Insulin analogues containing penta-fluoro-Phenylalanine at position B24
US9200053B2 · kind B2 · utility
Assignee
Inventor
Key dates
| Filing date | Oct 4, 2013 |
| Grant date | Dec 1, 2015 |
| Priority date | — |
| Expiry date | Oct 5, 2033 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K38/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
An insulin analog comprises a B-chain polypeptide incorporating a halogenated phenylalanine at position B24, B25 or B26. The halogenated phenylalanine may be ortho-monofluoro-phenylalanine, ortho-monobromo-phenylalanine, ortho-monochloro-phenylalanine, or para-monochloro-phenylalanine or penta-fluoro-Phenylalanine at position B24 alone or in combination with an acidic substitution (Aspartic Acid or Glutamic Acid) at position B10. The analog may be of a mammalian insulin, such as human insulin. A nucleic acid encodes such an insulin analog. The halogenated insulin analogs retain significant activity. A method of treating a patient comprises administering a physiologically effective amount of the insulin analog or a physiologically acceptable salt thereof to a patient. Halogen substitution-based stabilization of insulin may enhance the treatment of diabetes mellitus in regions of the developing world lacking refrigeration.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.