (de) * 2005-10-11 2010-08-15 Hoffmann La Roche Imidazobenzdiazepinderivate
CA2625210A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
WO2009139916A1 (en) * 2008-05-16 2009-11-19 Synta Pharmaceuticals Corp. Tricyclic triazole compounds that modulate hsp90 activity
AU2009317386B2 (en) * 2008-11-18 2013-07-25 F. Hoffmann-La Roche Ag Alkylcyclohexylethers of dihydrotetraazabenzoazulenes
ES2431279T3 (es) * 2008-11-28 2013-11-25 F. Hoffmann-La Roche Ag Arilciclohexiléteres de dihidro-tetraazabenzoazulenos para uso como antagonistas del receptor V1A de la vasopresina
CU20090172A6 (es) 2009-10-09 2011-10-05 Facultad De Quimica Universidad De La Habana Sistemas tricíclicos y tetracíclicos con actividad sobre el sistema nervioso central y vascular
AU2011328993B2 (en) 2010-11-15 2017-03-02 Agenebio, Inc. Pyridazine derivatives, compositions and methods for treating cognitive impairment
US20150374705A1 (en) 2012-02-14 2015-12-31 Shanghai Institues for Biological Sciences Substances for treatment or relief of pain
WO2014047413A1 (en) * 2012-09-21 2014-03-27 Uwm Research Foundation, Inc. Novel gabaa agonists and methods of using to control airway hyperresponsiveness and inflammation in asthma
JP6883988B2 (ja) * 2013-12-20 2021-06-09 エージンバイオ, インコーポレイテッド ベンゾジアゼピン誘導体、組成物、および認知障害を処置するための方法
EA036844B1 (ru) 2015-06-19 2020-12-28 Эйджинбайо, Инк. Производные бензодиазепина, композиции и способы для лечения когнитивного нарушения
US10059718B2 (en) 2016-01-04 2018-08-28 Tabomedex Biosciences, LLC Fused quadracyclic compounds, compositions and uses thereof
US10973479B2 (en) 2016-05-16 2021-04-13 Canon Medical Systems Corporation X-ray diagnosis apparatus, X-ray diagnosis apparatus controlling method, and X-ray diagnosis system
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
KR102512548B1 (ko) 2017-12-22 2023-03-22 삼성디스플레이 주식회사 유기 전계 발광 소자 및 유기 전계 발광 소자용 함질소 화합물
JP7514534B2 (ja) * 2018-06-19 2024-07-11 エージンバイオ, インコーポレイテッド 認知障害を処置するためのベンゾジアゼピン誘導体、組成物および方法
KR102151969B1 (ko) * 2019-12-11 2020-09-04 주식회사 지투비 투과도 가변창의 제조방법 및 그에 의해 제조된 투과도 가변창
CN112979658B (zh) * 2021-02-22 2022-05-31 南湖实验室 一种氟马西尼的制备方法
US20240132513A1 (en) 2022-08-19 2024-04-25 Agenebio, Inc. Benzazepine derivatives, compositions, and methods for treating cognitive impairment

Family Cites Families (2)

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DK174086D0 (da) 1986-04-16 1986-04-16 Ferrosan As Nye benzodiazepinderivater samt fremgangsmaade til fremstilling af samme
TW201311B (sh) 1991-06-17 1993-03-01 Hoffmann La Roche

Also Published As

Publication number Publication date
KR20030045192A (ko) 2003-06-09
EP1337535A2 (en) 2003-08-27
ZA200303435B (en) 2004-08-05
PE20020583A1 (es) 2002-07-06
DK1337535T3 (da) 2004-10-25
NO20032208L (no) 2003-05-15
BG107817A (bg) 2004-07-30
PL362925A1 (en) 2004-11-02
IL155813A0 (en) 2003-12-23
DE60103776D1 (de) 2004-07-15
AU2002217007B2 (en) 2006-11-30
KR100504300B1 (ko) 2005-07-28
GC0000375A (en) 2007-03-31
HK1062442A1 (en) 2004-11-05
CZ295256B6 (cs) 2005-06-15
CN1191255C (zh) 2005-03-02
PA8532401A1 (es) 2002-08-26
NO20032208D0 (no) 2003-05-15
US20020103371A1 (en) 2002-08-01
NZ525413A (en) 2005-02-25
TR200402073T4 (tr) 2004-10-21
MY141675A (en) 2010-06-15
RU2278865C2 (ru) 2006-06-27
CA2427576A1 (en) 2002-05-23
EP1337535B1 (en) 2004-06-09
SI1337535T1 (en) 2004-10-31
RU2003116895A (ru) 2005-02-20
HRP20030360A2 (en) 2005-04-30
SK7232003A3 (en) 2004-03-02
UY27026A1 (es) 2002-06-20
TWI239333B (en) 2005-09-11
BR0115393A (pt) 2004-07-06
DE60103776T2 (de) 2005-07-14
JP2004517070A (ja) 2004-06-10
WO2002040487A3 (en) 2002-09-26
AR031345A1 (es) 2003-09-17
ATE268776T1 (de) 2004-06-15
JO2359B1 (en) 2006-12-12
HUP0303281A2 (hu) 2004-01-28
MA26962A1 (fr) 2004-12-20
NO324706B1 (no) 2007-12-03
JP4088151B2 (ja) 2008-05-21
AU1700702A (en) 2002-05-27
WO2002040487A2 (en) 2002-05-23
PT1337535E (pt) 2004-09-30
GT200100230A (es) 2002-07-04
HUP0303281A3 (en) 2005-05-30
ECSP034607A (es) 2003-06-25
US6743789B2 (en) 2004-06-01
CZ20031597A3 (cs) 2003-11-12
CA2427576C (en) 2007-11-06
MXPA03004251A (es) 2003-09-22
ES2220831T3 (es) 2004-12-16
CN1474820A (zh) 2004-02-11

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