New compounds which are active against the tissue forms of malaria and method of preparation
US5110935A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Sep 22, 1989 |
| Grant date | May 5, 1992 |
| Priority date | — |
| Expiry date | Sep 22, 2009 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02A50/30
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The invention relates to new quinoline derivatives containing a free amine group and having antimalarial properties, in particular new primaquine derivatives or their addition salts with acids, and to a method for preparing them. According to the invention, these new derivatives are represented schematically by the formula: EQU PQ-X in which PQ denotes quinolines containing a free amine group and having antimalarial properties, in particular primaquine; X denotes an amino acid or a peptide of 2 to 4 amino acids; and the PQ-X bond being a covalent peptide bond between the free amine group of PQ and the carboxyl group of X, the PQ-X covalent bond being stable in serum and resistant to lysosomal hydrolases. In an embodiment of the invention, the amino acid or the first amino acid of a peptide linked to PQ is gamma-L-glutamic acid or beta-aspartic acid linked to PQ via their beta- or gamma-carboxyl group, or L-pyroglutamic acid or aspartic acid linked to PQ via their alpha-carboxyl group.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.