摘要:
A new triazene compound of the formula:R--CH.dbd.N--N.dbd.N--OHwherein R is alkyl, alkenyl or aryl and its pharmaceutically acceptable salts thereof. The production and use of such compounds are also disclosed. The compounds are useful as smooth muscle relaxants and hypotensives.
摘要:
The invention relates to a biologically pure culture of new strains of the microorganism Streptomyces which are capable upon fermentation of producing a peptide of pharmacological activity.
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 .Iadd.provided that when R.sup.1 is benzyloxycarbonyl R.sub.5.sup.1 is methyl, m is an integer 2 and n is an integer 1, then R.sup.2 is not protected carboxy, and .Iaddend.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,.]. .Iadd.--CH.sub.2 --CH.sub.2 --COOH, .Iaddend.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:
The invention concerns peptides, having the pharmaceutical property of enhancing the immune response, having the structure: ##STR1## wherein R.sup.1 is alkanoyl,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: ##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 is substituted by hydroxy or not substituted,R.sub.b.sup.2 is hydrogen or lower alkyl,R.sup.p is hydrogen, carboxy or protected carboxy,R.sup.q is carboxy, 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, andn is an integer 1.
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:
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##