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ZA99161B - Ó-ketoamide inhibitors of 20S proteasome. - Google Patents

Ó-ketoamide inhibitors of 20S proteasome.

Info

Publication number
ZA99161B
ZA99161B ZA9900161A ZA99161A ZA99161B ZA 99161 B ZA99161 B ZA 99161B ZA 9900161 A ZA9900161 A ZA 9900161A ZA 99161 A ZA99161 A ZA 99161A ZA 99161 B ZA99161 B ZA 99161B
Authority
ZA
South Africa
Prior art keywords
proteasome
ketoamide inhibitors
ketoamide
inhibitors
Prior art date
Application number
ZA9900161A
Other languages
English (en)
Inventor
Lisa Wang
Robert T Lum
Steven R Schow
Alison Joly
Suresh Kerwar
Michael M Wick
Original Assignee
Therapeutics Inc
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 Therapeutics Inc filed Critical Therapeutics Inc
Publication of ZA99161B publication Critical patent/ZA99161B/xx

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043Leu-amino acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
ZA9900161A 1998-01-26 1999-01-11 Ó-ketoamide inhibitors of 20S proteasome. ZA99161B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US09/013,365 US6075150A (en) 1998-01-26 1998-01-26 α-ketoamide inhibitors of 20S proteasome

Publications (1)

Publication Number Publication Date
ZA99161B true ZA99161B (en) 1999-07-28

Family

ID=21759598

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA9900161A ZA99161B (en) 1998-01-26 1999-01-11 Ó-ketoamide inhibitors of 20S proteasome.

Country Status (20)

Country Link
US (2) US6075150A (xx)
EP (1) EP1058689A1 (xx)
JP (1) JP3863370B2 (xx)
KR (1) KR100417888B1 (xx)
CN (1) CN1289340A (xx)
AR (1) AR012781A1 (xx)
AU (1) AU747835B2 (xx)
BR (1) BR9907256A (xx)
CA (1) CA2319150C (xx)
GE (1) GEP20032869B (xx)
HU (1) HUP0100901A3 (xx)
IL (2) IL137475A0 (xx)
NO (1) NO327049B1 (xx)
NZ (1) NZ505892A (xx)
PL (1) PL202504B1 (xx)
RU (1) RU2192429C2 (xx)
TW (1) TW593339B (xx)
UA (1) UA71559C2 (xx)
WO (1) WO1999037666A1 (xx)
ZA (1) ZA99161B (xx)

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US20040202645A1 (en) * 2003-04-08 2004-10-14 Khan Nisar Ahmed Administration of gene-regulatory peptides
US6844315B2 (en) 1998-05-20 2005-01-18 Erasmus Universiteit Rotterdam Immunoregulator
US6902721B1 (en) * 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
EP1300418A1 (en) * 2001-10-04 2003-04-09 Erasmus Universiteit Rotterdam Gene regulation by oligopeptides
US7358330B2 (en) * 2001-03-29 2008-04-15 Biotempt B.V. Immunoregulatory compositions
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US20080318871A1 (en) * 2001-12-21 2008-12-25 Khan Nisar A Treatment of neurological disorders
US20030220261A1 (en) * 2001-12-21 2003-11-27 Khan Nisar Ahmed Treatment of iatrogenic disease
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US7560433B2 (en) 2001-12-21 2009-07-14 Biotempt B.V. Treatment of multiple sclerosis (MS)
US20030220260A1 (en) * 2001-12-21 2003-11-27 Khan Nisar Ahmed Peptide compositions
US7786084B2 (en) * 2001-12-21 2010-08-31 Biotempt B.V. Treatment of burns
US20080242837A1 (en) * 2001-12-21 2008-10-02 Khan Nisar A Peptide compositions
US20040013661A1 (en) * 2001-12-21 2004-01-22 Gert Wensvoort Stratification
US7501391B2 (en) * 2001-12-21 2009-03-10 Biotempt B.V. Treatment of transplant survival
US7282512B2 (en) 2002-01-17 2007-10-16 Smithkline Beecham Corporation Cycloalkyl ketoamides derivatives useful as cathepsin K inhibitors
RU2004133044A (ru) * 2002-04-11 2006-01-27 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ингибиторы сериновых протеаз, в частности, протеазы ns3-ns4a hcv
US7576206B2 (en) * 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7223745B2 (en) * 2003-08-14 2007-05-29 Cephalon, Inc. Proteasome inhibitors and methods of using the same
MY148123A (en) 2003-09-05 2013-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
US20090227505A1 (en) * 2004-01-07 2009-09-10 Biotempt B.V. Methods and uses for protein breakdown products
PT2030981E (pt) * 2004-05-10 2014-10-14 Onyx Therapeutics Inc Compostos para inibição da enzima proteassoma
EP1637529A1 (en) 2004-09-20 2006-03-22 4Sc Ag Novel piperidin-4-yl-thiazole-carboxamide analogues as inhibitors of T-cell proliferation and uses thereof
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
CN101217971B (zh) * 2005-07-05 2011-11-09 比奥滕普特公司 肿瘤的治疗
BRPI0614696A2 (pt) 2005-07-29 2011-04-12 Tibotec Pharm Ltd inibidores macrocìclicos de vìrus da hepatite c
AR055361A1 (es) 2005-07-29 2007-08-22 Medivir Ab Inhibidores macrociclicos del virus de la hepatitis c
KR101434522B1 (ko) * 2005-11-09 2014-08-26 오닉스 세라퓨틱스, 인크. 효소 저해를 위한 화합물
US8594771B2 (en) * 2005-12-28 2013-11-26 General Electric Company Devices and methods for self-administered ECG examinations
EP1864692A1 (en) * 2006-06-07 2007-12-12 Biotempt B.V. Use of peptides for the control of radiation injury
RU2450016C2 (ru) 2006-06-19 2012-05-10 Протеоликс, Инк. Пептидные эпоксикетоны для ингибирования протеасомы
WO2008100140A1 (en) * 2007-02-12 2008-08-21 Biotempt B.V. Treatment of trauma hemorrhage with short oligopeptides
US8859021B2 (en) * 2007-05-14 2014-10-14 Sytheon Skin appearance through gene manipulation
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
SI2207791T2 (sl) * 2007-10-04 2019-09-30 Onyx Therapeutics, Inc. Kristalinični peptidepoksiketonski proteazni inhibitorji in sinteza aminokislinskih ketoepoksidov
US20090325903A1 (en) 2008-06-17 2009-12-31 Millennium Pharmaceuticals, Inc. Boronate ester compounds and pharmaceutical compositions thereof
EP2796134B1 (en) 2008-10-21 2016-12-07 Onyx Therapeutics, Inc. Combination of the peptide epoxyketone proteasome inhibitor carfilzomib with melphalan for use in the treatment of multiple myeloma
US20120190565A1 (en) 2009-02-20 2012-07-26 Pangea Biosciences, Inc. Method Of Diagnosis Or Prognosis Of A Neoplasm Comprising Determining The Level Of Expression Of A Protein In Stromal Cells Adjacent To The Neoplasm
AR075899A1 (es) 2009-03-20 2011-05-04 Onyx Therapeutics Inc Tripeptidos epoxicetonas cristalinos inhibidores de proteasa
EP2498793B1 (en) 2009-11-13 2019-07-10 Onyx Therapeutics, Inc. Oprozomib for use in metastasis suppression
WO2011087822A1 (en) 2009-12-22 2011-07-21 Cephalon, Inc. Proteasome inhibitors and processes for their preparation, purification and use
AU2011223795B2 (en) 2010-03-01 2015-11-05 Onyx Therapeutics, Inc. Compounds for immunoproteasome inhibition
KR20130094185A (ko) 2010-04-07 2013-08-23 오닉스 세라퓨틱스, 인크. 결정성 펩티드 에폭시케톤 면역프로테아좀 저해제
WO2013022935A1 (en) 2011-08-11 2013-02-14 Janssen Pharmaceutica Nv Predictors for cancer treatment
US9827246B2 (en) 2011-10-28 2017-11-28 Millennium Pharmaceuticals, Inc. Biomarkers of response to NAE inhibitors
WO2013071163A2 (en) 2011-11-11 2013-05-16 Millennium Pharamaceuticals, Inc. Biomarkers of response to proteasome inhibitors
US20160008382A1 (en) 2012-01-24 2016-01-14 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
US20140105921A1 (en) 2012-07-09 2014-04-17 Onyx Therapeutics, Inc. Prodrugs of Peptide Epoxy Ketone Protease Inhibitors
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Also Published As

Publication number Publication date
CN1289340A (zh) 2001-03-28
US6075150A (en) 2000-06-13
UA71559C2 (en) 2004-12-15
IL137475A (en) 2006-10-05
RU2192429C2 (ru) 2002-11-10
US6781000B1 (en) 2004-08-24
NO327049B1 (no) 2009-04-14
PL202504B1 (pl) 2009-06-30
AR012781A1 (es) 2000-11-08
TW593339B (en) 2004-06-21
KR100417888B1 (ko) 2004-02-11
HUP0100901A3 (en) 2001-11-28
HUP0100901A2 (hu) 2001-08-28
WO1999037666A1 (en) 1999-07-29
BR9907256A (pt) 2001-10-09
AU747835B2 (en) 2002-05-23
KR20010034381A (ko) 2001-04-25
JP3863370B2 (ja) 2006-12-27
EP1058689A1 (en) 2000-12-13
NO20003807D0 (no) 2000-07-25
NZ505892A (en) 2002-10-25
GEP20032869B (en) 2003-01-27
JP2002501080A (ja) 2002-01-15
CA2319150C (en) 2004-08-31
AU2326799A (en) 1999-08-09
NO20003807L (no) 2000-09-25
CA2319150A1 (en) 1999-07-29
PL343269A1 (en) 2001-08-13
IL137475A0 (en) 2001-07-24

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