CO6241190A2 - Compuestos para inhibicion enzimatica - Google Patents

Compuestos para inhibicion enzimatica

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Publication number
CO6241190A2
CO6241190A2 CO08135292A CO08135292A CO6241190A2 CO 6241190 A2 CO6241190 A2 CO 6241190A2 CO 08135292 A CO08135292 A CO 08135292A CO 08135292 A CO08135292 A CO 08135292A CO 6241190 A2 CO6241190 A2 CO 6241190A2
Authority
CO
Colombia
Prior art keywords
absent
alkyl
compound
independently selected
optionally
Prior art date
Application number
CO08135292A
Other languages
English (en)
Spanish (es)
Inventor
Kevin D Shenk
Francesco Parlatti
Han-Jie Zhou
Catherine Sylvain
Mark S Smyth
Mark K Bennett
Guy Laiding
Original Assignee
Proteolix 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 Proteolix Inc filed Critical Proteolix Inc
Publication of CO6241190A2 publication Critical patent/CO6241190A2/es

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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
JP5616569B2 (ja) 2004-04-15 2014-10-29 オニキス セラピューティクス， インク．Ｏｎｙｘ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． 酵素阻害のための化合物
CN102875642A (zh) 2004-05-10 2013-01-16 普罗特奥里克斯公司 用于酶抑制的化合物
AU2006311584B2 (en) 2005-11-09 2012-03-08 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
CN101506224B (zh) 2006-06-19 2016-03-30 欧尼斯治疗公司 蛋白酶体抑制用的肽环氧酮
PT2207791T (pt) 2007-10-04 2016-07-12 Onyx Therapeutics Inc Inibidores da epoxi cetona protease de péptido cristalino e a síntese de ceto-epóxidos de aminoácidos
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
WO2011060179A1 (en) * 2009-11-13 2011-05-19 Onyx Therapeutics, Inc Use of peptide epoxyketones for metastasis suppression
WO2011109355A1 (en) * 2010-03-01 2011-09-09 Onyx Therapeutics, Inc. Compounds for immunoproteasome inhibition
JP2013525282A (ja) * 2010-04-07 2013-06-20 オニキス セラピューティクス， インク． 結晶質ペプチドエポキシケトンイムノプロテアソーム阻害剤
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
WO2014003203A2 (en) 2012-06-29 2014-01-03 Nissan Chemical Industries, Ltd. Method for producing stereoselective epoxyketone compound
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
HK1211947A1 (en) * 2012-08-14 2016-06-03 Trillium Therapeutics Inc. Fluorinated epoxyketone-based compounds and uses thereof as proteasome inhibitors
EP2906582A1 (en) * 2012-10-12 2015-08-19 F. Hoffmann-La Roche AG Macrocyclic ketoamide immunoproteasome inhibitors
CN105164117B (zh) 2013-03-14 2019-02-01 欧尼斯治疗公司 二肽和三肽环氧酮蛋白酶抑制剂
AR095426A1 (es) * 2013-03-14 2015-10-14 Onyx Therapeutics Inc Inhibidores tripeptídicos de la epoxicetona proteasa
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
CA2920220A1 (en) * 2013-09-06 2015-03-12 Sandoz Ag Synthesis of peptide epoxy ketones
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
US10301273B2 (en) 2014-08-07 2019-05-28 Mayo Foundation For Medical Education And Research Compounds and methods for treating cancer
US11202817B2 (en) 2014-08-18 2021-12-21 Cornell University Dipeptidomimetics as inhibitors of human immunoproteasomes
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
US11066397B2 (en) 2015-10-15 2021-07-20 Cornell University Proteasome inhibitors and uses thereof
EP4296257A3 (en) 2016-06-29 2024-03-20 Kezar Life Sciences Process of preparing a peptide epoxyketone immunoproteasome inhibitor
PT3478670T (pt) 2016-06-29 2023-05-24 Kezar Life Sciences Sais cristalinos de inibidor peptídeo de imunoproteassoma de epoxicetona
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
EP3589659B1 (en) 2017-02-28 2025-04-09 Mayo Foundation for Medical Education and Research Combinations for use in the treatment of cancer
US11357817B2 (en) 2017-05-15 2022-06-14 The Regents Of The University Of California Immunoproteasome inhibitor
JP7289828B2 (ja) 2017-08-23 2023-06-12 ケザール ライフ サイエンシズ 自己免疫疾患の治療における免疫プロテアソーム阻害剤および免疫抑制剤
EP3694605A4 (en) 2017-10-11 2021-10-27 Cornell University PEPTIDOMIMETIC INHIBITORS OF PROTEASOME
US11243207B2 (en) 2018-03-29 2022-02-08 Mayo Foundation For Medical Education And Research Assessing and treating cancer
CN111918961B (zh) 2018-03-30 2023-10-24 国立大学法人京都大学 心肌细胞成熟促进剂
WO2021108705A2 (en) * 2019-11-25 2021-06-03 Cornell University Nuclear factor kappa b pathway inhibition to arrest calcific aortic stenosis
AU2021357717A1 (en) * 2020-10-05 2023-06-08 Merck Patent Gmbh Lmp7-selective inhibitors for the treatment of blood disorders and solid tumors

Family Cites Families (90)

* 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
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
JPH05506777A (ja) 1990-03-05 1993-10-07 セファロン、インコーポレーテッド キモトリプシン様プロテアーゼ及びそれらの阻害剤
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
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
DK0932617T3 (da) * 1996-10-18 2002-04-22 Vertex Pharma Inhibitorer af serinproteaser, især af hepatitis C-virus-NS3-protease
SI0932617T1 (en) 1996-10-18 2002-06-30 Vertex Pharmaceuticals Incorporated 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
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
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
CA2347275C (en) * 1998-10-20 2010-03-09 Millennium Pharmaceuticals, Inc. Method for monitoring proteasome inhibitor drug action
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
AU784304B2 (en) 1999-10-20 2006-03-09 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
US20040106539A1 (en) * 2000-10-12 2004-06-03 Ulrich Schubert Agents for the treatment of viral infections
EP2251344B2 (en) 2001-01-25 2024-04-24 THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES Formulation of boronic acid compounds
CA2447909C (en) 2001-05-21 2011-04-05 Alcon, Inc. Use of proteasome inhibitors to treat dry eye disorders
JPWO2003033506A1 (ja) 2001-10-12 2005-02-03 杏林製薬株式会社 アミノボラン酸誘導体およびそれを含有するプロテアソーム阻害薬
EP1463719A2 (en) * 2002-01-08 2004-10-06 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
EP1496916A2 (en) * 2002-04-09 2005-01-19 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
EP1581629B1 (en) 2002-12-06 2015-04-01 Millennium Pharmaceuticals, Inc. Methods for the identification, assessment, and treatment of patients with proteasome inhibition therapy
TW200418791A (en) 2003-01-23 2004-10-01 Bristol Myers Squibb Co Pharmaceutical compositions for inhibiting proteasome
SG175449A1 (en) 2003-04-08 2011-11-28 Novartis Ag Organic compounds
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
AU2004312096A1 (en) 2003-12-31 2005-07-21 Cydex Pharmaceuticals, Inc. Inhalant formulation containing sulfoalkyl ether gamma-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
US7232818B2 (en) 2004-04-15 2007-06-19 Proteolix, Inc. Compounds for enzyme inhibition
JP5616569B2 (ja) 2004-04-15 2014-10-29 オニキス セラピューティクス， インク．Ｏｎｙｘ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． 酵素阻害のための化合物
CN102875642A (zh) 2004-05-10 2013-01-16 普罗特奥里克斯公司 用于酶抑制的化合物
US20050256324A1 (en) * 2004-05-10 2005-11-17 Proteolix, Inc. Synthesis of amino acid keto-epoxides
CA2584515A1 (en) 2004-10-20 2006-04-27 Proteolix, Inc. Labeled compounds for proteasome inhibition
PL2260835T3 (pl) * 2004-12-07 2013-08-30 Onyx Therapeutics Inc Kompozycja do hamowania proteasomu
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
US7998938B2 (en) 2005-04-15 2011-08-16 Geron Corporation Cancer treatment by combined inhibition of proteasome and telomerase activities
GT200600350A (es) 2005-08-09 2007-03-28 Formulaciones líquidas
AU2006311584B2 (en) * 2005-11-09 2012-03-08 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
CN101506224B (zh) 2006-06-19 2016-03-30 欧尼斯治疗公司 蛋白酶体抑制用的肽环氧酮
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
AU2008209555A1 (en) 2007-01-23 2008-07-31 Gloucester Pharmaceuticals, Inc. Combination therapy comprising romidepsin and I.A. bortezomib
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
EP2527347A1 (en) 2007-08-06 2012-11-28 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
PT2207791T (pt) 2007-10-04 2016-07-12 Onyx Therapeutics Inc Inibidores da epoxi cetona protease de péptido cristalino e a síntese de ceto-epóxidos de aminoácidos
EP2212334B1 (en) 2007-10-16 2012-08-15 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
SG194349A1 (en) 2008-06-17 2013-11-29 Millennium Pharm 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
WO2011060179A1 (en) 2009-11-13 2011-05-19 Onyx Therapeutics, Inc Use of peptide epoxyketones for metastasis suppression
WO2011109355A1 (en) 2010-03-01 2011-09-09 Onyx Therapeutics, Inc. Compounds for immunoproteasome inhibition
SG184222A1 (en) 2010-03-31 2012-10-30 Millennium Pharm Inc Derivatives of 1-amino-2-cyclopropylethylboronic acid
JP2013525282A (ja) 2010-04-07 2013-06-20 オニキス セラピューティクス， インク． 結晶質ペプチドエポキシケトンイムノプロテアソーム阻害剤

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US20140100169A1 (en) 2014-04-10
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RU2012103671A (ru) 2013-08-10

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