Lysosomotropic fluorinated amine therapeutic agents and compositions containing them
申请人:Merck & Co., Inc.
公开号:EP0009944A2
公开(公告)日:1980-04-16
Compositions useful in the control of fertility, the inhibition of malignant cell growth, and the control of other diseases which accumulate macrophages at the disease site, comprising a pharmaceutical carrier and lysosomotropic substance comprising a weakly basic amine of pK 4.5 to 9 containing at least one hydrophobic substituent or a peptide conjugate hydrolyzable by lysosomal enzymes to a biologically active substance.
Certain of the amines, viz. those of formula :
in which R is an alkyl substituent of from 8-30 carbon atoms, R is hydrogen or alkyl, and R2 is fluoroloweralkyl of 2-3 carbons, are novel and constitute another embodiment of the present invention.
The compositions of the present invention are used to inhibit or alter the function of lysosome-bearing cells.