KR101544258B1 - 프로테아좀 효소 저해를 위한 화합물 - Google Patents

프로테아좀 효소 저해를 위한 화합물 Download PDF

Info

Publication number
KR101544258B1
KR101544258B1 KR1020127030701A KR20127030701A KR101544258B1 KR 101544258 B1 KR101544258 B1 KR 101544258B1 KR 1020127030701 A KR1020127030701 A KR 1020127030701A KR 20127030701 A KR20127030701 A KR 20127030701A KR 101544258 B1 KR101544258 B1 KR 101544258B1
Authority
KR
South Korea
Prior art keywords
mmol
quot
alkyl
treatment
proteasome
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
KR1020127030701A
Other languages
English (en)
Korean (ko)
Other versions
KR20120135355A (ko
Inventor
마크 에스. 스미스
가이 제이. 라이디그
Original Assignee
오닉스 세라퓨틱스, 인크.
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=KR101544258(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 오닉스 세라퓨틱스, 인크. filed Critical 오닉스 세라퓨틱스, 인크.
Publication of KR20120135355A publication Critical patent/KR20120135355A/ko
Application granted granted Critical
Publication of KR101544258B1 publication Critical patent/KR101544258B1/ko
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1016—Tetrapeptides 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
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • 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
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07—Tetrapeptides
    • 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
    • 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
    • C07K5/08—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
    • C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
    • 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
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1008—Tetrapeptides 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
    • C07K5/10—Tetrapeptides
    • C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material 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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Rheumatology (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)
KR1020127030701A 2004-08-06 2005-08-08 프로테아좀 효소 저해를 위한 화합물 Expired - Lifetime KR101544258B1 (ko)

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 Parent Applications (1)

Application Number Title Priority Date Filing Date
KR1020077003533A Division KR101354280B1 (ko) 2004-08-06 2005-08-08 프로테아좀 효소 저해를 위한 화합물

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020137016063A Division KR20130080064A (ko) 2004-08-06 2005-08-08 프로테아좀 효소 저해를 위한 화합물

Publications (2)

Publication Number Publication Date
KR20120135355A KR20120135355A (ko) 2012-12-12
KR101544258B1 true KR101544258B1 (ko) 2015-08-21

Family

ID=35502451

Family Applications (3)

Application Number Title Priority Date Filing Date
KR1020127030701A Expired - Lifetime KR101544258B1 (ko) 2004-08-06 2005-08-08 프로테아좀 효소 저해를 위한 화합물
KR1020137016063A Withdrawn KR20130080064A (ko) 2004-08-06 2005-08-08 프로테아좀 효소 저해를 위한 화합물
KR1020077003533A Expired - Lifetime KR101354280B1 (ko) 2004-08-06 2005-08-08 프로테아좀 효소 저해를 위한 화합물

Family Applications After (2)

Application Number Title Priority Date Filing Date
KR1020137016063A Withdrawn KR20130080064A (ko) 2004-08-06 2005-08-08 프로테아좀 효소 저해를 위한 화합물
KR1020077003533A Expired - Lifetime KR101354280B1 (ko) 2004-08-06 2005-08-08 프로테아좀 효소 저해를 위한 화합물

Country Status (24)

Country Link
US (12) US7232818B2 (enExample)
EP (4) EP2270026B1 (enExample)
JP (2) JP4743720B2 (enExample)
KR (3) KR101544258B1 (enExample)
CN (1) CN102286070B (enExample)
AT (1) ATE496062T1 (enExample)
AU (1) AU2005271232B2 (enExample)
BR (2) BR122020008634B8 (enExample)
CA (1) CA2589765C (enExample)
CY (3) CY1116771T1 (enExample)
DE (1) DE602005026019D1 (enExample)
DK (2) DK1781688T3 (enExample)
ES (2) ES2525248T3 (enExample)
FR (1) FR16C0017I2 (enExample)
HU (2) HUE038005T2 (enExample)
IL (3) IL181127A (enExample)
LT (2) LT3101026T (enExample)
LU (1) LU93015I2 (enExample)
NO (2) NO341015B1 (enExample)
PL (2) PL1781688T3 (enExample)
PT (2) PT1781688E (enExample)
SG (2) SG10201701794UA (enExample)
SI (2) SI1781688T1 (enExample)
WO (1) WO2006017842A1 (enExample)

Families Citing this family (81)

* 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
US8198270B2 (en) * 2004-04-15 2012-06-12 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
US7232818B2 (en) * 2004-04-15 2007-06-19 Proteolix, Inc. Compounds for enzyme inhibition
BRPI0509879A (pt) 2004-04-15 2007-10-16 Proteolix Inc compostos para inibição enzimática
US20050256324A1 (en) * 2004-05-10 2005-11-17 Proteolix, Inc. Synthesis of amino acid keto-epoxides
US8088741B2 (en) * 2004-05-10 2012-01-03 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
AU2005311709B2 (en) 2004-12-03 2011-07-28 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating neoplastic diseases
PT2261236E (pt) 2004-12-07 2015-10-30 Onyx Therapeutics Inc Composição para a inibição de proteassoma
NZ595196A (en) 2005-11-09 2013-03-28 Proteolix Inc Peptide-based compounds for enzyme inhibition
BRPI0713309A2 (pt) 2006-06-19 2012-04-17 Proteolix Inc compostos para inibição de enzimas
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
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
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
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
CA2723465A1 (en) 2008-05-12 2009-11-19 Nereus Pharmaceuticals, Inc. Proteasome inhibitors
EA035100B1 (ru) 2008-10-21 2020-04-28 Оникс Терапьютикс, Инк. Комбинированная терапия с применением пептид эпоксикетонов
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
US8853147B2 (en) 2009-11-13 2014-10-07 Onyx Therapeutics, Inc. Use of peptide epoxyketones for metastasis suppression
BR112012022060A2 (pt) 2010-03-01 2018-05-08 Onyx Therapeutics Inc composto para a inibição de imunoproteassoma
RU2012147246A (ru) 2010-04-07 2014-05-20 Оникс Терапьютикс, Инк. Кристаллический пептидный эпоксикетонный ингебитор иммунопротеасомы
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
US9272014B2 (en) 2011-03-29 2016-03-01 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
WO2013071142A1 (en) 2011-11-11 2013-05-16 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
CA2862492A1 (en) 2012-01-24 2013-08-01 Millennium Pharmaceuticals, Inc. Methods of treatment of cancer
DK3702374T3 (da) 2012-02-15 2022-06-27 Cydex Pharmaceuticals Inc Fremsgangsmåde til fremstilling for cyclodextrin-derivater
EP2662094B1 (en) * 2012-05-08 2024-04-17 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
MX2015000813A (es) 2012-07-18 2015-09-07 Onyx Therapeutics Inc Composiciones liposómicas de inhibidores de proteasoma basadas en epoxicetona.
CA2881986A1 (en) * 2012-08-21 2014-02-27 Fluorinov Pharma Inc. Fluorinated epoxyketone-based tetrapeptide compounds and uses thereof as proteasome inhibitors
WO2014066274A1 (en) 2012-10-22 2014-05-01 Cydex Pharmaceuticals, Inc. Alkylated cyclodextrin compositions and processes for preparing and using the same
IL241407B (en) 2013-03-13 2022-06-01 Univ California Compositions comprising anti-cd38 antibodies and carfilzomib
AR095426A1 (es) 2013-03-14 2015-10-14 Onyx Therapeutics Inc Inhibidores tripeptídicos de la epoxicetona proteasa
KR20150131276A (ko) 2013-03-14 2015-11-24 오닉스 세라퓨틱스, 인크. 디펩타이드 및 트리펩타이드 에폭시 케톤 프로테이스 억제제
MX372671B (es) 2013-07-19 2020-04-23 Onyx Therapeutics Inc Inhibidores de proteasoma de epoxicetona peptídica en combinacion con inhibidores de cinasa pim para el tratamiento de canceres.
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
CN105518019A (zh) * 2013-09-06 2016-04-20 桑多斯股份公司 肽环氧基酮的合成
EP3041832A1 (en) * 2013-09-06 2016-07-13 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
US10851184B2 (en) 2014-08-22 2020-12-01 Cydex Pharmaceuticals, Inc. Fractionated alkylated cyclodextrin compositions and processes for preparing and using the same
US10329325B2 (en) 2014-09-24 2019-06-25 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
WO2016069479A1 (en) 2014-10-27 2016-05-06 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
CN107548400A (zh) 2014-12-02 2018-01-05 费森尤斯卡比肿瘤学有限公司 卡非佐米的纯化方法
WO2016108204A1 (en) 2014-12-31 2016-07-07 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
EP3411363A1 (en) 2015-12-11 2018-12-12 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
DK3494108T3 (da) 2016-08-05 2021-01-11 Amgen Inc Syntese af (s)-2-amino-4-methyl-1-((r)-2-methyloxiran-2-yl)-pentan-1-on og farmaceutisk acceptable salte deraf
WO2018051237A1 (en) 2016-09-14 2018-03-22 Fresenius Kabi Oncology Limited A process for purification of carfilzomib intermediate
EP3512602B1 (en) 2016-09-16 2024-03-27 HSF Pharmaceuticals Inhibitors of heat shock factors (hsf) 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
CA3075714A1 (en) 2017-09-14 2019-03-21 Glaxosmithkline Intellectual Property Development Limited Combination treatment for cancer
WO2019099715A1 (en) 2017-11-16 2019-05-23 Amgen Inc. Stable compositions of pegylated carfilzomib compounds
KR20250050122A (ko) * 2017-12-08 2025-04-14 뉴로지엑스 엘엘씨 알츠하이머 질환에 대한 동기화된 세포 주기 유전자 발현 시험 및 관련된 치료 방법
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
AU2018357829B2 (en) 2017-12-30 2019-09-26 Unity Biotechnology, Inc. Peptide-based proteasome inhibitors for treating conditions mediated by senescent cells and for treating cancer
NZ771565A (en) * 2018-06-22 2025-08-29 Ucl Business Ltd Novel compounds
WO2021072212A1 (en) * 2019-10-11 2021-04-15 Mayo Foundation For Medical Education And Research Proteasome inhibitors
EP4139289A1 (en) * 2020-04-21 2023-03-01 University of Rochester Inhibitors of human epididymus protein 4
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
WO2023220641A2 (en) 2022-05-11 2023-11-16 Juno Therapeutics, Inc. Methods and uses related to t cell therapy and production of same
TW202430548A (zh) 2022-09-29 2024-08-01 日商武田藥品工業股份有限公司 Ｃｄ３８結合融合蛋白組合療法
EP4611798A1 (en) 2022-11-02 2025-09-10 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
US6462019B1 (en) 1998-07-10 2002-10-08 Osteoscreen, Inc. Inhibitors of proteasomal activity and production for stimulating bone growth
US6838436B1 (en) 1998-07-10 2005-01-04 Osteoscreen Inc. Inhibitors of proteasomal activity for stimulating bone growth
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
CA2385958A1 (en) 1999-10-20 2001-04-26 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone and hair growth
US7524883B2 (en) 2002-01-08 2009-04-28 Eisai R&D Management Co., Ltd. Eponemycin and epoxomicin analogs and uses thereof
US7232818B2 (en) 2004-04-15 2007-06-19 Proteolix, Inc. Compounds for enzyme inhibition
BRPI0509879A (pt) * 2004-04-15 2007-10-16 Proteolix Inc compostos para inibição enzimática
US8088741B2 (en) 2004-05-10 2012-01-03 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
US20050256324A1 (en) 2004-05-10 2005-11-17 Proteolix, Inc. Synthesis of amino acid keto-epoxides

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Chemistry and Biology, Vol.6, pp.811-822(1999.10.15.)
Chemistry and Biology, Vol.8, pp.739-158(2001.)

Also Published As

Publication number Publication date
KR20070047780A (ko) 2007-05-07
ES2525248T3 (es) 2014-12-19
LT3101026T (lt) 2018-07-10
HK1152716A1 (en) 2012-03-09
KR20120135355A (ko) 2012-12-12
EP2270026A2 (en) 2011-01-05
IL261892A (en) 2018-10-31
KR101354280B1 (ko) 2014-01-23
EP2266999A3 (en) 2011-09-14
PT3101026T (pt) 2018-08-03
NO344397B1 (no) 2019-11-25
JP5394423B2 (ja) 2014-01-22
US20070191284A1 (en) 2007-08-16
BRPI0514102A (pt) 2008-05-27
IL221572B (en) 2018-10-31
BRPI0514102B1 (pt) 2020-07-07
PL1781688T3 (pl) 2011-06-30
US20190211058A1 (en) 2019-07-11
US20140342977A1 (en) 2014-11-20
FR16C0017I1 (enExample) 2016-06-24
NO20070965L (no) 2007-04-16
BRPI0514102B8 (pt) 2021-05-25
JP2011148805A (ja) 2011-08-04
PL3101026T3 (pl) 2018-12-31
IL181127A (en) 2013-03-24
DE602005026019D1 (de) 2011-03-03
US20180170962A1 (en) 2018-06-21
EP3101026B1 (en) 2018-03-28
CA2589765C (en) 2015-06-30
HK1231491A1 (en) 2017-12-22
SI3101026T1 (en) 2018-08-31
EP2266999B1 (en) 2014-09-24
ATE496062T1 (de) 2011-02-15
CY2016009I2 (el) 2016-08-31
CN102286070A (zh) 2011-12-21
WO2006017842A1 (en) 2006-02-16
HK1103525A1 (en) 2007-12-21
EP2270026B1 (en) 2016-05-18
SG155187A1 (en) 2009-09-30
EP1781688A1 (en) 2007-05-09
BR122020008634B1 (pt) 2021-02-17
FR16C0017I2 (fr) 2016-08-26
KR20130080064A (ko) 2013-07-11
EP3101026A1 (en) 2016-12-07
CN102286070B (zh) 2014-12-10
CY1116771T1 (el) 2016-08-31
BR122020008634B8 (pt) 2021-07-27
PT1781688E (pt) 2011-04-05
US20220267372A1 (en) 2022-08-25
JP4743720B2 (ja) 2011-08-10
LTPA2016010I1 (lt) 2016-04-25
IL181127A0 (en) 2007-07-04
LU93015I2 (fr) 2016-06-06
US7417042B2 (en) 2008-08-26
US20200325172A1 (en) 2020-10-15
US20210179663A1 (en) 2021-06-17
US7491704B2 (en) 2009-02-17
JP2008509166A (ja) 2008-03-27
EP2266999A2 (en) 2010-12-29
LTC1781688I2 (lt) 2017-09-25
EP2270026A3 (en) 2011-09-14
ES2674277T3 (es) 2018-06-28
US20060030533A1 (en) 2006-02-09
HK1152536A1 (en) 2012-03-02
US20050245435A1 (en) 2005-11-03
US7232818B2 (en) 2007-06-19
SG10201701794UA (en) 2017-04-27
US20160222057A1 (en) 2016-08-04
DK3101026T3 (en) 2018-06-18
US20200071356A1 (en) 2020-03-05
CA2589765A1 (en) 2006-02-16
IL261892B (en) 2019-12-31
IL221572A0 (en) 2012-10-31
NO341015B1 (no) 2017-08-07
EP1781688B1 (en) 2011-01-19
NO20170381A1 (no) 2007-04-16
CY2016009I1 (el) 2016-08-31
DK1781688T3 (da) 2011-03-14
AU2005271232B2 (en) 2012-07-05
CY1120677T1 (el) 2019-12-11
AU2005271232A1 (en) 2006-02-16
HUE038005T2 (hu) 2018-09-28
HUS1600014I1 (hu) 2016-05-30
SI1781688T1 (sl) 2011-05-31
US20150361134A1 (en) 2015-12-17

Similar Documents

Publication Publication Date Title
KR101544258B1 (ko) 프로테아좀 효소 저해를 위한 화합물
KR101275445B1 (ko) 효소 저해를 위한 화합물
US8088741B2 (en) Compounds for enzyme inhibition
US20120329705A1 (en) Compounds for proteasome enzyme inhibition
HK1231491B (en) Compounds for proteasome enzyme inhibition
HK1152716B (en) Compounds for proteasome enzyme inhibition
HK1103525B (en) Compounds for proteasome enzyme inhibition
HK1182651A (en) Compounds for proteasome enzyme inhibition

Legal Events

Date Code Title Description
A107 Divisional application of patent
A201 Request for examination
PA0104 Divisional application for international application

St.27 status event code: A-0-1-A10-A18-div-PA0104

St.27 status event code: A-0-1-A10-A16-div-PA0104

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

R17-X000 Change to representative recorded

St.27 status event code: A-3-3-R10-R17-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

A107 Divisional application of patent
PA0104 Divisional application for international application

St.27 status event code: A-0-1-A10-A18-div-PA0104

St.27 status event code: A-0-1-A10-A16-div-PA0104

E601 Decision to refuse application
PE0601 Decision on rejection of patent

St.27 status event code: N-2-6-B10-B15-exm-PE0601

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

J201 Request for trial against refusal decision
PJ0201 Trial against decision of rejection

St.27 status event code: A-3-3-V10-V11-apl-PJ0201

N231 Notification of change of applicant
PN2301 Change of applicant

St.27 status event code: A-3-3-R10-R13-asn-PN2301

St.27 status event code: A-3-3-R10-R11-asn-PN2301

T16-X000 Administrative procedure resumed

St.27 status event code: U-3-3-T10-T16-oth-X000

J301 Trial decision

Free format text: TRIAL DECISION FOR APPEAL AGAINST DECISION TO DECLINE REFUSAL REQUESTED 20131204

Effective date: 20150528

Free format text: TRIAL NUMBER: 2013101008596; TRIAL DECISION FOR APPEAL AGAINST DECISION TO DECLINE REFUSAL REQUESTED 20131204

Effective date: 20150528

PJ1301 Trial decision

St.27 status event code: A-3-3-V10-V15-crt-PJ1301

Decision date: 20150528

Appeal event data comment text: Appeal Kind Category : Appeal against decision to decline refusal, Appeal Ground Text : 2012 7030701

Appeal request date: 20131204

Appellate body name: Patent Examination Board

Decision authority category: Office appeal board

Decision identifier: 2013101008596

PS0901 Examination by remand of revocation

St.27 status event code: A-6-3-E10-E12-rex-PS0901

S901 Examination by remand of revocation
GRNO Decision to grant (after opposition)
PS0701 Decision of registration after remand of revocation

St.27 status event code: A-3-4-F10-F13-rex-PS0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

S17-X000 Non-exclusive voluntary license recorded

St.27 status event code: A-4-4-S10-S17-lic-X000

A101 Application to extend term of patent right by permit
PA0101 Application to register extension of term of patent right by permit, etc.

St.27 status event code: A-4-4-G10-G18-tex-PA0101

Protection beyond ip right term event data comment text: Claim Total Quantity : 2, Claim Number : 1 4, Period Limitation Text : 40, Comment Text : 11

PE0702 Decision to register extension of term of patent right by permit, etc.

St.27 status event code: A-4-4-G10-G20-tex-PE0702

Protection beyond ip right term event data comment text: Claim Total Quantity : 2, Claim Number : 1 4, Period Limitation Text : 40, Comment Text : 11

FPAY Annual fee payment

Payment date: 20180718

Year of fee payment: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 5

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 6

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 7

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 8

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 9

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 10

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 11