KR100648578B1 - α-케토아미드 다촉매활성의 프로테아제 억제제 - Google Patents

α-케토아미드 다촉매활성의 프로테아제 억제제 Download PDF

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Publication number
KR100648578B1
KR100648578B1 KR1020007003684A KR20007003684A KR100648578B1 KR 100648578 B1 KR100648578 B1 KR 100648578B1 KR 1020007003684 A KR1020007003684 A KR 1020007003684A KR 20007003684 A KR20007003684 A KR 20007003684A KR 100648578 B1 KR100648578 B1 KR 100648578B1
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compound
group
phenyl
aryl
alkyl
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Korean (ko)
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KR20010030944A (ko
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산카 샤터지
존 피. 말라모
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세파론, 인코포레이티드
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • 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
    • C07D403/12Heterocyclic 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 chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020007003684A 1997-10-07 1998-10-07 α-케토아미드 다촉매활성의 프로테아제 억제제 Expired - Fee Related KR100648578B1 (ko)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US6138297P 1997-10-07 1997-10-07
US60/061,382 1997-10-07
US09/167,163 US6096778A (en) 1997-10-07 1998-10-06 α-ketoamide multicatalytic protease inhibitors
US9/167,163 1998-10-06
US09/167,163 1998-10-06
PCT/US1998/021053 WO1999017778A1 (en) 1997-10-07 1998-10-07 α-KETOAMIDE MULTICATALYTIC PROTEASE INHIBITORS

Publications (2)

Publication Number Publication Date
KR20010030944A KR20010030944A (ko) 2001-04-16
KR100648578B1 true KR100648578B1 (ko) 2006-11-24

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KR1020007003684A Expired - Fee Related KR100648578B1 (ko) 1997-10-07 1998-10-07 α-케토아미드 다촉매활성의 프로테아제 억제제

Country Status (12)

Country Link
US (2) US6096778A (https=)
EP (1) EP1027056B1 (https=)
JP (1) JP4317920B2 (https=)
KR (1) KR100648578B1 (https=)
CN (1) CN1172672C (https=)
AT (1) ATE423562T1 (https=)
AU (1) AU751963B2 (https=)
CA (1) CA2303428C (https=)
DE (1) DE69840603D1 (https=)
ES (1) ES2321249T3 (https=)
NZ (1) NZ503308A (https=)
WO (1) WO1999017778A1 (https=)

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US6150378A (en) * 1997-10-07 2000-11-21 Cephalon, Inc. Peptidyl-containing α-ketoamide cysteine and serine protease inhibitors
US6902721B1 (en) * 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6455587B1 (en) * 2000-03-15 2002-09-24 Pharmacor Inc. Amino acid derivatives as HIV aspartyl protease inhibitors
JP4666440B2 (ja) * 2000-06-30 2011-04-06 生化学工業株式会社 アミノアルコール誘導体
AU2001267886A1 (en) 2000-06-30 2002-01-14 Seikagaku Corporation Epoxycarboxylic acid amides, azides and amino alcohols and processes for preparation of alpha-keto amides by using them
FR2813315B1 (fr) 2000-08-23 2002-10-18 Genfit S A Procede d'identification de substances utiles pour le traitement de l'inflammation mettant en oeuvre l'element de reponse du recepteur ror du gene ikbalpha
EP1465862A1 (en) 2002-01-17 2004-10-13 SmithKline Beecham Corporation Cycloalkyl ketoamides derivatives useful as cathepsin k inhibitors
US7223745B2 (en) * 2003-08-14 2007-05-29 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7576206B2 (en) 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7468383B2 (en) * 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US20070027067A1 (en) * 2005-05-13 2007-02-01 Felicia Etzkorn Transition-state Inhibitors of Pin1, alpha-Ketoamide-containing peptidomimetics, and synthesis thereof
EP2095828A1 (en) * 2008-02-29 2009-09-02 Gnosis S.p.A. Use of S-adenosylmethionine (SAM) and superoxide dismutase (SOD) for the preparation of medicaments for the treatment of Alzeimer's disease
US20110111417A1 (en) 2008-05-14 2011-05-12 Millennium Pharmaceuticals, Inc. Methods and kits for monitoring the effects of immunomodulators on adaptive immunity
EP3656385A1 (en) 2008-05-28 2020-05-27 ReveraGen BioPharma, Inc. Non-hormonal steroid modulators of nf-kb for treatment of disease
WO2010096574A1 (en) 2009-02-20 2010-08-26 Lisanti Michael P A method of diagnosis or prognosis of a neoplasm comprising determining the level of expression of a protein in stromal cells adjacent to the neoplasm
US20120301463A1 (en) 2009-09-30 2012-11-29 President And Fellows Of Harvard College Methods for Modulation of Autophagy Through the Modulation of Autophagy-Enhancing Gene Products
AU2010341530B2 (en) 2009-12-22 2016-03-10 Cephalon, Inc. Proteasome inhibitors and processes for their preparation, purification and use
EP2556083A4 (en) 2010-04-05 2013-12-04 Validus Biopharma Inc NONHORMONAL STEROID MODULATORS OF NF-KAPPA-B FOR DISEASE TREATMENT
AU2012294493B2 (en) 2011-08-11 2017-02-23 Janssen Pharmaceutica Nv Predictors for cancer treatment
JP6238900B2 (ja) 2011-10-28 2017-11-29 ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. Nae阻害物質に対する応答のバイオマーカー
CN104126017A (zh) 2011-11-11 2014-10-29 米伦纽姆医药公司 对蛋白酶体抑制剂的反应的生物标记
CA2862492A1 (en) 2012-01-24 2013-08-01 Millennium Pharmaceuticals, Inc. Methods of treatment of cancer
WO2013112881A1 (en) 2012-01-27 2013-08-01 Thomas Jefferson University Mct protein inhibitor-related prognostic and therapeutic methods
EP2904115B1 (en) 2012-10-01 2018-08-08 Millennium Pharmaceuticals, Inc. Biomarkers and methods to predict response to inhibitors and uses thereof
US10022372B2 (en) 2013-04-19 2018-07-17 Thomas Jefferson University Caveolin-1 related methods for treating glioblastoma with temozolomide
US10799514B2 (en) 2015-06-29 2020-10-13 Reveragen Biopharma, Inc. Non-hormonal steroid modulators of NF-kappa beta for treatment of disease
US11382922B2 (en) 2019-03-07 2022-07-12 Reveragen Biopharma, Inc. Aqueous oral pharmaceutical suspension compositions

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5550262A (en) * 1994-11-14 1996-08-27 Cephalon, Inc. Multicatalytic protease inhibitors

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US5034376A (en) * 1986-10-31 1991-07-23 Pfizer Inc. Nor-statine and nor-cyclostatine polypeptides
US5162500A (en) * 1989-04-15 1992-11-10 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Poststatin and related compounds or salts thereof
US5340825A (en) * 1990-08-31 1994-08-23 Warner-Lambert Company Pro drugs for CCK antagonists
US5444042A (en) * 1990-12-28 1995-08-22 Cortex Pharmaceuticals Method of treatment of neurodegeneration with calpain inhibitors
US5340736A (en) * 1991-05-13 1994-08-23 The President & Fellows Of Harvard College ATP-dependent protease and use of inhibitors for same in the treatment of cachexia and muscle wasting
US5650508A (en) * 1991-12-27 1997-07-22 Georgia Tech Research Corporation Peptide ketoamides
US5514694A (en) * 1992-09-21 1996-05-07 Georgia Tech Research Corp Peptidyl ketoamides
US5434265A (en) * 1992-12-22 1995-07-18 Eli Lilly And Company Inhibitors of HIV protease
US5563127A (en) * 1993-03-24 1996-10-08 The Dupont Merck Pharmaceutical Company Boronic acid and ester inhibitors of thrombin
US5658885A (en) * 1993-04-27 1997-08-19 The Dupont Merck Pharmaceutical Company Amidino and guanidino substituted boronic acid inhibitors of trypsin-like enzymes
US5541290A (en) * 1993-06-24 1996-07-30 Harbeson; Scott L. Optically pure calpain inhibitor compounds
DE4331134A1 (de) * 1993-09-14 1995-03-16 Bayer Ag Neue antiviral wirksame Pseudopeptide
US5614649A (en) * 1994-11-14 1997-03-25 Cephalon, Inc. Multicatalytic protease inhibitors
FI974437A7 (fi) * 1995-06-06 1997-12-05 Pfizer Substituoituja N-(indoli-2-karbonyyli)amideja ja johdannaisia glykogee nifosforylaasi-inhibiittoreina
US5919765A (en) * 1995-06-07 1999-07-06 Cor Therapeutics, Inc. Inhibitors of factor XA

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
US5550262A (en) * 1994-11-14 1996-08-27 Cephalon, Inc. Multicatalytic protease inhibitors

Also Published As

Publication number Publication date
EP1027056A1 (en) 2000-08-16
CN1274285A (zh) 2000-11-22
EP1027056A4 (en) 2001-03-21
AU751963B2 (en) 2002-09-05
AU1068599A (en) 1999-04-27
CA2303428C (en) 2011-05-24
JP4317920B2 (ja) 2009-08-19
ATE423562T1 (de) 2009-03-15
CN1172672C (zh) 2004-10-27
CA2303428A1 (en) 1999-04-15
US6310057B1 (en) 2001-10-30
US6096778A (en) 2000-08-01
EP1027056B1 (en) 2009-02-25
ES2321249T3 (es) 2009-06-03
JP2002516817A (ja) 2002-06-11
HK1028568A1 (en) 2001-02-23
KR20010030944A (ko) 2001-04-16
WO1999017778A1 (en) 1999-04-15
NZ503308A (en) 2001-02-23
DE69840603D1 (de) 2009-04-09

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