AU2005238445B2 - Compounds for enzyme inhibition - Google Patents

Compounds for enzyme inhibition Download PDF

Info

Publication number
AU2005238445B2
AU2005238445B2 AU2005238445A AU2005238445A AU2005238445B2 AU 2005238445 B2 AU2005238445 B2 AU 2005238445B2 AU 2005238445 A AU2005238445 A AU 2005238445A AU 2005238445 A AU2005238445 A AU 2005238445A AU 2005238445 B2 AU2005238445 B2 AU 2005238445B2
Authority
AU
Australia
Prior art keywords
compound
alkyl
treating
hydrogen
administering
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
Application number
AU2005238445A
Other languages
English (en)
Other versions
AU2005238445A1 (en
Inventor
Ronald T. Borchardt
Barry A. Bunin
John Clifford Chabala
Craig M. Crews
Guy J. Laidig
John H. Musser
Mark S. Smyth
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=34965899&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AU2005238445(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
Priority to AU2005271232A priority Critical patent/AU2005271232B2/en
Publication of AU2005238445A1 publication Critical patent/AU2005238445A1/en
Application granted granted Critical
Publication of AU2005238445B2 publication Critical patent/AU2005238445B2/en
Priority to AU2012211349A priority patent/AU2012211349A1/en
Assigned to ONYX THERAPEUTICS, INC. reassignment ONYX THERAPEUTICS, INC. Request to Amend Deed and Register Assignors: PROTEOLIX, INC.
Anticipated expiration legal-status Critical
Expired 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
    • C07K5/10Tetrapeptides
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1016Tetrapeptides 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
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • C07K5/0827Tripeptides containing heteroatoms different from O, S, or N

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)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • AIDS & HIV (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines Containing Plant Substances (AREA)
AU2005238445A 2004-04-15 2005-04-14 Compounds for enzyme inhibition Expired AU2005238445B2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2005271232A AU2005271232B2 (en) 2004-04-15 2005-08-08 Compounds for proteasome enzyme inhibition
AU2012211349A AU2012211349A1 (en) 2004-04-15 2012-08-03 Compounds for enzyme inhibition

Applications Claiming Priority (15)

Application Number Priority Date Filing Date Title
US56234004P 2004-04-15 2004-04-15
US60/562,340 2004-04-15
US56909604P 2004-05-07 2004-05-07
US60/569,096 2004-05-07
US59940104P 2004-08-06 2004-08-06
US60/599,401 2004-08-06
US61000104P 2004-09-14 2004-09-14
US61015904P 2004-09-14 2004-09-14
US61000204P 2004-09-14 2004-09-14
US60/610,002 2004-09-14
US60/610,001 2004-09-14
US60/610,159 2004-09-14
US62057304P 2004-10-20 2004-10-20
US60/620,573 2004-10-20
PCT/US2005/012740 WO2005105827A2 (en) 2004-04-15 2005-04-14 Compounds for proteasome enzyme inhibition

Related Child Applications (2)

Application Number Title Priority Date Filing Date
AU2005271232A Division AU2005271232B2 (en) 2004-04-15 2005-08-08 Compounds for proteasome enzyme inhibition
AU2012211349A Division AU2012211349A1 (en) 2004-04-15 2012-08-03 Compounds for enzyme inhibition

Publications (2)

Publication Number Publication Date
AU2005238445A1 AU2005238445A1 (en) 2005-11-10
AU2005238445B2 true AU2005238445B2 (en) 2012-05-03

Family

ID=34965899

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2005238445A Expired AU2005238445B2 (en) 2004-04-15 2005-04-14 Compounds for enzyme inhibition

Country Status (17)

Country Link
US (9) US8129346B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EP (1) EP1745064B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
JP (3) JP5616569B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CN (2) CN103554222A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AT (1) ATE494298T1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AU (1) AU2005238445B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
BE (1) BE2016C014I2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
BR (1) BRPI0509879A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CA (1) CA2562411A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CY (1) CY1117244T1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
DE (1) DE602005025750D1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
DK (1) DK1745064T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IL (3) IL178400A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PL (1) PL1745064T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PT (1) PT1745064E (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
SG (2) SG185306A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
WO (1) WO2005105827A2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8198270B2 (en) 2004-04-15 2012-06-12 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
AU2012203602B2 (en) * 2004-04-15 2015-08-27 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
US7232818B2 (en) * 2004-04-15 2007-06-19 Proteolix, Inc. Compounds for enzyme inhibition
SG185306A1 (en) 2004-04-15 2012-11-29 Onyx Therapeutics Inc Compounds for proteasome enzyme inhibition
EP2564834A3 (en) 2004-05-10 2013-08-21 Onyx Therapeutics, Inc. Compounds for Proteasome Enzyme Inhibition
KR101299821B1 (ko) 2004-12-07 2013-09-03 프로테올릭스, 인코퍼레이티드 프로테아좀 저해를 위한 조성물
EP1948678B1 (en) 2005-11-09 2013-05-01 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
MY183014A (en) * 2006-06-19 2021-02-05 Onyx Therapeutics Inc Compounds for enzyme inhibition
NZ584814A (en) 2007-10-04 2012-03-30 Onyx Therapeutics Inc Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides
MX2011004225A (es) * 2008-10-21 2011-06-21 Onyx Therapeutics Inc Terapia de combinacion con epoxicetonas peptidicas.
JP5866277B2 (ja) 2009-03-16 2016-02-17 ザ ガバニング カウンシル オブ ザ ユニバーシティ オブ トロント 環状アミノ酸分子およびその製造方法
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
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
US8697646B2 (en) 2010-04-07 2014-04-15 Onyx Therapeutics, Inc. Crystalline peptide epoxyketone immunoproteasome inhibitor
HK1207827A1 (en) * 2012-05-08 2016-02-12 Onyx Therapeutics, Inc. Cylodextrin complexation methods for formulating peptide proteasome inhibitors
TW201414751A (zh) 2012-07-09 2014-04-16 歐尼克斯治療公司 肽環氧酮蛋白酶抑制劑之前驅藥物
US10076384B2 (en) 2013-03-08 2018-09-18 Symple Surgical, Inc. Balloon catheter apparatus with microwave emitter
CA2904630A1 (en) 2013-03-13 2014-10-02 Sanofi Compositions comprising anti-cd38 antibodies and carfilzomib
JP6851826B2 (ja) 2013-07-19 2021-03-31 オニキス セラピューティクス, インク.Onyx Therapeutics, Inc. がんの治療のためのpimキナーゼ阻害剤と組み合わせたペプチドエポキシケトンプロテアソーム阻害剤
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
WO2015032622A1 (en) * 2013-09-06 2015-03-12 Sandoz Ag Stereoselective synthesis of diols and triols by mannich reaction and their use in the synthesis of carfilzomib
CN105518019A (zh) * 2013-09-06 2016-04-20 桑多斯股份公司 肽环氧基酮的合成
CN104710507B (zh) * 2013-12-11 2018-08-14 深圳翰宇药业股份有限公司 一种卡非佐米的制备方法
WO2015121769A1 (en) 2014-02-13 2015-08-20 Ranbaxy Laboratories Limited Process for the preparation of methyl n-[(benzyloxy)-carbonyl]-l-leucyl-l-phenylalaninate
KR102462240B1 (ko) 2014-07-14 2022-11-03 센트랙스 인터내셔널, 아이엔씨. 효소 억제를 위한 에폭시케톤 화합물
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
US10253066B2 (en) 2014-12-02 2019-04-09 Fresenius Kabi Oncology Limited 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
WO2016116882A2 (en) * 2015-01-23 2016-07-28 Leiutis Pharmaceuticals Pvt Ltd Novel compositions of 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
WO2016170489A1 (en) 2015-04-24 2016-10-27 Fresenius Kabi Oncology Ltd. Pharmaceutical compositions of proteasome inhibitor
US10364269B2 (en) * 2015-05-21 2019-07-30 Laurus Labs Limited Processes for the preparation of carfilzomib or pharmaceutically acceptable salts thereof
US11072616B2 (en) 2015-11-11 2021-07-27 Universite De Montreal Cyclic peptides targeting alpha-4-beta-7 integrin
EP3494126A1 (en) 2016-08-02 2019-06-12 Synthon BV Process for making carfilzomib
CN109689635A (zh) 2016-09-14 2019-04-26 费森尤斯卡比肿瘤学有限公司 一种用于纯化卡非佐米中间体的方法
CN110088121A (zh) 2016-11-11 2019-08-02 循环治疗学公司 靶向α4β7整联蛋白的环肽多聚体
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
CN106946981B (zh) * 2017-03-08 2020-08-21 南京陵瑞医药科技有限公司 一种四肽环氧丙烷衍生物及其制备方法和用途
AU2018266248B2 (en) 2017-05-10 2022-01-27 Zealand Pharma A/S Homodetic cyclic peptides targeting a4β7 integrin
EP3694878A1 (en) 2017-09-14 2020-08-19 GlaxoSmithKline Intellectual Property Development Limited Combination treatment for cancer
CN113185575B (zh) * 2021-05-11 2022-07-12 四川大学 一种花生抗氧化多肽及其制备方法
WO2023220655A1 (en) 2022-05-11 2023-11-16 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
EP4522183A2 (en) 2022-05-11 2025-03-19 Celgene Corporation Methods and uses related to t cell therapy and production of same
EP4611798A1 (en) 2022-11-02 2025-09-10 Celgene Corporation Methods of treatment with t cell therapy and immunomodulatory agent maintenance therapy

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001028579A2 (en) * 1999-10-20 2001-04-26 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone and hair growth
US6831099B1 (en) * 1999-05-12 2004-12-14 Yale University Enzyme inhibition

Family Cites Families (48)

* 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
JPH01136498A (ja) 1987-11-21 1989-05-29 Nec Corp 状態監視用情報伝送装置
US5135919A (en) 1988-01-19 1992-08-04 Children's Medical Center Corporation Method and a pharmaceutical composition for the inhibition of angiogenesis
US5441944A (en) 1989-04-23 1995-08-15 The Trustees Of The University Of Pennsylvania Substituted cyclodextrin sulfates and their uses as growth modulating agents
US5071957A (en) 1989-08-04 1991-12-10 Bristol-Myers Company Antibiotic BU-4061T
US4990448A (en) 1989-08-04 1991-02-05 Bristol-Myers Company Bu-4061T
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
IE910713A1 (en) 1990-03-05 1991-09-11 Cephalon Inc Chymotrypsin-like proteases
US5340736A (en) 1991-05-13 1994-08-23 The President & Fellows Of Harvard College ATP-dependent protease and use of inhibitors for same in the treatment of cachexia and muscle wasting
GB9300048D0 (en) 1993-01-04 1993-03-03 Wellcome Found Endothelin converting enzyme inhibitors
US5693617A (en) 1994-03-15 1997-12-02 Proscript, Inc. Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein
US6083903A (en) 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
US6335358B1 (en) 1995-04-12 2002-01-01 President And Fellows Of Harvard College Lactacystin analogs
AU4499697A (en) 1996-09-13 1998-04-02 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
JP4080541B2 (ja) 1996-10-18 2008-04-23 バーテックス ファーマシューティカルズ インコーポレイテッド セリンプロテアーゼ、特にc型肝炎ウイルスns3プロテアーゼの阻害因子
WO1998025460A1 (en) 1996-12-13 1998-06-18 Zymogenetics, Inc. Compositions and methods for stimulating bone growth
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
AU750207B2 (en) 1997-06-13 2002-07-11 Cydex Pharmaceuticals, Inc. Polar drug or prodrug compositions with extended shelf-life storage and a method of making thereof
US6099851A (en) 1998-06-02 2000-08-08 Weisman; Kenneth M. Therapeutic uses of leuprolide acetate
US6902721B1 (en) 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6838436B1 (en) 1998-07-10 2005-01-04 Osteoscreen Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6462019B1 (en) 1998-07-10 2002-10-08 Osteoscreen, Inc. Inhibitors of proteasomal activity and production for stimulating bone growth
US6204257B1 (en) 1998-08-07 2001-03-20 Universtiy Of Kansas Water soluble prodrugs of hindered alcohols
KR20010080267A (ko) 1998-10-20 2001-08-22 밀레니엄 파머슈티컬스 인코퍼레이티드 프로테아솜 억제제 약물 작용을 모니터링하는 방법
US6492333B1 (en) 1999-04-09 2002-12-10 Osteoscreen, Inc. Treatment of myeloma bone disease with proteasomal and NF-κB activity inhibitors
DK1326632T3 (da) 2000-10-12 2007-01-15 Viromics Gmbh Protease-inhibitorer til behandling af infektioner af hepatitisvirus
WO2003059898A2 (en) 2002-01-08 2003-07-24 Eisai Co. Ltd. Eponemycin and epoxomicin analogs and uses thereof
AU2003220685A1 (en) 2002-04-09 2003-10-27 Greenville Hospital System Metastasis modulating activity of highly sulfated oligosaccharides
US20030224469A1 (en) 2002-06-03 2003-12-04 Buchholz Tonia J. Methods and kits for assays utilizing fluorescence polarization
US7232818B2 (en) 2004-04-15 2007-06-19 Proteolix, Inc. Compounds for enzyme inhibition
US8198270B2 (en) 2004-04-15 2012-06-12 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
SG185306A1 (en) * 2004-04-15 2012-11-29 Onyx Therapeutics Inc Compounds for proteasome enzyme inhibition
EP2564834A3 (en) 2004-05-10 2013-08-21 Onyx Therapeutics, Inc. Compounds for Proteasome Enzyme Inhibition
WO2005111009A2 (en) 2004-05-10 2005-11-24 Proteolix, Inc. Synthesis of amino acid keto-epoxides
EP1805208A2 (en) 2004-10-20 2007-07-11 Proteolix, Inc. Labeled compounds for proteasome inhibition
KR101299821B1 (ko) 2004-12-07 2013-09-03 프로테올릭스, 인코퍼레이티드 프로테아좀 저해를 위한 조성물
US7589066B2 (en) 2005-03-11 2009-09-15 The University Of North Carolina At Chapel Hill Potent and specific immunoproteasome inhibitors
EP1948678B1 (en) 2005-11-09 2013-05-01 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
AR057227A1 (es) 2005-12-09 2007-11-21 Centocor Inc Metodo para usar antagonistas de il6 con inhibidores del proteasoma
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
MY183014A (en) 2006-06-19 2021-02-05 Onyx Therapeutics Inc Compounds for enzyme inhibition
JP4325683B2 (ja) * 2007-02-14 2009-09-02 セイコーエプソン株式会社 画像表示装置、及び画像表示装置の制御方法
WO2008140782A2 (en) 2007-05-10 2008-11-20 Proteolix, Inc. Compounds for enzyme inhibition
NZ584814A (en) 2007-10-04 2012-03-30 Onyx Therapeutics Inc Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides
MX2011004225A (es) 2008-10-21 2011-06-21 Onyx Therapeutics Inc Terapia de combinacion con epoxicetonas peptidicas.

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6831099B1 (en) * 1999-05-12 2004-12-14 Yale University Enzyme inhibition
WO2001028579A2 (en) * 1999-10-20 2001-04-26 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone and hair growth

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Chemistry and Biology, 1995, 6 (11), 811-822. *
Medicinal Research Reviews, 2001, 21 (4), 245-273. *
Molecular Cell, 2001, 7 (2), 411-420. *

Also Published As

Publication number Publication date
AU2005238445A1 (en) 2005-11-10
BE2016C014I2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2024-10-09
JP2014012676A (ja) 2014-01-23
CN103554222A (zh) 2014-02-05
DK1745064T3 (da) 2011-04-11
EP1745064B1 (en) 2011-01-05
US20120101050A1 (en) 2012-04-26
US20080200398A1 (en) 2008-08-21
IL178400A0 (en) 2007-02-11
IL178400A (en) 2012-02-29
US20120094930A1 (en) 2012-04-19
SG152239A1 (en) 2009-05-29
EP1745064A2 (en) 2007-01-24
US20120094926A1 (en) 2012-04-19
WO2005105827A2 (en) 2005-11-10
US20120101048A1 (en) 2012-04-26
US8207127B2 (en) 2012-06-26
US8129346B2 (en) 2012-03-06
PL1745064T3 (pl) 2011-06-30
BRPI0509879A (pt) 2007-10-16
CN102174076A (zh) 2011-09-07
JP2012041346A (ja) 2012-03-01
US8324174B2 (en) 2012-12-04
US8207124B2 (en) 2012-06-26
IL217210A0 (en) 2012-01-31
WO2005105827A3 (en) 2006-03-30
US8207126B2 (en) 2012-06-26
SG185306A1 (en) 2012-11-29
US8207125B2 (en) 2012-06-26
CA2562411A1 (en) 2005-11-10
PT1745064E (pt) 2011-03-23
JP2008501637A (ja) 2008-01-24
JP5616569B2 (ja) 2014-10-29
IL217211A0 (en) 2012-01-31
ATE494298T1 (de) 2011-01-15
US20120094929A1 (en) 2012-04-19
CY1117244T1 (el) 2017-04-05
US8207297B2 (en) 2012-06-26
US20120277146A1 (en) 2012-11-01
US20120094928A1 (en) 2012-04-19
DE602005025750D1 (de) 2011-02-17
HK1097860A1 (en) 2007-07-06
US20130324459A1 (en) 2013-12-05

Similar Documents

Publication Publication Date Title
AU2005238445B2 (en) Compounds for enzyme inhibition
US7491704B2 (en) Compounds for enzyme inhibition
HK1231491B (en) Compounds for proteasome enzyme inhibition
HK1097860B (en) Compounds for proteasome enzyme inhibition
AU2012211349A1 (en) Compounds for enzyme inhibition
HK1152716B (en) Compounds for proteasome enzyme inhibition
HK1103525B (en) Compounds for proteasome enzyme inhibition

Legal Events

Date Code Title Description
DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: DELETE CO-INVENTOR SCHNEEKLOTH, JR JOHN S

FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired