Ribosome-Mediated Incorporation of Peptides and Peptidomimetics
US-2025197869-A1 · Jun 19, 2025 · US
Integrin antagonist conjugates for targeted delivery to cells expressing alpha-V-beta-3
US9586916B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9586916-B2 |
| Application number | US-201314374680-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jan 22, 2013 |
| Priority date | Jan 27, 2012 |
| Publication date | Mar 7, 2017 |
| Grant date | Mar 7, 2017 |
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- Title
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- Abstract
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Abstract
Official abstract text for this publication.
The invention relates to compounds of formula (I): wherein R 1 , R 2 , and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula (I) for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to alpha-V-beta-3 integrin antagonists to target cells expressing alpha-V-beta-3.
First claim
Opening claim text (preview).
The invention claimed is: 1. A compound of formula I: or a pharmaceutically acceptable salt or ester thereof; wherein n is 1-24 and wherein: R 1 is selected from the group consisting of: (1) a moiety of the formula: wherein m is 0 or 1; (2) a moiety of the formula: wherein X is N or CH; (3) a moiety of the formula: (4) a moiety of the formula: and (5) a moiety of the formula: R 2 is selected from the group consisting of: (1) a moiety of the formula: (2) a moiety of the formula: (3) a moiety of the formula: and (4) a moiety of the formula: wherein R 3 is a conjugated moiety and X represents either sulfur or a moiety of the formula: 2. A compound according to claim 1 , wherein R 1 is a moiety of the formula: wherein m is 0 or 1. 3. A compound according to claim 1 , wherein R 1 is a moiety of the formula: wherein X is N or CH. 4. A compound according to claim 1 , wherein R 1 is a moiety of the formula: 5. A compound according to claim 1 , wherein R 1 is a moiety of the formula: 6. A compound according to claim 1 , wherein R 1 is moiety of the formula: 7. A compound according to claim 1 , wherein R 2 is a moiety of the formula: wherein R 2 is a moiety of the formula: wherein R 2 is a moiety of the formula: or wherein R 2 is a moiety of the formula: wherein R 3 is a single or double stranded oligonucleotide and X represents either sulfur or a moiety of the formula: 8. A compound according to claim 2 , wherein R 2 is a moiety of the formula: wherein R 2 is a moiety of the formula: wherein R 2 is a moiety of the formula: or wherein R 2 is a moiety of the formula: wherein R 3 is a single or double stranded oligonucleotide and X represents either sulfur or a moiety of the formula: 9. A compound according to claim 3 , wherein R 2 is a moiety of the formula: wherein R 2 is a moiety of the formula: wherein R 2 is a moiety of the formula: or wherein R 2 is a moiety of the formula: wherein R 3 is a single or double stranded oligonucleotide and X represents either sulfur or a moiety of the formula: 10. A compound according to claim 4 , wherein R 2 is a moiety of the formula: wherein R 2 is a moiety of the formula: wherein R 2 is a moiety of the formula: or wherein R 2 is a moiety of the formula: wherein R 3 is a single or double stranded oligonucleotide and X represents either sulfur or a moiety of the formula: 11. A compound according to claim 5 , wherein R 2 is a moiety of the formula: wherein R 2 is a moiety of the formula: wherein R 2 is a moiety of the formula: or wherein R 2 is a moiety of the formula: wherein R 3 is a single or double stranded oligonucleotide and X represents either sulfur or a moiety of the formula: 12. A compound according to claim 6 , wherein R 2 is a moiety of the formula: wherein R 2 is a moiety of the formula: wherein R 2 is a moiety of the formula:
Assignees
Inventors
Classifications
Antineoplastic agents · CPC title
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to said nitrogen atoms · CPC title
Heterocyclic compounds (A61K47/558 takes precedence) · CPC title
- C07D277/593Primary
Z being doubly bound oxygen or doubly bound nitrogen, which nitrogen is part of a possibly substituted oximino radical · CPC title
linked by a chain containing hetero atoms as chain links · CPC title
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Frequently asked questions
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- What does patent US9586916B2 cover?
- The invention relates to compounds of formula (I): wherein R 1 , R 2 , and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula (I) for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to alpha-V-beta-3 integrin…
- Who is the assignee on this patent?
- Hoffmann La Roche
- What technology area does this patent fall under?
- Primary CPC classification C07D277/593. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Mar 07 2017 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).