Novel rhodamine derivatives for photodynamic therapy of cancer and in vitro purging of the leukemias
US5556992A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Sep 2, 1994 |
| Grant date | Sep 17, 1996 |
| Priority date | — |
| Expiry date | Sep 2, 2014 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K41/0057
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The present invention relates to novel photoactivable rhodamine derivatives for enhancing high quantum-yield production and singlet oxygen generation upon irradiation with light while maintaining desirable differential retention of rhodamine between normal and cancer cells, said derivatives are selected from the group consisting of 4,5-dibromorhodamine 123 (2-(4,5-dibromo-6-amino-3-imino-3H-xanthen-9-yl)-benzoic acid methyl ester hydrochloride); 4, 5-dibromorhodamine 123 (2-(4,5-dibromo-6-amino-3-imino-3H-xanthen-9-yl)-benzoic acid ethyl ester hydrochloride); 4, 5-dibromorhodamine 123 (2-(4,5-dibromo-6-amino-3-imino-3H-xanthen-9-yl)-benzoic acid octhyl ester hydrochloride); 4,5-dibromorhodamine 110 n-butyl ester (2-(4,5-dibromo-6-amino-3-imino-3H-xanthen-9-yl)-benzoic acid n-butyl ester hydrochloride); Rhodamine B n-butyl ester (2-(6-ethyl amino-3-ethyl imino-3H-xanthen-9-yl)-benzoic acid n-butyl ester hydrochloride); and photoactivable derivatives thereof; whereby photoactivation of the derivatives induces cell killing while unactivated derivatives are substantially non-toxic to cells. Also, the present invention relates to the use of the photoactivable derivatives of the present …
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.