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

    • 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
    • C07D401/06Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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
    • C07D211/56Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62Carbon 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
    • 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
    • C07D401/12Heterocyclic 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
    • 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
    • C07D403/06Heterocyclic 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)
  • Neurology (AREA)
  • Neurosurgery (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)

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US6984522B2 (en) 2000-08-03 2006-01-10 Regents Of The University Of Michigan Isolation and use of solid tumor stem cells
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
CA2455861A1 (en) * 2001-08-03 2003-02-20 Schering Corporation Sulfonamide derivatives as gamma secretase inhibitors
CN100562516C (zh) 2001-12-27 2009-11-25 第一制药株式会社 β-淀粉样蛋白产生和分泌的抑制剂
GB0223038D0 (en) * 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
GB0223039D0 (en) * 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
DK1594840T3 (da) * 2003-02-17 2007-02-05 Hoffmann La Roche Piperidin-benzensulfonamid-derivater
US7521481B2 (en) 2003-02-27 2009-04-21 Mclaurin Joanne Methods of preventing, treating and diagnosing disorders of protein aggregation
WO2004080411A2 (en) * 2003-03-07 2004-09-23 Neurocrine Biosciences, Inc. Melanin-concentrating hormone receptor antagonists and compositions and methods related thereto
RU2336270C2 (ru) 2003-06-30 2008-10-20 Дайити Фармасьютикал Ко., Лтд. Гетероциклические метилсульфоновые производные
CA2534672A1 (en) 2003-08-08 2005-02-17 Schering Corporation Cyclic amine bace-1 inhibitors having a heterocyclic substituent
CN1863797A (zh) 2003-08-08 2006-11-15 先灵公司 具有苯甲酰胺取代基的环胺bace-1抑制剂
JP2007512242A (ja) * 2003-10-29 2007-05-17 イーラン ファーマスーティカルズ、インコーポレイテッド N−置換ベンゼンスルホンアミド
ATE552851T1 (de) 2004-02-03 2012-04-15 Univ Michigan Zusammensetzungen zur behandlung von brust- und bauchspeicheldrüsenkrebs
AU2005209909B8 (en) * 2004-02-03 2009-01-15 The Regents Of The University Of Michigan Compositions and methods for characterizing, regulating, diagnosing, and treating cancer
AU2005230681B2 (en) * 2004-04-05 2009-07-30 Schering Corporation Novel gamma secretase inhibitors
CN1968924B (zh) * 2004-06-15 2011-08-03 默沙东公司 作为β-分泌酶抑制剂用于治疗阿尔茨海默氏病的吡咯烷-3-基化合物
US7763613B2 (en) 2004-06-30 2010-07-27 Schering Corporation Substituted N-arylsulfonylheterocyclic amines as gamma-secretase inhibitors
JP2008507538A (ja) 2004-07-22 2008-03-13 シェーリング コーポレイション 置換アミドβセクレターゼインヒビター
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
EP1945754B1 (en) 2005-10-31 2014-07-23 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
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
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
TW200815353A (en) 2006-04-13 2008-04-01 Euro Celtique Sa Benzenesulfonamide compounds and their use
DK2041181T3 (da) * 2006-06-08 2011-08-29 Helmholtz Zentrum Muenchen Specifikke proteaseinhibitorer og deres anvendelse i cancerterapi
AU2007316597B2 (en) 2006-11-07 2013-01-31 Katholieke Universiteit Leuven, K. U. Leuven R & D 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
WO2008092002A2 (en) 2007-01-24 2008-07-31 The Regents Of The University Of Michigan Compositions and methods for treating and diagnosing pancreatic cancer
WO2008104580A1 (en) 2007-03-01 2008-09-04 Probiodrug Ag New use of glutaminyl cyclase inhibitors
WO2008124118A1 (en) 2007-04-09 2008-10-16 Purdue Pharma L.P. Benzenesulfonyl compounds and the use therof
DK2142514T3 (da) 2007-04-18 2015-03-23 Probiodrug Ag Thioureaderivater som glutaminylcyclase-inhibitorer
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
US8765736B2 (en) 2007-09-28 2014-07-01 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
US20120129189A1 (en) * 2009-07-17 2012-05-24 Chulan Kwon Methods of Controlling Cell Proliferation
US20120225862A1 (en) * 2009-07-21 2012-09-06 Auckland Univservices Limited Heteroaryl benzamides, compositions and methods of use
US8486940B2 (en) 2009-09-11 2013-07-16 Probiodrug Ag Inhibitors
US9181233B2 (en) 2010-03-03 2015-11-10 Probiodrug Ag Inhibitors of glutaminyl cyclase
EP2545047B9 (en) 2010-03-10 2015-06-10 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
EP2686313B1 (en) 2011-03-16 2016-02-03 Probiodrug AG Benzimidazole derivatives as inhibitors of glutaminyl cyclase
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WO2002024649A1 (en) * 2000-09-25 2002-03-28 Actelion Pharmaceuticals Ltd Substituted amino-aza-cycloalkanes useful against malaria
CA2455861A1 (en) * 2001-08-03 2003-02-20 Schering Corporation Sulfonamide derivatives as gamma secretase inhibitors

Also Published As

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

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Legal Events

Date Code Title Description
FZDE Discontinued