DOP2012000238A - Compuestos de para la inhibición de inmunoproteasomas - Google Patents

Compuestos de para la inhibición de inmunoproteasomas

Info

Publication number
DOP2012000238A
DOP2012000238A DO2012000238A DO2012000238A DOP2012000238A DO P2012000238 A DOP2012000238 A DO P2012000238A DO 2012000238 A DO2012000238 A DO 2012000238A DO 2012000238 A DO2012000238 A DO 2012000238A DO P2012000238 A DOP2012000238 A DO P2012000238A
Authority
DO
Dominican Republic
Prior art keywords
immunoproteasomas
inhibition
compounds
invention refers
administer
Prior art date
Application number
DO2012000238A
Other languages
English (en)
Inventor
Mark K Bennett
Kevin D Shenk
Francesco Parlati
Original Assignee
Onyx 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43983939&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=DOP2012000238(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Onyx Therapeutics Inc filed Critical Onyx Therapeutics Inc
Publication of DOP2012000238A publication Critical patent/DOP2012000238A/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
    • C07K5/08Tripeptides
    • C07K5/0827Tripeptides containing heteroatoms different from O, S, or N
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • 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
    • A61P31/04Antibacterial agents
    • 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
    • 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
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/20Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/10Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
    • C07D295/104Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D303/00Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02Compounds containing oxirane rings
    • C07D303/36Compounds containing oxirane rings with hydrocarbon radicals, substituted by nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/04Esters of boric acids

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)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)

Abstract

UN ASPECTO DE LA INVENCIÓN SE REFIERE A INHIBIDORES QUE INHIBEN PREFERENCIALMENTE LA ACTIVIDAD DE INMUNOPROTEASOMAS CON RESPECTO A LA ACTIVIDAD DE PROTEASOMAS CONSTITUTIVOS. EN CIERTAS REALIZACIONES, LA INVENCIÓN SE REFIERE AL TRATAMIENTO DE ENFERMEDADES INMUNORRELACIONADAS QUE COMPRENDE ADMINISTRAR UN COMPUESTO DE LA INVENCIÓN. EN CIERTAS REALIZACIONES, LA INVENCIÓN SE REFIERE AL TRATAMIENTO DE CÁNCER QUE COMPRENDE ADMINISTRAR UN COMPUESTO DE LA INVENCIÓN.
DO2012000238A 2010-03-01 2012-08-29 Compuestos de para la inhibición de inmunoproteasomas DOP2012000238A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US30936610P 2010-03-01 2010-03-01

Publications (1)

Publication Number Publication Date
DOP2012000238A true DOP2012000238A (es) 2013-01-15

Family

ID=43983939

Family Applications (1)

Application Number Title Priority Date Filing Date
DO2012000238A DOP2012000238A (es) 2010-03-01 2012-08-29 Compuestos de para la inhibición de inmunoproteasomas

Country Status (20)

Country Link
US (1) US9359398B2 (es)
EP (1) EP2542238B1 (es)
JP (1) JP6042724B2 (es)
KR (1) KR20130075723A (es)
CN (1) CN102892417A (es)
AU (1) AU2011223795B2 (es)
BR (1) BR112012022060A2 (es)
CA (1) CA2791651C (es)
CL (1) CL2012002404A1 (es)
CO (1) CO6612265A2 (es)
CR (1) CR20120451A (es)
CU (1) CU20120125A7 (es)
DO (1) DOP2012000238A (es)
EA (1) EA201290844A1 (es)
EC (1) ECSP12012140A (es)
MA (1) MA34133B1 (es)
MX (1) MX2012010017A (es)
SG (1) SG183843A1 (es)
WO (1) WO2011109355A1 (es)
ZA (1) ZA201206479B (es)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
HUE029665T2 (en) 2007-10-04 2017-03-28 Onyx Therapeutics Inc Synthesis of crystalline peptide epoxy ketone protease inhibitors and amino acid keto epoxides \ t
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
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
US8853147B2 (en) 2009-11-13 2014-10-07 Onyx Therapeutics, Inc. Use of peptide epoxyketones for metastasis suppression
MA34133B1 (fr) 2010-03-01 2013-04-03 Onyx Therapeutics Inc Composes pour inhibiteurs de l'immunoproteasome
RU2012147246A (ru) 2010-04-07 2014-05-20 Оникс Терапьютикс, Инк. Кристаллический пептидный эпоксикетонный ингебитор иммунопротеасомы
UY34897A (es) 2012-07-09 2014-01-31 Onyx Therapeutics Inc Profarmacos de inhibidores peptidicos de expoxi cetona proteasa
JP6018319B2 (ja) * 2012-12-03 2016-11-02 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 置換トリアゾールボロン酸化合物
CA2904085C (en) * 2013-03-14 2021-07-06 Onyx Therapeutics, Inc. Dipeptide and tripeptide epoxy ketone protease inhibitors
BR112015023761A2 (pt) * 2013-03-15 2017-07-18 Adaerata Lp moduladores de molécula pequena de pcsk9 e seus métodos e usos
WO2015106200A2 (en) 2014-01-10 2015-07-16 Cornell University Dipeptides as inhibitors of human immunoproteasomes
CN103804469B (zh) * 2014-02-17 2016-04-06 苏州明锐医药科技有限公司 卡非佐米中间体的制备方法
US11202817B2 (en) 2014-08-18 2021-12-21 Cornell University Dipeptidomimetics as inhibitors of human immunoproteasomes
US10253049B2 (en) * 2014-10-01 2019-04-09 Merck Patent Gmbh Boronic acid derivatives
WO2017066763A1 (en) 2015-10-15 2017-04-20 Cornell University Proteasome inhibitors and uses thereof
CN106588965A (zh) * 2015-10-15 2017-04-26 北京大学 脲拟肽硼酸化合物及其药物组合物、制备方法和用途
EP3472151A4 (en) 2016-06-21 2020-03-04 Orion Ophthalmology LLC CARBOCYCLIC PROLINAMIDE DERIVATIVES
JP7179721B2 (ja) 2016-06-21 2022-11-29 オリオン・オフサルモロジー・エルエルシー 複素環式プロリンアミド誘導体
WO2019075252A1 (en) 2017-10-11 2019-04-18 Cornell University PEPTIDOMIMETIC INHIBITORS OF PROTEASOME
CN111491938B (zh) * 2017-11-16 2024-05-24 普林斯匹亚生物制药公司 免疫蛋白酶体抑制剂
JP2021503441A (ja) * 2017-11-16 2021-02-12 アムジエン・インコーポレーテツド Peg化されたカルフィルゾミブ化合物の安定組成物
LV15544A (lv) * 2019-07-01 2021-01-20 Latvijas Organiskās Sintēzes Institūts Jauni borskābi saturoši peptidomimētiķi kā malārijas serīna proteāzes inhibitori

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
DE3827340A1 (de) * 1988-08-12 1990-02-15 Hoechst Ag Verwendung von (alpha)-aminoboronsaeure-derivaten zur prophylaxe und behandlung von viruserkrankungen
JPH0291023U (es) 1989-01-05 1990-07-19
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
EP0732399A3 (en) 1990-03-05 1997-03-12 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
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
SI0932617T1 (en) 1996-10-18 2002-06-30 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
UA79749C2 (en) 1996-10-18 2007-07-25 Vertex Pharma 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
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
US6902721B1 (en) 1998-07-10 2005-06-07 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
BR9914648A (pt) 1998-10-20 2001-11-27 Millennium Pharm Inc Processo para monitorar ação medicamentosa deinibidor de proteasoma
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
EP1221962A2 (en) 1999-10-20 2002-07-17 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone and hair growth
DE50110956D1 (de) 2000-10-12 2006-10-19 Viromics Gmbh Proteasome inhibitoren zur behandlung von hepatitis-virus infektionen
PT1355910E (pt) 2001-01-25 2011-03-24 Us Of America Represented By The Secretary Dept Of Health And Human Services Formulação de compostos do ácido borónico
DK1392355T3 (da) 2001-05-21 2007-04-30 Alcon Inc Anvendelse af proteasominhibitorer tilbehandling af öjentörhedslidelser
BR0210112A (pt) * 2001-05-30 2004-06-08 Novartis Ag Derivados do ácido 2-{[n-(2-amino-3-(heteroarila ou arila)propionil)-aminoacil]-amino}-alquilborÈnico
US7524883B2 (en) 2002-01-08 2009-04-28 Eisai R&D Management 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
WO2003101481A1 (en) 2002-06-03 2003-12-11 Als Therapy Development Foundation 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
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
DE602004017847D1 (de) 2003-04-08 2009-01-02 Novartis Ag Feste pharmazeutische darreichungsformen mit einem s1p rezeptoragonisten und einem zuckeralkohol
ATE506456T1 (de) 2003-06-10 2011-05-15 David Gladstone Inst Verfahren zur behandlung von lentivirusinfektionen
US7012063B2 (en) 2003-06-13 2006-03-14 Children's Medical Center Corporation Reducing axon degeneration with proteasome inhibitors
HUE032527T2 (en) 2003-12-31 2017-09-28 Cydex Pharmaceuticals Inc Sulphoalkyl ether cyclodextrin and corticosteroid inhalation preparation
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
CN102174076A (zh) 2004-04-15 2011-09-07 普罗特奥里克斯公司 用于抑制蛋白酶体酶的化合物
US8198270B2 (en) 2004-04-15 2012-06-12 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
RU2384585C2 (ru) 2004-05-10 2010-03-20 Протеоликс, Инк. Соединения для ингибирования ферментов
AU2005243140A1 (en) 2004-05-10 2005-11-24 Proteolix, Inc. Synthesis of amino acid keto-epoxides
CA2584515A1 (en) 2004-10-20 2006-04-27 Proteolix, Inc. Labeled compounds for proteasome inhibition
PT2260835E (pt) 2004-12-07 2013-05-28 Onyx Therapeutics Inc Composição para inibição do proteassoma
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
ATE553198T1 (de) 2005-04-15 2012-04-15 Geron Corp Behandlung von krebs durch die kombinierte hemmung der proteasom- und telomeraseaktivitäten
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
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
KR20160040735A (ko) 2007-08-06 2016-04-14 밀레니엄 파머슈티컬스 인코퍼레이티드 프로테아좀 억제제
HUE029665T2 (en) 2007-10-04 2017-03-28 Onyx Therapeutics Inc Synthesis of crystalline peptide epoxy ketone protease inhibitors and amino acid keto epoxides \ t
JP5600595B2 (ja) 2007-10-16 2014-10-01 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 プロテアソーム阻害剤
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
EA027346B1 (ru) 2008-06-17 2017-07-31 Милленниум Фармасьютикалз, Инк. Соединения боронатного эфира и его фармацевтические составы
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.
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
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
US8853147B2 (en) 2009-11-13 2014-10-07 Onyx Therapeutics, Inc. Use of peptide epoxyketones for metastasis suppression
MA34133B1 (fr) * 2010-03-01 2013-04-03 Onyx Therapeutics Inc Composes pour inhibiteurs de l'immunoproteasome
CN107266485A (zh) 2010-03-31 2017-10-20 米伦纽姆医药公司 1‑氨基‑2‑环丙基乙硼酸衍生物
RU2012147246A (ru) 2010-04-07 2014-05-20 Оникс Терапьютикс, Инк. Кристаллический пептидный эпоксикетонный ингебитор иммунопротеасомы
FR2962092B1 (fr) * 2010-06-30 2013-06-28 Valeo Systemes Dessuyage Adaptateur d'essuie-glace a contacts electriques

Also Published As

Publication number Publication date
MX2012010017A (es) 2012-10-01
EP2542238A1 (en) 2013-01-09
CA2791651C (en) 2019-08-20
CO6612265A2 (es) 2013-02-01
MA34133B1 (fr) 2013-04-03
BR112012022060A2 (pt) 2018-05-08
EP2542238B1 (en) 2015-08-12
ZA201206479B (en) 2015-08-26
CA2791651A1 (en) 2011-09-09
JP6042724B2 (ja) 2016-12-14
CU20120125A7 (es) 2012-11-15
CL2012002404A1 (es) 2012-12-21
CR20120451A (es) 2012-10-16
EA201290844A1 (ru) 2013-03-29
WO2011109355A1 (en) 2011-09-09
US9359398B2 (en) 2016-06-07
US20130072422A1 (en) 2013-03-21
ECSP12012140A (es) 2012-10-30
AU2011223795B2 (en) 2015-11-05
KR20130075723A (ko) 2013-07-05
AU2011223795A1 (en) 2012-09-20
SG183843A1 (en) 2012-10-30
CN102892417A (zh) 2013-01-23
JP2013521295A (ja) 2013-06-10

Similar Documents

Publication Publication Date Title
DOP2012000238A (es) Compuestos de para la inhibición de inmunoproteasomas
AR110381A2 (es) Inhibidores biarilo de tirosina cinasa de bruton
NI201400078A (es) Derivados de lactamas útiles como inhibidores mutantes de idh1
BR112014017799A8 (pt) Compostos inibidores de metaloenzima
HK1207861A1 (en) Substituted cycloalkenopyrazoles as bub1 inhibitors for the treatment of cancer bub1
CR20110560A (es) Métodos de tratamiento para tumores sólidos
BR112013025415A2 (pt) métodos para aumentar eficácia de terapia de câncer de folr1
CO6842020A2 (es) Inhibidores de la tirosina-quinasa de bruton
UY34165A (es) ?compuestos aldh-2 mitocondriales humanos para el tratamiento de la adicción?.
PE20150887A1 (es) Compuestos de benceno sustituidos
PH12015501058A1 (en) Pyrimidine-2,4-diamine derivatives for treatment of cancer
CR20140024A (es) Compuestos inhibidores de metaloenzimas
GT201300124A (es) Inhibidores de nampt y rock
ECSP12012318A (es) Inhibidores de pirazolil quinazolina cinasa
CR20140229A (es) Nuevos derivados bicíclicos de dihidroisoquinolin-1-ona
BR112013028281A2 (pt) compostos e composições para inibição de nampt
BR112016015236A2 (pt) inibidores de serina/treonina quinase
ECSP13012394A (es) Nuevas formas de dosificación de liberación modificada de un inhibidor de la xantina oxidorreductasa o de inhibidores de xantina oxidasa
HK1193823A1 (zh) 用於治療癌症的作為 -激酶抑制劑的苯並吡喃酮化合物
BR112013024211A2 (pt) tratamento de tumores sólidos
MX2013007835A (es) Combinacion de sirosingopina e inhibidores mitocondriales para el tratamiento de cancer e inmunosupresion.
CL2011000258A1 (es) Compuestos derivados de fenilamino-isonicotinamida; inhibidores de mek; composicion farmaceutica y uso para el tratamiento de enfermedades hiperproliferativas tales como cancer e inflamacion.
EA201590744A1 (ru) Лечение рака tor киназными ингибиторами
EA201270728A1 (ru) Пуриновые соединения
EA201390616A1 (ru) ЛЕЧЕНИЕ НАРУШЕНИЙ, АССОЦИИРОВАННЫХ С ГЕНОМ MeCP2