Abstract: This invention provides 4-N-acylfortimicin B derivatives of the structure ##STR1## wherein R is acyl, aminoacyl, N-monoloweralkylminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, or substituted aminoacyl of the formula ##STR2## where R.sup.1 is an acyl radical derived from an amino acid or a short peptide, and the pharmaceutically acceptable salts thereof.The compounds are useful as intermediates for preparing 4-N-alkyl or substituted alkylfortimicin B derivatives. In addition to their utility as intermediates, some of the compounds of this invention are also useful as antimicrobial agents.
Type:
Grant
Filed:
January 10, 1979
Date of Patent:
November 4, 1980
Assignee:
Abbott Laboratories
Inventors:
John S. Tadanier, Jerry R. Martin, Paul Kurath
Abstract: The present invention encompasses an improved method for detecting antigen or antibody bound to a solid support which involves the reaction of hapten-labeled antibody to the antigen or antibody to be detected followed by reaction of the hapten moiety with labeled antibody to the hapten and the determination of the amount of label bound to the solid support.
Type:
Grant
Filed:
August 9, 1978
Date of Patent:
October 28, 1980
Assignee:
Abbott Laboratories
Inventors:
Richard H. Decker, Chung-Mei Ling, Lacy R. Overby
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: Automatic dispensing apparatus such as used in a chemical analysis system for transferring liquids from sample containers to analysis containers, including a pipet probe assembly with an elongated probe, probe drive means for inserting the probe into the sample and moving the probe assembly between the sample container and analysis container, means for aspirating and dispensing a portion of the sample from the probe into a respective analysis container, an elongated level sensing probe extending downwardly from the probe assembly, with the difference in distance between the tip of the level sensing probe and the tip of the pipet probe defining the amount of penetration of the pipet probe tip below the sample level, and control means, including means responding to the tip of the level sensing probe contacting said sample level to stop the probe drive means thereby minimizing the penetration of the pipet probe tip below the sample level.
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: A pre-amplifier for photomultiplier tubes includes means to compensate for the combined dark current and noise output of a photomultiplier tube without inducing a noise dependent offset voltage at the pre-amplifier output. A feedback amplifier and a compensating network, including a capacitor, cooperate to monitor the pre-amplifier output and during this time to maintain the feedback amplifier in a linearly responsive state while charging the capacitor to an amount necessary to clamp the average value of the most negative excursion of the pre-amplifier output to ground.
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: 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: A prefilled, readily activated syringe assembly wherein a fluid medicament and a diluent therefor can be intermixed in a syringe barrel with a venting thereof. A medical powder is sealed in a barrel by means of an intermediate slidable stopper and the diluent is sealed in the same barrel between the stopper and a plunger stopper. A bypass channel is provided in the syringe barrel which permits intermixing of the diluent and the medicament when the plunger stopper is moved toward the intermediate stopper. Movement of the plunger stopper inwardly in the barrel is afforded by means of a hydrophobic filter element associated with the nozzle portion. After intermixing of the diluent and the medicament the filter vent is pierced by means of a piercing tubular member to which is attached a hypodermic needle. Continued movement of the plunger stopper will expel the mixed medicament from the syringe.
Abstract: The present invention encompasses a method for enumerating microbial cells in an aqueous test sample comprising: fluorescently labeling the microbial cells in test sample intermixing a known amount of monodispersed fluorescently labeled beads of about cell size into the test sample, and determining the ratio of bacterial cells to fluorescently labeled beads, the reagents for practicing this method. The methods and reagents of the present invention are particularly useful in counting bacterial cells in urine.
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: A novel valve employing hydrophobic and hydrophilic membranes and providing a combined air barrier and liquid sequencing valve. The novel valve is useful in gravitational flow systems and equipment sets for the sequential administration of medical liquids, wherein a primary liquid can be administered at a flow rate independent of the flow rate of a secondary liquid, and includes barriers substantially impervious to air to prevent the inadvertent administration of air when the liquids are depleted.
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: The present invention comprises compounds of the formula ##STR1## and the biologically acceptable acid addition salts thereof, wherein R.sub.1 represents hydrogen or lower alkyl having 1 to 4 carbon atoms; R.sub.2 represents an alkylene having 2 to 4 carbon atoms; R.sub.3 represents amino or guanidino; R.sub.4 represents nitrophenyl, methylnitrophenyl, dinitropheyl, naphthyl, or nitronaphtyl; m is 2 or 3; and n is 3 or 4. The compounds of the present invention are analytical reagents useful for measuring proteolytic enzymes such as thrombin and trypsin. The enzymatic hydrolysis of the invention compounds provides a chromogenic amine by which the proteolytic enzyme concentration can be determined spectrophotometrically.