CA2455861A1 - Sulfonamide derivatives as gamma secretase inhibitors - Google Patents

Sulfonamide derivatives as gamma secretase inhibitors Download PDF

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Publication number
CA2455861A1
CA2455861A1 CA002455861A CA2455861A CA2455861A1 CA 2455861 A1 CA2455861 A1 CA 2455861A1 CA 002455861 A CA002455861 A CA 002455861A CA 2455861 A CA2455861 A CA 2455861A CA 2455861 A1 CA2455861 A1 CA 2455861A1
Authority
CA
Canada
Prior art keywords
alkyl
compound
aryl
alkylene
heteroaryl
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.)
Abandoned
Application number
CA002455861A
Other languages
English (en)
French (fr)
Inventor
Hubert B. Josien
John W. Clader
Theodros Asberom
Dmitri A. Pissarnitski
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.)
Merck Sharp and Dohme LLC
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2455861A1 publication Critical patent/CA2455861A1/en
Abandoned legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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 linked by a carbon chain containing only aliphatic 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/56—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/06—Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
CA002455861A 2001-08-03 2002-08-01 Sulfonamide derivatives as gamma secretase inhibitors Abandoned CA2455861A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US31006801P 2001-08-03 2001-08-03
US60/310,068 2001-08-03
PCT/US2002/024293 WO2003013527A1 (en) 2001-08-03 2002-08-01 Sulfonamide derivatives as gamma secretase inhibitors

Publications (1)

Publication Number Publication Date
CA2455861A1 true CA2455861A1 (en) 2003-02-20

Family

ID=23200871

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002455861A Abandoned CA2455861A1 (en) 2001-08-03 2002-08-01 Sulfonamide derivatives as gamma secretase inhibitors

Country Status (8)

Country Link
US (2) US7122675B2 (enExample)
EP (1) EP1411944A1 (enExample)
JP (1) JP2005504042A (enExample)
CN (1) CN1780621A (enExample)
AR (1) AR035260A1 (enExample)
CA (1) CA2455861A1 (enExample)
MX (1) MXPA04001016A (enExample)
WO (1) WO2003013527A1 (enExample)

Families Citing this family (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8044259B2 (en) 2000-08-03 2011-10-25 The Regents Of The University Of Michigan Determining the capability of a test compound to affect solid tumor stem cells
US6984522B2 (en) 2000-08-03 2006-01-10 Regents Of The University Of Michigan Isolation and use of solid tumor stem cells
WO2003013527A1 (en) * 2001-08-03 2003-02-20 Schering Corporation Sulfonamide derivatives as gamma secretase inhibitors
AU2002367147A1 (en) 2001-12-27 2003-07-15 Daiichi Pharmaceutical Co., Ltd. Beta-AMYLOID PROTEIN PRODUCTION/SECRETION INHIBITORS
GB0223039D0 (en) * 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
GB0223038D0 (en) * 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
WO2004072034A1 (en) * 2003-02-17 2004-08-26 F. Hoffmann-La Roche Ag Piperidine-benzenesulfonamide derivatives
US7521481B2 (en) * 2003-02-27 2009-04-21 Mclaurin Joanne Methods of preventing, treating and diagnosing disorders of protein aggregation
US7067509B2 (en) * 2003-03-07 2006-06-27 Neurocrine Biosciences, Inc. Melanin-concentrating hormone receptor antagonists and compositions and methods related thereto
CA2526487A1 (en) 2003-06-30 2005-01-06 Daiichi Pharmaceutical Co., Ltd. Heterocyclic methyl sulfone derivative
WO2005014540A1 (en) 2003-08-08 2005-02-17 Schering Corporation Cyclic amine base-1 inhibitors having a heterocyclic substituent
AU2004265298A1 (en) 2003-08-08 2005-02-24 Pharmacopeia, Inc. Cyclic amine BACE-1 inhibitors having a benzamide substituent
AU2004285022A1 (en) 2003-10-29 2005-05-12 Elan Pharmaceuticals, Inc. N-substituted benzene sulfonamides
CA2554779A1 (en) * 2004-02-03 2005-08-18 The Regents Of The University Of Michigan Compositions and methods for characterizing, regulating, diagnosing, and treating cancer
ATE552851T1 (de) 2004-02-03 2012-04-15 Univ Michigan Zusammensetzungen zur behandlung von brust- und bauchspeicheldrüsenkrebs
AU2005230681B2 (en) * 2004-04-05 2009-07-30 Schering Corporation Novel gamma secretase inhibitors
JP2008502684A (ja) * 2004-06-15 2008-01-31 メルク　エンド　カムパニー　インコーポレーテッド アルツハイマー病を治療するためのベータ−セクレターゼ阻害剤として有用なピロリジン−３−イル化合物
JP2008505100A (ja) 2004-06-30 2008-02-21 シェーリング　コーポレイション ガンマ−セクレターゼ阻害剤としての置換ｎ−アリールスルホニル複素環アミン
AR049726A1 (es) 2004-07-22 2006-08-30 Schering Corp Amidas sustituidas inhibidoras de beta secretasa
TW200630337A (en) 2004-10-14 2006-09-01 Euro Celtique Sa Piperidinyl compounds and the use thereof
US20060252073A1 (en) * 2005-04-18 2006-11-09 Regents Of The University Of Michigan Compositions and methods for the treatment of cancer
WO2007053648A2 (en) 2005-10-31 2007-05-10 The Regents Of The University Of Michigan Compositions and methods for treating and diagnosing cancer
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
US9567396B2 (en) 2006-03-07 2017-02-14 Evonik Degussa Gmbh Notch inhibition in the prevention of vein graft failure
US8133857B2 (en) * 2006-03-07 2012-03-13 The Brigham and Women's FHospital, Inc. NOTCH inhibition in the treatment of atherosclerosis
US8247442B2 (en) 2006-03-29 2012-08-21 Purdue Pharma L.P. Benzenesulfonamide compounds and their use
WO2007118854A1 (en) 2006-04-13 2007-10-25 Euro-Celtique S.A. Benzenesulfonamide compounds and the use thereof
US8791264B2 (en) 2006-04-13 2014-07-29 Purdue Pharma L.P. Benzenesulfonamide compounds and their use as blockers of calcium channels
WO2007141029A1 (en) * 2006-06-08 2007-12-13 Helmholtz Zentrum München Deutsches Forschungszentrum Für Gesundheit Und Umwelt (Gmbh) Specific protease inhibitors and their use in cancer therapy
WO2008055924A1 (en) 2006-11-07 2008-05-15 Vib Vzw Diagnosis and treatment of t-cell acute lymphoblastic leukemia
US8278345B2 (en) 2006-11-09 2012-10-02 Probiodrug Ag Inhibitors of glutaminyl cyclase
SI2091948T1 (sl) 2006-11-30 2012-07-31 Probiodrug Ag Novi inhibitorji glutaminil ciklaze
US8148147B2 (en) 2007-01-24 2012-04-03 The Regents Of The University Of Michigan Compositions and methods for treating and diagnosing pancreatic cancer
EA200901140A1 (ru) 2007-03-01 2010-04-30 Пробиодруг Аг Новое применение ингибиторов глутаминилциклазы
US8399486B2 (en) * 2007-04-09 2013-03-19 Purdue Pharma L.P. Benzenesulfonyl compounds and the use thereof
EP2142514B1 (en) 2007-04-18 2014-12-24 Probiodrug AG Thiourea derivatives as glutaminyl cyclase inhibitors
EP1997805A1 (en) * 2007-06-01 2008-12-03 Commissariat à l'Energie Atomique Compounds with antiparasitic activity, applications thereof to the treatment of infectious diseases caused by apicomplexans
WO2009040659A2 (en) 2007-09-28 2009-04-02 Purdue Pharma L.P. Benzenesulfonamide compounds and the use thereof
WO2009051661A2 (en) * 2007-10-12 2009-04-23 The Brigham And Women's Hospital, Inc. Substituted aryl alkylamino-oxy-analogs and uses thereof
WO2011009064A1 (en) * 2009-07-17 2011-01-20 The J. David Gladstone Institutes Methods of controlling cell proliferation
EP2456435B1 (en) * 2009-07-21 2015-06-24 The Board of Trustees of the Leland Stanford Junior University Heteroaryl benzamides, compositions and methods of use
CN102695546B (zh) 2009-09-11 2014-09-10 前体生物药物股份公司 作为谷氨酰胺酰环化酶抑制剂的杂环衍生物
WO2011107530A2 (en) 2010-03-03 2011-09-09 Probiodrug Ag Novel inhibitors
SG183229A1 (en) 2010-03-10 2012-09-27 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
EP2560953B1 (en) 2010-04-21 2016-01-06 Probiodrug AG Inhibitors of glutaminyl cyclase
WO2012123563A1 (en) 2011-03-16 2012-09-20 Probiodrug Ag Benz imidazole derivatives as inhibitors of glutaminyl cyclase
WO2013059302A1 (en) 2011-10-17 2013-04-25 Nationwide Children's Hospital, Inc. Products and methods for aortic abdominal aneurysm
WO2016059220A1 (en) 2014-10-16 2016-04-21 INSERM (Institut National de la Santé et de la Recherche Médicale) Tcr-activating agents for use in the treatment of t-all
WO2017023999A1 (en) * 2015-08-03 2017-02-09 Emory University Methylsulfonamide derivatives and uses related thereto
DK3461819T3 (da) 2017-09-29 2020-08-10 Probiodrug Ag Inhibitorer af glutaminylcyklase
EP3823672A1 (en) 2018-07-19 2021-05-26 Institut National de la Santé et de la Recherche Médicale (INSERM) Combination for treating cancer

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5646167A (en) * 1993-01-06 1997-07-08 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamix acids
US5559128A (en) * 1995-04-18 1996-09-24 Merck & Co., Inc. 3-substituted piperidines promote release of growth hormone
CN1348442A (zh) * 1999-02-26 2002-05-08 默克公司 新的磺胺化合物及其应用
FR2802206B1 (fr) * 1999-12-14 2005-04-22 Sod Conseils Rech Applic Derives de 4-aminopiperidine et leur utilisation en tant que medicament
CA2406652A1 (en) * 2000-04-20 2001-11-01 Nps Allelix Corp. Aminopiperidines for use as glyt-1 inhibitors
KR20030029978A (ko) * 2000-09-25 2003-04-16 액테리온 파마슈티칼 리미티드 말라리아에 유용한 치환된 아미노-아자-사이클로알칸
WO2003013527A1 (en) * 2001-08-03 2003-02-20 Schering Corporation Sulfonamide derivatives as gamma secretase inhibitors

Also Published As

Publication number Publication date
US20060009467A1 (en) 2006-01-12
EP1411944A1 (en) 2004-04-28
WO2003013527A1 (en) 2003-02-20
CN1780621A (zh) 2006-05-31
US20030216380A1 (en) 2003-11-20
US7122675B2 (en) 2006-10-17
MXPA04001016A (es) 2004-05-27
AR035260A1 (es) 2004-05-05
JP2005504042A (ja) 2005-02-10

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FZDE Discontinued