KR101441703B1 - 프로테아좀 저해를 위한 펩티드 에폭시케톤 - Google Patents

프로테아좀 저해를 위한 펩티드 에폭시케톤 Download PDF

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KR101441703B1
KR101441703B1 KR1020097000551A KR20097000551A KR101441703B1 KR 101441703 B1 KR101441703 B1 KR 101441703B1 KR 1020097000551 A KR1020097000551 A KR 1020097000551A KR 20097000551 A KR20097000551 A KR 20097000551A KR 101441703 B1 KR101441703 B1 KR 101441703B1
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alkyl
compound
pharmaceutically acceptable
heterocyclyl
hydrogen
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KR20090023477A (ko
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케빈 디. 센크
프란세스코 파를라티
한-지에 쥬
캐터린 실베인
마크 에스. 스미스
마크 케이. 벤네트
가이 제이. 레이디그
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오닉스 세라퓨틱스, 인크.
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    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
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Families Citing this family (41)

* 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
US8129346B2 (en) 2004-04-15 2012-03-06 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
EP2030981B1 (en) * 2004-05-10 2014-07-09 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
MY171061A (en) * 2005-11-09 2019-09-24 Onyx Therapeutics Inc Compounds for enzyme inhibition
CA2657213C (en) 2006-06-19 2017-01-03 Proteolix, Inc. Peptide epoxyketones for proteasome inhibition
KR20170125413A (ko) 2007-10-04 2017-11-14 오닉스 세라퓨틱스, 인크. 결정형 펩티드 에폭시 케톤 프로테아제 저해제 및 아미노산 케토-에폭시드의 합성
EP3090737A1 (en) 2008-10-21 2016-11-09 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
US8853147B2 (en) 2009-11-13 2014-10-07 Onyx Therapeutics, Inc. Use of peptide epoxyketones for metastasis suppression
EP2542238B1 (en) 2010-03-01 2015-08-12 Onyx Therapeutics, Inc. Compounds for immunoproteasome inhibition
NZ602872A (en) * 2010-04-07 2014-05-30 Onyx Therapeutics Inc Crystalline peptide epoxyketone immunoproteasome inhibitor
US8609610B2 (en) * 2011-02-18 2013-12-17 Trustees Of Dartmouth College Inhibitors of the trypsin-like site of the proteasome and methods of use thereof
JP2014509323A (ja) * 2011-02-28 2014-04-17 マックマスター ユニヴァーシティ ドーパミン受容体遮断薬による癌の処置
WO2013009923A1 (en) * 2011-07-13 2013-01-17 Creighton University Methods of promoting neuron growth
CN104411682B (zh) * 2012-06-29 2016-11-16 日产化学工业株式会社 用于制备立体选择性环氧酮化合物的方法
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
WO2014056954A1 (en) * 2012-10-12 2014-04-17 F. Hoffmann-La Roche Ag Macrocyclic ketoamide immunoproteasome inhibitors
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
CN104174021A (zh) * 2013-05-22 2014-12-03 复旦大学附属华山医院 蛋白酶体抑制剂在制备治疗慢性低度炎症性疾病药物中的用途
CN105518019A (zh) * 2013-09-06 2016-04-20 桑多斯股份公司 肽环氧基酮的合成
EP3092244B1 (en) 2014-01-10 2019-08-14 Cornell University Dipeptides as inhibitors of human immunoproteasomes
JP6551825B2 (ja) * 2014-02-10 2019-07-31 公立大学法人首都大学東京 クロマチン構造制御剤
DE102014010220A1 (de) 2014-07-10 2016-01-14 Immunologik Gmbh Mittel zur Behandlung retroviraler Infektionen
WO2016022955A1 (en) 2014-08-07 2016-02-11 Mayo Foundation For Medical Education And Research Compounds and methods for treating cancer
CN107073069B (zh) 2014-08-18 2022-03-08 康奈尔大学 作为人免疫蛋白酶体的抑制剂的二肽模拟物
CN105017181B (zh) * 2015-07-02 2017-10-10 南京师范大学 卡非佐米关键中间体及其衍生物的制备方法
WO2017032487A1 (en) 2015-08-27 2017-03-02 Technische Universität München Proteasome inhibitor comprising a signal-emitting moiety
WO2017066763A1 (en) * 2015-10-15 2017-04-20 Cornell University Proteasome inhibitors and uses thereof
SG11201811507YA (en) 2016-06-29 2019-01-30 Kezar Life Sciences Crystalline salts of peptide epoxyketone immunoproteasome inhibitor
BR112018077250A2 (pt) 2016-06-29 2019-04-02 Kezar Life Sciences processo de preparação de um inibidor de imunoproteassoma de epoxicetona peptídica e precursores dos mesmos
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
EP4606431A3 (en) 2017-02-28 2025-11-19 Mayo Foundation for Medical Education and Research Compounds and methods for treating cancer
US11357817B2 (en) 2017-05-15 2022-06-14 The Regents Of The University Of California Immunoproteasome inhibitor
WO2019040680A1 (en) 2017-08-23 2019-02-28 Krzar Life Sciences IMMUNOPROTEASOME INHIBITORS AND IMMUNOSUPPRESSANT AGENT IN THE TREATMENT OF AUTOIMMUNE DISORDERS
US11203613B2 (en) 2017-10-11 2021-12-21 Cornell University Peptidomimetic proteasome inhibitors
US11243207B2 (en) 2018-03-29 2022-02-08 Mayo Foundation For Medical Education And Research Assessing and treating cancer
JP7344486B2 (ja) 2018-03-30 2023-09-14 国立大学法人京都大学 心筋細胞成熟促進剤
US20240216325A1 (en) * 2019-11-25 2024-07-04 Cornell University Nuclear factor kappa b pathway inhibition to arrest calcific aortic stenosis
EP4225281A1 (en) * 2020-10-05 2023-08-16 Merck Patent GmbH Lmp7-selective inhibitors for the treatment of blood disorders and solid tumors

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994015956A1 (en) 1993-01-04 1994-07-21 The Wellcome Foundation Limited Endothelin converting enzyme inhibitors
WO2003033506A1 (en) 2001-10-12 2003-04-24 Kyorin Pharmaceutical Co., Ltd. Aminoborane acid derivative and proteasome inhibitory drug containing the same
US20040156854A1 (en) 2002-12-06 2004-08-12 Millennium Pharmaceuticals, Inc. Methods for the identification, assessment, and treatment of patients with proteasome inhibition therapy
JP2006089498A (ja) 1998-07-10 2006-04-06 Osteoscreen Inc 骨成長および毛成長を刺激するためのプロテアソーム活性のインヒビター

Family Cites Families (86)

* 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
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
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
AU661270B2 (en) 1990-03-05 1995-07-20 Cephalon, Inc. Chymotrypsin-like proteases and their inhibitors
US5340736A (en) 1991-05-13 1994-08-23 The President & Fellows Of Harvard College ATP-dependent protease and use of inhibitors for same in the treatment of cachexia and muscle wasting
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
AU4499697A (en) 1996-09-13 1998-04-02 New York University Method for treating parasitic diseases with proteasome inhibitors
KR100509388B1 (ko) 1996-10-18 2005-08-23 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 간염 c 바이러스 ns3 프로테아제의 저해제
SI0932617T1 (en) 1996-10-18 2002-06-30 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
US6046177A (en) 1997-05-05 2000-04-04 Cydex, Inc. Sulfoalkyl ether cyclodextrin based controlled release solid pharmaceutical formulations
US5874418A (en) 1997-05-05 1999-02-23 Cydex, Inc. Sulfoalkyl ether cyclodextrin based solid pharmaceutical formulations and their use
US6133248A (en) 1997-06-13 2000-10-17 Cydex, Inc. Polar drug of prodrug compositions with extended shelf-life storage and a method of making thereof
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
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
CA2385958A1 (en) 1999-10-20 2001-04-26 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone and hair growth
ES2272558T3 (es) 2000-10-12 2007-05-01 Viromics Gmbh Inhibidores del proteasoma para el tratamiento de infecciones causadas por virus de la hepatitis.
ES2571219T3 (es) 2001-01-25 2024-09-23 The United States Of America Represented By The Sec Dep Of Health And Human Services Formulación de compuestos de ácido borónico
BR0209883A (pt) 2001-05-21 2004-06-08 Alcon Inc Uso de inibidores da proteasoma para o tratamento de distúrbios do olho seco
AU2003219652A1 (en) 2002-01-08 2003-07-30 Eisai Co. Ltd. Eponemycin and epoxomicin analogs and uses thereof
US20040116329A1 (en) 2002-01-29 2004-06-17 Epstein Stephen E. Inhibition of proteasomes to prevent restenosis
CA2481306A1 (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
WO2003101481A1 (en) 2002-06-03 2003-12-11 Als Therapy Development Foundation Treatment of neurodegenerative diseases using proteasome modulators
US20030224469A1 (en) 2002-06-03 2003-12-04 Buchholz Tonia J. Methods and kits for assays utilizing fluorescence polarization
WO2004010937A2 (en) 2002-07-26 2004-02-05 Advanced Research & Technology Institute At Indiana University Method 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
PE20130200A1 (es) 2003-04-08 2013-03-09 Novartis Ag Composicion farmaceutica que contiene un agonista del receptor s1p y un alcohol de azucar
ATE506456T1 (de) 2003-06-10 2011-05-15 David Gladstone Inst Verfahren zur behandlung von lentivirusinfektionen
US7012063B2 (en) 2003-06-13 2006-03-14 Children's Medical Center Corporation Reducing axon degeneration with proteasome inhibitors
AU2004311478A1 (en) 2003-12-31 2005-07-21 Cydex Pharmaceuticals, Inc. Inhalant formulation containing sulfoalkyl ether cyclodextrin and corticosteroid
GB0400804D0 (en) 2004-01-14 2004-02-18 Innoscience Technology Bv Pharmaceutical compositions
US8198270B2 (en) 2004-04-15 2012-06-12 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
US8129346B2 (en) 2004-04-15 2012-03-06 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
US7232818B2 (en) 2004-04-15 2007-06-19 Proteolix, Inc. Compounds for enzyme inhibition
EP2030981B1 (en) * 2004-05-10 2014-07-09 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
AU2005243140A1 (en) 2004-05-10 2005-11-24 Proteolix, Inc. Synthesis of amino acid keto-epoxides
US20060088471A1 (en) 2004-10-20 2006-04-27 Proteolix, Inc. Compounds for enzyme inhibition
PT2260835E (pt) 2004-12-07 2013-05-28 Onyx Therapeutics Inc Composição para inibição do proteassoma
US7468383B2 (en) 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
EP1863513A2 (en) 2005-03-11 2007-12-12 The University of North Carolina at Chapel Hill Potent and specific immunoproteasome inhibitors
WO2006113470A2 (en) 2005-04-15 2006-10-26 Geron Corporation Cancer treatment by combined inhibition of proteasome and telomerase activities
GT200600350A (es) 2005-08-09 2007-03-28 Formulaciones líquidas
MY171061A (en) * 2005-11-09 2019-09-24 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
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
CA2657213C (en) 2006-06-19 2017-01-03 Proteolix, Inc. Peptide epoxyketones for proteasome 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
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
PL2178888T3 (pl) 2007-08-06 2012-11-30 Millennium Pharm Inc Inhibitory proteasomów
KR20170125413A (ko) 2007-10-04 2017-11-14 오닉스 세라퓨틱스, 인크. 결정형 펩티드 에폭시 케톤 프로테아제 저해제 및 아미노산 케토-에폭시드의 합성
US7838673B2 (en) 2007-10-16 2010-11-23 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
WO2009051581A1 (en) 2007-10-16 2009-04-23 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
US20090131367A1 (en) 2007-11-19 2009-05-21 The Regents Of The University Of Colorado Combinations of HDAC Inhibitors and Proteasome Inhibitors
EP2730579A1 (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.
EP3090737A1 (en) 2008-10-21 2016-11-09 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
CN101928329B (zh) 2009-06-19 2013-07-17 北京大学 三肽硼酸(酯)类化合物、其制备方法和应用
US8853147B2 (en) 2009-11-13 2014-10-07 Onyx Therapeutics, Inc. Use of peptide epoxyketones for metastasis suppression
EP2542238B1 (en) 2010-03-01 2015-08-12 Onyx Therapeutics, Inc. Compounds for immunoproteasome inhibition
MX2012011298A (es) 2010-03-31 2012-11-06 Millennium Pharm Inc Derivados del acido 1-amino-2-ciclopropiletilboronico.
NZ602872A (en) 2010-04-07 2014-05-30 Onyx Therapeutics Inc Crystalline peptide epoxyketone immunoproteasome inhibitor

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994015956A1 (en) 1993-01-04 1994-07-21 The Wellcome Foundation Limited Endothelin converting enzyme inhibitors
JP2006089498A (ja) 1998-07-10 2006-04-06 Osteoscreen Inc 骨成長および毛成長を刺激するためのプロテアソーム活性のインヒビター
WO2003033506A1 (en) 2001-10-12 2003-04-24 Kyorin Pharmaceutical Co., Ltd. Aminoborane acid derivative and proteasome inhibitory drug containing the same
US20040156854A1 (en) 2002-12-06 2004-08-12 Millennium Pharmaceuticals, Inc. Methods for the identification, assessment, and treatment of patients with proteasome inhibition therapy

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NZ597545A (en) 2013-07-26
US20120088762A1 (en) 2012-04-12
MY147832A (en) 2013-01-31
CO6241190A2 (es) 2011-01-20
NZ603303A (en) 2014-05-30
US8080576B2 (en) 2011-12-20
SI2041158T1 (sl) 2013-09-30
UA101303C2 (uk) 2013-03-25
US9657058B2 (en) 2017-05-23
NZ573759A (en) 2012-03-30
IL196064A (en) 2015-10-29
PT2041158E (pt) 2013-07-17
IL196064A0 (en) 2009-09-01
AU2007261345B2 (en) 2012-02-23
AU2007261345A1 (en) 2007-12-27
CA2657213A1 (en) 2007-12-27
US20130338057A1 (en) 2013-12-19
EP2484688B1 (en) 2016-06-08
EP2041158B1 (en) 2013-04-17
RU2009101319A (ru) 2010-07-27
JP5226679B2 (ja) 2013-07-03
EP2484688A1 (en) 2012-08-08
IL218033A0 (en) 2012-03-29
WO2007149512A3 (en) 2008-02-21
CN101506224B (zh) 2016-03-30
DK2041158T3 (da) 2013-06-24
CN101506224A (zh) 2009-08-12
NZ613252A (en) 2015-01-30
US8765745B2 (en) 2014-07-01
BRPI0713309A2 (pt) 2012-04-17
US20130035297A1 (en) 2013-02-07
US20150353601A1 (en) 2015-12-10
US20130041008A1 (en) 2013-02-14
US8609654B1 (en) 2013-12-17
MX2008016512A (es) 2009-02-26
US8357683B2 (en) 2013-01-22
JP2009541327A (ja) 2009-11-26
US20140100169A1 (en) 2014-04-10
ES2415632T3 (es) 2013-07-26

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