DE60134874D1 - Benzodiazepin-derivate als gamma-secretase inhibitoren - Google Patents

Benzodiazepin-derivate als gamma-secretase inhibitoren

Info

Publication number
DE60134874D1
DE60134874D1 DE60134874T DE60134874T DE60134874D1 DE 60134874 D1 DE60134874 D1 DE 60134874D1 DE 60134874 T DE60134874 T DE 60134874T DE 60134874 T DE60134874 T DE 60134874T DE 60134874 D1 DE60134874 D1 DE 60134874D1
Authority
DE
Germany
Prior art keywords
gamma
secretase inhibitors
benzodiazepine derivatives
compounds
benzodiazepine
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
DE60134874T
Other languages
English (en)
Inventor
Ian Churcher
Alan John Nadin
Andrew Pate Owens
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Organon Pharma UK Ltd
Original Assignee
Merck Sharp and Dohme Ltd
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 and Dohme Ltd filed Critical Merck Sharp and Dohme Ltd
Application granted granted Critical
Publication of DE60134874D1 publication Critical patent/DE60134874D1/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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)
DE60134874T 2000-10-13 2001-10-08 Benzodiazepin-derivate als gamma-secretase inhibitoren Expired - Fee Related DE60134874D1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0025173.6A GB0025173D0 (en) 2000-10-13 2000-10-13 Therapeutic agents
PCT/GB2001/004474 WO2002030912A1 (en) 2000-10-13 2001-10-08 Benzodiazepine derivatives as inhibitors of gamma secretase

Publications (1)

Publication Number Publication Date
DE60134874D1 true DE60134874D1 (de) 2008-08-28

Family

ID=9901256

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60134874T Expired - Fee Related DE60134874D1 (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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JP2001125908A (ja) * 1999-10-26 2001-05-11 Sony Corp 入力装置および方法
GB0012671D0 (en) * 2000-05-24 2000-07-19 Merck Sharp & Dohme Therapeutic agents
ATE485006T1 (de) * 2000-09-08 2010-11-15 Abbott Vascular Inc Vorrichtung zum orten eines punktierten blutgefässes
US7060698B2 (en) 2003-05-19 2006-06-13 Hoffmann-La Roche Inc. Benzoxazepinone derivatives
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
ATE550019T1 (de) 2005-05-17 2012-04-15 Merck Sharp & Dohme Cis-4-ä(4-chlorophenyl)sulfonylü-4-(2,5- difluorophenyl)cyclohexanepropansäure zur behandlug von krebs
US9567396B2 (en) 2006-03-07 2017-02-14 Evonik Degussa Gmbh Notch inhibition in the prevention of vein graft failure
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
WO2007103114A2 (en) 2006-03-07 2007-09-13 The Brigham & Women's Hospital, Inc. Notch inhibition in the treatment or prevention of atherosclerosis
WO2008099210A2 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
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
EP2291181B9 (de) 2008-04-18 2013-09-11 University College Dublin National University Of Ireland, Dublin Captodiamine zur Behandlung von depressionartigen Symptomen
US8691825B2 (en) 2009-04-01 2014-04-08 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
US20120129189A1 (en) * 2009-07-17 2012-05-24 Chulan Kwon Methods of Controlling Cell Proliferation
UA109417C2 (uk) 2009-10-14 2015-08-25 Мерк Шарп Енд Доме Корп. ЗАМІЩЕНІ ПІПЕРИДИНИ, ЯКІ ПІДВИЩУЮТЬ АКТИВНІСТЬ p53, І ЇХ ЗАСТОСУВАННЯ
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
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
EP3327125B1 (de) 2010-10-29 2020-08-05 Sirna Therapeutics, Inc. Rna-interferenz-vermittelte inhibition von genexpression unter verwendung kurzer interferierender nukleinsäure (sina)
US9351965B2 (en) 2010-12-21 2016-05-31 Merck Sharp & Dohme Corp. 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
EP2770987B1 (de) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Neue verbindungen als erk-hemmer
EP2844261B1 (de) 2012-05-02 2018-10-17 Sirna Therapeutics, Inc. Sina-zusammensetzungen
EP2900241B1 (de) 2012-09-28 2018-08-08 Merck Sharp & Dohme Corp. Neuartige verbindungen als erk-hemmer
WO2014085216A1 (en) 2012-11-28 2014-06-05 Merck Sharp & Dohme Corp. Compositions and methods for treating cancer
AR094116A1 (es) 2012-12-20 2015-07-08 Merck Sharp & Dohme Imidazopiridinas sustituidas como inhibidores de hdm2
WO2014096212A1 (en) * 2012-12-20 2014-06-26 Janssen Pharmaceutica Nv NOVEL TRICYCLIC 3,4-DIHYDRO-2H-PYRIDO[1,2-α]PYRAZINE-1,6-DIONE DERIVATIVES AS GAMMA SECRETASE MODULATORS
CN104936958B (zh) 2013-01-17 2019-07-26 詹森药业有限公司 作为γ分泌酶调节剂的新颖的经取代的吡啶并-哌嗪酮衍生物
EP2951180B1 (de) 2013-01-30 2018-05-02 Merck Sharp & Dohme Corp. 2,6,7,8-substituierte purine als hdm2-inhibitoren
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
WO2018071283A1 (en) 2016-10-12 2018-04-19 Merck Sharp & Dohme Corp. Kdm5 inhibitors
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
EP3706747A4 (de) 2017-11-08 2021-08-04 Merck Sharp & Dohme Corp. Prmt5-inhibitoren
JP2021523189A (ja) * 2018-05-15 2021-09-02 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company ビスフルオロアルキル−1,4−ベンゾジアゼピノン化合物を含む組成物およびその使用方法
EP3823672A1 (de) 2018-07-19 2021-05-26 Institut National de la Santé et de la Recherche Médicale (INSERM) Kombinationen zur behandlung von krebs
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833668A4 (de) 2018-08-07 2022-05-11 Merck Sharp & Dohme Corp. Prmt5-inhibitoren
MX2022007535A (es) 2019-12-17 2022-09-23 Merck Sharp & Dohme Llc Inhibidores de prmt5.
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
WO2024049931A1 (en) 2022-09-02 2024-03-07 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
TW202430140A (zh) 2022-12-14 2024-08-01 美商默沙東有限責任公司 奧里斯他汀(auristatin)連接子藥物(payload)、醫藥組合物及其用途

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5426185A (en) 1993-11-22 1995-06-20 Merck & Co., Inc. Antiarrhythmic benzodiazepines
ZA9711537B (en) 1996-12-23 1998-06-25 Athena Neurosciences Inc Eli L Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ß-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
BR9917082A (pt) 1998-12-24 2001-11-06 Du Pont Pharm Co Compostos inibidores da produção de proteìnas a"beta", método de tratamento de disfunções neurológicas associadas com a produção de "beta"-amilóide, composição farmacêutica e, método de inibição da atividade de y-secretase
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
WO2002030912A1 (en) 2002-04-18
EP1326849A1 (de) 2003-07-16
CA2424812A1 (en) 2002-04-18
GB0025173D0 (en) 2000-11-29
EP1326849B1 (de) 2008-07-16
JP2004511474A (ja) 2004-04-15
ATE401314T1 (de) 2008-08-15
AU2001292126A1 (en) 2002-04-22

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Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee