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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JP2004508092A (ja) * 2000-09-08 2004-03-18 コールマン ジェイムス イー 外科用ステープラ
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US20060084672A1 (en) * 2004-10-20 2006-04-20 The Hospital For Sick Children Method for modification of y-secretase activity through inhibition of Fkbp13
US8362075B2 (en) 2005-05-17 2013-01-29 Merck Sharp & Dohme Corp. Cyclohexyl sulphones for treatment of cancer
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
EP2121633A2 (de) 2007-02-12 2009-11-25 Merck & Co., Inc. Piperazinderivate zur behandlung von alzheimer-krankheit und verwandten leiden
JP5539221B2 (ja) 2007-12-21 2014-07-02 リガンド・ファーマシューティカルズ・インコーポレイテッド 選択的アンドロゲン受容体モジュレーター(sarm)およびその使用
US8461389B2 (en) 2008-04-18 2013-06-11 University College Dublin, National University Of Ireland, Dublin Psycho-pharmaceuticals
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
JP5099731B1 (ja) 2009-10-14 2012-12-19 メルク・シャープ・アンド・ドーム・コーポレーション p53活性を増大する置換ピペリジン及びその使用
EP2493497A4 (de) 2009-11-01 2013-07-24 Brigham & Womens Hospital Notch-hemmung bei der behandlung und prophylaxe von adipositas und dem stoffwechselsyndrom
EP2584903B1 (de) 2010-06-24 2018-10-24 Merck Sharp & Dohme Corp. Neue heterozyklische verbindungen als erk-hemmer
AU2011285909B2 (en) 2010-08-02 2016-11-10 Sirna Therapeutics, Inc. RNA interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (CTNNB1) gene expression using short interfering nucleic acid (siNA)
EP2606134B1 (de) 2010-08-17 2019-04-10 Sirna Therapeutics, Inc. Rna-interferenz-vermittelte hemmung der hepatitis b-virus (hbv)-genexpression mittels kurzer interferierender nukleinsäure (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
EP3766975A1 (de) 2010-10-29 2021-01-20 Sirna Therapeutics, Inc. Rna-interferenz-vermittelte inhibition von genexpression unter verwendung kurzer interferierender nukleinsäure (sina)
EP2654748B1 (de) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazolderivate als erk-hemmer
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
EP3358013B1 (de) 2012-05-02 2020-06-24 Sirna Therapeutics, Inc. Sina-zusammensetzungen
KR20150060724A (ko) 2012-09-28 2015-06-03 머크 샤프 앤드 돔 코포레이션 Erk 억제제인 신규 화합물
DK2925888T3 (en) 2012-11-28 2017-12-18 Merck Sharp & Dohme COMPOSITIONS AND METHODS OF CANCER TREATMENT
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
EP2935263B1 (de) 2012-12-20 2018-12-05 Merck Sharp & Dohme Corp. Substituierte imidazopyridine als hdm2 inhibitoren
AU2014206834B2 (en) 2013-01-17 2017-06-22 Janssen Pharmaceutica Nv Novel substituted pyrido-piperazinone derivatives as gamma secretase modulators
US9540377B2 (en) 2013-01-30 2017-01-10 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
WO2015108988A2 (en) 2014-01-17 2015-07-23 Ligand Pharmaceuticals, Inc. Methods and compositions for modulating hormone levels
WO2018071283A1 (en) 2016-10-12 2018-04-19 Merck Sharp & Dohme Corp. Kdm5 inhibitors
US11098059B2 (en) 2017-11-08 2021-08-24 Merck Sharp & Dohme Corp. PRMT5 inhibitors
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2019222298A1 (en) * 2018-05-15 2019-11-21 Bristol-Myers Squibb Company Compositions comprising bisfluoroalkyl-1,4-benzodiazepinone compounds and methods of use thereof
WO2020016377A1 (en) 2018-07-19 2020-01-23 INSERM (Institut National de la Santé et de la Recherche Médicale) Combination for treating cancer
EP3833667B1 (de) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC Prmt5-inhibitoren
BR112021002267A8 (pt) 2018-08-07 2023-02-07 Merck Sharp & Dohme Inibidores de prmt5
WO2020033285A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833668B1 (de) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5-inhibitoren
KR20220003554A (ko) 2019-04-19 2022-01-10 리간드 파마슈티칼스 인코포레이티드 화합물의 결정질 형태 및 결정질 형태를 제조하는 방법
EP4076459B1 (de) 2019-12-17 2026-04-29 Merck Sharp & Dohme LLC Prmt5-inhibitoren
BR112022012015A2 (pt) 2019-12-17 2022-08-30 Merck Sharp & Dohme Llc Inibidores de prmt5
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
CA3160153A1 (en) 2019-12-17 2021-06-24 Michelle Machacek Prmt5 inhibitors
EP4244391A1 (de) 2020-11-16 2023-09-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Verfahren und zusammensetzungen zur vorhersage und behandlung von uvealem melanom
KR20250053961A (ko) 2022-09-02 2025-04-22 머크 샤프 앤드 돔 엘엘씨 엑사테칸-유래 토포이소머라제-1 억제제 제약 조성물 및 그의 용도
TW202432099A (zh) 2022-10-25 2024-08-16 美商默沙東有限責任公司 源自依克沙替康(exatecan)之adc連接子-載藥(payload)、醫藥組合物及其用途
IL321395A (en) 2022-12-14 2025-08-01 Merck Sharp & Dohme Llc Auristatin cargo-linkers, pharmaceutical compounds, and their uses

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US5426185A (en) 1993-11-22 1995-06-20 Merck & Co., Inc. Antiarrhythmic benzodiazepines
TR199901343T2 (xx) 1996-12-23 1999-09-21 Elan Pharmaceuticals, Inc. Sikloalkil, laktam, lakton ve ilgili bile�ikler, bunlar� i�eren farmas�tik bile�imler ve b�yle bile�ikler kullan�larak �-amiloid peptidinin sal�nmas�n� ve/veya sentezini inhibe etmek i�in y�ntemler.
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
GB0025173D0 (en) 2000-11-29
EP1326849A1 (de) 2003-07-16
CA2424812A1 (en) 2002-04-18
US20040024203A1 (en) 2004-02-05
US6995155B2 (en) 2006-02-07
DE60134874D1 (de) 2008-08-28
AU2001292126A1 (en) 2002-04-22
JP2004511474A (ja) 2004-04-15
EP1326849B1 (de) 2008-07-16
WO2002030912A1 (en) 2002-04-18

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