JP2005504042A - γセクレターゼインヒビターのようなスルホンアミド誘導体 - Google Patents

γセクレターゼインヒビターのようなスルホンアミド誘導体 Download PDF

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Publication number
JP2005504042A
JP2005504042A JP2003518536A JP2003518536A JP2005504042A JP 2005504042 A JP2005504042 A JP 2005504042A JP 2003518536 A JP2003518536 A JP 2003518536A JP 2003518536 A JP2003518536 A JP 2003518536A JP 2005504042 A JP2005504042 A JP 2005504042A
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JP
Japan
Prior art keywords
alkyl
aryl
alkylene
heteroaryl
substituted
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Pending
Application number
JP2003518536A
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English (en)
Japanese (ja)
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JP2005504042A5 (enExample
Inventor
ヒュバート ビー. ジョシエン,
ジョン ダブリュー. クレイダー,
テオドロス アズベロン,
ドミトリ エー. ピサニツキ,
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
Schering Corp
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Application filed by Schering Corp filed Critical Schering Corp
Publication of JP2005504042A publication Critical patent/JP2005504042A/ja
Publication of JP2005504042A5 publication Critical patent/JP2005504042A5/ja
Pending legal-status Critical Current

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    • 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

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  • 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)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
JP2003518536A 2001-08-03 2002-08-01 γセクレターゼインヒビターのようなスルホンアミド誘導体 Pending JP2005504042A (ja)

Applications Claiming Priority (2)

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

Publications (2)

Publication Number Publication Date
JP2005504042A true JP2005504042A (ja) 2005-02-10
JP2005504042A5 JP2005504042A5 (enExample) 2006-01-05

Family

ID=23200871

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2003518536A Pending JP2005504042A (ja) 2001-08-03 2002-08-01 γセクレターゼインヒビターのようなスルホンアミド誘導体

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)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006501295A (ja) * 2002-10-04 2006-01-12 メルク シャープ エンド ドーム リミテッド ガンマ−セクレターゼ阻害剤としてのシクロヘキシルスルホン
JP2006501292A (ja) * 2002-10-04 2006-01-12 メルク シャープ エンド ドーム リミテッド ガンマ−セクレターゼインヒビターとしてのシクロヘキシルスルホン誘導体
JP2013500254A (ja) * 2009-07-21 2013-01-07 ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティ ヘテロアリールベンズアミド、組成物および使用の方法

Families Citing this family (48)

* 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
US7122675B2 (en) * 2001-08-03 2006-10-17 Schering Corporation Gamma secretase inhibitors
KR100927304B1 (ko) 2001-12-27 2009-11-18 다이이찌 세이야꾸 가부시기가이샤 β-아밀로이드 단백 생산·분비 저해제
SI1594840T1 (sl) 2003-02-17 2006-12-31 Hoffmann La Roche Derivati piperidin-benzensulfonamida
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
PL379466A1 (pl) 2003-06-30 2006-09-18 Daiichi Sankyo Company , Limited Heterocykliczne pochodne metylosulfonu
AR045219A1 (es) 2003-08-08 2005-10-19 Pharmacopeia Inc Aminas ciclicas inhibidoras de base - 1 que poseen un sustiuyente heterociclico
WO2005016876A2 (en) 2003-08-08 2005-02-24 Schering Corporation Cyclic amine bace-1 inhibitors having a benzamide substituent
CA2544350A1 (en) * 2003-10-29 2005-05-12 Elan Pharmaceuticals, Inc. N-substituted benzene sulfonamides
EP2369014A1 (en) 2004-02-03 2011-09-28 The Regents Of The University Of Michigan Office Of Technology Transfer Compositions and methods for characterizing, regulating, diagnosing and treating cancer
WO2005074633A2 (en) * 2004-02-03 2005-08-18 The Regents Of The University Of Michigan Compositions and methods for characterizing, regulating, diagnosing, and treating cancer
WO2005097768A2 (en) * 2004-04-05 2005-10-20 Schering Corporation Novel gamma secretase inhibitors
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
PE20060481A1 (es) * 2004-06-30 2006-06-19 Schering Corp N-arilsulfonilaminas heterociclicas sustituidas como inhibidores de gamma-secretasas
CA2574218A1 (en) 2004-07-22 2006-02-09 Schering Corporation Substituted amide beta secretase inhibitors
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
CA2628255C (en) 2005-10-31 2016-04-19 The Regents Of The University Of Michigan Compositions and methods for treating and diagnosing cancer
WO2007103114A2 (en) 2006-03-07 2007-09-13 The Brigham & Women's Hospital, Inc. Notch inhibition in the treatment or prevention of atherosclerosis
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
WO2007110449A1 (en) 2006-03-29 2007-10-04 Euro-Celtique S.A. 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
DK2041181T3 (da) * 2006-06-08 2011-08-29 Helmholtz Zentrum Muenchen Specifikke proteaseinhibitorer og deres anvendelse i cancerterapi
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
ATE554085T1 (de) 2006-11-30 2012-05-15 Probiodrug Ag Neue inhibitoren von glutaminylcyclase
WO2008092002A2 (en) 2007-01-24 2008-07-31 The Regents Of The University Of Michigan Compositions and methods for treating and diagnosing pancreatic cancer
JP5930573B2 (ja) 2007-03-01 2016-06-15 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤の新規使用
WO2008124118A1 (en) * 2007-04-09 2008-10-16 Purdue Pharma L.P. Benzenesulfonyl compounds and the use therof
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
US20120129189A1 (en) * 2009-07-17 2012-05-24 Chulan Kwon Methods of Controlling Cell Proliferation
JP5934645B2 (ja) 2009-09-11 2016-06-15 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体
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
NZ602312A (en) 2010-03-10 2014-02-28 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
EP2686313B1 (en) 2011-03-16 2016-02-03 Probiodrug AG Benzimidazole derivatives as inhibitors of glutaminyl cyclase
US9629891B2 (en) 2011-10-17 2017-04-25 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
US10434195B2 (en) 2015-08-03 2019-10-08 Emory University Methylsulfonamide derivatives and uses related thereto
ES2812698T3 (es) 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa
US12485126B2 (en) 2018-07-19 2025-12-02 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
NZ514453A (en) 1999-02-26 2003-04-29 Merck & Co Inc Novel sulfonamide compounds and uses thereof
FR2802206B1 (fr) * 1999-12-14 2005-04-22 Sod Conseils Rech Applic Derives de 4-aminopiperidine et leur utilisation en tant que medicament
EP1296950A2 (en) * 2000-04-20 2003-04-02 NPS Allelix Corp. Aminopiperidines for use as glyt-1 inhibitors
US20040102431A1 (en) * 2000-09-25 2004-05-27 Christoph Boss Substituted amino-aza-cycloalkanes useful against malaria
US7122675B2 (en) * 2001-08-03 2006-10-17 Schering Corporation Gamma secretase inhibitors

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006501295A (ja) * 2002-10-04 2006-01-12 メルク シャープ エンド ドーム リミテッド ガンマ−セクレターゼ阻害剤としてのシクロヘキシルスルホン
JP2006501292A (ja) * 2002-10-04 2006-01-12 メルク シャープ エンド ドーム リミテッド ガンマ−セクレターゼインヒビターとしてのシクロヘキシルスルホン誘導体
JP2013500254A (ja) * 2009-07-21 2013-01-07 ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティ ヘテロアリールベンズアミド、組成物および使用の方法

Also Published As

Publication number Publication date
US20060009467A1 (en) 2006-01-12
US7122675B2 (en) 2006-10-17
CN1780621A (zh) 2006-05-31
EP1411944A1 (en) 2004-04-28
US20030216380A1 (en) 2003-11-20
MXPA04001016A (es) 2004-05-27
WO2003013527A1 (en) 2003-02-20
CA2455861A1 (en) 2003-02-20
AR035260A1 (es) 2004-05-05

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