摘要:
Novel bis(aminomethyl)phosphinic acid derivatives and process for the preparation of bis(aminomethyl)phosphinic acid derivativesCompounds of the formula VI ##STR1## can be prepared by reaction of a compound of the formula IV ##STR2## with a base to give a compound of the formula Va or Vb ##STR3## and subsequent reaction with carbon nucleophiles; alternatively the compound of the formula VI is prepared by direct reaction of the compound of the formula IV e.g. with R.sup.2 Cu(CN)Li.sub.2, the above substituents having the meanings mentioned.
摘要:
The present invention relates to a compound of the formula ##STR1## in which A, Q, R.sup.2, R.sup.3 and R.sup.4, and also the corresponding, asterisked radicals, are defined as indicated in the description, to a process for their preparation, and also to their use for inhibiting retroviral proteases.
摘要:
A process for the preparation of .alpha.- or .alpha.,.alpha.'-substituted derivatives of the bis(aminomethyl)phosphinic acid of the formula I and their acid or basic salts, ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are defined as in the description, wherein a bis(aminomethyl)phosphinate is converted into the corresponding bisimine, which is alkylated by R.sup.2 and R.sup.3 in the .alpha.- and/or .alpha.,.alpha.'-position after reaction with a base, and is converted into a compound of the formula I by subsequent treatment with an acid.
摘要:
The invention concerns prodrugs of enzyme inhibitors in which at least one OH-- group in the enzyme inhibitor has been converted into a derivative grouping of the formula III, IV or V: ##STR1## in which the groups R.sup.11 to R.sup.25 and s,l, m, o, q, and r are as defined in the description. Such prodrugs exhibit an improved solubility in water and improved pharmaco-kinetic characteristics.
摘要:
Compounds of the formula I, ##STR1## in which the symbols or substituents A, B, D, D*, E and E* have the meanings given in the specification, inhibit aspartyl proteases and are suitable for controlling viral diseases.
摘要:
The present invention relates to compounds of the formula I ##STR1## in which A, Q, R.sup.2, R.sup.3, R.sup.4 and the corresponding radicals with an * are defined as indicated in the description, a process for the preparation thereof, and the use thereof for inhibiting retroviral proteases.
摘要:
The present invention relates to compounds of the formula I ##STR1## wherein A, Y, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, l, m and the corresponding radicals labeled with * are defined as stated in the description, a process for their preparation and their use for the inhibition of retroviral proteases.