Abstract: The present invention provides a process for the preparation of 11.alpha.-alkylprostaglandin E compounds from corresponding prostaglandin A compounds via reaction with alkyllithium complexes, and novel 11-deoxy-11.alpha.-alkylprostaglandin E compounds useful for the same pharmacological purposes as the natural PGE compounds, e.g., antiulcer and antisecretory effects.
Abstract: A process for treating viral diseases in humans and animals which comprises administering a therapeutic amount of a compound of the formula ##STR1## the compounds are formulated with pharmaceutical carriers for systemic or local means of administration.
Abstract: A process for treating Herpes Type II virus by the systemic administration or topical application of flurbiprofen (3-fluoro-4-phenylhydratropic acid) or a salt or ester thereof. Dosage forms are also disclosed.
Abstract: Ibuprofen is crystallized from a .delta.H.gtoreq.8 liquid such as a C.sub.1 to C.sub.3 -alkanol, e.g., methanol, containing solutions thereof to obtain ibuprofen crystals which are equant (cube, sphere or grain) in shape, which ibuprofen crystals have larger average partile size, higher bulk density, lower bulk volume and improved flow properties compared to previously known bulk ibuprofen crystalline materials.
Abstract: Therapeutic process for treating panic disorders in humans comprising the systemic administration of a 8-chloro-1-R-oxymethyl-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine of the formula ##STR1## wherein R is hydrogen, alkyl of from 1 to 3 carbon atoms, inclusive, ##STR2## wherein n is 0 to 16, inclusive, and m is 1 to 16 inclusive, including the N-oxides, esters, and pharmacologically acceptable acid addition salts thereof in combination with a pharmaceutical carrier.
Abstract: The present invention provides novel 19-hydroxy-7a-homo-PGI.sub.1 19-hydroxy-19-methyl-7a-homo-PGI.sub.1 compounds which are useful for pharmacological purposes, e.g., anti-asthmatic indications.
Abstract: The present invention provides novel methods of inducing diuresis and/or an antihypertensive effect employing certain 2,6-diaryl-4-pyridinecarboxylic acid derivatives. Also provided are novel compositions to be used in these methods.
Abstract: An improved process for preparing a 1-aminomethyl-6-substituted-4H-s-triazolo[4,3-a][1,4]benzodiazepine product, e.g., adinazolam, directly from the corresponding 1-hydrogen-6-substituted-4H-s-triazolo[4,3-a][1,4]benzodiazepine starting material, e.g., from estazolam, by conducting the reaction between the estazolam-type compound and the dimethylaminomethylene salt in the selected solvent in the presence of an alkali metal carbonate, and thereafter extracting the 1-aminomethyl-6-substituted-4H-s-triazolo[4,3-a]-[1,4]benzodiazepine from an aqueous organic solvent mixture thereof into a halogenated C.sub.1 to C.sub.3 -alkane solvent while maintaining the pH of the aqueous phase between pH 3.0 and 4.0, and thereafter recovering the product from the halogenated alkane solvent.
Type:
Grant
Filed:
May 25, 1983
Date of Patent:
October 2, 1984
Assignee:
The Upjohn Company
Inventors:
Donald J. Cram, Martin Gall, Michael F. Lipton
Abstract: Racemic mixtures and optically active isomers of (.alpha.S-5S)-.alpha.-amino-3-chloro-.alpha.-isoxazoline-5-acetic acid (AT-125). Provides process for preparing AT-125 and its analogs and intermediates used in the process.
Abstract: A process for treating Herpes Type I virus by the systemic administration or topical application of flurbiprofen (3-fluoro-4-phenylhydratropic acid) or a salt or ester thereof. Dosage forms are also disclosed.
Abstract: Novel antibiotic U-64,864 producible in a fermentation under controlled conditions using a biologically pure culture of the microorganism Streptomyces braegensis Dietz sp.n., NRRL 12567. This antibiotic is active against various Gram-positive bacteria, for example, Staphylococcus aureus, Streptococcus pyogenes and Streptococcus pneumoniae. Thus, antibiotic U-64,864 can be used in various environments to eradicate or control such bacteria.
Type:
Grant
Filed:
September 2, 1982
Date of Patent:
September 25, 1984
Assignee:
The Upjohn Company
Inventors:
Lester A. Dolak, Fritz Reusser, Thomas M. Castle, Betty R. Hannon, Alice L. Laborde, Charles K. Marschke
Abstract: This invention pertains to some new organic compounds, to a process for preparing them, and to formulations of them suitable for pesticidal use. The invention is more particularly directed to imidic acid derivatives of N-thio(methyl)carbamates.
Abstract: Disclosed is an improved process for the production of organic polyisocyanate based molded polymers prepared from at least one organic polyisocyanate and at least one polyol in the presence of an internal release agent wherein the improvement comprises employing as said agent a polysiloxane having at least one unit of the formula ##STR1## wherein R is selected from the group consisting of lower-alkyl and aryl, R.sup.1 is a divalent hydrocarbon radical, and R.sup.2 is selected from the group consisting of lower-alkoxy, aryloxy, particular hydroxyalkyleneoxy, alkoxyalkyleneoxy, amino, and hydroxyalkylamino radicals.The molding process can be repeated in many cycles before the molds require cleaning or treatment with release agent. The ease and rapidity with which the present process can be carried out makes it particularly suited to RIM production methods.
Type:
Grant
Filed:
July 5, 1983
Date of Patent:
September 18, 1984
Assignee:
The Upjohn Company
Inventors:
Louis M. Alberino, Dale F. Regelman, George H. Temme
Abstract: Certain 1-(Nitrogen-containing group)-triazolo-benzodiazepines, e.g., adinazolam, are useful for treating psychotic, including schizophrenic, conditions in human patients.
Abstract: Cis- and trans-N-[2-amino(oxy- or thia group-substituted-cycloaliphatic)]benzeneacetamide and -benzamide compounds, e.g., 3,4-dichloro-N-[4,4-dimethoxy-2-(1-pyrrolidinyl)cyclohexyl]-N-methylbenzen eacetamide, and salts thereof, are provided. These compounds have analgesic properties. Processes for their preparation are disclosed. Pharmaceutical compositions and methods of use are also provided.
Abstract: The present invention relates to novel methods of preparing a wide variety of spectinomycin analogs and biologically acceptable salts thereof. Further, the invention relates both to novel intermediates and novel products therein. The novel products are spectinomycin analogs which can be used for the same biological purposes as spectinomycin. The processes of the invention provide for novel intermediates that are versatile and highly reactive exocyclic enones.
Abstract: Polyurethane polyether-based elastomers are described which are thermoplastic, recyclable and have increased high temperature resistance which permits fabrication by injection molding. The elastomers are the product of reaction of 4,4'-methylenebis(phenyl isocyanate), a particular group of polypropylene oxide-polyethylene oxide block copolymers and an extender [straight chain aliphatic diols C.sub.2-6 or the bis(2-hydroxyethyl ether) of hydroquinone or resorcinol]. The block copolymers have at least 50 percent primary hydroxyl groups, a pH in the range of 4.5 to 9, a content of alkali metal ion less than 25 ppm and a molecular weight of 1000 to 3000. The minimum ethylene oxide (E.O.) residue content (percent by weight) of the polyether for any molecular weight (M.W.) is governed by the equation: ##EQU1## In a particularly preferred embodiment the elastomers are prepared by replacing up to 25 percent by equivalents of the extender by certain diols (polyethylene glycols up to 1500 M.W. preferred).
Abstract: A process is disclosed for the preparation of liquid, storage-stable, polyisocyanate compositions containing a release agent formed in situ which compositions are useful, for example, as binder resins in the formation of particle boards which latter, because of the presence of the release agent, show no tendency to adhere to the face of metal platens used in their formation. The process comprises heating an organic polyisocyanate (polymethylene polyphenyl polyisocyanate preferred) with an acid phosphate (e.g. a mixture of mono- and di-alkyl acid phosphates) under conditions controlled as to time and temperature so as to yield a product which is storage stable and shows no tendency to deposit solid or to separate into two liquid phases.
Type:
Grant
Filed:
August 2, 1982
Date of Patent:
October 9, 1984
Assignee:
The Upjohn Company
Inventors:
Richard A. Prather, David L. Williams, Robert M. Partin, Warren J. Rabourn, deceased