CA2455861A1 - Sulfonamide derivatives as gamma secretase inhibitors - Google Patents

Sulfonamide derivatives as gamma secretase inhibitors Download PDF

Info

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

Links

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
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
CN1780621A (zh) * 2001-08-03 2006-05-31 先灵公司 作为γ分泌酶抑制剂的磺酰胺衍生物
US7399775B2 (en) 2001-12-27 2008-07-15 Daiichi Pharmaceutical Co., Ltd. β-amyloid protein production/secretion inhibitor
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
CN100372838C (zh) * 2003-02-17 2008-03-05 弗·哈夫曼-拉罗切有限公司 哌啶-苯磺酰胺衍生物
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
EP1660443B1 (en) 2003-08-08 2009-03-04 Schering Corporation Cyclic amine bace-1 inhibitors having a benzamide substituent
MXPA06001558A (es) 2003-08-08 2006-05-15 Schering Corp Inhibidores de amina ciclica bace-1 que poseen un sustituyente heterociclico.
CA2544350A1 (en) 2003-10-29 2005-05-12 Elan Pharmaceuticals, Inc. N-substituted benzene sulfonamides
ATE552851T1 (de) 2004-02-03 2012-04-15 Univ Michigan Zusammensetzungen zur behandlung von brust- und bauchspeicheldrüsenkrebs
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
KR20070010144A (ko) * 2004-04-05 2007-01-22 쉐링 코포레이션 신규한 감마 세크레타제 억제제
US7714021B2 (en) * 2004-06-15 2010-05-11 Merck & Co., Inc. Pyrrolidin-3-yl compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
CN101602741A (zh) * 2004-06-30 2009-12-16 先灵公司 作为γ-分泌酶抑制剂的取代的N-芳基磺酰基杂环胺
ATE491693T1 (de) 2004-07-22 2011-01-15 Schering Corp Substituierte amide als inhibitoren der beta- sekretase
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
US7723112B2 (en) 2005-10-31 2010-05-25 The Regents Of The University Of Michigan Compositions and methods for treating and diagnosing cancer
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
TW200812963A (en) 2006-04-13 2008-03-16 Euro Celtique Sa Benzenesulfonamide compounds and the use thereof
TW200815353A (en) 2006-04-13 2008-04-01 Euro Celtique Sa Benzenesulfonamide compounds and their use
EP2041181B1 (en) * 2006-06-08 2011-05-18 Helmholtz Zentrum München Deutsches Forschungszentrum für Gesundheit und Umwelt (GmbH) Specific protease inhibitors and their use in cancer therapy
US8173423B2 (en) 2006-11-07 2012-05-08 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
JP5523107B2 (ja) 2006-11-30 2014-06-18 プロビオドルグ エージー グルタミニルシクラーゼの新規阻害剤
WO2008092002A2 (en) 2007-01-24 2008-07-31 The Regents Of The University Of Michigan Compositions and methods for treating and diagnosing pancreatic cancer
EP2481408A3 (en) 2007-03-01 2013-01-09 Probiodrug AG New use of glutaminyl cyclase inhibitors
US8399486B2 (en) 2007-04-09 2013-03-19 Purdue Pharma L.P. Benzenesulfonyl compounds and the use thereof
WO2008128985A1 (en) 2007-04-18 2008-10-30 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
US8765736B2 (en) 2007-09-28 2014-07-01 Purdue Pharma L.P. Benzenesulfonamide compounds and the use thereof
US20100286164A1 (en) * 2007-10-12 2010-11-11 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
ES2547072T3 (es) * 2009-07-21 2015-10-01 The Board Of Trustees Of The Leland Stanford Junior University Heteroaril benzamidas, composiciones y métodos de utilización
MX2012002993A (es) 2009-09-11 2012-04-19 Probiodrug Ag Derivados heterociclicos como inhibidores de ciclasa glutaminilo.
EP2493497A4 (en) 2009-11-01 2013-07-24 Brigham & Womens Hospital NOTCH INHIBITION IN THE TREATMENT AND PROPHYLAXIS OF ADIPOSITAS AND METABOLISM SYNDROME
JP6026284B2 (ja) 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
US8269019B2 (en) 2010-03-10 2012-09-18 Probiodrug Ag Inhibitors
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
ES2570167T3 (es) 2011-03-16 2016-05-17 Probiodrug Ag Derivados de benzimidazol como inhibidores de glutaminil ciclasa
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
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
WO2020016377A1 (en) 2018-07-19 2020-01-23 INSERM (Institut National de la Santé et de la Recherche Médicale) 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
MXPA01008606A (es) * 1999-02-26 2003-05-05 Merck & Co Inc Compuestos de sulfonamida novedosos y uso de los mismos.
FR2802206B1 (fr) * 1999-12-14 2005-04-22 Sod Conseils Rech Applic Derives de 4-aminopiperidine et leur utilisation en tant que medicament
WO2001081308A2 (en) * 2000-04-20 2001-11-01 Nps Allelix Corp. Aminopiperidines for use as glyt-1 inhibitors
AU2001291830A1 (en) * 2000-09-25 2002-04-02 Actelion Pharmaceuticals Ltd. Substituted amino-aza-cycloalkanes useful against malaria
CN1780621A (zh) * 2001-08-03 2006-05-31 先灵公司 作为γ分泌酶抑制剂的磺酰胺衍生物

Also Published As

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

Similar Documents

Publication Publication Date Title
US20030216380A1 (en) Novel gamma secretase inhibitors
AU705851B2 (en) Aroyl-piperidine derivatives
EP3573983B1 (en) N-[4-fluoro-5-[[(2s,4s)-2-methyl-4-[(5-methyl-1,2,4-oxadiazol-3-yl)methoxy]-1-piperidyl]methyl]thiazol-2-yl]acetamide as oga inhibitor
AU719990B2 (en) Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
AU2003210865B2 (en) Gamma secretase inhibitors
JP4012068B2 (ja) ムスカリンアンタゴニスト
CA2551686C (en) Stereoisomeric compounds and methods for the treatment of gastrointestinal and central nervous system disorders
CA2455863C (en) Tetrahydroquinoline derivatives as gamma secretase inhibitors
EP4089083A1 (en) Piperidine-2,6-dione substituted isoindoles in the preparation of substituted quinoline-8-carbonitrile derivatives having androgen receptor degradation activity and uses thereof
JP4558331B2 (ja) 三環式トロンビンレセプターアンタゴニスト
ES2266171T3 (es) Compuestos de amida y su uso.
TWI838430B (zh) 作為vanin抑制劑之雜芳族化合物
JP2002523451A (ja) カリウムチャネル抑制剤および方法
JP2016510033A (ja) 強力なｒｏｃｋ１およびｒｏｃｋ２阻害剤としてのフェニルピラゾール誘導体
CA3117849A1 (en) Trifluoromethyl-substituted sulfonamide as bcl-2-selective inhibitor
EA005943B1 (ru) Ингибиторы серинпротеазы
AU2019242518B2 (en) Compound with anticancer activity
US6204265B1 (en) Substituted oximes and hydrazones as neurokinin antagonists
AU2006284601B2 (en) Synthetic methods and intermediates for stereoisomeric compounds useful for the treatment of gastrointestinal and central nervous system disorders
WO2004002483A1 (en) Substituted 3- and 4- aminomethylpiperidines for use as beta-secretase in the treatment of alzheimer’s disease
EP1144402B1 (en) Substituted oximes and hydrazones as neurokinin antagonists
JPH08511277A (ja) ｎ−アリール脂肪族−ｎ−アルキルで機能化された新規なアミド、これらを製造する方法及びこれらが存在する薬学的組成物
WO2003010160A2 (en) 1-glycinyl-4 (methylpiperidin-4-yl) piperazines and -piperridines as factor xa antagonists
JP2013501800A (ja) カテプシンｃ阻害剤
JPH08511276A (ja) 置換された窒素性ヘテロ芳香族化合物の塩、これらの製造方法及びこれらを含有する薬学的組成物

Legal Events

Date Code Title Description
FZDE Discontinued