CA3026564A1 - Inhibiteurs de proteasome - Google Patents
Inhibiteurs de proteasome Download PDFInfo
- Publication number
- CA3026564A1 CA3026564A1 CA3026564A CA3026564A CA3026564A1 CA 3026564 A1 CA3026564 A1 CA 3026564A1 CA 3026564 A CA3026564 A CA 3026564A CA 3026564 A CA3026564 A CA 3026564A CA 3026564 A1 CA3026564 A1 CA 3026564A1
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- Prior art keywords
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- proteasome
- compound
- activity
- ome
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- 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.)
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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
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
- C07K5/06069—Ser-amino acid
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
La présente invention concerne un composé de formule (I), X représentant C=0, C=S ou B-OH ; Y représente un électrophile et Z représente un groupe partant, ou Y--Z représente un électrophile ; R1 comprend ou est constitué (a) (i) d'un premier groupe se liant à un site protéolytique d'un protéasome, ledit premier groupe étant lié à X ; et (ii) éventuellement d'un second groupe améliorant l'administration ; ou (b) d'un groupe se liant entre les sous-unités ß1 et ß2 d'un protéasome ; R2 et R3 étant indépendamment choisis parmi H, méthyle, méthoxy, éthyle, éthényle, éthinyle et cyano, méthyle et éthyle pouvant être substitués par OH ou halogène.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662346203P | 2016-06-06 | 2016-06-06 | |
| EP16173057 | 2016-06-06 | ||
| US62/346,203 | 2016-06-06 | ||
| EP16173057.7 | 2016-06-06 | ||
| PCT/EP2017/063699 WO2017211818A1 (fr) | 2016-06-06 | 2017-06-06 | Inhibiteurs de protéasome |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3026564A1 true CA3026564A1 (fr) | 2017-12-14 |
Family
ID=56289289
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3026564A Pending CA3026564A1 (fr) | 2016-06-06 | 2017-06-06 | Inhibiteurs de proteasome |
Country Status (2)
| Country | Link |
|---|---|
| CA (1) | CA3026564A1 (fr) |
| WO (1) | WO2017211818A1 (fr) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110357940A (zh) * | 2019-08-02 | 2019-10-22 | 苏州艾和医药科技有限公司 | 奥普佐米合成工艺研究 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3592922A (en) * | 1968-07-16 | 1971-07-13 | Chemagro Corp | Process of killing fungi and nematodes with acetylenic ketones |
| DE3343531A1 (de) * | 1983-12-01 | 1985-06-13 | Bayer Ag, 5090 Leverkusen | Substituierte acetylenketone |
| WO2004103270A2 (fr) * | 2003-04-02 | 2004-12-02 | Suntory Pharmaceutical Research Laboratories Llc | Composes et procedes destines au traitement de la thrombose |
| UA105794C2 (uk) * | 2009-06-26 | 2014-06-25 | Новартіс Аг | 1,3-ДИЗАМІЩЕНІ ПОХІДНІ ІМІДАЗОЛІДИН-2-ОНУ ЯК ІНГІБІТОРИ Cyp17 |
| US20120165541A1 (en) * | 2009-07-31 | 2012-06-28 | Sandoz Ag | Method for the preparation of w-amino- alkaneamides and w-amino-alkanethioamides as well as intermediates of this method |
-
2017
- 2017-06-06 WO PCT/EP2017/063699 patent/WO2017211818A1/fr unknown
- 2017-06-06 CA CA3026564A patent/CA3026564A1/fr active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| WO2017211818A1 (fr) | 2017-12-14 |
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