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CY1119405T1 - Ενωση για την αναστολη ενζυμων - Google Patents

Ενωση για την αναστολη ενζυμων

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Publication number
CY1119405T1
CY1119405T1 CY20171100781T CY171100781T CY1119405T1 CY 1119405 T1 CY1119405 T1 CY 1119405T1 CY 20171100781 T CY20171100781 T CY 20171100781T CY 171100781 T CY171100781 T CY 171100781T CY 1119405 T1 CY1119405 T1 CY 1119405T1
Authority
CY
Cyprus
Prior art keywords
peptide
based compounds
union
enzymes
suspension
Prior art date
Application number
CY20171100781T
Other languages
English (en)
Inventor
Han-Jie Zhou
Congcong M. Sun
Kevin D. Shenk
Guy J. Laidig
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
Application filed by Onyx Therapeutics, Inc. filed Critical Onyx Therapeutics, Inc.
Publication of CY1119405T1 publication Critical patent/CY1119405T1/el

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    • A61K38/00Medicinal preparations containing peptides
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
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Abstract

Οι ενώσεις που βασίζονται σε πεπτίδια οι οποίες περιλαμβάνουν τριμελείς δακτυλίους που περιέχουν ετεροάτομα αναστέλλουν αποτελεσματικά και επιλεκτικά συγκεκριμένες δράσεις πυρηνόφιλων υδρολασών με τελικό άκρο Ν (Ntn) οι οποίες σχετίζονται με το πρωτεάσωμα. Οι ενώσεις που βασίζονται σε πεπτίδια περιλαμβάνουν ένα εποξείδιο ή αζιριδίνη, και λειτουργικοποίηση στο τελικό άκρο Ν. Ανάμεσα σε άλλες θεραπευτικές χρήσεις, οι ενώσεις που βασίζονται σε πεπτίδια αναμένεται να παρουσιάζουν αντι-φλεγμονώδεις ιδιότητες και αναστολή του κυτταρικού πολλαπλασιασμού. Η χορήγηση από το στόμα αυτών των αναστολέων πρωτεασώματος που βασίζονται σε πεπτίδια είναι δυνατή εξαιτίας των προφίλ βιοδιαθεσιμότητάς τους.
CY20171100781T 2005-11-09 2017-07-21 Ενωση για την αναστολη ενζυμων CY1119405T1 (el)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US73611805P 2005-11-09 2005-11-09
US84258206P 2006-09-05 2006-09-05
EP06837164.0A EP1948678B1 (en) 2005-11-09 2006-11-09 Compounds for enzyme inhibition

Publications (1)

Publication Number Publication Date
CY1119405T1 true CY1119405T1 (el) 2018-03-07

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CY20171100781T CY1119405T1 (el) 2005-11-09 2017-07-21 Ενωση για την αναστολη ενζυμων

Country Status (29)

Country Link
US (8) US8716322B2 (el)
EP (2) EP2623113B1 (el)
JP (3) JP5436860B2 (el)
KR (3) KR101434522B1 (el)
CN (2) CN101405294B (el)
AU (1) AU2006311584B2 (el)
BR (1) BRPI0618468A2 (el)
CA (1) CA2629084C (el)
CY (1) CY1119405T1 (el)
DK (2) DK1948678T3 (el)
EC (1) ECSP088460A (el)
ES (2) ES2628620T3 (el)
GT (1) GT200800063A (el)
HK (1) HK1220208A1 (el)
HN (1) HN2008000738A (el)
HU (1) HUE034863T2 (el)
IL (2) IL191344A (el)
LT (1) LT2623113T (el)
MX (1) MX2008006090A (el)
MY (2) MY145757A (el)
NZ (2) NZ595196A (el)
PH (1) PH12013501656A1 (el)
PL (2) PL1948678T3 (el)
PT (2) PT1948678E (el)
RU (2) RU2453556C2 (el)
SI (1) SI2623113T1 (el)
SV (1) SV2009002903A (el)
WO (1) WO2007056464A1 (el)
ZA (1) ZA200804455B (el)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8129346B2 (en) 2004-04-15 2012-03-06 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
US8198270B2 (en) * 2004-04-15 2012-06-12 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
CA2565407A1 (en) * 2004-05-10 2005-11-24 Proteolix, Inc. Compounds for enzyme inhibition
KR101434522B1 (ko) 2005-11-09 2014-08-26 오닉스 세라퓨틱스, 인크. 효소 저해를 위한 화합물
US7691852B2 (en) 2006-06-19 2010-04-06 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
WO2008140782A2 (en) * 2007-05-10 2008-11-20 Proteolix, Inc. Compounds for enzyme inhibition
RS54847B2 (sr) 2007-10-04 2019-09-30 Onyx Therapeutics Inc Inhibitori kristalne peptid epoksi keton proteaze i sinteza aminokiselinskih keto-epoksida
JP5554720B2 (ja) * 2007-12-19 2014-07-23 エイボン プロダクツ インコーポレーテッド 非タンパク質性アミノ酸を含む局所用組成物
JP5675629B2 (ja) 2008-10-21 2015-02-25 オニキス セラピューティクス, インク.Onyx Therapeutics, Inc. ペプチドエポキシケトンを用いた併用療法
AR075899A1 (es) 2009-03-20 2011-05-04 Onyx Therapeutics Inc Tripeptidos epoxicetonas cristalinos inhibidores de proteasa
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
MA34133B1 (fr) 2010-03-01 2013-04-03 Onyx Therapeutics Inc Composes pour inhibiteurs de l'immunoproteasome
WO2011136905A2 (en) 2010-04-07 2011-11-03 Onyx Therapeutics, Inc. Crystalline peptide epoxyketone immunoproteasome inhibitor
EP2810066B1 (en) 2012-01-24 2019-07-31 Millennium Pharmaceuticals, Inc. Methods of treatment of cancer
MY165002A (en) * 2012-05-08 2018-02-28 Onyx Therapeutics Inc Cylodextrin complexation methods for formulating peptide proteasome inhibitors
US20140105921A1 (en) 2012-07-09 2014-04-17 Onyx Therapeutics, Inc. Prodrugs of Peptide Epoxy Ketone Protease Inhibitors
CA2881999A1 (en) * 2012-08-14 2014-02-20 Abdelmalik Slassi Fluorinated epoxyketone-based compounds and uses thereof as proteasome inhibitors
TW201422255A (zh) * 2012-10-24 2014-06-16 Onyx Therapeutics Inc 用於蛋白酶體抑制劑之調整釋放製劑
AR095426A1 (es) * 2013-03-14 2015-10-14 Onyx Therapeutics Inc Inhibidores tripeptídicos de la epoxicetona proteasa
EA030957B1 (ru) 2013-03-14 2018-10-31 Оникс Терапьютикс, Инк. Дипептидные и трипептидные эпоксикетонные ингибиторы протеазы
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
CN104945470B (zh) * 2014-03-30 2020-08-11 浙江大学 杂环构建的三肽环氧酮类化合物及制备和应用
KR102462240B1 (ko) 2014-07-14 2022-11-03 센트랙스 인터내셔널, 아이엔씨. 효소 억제를 위한 에폭시케톤 화합물
US10301273B2 (en) 2014-08-07 2019-05-28 Mayo Foundation For Medical Education And Research Compounds and methods for treating cancer
WO2016069479A1 (en) 2014-10-27 2016-05-06 Apicore Us Llc Methods of making carfilzomib and intermediates thereof
US9980976B2 (en) * 2015-02-17 2018-05-29 Northwestern University Use of REDD1 inhibitors to dissociate therapeutic and adverse atrophogenic effects of glucocorticoid receptor agonists
WO2017147410A1 (en) 2016-02-25 2017-08-31 Amgen Inc. Compounds that inhibit mcl-1 protein
EP4296257A3 (en) 2016-06-29 2024-03-20 Kezar Life Sciences Process of preparing a peptide epoxyketone immunoproteasome inhibitor
US10836756B2 (en) 2016-06-29 2020-11-17 Kezar Life Sciences Crystalline salts of peptide epoxyketone immunoproteasome inhibitor
KR101720736B1 (ko) 2016-12-15 2017-03-28 이숙자 스플린트용 커버 조립체
EP3589659B1 (en) 2017-02-28 2025-04-09 Mayo Foundation for Medical Education and Research Combinations for use in the treatment of cancer
EP3694878A1 (en) 2017-09-14 2020-08-19 GlaxoSmithKline Intellectual Property Development Limited Combination treatment for cancer
US10537585B2 (en) 2017-12-18 2020-01-21 Dexcel Pharma Technologies Ltd. Compositions comprising dexamethasone
US11243207B2 (en) 2018-03-29 2022-02-08 Mayo Foundation For Medical Education And Research Assessing and treating cancer
CN110092813B (zh) * 2019-06-05 2021-05-11 南京师范大学 一种三肽环氧丙烷衍生物及其制备方法和用途
TWI879949B (zh) * 2020-04-27 2025-04-11 南韓商奧土擇破利悟股份有限公司 用於ubr盒結構域配體之化合物、組成物以及醫藥組成物
WO2025092827A1 (zh) * 2023-10-30 2025-05-08 上海汇伦医药股份有限公司 一种环氧类化合物及其应用

Family Cites Families (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4733665C2 (en) * 1985-11-07 2002-01-29 Expandable Grafts Partnership Expandable intraluminal graft and method and apparatus for implanting an expandable intraluminal graft
US5135919A (en) * 1988-01-19 1992-08-04 Children's Medical Center Corporation Method and a pharmaceutical composition for the inhibition of angiogenesis
US5441944A (en) * 1989-04-23 1995-08-15 The Trustees Of The University Of Pennsylvania Substituted cyclodextrin sulfates and their uses as growth modulating agents
US4990448A (en) 1989-08-04 1991-02-05 Bristol-Myers Company Bu-4061T
US5071957A (en) 1989-08-04 1991-12-10 Bristol-Myers Company Antibiotic BU-4061T
KR0166088B1 (ko) * 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
HUT62312A (en) 1990-03-05 1993-04-28 Cephalon Inc Process for producing chymotrypsin-like proteases and their inhibitors
US5340736A (en) * 1991-05-13 1994-08-23 The President & Fellows Of Harvard College ATP-dependent protease and use of inhibitors for same in the treatment of cachexia and muscle wasting
US5519029A (en) * 1992-09-08 1996-05-21 Boehringer Mannheim Italia, S.P.A. 2-aminoalkyl-5-aminoalkylamino substituted-isoquinoindazole-6(2H)-ones
GB9300048D0 (en) 1993-01-04 1993-03-03 Wellcome Found Endothelin converting enzyme inhibitors
TW380137B (en) 1994-03-04 2000-01-21 Merck & Co Inc Process for making an epoxide
US5693617A (en) 1994-03-15 1997-12-02 Proscript, Inc. Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein
US6660268B1 (en) * 1994-03-18 2003-12-09 The President And Fellows Of Harvard College Proteasome regulation of NF-KB activity
US6506876B1 (en) * 1994-10-11 2003-01-14 G.D. Searle & Co. LTA4 hydrolase inhibitor pharmaceutical compositions and methods of use
US6083903A (en) 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
DE19505263A1 (de) 1995-02-16 1996-08-22 Consortium Elektrochem Ind Verfahren zur Reinigung von wasserlöslichen Cyclodextrinderivaten
US6335358B1 (en) * 1995-04-12 2002-01-01 President And Fellows Of Harvard College Lactacystin analogs
US6150415A (en) 1996-08-13 2000-11-21 The Regents Of The University Of California Epoxide hydrolase complexes and methods therewith
WO1998010779A1 (en) 1996-09-13 1998-03-19 New York University Method for treating parasitic diseases with proteasome inhibitors
SI0932617T1 (en) 1996-10-18 2002-06-30 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
HU227742B1 (en) * 1996-10-18 2012-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
US5874418A (en) * 1997-05-05 1999-02-23 Cydex, Inc. Sulfoalkyl ether cyclodextrin based solid pharmaceutical formulations and their use
US6046177A (en) * 1997-05-05 2000-04-04 Cydex, Inc. Sulfoalkyl ether cyclodextrin based controlled release solid pharmaceutical formulations
DE69819721T2 (de) * 1997-06-13 2004-09-23 Cydex Inc., Overland Park Zusammensetzung mit erhöhter lagerstabilität enthaltend cyclodextrin und wirkstoffe oder wirkstoff-vorstufen, die in wasserunlösliche komponenten zersetzt werden
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
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
US6831099B1 (en) 1999-05-12 2004-12-14 Yale University Enzyme inhibition
RS50470B (sr) * 1999-08-13 2010-03-02 Biogen Idec Ma Inc. Inhibitori ćelijske adhezije
CA2385958A1 (en) 1999-10-20 2001-04-26 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone and hair growth
CN1452771A (zh) * 2000-09-04 2003-10-29 索尼公司 反射层、具有反射层的光学记录介质和用于形成反射层的溅射标板
EP2305291A1 (de) 2000-10-12 2011-04-06 ViroLogik GmbH Verwendung von Proteasome Hemmern zur Behandlung von HIV Infektionen
US6699835B2 (en) * 2001-01-25 2004-03-02 The United States Of America As Represented By The Department Of Health And Human Services Formulation of boronic acid compounds
US6740674B2 (en) * 2001-05-21 2004-05-25 Alcon, Inc. Use of proteasome inhibitors to treat dry eye disorders
JP4412586B2 (ja) 2002-01-08 2010-02-10 エーザイ・アール・アンド・ディー・マネジメント株式会社 エポネマイシンおよびエポキソマイシン類似物およびそれらの用途
US20040116329A1 (en) * 2002-01-29 2004-06-17 Epstein Stephen E. Inhibition of proteasomes to prevent restenosis
WO2003086283A2 (en) 2002-04-09 2003-10-23 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
US20030224469A1 (en) 2002-06-03 2003-12-04 Buchholz Tonia J. Methods and kits for assays utilizing fluorescence polarization
US7902185B2 (en) * 2002-06-03 2011-03-08 Als Therapy Development Foundation, Inc. Treatment of neurodegenerative diseases using proteasome modulators
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
KR101367574B1 (ko) 2003-04-08 2014-02-25 미쓰비시 타나베 파마 코퍼레이션 S1p 수용체 아고니스트 및 당 알콜을 포함하는 고형 제약 조성물
AU2004255564A1 (en) * 2003-06-10 2005-01-20 The J. David Gladstone Institutes Methods for treating lentivirus infections
US7012063B2 (en) 2003-06-13 2006-03-14 Children's Medical Center Corporation Reducing axon degeneration with proteasome inhibitors
KR20070007075A (ko) 2003-12-31 2007-01-12 사이덱스 인크 술포알킬 에테르 시클로덱스트린 및 코르티코스테로이드를함유한 흡입용 제형
GB0400804D0 (en) * 2004-01-14 2004-02-18 Innoscience Technology Bv Pharmaceutical compositions
US8129346B2 (en) * 2004-04-15 2012-03-06 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
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
US20050256324A1 (en) 2004-05-10 2005-11-17 Proteolix, Inc. Synthesis of amino acid keto-epoxides
CA2565407A1 (en) * 2004-05-10 2005-11-24 Proteolix, Inc. Compounds for enzyme inhibition
US20060088471A1 (en) * 2004-10-20 2006-04-27 Proteolix, Inc. Compounds for enzyme inhibition
ES2549763T3 (es) * 2004-12-07 2015-11-02 Onyx Therapeutics, Inc. Composición para inhibición del proteasoma
US7468383B2 (en) 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
WO2006099261A2 (en) 2005-03-11 2006-09-21 The University Of North Carolina At Chapel Hill Potent and specific immunoproteasome inhibitors
EP1876893B1 (en) 2005-04-15 2012-04-11 Geron Corporation Cancer treatment by combined inhibition of proteasome and telomerase activities
GT200600350A (es) 2005-08-09 2007-03-28 Formulaciones líquidas
KR101434522B1 (ko) 2005-11-09 2014-08-26 오닉스 세라퓨틱스, 인크. 효소 저해를 위한 화합물
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
US7691852B2 (en) * 2006-06-19 2010-04-06 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
WO2008033807A2 (en) 2006-09-13 2008-03-20 The Arizona Board Of Regents On Behalf Of The University Of Arizona Synergistic combinations of antineoplastic thiol-binding mitochondrial oxidants and antineoplastic proteasome inhibitors for the treatment of cancer
JP2010516767A (ja) 2007-01-23 2010-05-20 グラスター ファーマシューティカルズ, インコーポレイテッド ロミデプシンおよびi.a.ボルテゾミブを含む併用療法
JP4325683B2 (ja) * 2007-02-14 2009-09-02 セイコーエプソン株式会社 画像表示装置、及び画像表示装置の制御方法
WO2008140782A2 (en) 2007-05-10 2008-11-20 Proteolix, Inc. Compounds for enzyme inhibition
CN101772507B (zh) 2007-08-06 2012-12-12 米伦纽姆医药公司 蛋白酶体抑制剂
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
RS54847B2 (sr) * 2007-10-04 2019-09-30 Onyx Therapeutics Inc Inhibitori kristalne peptid epoksi keton proteaze i sinteza aminokiselinskih keto-epoksida
WO2009051581A1 (en) 2007-10-16 2009-04-23 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
US7838673B2 (en) * 2007-10-16 2010-11-23 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
WO2009067453A1 (en) 2007-11-19 2009-05-28 Syndax Pharmaceuticals, Inc. Combinations of hdac inhibitors and proteasome inhibitors
EP2730580A1 (en) 2008-06-17 2014-05-14 Millennium Pharmaceuticals, Inc. Boronate ester compounds and pharmaceutical compositions thereof
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.
JP5675629B2 (ja) * 2008-10-21 2015-02-25 オニキス セラピューティクス, インク.Onyx Therapeutics, Inc. ペプチドエポキシケトンを用いた併用療法
AR075899A1 (es) * 2009-03-20 2011-05-04 Onyx Therapeutics Inc Tripeptidos epoxicetonas cristalinos inhibidores de proteasa
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
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
MA34133B1 (fr) 2010-03-01 2013-04-03 Onyx Therapeutics Inc Composes pour inhibiteurs de l'immunoproteasome
UA110612C2 (uk) 2010-03-31 2016-01-25 Мілленніум Фармасьютікалз, Інк. Похідні 1-аміно-2-циклопропілетилборонової кислоти
WO2011136905A2 (en) * 2010-04-07 2011-11-03 Onyx Therapeutics, Inc. Crystalline peptide epoxyketone immunoproteasome inhibitor

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