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Lysine-glutamic acid dipeptide derivatives
US9522874B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9522874-B2 |
| Application number | US-201414539126-A |
| Country | US |
| Kind code | B2 |
| Filing date | Nov 12, 2014 |
| Priority date | May 15, 2012 |
| Publication date | Dec 20, 2016 |
| Grant date | Dec 20, 2016 |
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- Title
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- Abstract
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- Assignees and inventors
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- Key dates
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- First independent claim
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- CPC / IPC classifications
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- Citations and related patents
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Abstract
Official abstract text for this publication.
The invention relates to compounds of the formula I. The compounds of formula I are versatile peptide intermediates for the solid phase peptide synthesis (SPPS) of peptide drugs which comprise a Glu-fatty alkyl side chain building block attached to a Lys-part of the peptide chain.
First claim
Opening claim text (preview).
The invention claimed is: 1. A compound of the formula wherein, R 1 is t-butyl, R 2 is hydrogen or an ester protecting group, R 3 is hydrogen or an amino protecting group, and R 4 is C 12-20 -alkyl, and enantiomers, diastereomers and salts thereof. 2. The compound of claim 1 wherein, the ester protecting group is selected from C 1-4 -alkyl, optionally substituted with phenyl, C 2-4 -alkenyl, piperidinyl or dimethylaminoboranyl. 3. The compound of claim 1 , wherein R 2 is hydrogen or C 2-4 -alkenyl. 4. The compound of claim 1 , wherein R 2 is hydrogen or allyl. 5. The compound of claim 1 , wherein R 3 is 9H-fluoren-9-ylmethoxycarbonyl. 6. The compound of claim 1 , wherein R 4 is C 14-16 -alkyl. 7. A compound of the formula wherein, R 1 is t-butyl, R 2 is hydrogen or an ester protecting group, R 3 is hydrogen or an amino protecting group, and R 4 is C 12-20 -alkyl, and salts thereof. 8. The compound of claim 7 , wherein, R 2 is hydrogen, R 3 is 9H-fluoren-9-ylmethoxycarbonyl and R 4 is C 15 -alkyl; or R 2 is allyl, R 3 is 9H-fluoren-9-ylmethoxycarbonyl and R 4 is C 15 -alkyl. 9. The compound of claim 7 , wherein, R 2 is hydrogen, R 3 is 9H-fluoren-9-ylmethoxycarbonyl and R 4 is pentadecyl; or R 2 is allyl, R 3 is 9H-fluoren-9-ylmethoxycarbonyl and R 4 is pentadecyl. 10. The compound of claim 1 , wherein R 2 is hydrogen, R 3 is 9H-fluoren-9-ylmethoxycarbonyl and R 4 is C 15 -alkyl. 11. The compound of claim 1 , wherein R 2 is allyl, R 3 is 9H-fluoren-9-ylmethoxycarbonyl and R 4 is C 15 -alkyl. 12. The compound of claim 1 , wherein R 2 is hydrogen, R 3 is 9H-fluoren-9-ylmethoxycarbonyl and R 4 is pentadecyl. 13. The compound of claim 1 , wherein R 2 is allyl, R 3 is 9H-fluoren-9-ylmethoxycarbonyl and R 4 is pentadecyl. 14. A compound of the formula wherein, R 1 is t-butyl, R 2 is hydrogen or an ester protecting group, R 3 is hydrogen or an amino protecting group, and R 4 is C 12-20 -alkyl, and salts thereof. 15. The compound of claim 14 , wherein, R 2 is hydrogen, R 3 is 9H-fluoren-9-ylmethoxycarbonyl and R 4 is C 15 -alkyl; or R 2 is allyl, R 3 is 9H-fluoren-9-ylmethoxycarbonyl and R 4 is C 15 -alkyl. 16. The compound of claim 14 , wherein, R 2 is hydrogen, R 3 is 9H-fluoren-9-ylmethoxycarbonyl and R 4 is pentadecyl; or R 2 is allyl, R 3 is 9H-fluoren-9-ylmethoxycarbonyl and R 4 is pentadecyl. 17. The compound of claim 1 , wherein R 2 is allyl. 18. The compound of claim 7 , wherein R 2 is hydrogen or allyl. 19. The compound of claim 7 , wherein R 3 is 9H-fluoren-9-ylmethoxycarbonyl. 20. The compound of claim 7 , wherein R 4 is C 14-16 -alkyl. 21. The compound of claim 7 wherein R 2 is allyl. 22. The compound of claim 14 , wherein R 2 is hydrogen or allyl. 23. The compound of claim 14 , wherein R 3 is 9H-fluoren-9-ylmethoxycarbonyl. 24. The compound of claim 14 , wherein R 4 is C 14-16 -alkyl. 25. The compound of claim 14 , wherein R 2 is allyl.
Assignees
Inventors
Classifications
- C07C271/22Primary
to carbon atoms of hydrocarbon radicals substituted by carboxyl groups · CPC title
Fluorenes; Hydrogenated fluorenes · CPC title
with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms · CPC title
Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups · CPC title
Chemical, physical or physico-chemical processes in general; Their relevant apparatus · CPC title
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Frequently asked questions
Answers are generated from the same data shown on this page.
- What does patent US9522874B2 cover?
- The invention relates to compounds of the formula I. The compounds of formula I are versatile peptide intermediates for the solid phase peptide synthesis (SPPS) of peptide drugs which comprise a Glu-fatty alkyl side chain building block attached to a Lys-part of the peptide chain.
- Who is the assignee on this patent?
- Hoffmann La Roche
- What technology area does this patent fall under?
- Primary CPC classification C07C271/22. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Dec 20 2016 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).