JP4743720B2 - プロテアソーム酵素阻害のための化合物 - Google Patents

プロテアソーム酵素阻害のための化合物 Download PDF

Info

Publication number
JP4743720B2
JP4743720B2 JP2007525077A JP2007525077A JP4743720B2 JP 4743720 B2 JP4743720 B2 JP 4743720B2 JP 2007525077 A JP2007525077 A JP 2007525077A JP 2007525077 A JP2007525077 A JP 2007525077A JP 4743720 B2 JP4743720 B2 JP 4743720B2
Authority
JP
Japan
Prior art keywords
alkyl
compound
mmol
hydrogen
aralkyl
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
JP2007525077A
Other languages
English (en)
Japanese (ja)
Other versions
JP2008509166A (ja
JP2008509166A5 (cg-RX-API-DMAC7.html
Inventor
マーク エス. スミス,
ガイ ジェイ. レイディグ,
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Onyx Therapeutics Inc
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=35502451&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JP4743720(B2) "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 JP2008509166A publication Critical patent/JP2008509166A/ja
Publication of JP2008509166A5 publication Critical patent/JP2008509166A5/ja
Application granted granted Critical
Publication of JP4743720B2 publication Critical patent/JP4743720B2/ja
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1016Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • 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
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07Tetrapeptides
    • 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
    • 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
    • C07K5/08Tripeptides
    • 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
    • C07K5/0827Tripeptides containing heteroatoms different from O, S, or N
    • 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
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1005Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1008Tetrapeptides 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
    • C07K5/10Tetrapeptides
    • C07K5/1024Tetrapeptides with the first amino acid being heterocyclic

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • AIDS & HIV (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Enzymes And Modification Thereof (AREA)
JP2007525077A 2004-08-06 2005-08-08 プロテアソーム酵素阻害のための化合物 Expired - Lifetime JP4743720B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US59940104P 2004-08-06 2004-08-06
US60/599,401 2004-08-06
US61000104P 2004-09-14 2004-09-14
US60/610,001 2004-09-14
US11/106,879 2005-04-14
US11/106,879 US7232818B2 (en) 2004-04-15 2005-04-14 Compounds for enzyme inhibition
PCT/US2005/028246 WO2006017842A1 (en) 2004-08-06 2005-08-08 Compounds for proteasome enzyme inhibition

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2011047047A Division JP5394423B2 (ja) 2004-08-06 2011-03-04 プロテアソーム酵素阻害のための化合物

Publications (3)

Publication Number Publication Date
JP2008509166A JP2008509166A (ja) 2008-03-27
JP2008509166A5 JP2008509166A5 (cg-RX-API-DMAC7.html) 2008-10-02
JP4743720B2 true JP4743720B2 (ja) 2011-08-10

Family

ID=35502451

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2007525077A Expired - Lifetime JP4743720B2 (ja) 2004-08-06 2005-08-08 プロテアソーム酵素阻害のための化合物
JP2011047047A Expired - Lifetime JP5394423B2 (ja) 2004-08-06 2011-03-04 プロテアソーム酵素阻害のための化合物

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2011047047A Expired - Lifetime JP5394423B2 (ja) 2004-08-06 2011-03-04 プロテアソーム酵素阻害のための化合物

Country Status (24)

Country Link
US (12) US7232818B2 (cg-RX-API-DMAC7.html)
EP (4) EP3101026B1 (cg-RX-API-DMAC7.html)
JP (2) JP4743720B2 (cg-RX-API-DMAC7.html)
KR (3) KR101354280B1 (cg-RX-API-DMAC7.html)
CN (1) CN102286070B (cg-RX-API-DMAC7.html)
AT (1) ATE496062T1 (cg-RX-API-DMAC7.html)
AU (1) AU2005271232B2 (cg-RX-API-DMAC7.html)
BR (2) BRPI0514102B8 (cg-RX-API-DMAC7.html)
CA (1) CA2589765C (cg-RX-API-DMAC7.html)
CY (3) CY1116771T1 (cg-RX-API-DMAC7.html)
DE (1) DE602005026019D1 (cg-RX-API-DMAC7.html)
DK (2) DK1781688T3 (cg-RX-API-DMAC7.html)
ES (2) ES2674277T3 (cg-RX-API-DMAC7.html)
FR (1) FR16C0017I2 (cg-RX-API-DMAC7.html)
HU (2) HUE038005T2 (cg-RX-API-DMAC7.html)
IL (3) IL181127A (cg-RX-API-DMAC7.html)
LT (2) LT3101026T (cg-RX-API-DMAC7.html)
LU (1) LU93015I2 (cg-RX-API-DMAC7.html)
NO (2) NO341015B1 (cg-RX-API-DMAC7.html)
PL (2) PL1781688T3 (cg-RX-API-DMAC7.html)
PT (2) PT3101026T (cg-RX-API-DMAC7.html)
SG (2) SG155187A1 (cg-RX-API-DMAC7.html)
SI (2) SI3101026T1 (cg-RX-API-DMAC7.html)
WO (1) WO2006017842A1 (cg-RX-API-DMAC7.html)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011148805A (ja) * 2004-08-06 2011-08-04 Proteolix Inc プロテアソーム酵素阻害のための化合物

Families Citing this family (80)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7176232B2 (en) 2002-06-24 2007-02-13 The Regents Of The University Of California Salinosporamides and methods for use thereof
DK1745064T3 (da) 2004-04-15 2011-04-11 Proteolix Inc Forbindelser til proteasomenzyminhibering
US8198270B2 (en) * 2004-04-15 2012-06-12 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
US8088741B2 (en) * 2004-05-10 2012-01-03 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
AU2005243140A1 (en) * 2004-05-10 2005-11-24 Proteolix, Inc. Synthesis of amino acid keto-epoxides
SG157365A1 (en) 2004-12-03 2009-12-29 Dana Farber Cancer Inst Inc Compositions and methods for treating neoplastic diseases
ES2408216T3 (es) * 2004-12-07 2013-06-19 Onyx Therapeutics, Inc. Composición para la inhibición del proteasoma
KR101434522B1 (ko) 2005-11-09 2014-08-26 오닉스 세라퓨틱스, 인크. 효소 저해를 위한 화합물
UA101303C2 (uk) 2006-06-19 2013-03-25 Протеолікс, Інк. Сполуки для інгібування ферменту протеасоми
US20090234150A1 (en) * 2006-07-14 2009-09-17 Peter Carmeliet Use of ppar-alpha agonists to treat skeletal muscle wasting disorders
US7642369B2 (en) * 2006-09-12 2010-01-05 University Of Kentucky Research Foundation Epoxyketone-based immunoproteasome inhibitors
ES2684340T3 (es) * 2007-10-04 2018-10-02 Onyx Therapeutics, Inc. Inhibidores de proteasa epoxi cetona de péptidos cristalinos y síntesis de cetoepóxidos de aminoácidos
AU2013203566B2 (en) * 2007-10-04 2016-10-13 Onyx Therapeutics, Inc. Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides
AU2016231532B2 (en) * 2007-10-04 2018-05-10 Onyx Therapeutics, Inc. Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides
US8394816B2 (en) * 2007-12-07 2013-03-12 Irene Ghobrial Methods of using [3.2.0] heterocyclic compounds and analogs thereof in treating Waldenstrom's Macroglobulinemia
EP2088205A1 (en) 2008-02-11 2009-08-12 Institut National De La Sante Et De La Recherche Medicale (Inserm) PSMB10: A diagnosis marker and therapeutic target of chronic rejection.
US7635773B2 (en) 2008-04-28 2009-12-22 Cydex Pharmaceuticals, Inc. Sulfoalkyl ether cyclodextrin compositions
EP2276765A4 (en) * 2008-05-12 2011-10-19 Nereus Pharmaceuticals Inc SALINOSPORAMIDE DERIVATIVES AS PROTEASOMAL HEMMER
AU2009308516B2 (en) 2008-10-21 2016-08-25 Onyx Therapeutics, Inc. Combination therapy with peptide epoxyketones
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
US20110009332A1 (en) * 2009-07-09 2011-01-13 Southwest Research Institute Therapeutic Treatment Of Wounds
GB0914883D0 (en) 2009-08-26 2009-09-30 Univ Belfast Compound
JP5919196B2 (ja) 2009-11-13 2016-05-18 オニキス セラピューティクス, インク.Onyx Therapeutics, Inc. 転移抑制のためのペプチドエポキシケトンの使用
CA2791651C (en) 2010-03-01 2019-08-20 Onyx Therapeutics, Inc. Compounds for immunoproteasome inhibition
CA2795559A1 (en) 2010-04-07 2011-11-03 Onyx Therapeutics, Inc. Crystalline peptide epoxyketone immunoproteasome inhibitor
US9126997B1 (en) 2010-09-07 2015-09-08 Northwestern University Synergistic effect of glucocorticoid receptor agonists in combination with proteosome inhibitors for treating leukemia and myeloma
WO2012135528A2 (en) 2011-03-29 2012-10-04 Texas Tech University System Galectin-3c combination therapy for human cancer
WO2013009923A1 (en) * 2011-07-13 2013-01-17 Creighton University Methods of promoting neuron growth
EP2776043B1 (en) 2011-11-11 2018-02-21 Millennium Pharmaceuticals, Inc. Biomarkers of response to proteasome inhibitors
JP6286358B2 (ja) 2011-11-11 2018-02-28 ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. プロテアソーム阻害剤に応答するバイオマーカー
EP2810066B1 (en) 2012-01-24 2019-07-31 Millennium Pharmaceuticals, Inc. Methods of treatment of cancer
ES2774901T3 (es) 2012-02-15 2020-07-23 Cydex Pharmaceuticals Inc Proceso para la fabricación de derivados de ciclodextrina
KR20240119191A (ko) 2012-05-08 2024-08-06 오닉스 세라퓨틱스, 인크. 펩티드 프로테아좀 억제제 제제화를 위한 사이클로덱스트린 복합체화 방법
WO2014011695A2 (en) 2012-07-09 2014-01-16 Onyx Therapeutics, Inc. Prodrugs of peptide epoxy ketone protease inhibitors
EP2874606B1 (en) 2012-07-18 2019-03-06 Onyx Therapeutics, Inc. Liposomal compositions of epoxyketone-based proteasome inhibitors
CA2881986A1 (en) * 2012-08-21 2014-02-27 Fluorinov Pharma Inc. Fluorinated epoxyketone-based tetrapeptide compounds and uses thereof as proteasome inhibitors
UA121095C2 (uk) 2012-10-22 2020-04-10 Сідекс Фармасьютікалс, Інк. Композиції алкілованого циклодекстрину і способи їх одержання і застосування
ES2808565T3 (es) 2013-03-13 2021-03-01 Sanofi Sa Composiciones que comprenden anticuerpos anti-CD38 y carfilzomib
AR095426A1 (es) 2013-03-14 2015-10-14 Onyx Therapeutics Inc Inhibidores tripeptídicos de la epoxicetona proteasa
JP2016515127A (ja) 2013-03-14 2016-05-26 オニキス セラピューティクス, インク.Onyx Therapeutics, Inc. ジペプチド及びトリペプチドエポキシケトンプロテアーゼ阻害剤
AU2014290012B2 (en) 2013-07-19 2020-01-16 Onyx Therapeutics, Inc. Peptide epoxyketone proteasome inhibitors in combination with PIM kinase inhibitors for treatment of cancers
CN103360348B (zh) * 2013-07-25 2015-06-24 苏州鹏旭医药科技有限公司 一种Carfilzomib中间体及其制备方法和制备Carfilzomib的方法
US20160215016A1 (en) * 2013-09-06 2016-07-28 Sandoz Ag Synthesis of peptide epoxy ketones
US20160194354A1 (en) * 2013-09-06 2016-07-07 Sandoz Ag Stereoselective synthesis of diols and triols by mannich reaction and their use in the synthesis of carfilzomib
WO2015121769A1 (en) 2014-02-13 2015-08-20 Ranbaxy Laboratories Limited Process for the preparation of methyl n-[(benzyloxy)-carbonyl]-l-leucyl-l-phenylalaninate
CN103864889B (zh) * 2014-04-04 2017-01-11 重庆泰濠制药有限公司 环氧酮化合物、其制备方法及卡非佐米的制备方法
EP3183295B1 (en) 2014-08-22 2023-08-02 CyDex Pharmaceuticals, Inc. Fractionated alkylated cyclodextrin compositions and processes for preparing and using the same
WO2016046843A1 (en) 2014-09-24 2016-03-31 Biophore India Pharmaceuticals Pvt. Ltd. Process for the preparation of (s)-4-methyl-n-((s)-1-(((s)-4-methyl-1-((r)-2-methyloxiran-2-yl)-1-oxo pentan-2-yl) amino)-1-oxo-3-phenylpropan-2-yl)-2-((s)-2-(2-morpholinoacetamido)-4-phenylbutanamido) pentanamide
US20160115198A1 (en) 2014-10-27 2016-04-28 Apicore Us Llc Methods of making carfilzomib and intermediates thereof
CN104402973A (zh) * 2014-11-24 2015-03-11 重庆泰濠制药有限公司 一种卡非佐米无定型晶的制备方法
EP3227312B1 (en) 2014-12-02 2019-05-29 Fresenius Kabi Oncology Limited A process for purification of carfilzomib
US10301353B2 (en) 2014-12-31 2019-05-28 Dr. Reddy's Laboratories Limited Co-crystal of carfilzomib with maleic acid and process for the preparation of pure carfilzomib
WO2016170544A1 (en) * 2015-04-22 2016-10-27 Msn Laboratories Private Limited Process for the preparation of (2s)-n-((s)-1-((s)-4-methyl-1-((r)-2-methyl oxiran-2-yl)-1-oxopentan-2-ylcarbamoyl)-2-phenylethyl)-2-((s)-2-(2-morpholino acetamido)-4-phenylbutanamido)-4-methylpentanamide
WO2016185450A1 (en) 2015-05-21 2016-11-24 Laurus Labs Private Limited An improved processes for the preparation of carfilzomib or pharmaceutically acceptable salts thereof
CN106317188A (zh) * 2015-06-18 2017-01-11 重庆医药工业研究院有限责任公司 一种制备卡非佐米无定型物的方法
WO2017032487A1 (en) 2015-08-27 2017-03-02 Technische Universität München Proteasome inhibitor comprising a signal-emitting moiety
US20180362580A1 (en) 2015-12-11 2018-12-20 Mylan Laboratories Limited Crystalline and amorphous forms of carfilzomib
TWI636052B (zh) * 2015-12-31 2018-09-21 中化合成生技股份有限公司 無定形卡非佐米(i)的製備方法
WO2017147410A1 (en) 2016-02-25 2017-08-31 Amgen Inc. Compounds that inhibit mcl-1 protein
TWI759301B (zh) 2016-05-24 2022-04-01 美商安美基公司 聚乙二醇化卡非佐米化合物
EP3494126A1 (en) 2016-08-02 2019-06-12 Synthon BV Process for making carfilzomib
SG11201900991UA (en) 2016-08-05 2019-03-28 Amgen Inc Synthesis of (s)-2-amino-4-methyl-1-((r)-2-methyloxirane-2-yl)-pentan-1-one and pharmaceutically acceptable salts thereof
EP3512835B1 (en) 2016-09-14 2021-06-09 Fresenius Kabi Oncology Limited A process for purification of carfilzomib intermediate
US11597708B2 (en) 2016-09-16 2023-03-07 Hsf Pharmaceuticals Sa Inhibitors of heat shock factors and uses thereof
EP3330260A1 (en) 2016-12-01 2018-06-06 Enantia, S.L. Process for the preparation of an intermediate for the synthesis of i.a. carfilzomib
WO2019053611A1 (en) 2017-09-14 2019-03-21 Glaxosmithkline Intellectual Property Development Limited POLY THERAPY FOR THE TREATMENT OF CANCER
EP3710063A1 (en) 2017-11-16 2020-09-23 Amgen Inc. Stable compositions of pegylated carfilzomib compounds
WO2019113363A1 (en) * 2017-12-08 2019-06-13 NeuroDiagnostics LLC Synchronized cell cycle gene expression test for alzheimer's disease and related therapeutic methods
US10537585B2 (en) 2017-12-18 2020-01-21 Dexcel Pharma Technologies Ltd. Compositions comprising dexamethasone
US10689416B2 (en) * 2017-12-30 2020-06-23 Unity Biotechnology, Inc. Peptide-based proteasome inhibitors for treating conditions mediated by senescent cells and for treating cancer
WO2019133988A1 (en) 2017-12-30 2019-07-04 Unity Biotechnology, Inc. Peptide-based proteasome inhibitors for treating conditions mediated by senescent cells and for treating cancer
MX2020013853A (es) * 2018-06-22 2021-05-27 Ucl Business Ltd Compuestos innovadores.
WO2021072212A1 (en) * 2019-10-11 2021-04-15 Mayo Foundation For Medical Education And Research Proteasome inhibitors
CA3175499A1 (en) * 2020-04-21 2021-10-28 University Of Rochester Inhibitors of human epididymus protein 4
KR20250008774A (ko) 2022-05-11 2025-01-15 셀진 코포레이션 T 세포 요법 및 그의 생산과 관련된 방법 및 용도
US20250302954A1 (en) 2022-05-11 2025-10-02 Celgene Corporation Methods to overcome drug resistance by re-sensitizing cancer cells to treatment with a prior therapy via treatment with a t cell therapy
WO2024069240A2 (en) 2022-09-29 2024-04-04 Takeda Pharmaceutical Company Limited Cd38-binding fusion protein combination therapy
WO2024097905A1 (en) 2022-11-02 2024-05-10 Celgene Corporation Methods of treatment with t cell therapy and immunomodulatory agent maintenance therapy
CN116768972A (zh) * 2023-06-25 2023-09-19 重庆药友制药有限责任公司 一种卡非佐米中间体的制备方法
WO2025035020A2 (en) 2023-08-09 2025-02-13 Amgen Inc. Methods of using carfilzomib

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US569748A (en) 1896-10-20 Henry edmunds
US4733665C2 (en) 1985-11-07 2002-01-29 Expandable Grafts Partnership Expandable intraluminal graft and method and apparatus for implanting an expandable intraluminal graft
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
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
AU4499697A (en) 1996-09-13 1998-04-02 New York University Method for treating parasitic diseases with proteasome inhibitors
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
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
EP1477180A1 (en) 1999-10-20 2004-11-17 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone and hair growth
AU2003219652A1 (en) 2002-01-08 2003-07-30 Eisai Co. Ltd. Eponemycin and epoxomicin analogs and uses thereof
DK1745064T3 (da) * 2004-04-15 2011-04-11 Proteolix Inc Forbindelser til proteasomenzyminhibering
US7232818B2 (en) 2004-04-15 2007-06-19 Proteolix, Inc. Compounds for enzyme inhibition
US8088741B2 (en) 2004-05-10 2012-01-03 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
AU2005243140A1 (en) 2004-05-10 2005-11-24 Proteolix, Inc. Synthesis of amino acid keto-epoxides

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011148805A (ja) * 2004-08-06 2011-08-04 Proteolix Inc プロテアソーム酵素阻害のための化合物

Also Published As

Publication number Publication date
BRPI0514102B1 (pt) 2020-07-07
EP2266999A3 (en) 2011-09-14
LTC1781688I2 (lt) 2017-09-25
HK1231491A1 (en) 2017-12-22
US7417042B2 (en) 2008-08-26
SI1781688T1 (sl) 2011-05-31
EP2266999B1 (en) 2014-09-24
BR122020008634B1 (pt) 2021-02-17
CN102286070A (zh) 2011-12-21
NO20170381A1 (no) 2007-04-16
LU93015I2 (fr) 2016-06-06
CN102286070B (zh) 2014-12-10
NO20070965L (no) 2007-04-16
US20140342977A1 (en) 2014-11-20
HUS1600014I1 (hu) 2016-05-30
BRPI0514102B8 (pt) 2021-05-25
IL221572B (en) 2018-10-31
PL1781688T3 (pl) 2011-06-30
HK1103525A1 (en) 2007-12-21
US20190211058A1 (en) 2019-07-11
US20070191284A1 (en) 2007-08-16
PL3101026T3 (pl) 2018-12-31
ES2525248T3 (es) 2014-12-19
SG10201701794UA (en) 2017-04-27
NO341015B1 (no) 2017-08-07
CY2016009I1 (el) 2016-08-31
KR20130080064A (ko) 2013-07-11
HUE038005T2 (hu) 2018-09-28
IL181127A0 (en) 2007-07-04
BRPI0514102A (pt) 2008-05-27
PT1781688E (pt) 2011-04-05
EP1781688A1 (en) 2007-05-09
EP3101026B1 (en) 2018-03-28
US20060030533A1 (en) 2006-02-09
CA2589765A1 (en) 2006-02-16
DK1781688T3 (da) 2011-03-14
US20220267372A1 (en) 2022-08-25
IL261892B (en) 2019-12-31
JP2008509166A (ja) 2008-03-27
LT3101026T (lt) 2018-07-10
KR101544258B1 (ko) 2015-08-21
EP3101026A1 (en) 2016-12-07
JP5394423B2 (ja) 2014-01-22
NO344397B1 (no) 2019-11-25
HK1152716A1 (en) 2012-03-09
FR16C0017I2 (fr) 2016-08-26
US20050245435A1 (en) 2005-11-03
US7232818B2 (en) 2007-06-19
CY2016009I2 (el) 2016-08-31
US20180170962A1 (en) 2018-06-21
US20200071356A1 (en) 2020-03-05
BR122020008634B8 (pt) 2021-07-27
US20200325172A1 (en) 2020-10-15
US20210179663A1 (en) 2021-06-17
IL261892A (en) 2018-10-31
JP2011148805A (ja) 2011-08-04
DE602005026019D1 (de) 2011-03-03
EP1781688B1 (en) 2011-01-19
WO2006017842A1 (en) 2006-02-16
AU2005271232A1 (en) 2006-02-16
ATE496062T1 (de) 2011-02-15
ES2674277T3 (es) 2018-06-28
CY1116771T1 (el) 2016-08-31
PT3101026T (pt) 2018-08-03
IL181127A (en) 2013-03-24
SI3101026T1 (en) 2018-08-31
EP2270026B1 (en) 2016-05-18
US7491704B2 (en) 2009-02-17
US20160222057A1 (en) 2016-08-04
KR101354280B1 (ko) 2014-01-23
LTPA2016010I1 (lt) 2016-04-25
EP2270026A3 (en) 2011-09-14
EP2266999A2 (en) 2010-12-29
EP2270026A2 (en) 2011-01-05
HK1152536A1 (en) 2012-03-02
SG155187A1 (en) 2009-09-30
CA2589765C (en) 2015-06-30
CY1120677T1 (el) 2019-12-11
KR20120135355A (ko) 2012-12-12
KR20070047780A (ko) 2007-05-07
FR16C0017I1 (cg-RX-API-DMAC7.html) 2016-06-24
IL221572A0 (en) 2012-10-31
AU2005271232B2 (en) 2012-07-05
DK3101026T3 (en) 2018-06-18
US20150361134A1 (en) 2015-12-17

Similar Documents

Publication Publication Date Title
JP4743720B2 (ja) プロテアソーム酵素阻害のための化合物
EP1745064B1 (en) Compounds for proteasome enzyme inhibition
US20120329705A1 (en) Compounds for proteasome enzyme inhibition
CN101044157B (zh) 用于抑制蛋白酶体的化合物
HK1231491B (en) Compounds for proteasome enzyme inhibition
HK1152716B (en) Compounds for proteasome enzyme inhibition
HK1103525B (en) Compounds for proteasome enzyme inhibition
HK1097860B (en) Compounds for proteasome enzyme inhibition

Legal Events

Date Code Title Description
RD02 Notification of acceptance of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7422

Effective date: 20080327

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20080415

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20080807

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20080807

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20101130

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20110228

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110304

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20110307

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20110405

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20110502

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20140520

Year of fee payment: 3

R150 Certificate of patent or registration of utility model

Ref document number: 4743720

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

Free format text: JAPANESE INTERMEDIATE CODE: R150

S533 Written request for registration of change of name

Free format text: JAPANESE INTERMEDIATE CODE: R313533

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R153 Grant of patent term extension

Free format text: JAPANESE INTERMEDIATE CODE: R153

R153 Grant of patent term extension

Free format text: JAPANESE INTERMEDIATE CODE: R153

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R153 Grant of patent term extension

Free format text: JAPANESE INTERMEDIATE CODE: R153

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250