ATE354563T1 - Sulfonderivate zur hemmung von gamma-secretase - Google Patents

Sulfonderivate zur hemmung von gamma-secretase

Info

Publication number
ATE354563T1
ATE354563T1 AT03753700T AT03753700T ATE354563T1 AT E354563 T1 ATE354563 T1 AT E354563T1 AT 03753700 T AT03753700 T AT 03753700T AT 03753700 T AT03753700 T AT 03753700T AT E354563 T1 ATE354563 T1 AT E354563T1
Authority
AT
Austria
Prior art keywords
gamma secretase
sulfone derivatives
inhibiting gamma
inhibiting
secretase
Prior art date
Application number
AT03753700T
Other languages
English (en)
Inventor
James Michael Crawforth
Jason Matthew Elliott
Andrew Pate Owens
Francine Sternfeld
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 ATE354563T1 publication Critical patent/ATE354563T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/16—Preparation of optical isomers
    • C07C231/18—Preparation of optical isomers by stereospecific synthesis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/28—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/96—Sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/36—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/18—One oxygen or sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/02—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings
    • C07D275/03—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/04—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/36—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/34—Sulfur atoms

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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Quinoline Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Picture Signal Circuits (AREA)
AT03753700T 2002-10-04 2003-09-25 Sulfonderivate zur hemmung von gamma-secretase ATE354563T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0223040.7A GB0223040D0 (en) 2002-10-04 2002-10-04 Therapeutic compounds

Publications (1)

Publication Number Publication Date
ATE354563T1 true ATE354563T1 (de) 2007-03-15

Family

ID=9945314

Family Applications (1)

Application Number Title Priority Date Filing Date
AT03753700T ATE354563T1 (de) 2002-10-04 2003-09-25 Sulfonderivate zur hemmung von gamma-secretase

Country Status (10)

Country Link
US (1) US7161006B2 (de)
EP (1) EP1551798B1 (de)
JP (1) JP4478025B2 (de)
AT (1) ATE354563T1 (de)
AU (1) AU2003271862B2 (de)
CA (1) CA2500966A1 (de)
DE (1) DE60312017T2 (de)
ES (1) ES2280785T3 (de)
GB (1) GB0223040D0 (de)
WO (1) WO2004031138A1 (de)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0108591D0 (en) 2001-04-05 2001-05-23 Merck Sharp & Dohme Therapeutic agents
GB0120347D0 (en) 2001-08-21 2001-10-17 Merck Sharp & Dohme Therapeutic agents
US7399775B2 (en) 2001-12-27 2008-07-15 Daiichi Pharmaceutical Co., Ltd. β-amyloid protein production/secretion inhibitor
GB0223039D0 (en) 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
GB0308318D0 (en) * 2003-04-10 2003-05-14 Merck Sharp & Dohme Therapeutic agents
PL379466A1 (pl) * 2003-06-30 2006-09-18 Daiichi Sankyo Company , Limited Heterocykliczne pochodne metylosulfonu
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
WO2007103114A2 (en) * 2006-03-07 2007-09-13 The Brigham & Women's Hospital, Inc. Notch inhibition in the treatment or prevention of atherosclerosis
CA2676715A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
ES2428326T3 (es) 2007-10-04 2013-11-07 Merck Sharp & Dohme Corp. Derivados de aril sulfona sustituida como bloqueadores de canales de calcio
WO2009128057A2 (en) 2008-04-18 2009-10-22 UNIVERSITY COLLEGE DUBLIN, NATIONAL UNIVERSITY OF IRELAND, DUBLIN et al Psycho-pharmaceuticals
EP2413932A4 (de) 2009-04-01 2012-09-19 Merck Sharp & Dohme Hemmer der akt-aktivität
US20120129189A1 (en) * 2009-07-17 2012-05-24 Chulan Kwon Methods of Controlling Cell Proliferation
CA2777043C (en) 2009-10-14 2015-12-15 Schering Corporation Substituted piperidines that increase p53 activity and the uses thereof
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
CN103068980B (zh) 2010-08-02 2017-04-05 瑟纳治疗公司 使用短干扰核酸(siNA)的RNA干扰介导的联蛋白(钙粘蛋白关联蛋白质),β1(CTNNB1)基因表达的抑制
RU2745848C2 (ru) 2010-08-17 2021-04-01 Сирна Терапьютикс, Инк. ОПОСРЕДУЕМОЕ РНК-ИНТЕРФЕРЕНЦИЕЙ ИНГИБИРОВАНИЕ ЭКСПРЕССИИ ГЕНОВ ВИРУСА ГЕПАТИТА B (HBV) С ПРИМЕНЕНИЕМ МАЛОЙ ИНТЕРФЕРИРУЮЩЕЙ НУКЛЕИНОВОЙ КИСЛОТЫ (миНК)
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
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
EP3919620A1 (de) 2012-05-02 2021-12-08 Sirna Therapeutics, Inc. Zusammensetzungen mit kurzer interferierender nukleinsäure (sina)
CA2882950A1 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
SMT201700595T1 (it) 2012-11-28 2018-03-08 Merck Sharp & Dohme Composizioni e metodi per trattare il cancro
WO2014100065A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
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
US10975084B2 (en) 2016-10-12 2021-04-13 Merck Sharp & Dohme Corp. KDM5 inhibitors
WO2019094312A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3706742B1 (de) 2017-11-08 2023-03-15 Merck Sharp & Dohme LLC Prmt5-inhibitoren
WO2020016377A1 (en) 2018-07-19 2020-01-23 INSERM (Institut National de la Santé et de la Recherche Médicale) Combination for treating cancer
WO2020033285A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2020033282A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
CA3108388A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833667B1 (de) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC Prmt5-inhibitoren
EP4076459B1 (de) 2019-12-17 2026-04-29 Merck Sharp & Dohme LLC Prmt5-inhibitoren
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
ES3074517T3 (en) 2019-12-17 2026-07-21 Merck Sharp & Dohme Llc 4-(3,4-dihydroisoquinolin-2(1h)-yl)-3-hydroxypiperidine derivatives as prmt5 inhibitors for the treatment of cancer and sickle cell disease
ES3022307T3 (en) 2019-12-17 2025-05-28 Merck Sharp & Dohme Llc 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
CN120225528A (zh) 2022-09-02 2025-06-27 默沙东有限责任公司 依喜替康衍生的拓扑异构酶-1抑制剂药物组合物及其用途
KR20250079227A (ko) 2022-10-25 2025-06-04 머크 샤프 앤드 돔 엘엘씨 엑사테칸-유래 adc 링커-페이로드, 제약 조성물, 및 그의 용도
KR20250116773A (ko) 2022-12-14 2025-08-01 머크 샤프 앤드 돔 엘엘씨 아우리스타틴 링커-페이로드, 제약 조성물, 및 그의 용도

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1348442A (zh) 1999-02-26 2002-05-08 默克公司 新的磺胺化合物及其应用

Also Published As

Publication number Publication date
WO2004031138A1 (en) 2004-04-15
US20050261276A1 (en) 2005-11-24
JP4478025B2 (ja) 2010-06-09
JP2006501293A (ja) 2006-01-12
DE60312017T2 (de) 2007-10-25
ES2280785T3 (es) 2007-09-16
EP1551798B1 (de) 2007-02-21
AU2003271862A1 (en) 2004-04-23
CA2500966A1 (en) 2004-04-15
GB0223040D0 (en) 2002-11-13
US7161006B2 (en) 2007-01-09
AU2003271862B2 (en) 2009-12-17
DE60312017D1 (de) 2007-04-05
EP1551798A1 (de) 2005-07-13

Similar Documents

Publication Publication Date Title
DE60312017D1 (de) Sulfonderivate zur hemmung von gamma-secretase
ATE368031T1 (de) Neue gamma secretase inhibitoren
ATE443043T1 (de) Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer
ATE386028T1 (de) Zyklohexylsulfone als gamma-sekretase-inhibitoren
DE60329533D1 (de) Cyclische sulfamide zur inhibierung von gamma-sekretase
ATE299890T1 (de) Inhibitoren von gamma-secretase
ATE464287T1 (de) Cyclohexyl-sulphone als gamma-sekretase- inhibitoren
DE60112957D1 (de) Sulfamide als gamma-secretase-inhibitoren
ATE401314T1 (de) Benzodiazepin-derivate als gamma-secretase inhibitoren
ATE416761T1 (de) Prävention und behandlung von durch entzündung ausgelöstem und/oder immunvermitteltem knochenschwund
BR0308243A (pt) Composto, formulação farmacêutica, e, métodos de tratar diabetes, doença de alzheimer, e de inibir gsk-3 em um mamìfero
ATE427300T1 (de) Heterocyclisch substituierte amide als calpainhemmer
WO2005004803A3 (en) Phenylcarboxylate beta-secretase inhibitors for the treatment of alzheimer's disease
ATE414089T1 (de) Verwendung von rapamycin und dessen derivaten zur behandlung von knochenverlust
DE60221627D1 (de) Thiazolderivate und ihre Verwendung zur Behandlung oder Vorbeugung von Infektionen durch Flaviviren
WO2005004802A3 (en) N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
ATE550338T1 (de) Spiropiperidininhibitoren von beta-secretase zur behandlung von alzheimer-krankheit
ATE396174T1 (de) Hydroxyalkylaminderivate als beta-secretase- inhibitoren und deren verwendung zur behandlung der alzheimerschen krankheit oder ähnlicher krankheiten
DE60237725D1 (de) Vervendung von dexrazoxane in der prävention und behandlung der alzeheimer-krankheit
DE60328182D1 (de) Heteroaryl substituierte spirocyclische sulfamide zur hemmung von gamma sekretase
DE602004011255D1 (de) Phosphinsäurederivate, inhibitoren von beta-sekretase zur behandlung von alzheimer-krankheit
ATE357438T1 (de) 1,2,4-triaminobenzolderivate zur behandlung von erkrankungen des zentralnervensystems
NO20054744L (no) Behandling av Alzheimers sykdom
ATE469886T1 (de) 17beta-hydroxysteroid dehydrogenase typ-3 hemmer zur behandlung von androgen abhängigen erkrankungen
DE602004006118D1 (de) 2,3,4,5-TETRAHYDROBENZOiFöi1,4öOXAZEPIN-5-CARBONSÄUREAMID DERIVATE ALS GAMMA-SECRETASE INHIBITOREN ZUR BEHANDLUNG VON ALZHEIMER

Legal Events

Date Code Title Description
RER Ceased as to paragraph 5 lit. 3 law introducing patent treaties