Parathyroid hormone analogues for the treatment of osteoporosis
US5955425A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Aug 2, 1996 |
| Grant date | Sep 21, 1999 |
| Priority date | — |
| Expiry date | Aug 2, 2016 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K38/29
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
This invention describes analogs of human parathyroid hormone which have increased activities in bone restoration, and increased bioavailabilities. The peptides described are derivatives of hPTH-(1-31) which have lactams formed for example, between either Glu.sup.22 and Lys.sup.26 or Lys.sup.26 and Asp.sup.30. In addition, the natural Lys.sup.27 may be substituted by either a Leu or other hydrophobic residues, such as Ile, norleucine, Met, Val, Ala, Trp, or Phe. Typically, these analogs have enhanced abilities to stimulate adenylyl cyclase in rat osteosarcoma cells, and show increased activities in bone restoration, using the ovariectomized rat model. The analogs also show enhanced activities and bioavailabilities, as demonstrated by their hypotensive effects in the rat.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.