Polyalkylene glycol derivatives of inhibitors of epidermal growth factor receptor tyrosine kinase
US8461166B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Mar 7, 2007 |
| Grant date | Jun 11, 2013 |
| Priority date | — |
| Expiry date | Dec 13, 2031 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07B2200/05
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Novel epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitors, pharmaceutical compositions including same and their use in the treatment of EGFR-TK related diseases or disorders are disclosed. Novel radiolabeled EGFR-TK inhibitors as their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as radiopharmaceuticals for radiotherapy are further disclosed. The disclosed EGFR-TK inhibitors comprise a polyalkylene glycol moiety and/or a hydroxy-containing moiety and are characterized by improved solubility, biostability and bioavailability. Processes of preparing the disclosed EGFR-TK inhibitors and of radiolabeling same, via, for example, one-step radiosyntheses, are also disclosed.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.