[go: up one dir, main page]

HN2008000738A - Compuestos para la inhibicion de enzimas - Google Patents

Compuestos para la inhibicion de enzimas

Info

Publication number
HN2008000738A
HN2008000738A HN2008000738A HN2008000738A HN2008000738A HN 2008000738 A HN2008000738 A HN 2008000738A HN 2008000738 A HN2008000738 A HN 2008000738A HN 2008000738 A HN2008000738 A HN 2008000738A HN 2008000738 A HN2008000738 A HN 2008000738A
Authority
HN
Honduras
Prior art keywords
enzymes
inhibition
compounds
peptide
terminal
Prior art date
Application number
HN2008000738A
Other languages
English (en)
Inventor
Hand-Jie Zhou
Congcong M Sun
Guy J Llaiding
Original Assignee
Proteolix 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 Proteolix Inc filed Critical Proteolix Inc
Publication of HN2008000738A publication Critical patent/HN2008000738A/es

Links

Classifications

    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/69Boron compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06Tripeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/55Protease inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • 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
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • 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
    • 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
    • C07K5/0606Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
    • 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
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • 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
    • C07K5/0806Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • 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
    • 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
    • C07K5/081Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • 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
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/0821Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • 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
    • C07K5/10Tetrapeptides
    • C07K5/1024Tetrapeptides with the first amino acid being heterocyclic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Neurology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

SE DESCRIBEN COMPUESTOS BASADOS EN EL PEPTIDO QUE INCLUYEN ACTIVIDADES ESPECIFICAS QUE INHIBEN EFICIENTEMENTE Y SELECTIVAMENTE TRES MIEMBROS QUE CONTIENEN HETEROATOMOS DE LAS HIDROLASAS (Ntn) DEL NUCLEOFILO DE TERMINAL N ASOCIADAS CON LA PROTEOSOMA. LOS COMPUESTOS BASADOS EN EL PEPTIDO INCLUYEN UN EPOXIDO O AZIRIDINA Y FUNCIONALIZACION EN LA TERMINAL N.
HN2008000738A 2005-11-09 2008-05-09 Compuestos para la inhibicion de enzimas HN2008000738A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US73611805P 2005-11-09 2005-11-09
US84258206P 2006-09-05 2006-09-05

Publications (1)

Publication Number Publication Date
HN2008000738A true HN2008000738A (es) 2011-11-03

Family

ID=37671954

Family Applications (1)

Application Number Title Priority Date Filing Date
HN2008000738A HN2008000738A (es) 2005-11-09 2008-05-09 Compuestos para la inhibicion de enzimas

Country Status (29)

Country Link
US (8) US7687456B2 (es)
EP (2) EP1948678B1 (es)
JP (3) JP5436860B2 (es)
KR (3) KR101434522B1 (es)
CN (2) CN105237621A (es)
AU (1) AU2006311584B2 (es)
BR (1) BRPI0618468A2 (es)
CA (1) CA2629084C (es)
CY (1) CY1119405T1 (es)
DK (2) DK1948678T3 (es)
EC (1) ECSP088460A (es)
ES (2) ES2415756T3 (es)
GT (1) GT200800063A (es)
HK (1) HK1220208A1 (es)
HN (1) HN2008000738A (es)
HU (1) HUE034863T2 (es)
IL (2) IL191344A (es)
LT (1) LT2623113T (es)
MX (1) MX2008006090A (es)
MY (2) MY171061A (es)
NZ (2) NZ595196A (es)
PH (1) PH12013501656A1 (es)
PL (2) PL1948678T3 (es)
PT (2) PT2623113T (es)
RU (2) RU2453556C2 (es)
SI (1) SI2623113T1 (es)
SV (1) SV2009002903A (es)
WO (1) WO2007056464A1 (es)
ZA (1) ZA200804455B (es)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8198270B2 (en) * 2004-04-15 2012-06-12 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
WO2005105827A2 (en) 2004-04-15 2005-11-10 Proteolix, Inc. Compounds for proteasome enzyme inhibition
JP5108509B2 (ja) * 2004-05-10 2012-12-26 プロテオリックス, インコーポレイテッド 酵素阻害のための化合物
MX2008006090A (es) 2005-11-09 2008-10-23 Proteolix Inc Compuestos para inhibicion de la enzima.
RU2450016C2 (ru) 2006-06-19 2012-05-10 Протеоликс, Инк. Пептидные эпоксикетоны для ингибирования протеасомы
WO2008140782A2 (en) * 2007-05-10 2008-11-20 Proteolix, Inc. Compounds for enzyme inhibition
KR20160086980A (ko) 2007-10-04 2016-07-20 오닉스 세라퓨틱스, 인크. 결정형 펩티드 에폭시 케톤 프로테아제 저해제 및 아미노산 케토-에폭시드의 합성
EP2229138B1 (en) 2007-12-19 2019-08-28 Avon Products, Inc. Topical compositions comprising non-proteogenic amino acids and methods of treating skin
MX2011004225A (es) 2008-10-21 2011-06-21 Onyx Therapeutics Inc Terapia de combinacion con epoxicetonas peptidicas.
AR075899A1 (es) 2009-03-20 2011-05-04 Onyx Therapeutics Inc Tripeptidos epoxicetonas cristalinos inhibidores de proteasa
WO2011060179A1 (en) 2009-11-13 2011-05-19 Onyx Therapeutics, Inc Use of peptide epoxyketones for metastasis suppression
BR112012022060A2 (pt) 2010-03-01 2018-05-08 Onyx Therapeutics Inc composto para a inibição de imunoproteassoma
EP2555621A4 (en) 2010-04-07 2014-07-02 Onyx Therapeutics Inc CRYSTALLINE EPOXYCETONE PEPTIDE IMMUNOPROTEASOME INHIBITOR
WO2013112601A1 (en) 2012-01-24 2013-08-01 Millennium Pharmaceuticals, Inc. Methods of treatment of cancer
WO2013169282A1 (en) * 2012-05-08 2013-11-14 Onyx Therapeutics, Inc. Cylodextrin complexation methods for formulating peptide proteasome inhibitors
WO2014011695A2 (en) 2012-07-09 2014-01-16 Onyx Therapeutics, Inc. Prodrugs of peptide epoxy ketone protease inhibitors
US9441012B2 (en) 2012-08-14 2016-09-13 Trillium Therapeutics Inc. Fluorinated epoxyketone-based compounds and uses thereof as proteasome inhibitors
UY35091A (es) * 2012-10-24 2014-05-30 Onyx Therapeutics Inc Formulaciones de liberacion modificada para oprozomib
EP2970225B1 (en) * 2013-03-14 2018-08-15 Onyx Therapeutics, Inc. Dipeptide and tripeptide epoxy ketone protease inhibitors
AR095426A1 (es) 2013-03-14 2015-10-14 Onyx Therapeutics Inc Inhibidores tripeptídicos de la epoxicetona proteasa
MX372671B (es) 2013-07-19 2020-04-23 Onyx Therapeutics Inc Inhibidores de proteasoma de epoxicetona peptídica en combinacion con inhibidores de cinasa pim para el tratamiento de canceres.
CN104945470B (zh) * 2014-03-30 2020-08-11 浙江大学 杂环构建的三肽环氧酮类化合物及制备和应用
JP6608442B2 (ja) * 2014-07-14 2019-11-20 セントラックス インターナショナル,インコーポレイテッド 酵素阻害に用いられるエポキシケトン化合物
EP3808349B1 (en) 2014-08-07 2022-10-05 Mayo Foundation for Medical Education and Research Compounds and methods for treating cancer
WO2016069479A1 (en) 2014-10-27 2016-05-06 Apicore Us Llc Methods of making carfilzomib and intermediates thereof
US9980976B2 (en) * 2015-02-17 2018-05-29 Northwestern University Use of REDD1 inhibitors to dissociate therapeutic and adverse atrophogenic effects of glucocorticoid receptor agonists
WO2017147410A1 (en) 2016-02-25 2017-08-31 Amgen Inc. Compounds that inhibit mcl-1 protein
SG11201811507YA (en) 2016-06-29 2019-01-30 Kezar Life Sciences Crystalline salts of peptide epoxyketone immunoproteasome inhibitor
KR102524751B1 (ko) 2016-06-29 2023-04-21 케자르 라이프 사이언스 펩티드 에폭시케톤 면역프로테아제 저해제 및 그 전구체의 제조 방법
KR101720736B1 (ko) 2016-12-15 2017-03-28 이숙자 스플린트용 커버 조립체
WO2018160717A1 (en) 2017-02-28 2018-09-07 Mayo Foundation For Medical Education And Research Compounds and methods for treating cancer
BR112020005079A2 (pt) 2017-09-14 2020-09-15 Glaxosmithkline Intellectual Property Development Limited tratamento de combinação para câncer
US10537585B2 (en) 2017-12-18 2020-01-21 Dexcel Pharma Technologies Ltd. Compositions comprising dexamethasone
US11243207B2 (en) 2018-03-29 2022-02-08 Mayo Foundation For Medical Education And Research Assessing and treating cancer
CN110092813B (zh) * 2019-06-05 2021-05-11 南京师范大学 一种三肽环氧丙烷衍生物及其制备方法和用途
KR20220162155A (ko) 2020-04-27 2022-12-07 주식회사 오토텍바이오 Ubr 박스 도메인 리간드로의 화합물
WO2025092827A1 (zh) * 2023-10-30 2025-05-08 上海汇伦医药股份有限公司 一种环氧类化合物及其应用

Family Cites Families (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4733665C2 (en) 1985-11-07 2002-01-29 Expandable Grafts Partnership Expandable intraluminal graft and method and apparatus for implanting an expandable intraluminal graft
US5135919A (en) 1988-01-19 1992-08-04 Children's Medical Center Corporation Method and a pharmaceutical composition for the inhibition of angiogenesis
US5441944A (en) 1989-04-23 1995-08-15 The Trustees Of The University Of Pennsylvania Substituted cyclodextrin sulfates and their uses as growth modulating agents
US5071957A (en) 1989-08-04 1991-12-10 Bristol-Myers Company Antibiotic BU-4061T
US4990448A (en) 1989-08-04 1991-02-05 Bristol-Myers Company Bu-4061T
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
IE910713A1 (en) 1990-03-05 1991-09-11 Cephalon Inc Chymotrypsin-like proteases
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
US5519029A (en) * 1992-09-08 1996-05-21 Boehringer Mannheim Italia, S.P.A. 2-aminoalkyl-5-aminoalkylamino substituted-isoquinoindazole-6(2H)-ones
GB9300048D0 (en) 1993-01-04 1993-03-03 Wellcome Found Endothelin converting enzyme inhibitors
TW380137B (en) 1994-03-04 2000-01-21 Merck & Co Inc Process for making an epoxide
US5693617A (en) 1994-03-15 1997-12-02 Proscript, Inc. Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein
US6660268B1 (en) 1994-03-18 2003-12-09 The President And Fellows Of Harvard College Proteasome regulation of NF-KB activity
US6506876B1 (en) 1994-10-11 2003-01-14 G.D. Searle & Co. LTA4 hydrolase inhibitor pharmaceutical compositions and methods of use
US6083903A (en) 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
DE19505263A1 (de) 1995-02-16 1996-08-22 Consortium Elektrochem Ind Verfahren zur Reinigung von wasserlöslichen Cyclodextrinderivaten
US6335358B1 (en) 1995-04-12 2002-01-01 President And Fellows Of Harvard College Lactacystin analogs
US6150415A (en) 1996-08-13 2000-11-21 The Regents Of The University Of California Epoxide hydrolase complexes and methods therewith
AU4499697A (en) 1996-09-13 1998-04-02 New York University Method for treating parasitic diseases with proteasome inhibitors
DE69709671T2 (de) 1996-10-18 2002-08-22 Vertex Pharmaceuticals Inc., Cambridge Inhibitoren von serinproteasen, insbesondere von ns3-protease des hepatitis-c-virus
SI0932617T1 (en) 1996-10-18 2002-06-30 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
US5874418A (en) 1997-05-05 1999-02-23 Cydex, Inc. Sulfoalkyl ether cyclodextrin based solid pharmaceutical formulations and their use
US6046177A (en) 1997-05-05 2000-04-04 Cydex, Inc. Sulfoalkyl ether cyclodextrin based controlled release solid pharmaceutical formulations
ES2210769T3 (es) 1997-06-13 2004-07-01 Cydex Inc. Compuesto con vida de almacenamiento prolongada que comprende ciclodextrina y medicamentos y promedicamentos que se descomponen en componentes insolubles en agua.
US6133308A (en) 1997-08-15 2000-10-17 Millennium Pharmaceuticals, Inc. Synthesis of clasto-lactacystin beta-lactone and analogs thereof
US6075150A (en) 1998-01-26 2000-06-13 Cv Therapeutics, Inc. α-ketoamide inhibitors of 20S proteasome
US6099851A (en) 1998-06-02 2000-08-08 Weisman; Kenneth M. Therapeutic uses of leuprolide acetate
US6902721B1 (en) 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6462019B1 (en) 1998-07-10 2002-10-08 Osteoscreen, Inc. Inhibitors of proteasomal activity and production for stimulating bone growth
US6838436B1 (en) 1998-07-10 2005-01-04 Osteoscreen Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6204257B1 (en) 1998-08-07 2001-03-20 Universtiy Of Kansas Water soluble prodrugs of hindered alcohols
AU762373B2 (en) 1998-10-20 2003-06-26 Millennium Pharmaceuticals, Inc. Method for monitoring proteasome inhibitor drug action
US6492333B1 (en) 1999-04-09 2002-12-10 Osteoscreen, Inc. Treatment of myeloma bone disease with proteasomal and NF-κB activity inhibitors
US6831099B1 (en) * 1999-05-12 2004-12-14 Yale University Enzyme inhibition
PT1265606E (pt) * 1999-08-13 2007-01-31 Biogen Idec Inc Inibidores da adesão celular
EP1716861A3 (en) 1999-10-20 2007-08-29 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone and hair growth
US20040101781A1 (en) * 2000-09-04 2004-05-27 Nobuhiro Oda Reflecting layer, optical recording medium and sputtering target for forming reflecting layer
DK1326632T3 (da) 2000-10-12 2007-01-15 Viromics Gmbh Protease-inhibitorer til behandling af infektioner af hepatitisvirus
EP1355910B1 (en) 2001-01-25 2011-03-09 The United States of America, represented by the Secretary, Department of Health and Human Services Formulation of boronic acid compounds
WO2002094311A1 (en) 2001-05-21 2002-11-28 Alcon, Inc. Use of proteasome inhibitors to treat dry eye disorders
WO2003059898A2 (en) 2002-01-08 2003-07-24 Eisai Co. Ltd. Eponemycin and epoxomicin analogs and uses thereof
US20040116329A1 (en) 2002-01-29 2004-06-17 Epstein Stephen E. Inhibition of proteasomes to prevent restenosis
AU2003220685A1 (en) 2002-04-09 2003-10-27 Greenville Hospital System Metastasis modulating activity of highly sulfated oligosaccharides
US7968569B2 (en) 2002-05-17 2011-06-28 Celgene Corporation Methods for treatment of multiple myeloma using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione
US20030224469A1 (en) 2002-06-03 2003-12-04 Buchholz Tonia J. Methods and kits for assays utilizing fluorescence polarization
AU2003249682A1 (en) 2002-06-03 2003-12-19 Als Therapy Development Foundation Treatment of neurodegenerative diseases using proteasome modulators
US20040167139A1 (en) 2002-07-26 2004-08-26 Potter David A. Methods of treating cancer
US7189740B2 (en) 2002-10-15 2007-03-13 Celgene Corporation Methods of using 3-(4-amino-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione for the treatment and management of myelodysplastic syndromes
TW200418791A (en) 2003-01-23 2004-10-01 Bristol Myers Squibb Co Pharmaceutical compositions for inhibiting proteasome
CA2521325C (en) 2003-04-08 2010-09-14 Novartis Ag Solid pharmaceutical compositions comprising a s1p receptor agonist and a sugar alcohol
CA2528120A1 (en) 2003-06-10 2005-01-20 The J. David Gladstone Institutes Methods for treating lentivirus infections
US7012063B2 (en) 2003-06-13 2006-03-14 Children's Medical Center Corporation Reducing axon degeneration with proteasome inhibitors
AU2004312096A1 (en) 2003-12-31 2005-07-21 Cydex Pharmaceuticals, Inc. Inhalant formulation containing sulfoalkyl ether gamma-cyclodextrin and corticosteroid
GB0400804D0 (en) 2004-01-14 2004-02-18 Innoscience Technology Bv Pharmaceutical compositions
WO2005105827A2 (en) 2004-04-15 2005-11-10 Proteolix, Inc. Compounds for proteasome enzyme inhibition
US8198270B2 (en) 2004-04-15 2012-06-12 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
US7232818B2 (en) 2004-04-15 2007-06-19 Proteolix, Inc. Compounds for enzyme inhibition
AU2005243140A1 (en) 2004-05-10 2005-11-24 Proteolix, Inc. Synthesis of amino acid keto-epoxides
JP5108509B2 (ja) 2004-05-10 2012-12-26 プロテオリックス, インコーポレイテッド 酵素阻害のための化合物
EP2100899A3 (en) 2004-10-20 2009-09-30 Proteolix, Inc. Compounds for proteasome enzyme inhibition
KR101299821B1 (ko) 2004-12-07 2013-09-03 프로테올릭스, 인코퍼레이티드 프로테아좀 저해를 위한 조성물
US7468383B2 (en) 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
WO2006099261A2 (en) 2005-03-11 2006-09-21 The University Of North Carolina At Chapel Hill Potent and specific immunoproteasome inhibitors
EP1876893B1 (en) 2005-04-15 2012-04-11 Geron Corporation Cancer treatment by combined inhibition of proteasome and telomerase activities
GT200600350A (es) 2005-08-09 2007-03-28 Formulaciones líquidas
MX2008006090A (es) 2005-11-09 2008-10-23 Proteolix Inc Compuestos para inhibicion de la enzima.
AR057227A1 (es) 2005-12-09 2007-11-21 Centocor Inc Metodo para usar antagonistas de il6 con inhibidores del proteasoma
US20070207950A1 (en) 2005-12-21 2007-09-06 Duke University Methods and compositions for regulating HDAC6 activity
WO2007122686A1 (ja) 2006-04-14 2007-11-01 Eisai R & D Management Co., Ltd. ベンズイミダゾール化合物
DE102006026464A1 (de) 2006-06-01 2007-12-06 Virologik Gmbh Innovationszentrum Medizintechnik Und Pharma Pharmazeutische Zusammensetzung zur Behandlung von Virusinfektionen und / oder Tumorerkrankungen durch Inhibition der Proteinfaltung und des Proteinabbaus
RU2450016C2 (ru) 2006-06-19 2012-05-10 Протеоликс, Инк. Пептидные эпоксикетоны для ингибирования протеасомы
WO2008033807A2 (en) 2006-09-13 2008-03-20 The Arizona Board Of Regents On Behalf Of The University Of Arizona Synergistic combinations of antineoplastic thiol-binding mitochondrial oxidants and antineoplastic proteasome inhibitors for the treatment of cancer
EP2117556A2 (en) 2007-01-23 2009-11-18 Gloucester Pharmaceuticals, Inc. Combination therapy comprising romidepsin and i.a. bortezomib
JP4325683B2 (ja) 2007-02-14 2009-09-02 セイコーエプソン株式会社 画像表示装置、及び画像表示装置の制御方法
WO2008140782A2 (en) 2007-05-10 2008-11-20 Proteolix, Inc. Compounds for enzyme inhibition
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
KR20150010802A (ko) 2007-08-06 2015-01-28 밀레니엄 파머슈티컬스 인코퍼레이티드 프로테아좀 억제제
KR20160086980A (ko) 2007-10-04 2016-07-20 오닉스 세라퓨틱스, 인크. 결정형 펩티드 에폭시 케톤 프로테아제 저해제 및 아미노산 케토-에폭시드의 합성
WO2009051581A1 (en) 2007-10-16 2009-04-23 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
US7838673B2 (en) 2007-10-16 2010-11-23 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
US20090131367A1 (en) 2007-11-19 2009-05-21 The Regents Of The University Of Colorado Combinations of HDAC Inhibitors and Proteasome Inhibitors
KR101691093B1 (ko) 2008-06-17 2016-12-29 밀레니엄 파머슈티컬스 인코퍼레이티드 보로네이트 에스테르 화합물 및 이의 제약학적 조성물
AR075090A1 (es) 2008-09-29 2011-03-09 Millennium Pharm Inc Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden.
MX2011004225A (es) 2008-10-21 2011-06-21 Onyx Therapeutics Inc Terapia de combinacion con epoxicetonas peptidicas.
AR075899A1 (es) 2009-03-20 2011-05-04 Onyx Therapeutics Inc Tripeptidos epoxicetonas cristalinos inhibidores de proteasa
CN101928329B (zh) 2009-06-19 2013-07-17 北京大学 三肽硼酸(酯)类化合物、其制备方法和应用
WO2011060179A1 (en) 2009-11-13 2011-05-19 Onyx Therapeutics, Inc Use of peptide epoxyketones for metastasis suppression
BR112012022060A2 (pt) 2010-03-01 2018-05-08 Onyx Therapeutics Inc composto para a inibição de imunoproteassoma
MX2012011298A (es) 2010-03-31 2012-11-06 Millennium Pharm Inc Derivados del acido 1-amino-2-ciclopropiletilboronico.
EP2555621A4 (en) 2010-04-07 2014-07-02 Onyx Therapeutics Inc CRYSTALLINE EPOXYCETONE PEPTIDE IMMUNOPROTEASOME INHIBITOR

Also Published As

Publication number Publication date
KR101275445B1 (ko) 2013-06-14
PT1948678E (pt) 2013-07-16
ES2628620T3 (es) 2017-08-03
JP5799060B2 (ja) 2015-10-21
RU2453556C2 (ru) 2012-06-20
CY1119405T1 (el) 2018-03-07
RU2012110718A (ru) 2013-09-27
HUE034863T2 (en) 2018-03-28
US7687456B2 (en) 2010-03-30
GT200800063A (es) 2009-03-12
JP2009514971A (ja) 2009-04-09
US20160083421A1 (en) 2016-03-24
EP2623113A3 (en) 2014-04-16
PL1948678T3 (pl) 2013-09-30
JP2012255012A (ja) 2012-12-27
CN101405294A (zh) 2009-04-08
US8716322B2 (en) 2014-05-06
CN105237621A (zh) 2016-01-13
MY145757A (en) 2012-04-13
US20090203698A1 (en) 2009-08-13
US20170260230A1 (en) 2017-09-14
AU2006311584B2 (en) 2012-03-08
ZA200804455B (en) 2009-05-27
US20140051641A1 (en) 2014-02-20
KR101434522B1 (ko) 2014-08-26
CA2629084C (en) 2015-08-11
MX2008006090A (es) 2008-10-23
KR20080070049A (ko) 2008-07-29
NZ568068A (en) 2011-10-28
PL2623113T3 (pl) 2018-05-30
ES2415756T3 (es) 2013-07-26
CN101405294B (zh) 2015-11-25
RU2008122779A (ru) 2009-12-20
US20140050737A1 (en) 2014-02-20
KR20130041367A (ko) 2013-04-24
US20130130968A1 (en) 2013-05-23
BRPI0618468A2 (pt) 2011-08-30
SI2623113T1 (sl) 2017-08-31
EP1948678B1 (en) 2013-05-01
JP2014028808A (ja) 2014-02-13
KR101274417B1 (ko) 2013-06-17
DK1948678T3 (da) 2013-06-24
US9205124B2 (en) 2015-12-08
IL191344A (en) 2015-11-30
PT2623113T (pt) 2017-07-14
JP5436860B2 (ja) 2014-03-05
US20140031297A1 (en) 2014-01-30
MY171061A (en) 2019-09-24
US9205125B2 (en) 2015-12-08
SV2009002903A (es) 2009-02-17
IL242282A0 (en) 2015-11-30
NZ595196A (en) 2013-03-28
HK1220208A1 (zh) 2017-04-28
LT2623113T (lt) 2017-07-10
PH12013501656A1 (en) 2016-02-01
WO2007056464A1 (en) 2007-05-18
IL242282B (en) 2018-06-28
ECSP088460A (es) 2008-08-29
KR20120117003A (ko) 2012-10-23
US20070105786A1 (en) 2007-05-10
HK1121172A1 (en) 2009-04-17
EP2623113A2 (en) 2013-08-07
EP1948678A1 (en) 2008-07-30
AU2006311584A1 (en) 2007-05-18
DK2623113T3 (en) 2017-07-17
US10150794B2 (en) 2018-12-11
EP2623113B1 (en) 2017-05-31
US9205126B2 (en) 2015-12-08
JP5778097B2 (ja) 2015-09-16
CA2629084A1 (en) 2007-05-18

Similar Documents

Publication Publication Date Title
HN2008000738A (es) Compuestos para la inhibicion de enzimas
CR8402A (es) Indazol-o-glucosidos sustitutos
ECSP088440A (es) Imidazopirazinas como inhibidores de proteinquinasa
ECSP078013A (es) Inhibidores heterocíclicos de mek y métodos de uso de ellos
NO20082191L (no) Forbindelser
CR9664A (es) Inhibidores de histona deacetilasa
CL2008001879A1 (es) Compuestos derivados de isaxolinas-naftalen-carboamida; y el uso de los compuestos en el control de plagas de invertebrados en animales.
ECSP109940A (es) Anticuerpos anti-cd79b e inmunoconjugados humanizados y métodos de uso
EP1963530A4 (en) ACTIVE SURFACE COATED POLYMERASES
CL2008002430A1 (es) Compuestos derivados de bencenosulfonamida, inhibidores de catepsina c; composicion farmaceutica que los comprende; y su uso para el tratamiento de la epoc.
CR11216A (es) Anticuerpos anti-cd79b e inmmunoconjugados y metodos de uso de los mismos
CR20140422A (es) Composiciones de enzima digestiva estable
CR9869A (es) Compuestos activos en ppar
ECSP088503A (es) COMPUESTOS de LACTAMa y MÉTODOS DE USO DE LOS MISMOS
NI200900187A (es) Polipeptidos de factor vii modificados y usos de los mismos.
CL2007002383A1 (es) Uso de compuestos derivados de 2,5-dihidroxibenceno, sus sales, solvatos o isomeros y uso de la combinacion con otros compuestos activos tales como esteroides, antiinflamatorios, antibioticos, antioxidantes, inmunomoduladores, entre otros, para el tratamiento o profilaxis de la rosacea.
CL2007001391A1 (es) Compuestos derivados de pirrolidinas sustituidas, inhibidores del factor xa y/o inhibidores sobre la serina proteasa; composicion farmaceutica que comprende a dichos compuestos; proedimiento para preparar la composicon farmaceutica; y uso de los compuestos preparar un medicamneto con un efecto antitrombotico
UY27894A1 (es) Derivados de cinamida.
CL2008001560A1 (es) Compuestos derivados de heterociclo de nitrogenado, moduladores de gamma secretasa; composicion farmaceutica que los comprende; y su uso en el tratamiento de enfermedades neurodegenerativas como el alzheimer, sindrome de down; kit farmaceutico.
CL2023000524A1 (es) Compuestos fosfolípidos y usos de los mismos
CL2019000631A1 (es) Módulo flotante para plataformas de paneles solares modulares.
EA200970407A1 (ru) Ингибиторы киназ mapk/erk
MX2020012803A (es) Metodos y composiciones esporicidas.
DE502006004472D1 (de) Organische elektrolumineszenzvorrichtungen
EA201000566A1 (ru) Гетероциклические сетр ингибиторы