Abstract: A 1,5-fortimicin B carbamate represented by the formula: ##STR1## wherein each R is hydrogen or monocyclicaryloxycarbonyl and R.sub.1 is selected from the group consisting of: loweralkyl, hydroxyloweralkyl, hydrogen, aminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, trihaloalkoxycarbonyl, an amino acid residue and an N-protected amino acid residue and the pharmaceutically acceptable salts thereof.
Abstract: An improved process for producing 3-O-demethylfortimicins comprising the steps of reacting the fortimicin to be 3-O-demethylated with a borontrihalide and recovering the 3-O-demethylfortimicin from the reaction mixture.
Abstract: Disclosed are pyrazoles of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, or phenyl, R.sub.2 is hydrogen or lower alkyl, R.sub.3 is alkoxy or hydroxy, R.sub.4 is lower alkyl, and the pharmaceutically acceptable acid addition salts thereof. The compounds are useful primarily as antipsychotic agents. As an example, they exhibit central nervous system activity as antischizophrenic agents.
Abstract: A new fortimicin, fortimicin AK. The compound is coproduced in the fermentation of Micromonospora olivoasterospora ATCC No. 21819, 31009 or 31010 along with fortimicin A, fortimicin B isofortimicin, fortimicin E and a number of other minor factors. The compound is useful as an intermediate in synthesizing fortimicin AK derivatives which are useful as antibiotics.
Abstract: Described is a method of increasing urinary excretion by administering effective amounts to a subject in need thereof of compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, loweralkyl, lowercycloalkyl, aralkyl, aryl, pyridyl, isoquinolyl or phthalazinyl, or aryl substituted by one or more hydrogen, halo, loweralkyl, lowercycloalkyl, haloloweralkyl, aminosulfonyl, nitro, hydroxy, alkoxy, carboxy, alkoxycarbonyl, cycloalkoxy carbonyl, aminocarbonyl, diloweralkylaminocarbonyl or ##STR2## wherein n is 4 or 5.R.sub.3 is hydrogen, halogen, loweralkyl or aryl, andR.sub.4 is hydrogen, acyl, amino or loweralkyl, and the pharmaceutically acceptable acid addition salts thereof.
Abstract: Described is a method of obtaining complete copying of the entire length of single stranded ribonucleic acid (RNA) into its complementary deoxyribonucleic acid (cDNA) by reverse transcription using binding protein. The method can be used in recombinant DNA research to copy total messenger RNA into DNA.
Abstract: 4"-O-alkylgentamicins and sagamicins represented by the formula: ##STR1## wherein R.sub.1 is hydrogen or methyl: R.sub.2 is hydrogen or methyl; R.sub.3 is hydrogen or hydroxy; R.sub.4 is hydroxy when R.sub.3 is hydrogen and hydrogen when R.sub.3 is hydroxy; and R.sub.5 is loweralkyl; and the pharmaceutically acceptable salts thereof, intermediates therefor, and compositions and methods employing the potent antibiotics of this invention.
Abstract: An improved method of 3-O-demethylating fortimicin B or a 4-N-alkylfortimicin B derivative comprising the steps of reacting fortimicin B with lithium in the presence of ethylenediamine and thereafter isolating 3-O-demethylfortimicin B from the reaction mixture.
Abstract: New fortimicins, fortimicins AH and AI. The compounds are coproduced in the fermentation of Micromonospora olivoasterospora ATCC No. 21819, 31009 or 31010 along with fortimicin A, Isofortimicin, Fortimicin E and a number of other minor factors. The compounds are useful as an intermediate in synthesizing fortimicins AH and AI derivatives which are useful as antibiotics.
Abstract: A new fortimicin, fortimicin AO. The compound is coproduced in the fermentation of Micromonospora olivoasterospora ATCC No. 21819, 31009 or 31010 along with fortimicin A, Isofortimicin, Fortimicin E and a number of other minor factors. The compound is useful as an intermediate in synthesizing fortimicin A0 derivatives which are useful as antibiotics.
Abstract: Fortimicin AN is coproduced with fortimicin A, fortimicin B and a number of other minor factors in the fermentation of Micromonospora olivoasterospora ATCC Nos. 21819, 31009 or 31010. Structurally, fortimicin AN is 1-N-glycyl-3-O-demethylfortimicin B. The compound is useful as an intermediate for 3-O-demethylfortimicin B which is readily obtained by hydrolysis of fortimicin AN in base.
Abstract: A new seldomycin factor 5 derivative is provided, O-demethylseldomycin factor 5. The compound is represented by the formula: ##STR1## The compound is a potent anti-bacterial agent.
Type:
Grant
Filed:
March 29, 1979
Date of Patent:
August 19, 1980
Assignee:
Abbott Laboratories
Inventors:
Ronald E. Carney, Robert L. DeVault, James B. McAlpine, Arthur C. Sinclair
Abstract: A 1-Epi fortimicin represented by the formula ##STR1## wherein: R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen or hydroxyl, R.sub.3 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminohydroxyloweralkyl, acyl, aminoacyl, diaminoacyl, hydroxyacyl, hydroxy-substituted aminoacyl, hydroxy-substituted diaminoacyl, N-loweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted N-loweralkylaminoacyl or hydroxy-substituted N,N-diloweralkylaminoacyl; R.sub.4 is hydrogen or methyl; and the pharmaceutically acceptable salts thereof.
Abstract: A method of reducing intra-ocular pressure in mammalian patients comprising administering to a glaucoma patient a therapeutically effective amount of a compound of the formula ##STR1## wherein, in the C ring, X is CH.sub.2, S, ##STR2## or NR.sub.4 where R.sub.4 is H, loweralkyl, loweralkenyl, loweralkynyl or loweralkanoyl; n is an integer of 0 to 3; m is an integer of 0 to 3, or the C ring is a quinuclidine ring ##STR3## each R.sub.1 is loweralkyl, and when taken together, the substituents R.sub.1 R.sub.1 form oxygen; R.sub.2 is a C.sub.1 -C.sub.20 straight or branched chain alkyl, cycloalkyl, or ##STR4## wherein Y is a straight or branched chain alkylene group having from 1 to 10 carbon atoms, and each R.sub.5, R.sub.6 and R.sub.7 are the same or different members of the group consisting of H, halo or loweralkyl; R.sub.3 is H or ##STR5## wherein Y' is a straight or branched chain alkylene group having 1 to 8 carbon atoms, a is an integer from 1 to 4, b is an integer from 1 to 4, Z is CH.sub.2, O, S or NR.
Abstract: 4,N, 2'-N and 4,2'-Di-N-derivatives of fortimicin AM and fortimicin AP are provided by this invention. The compounds are useful as anti-bacterial agents.
Abstract: A new fortimicin, fortimicin AL. The compound is coproduced in the fermentation of Micromonospora olivoasterospora ATCC No. 21819, 31009 or 31010 along with fortimicin A, Isofortimicin, Fortimicin E and a number of other minor factors. The compound is useful as an intermediate in synthesizing fortimicin AL derivatives which are useful as antibiotics.
Abstract: 6'-Epi-fortimicin A and B derivatives represented by the formula ##STR1## wherein R.sub.1 is hydrogen or loweralkyl, R.sub.2 is hydrogen or loweralkyl and R.sub.3 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, hydroxyloweralkyl, acyl, aminoacyl, hydroxyacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl or an amino acid residue; the pharmaceutically acceptable salts thereof; intermediates useful in their preparation, compositions employing the compounds; and methods of using the compounds. The compounds are useful as antibiotics.