JO3326B1 - مثبطات إيبوكسي كيتون بروتياز ثلاثي الببتيد - Google Patents

مثبطات إيبوكسي كيتون بروتياز ثلاثي الببتيد

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Publication number
JO3326B1
JO3326B1 JOP/2014/0111A JOP20140111A JO3326B1 JO 3326 B1 JO3326 B1 JO 3326B1 JO P20140111 A JOP20140111 A JO P20140111A JO 3326 B1 JO3326 B1 JO 3326B1
Authority
JO
Jordan
Prior art keywords
protease inhibitors
epoxy ketone
ketone protease
tripeptide epoxy
compositions
Prior art date
Application number
JOP/2014/0111A
Other languages
English (en)
Inventor
Mcminn Dustin
C Moebius David
Bowers Simeon
Johnson Henry
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
Application granted granted Critical
Publication of JO3326B1 publication Critical patent/JO3326B1/ar

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    • 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
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
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    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
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Abstract

يتعلق الاختراع الحالي بمثبطات إيبوكسي كيتون بروتياز ثلاثي الببتيد، وطرق لتحضيرها، والتركيبات الصيدلية ذات الصلة، وطرق استخدامها. على سبيل المثال، يتوفر هنا مركبات وفقًا للصيغة (X): وأملاح وتركيبات مقبولة صيدليًا تتضمنها. يمكن استخدام المركبات والتركيبات المتوفرة هنا، على سبيل المثال، في علاج الأمراض وتتضمن أمراض الالتهاب وضمور الأعصاب.
JOP/2014/0111A 2013-03-14 2014-03-16 مثبطات إيبوكسي كيتون بروتياز ثلاثي الببتيد JO3326B1 (ar)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201361785608P 2013-03-14 2013-03-14
US201361786086P 2013-03-14 2013-03-14
US201361847780P 2013-07-18 2013-07-18
US201361856847P 2013-07-22 2013-07-22
US201361883798P 2013-09-27 2013-09-27
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Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2726367C2 (ru) * 2016-03-28 2020-07-13 Пресидж Байосайенсиз, Инк. Фармацевтические комбинации для лечения злокачественной опухоли
AR108919A1 (es) * 2016-06-29 2018-10-10 Kezar Life Sciences Proceso de preparación del inhibidor de inmunoproteasoma de péptido epoxicetona, y sus precursores
CA3029032C (en) 2016-06-29 2024-10-29 Kezar Life Sciences CRYSTAL SALTS OF AN IMMUNOPROTEASOME PEPTIDE INHIBITOR EPOXYCETONE
EP3318276A1 (en) * 2016-11-04 2018-05-09 Janssen Biotech, Inc. Combinations of a telomerase inhibitor and a bcl-2 inhibitor for the treatment of hematological cancers
US11357817B2 (en) 2017-05-15 2022-06-14 The Regents Of The University Of California Immunoproteasome inhibitor
CN107652219B (zh) 2017-08-14 2021-06-08 上海新理念生物医药科技有限公司 四马来酰亚胺型连接子及其应用
CN117338932A (zh) * 2017-08-23 2024-01-05 科智生命科学公司 自身免疫性病症的治疗中的免疫蛋白酶体抑制剂和免疫抑制剂
WO2019060651A1 (en) 2017-09-21 2019-03-28 Kezar Life Sciences POLY THERAPY FOR IMMUNOLOGICAL DISEASES
JP2021503441A (ja) * 2017-11-16 2021-02-12 アムジエン・インコーポレーテツド Ｐｅｇ化されたカルフィルゾミブ化合物の安定組成物
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
US20200360386A1 (en) * 2017-12-30 2020-11-19 Unity Biotechnology, Inc. Inhibitors of HSP90, PI3-Kinase, Proteasome, HDAC, and P97 Pathways for Selective Removal of Senescent Cells in the Treatment of Age Related Conditions
CA3043103C (en) * 2017-12-30 2021-02-09 Unity Biotechnology Peptide-based proteasome inhibitors for treating conditions mediated by senescent cells and for 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
CN118255835A (zh) * 2022-12-27 2024-06-28 上海美悦生物科技发展有限公司 三肽环氧酮化合物、药物组合物及其制备方法和用途
TW202521102A (zh) * 2023-09-26 2025-06-01 大陸商上海齊魯製藥研究中心有限公司 免疫蛋白酶體選擇性抑制劑
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 (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
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
US5858784A (en) 1991-12-17 1999-01-12 The Regents Of The University Of California Expression of cloned genes in the lung by aerosol- and liposome-based delivery
AU4499697A (en) 1996-09-13 1998-04-02 New York University Method for treating parasitic diseases with proteasome inhibitors
US6042820A (en) 1996-12-20 2000-03-28 Connaught Laboratories Limited Biodegradable copolymer containing α-hydroxy acid and α-amino acid units
US6472375B1 (en) 1998-04-16 2002-10-29 John Wayne Cancer Institute DNA vaccine and methods for its use
CN1498224A (zh) 2000-07-21 2004-05-19 ���鹫˾ 用作丙型肝炎病毒ns3-丝氨酸蛋白酶抑制剂的新型肽
US7232818B2 (en) 2004-04-15 2007-06-19 Proteolix, Inc. Compounds for enzyme inhibition
US8088741B2 (en) * 2004-05-10 2012-01-03 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
HUE027850T2 (en) 2004-12-07 2016-11-28 Onyx Therapeutics Inc Preparation for proteasome inhibition
US7589066B2 (en) * 2005-03-11 2009-09-15 The University Of North Carolina At Chapel Hill Potent and specific immunoproteasome inhibitors
RU2453556C2 (ru) * 2005-11-09 2012-06-20 Протеоликс, Инк. Соединения для ингибирования фермента
RU2450016C2 (ru) * 2006-06-19 2012-05-10 Протеоликс, Инк. Пептидные эпоксикетоны для ингибирования протеасомы
AU2009308516B2 (en) 2008-10-21 2016-08-25 Onyx Therapeutics, Inc. Combination therapy with peptide epoxyketones
CA2791651C (en) * 2010-03-01 2019-08-20 Onyx Therapeutics, Inc. Compounds for immunoproteasome inhibition
US8455431B2 (en) * 2011-02-18 2013-06-04 Trustees of Dartmout College Inhibitors of the trypsin-like site of the proteasome and methods of use thereof
PH12012502259A1 (en) 2012-05-08 2019-07-03 Onyx Therapeutics Inc Cylodextrin complexation methods for formulating peptide proteasome inhibitors

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