摘要:
The invention relates to novel peptides, of pharmacological activity, of the formula: ##STR1## wherein R.sup.1 is hydrogen,R.sub.b.sup.1 is methyl,R.sup.2 is carboxy, carboxymethylcarbamoyl, 1-carboxyethylcarbamoyl or ethoxycarbonylmethylcarbamoyl,R.sup.q is carboxy or 3-t-butoxycarbonylcarbazoyl,R.sup.p is carboxy or methoxycarbonyl,R.sup.r is hydrogen, t-butoxycarbonyl or benzyloxycarbonyl,m is the integer 2, andn is the integer 1, or its pharmaceutically acceptable salt.
摘要:
The invention relates to novel peptides of enhanced pharmacological activity of the formula: ##STR1## wherein R.sup.1 is hydroxyalkanoyl,R.sup.2 and R.sup.q are each hydrogen, carboxy, protected carboxy, or a group of the formula: ##STR2## wherein R.sub.a.sup.2 is mono- or di-carboxy (or protected carboxy) lower alkyl or ar(carboxy or protected carboxy) lower alkyl whose aryl moiety may be substituted by hydroxy, R.sup. 2 is hydrogen or lower alkyl; R.sup.p is hydrogen, carboxy, protected carboxy, with proviso that when one of R.sup.2 and R.sup.q is hydrogen, then the other is carboxy or protected carboxy or a group of the formula: ##STR3## wherein R.sub.a.sup.2 and R.sub.b.sup.2 are each as defined above; R.sup.r is hydrogen or amino protective group; m is an integer 1 to 3;or its pharmaceutically acceptable salt.
摘要:
The invention relates to compounds and salts of compounds which are diaminopimelyl peptides, N-acetoxypropionyl or N-t-butoxycarbonyl-amino-acid - (.alpha.-OBzl) glutamic acid peptides or N-acylated derivatives of (.alpha.-OBzl) glytamic acid or of (.alpha.-OBzl) aminoadipic acid.The compounds and their salts are starting materials for the preparation of pharmacologically active peptides.
摘要:
The invention relates to novel intermediates for the preparation of peptides of pharmacological activity, said intermediates being of the formulas: ##STR1## wherein R.sub.2.sup.r is amino protective group andY is hydrogen or amino protective group; and : ##STR2##
摘要:
A compound of high antimicrobial activity of the formula: ##STR1## in which R.sup.1 is amino or a substituted amino group andR.sup.2 is hydrogen or lower alkoxy, orR.sup.1 and R.sup.2 are combined together to form a group of the formula: ##STR2## wherein R.sup.6 and R.sup.7 are each hydrogen or lower alkyl, andA is a group of the formula: ##STR3## wherein X is --S-- or ##STR4## R.sup.3 is carboxy or a protected carboxy group and R.sup.4 is hydrogen, hydroxy or acyl,and pharmaceutically acceptable salts thereof.
摘要:
The invention relates to novel peptides of enhanced pharmacological activity of the formula: ##STR1## wherein R.sup.1 is alkanoyl;R.sup.2 and R.sup.q are each hydrogen, carboxy, protected carboxy, or a group of the formula: ##STR2## wherein R.sub.a.sup.2 is mono- or di-carboxy (or protected carboxy) lower alkyl or ar(carboxy or protected carboxy) lower alkyl whose aryl moiety may be substituted by hydroxy,R.sub.b.sup.2 is hydrogen or lower alkyl;R.sup.P is hydrogen, carboxy, protected carboxy, with proviso that when one of R.sup.2 and R.sup.q is hydrogen, then the other is carboxy or protected carboxy or a group of the formula: ##STR3## wherein R.sub.a.sup.2 and R.sub.b.sup.2 are each as defined above; R.sup.r is hydrogen or amino protective group;m is an integer 1 to 3;or its pharmaceutically acceptable salt.
摘要:
The invention deals with novel peptides useful for the therapeutic treatment of infectious diseases caused by pathogenic microorganisms. Included is the peptide FR900156 having the structure: ##STR1## as well as the peptides of the structure ##STR2## wherein R.sup.1 is acyl;R.sub.b.sup.1 is hydrogen, methyl, isopropyl, hydroxymethyl, protected hydroxymethyl or benzyl;R.sup.2 is hydrogen, carboxy, protected carboxy, or a group of the formula: ##STR3## wherein R.sub.a.sup.2 is mono- or di-carboxy lower alkyl or ar(carboxy) lower alkyl whose aryl moiety may be substituted by hydroxy,R.sub.b.sup.2 is hydrogen or lower alkyl;R.sup.p and R.sup.q are each hydrogen, carboxy, protected carboxy, with proviso that when one of R.sup.2 and R.sup.q is hydrogen, then the other is carboxy or protected carboxy;R.sup.r is hydrogen or amino protective group; m is an integer 1 to 3; and n is 1 provided that when R.sup.1 is hydrogen, t-butoxycarbonyl or N-acetylmuramyl, R.sub.b.sup.1 is methyl, m is an integer 2 and n is an integer 1, then R.sup.2 is hydrogen, protected carboxy or a group of the formula: ##STR4## wherein R.sub.a.sup.2 is mono- or di-carboxy lower alkyl having 1 and 3 to 6, carbon atoms, .alpha.-carboxyethyl, ar(carboxy) lower alkyl whose aryl moiety may be substituted by hydroxy and R.sub.b.sup.2 is as defined above, or its pharmaceutically acceptable salt.
摘要:
Compounds of the formula ##STR1## wherein X is --O--or --S--;R.sup.1 is amino or a substituted amino group;R.sup.2 is carboxy or a protected carboxy group; and the heavy solid line means single or double bond; the compounds are useful in the treatment of infectious diseases particularly fungal infection, in human beings and animals.
摘要:
Cephalosporin analogues represented by the formula ##STR1## wherein R.sup.1 is amino or a substituted amino,R.sup.2 is carboxy or a protected carboxy, andR.sup.3 is hydrogen or lower alkoxy, processes for making the same, azetidinone intermediates and pharmaceutical compositions comprising said cephalosporin analogues as active ingredients.
摘要:
This invention relates to .alpha.-crystals of cefazolin sodium with a water content in the range of 13.0 to 15.8%, useful as an antibiotic of improved thermal and light stability.