Abstract: The invention relates to the chemical industry.A stable aqueous solution of a complex of polyvinylpyrrolidone and halogen is prepared by carrying out the following steps:(a) The halogen is put in solution in the presence of PVP in a solvent that solubilizes the two components, the said solvent having a boiling point lower than that of water, being insoluble in water, and forming no azeotrope with the latter;(b) The solution obtained is heated to react the PVP and the halogen;(c) The said solvent is displaced by addition of water brought to a temperature higher than the boiling point of the said solvent.These solutions are used as germicides and bactericides.
Abstract: Benzenesulfonamide derivatives as defined in the specification have an outstanding salidiuretic action. Some of the compounds exhibit a significant increase in the excretion of uric acid and the uric acid clearance. They are distinguished by a long-lasting period of action and are suitable for the treatment of hypertonic conditions in humans, optionally in combination with anti-hypertonic agents.
Type:
Grant
Filed:
August 16, 1978
Date of Patent:
November 25, 1980
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Hans-Jochen Lang, Roman Muschaweck, Max Hropot
Abstract: 5-Phenethyl oxazolidone compounds having the formula: ##STR1## wherein R represents a hydrogen or halogen atom or a lower alkoxy group have muscular relaxing, analgetic and antiinflammatory activities.
Abstract: 2-Chloro-4-(4-lower alkyl-1-piperazinyl)benzenemethanol, N.sup..omega. -oxides and their acid addition salts. These compounds are prepared by oxidizing the corresponding 2-chloro-4-(4-lower alkyl-1-piperazinyl)benzenemethanol. In addition, pharmaceutical compositions comprising said N-oxides and methods for treating schistosomiasis are disclosed.
Type:
Grant
Filed:
November 30, 1978
Date of Patent:
November 18, 1980
Assignee:
Edna McConnell Clark Foundation
Inventors:
Ernest Bueding, Leslie M. Werbel, Donald F. Worth
Abstract: Covers a process for preparing a mixture of piperazine and ethylenediamine by the hydrogenation reaction of monoethanolamine and ammonia utilizing a nickel-copper-chromium catalyst. The improvement of the invention involves predetermining the ratio of ethylenediamine to piperazine in the product mix by varying the hydrogen feed rate. Increasing said feed rate causes said ratio to decrease.
Abstract: 3-(N-Alkylcarbamyl)-5-(carboalkoxy)-1,3,4-oxadiazole-2-thione compound having the structural formula ##STR1## wherein R is alkyl having 1 to 4 carbon atoms and R.sup.1 is alkyl having 1 to 4 carbon atoms, and their use as anti-inflammatory agents.
Type:
Grant
Filed:
March 20, 1979
Date of Patent:
November 18, 1980
Assignee:
Stauffer Chemical Company
Inventors:
Jack R. DeBaun, Ferenc M. Pallos, Arnold D. Gutman
Abstract: Novel 1-substituted-3-acylpyrrole derivatives of the formula ##STR1## wherein all symbols are as defined in the specification; and platelet aggregation inhibiting agents comprising them as active ingredients. These novel 1-substituted-3-acylpyrrole derivatives are prepared by condensing the corresponding 1-substituted pyrrole derivatives with the corresponding acylating agents in the presence of acid catalysts, and if desired, subjecting the products to oxidation, hydrolysis, amidation or acetal-forming reaction. These 1-substituted-3-acylpyrrole derivatives exhibit unique properties in that they have superior platelet aggregation inhibiting actions with low antiinflammatory activity.
Abstract: In a process of preparing 2,2,2-trichloro-1-(N-hydrocarbylpyrryl-2)-ethanol by mixing and reacting essentially equimolar quantities of chloral and N-hydrocarbylpyrrole in a liquid reaction system containing a protonic acid added in the form of an organic acid, improvements have been made. The improvement involves (i) performing the reaction in a methylene chloride reaction medium containing protonic acid added in the form of a carboxylic acid whose acidic dissociation constant is not substantially greater than that of acetic acid, and (ii) proportioning the relative amounts of the chloral, N-hydrocarbylpyrrole and methylene chloride reaction medium so as to result in the formation of a solution of 2,2,2-trichloro-1-(N-hydrocarbylpyrryl-2)-ethanol in the reaction medium having a concentration in the range of about 1 to about 8 molar.
Abstract: N-(hydroxyphenyl) maleimides of the general formula ##STR1## where R' stands for H, CH.sub.3, C.sub.2 H.sub.5, F, Cl, Br or I and n is an integer of 1-5 are produced by treating the corresponding maleamic acid or by treating the ester of said N-(hydroxyphenyl) maleimide at a temperature of 0-150.degree. C. in the presence of at least one dehydrating agent selected from the group consisting of oxides and oxyacids of sulfur or phosphorus and alkali metal and alkaline earth metal salts of the said oxyacids. The corresponding maleamic acid can be obtained by reacting an aminophenol having one or more hydroxyl groups on its phenyl nucleus with maleic anhydride. The esters of the N-(hydroxyphenyl maleimide) can be obtained by reacting said aminophenol and said maleic anhydride in the presence of a conventional acid anhydride dehydrating agent and a conventional imide-forming cyclization catalyst.
Type:
Grant
Filed:
November 2, 1978
Date of Patent:
November 4, 1980
Assignee:
Mitsui Toatsu Chemicals, Incorporated
Inventors:
Masayuki Oba, Motoo Kawamata, Hikotada Tsuboi, Nobuhito Koga
Abstract: The present invention is related to a process in which an oxazolidinone is reacted with phosphorus pentachloride and the resulting mixture is reacted with a nucleophilic agent in an inert solvent to give P-substituted N,N'-bis-(3-oxazolidinyl-2-one)phosphoramides having the general formula ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4 are each a group selected from among hydrogen, C.sub.1 -C.sub.4 alkyls or an aromatic nucleus and X is a group which may be introduced by nucleophilic substitution. The invention is also related to the compounds thus obtained.
Abstract: 3,4-Epoxypyrrolidines substituted in the 1-position with alkyl, cycloalkyl and phenylalkyl are disclosed which have pharmaceutical application in cataract prevention in animals and as intermediates in preparation of trans-3-aryloxy-4-hydroxypyrrolidines. The epoxypyrrolidines are prepared by a novel route involving chlorination of pyrrolines in aqueous medium.
Type:
Grant
Filed:
January 9, 1979
Date of Patent:
October 28, 1980
Assignee:
A. H. Robins Company, Inc.
Inventors:
David A. Walsh, William J. Welstead, Jr.
Abstract: Pyrrolidine derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as hereinafter described, prepared inter alia from the corresponding pyrrolines, are described. The compounds are useful as analgesic agents.
Type:
Grant
Filed:
November 13, 1978
Date of Patent:
October 28, 1980
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Karl Bernauer, Karlheinz Pfoertner, Fernand Schneider, Hans Schmid, deceased, by Mary Margrith Baumann-Schmid, heir, by Maria Albertine Schmid-Suter, heir, by Jeannette Martha Wawrla-Schmid, heir, by Ernst Georges Schmid-Gautschi, heir
Abstract: A process for the activation of carboxylic acids which is useful for the subsequent conversion of said carboxylic acids into their corresponding amides or esters, based on reacting a 2-oxazolidinone with phosphorus pentachloride and subsequent addition of a salt of the carboxylic acid to be activated.
Type:
Grant
Filed:
July 2, 1979
Date of Patent:
October 28, 1980
Assignee:
Antibioticos, S.A.
Inventors:
Antonio L. Palomo Coll, Jose Diago Meseguer
Abstract: Compounds of the general formula ##STR1## wherein X is halogen, lower alkyl or lower haloalkyl, andn is 0, 1 or 2;are outstanding effective fungicides.
Abstract: In the production of maleimides of the general formula I ##STR1## in which n is one of the numbers 1, 2 or 3, R.sup.1 and R.sup.2 are each a hydrogen atom or methyl, and A is an n-valent aliphatic, cycloaliphatic, aliphatic-cycloaliphatic or aliphatic-aromatic radical having up to 30 C atoms, by means of cyclising dehydration of a maleamic acid of the formula II ##STR2## in which the acid amide group (s) is (are) attached to aliphatic or cycloaliphatic C atoms, in the presence of low-molecular dehydrating carboxylic anhydrides in an organic solvent and in the present of catalysts, there is advantageously used as solvent a polar aprotic solvent containing at least one N-lower-alkyl-substituted acid amide group in the molecule, or a solvent mixture containing an aprotic solvent of this type, and as catalyst a metal compound, and the cyclising dehydration is performed in the temperature range of 40.degree. to 100.degree. C.
Abstract: 9-(.beta.-hydroxyethyl) piperazinyl-carbonyl-2-trifluoromethyl-10, 11-dihydrodibenzo[b,f]thiepin is prepared and disclosed as having antiinflamatory action.
Abstract: Novel spiro-oxazolidinediones useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications are disclosed. Pharmaceutical compositions containing the novel compounds and a method of treating chronic diabetic complications are also disclosed.
Abstract: Insecticidal or miticidal compounds have the formula ##STR1## in which R is selected from the group consisting of 1-4 carbon alkoxy, phenyloxy, and 1-6 carbon alkylthio;R.sub.1 is selected from the group consisting of 1-4 carbon alkyl, and 1-4 carbon alkoxy;R.sub.2 is 1-6 carbon alkoxy;X is hydrogen or methyl; andY is sulfur or oxygen.