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: 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: The compound of the formula ##STR1## has been found to be an important and practical intermediate with the proper stereo-isomerism for the preparation of numerous prostaglandin derivatives. It can easily be converted to 4.alpha.-acetoxy-2-cyclopentenone by a variety of processes.
Type:
Grant
Filed:
February 6, 1978
Date of Patent:
October 21, 1980
Assignee:
Kansas University Endowment Association
Inventors:
Lester A. Mitscher, George W. Clark, III, Paul B. Hudson
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: 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: 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 feminine syringe unit wherein a housing with a valve member and nozzle serve as both a filling and dispensing port for an expandable syringe bag. The syringe unit includes a removable nozzle retainer which has slidably secured thereto a nozzle member. When the nozzle member is removed, the bag is easily filled through a filling orifice and a dispensing flap valve. For cleaning and drying purposes, the valve is also removable from the bag by means of its being engaged by a valve retainer which in turn is threadably engaged on a bag retainer. The unit is activated by moving the nozzle toward the bag whereby the inlet portion of the nozzle will abut against a flap valve so as to create fluid communication between the inside of the bag and the nozzle. A hold-open means is also provided for the nozzle inlet portion in the valve member so that when a force is exerted on the bag to eject liquid through the nozzle it will not force the valve closed.
Abstract: A closure for a syringe of the feminine or enema type wherein the nozzle of the syringe is intended to be transported separately from the flexible bag. The neck of the flexible bag which has a bead is secured on a support ledge of an inner connecting member which threadably receives the nozzle. An outer connecting member having spaced internal flange members is snap fitted over the inner connecting member to engage a portion of the bag and resiliently hold it against the inner connecting member. In a preferred manner, an accommodating compartment is formed between the two connecting members to accommodate the bead of the bag.
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: 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: 2,3-Dichloro-4-(hydroxybenzoyl)phenoxyacetic acid, its analogs and their salts are powerful uricosuric diuretics; they can be made in a one-pot reaction from a loweralkyl 2,3-dichloro-4-(nitrobenzoyl)phenoxyacetate or its analogs.
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: 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 prevent the inadvertent administration of air when the secondary liquid is depleted. The sets of this invention employ parallel flowpaths for the secondary liquid and a single liquid sequencing valve to control the flow of the primary liquid and the secondary liquid in one of the parallel flowpaths.
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.