ATE401314T1 - Benzodiazepin-derivate als gamma-secretase inhibitoren - Google Patents

Benzodiazepin-derivate als gamma-secretase inhibitoren

Info

Publication number
ATE401314T1
ATE401314T1 AT01972352T AT01972352T ATE401314T1 AT E401314 T1 ATE401314 T1 AT E401314T1 AT 01972352 T AT01972352 T AT 01972352T AT 01972352 T AT01972352 T AT 01972352T AT E401314 T1 ATE401314 T1 AT E401314T1
Authority
AT
Austria
Prior art keywords
gamma
secretase inhibitors
benzodiazepine derivatives
compounds
benzodiazepine
Prior art date
Application number
AT01972352T
Other languages
English (en)
Inventor
Ian Churcher
Alan Nadin
Andrew Owens
Original Assignee
Merck Sharp & Dohme
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 Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Application granted granted Critical
Publication of ATE401314T1 publication Critical patent/ATE401314T1/de

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/161,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/181,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hospice & Palliative Care (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Psychiatry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)
AT01972352T 2000-10-13 2001-10-08 Benzodiazepin-derivate als gamma-secretase inhibitoren ATE401314T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0025173.6A GB0025173D0 (en) 2000-10-13 2000-10-13 Therapeutic agents

Publications (1)

Publication Number Publication Date
ATE401314T1 true ATE401314T1 (de) 2008-08-15

Family

ID=9901256

Family Applications (1)

Application Number Title Priority Date Filing Date
AT01972352T ATE401314T1 (de) 2000-10-13 2001-10-08 Benzodiazepin-derivate als gamma-secretase inhibitoren

Country Status (9)

Country Link
US (1) US6995155B2 (de)
EP (1) EP1326849B1 (de)
JP (1) JP2004511474A (de)
AT (1) ATE401314T1 (de)
AU (1) AU2001292126A1 (de)
CA (1) CA2424812A1 (de)
DE (1) DE60134874D1 (de)
GB (1) GB0025173D0 (de)
WO (1) WO2002030912A1 (de)

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EP1888050B1 (de) 2005-05-17 2012-03-21 Merck Sharp & Dohme Ltd. Cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropansäure zur Behandlug von Krebs
WO2011053822A2 (en) 2009-11-01 2011-05-05 The Brigham And Women's Hospital, Inc. Notch inhibition in the treatment and prevention of obesity and metabolic syndrome
US8133857B2 (en) 2006-03-07 2012-03-13 The Brigham and Women's FHospital, Inc. NOTCH inhibition in the treatment of atherosclerosis
US9567396B2 (en) 2006-03-07 2017-02-14 Evonik Degussa Gmbh Notch inhibition in the prevention of vein graft failure
AU2008215948A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of AD and related conditions
PT2222636E (pt) 2007-12-21 2013-07-16 Ligand Pharm Inc Moduladores seletivos de recetores de andrógeno (sarms) e suas utilizações
US8461389B2 (en) 2008-04-18 2013-06-11 University College Dublin, National University Of Ireland, Dublin Psycho-pharmaceuticals
US8691825B2 (en) 2009-04-01 2014-04-08 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
WO2011009064A1 (en) * 2009-07-17 2011-01-20 The J. David Gladstone Institutes Methods of controlling cell proliferation
EP2488028B1 (de) 2009-10-14 2020-08-19 Merck Sharp & Dohme Corp. Substituierte piperidine zur erhöhung der p53-aktivität und ihre verwendung
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
CN107090456B (zh) 2010-08-02 2022-01-18 瑟纳治疗公司 使用短干扰核酸的RNA干扰介导的联蛋白(钙粘蛋白关联蛋白质),β1基因表达的抑制
JP2013537423A (ja) 2010-08-17 2013-10-03 メルク・シャープ・エンド・ドーム・コーポレイション 低分子干渉核酸(siNA)を用いたB型肝炎ウイルス(HBV)遺伝子発現のRNA干渉媒介性阻害
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation Indazole derivatives useful as erk inhibitors
EP2615916B1 (de) 2010-09-16 2017-01-04 Merck Sharp & Dohme Corp. Kondensierte pyrazolderivate als neue erk-hemmer
DK2632472T3 (en) 2010-10-29 2018-03-19 Sirna Therapeutics Inc RNA INTERFERENCE-MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERRING NUCLEIC ACIDS (SINA)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
WO2013059302A1 (en) 2011-10-17 2013-04-25 Nationwide Children's Hospital, Inc. Products and methods for aortic abdominal aneurysm
WO2013063214A1 (en) 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
EP2844261B1 (de) 2012-05-02 2018-10-17 Sirna Therapeutics, Inc. Sina-zusammensetzungen
CN105050598B (zh) 2012-09-28 2018-04-27 默沙东公司 作为erk抑制剂的新型化合物
RS56680B1 (sr) 2012-11-28 2018-03-30 Merck Sharp & Dohme Kompozicije i postupci za lečenje kancera
US8846657B2 (en) 2012-12-20 2014-09-30 Merck Sharp & Dohme Corp. Substituted imidazopyridines as HDM2 inhibitors
US10112943B2 (en) 2012-12-20 2018-10-30 Janssen Pharmaceutica Nv Substituted imidazoles as gamma secretase modulators
WO2014111457A1 (en) 2013-01-17 2014-07-24 Janssen Pharmaceutica Nv Novel substituted pyrido-piperazinone derivatives as gamma secretase modulators
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
EP3041938A1 (de) 2013-09-03 2016-07-13 Moderna Therapeutics, Inc. Kreisförmige polynukleotide
US10562897B2 (en) 2014-01-16 2020-02-18 Janssen Pharmaceutica Nv Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators
US10441567B2 (en) 2014-01-17 2019-10-15 Ligand Pharmaceuticals Incorporated Methods and compositions for modulating hormone levels
US10975084B2 (en) 2016-10-12 2021-04-13 Merck Sharp & Dohme Corp. KDM5 inhibitors
EP3706742B1 (de) 2017-11-08 2023-03-15 Merck Sharp & Dohme LLC Prmt5-inhibitoren
US11098059B2 (en) 2017-11-08 2021-08-24 Merck Sharp & Dohme Corp. PRMT5 inhibitors
CN112236147A (zh) * 2018-05-15 2021-01-15 百时美施贵宝公司 包含双氟烷基-1,4-苯并二氮杂*酮化合物的组合物和其使用方法
WO2020016377A1 (en) 2018-07-19 2020-01-23 INSERM (Institut National de la Santé et de la Recherche Médicale) Combination for treating cancer
EP3833668B1 (de) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5-inhibitoren
EP3833667B1 (de) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC Prmt5-inhibitoren
CA3108388A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2020033285A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
MX2021012690A (es) 2019-04-19 2022-01-31 Ligand Pharm Inc Formas cristalinas y metodos para producir formas cristalinas de un compuesto.
EP4076460B1 (de) 2019-12-17 2026-01-21 Merck Sharp & Dohme LLC 1,4-dihydro-2h-spiro[isoquinoline-3,4'-piperidin]-derivate als prmt5 inhibitoren zur behandlung von krebs
WO2021126728A1 (en) 2019-12-17 2021-06-24 Merck Sharp & Dohme Corp. Prmt5 inhibitors
JP7589247B2 (ja) 2019-12-17 2024-11-25 メルク・シャープ・アンド・ドーム・エルエルシー Prmt5阻害剤
WO2022101481A1 (en) 2020-11-16 2022-05-19 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and compositions for predicting and treating uveal melanoma
GEAP202516720A (en) 2022-09-02 2025-07-10 Merck Sharp & Dohme Llc Exatecan-derived topoisomerase-1 inhibitors pharmaceutical compositions, and uses thereof
IL320396A (en) 2022-10-25 2025-06-01 Merck Sharp & Dohme Llc Charge-linkers of anti-drug conjugates derived from extacan, pharmaceutical compositions, and uses thereof
US20240207425A1 (en) 2022-12-14 2024-06-27 Merck Sharp & Dohme Llc Auristatin linker-payloads, pharmaceutical compositions, and uses thereof

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US5426185A (en) 1993-11-22 1995-06-20 Merck & Co., Inc. Antiarrhythmic benzodiazepines
HRP970705A2 (en) 1996-12-23 1998-10-31 Warren J. Porter CYCLOALKYL, LACTAM, LACTONE AND RELATED COMPOUNDS, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND METHODS FOR INHIBITING "beta" -AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS BY USE OF SUCH COMPOUNDS
FR2782997A1 (fr) 1998-09-08 2000-03-10 Hoechst Marion Roussel Inc Nouveaux derives de la benzodiazepinone, procede de preparation et intermediaires de ce procede, application a titre de medicaments et compositions pharmaceutiques les renfermant
JP4615727B2 (ja) 1998-12-24 2011-01-19 ブリストル−マイヤーズ スクイブ ファーマ カンパニー Aβタンパク質生成の阻害剤としてのスクシノイルアミノベンゾジアゼピン
GB0012671D0 (en) * 2000-05-24 2000-07-19 Merck Sharp & Dohme Therapeutic agents

Also Published As

Publication number Publication date
US20040024203A1 (en) 2004-02-05
US6995155B2 (en) 2006-02-07
DE60134874D1 (de) 2008-08-28
JP2004511474A (ja) 2004-04-15
AU2001292126A1 (en) 2002-04-22
EP1326849A1 (de) 2003-07-16
GB0025173D0 (en) 2000-11-29
WO2002030912A1 (en) 2002-04-18
CA2424812A1 (en) 2002-04-18
EP1326849B1 (de) 2008-07-16

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