Abstract: The new compound 4-hydroxy-1,2-benzisothiazole and its derivatives, and their manufacture. The products are intermediates for new drugs which are useful in cardiac and circulatory disorders.
Type:
Grant
Filed:
January 23, 1978
Date of Patent:
February 19, 1980
Assignee:
BASF Aktiengesellschaft
Inventors:
Ulrich Ohnsorge, Helmut Hagen, Fritz-Frieder Frickel
Abstract: 3,4-Dihydro-10-[2-(dialkylamino)ethyl]-1-phenyl-1H-thiazino[4,3-a]indol-4-o l compounds having in free base form the formula ##STR1## where R.sub.1 and R.sub.2 are lower alkyl groups. The compounds of this invention exhibit anti-allergy properties and are indicated in the management of allergy.
Abstract: O-Alkyl-O-(6-dialkylcarbamoyloxy-pyrimidin-4-yl)-(thiono)(thiol)-phosphoric (phosphonic) acid esters and esteramides of the formula ##STR1## in which R is alkyl,R.sup.1 is alkoxy, alkylthio, alkylamino, alkyl or phenyl,R.sup.2 is hydrogen, alkyl, alkoxy, alkylthio, alkylamino or phenyl,R.sup.3 and R.sup.4 each independently is alkyl,R.sup.5 is hydrogen, alkyl or halogen, andX is oxygen or sulphur,which possess arthropodicidal properties.
Abstract: The invention provides novel amides of (2-pyrimidinyl-thio)-alkanoic acids having antilipemic activity combined with a lower toxicity than the corresponding acids.
Abstract: Compounds represented below ##STR1## and pharmaceutical compositions thereof, the compositions including the non-substituted phenylene dioxamates are useful in the prophylactic treatment of sensitized mammals for allergy and all anaphylactic reactions of a reagin or non-reagin mediated nature.
Abstract: This invention relates to 3-(phenyl/naphthyl)-benz[d]isothiazole-1,1-dioxides wherein the 3-phenyl or the 3-naphthyl group is substituted in the para position with hydroxy blocked with certain protecting groups. These compounds are useful as intermediates in the synthesis of certain 3,3-disubstituted-2,3-dihydrobenz[d]isothiazole-1,1-dioxide dyes which find utility, for example, as photographic optical filter agents and filter agent precursors.
Type:
Grant
Filed:
September 23, 1977
Date of Patent:
January 1, 1980
Assignee:
Polaroid Corporation
Inventors:
Alan L. Borror, Louis Cincotta, Ernest W. Ellis, James W. Foley, Marcis M. Kampe
Abstract: A compound selected from a 2,4-diamino-5-thiobenzylpyrimidine of the formula: ##STR1## in which R is selected from hydrogen, alkyl, lower alkoxy, and halogen and R' is alkyl; and pharmacologically acceptable acid addition salts thereof. These compounds have an anti-bacterial action and are sulphonamide potentiators.
Type:
Grant
Filed:
March 29, 1978
Date of Patent:
December 25, 1979
Assignee:
Ludwig Heumann, & Co. GmbH
Inventors:
Edgar Fritschi, Walter Liebenow, Jaroslav Prikryl
Abstract: New furo[2, 3d]pyrimidine derivatives of the general formula: ##STR1## wherein R.sub.1 represents a lower alkyl, a lower alkenyl or an aralkyl group, and R.sub.2 represents a lower alkyl, unsubstituted phenyl, carboxyl, methylsulphonyl, methoxycarbonyl or a nitro-substituted phenyl group, or the corresponding pharmacologically acceptable acid addition salts. The new compounds exhibit the outstanding anti-ulcer, anti-inflammatory and anti-edema effects.
Abstract: This invention relates to a method of synthesizing certain 3-(carbocyclic aryl)-3-(4'-OP-carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxides (and -2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxides) by reacting (a) a 4-OP-carbocyclic aryllithium compound wherein P is a protecting group and (b) a 3-(carbocyclic aryl)benz[d]isothiazole-1,1-dioxide wherein said 3-(carbocyclic aryl) moiety is other than a 3-(4'-OP-carbocyclic aryl) moiety to give (c) the corresponding 3-carbocyclic aryl)-3-(4'-OP-carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxide. The -2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxides are prepared in the same manner by reacting a 3-(carbocyclic aryl)naphtho[1,8-de]-1,2-thiazine-1,1-dioxide with said 4'-OP-carbocyclic aryllithium compound.
Type:
Grant
Filed:
September 23, 1977
Date of Patent:
December 11, 1979
Assignee:
Polaroid Corporation
Inventors:
Alan L. Borror, James W. Foley, Marcis M. Kampe, John W. Lee, Jr.
Abstract: Compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, halogen, alkyl, alkoxy or nitro; R.sub.2 is hydrogen, halogen or alkoxy; and R.sub.3 is alkoxycarbonyl, ##STR2## pyridinylcarbonyl, pyrimidinylcarbonyl, or pyrazinylcarbonyl; have antiinflammatory activity.
Abstract: Herbicidal N-(haloacetyl)-N-(N'-methylenepyrrolidonyl)-2-alkoxyanilines are provided in this invention having the formula: ##STR1## where R is alkyl of 1-6 carbon atoms, R' is hydrogen or lower alkyl of 1-3 carbon atoms, and X is halogen.Another feature of the invention is the provision of N-(N'-methylenepyrrolidone)-2-alkoxyaniline or intermediates useful in making such herbicides. These intermediates are prepared by reaction of a 2-alkoxyaniline with an N-methylolpyrrolidone or an N-halomethylenepyrrolidone. The herbicide product than is obtained by acylation of the intermediate with a haloacetyl halide.The compounds of the present invention show good herbicidal activity against grassy weeds.
Abstract: Herbicidal compounds having the formula: ##STR1## where n is 1-3,R is alkyl of 1-3 carbon atoms,R' is hydrogen or alkyl of 1-3 carbon atoms, andx is chloro or bromo,are disclosed herein.The compounds of the invention show good herbicidal activity, especially against wild grasses.
Abstract: This invention relates to phenol sulfam(na)phthaleins possessing a ##STR1## group wherein Y represents an electron-withdrawing group substituted on the N atom of the sulfam(na)phthalein ring, which compounds find utility as photographic optical filter agents and filter agent precursors.
Type:
Grant
Filed:
September 23, 1977
Date of Patent:
December 11, 1979
Assignee:
Polaroid Corporation
Inventors:
Stanley M. Bloom, Alan L. Borror, James W. Foley
Abstract: Benzisothiazolines having the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl, alkoxy, halogen or nitro;R.sub.2 is alkyl; and R.sub.3 is (i) ##STR2## wherein X is oxygen, sulfur or imino or (ii) ##STR3## wherein Y is alkoxy, alkyl, or arylalkyl, have useful pharmacological activity.
Type:
Grant
Filed:
July 20, 1978
Date of Patent:
December 4, 1979
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Peter C. Wade, B. Richard Vogt, Thomas P. Kissick
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is lower alkyl; phenyl-lower alkyl; cycloalkyl of 3 to 6 carbon atoms; phenyl; mono- or di-substituted phenyl, where the substituents, which may be identical to or different from each other, are each halogen, hydroxyl, methoxy, methylmercapto, methylsulfinyl, methylsulfonyl or benzyloxy; andA is hydrogen or ##STR2## where R.sub.2 is hydrogen or lower alkyl;R.sub.3 is lower alkyl or dimethoxyphenyl-lower alkyl; orR.sub.2 and R.sub.3, together with each other and the nitrogen atom to which they are attached, are piperidino, morpholino or N'-lower alkyl-piperazino; andn is 2 or 3;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as cardiotonics, hypotensives, antithrombotics and antiarrhythmics.
Type:
Grant
Filed:
July 17, 1978
Date of Patent:
November 27, 1979
Assignee:
Boehringer Ingelheim GmbH
Inventors:
Volkhard Austel, Eberhard Kutter, Joachim Heider, Wolfgang Eberlein, Walter Kobinger, Christian Lillie, Willi Diederen, Walter Haarmann
Abstract: Compounds which have the general formula ##STR1## and those which can be obtained from them with a Vilsmeier type reagent and have the formula ##STR2## as well as salts thereof, are useful as anti-inflammatory agents.
Abstract: The compounds are dithiocarbamates and isothioureas which are histamine H.sub.2 -antagonists. Two compounds of the invention are 2-(5-methyl-4-imidazolylmethylthio)ethyl N-methyldithiocarbamate and S-[2-(5-methyl-4-imidazolyl-methylthio)ethyl]-N-cyano-N'-methylisothiourea .
Type:
Grant
Filed:
July 28, 1978
Date of Patent:
November 6, 1979
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Thomas H. Brown, Graham J. Durant, Charon R. Ganellin, Robert J. Ife
Abstract: Preparation of compounds of the formula: ##STR1## wherein n is 1, 2 or 3, R.sub.1 and R.sub.2, which may be the same or different, are hydrogen or alkyl containing 1 to 3 carbon atoms and the asterisk indicates the center of asymmetry of the molecule, and compounds of the formula ##STR2## wherein R" is a saturated or unsaturated aliphatic hydrocarbon containing 1 to 6 carbon atoms, R.sub.3 is hydrogen or acyl containing 1 to 7 carbon atoms and the asterisk indicates the center of asymmetry of the molecule. The compounds produced by the present invention improve learning memory and display a protecting effect against the E.E.G. consequence of an overdose of barbiturates and against the reduced performance following brain damage (e.g. cerebral edema).
Type:
Grant
Filed:
February 8, 1978
Date of Patent:
November 6, 1979
Assignee:
I.S.F. SpA
Inventors:
Silvano Banfi, Renato Pellegata, Giorgio Pifferi, Mario Pinza