摘要:
compound of the formula wherein R' and R 4 are independently amino or an organic residue bonded through nitrogen, R 2 is hydrogen or alkyl which may be substituted, R 3 is hydrogen or a protecting group and R5 is hydroxyl which may be substituted or amino which may be substituted or salts thereof; with the proviso that when R 1 is amino, sorbylamino or hexanoylamino, R 2 is hydrogen or methyl, R 4 is amino which may be protected adn R 5 is hydroxyl or 2-amidinoethylamino, R 3 is a protecting group, and that when R 1 is amino, leucylamino, acetylamino or benzyloxycarbonylamino, R 3 is hydrogen, methyl or 2-tettrahydropyranyl, R 4 is amino, acetylamino or benzyloxycarbonylamino and R 5 is hydroxyl which may be substituted or amino which may be substituted, R 2 is alkyl which may be substituted, has antibacterial activities against drug-resistant bacteria and therefore can be useful as a chemotherapeutic drug for bacterial infections in mammals.
摘要:
Die Erfindung betrifft Derivate cyclischer Aminosäuren der allgemeinen Formel in welcher R¹ Wasserstoff, Alkyl, Alkenyl oder (subst.) Aryl bedeutet, R² Wasserstoff, Alkyl, Hydroxy, Alkoxy, (subst.) Aryl, (subst.) Aryloxy oder (subst.) Aroyl ist, oder R¹ und R² zusammen für (subst.) Benzyliden oder R¹ und R² zusammen mit dem sie tragenden C-Atom für (subst.) Cycloalkyl stehen, R³ Wasserstoff, Hydroxymethyl, Formyl, (subst.) Alkenyl, (subst.) Carboxylatocarbonyl, (subst.) Carbamoylatocarbonyl oder (subst.) Trifluormethylcarbonyl bedeutet, A für eine cyclische Aminosäure steht, X Sauerstoff, Imino oder N-Alkylimino bedeutet, m = 0-5 ist und n = 0 oder 1 ist, Verfahren zu ihrer Herstellung, sie enthaltende Mittel sowie deren Verwendung.
摘要:
The present invention relates to novel 1-phenyl-3-(1-piperazinyl)-1H-indazoles and intermediates and a process for the preparation thereof. The compounds according to the invention exhibit analgesic, anti-convulsive and anti-depressant activities, and can therefore be used as medicaments.
摘要:
The present invention relates a process for the production of polyurethanes wherein a tertiary amine functionality is incorporated into the side chain of an aromatic diamine, preferably a diaminobenzamide, to form a non-fugitive catalytic polyurethane chain extender. These non-fugitive chain extruders are polyurethane catalysts that provide adequate cure without residual odor and safety hazards associated with the more traditional tertiary amine catalysts. When reacted with the isocyanate reactive group the non-tertiary amine portion of the chain extender is bound to the polymeric network. Diffusion of the catalyst species from the polyurethane has been prevented, thus negating odor and toxicity as a problem. The aromatic diamine provides enhanced polyurethane physical properties.
摘要:
Novel amino acid derivatives useful as a therapeutic agent are disclosed. These amino acid derivatives and the pharmaceutically acceptable salts thereof have a human renin inhibitory effect when administered orally and are useful for treatment of hypertension, especially renin-associated hypertension.