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)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (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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WO2005090319A1 (en) * 2004-03-19 2005-09-29 Arrow Therapeutics Limited Process for preparing benzodiazepines
US20060084672A1 (en) * 2004-10-20 2006-04-20 The Hospital For Sick Children Method for modification of y-secretase activity through inhibition of Fkbp13
ES2382814T3 (es) 2005-05-17 2012-06-13 Merck Sharp & Dohme Ltd. Ácido cis-4-[(4-clorofenil)sulfonil]-4-(2,5-difluorofenil)ciclohexanopropanoico para el tratamiento del cáncer
US9567396B2 (en) 2006-03-07 2017-02-14 Evonik Degussa Gmbh Notch inhibition in the prevention of vein graft failure
WO2007103114A2 (en) 2006-03-07 2007-09-13 The Brigham & Women's Hospital, Inc. Notch inhibition in the treatment or prevention of atherosclerosis
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
CA2676715A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
EP2222636B1 (de) 2007-12-21 2013-04-10 Ligand Pharmaceuticals Inc. Selektive androgenrezeptormodulatoren (sarms) und ihre verwendung
EP2291181B9 (de) 2008-04-18 2013-09-11 University College Dublin National University Of Ireland, Dublin Captodiamine zur Behandlung von depressionartigen Symptomen
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
US20120129189A1 (en) * 2009-07-17 2012-05-24 Chulan Kwon Methods of Controlling Cell Proliferation
PE20121172A1 (es) 2009-10-14 2012-09-05 Merck Sharp & Dohme Piperidinas sustituidas con actividad en la hdm2
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
EP3330377A1 (de) 2010-08-02 2018-06-06 Sirna Therapeutics, Inc. Durch rna-interferenz vermittelte hemmung der catenin (cadherin-assoziiertes protein)-beta-1 (ctnnb1)- genexpression mittels kurzer interferierender nukleinsäuren (sina)
US9029341B2 (en) 2010-08-17 2015-05-12 Sirna Therapeutics, Inc. RNA interference mediated inhibition of hepatitis B virus (HBV) gene expression using short interfering nucleic acid (siNA)
EP2613782B1 (de) 2010-09-01 2016-11-02 Merck Sharp & Dohme Corp. Indazolderivate als erk-hemmer
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
WO2012058210A1 (en) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
US9629891B2 (en) 2011-10-17 2017-04-25 Nationwide Children's Hospital, Inc. Products and methods for aortic abdominal aneurysm
EP2770987B1 (de) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Neue verbindungen als erk-hemmer
US20150299696A1 (en) 2012-05-02 2015-10-22 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
RU2660429C2 (ru) 2012-09-28 2018-07-06 Мерк Шарп И Доум Корп. Новые соединения, которые являются ингибиторами erk
RS56680B1 (sr) 2012-11-28 2018-03-30 Merck Sharp & Dohme Kompozicije i postupci za lečenje kancera
KR102196882B1 (ko) 2012-12-20 2020-12-30 머크 샤프 앤드 돔 코포레이션 Hdm2 억제제로서의 치환된 이미다조피리딘
AU2013366668B2 (en) * 2012-12-20 2017-07-20 Janssen Pharmaceutica Nv Novel tricyclic 3,4-dihydro-2H-pyrido[1,2-alpha]pyrazine -1,6-dione derivatives as gamma secretase modulators
ES2612215T3 (es) 2013-01-17 2017-05-12 Janssen Pharmaceutica, N.V. Novedosos derivados de pirido-piperazinona sustituidos como moduladores de gamma secretasa
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
WO2015034925A1 (en) 2013-09-03 2015-03-12 Moderna Therapeutics, Inc. Circular polynucleotides
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
EP3525785B1 (de) 2016-10-12 2025-08-27 Merck Sharp & Dohme LLC Kdm5-inhibitoren
EP3706747B1 (de) 2017-11-08 2025-09-03 Merck Sharp & Dohme LLC Prmt5-inhibitoren
US10947234B2 (en) 2017-11-08 2021-03-16 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
US12485126B2 (en) 2018-07-19 2025-12-02 INSERM (Institut National de la Santé et de la Recherche Médicale) Combination for treating cancer
US12173026B2 (en) 2018-08-07 2024-12-24 Merck Sharp & Dohme Llc PRMT5 inhibitors
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
US12552826B2 (en) 2018-08-07 2026-02-17 Merck Sharp & Dohme Llc PRMT5 inhibitors
EP3833668B1 (de) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5-inhibitoren
WO2020214834A1 (en) 2019-04-19 2020-10-22 Ligand Pharmaceuticals Inc. Crystalline forms and methods of producing crystalline forms of a compound
US12441730B2 (en) 2019-12-17 2025-10-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
BR112022012015A2 (pt) 2019-12-17 2022-08-30 Merck Sharp & Dohme Llc Inibidores de prmt5
WO2021126731A1 (en) 2019-12-17 2021-06-24 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US12595248B2 (en) 2019-12-17 2026-04-07 Merck Sharp & Dohme Llc PRMT5 inhibitors
US20230416830A1 (en) 2020-11-16 2023-12-28 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and compositions for predicting and treating uveal melanoma
US20240116945A1 (en) 2022-09-02 2024-04-11 Merck Sharp & Dohme Llc Exatecan-derived topoisomerase-1 inhibitors pharmaceutical compositions, and uses thereof
WO2024091437A1 (en) 2022-10-25 2024-05-02 Merck Sharp & Dohme Llc Exatecan-derived adc linker-payloads, pharmaceutical compositions, and uses thereof
GEAP202516798A (en) 2022-12-14 2025-10-27 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
HUP0001232A3 (en) 1996-12-23 2001-02-28 Elan Pharmaceuticals Inc San F Cycloalkyl, lactam, lactone derivatives and their thio analogues inhibiting betha-amyloid peptide release and/or its synthesis and pharmaceutical compositions containing the 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
WO2000038618A2 (en) 1998-12-24 2000-07-06 Du Pont Pharmaceuticals Company SUCCINOYLAMINO BENZODIAZEPINES AS INHIBITORS OF Aβ PROTEIN PRODUCTION
GB0012671D0 (en) 2000-05-24 2000-07-19 Merck Sharp & Dohme Therapeutic agents

Also Published As

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

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