CN102174076A - 用于抑制蛋白酶体酶的化合物 - Google Patents
用于抑制蛋白酶体酶的化合物 Download PDFInfo
- Publication number
- CN102174076A CN102174076A CN201110037869XA CN201110037869A CN102174076A CN 102174076 A CN102174076 A CN 102174076A CN 201110037869X A CN201110037869X A CN 201110037869XA CN 201110037869 A CN201110037869 A CN 201110037869A CN 102174076 A CN102174076 A CN 102174076A
- Authority
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- China
- Prior art keywords
- alkyl
- described compound
- zaz
- hydrogen
- aralkyl
- 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.)
- Pending
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- 0 CC(C)CC(C(C1(C)OC1)=O)NC(C(CC1=CC=CCC1)NC([C@](CC(C)C)NC(C(CCC1=CCCC=C1)NC(CN1CCCCC1)=O)=*)=O)=O Chemical compound CC(C)CC(C(C1(C)OC1)=O)NC(C(CC1=CC=CCC1)NC([C@](CC(C)C)NC(C(CCC1=CCCC=C1)NC(CN1CCCCC1)=O)=*)=O)=O 0.000 description 8
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
- C07K5/1002—Tetrapeptides with the first amino acid being neutral
- C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- 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
- C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0827—Tripeptides 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)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Neurology (AREA)
- Oncology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Immunology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (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)
Applications Claiming Priority (14)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US56234004P | 2004-04-15 | 2004-04-15 | |
| US60/562340 | 2004-04-15 | ||
| US56909604P | 2004-05-07 | 2004-05-07 | |
| US60/569096 | 2004-05-07 | ||
| US59940104P | 2004-08-06 | 2004-08-06 | |
| US60/599401 | 2004-08-06 | ||
| US61000104P | 2004-09-14 | 2004-09-14 | |
| US61015904P | 2004-09-14 | 2004-09-14 | |
| US61000204P | 2004-09-14 | 2004-09-14 | |
| US60/610159 | 2004-09-14 | ||
| US60/610002 | 2004-09-14 | ||
| US60/610001 | 2004-09-14 | ||
| US62057304P | 2004-10-20 | 2004-10-20 | |
| US60/620573 | 2004-10-20 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200580019845.4A Division CN101006098B (zh) | 2004-04-15 | 2005-04-14 | 用于抑制蛋白酶体酶的化合物 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102174076A true CN102174076A (zh) | 2011-09-07 |
Family
ID=34965899
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310512372.8A Pending CN103554222A (zh) | 2004-04-15 | 2005-04-14 | 用于抑制蛋白酶体酶的化合物 |
| CN201110037869XA Pending CN102174076A (zh) | 2004-04-15 | 2005-04-14 | 用于抑制蛋白酶体酶的化合物 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310512372.8A Pending CN103554222A (zh) | 2004-04-15 | 2005-04-14 | 用于抑制蛋白酶体酶的化合物 |
Country Status (17)
| Country | Link |
|---|---|
| US (9) | US8129346B2 (https=) |
| EP (1) | EP1745064B1 (https=) |
| JP (3) | JP5616569B2 (https=) |
| CN (2) | CN103554222A (https=) |
| AT (1) | ATE494298T1 (https=) |
| AU (1) | AU2005238445B2 (https=) |
| BE (1) | BE2016C014I2 (https=) |
| BR (1) | BRPI0509879A (https=) |
| CA (1) | CA2562411A1 (https=) |
| CY (1) | CY1117244T1 (https=) |
| DE (1) | DE602005025750D1 (https=) |
| DK (1) | DK1745064T3 (https=) |
| IL (3) | IL178400A (https=) |
| PL (1) | PL1745064T3 (https=) |
| PT (1) | PT1745064E (https=) |
| SG (2) | SG152239A1 (https=) |
| WO (1) | WO2005105827A2 (https=) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104710507A (zh) * | 2013-12-11 | 2015-06-17 | 深圳翰宇药业股份有限公司 | 一种卡非佐米的制备方法 |
| CN106946981A (zh) * | 2017-03-08 | 2017-07-14 | 南京师范大学 | 一种四肽环氧丙烷衍生物及其制备方法和用途 |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| AU2012203602B2 (en) * | 2004-04-15 | 2015-08-27 | 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 |
| PT2260835E (pt) | 2004-12-07 | 2013-05-28 | Onyx Therapeutics Inc | Composição para inibição do proteassoma |
| 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 |
| PT2408802T (pt) * | 2009-03-16 | 2017-08-03 | Governing Council Univ Toronto | Moléculas de aminoácido ciclicas e métodos para as preparar |
| 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 |
| 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 |
| SG11201407337QA (en) * | 2012-05-08 | 2014-12-30 | Onyx Therapeutics Inc | Cyclodextrin 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 |
| US10076384B2 (en) | 2013-03-08 | 2018-09-18 | Symple Surgical, Inc. | Balloon catheter apparatus with microwave emitter |
| SG10201913777XA (en) | 2013-03-13 | 2020-03-30 | Sanofi Sa | Compositions comprising anti-cd38 antibodies and carfilzomib |
| MX372671B (es) | 2013-07-19 | 2020-04-23 | Onyx Therapeutics Inc | Inhibidores de proteasoma de epoxicetona peptídica en combinacion con inhibidores de cinasa pim para el tratamiento de canceres. |
| 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 |
| CN105518019A (zh) * | 2013-09-06 | 2016-04-20 | 桑多斯股份公司 | 肽环氧基酮的合成 |
| CN105517998A (zh) * | 2013-09-06 | 2016-04-20 | 桑多斯股份公司 | 通过曼尼希反应立体选择性合成二醇和三醇以及它们在卡非佐米合成中的用途 |
| 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 |
| CN107548400A (zh) | 2014-12-02 | 2018-01-05 | 费森尤斯卡比肿瘤学有限公司 | 卡非佐米的纯化方法 |
| 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 |
| US10544189B2 (en) * | 2015-04-22 | 2020-01-28 | 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-morpholinoacetamido)-4-phenylbutanamido)-4-methylpentanamide |
| WO2016170489A1 (en) | 2015-04-24 | 2016-10-27 | Fresenius Kabi Oncology Ltd. | Pharmaceutical compositions of proteasome inhibitor |
| WO2016185450A1 (en) | 2015-05-21 | 2016-11-24 | Laurus Labs Private Limited | An improved 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 |
| WO2018024645A1 (en) | 2016-08-02 | 2018-02-08 | Synthon B.V. | Process for making carfilzomib |
| ES2874683T3 (es) | 2016-09-14 | 2021-11-05 | Fresenius Kabi Oncology Ltd | Un proceso para la purificación de un intermedio de carfilzomib |
| ES2884107T3 (es) | 2016-11-11 | 2021-12-10 | Zealand Pharma As | Multímeros de péptidos cíclicos con diana en la integrina alfa-4 beta-7 |
| 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 |
| US11286281B2 (en) | 2017-05-10 | 2022-03-29 | Zealand Pharma A/S | Homodetic cyclic peptides targeting alpha-4-beta-7 integrin |
| JP2020533382A (ja) | 2017-09-14 | 2020-11-19 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited | 癌の組合せ治療 |
| 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 |
| US20250295771A1 (en) | 2022-05-11 | 2025-09-25 | Celgene Corporation | Methods and uses related to t cell therapy and production of same |
| WO2024097905A1 (en) | 2022-11-02 | 2024-05-10 | Celgene Corporation | Methods of treatment with t cell therapy and immunomodulatory agent maintenance therapy |
| EP4685151A1 (en) | 2024-07-24 | 2026-01-28 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Proteasome inhibitor |
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2005
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- 2005-04-14 PT PT05735686T patent/PT1745064E/pt unknown
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- 2005-04-14 CN CN201310512372.8A patent/CN103554222A/zh active Pending
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- 2012-03-02 US US13/411,044 patent/US20120277146A1/en not_active Abandoned
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104710507A (zh) * | 2013-12-11 | 2015-06-17 | 深圳翰宇药业股份有限公司 | 一种卡非佐米的制备方法 |
| 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 |
| CN106946981A (zh) * | 2017-03-08 | 2017-07-14 | 南京师范大学 | 一种四肽环氧丙烷衍生物及其制备方法和用途 |
| 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 |
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