Substituted phosphinate based peptide derivatives

摘要

Compounds of Formula (I) are proposed for use in the treatment of metabolic bone diseases such as osteoporosis and bone metastasis. In the formulas wherein R<1> is 1. a hydrogen atom, 2. an amino-protecting group, 3. an alkyl, alkenyl, alkynyl or aryl group, 4. a group R<1b>-NH-CR<1c>R<1d>-CO- in which 4.1. R<1b> is 4.1.1. a hydrogen atom, 4.1.2. a natural or unnatural alpha -amino acid, or a peptide consisting of the same, 4.1.3. an alkyl, alkenyl, alkynyl or aryl group, 4.2. R<1c> and R<1d> independently of each other are 4.2.1. a hydrogen atom, 4.2.2. a radical corresponding to a side chain of a natural or non-natural alpha -amino acid, 4.2.3. an alkyl, alkenyl, alkynyl or aryl group, 5. a group R<1e>-CO- in which R<1e> is 5.1. a hydrogen atom, 5.2. an alkyl, alkenyl, alkynyl or aryl group, 6. a group of R<1f>-SO2- in which R<1f> is an alkyl, alkenyl, alkynyl or aryl group. R<2>, R<3>, R<4> and R<8> independently of each other are 1. a group as defined for R<1c>, 2. a group R<2a>-CH2- in which R<2a> is 2.1. an aryl group, 2.3. a heteroalicylic or heteroaromatic group. R<5> is 1. a hydrogen atom, or 2. an alkyl, alkenyl, alkynyl or aryl group. R<6> and R<7> independently of each other are 1. a hydrogen atom, or 2. an alkyl group. R<9> is 1. a group R<3a>-X- in which 1.1. R<3a> is 1.1.3., an alkyl, alkenyl, alkynyl or aryl group, 1.1.4. a heteroalicylic or heteroaromatic group 1.1.3. a group as defined for R<2>, 1.2. X is O, S or NH. X and X are: O, S or NH.