Compounds of formula:
 in which M is a peptide substituent comprising z-gly-phe, gly-phe, z-arg-arg, or benzoyl-arg, and A or N=A is an active lysosome-inhibiting substance comprising a known therapeutic drug residue or an amino radical of the formula:
 in which R is an alkyl or substituted alkyl substituent of from 8 to 18 carbons and R 2 is fluoroalkyl or hydrogen, are useful in the control of fertility, in the inhibition of malignant cell growth, and in the control of other diseases which accumulate macrophages at the disease site. They can be incorporated in pharmaceutical compositions for this purpose.

Lysosomotropic detergent therapeutic agents, compositions containing them and their uses

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 R 2 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.

Lysosomotropic fluorinated amine therapeutic agents and compositions containing them

The present invention relates to a new method for preparing 4,4'-(1-methyl-1,2- ethandiyl)-bis-(2,6-piperazinedione) of formula (I) or its enantiomers. More specifically this invention relates to a new process for preparing 4,4'-(1-methyl- 1,2- ethandiyl)-bis-(2,6-piperazinedione), which gives better yield and purity and involves new intermediate.

A process for preparation of 4,4'-(1-methyl-1,2-ethandiyl)-bis-(2,6-piperazinedione)

1. A COMPOUND OF THE STRUCTURE 1-((R3)1-),2,5-DI(O=),3,6-BIS(1-AZABICYCLO(3,1,0)- HEX-2-YL-),3-R4,4-R3,6-((R4)1-)-PIPERAZINE WHEREIN R3 AND R31 ARE EACH HYDROGEN, LOWER ALKYL OF 1 TO 6 CARBON ATOMS, LOWER ALKANOYL OF 2 TO 4 CARBON ATOMS, DILOWER ALKYLAMINOMETHYL WHEREIN THE LOWER ALKYLS CONTAIN 2 TO 5 CARBON ATOMS; R4 AND R41 ARE EACH HYDROGEN OR MERCAPTO.

Shen Tsung-Ying

Papers

Derivatives of 3,6-bis-(2-(1-azabicyclo-(3,1,0)hexane))-2,5-piperazinedione