SV2009002903A - Compuestos para la inhibicion de enzimas - Google Patents

Compuestos para la inhibicion de enzimas

Info

Publication number
SV2009002903A
SV2009002903A SV2008002903A SV2008002903A SV2009002903A SV 2009002903 A SV2009002903 A SV 2009002903A SV 2008002903 A SV2008002903 A SV 2008002903A SV 2008002903 A SV2008002903 A SV 2008002903A SV 2009002903 A SV2009002903 A SV 2009002903A
Authority
SV
El Salvador
Prior art keywords
peptide
based compounds
inhibition
terminal
compounds
Prior art date
Application number
SV2008002903A
Other languages
English (en)
Inventor
Han-Jie Zhou
Congcong M Sun
Kevin D Sheik
Guy J Laidig
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 SV2009002903A publication Critical patent/SV2009002903A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/69—Boron compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/55—Protease inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/0606—Dipeptides 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/081—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Neurology (AREA)
  • Communicable Diseases (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (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

COMPUESTOS BASADOS EN EL PEPTIDO QUE INCLUYEN ACTIVIDADES ESPECIFICAS QUE INHIBEN EFICIENTEMENTE Y SELECGTIVAMENTE 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- ENTRE OTRAS UTILIDADES TERAPEUTICAS, LOS COMPUESTOS BASADOS EN EL PEPTIDO SE ESPERAN QUE EXHIBAN PROPIEDADES ANTI-INFLAMATORIAS Y INHIBICION DE LA PROLIFERACION. LA ADMINISTRACION ORAL DE LOS INHIBIDORES DE PROTEOSOMA BASADOS EN EL PEPTIDO ES POSIBLE DEBIDO A SUS PERFILES BIODISPONIBLES
SV2008002903A 2005-11-09 2008-05-09 Compuestos para la inhibicion de enzimas SV2009002903A (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
SV2009002903A true SV2009002903A (es) 2009-02-17

Family

ID=37671954

Family Applications (1)

Application Number Title Priority Date Filing Date
SV2008002903A SV2009002903A (es) 2005-11-09 2008-05-09 Compuestos para la inhibicion de enzimas

Country Status (29)

Country Link
US (8) US7687456B2 (es)
EP (2) EP2623113B1 (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) DK2623113T3 (es)
EC (1) ECSP088460A (es)
ES (2) ES2628620T3 (es)
GT (1) GT200800063A (es)
HK (2) HK1121172A1 (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) NZ568068A (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 (36)

* 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
EP1745064B1 (en) 2004-04-15 2011-01-05 Proteolix, Inc. Compounds for proteasome enzyme inhibition
PL2030981T3 (pl) * 2004-05-10 2014-12-31 Onyx Therapeutics Inc Związki do enzymatycznej inhibicji proteasomu
PT2623113T (pt) 2005-11-09 2017-07-14 Onyx Therapeutics Inc Compostos para inibição de enzimas
JP5226679B2 (ja) * 2006-06-19 2013-07-03 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
WO2008140782A2 (en) * 2007-05-10 2008-11-20 Proteolix, Inc. Compounds for enzyme inhibition
EA024437B1 (ru) * 2007-10-04 2016-09-30 Оникс Терапьютикс, Инк. Синтез кето-эпоксидов аминокислот
EP2229138B1 (en) * 2007-12-19 2019-08-28 Avon Products, Inc. Topical compositions comprising non-proteogenic amino acids and methods of treating skin
BRPI0919668A2 (pt) 2008-10-21 2018-05-29 Onyx Therapeutics, Inc. terapia de combinação com epóxi-cetonas de peptídeo
TWI504598B (zh) 2009-03-20 2015-10-21 Onyx Therapeutics Inc 結晶性三肽環氧酮蛋白酶抑制劑
WO2011060179A1 (en) 2009-11-13 2011-05-19 Onyx Therapeutics, Inc Use of peptide epoxyketones for metastasis suppression
EP2542238B1 (en) 2010-03-01 2015-08-12 Onyx Therapeutics, Inc. Compounds for immunoproteasome inhibition
WO2011136905A2 (en) 2010-04-07 2011-11-03 Onyx Therapeutics, Inc. Crystalline peptide epoxyketone immunoproteasome inhibitor
CN104204797B (zh) 2012-01-24 2017-05-31 米伦纽姆医药公司 治疗癌症的方法
US20130303465A1 (en) * 2012-05-08 2013-11-14 Onyx Therapeutics, Inc. Cylodextrin Complexation Methods for Formulating Peptide Proteasome Inhibitors
US9309283B2 (en) 2012-07-09 2016-04-12 Onyx Therapeutics, Inc. Prodrugs of peptide epoxy ketone protease inhibitors
WO2014026282A1 (en) * 2012-08-14 2014-02-20 Abdelmalik Slassi Fluorinated epoxyketone-based compounds and uses thereof as proteasome inhibitors
TW201422255A (zh) * 2012-10-24 2014-06-16 Onyx Therapeutics Inc 用於蛋白酶體抑制劑之調整釋放製劑
DK2970225T3 (en) * 2013-03-14 2018-09-24 Onyx Therapeutics Inc DIPEPTIDE AND TRIPEPTIDE AS EPOXY-KETONE PROTEASE INHIBITORS
AR095426A1 (es) * 2013-03-14 2015-10-14 Onyx Therapeutics Inc Inhibidores tripeptídicos de la epoxicetona proteasa
US20160166632A1 (en) 2013-07-19 2016-06-16 Onyx Therapeutics, Inc. Peptide epoxyketone proteasome inhibitors in combination with pim kinase inhibitors for treatment of cancers
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
US10301273B2 (en) 2014-08-07 2019-05-28 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
ES2944958T3 (es) 2016-06-29 2023-06-27 Kezar Life Sciences Sales cristalinas de inhibidor del inmunoproteasoma de epoxicetona peptídico
KR102571568B1 (ko) 2016-06-29 2023-08-25 케자르 라이프 사이언스 펩티드 에폭시케톤 면역프로테아제 저해제 및 그 전구체의 제조 방법
KR101720736B1 (ko) 2016-12-15 2017-03-28 이숙자 스플린트용 커버 조립체
EP3589659A4 (en) 2017-02-28 2021-03-24 Mayo Foundation for Medical Education and Research CANCER TREATMENT COMPOUNDS AND METHODS
WO2019053611A1 (en) 2017-09-14 2019-03-21 Glaxosmithkline Intellectual Property Development Limited POLY THERAPY FOR THE TREATMENT OF CANCER
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
CN115768744B (zh) * 2020-04-27 2024-06-28 奧土择破利悟 作为ubr盒结构域配体的化合物

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
US4990448A (en) 1989-08-04 1991-02-05 Bristol-Myers Company Bu-4061T
US5071957A (en) 1989-08-04 1991-12-10 Bristol-Myers Company Antibiotic BU-4061T
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
KR0166088B1 (ko) * 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
AU661270B2 (en) 1990-03-05 1995-07-20 Cephalon, Inc. Chymotrypsin-like proteases and their 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
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
WO1998010779A1 (en) 1996-09-13 1998-03-19 New York University Method for treating parasitic diseases with proteasome inhibitors
ES2169880T3 (es) * 1996-10-18 2002-07-16 Vertex Pharma Inhibidores de proteasas de serina, particularmente de la proteasa ns3 del virus de la hepatitis c.
EP1136498A1 (en) 1996-10-18 2001-09-26 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus NS3 protease
US6046177A (en) * 1997-05-05 2000-04-04 Cydex, Inc. Sulfoalkyl ether cyclodextrin based controlled release solid pharmaceutical formulations
US5874418A (en) * 1997-05-05 1999-02-23 Cydex, Inc. Sulfoalkyl ether cyclodextrin based solid pharmaceutical formulations and their use
JP4439596B2 (ja) * 1997-06-13 2010-03-24 サイデクス ファーマシューティカルズ、 インク． 長期の貯蔵寿命を有する、極性薬物又は極性プロドラッグを含有する医薬組成物、及びその製造方法
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
US6838436B1 (en) * 1998-07-10 2005-01-04 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
US6204257B1 (en) * 1998-08-07 2001-03-20 Universtiy Of Kansas Water soluble prodrugs of hindered alcohols
JP4503182B2 (ja) * 1998-10-20 2010-07-14 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 プロテアソーム・インヒビター薬物作用のモニター方法
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
PL354063A1 (en) * 1999-08-13 2003-12-15 Biogen, Inc.Biogen, Inc. Cell adhesion inhibitors
EP1221962A2 (en) 1999-10-20 2002-07-17 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone and hair growth
WO2002021524A1 (fr) * 2000-09-04 2002-03-14 Sony Corporation Couche reflechissante, support d'enregistrement optique et cible de pulverisation cathodique permettant de former une couche reflechissante
AU2002218133A1 (en) 2000-10-12 2002-04-22 Viromics Gmbh Agents for the treatment of viral infections
EP2251344B2 (en) * 2001-01-25 2024-04-24 THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES Formulation of boronic acid compounds
DE60218153T2 (de) * 2001-05-21 2007-06-28 Alcon Inc. Verwendung von proteasom-inhibitoren zur behandlung des trockenen auges
EP1463719A2 (en) * 2002-01-08 2004-10-06 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
EP1496916A2 (en) 2002-04-09 2005-01-19 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
US7902185B2 (en) * 2002-06-03 2011-03-08 Als Therapy Development Foundation, Inc. Treatment of neurodegenerative diseases using proteasome modulators
US20030224469A1 (en) 2002-06-03 2003-12-04 Buchholz Tonia J. Methods and kits for assays utilizing fluorescence polarization
WO2004010937A2 (en) * 2002-07-26 2004-02-05 Advanced Research & Technology Institute At Indiana University Method 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
CN1767819B (zh) 2003-04-08 2010-07-28 诺瓦提斯公司 包含s1p受体激动剂和糖醇的固体药物组合物
EP1639141B1 (en) * 2003-06-10 2011-04-20 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
EP1729724A4 (en) 2003-12-31 2008-07-23 Cydex Inc INHALATION FORMULATION WITH SULFOALKYL ETHER GAMMA CYCLODEXTRIN AND CORTICOSTEROID
GB0400804D0 (en) * 2004-01-14 2004-02-18 Innoscience Technology Bv Pharmaceutical compositions
US7232818B2 (en) * 2004-04-15 2007-06-19 Proteolix, Inc. Compounds for enzyme inhibition
EP1745064B1 (en) 2004-04-15 2011-01-05 Proteolix, Inc. Compounds for proteasome enzyme inhibition
US8198270B2 (en) 2004-04-15 2012-06-12 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
US20050256324A1 (en) 2004-05-10 2005-11-17 Proteolix, Inc. Synthesis of amino acid keto-epoxides
PL2030981T3 (pl) * 2004-05-10 2014-12-31 Onyx Therapeutics Inc Związki do enzymatycznej inhibicji proteasomu
EP1805208A2 (en) * 2004-10-20 2007-07-11 Proteolix, Inc. Labeled compounds for proteasome inhibition
US7737112B2 (en) 2004-12-07 2010-06-15 Onyx Therapeutics, Inc. Composition for enzyme inhibition
US7468383B2 (en) 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
EP1863513A2 (en) * 2005-03-11 2007-12-12 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
PT2623113T (pt) * 2005-11-09 2017-07-14 Onyx Therapeutics Inc Compostos para inibição de enzimas
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
JP5226679B2 (ja) * 2006-06-19 2013-07-03 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
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
JP2010516767A (ja) 2007-01-23 2010-05-20 グラスター ファーマシューティカルズ， インコーポレイテッド ロミデプシンおよびｉ．ａ．ボルテゾミブを含む併用療法
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
DK2178888T3 (da) 2007-08-06 2012-10-01 Millennium Pharm Inc Proteasomhæmmere
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
EA024437B1 (ru) * 2007-10-04 2016-09-30 Оникс Терапьютикс, Инк. Синтез кето-эпоксидов аминокислот
US7838673B2 (en) * 2007-10-16 2010-11-23 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
EP2212334B1 (en) 2007-10-16 2012-08-15 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
WO2009067453A1 (en) 2007-11-19 2009-05-28 Syndax Pharmaceuticals, Inc. Combinations of hdac inhibitors and proteasome inhibitors
EA030685B1 (ru) 2008-06-17 2018-09-28 Милленниум Фармасьютикалз, Инк. Способ получения соединения боронатного эфира
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.
BRPI0919668A2 (pt) 2008-10-21 2018-05-29 Onyx Therapeutics, Inc. terapia de combinação com epóxi-cetonas de peptídeo
TWI504598B (zh) * 2009-03-20 2015-10-21 Onyx Therapeutics Inc 結晶性三肽環氧酮蛋白酶抑制劑
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
EP2542238B1 (en) * 2010-03-01 2015-08-12 Onyx Therapeutics, Inc. Compounds for immunoproteasome inhibition
CN106008570A (zh) 2010-03-31 2016-10-12 米伦纽姆医药公司 1-氨基-2-环丙基乙硼酸衍生物
WO2011136905A2 (en) * 2010-04-07 2011-11-03 Onyx Therapeutics, Inc. Crystalline peptide epoxyketone immunoproteasome inhibitor

Also Published As

Publication number Publication date
JP2014028808A (ja) 2014-02-13
JP5799060B2 (ja) 2015-10-21
DK1948678T3 (da) 2013-06-24
MY171061A (en) 2019-09-24
ES2628620T3 (es) 2017-08-03
US20140051641A1 (en) 2014-02-20
CN101405294B (zh) 2015-11-25
MX2008006090A (es) 2008-10-23
BRPI0618468A2 (pt) 2011-08-30
HK1220208A1 (zh) 2017-04-28
US20170260230A1 (en) 2017-09-14
US20090203698A1 (en) 2009-08-13
HN2008000738A (es) 2011-11-03
CN105237621A (zh) 2016-01-13
SI2623113T1 (sl) 2017-08-31
CA2629084A1 (en) 2007-05-18
US10150794B2 (en) 2018-12-11
EP2623113B1 (en) 2017-05-31
IL242282B (en) 2018-06-28
KR20130041367A (ko) 2013-04-24
RU2453556C2 (ru) 2012-06-20
CY1119405T1 (el) 2018-03-07
EP2623113A3 (en) 2014-04-16
US9205126B2 (en) 2015-12-08
US20160083421A1 (en) 2016-03-24
JP5778097B2 (ja) 2015-09-16
US20140031297A1 (en) 2014-01-30
MY145757A (en) 2012-04-13
RU2012110718A (ru) 2013-09-27
PH12013501656A1 (en) 2016-02-01
EP2623113A2 (en) 2013-08-07
HUE034863T2 (en) 2018-03-28
US7687456B2 (en) 2010-03-30
US9205124B2 (en) 2015-12-08
DK2623113T3 (en) 2017-07-17
GT200800063A (es) 2009-03-12
NZ595196A (en) 2013-03-28
PL1948678T3 (pl) 2013-09-30
IL242282A0 (en) 2015-11-30
EP1948678B1 (en) 2013-05-01
ES2415756T3 (es) 2013-07-26
KR101275445B1 (ko) 2013-06-14
HK1121172A1 (en) 2009-04-17
NZ568068A (en) 2011-10-28
IL191344A (en) 2015-11-30
WO2007056464A1 (en) 2007-05-18
US8716322B2 (en) 2014-05-06
US20070105786A1 (en) 2007-05-10
EP1948678A1 (en) 2008-07-30
ZA200804455B (en) 2009-05-27
LT2623113T (lt) 2017-07-10
RU2008122779A (ru) 2009-12-20
US20130130968A1 (en) 2013-05-23
US9205125B2 (en) 2015-12-08
KR101434522B1 (ko) 2014-08-26
CA2629084C (en) 2015-08-11
AU2006311584A1 (en) 2007-05-18
CN101405294A (zh) 2009-04-08
KR101274417B1 (ko) 2013-06-17
PT1948678E (pt) 2013-07-16
KR20120117003A (ko) 2012-10-23
JP2012255012A (ja) 2012-12-27
KR20080070049A (ko) 2008-07-29
US20140050737A1 (en) 2014-02-20
JP2009514971A (ja) 2009-04-09
JP5436860B2 (ja) 2014-03-05
AU2006311584B2 (en) 2012-03-08
PT2623113T (pt) 2017-07-14
ECSP088460A (es) 2008-08-29
PL2623113T3 (pl) 2018-05-30

Similar Documents

Publication Publication Date Title
SV2009002903A (es) Compuestos para la inhibicion de enzimas
CR11518A (es) Compuestos de carbamoilo como inhibidores de dgat1 190
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
CL2008002430A1 (es) Compuestos derivados de bencenosulfonamida, inhibidores de catepsina c; composicion farmaceutica que los comprende; y su uso para el tratamiento de la epoc.
BRPI0514102B8 (pt) composto para inibição da enzima de proteassoma e composição farmacêutica compreendendo dito composto
CL2004000848A1 (es) Compuestos derivados de fenacil-2-hidroxi-3-diaminoalcanos, inhibidores de la enzima betasecretasa, utiles para preparar un medicamento para tratar alzheimer, sindrome de down, hemorragia cerebral hereditaria con amiloidosis de tipo holandes, y otras
UY30759A1 (es) Compuestos quimicos
CR9664A (es) Inhibidores de histona deacetilasa
GT200600206A (es) Nuevos derivados del fluoreno, composiciones que los contienen y su utilizacion
ECSP045491A (es) Nueva sal formiato de o-desmetil venlafaxina
CR9694A (es) Inhibidores de la transcriptasa reversa de vih
UY32158A (es) Derivados heterociclicos y metodos de uso de los mismos
WO2008140782A3 (en) Compounds for enzyme inhibition
BRPI0618654A8 (pt) variante de zimogênio/protease de fator x/fator xa, ácido nucléico, composição farmacêutica que os contém, vetor, bem como uso dos mesmos
UY27619A1 (es) Ésteres hidroxamato del ácido n-(4-fenil sustituido)- antranílico
UY30544A1 (es) Compuestos de pirrolo-piperidina y sales farmacéuticametne aceptables de los mismos, procesos de fabricacion, composiciones y aplicaciones
CL2003002611A1 (es) Compuestos derivados del acido tiofeno hidroxamico, 2-hidroxamida-5-[(aril o heteroaril)-disutituido-metil]-amida del acido tiofeno-2,5-dicarboxilico enantiomeros, composicion farmaceutica, procedimiento de preparacion, y su uso para el tratamiento d
UY31141A1 (es) Compuestos de piperidina y sus usos
UY27894A1 (es) Derivados de cinamida.
ECSP13012538A (es) Combinaciones que contienen n-(2-arilamino)arilsulfonamida sustituida
DOP2022000235A (es) Inhibidores macrocíclicos de las peptidilarginina deiminasas
DK1987063T3 (da) Peptider og peptidderivater, fremstilling deraf samt deres anvendelse til fremstilling af en terapeutisk og/eller præventivt aktiv farmaceutisk sammensætning
BR0306928A (pt) Composições farmacêuticas estáveis compreendendo inibidores de enzimas conversoras de angiotensina (ace)
UY27727A1 (es) Nueva composicion farmacéutica-
ITMI20050477A1 (it) Cerotto transdermico

Legal Events

Date Code Title Description
FG Grant
FG Grant