Thiadiazines Patents (Class 544/8)
  • Patent number: 4861879
    Abstract: Substituted [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]methyl]-1H -imidazoles and 1H-1,2,4-triazoles having antimicrobial properties and being particularly useful in the treatment of vaginal candidosis.
    Type: Grant
    Filed: February 9, 1988
    Date of Patent: August 29, 1989
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Heeres, Raymond A. Stokbroekx, Leo J. J. Backx
  • Patent number: 4855309
    Abstract: The compounds of the formula (I) ##STR1## in which A denotes N or N.fwdarw.0,R denotes a radical of the formula R.sup.4 --CY.sup.1 --NR.sup.5 --CY.sup.2 --NR.sup.6 --, ##STR2## R.sup.1 denotes halogen, alkyl, alkenyl, alkynyl, alkoxy, alkoxycarbonyl or alkylcarbonyl, where these radicals may be halogenated, nitro, cyano or carboxyl, R.sup.2 denotes halogenated alkoxy, halogenated alkenyloxy or halogenated alkynloxy, R.sup.3 denotes halogen, n denotes 0, 1 or 2, m denotes 0, 1, 2 or 3, and p denotes 0 or 1, and also the salts thereof, are advantageously suitable for combating noxious insects, acarides, nematodes or mollusks.
    Type: Grant
    Filed: December 19, 1986
    Date of Patent: August 8, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Volker Koch, Andreas Fuss, Werner Bonin, Werner Knauf, Anna Waltersdorfer
  • Patent number: 4851406
    Abstract: The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl, cycloalkyl, cycloalkenyl, carboxyl, cyano, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or aryl radical, R.sub.2 is a hydrogen atom or an alkyl, trihalogenomethyl, hydroxyl, cycloalkyl, cyano, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl radical; R.sub.2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and six-membered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R.sub.
    Type: Grant
    Filed: September 4, 1986
    Date of Patent: July 25, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Alfred Mertens, Wolfgang von der Saal, Walter-Gunar Friebe, Bernd Muller-Beckmann, Gisbert Sponer
  • Patent number: 4775406
    Abstract: The salts of 1-phenylimidazole-5-carboxylic acids substituted in the phenyl ring, of the general formula (I) ##STR1## exhibit a good plant growth-regulating activity. In the general formula the symbols have the following meaning:Y is an ammonium ion substituted up to fourfold by (substituted) alkyl, (substituted) alkenyl, alkynyl, (substituted) cycloalkyl, cycloalkenyl, and (substituted) phenyl, wherein the charged N may be part of a heterocyclic radial (NH.sub.4.sup.+ is excepted); phosphonium ion substituted fourfold by alkyl, (substituted) phenyl or (substituted) benzyl; sulfonium- or sulfoxonium ion substituted threefold by alkyl, (substituted) phenyl or (substituted) benzyl; the guanidinium ion or an O-alkylisourea cation;R.sup.1, R.sup.2 independently of each other are alkyl;R.sup.3 is alkyl, alkoxy or halogen; andn is 0, 1, 2 or 3.
    Type: Grant
    Filed: November 21, 1985
    Date of Patent: October 4, 1988
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Roland Schmierer, Ernst-Friedrich Schulze, Helmut Bustell, Erwin Hacker
  • Patent number: 4772309
    Abstract: A 5-Acylamino-pyrazole derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen or nitro,R.sup.2 represents hydrogen, alkyl, alkenyl, alkinyl or optionally substituted cycloalkyl,R.sup.3 represents hydrogen or alkyl,R.sup.4 represents hydrogen or alkyl,X represents oxygen or sulphur,n represents the integer 0, 1 or 2,Ar represents in each case optionally substituted phenyl or pyridyl andHet represents an optionally substituted 5- or 6- membered heterocyclic radical linked via a carbon atom,which exhibit herbicidal and plant growth regulating activity.
    Type: Grant
    Filed: March 19, 1987
    Date of Patent: September 20, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Jorg Stetter, Reinhold Gehring, Otto Schallner, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
  • Patent number: 4771048
    Abstract: The present invention relates to the use of thiadiazinones of the formula I ##STR1## in which R represents the radical of the formula ##STR2## wherein X.sup.1 represents O or S,R.sup.4 represents hydrogen or alkyl,R.sup.5 represents optionally substituted phenyl,R.sup.2 represents hydrogen, alkyl, cycloalkyl, aryl or aralkylfor combating endoparasites in veterinary medicine and to new thiadiazinones of the formula I and the preparation thereof.
    Type: Grant
    Filed: June 25, 1987
    Date of Patent: September 13, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Nikolaus Muller, Peter Andrews
  • Patent number: 4762550
    Abstract: This invention relates to novel pyrazolesulfonamides, agricultural compositions thereof and the methods of their use as general and/or selective herbicides and/or plant growth regulants.
    Type: Grant
    Filed: August 13, 1987
    Date of Patent: August 9, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Stephen L. Hartzell
  • Patent number: 4759790
    Abstract: This invention relates to herbicidally active sulfonamide compounds having a heterocyclic carbonyl group ortho to the sulfonyl bridge.
    Type: Grant
    Filed: May 21, 1987
    Date of Patent: July 26, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Joel R. Christensen
  • Patent number: 4740231
    Abstract: 1-Aryl-5-alkoximinoalkylamino-pyrazoles of the formula ##STR1## in which R represents cyano or nitro, or represents an optionally substituted heterocyclic radical,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl, or represents optionally substituted aryl,R.sup.3 represents hydrogen, alkyl or alkenyl, or represents in each case optionally substituted aralkyl or aryl andAr represents optionally substituted phenyl or pyridyl,are active as herbicides and plant growth regulants. Compounds of the formula ##STR2## in which R" has the same definition as R other than cyano, are also active and useful as intermediates as well.
    Type: Grant
    Filed: May 22, 1986
    Date of Patent: April 26, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhold Gehring, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
  • Patent number: 4737184
    Abstract: Novel N-(heterocyclicaminocarbonyl) substituted thiophene-, furan- and pyrrolesulfonamides, such as N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno- [3,2-b]thiopyran-3-sulfonamide, 4,4-dioxide and N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno[3,2-b ]thiopyran-3-sulfonamide, 4,4-dioxide and their method-of-use as herbicides are described.
    Type: Grant
    Filed: May 10, 1985
    Date of Patent: April 12, 1988
    Assignee: E. I. Du Pont De Nemours and Company
    Inventor: Robert J. Pasteris
  • Patent number: 4737497
    Abstract: Disclosed are novel bis-dioxopiperazine derivatives, process for their preparation, antitumor agents comprising them and compositions containing them.The bis-dioxopiperazine derivatives are represented by the following general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms; R.sub.2 represents a hydrogen atom or a group of ##STR2## R.sub.3 and R.sub.4, which are respectively independent and are the same or different, represent respectively a lower alkyl group having 1 to 4 carbon atoms, a cycloalkyl group having 3 to 7 carbon atoms or a heterocyclic radical selected from the group consisting of substituted or unsubstituted piperidino, substituted or unsubstituted piperazino, substituted or unsubstituted morpholino and substituted or unsubstituted thiomorpholino, or R.sub.3 and R.sub.
    Type: Grant
    Filed: April 4, 1984
    Date of Patent: April 12, 1988
    Assignee: Zenyaki Kogyo Kabushiki Kaisha
    Inventor: Yun-feng Ren
  • Patent number: 4737500
    Abstract: Thiazoles or pharmaceutically acceptable acid addition salts thereof are useful as anxiolytic, psychogeriatric, antidepressant and antischizophrenic agents.
    Type: Grant
    Filed: June 20, 1986
    Date of Patent: April 12, 1988
    Assignee: Sandoz Pharm. Corp.
    Inventor: Dieter Sorg
  • Patent number: 4725305
    Abstract: Herbicidally active novel N,N'-bis-sulphonyl guanidines of the formula ##STR1## in which M is hydrogen, a metal or an ammonium radical, andR.sup.4, R.sup.5, R.sup.40 and R.sup.41 are various organic radicals.
    Type: Grant
    Filed: November 14, 1986
    Date of Patent: February 16, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Koichi Moriya, Theodor Pfister, Hans-Jochem Riebel, Ludwig Eue, Robert R. Schmidt, Klaus Lurssen, Hans-Joachim Diehr, Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Uwe Priesnitz, Wolfgang Roy, Hans-Joachim Santel
  • Patent number: 4723988
    Abstract: Thiophenesulfonamides such as N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-3-(isoxazol-3-yl)-2-thiophen esulfonamide are useful as herbicides and plant growth regulants.
    Type: Grant
    Filed: March 27, 1987
    Date of Patent: February 9, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Rafael Shapiro
  • Patent number: 4716164
    Abstract: Heterocyclic compounds of the formula: ##STR1## wherein A is a direct link, or is alkylene of 1 to 4 carbon atoms or alkenylene of 2 to 4 carbon atoms; wherein either X is --CR.sup.1 R.sup.2 -- and Y is --O--, --S-- or --NR.sup.3 --, wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each is hydrogen or alkyl of up to 4 carbon atoms; or X is --O--, --S-- or --NH-- and Y is --CR.sup.1 R.sup.2 -- wherein R.sup.1 and R.sup.2 have the meanings stated above; and wherein Het is a 5- or 5- membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from nitrogen, oxygen or sulphur atoms, which ring may be unsubstituted or may bear one or two substituents as set out in claim 1, provided that when X is --CR.sup.1 R.sup.2 -- and A is a direct link, Het is not unsubstituted 2-furyl; and salts thereof where appropriate; processes for their manufacture and pharmaceutical compositions containing them. The compounds possess cardiotonic and/or antihypertensive activity.
    Type: Grant
    Filed: October 31, 1985
    Date of Patent: December 29, 1987
    Assignee: Imperial Chemical Industries PLC
    Inventors: Rodney B. Hargreaves, Bernard J. McLoughlin, Stuart D. Mills
  • Patent number: 4713381
    Abstract: An oxodiazine compound of the formula: ##STR1## or a pharamceutically acceptable acid addition salt thereof, wherein each of R.sup.1 and R.sup.2 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxy-C.sub.1-4 alkoxy, phenyl-C.sub.1-4 alkyl-oxy which may be optionally substituted by at least one substituent selected from the group consisting of halogen, C.sub.1-4 alkyl and C.sub.1-4 alkoxy on the phenyl nucleus, or phenyl which may be substituted by at least one substituent selected from the group consisting of halogen, C.sub.1-4 alkyl and C.sub.1-4 alkoxy on the phenyl nucleus; X is --S--, --CH.dbd.N-- or --C(R.sup.3).dbd.C(R.sup.4)--, where each of R.sup.3 and R.sup.4 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxy-C.sub.1-4 alkoxy or phenyl-C.sub.1-4 alkyl-oxy which may be optionally substituted by at least one substituent selected from the group consisting of halogen, C.sub.1-4 alkyl and C.sub.
    Type: Grant
    Filed: May 27, 1986
    Date of Patent: December 15, 1987
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Hideki Ao, Minoru Obata, Tsutomu Yamanaka, Hiroshi Mikashima
  • Patent number: 4713456
    Abstract: A process for the preparation of a 5-acylpyrimidine of the formula ##STR1## in which R is an organic radical comprising reacting a methyl ketone of the formulaR--CO--CH.sub.3in a first stage with a formylating reagent in the presence of a base to form an enolketone of the formulaR--CO--CH.dbd.CH--OR.sup.10in which R.sup.10 represents hydrogen or a base radical, thereafter reacting the enolketone in 2nd and 3rd stages with formamidine or a formamidine salt, and with an amino-formylating agent, and, in a 4th stage heating to cyclize the compound formed.The end products, some of which are new, are intermediates for making herbicides.
    Type: Grant
    Filed: August 26, 1985
    Date of Patent: December 15, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Ludwig Elbe, Graham Holmwood
  • Patent number: 4709027
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or lower alkyl, or R.sup.1 and R.sup.2 taken together represent ##STR2## A is O or NR.sup.3 ; B is --(CH.sub.2).sub.n --, ##STR3## R.sup.3 is hydrogen or lower alkyl; R.sup.4 is hydrogen, lower alkyl, aryl of 6-12 carbon atoms or halo;R.sup.5 is unsubstituted or substituted phenyl, 2-pyridinyl, 2-pyrimidinyl, 2-pyrazinyl or 3-pyridazinyl, where the substituents are selected from the group lower alkyl, lower alkoxy, halo, cyano, nitro and trifluoromethyl;Z is --(CH.sub.2).sub.n -- or vinylene;X is lower alkylene, vinylene or O;m is 2-5;n is 1-3;o is 1-5;and the pharmaceutically acceptable salts thereof and their use as antipsychotic/anxiolytic agents having a low liability for extrapyramidal side effects.
    Type: Grant
    Filed: June 25, 1986
    Date of Patent: November 24, 1987
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Guy A. Schiehser
  • Patent number: 4689414
    Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3 or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;R.sub.5 is hydrogen, alkyl, aryl, arylalkyl, cyano, nitro, ##STR2## Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl-(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl-(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR3## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR4## amino, or substituted amino; m is 0 or an integer of 1 to 6;n is an integer of 1 to 6; andp is an integer of 2 to 6.
    Type: Grant
    Filed: February 24, 1986
    Date of Patent: August 25, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4684656
    Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur;R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR2## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR3## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.
    Type: Grant
    Filed: March 14, 1986
    Date of Patent: August 4, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4683228
    Abstract: A guanidine derivative of the formula I: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, ring X and D are a variety of radicals defined in the specification and A is a 3-8C alkylene chain which is substituted by a hydroxy radical and into which is optionally inserted, as part of the backbone of the chain, one or two groups selected from oxygen and sulphur atoms and NH and 1-6C N-alkyl radicals; and the pharmaceutically-acceptable acid additions salts thereof. Pharmaceutical compositions and methods of manufacture are also described. The compound of the formula I is a histamine H-2 antagonist and is therefore useful in ulcer therapy.
    Type: Grant
    Filed: January 22, 1985
    Date of Patent: July 28, 1987
    Assignees: ICI Americas Inc., Imperial Chemical Industries PLC
    Inventors: Karin M. Kirkland, Derrick M. Mant
  • Patent number: 4678785
    Abstract: A thiadiazine compound of the formula: ##STR1## a method for preparing said compound and a pharmaceutical composition containing said compound, wherein X is methylene which may be optionally substituted by an alkyl of up to 3 carbon atoms; R is hydrogen atom or methyl group; and n is an integer of 1 or 2.Since the compounds exhibit potent cardiotonic and coronary vasodilator activities and further inhibitory activity on platelet aggregation, they are useful as cardiotonic and antithrombotic drugs.
    Type: Grant
    Filed: October 29, 1985
    Date of Patent: July 7, 1987
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Hideki Ao, Minoru Obata, Jun Inui
  • Patent number: 4668279
    Abstract: Novel pyridinesulfonamide compounds containing ortho-heterocyclic substituents such as N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-2-(1H-1,2,4-triazol-1-yl)-3 -pyridinesulfonamide display utility as herbicides and plant growth regulants.
    Type: Grant
    Filed: April 22, 1985
    Date of Patent: May 26, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Morris P. Rorer
  • Patent number: 4665177
    Abstract: This invention relates to new tetrahydropyrimidines, to a process for their production and to their use as catalysts in the production of polyurethane plastics, including polyurethane foams.
    Type: Grant
    Filed: August 5, 1985
    Date of Patent: May 12, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Werner Rasshofer, Gerhard Grogler, Richard Kopp
  • Patent number: 4654338
    Abstract: Novel 1,2,4-thiadiazines of the formula ##STR1## wherein R.sub.3 is selected from the group consisting of hydrogen, --OH, --CF.sub.3, alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms optionally substituted with alkyl of 1 to 6 carbon atoms and ##STR2## R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms or taken together with the nitrogen to which they are attached form a saturated heterocycle of 4 to 8 carbon atoms optionally containing a heteroatom of the group consisting of --O--, --S-- and ##STR3## and R' is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.5 is ##STR4## R.sub.4 is selected from the group consisting of hydrogen, halogen and alkyl and alkoxy of 1 to 3 carbon atoms, R.sub.6 is selected from the group consisting of hydrogen, halogen and alkyl of 1 to 3 carbon atoms with the proviso that R.sub.6 may represent halogen only when R.sub.
    Type: Grant
    Filed: March 26, 1985
    Date of Patent: March 31, 1987
    Assignee: Roussel Ulcaf
    Inventors: Stuart D. Jones, Wilfred R. Tully, Peter D. Kennewell
  • Patent number: 4640926
    Abstract: 3,5-Substituted-2-pyridylalkylaminothiadiazole compounds are disclosed which are useful as histamine H.sub.1 -antagonists.
    Type: Grant
    Filed: May 17, 1985
    Date of Patent: February 3, 1987
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: George S. Sach
  • Patent number: 4639444
    Abstract: A compound of the formula: ##STR1## wherein R is methyl or ethyl, X is hydrogen (provided R is ethyl), lower alkyl, lower alkoxy, lower alkylthio, fluorine, bromine, phenoxy or substituted phenoxy, X.sub.m is methylenedioxy or --CH.dbd.CH--CH.dbd.CH--, and m is 1, 2 or 3.
    Type: Grant
    Filed: November 20, 1985
    Date of Patent: January 27, 1987
    Assignee: Nissan Chemical Industries Ltd.
    Inventors: Yoshihiro Fujikawa, Mitsuaki Sakashita, Nobutomo Tsuruzoe
  • Patent number: 4634689
    Abstract: Phosphinylalkanoyl imino acids useful in the treatment of hypertension are disclosed.
    Type: Grant
    Filed: October 31, 1985
    Date of Patent: January 6, 1987
    Assignee: Schering Corporation
    Inventors: Joseph T. Witkowski, Michael F. Czarniecki
  • Patent number: 4629495
    Abstract: Herbicidal compounds of the formula: ##STR1## wherein A represents R.sup.1 R.sup.2 N-- (wherein R.sup.1 represents C.sub.1-8 alkyl or C.sub.2-8 alkenyl or alkynyl unsubstituted or substituted by CN, OH, C.sub.1-6 alkoxy, carboxy, C.sub.2-9 alkoxycarbonyl, aminocarbonyl optionally substituted by C.sub.1-8 alkyl or C.sub.2-8 alkenyl, C.sub.1-8 alkoxyaminocarbonyl, C.sub.1-8 alkanesulphonamidocarbonyl, --C(.dbd.O)Het, where Het represents a nitrogen-containing heterocyclic group, or one or more halogen atoms or R.sup.1 represents C.sub.3-6 cycloalkyl optionally substituted by C.sub.1-4 alkyl and R.sup.2 represents H or R.sup.1, or R.sup.1 represents C.sub.1-4 alkylthio and R.sup.2 represents H, or A represents R.sup.p (R.sup.q)--C.dbd.N-- (wherein R.sup.p represents C.sub.1-4 alkoxy or amino substituted by one or two C.sub.1-4 alkyl groups and R.sup.q represents H or C.sub.1-4 alkyl) or A represents 2-oxo-azetidin-1-yl, 2-oxo-pyrrolidin-1-yl or 2-oxo-piperidin-1-yl optionally substituted by C.sub.
    Type: Grant
    Filed: July 13, 1983
    Date of Patent: December 16, 1986
    Assignee: May & Baker Limited
    Inventors: Leslie R. Hatton, Edgar W. Parnell, David A. Roberts
  • Patent number: 4624950
    Abstract: 3,5-Dimethyl-4,6-diphenyl-tetrahydro-2H-1,3,5-thiadiazine-2-thione having the formula: ##STR1## as an antiatherosclerotic agent.
    Type: Grant
    Filed: August 13, 1984
    Date of Patent: November 25, 1986
    Assignee: Nissan Chemical Industries Ltd.
    Inventors: Tadashi Sasaki, Yoshihiro Fujikawa, Ryozo Sakoda, Mitsuaki Sakashita, Morihide Hibi
  • Patent number: 4587246
    Abstract: Novel heterocyclic compounds of the formula: ##STR1## wherein either X is --CR.sup.1 R.sup.2 -- and Y is oxygen, sulphur or --NR.sup.3 --, wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each is hydrogen or alkyl of up to 4 carbon atoms; or X is oxygen, sulphur or --NH-- and Y is --CH.sub.2 --; wherein R.sup.4 and R.sup.5, which may be the same or different, each is hydrogen, cyano, nitro, amino or hydroxy, or alkylthio of up to 4 carbon atoms, or has various other meanings defined in claim 1, provided that R.sup.4 and R.sup.5 are not both hydrogen; or wherein R.sup.4 and R.sup.5 are joined together such that with the benzene ring A they form a benzheterocyclic ring as defined in claim 1; and therein the benzene ring A may optionally bear one or more further substituents; or a salt thereof where appropriate.
    Type: Grant
    Filed: November 28, 1984
    Date of Patent: May 6, 1986
    Assignee: Imperial Chemical Industries PLC
    Inventors: David Brown, Robert I. Dowell, Rodney B. Hargreaves, Brian G. Main
  • Patent number: 4584285
    Abstract: (Benzothiadiazine, benzamido and benzenesulfonyl)phenyl-substituted carboxyalkyl dipeptide compounds are disclosed. Compounds of this invention are useful as antihypertensive agents.
    Type: Grant
    Filed: September 17, 1984
    Date of Patent: April 22, 1986
    Assignee: Schering Corporation
    Inventors: Ronald J. Doll, Bernard R. Neustadt, Elizabeth M. Smith, Charles V. Magatti, Elijah H. Gold
  • Patent number: 4578459
    Abstract: Heterocyclic compounds which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A specific compound of this invention is 2-[2-(4-methyl-5-imidazolylmethylthio)ethylamino]-4-pyrimidone.
    Type: Grant
    Filed: June 8, 1984
    Date of Patent: March 25, 1986
    Assignee: SmithKline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Patent number: 4568672
    Abstract: 3,6-Disubstituted 2-thioxo-1,3,5-thiadiazin-4-ones of the formula ##STR1## in which R.sup.1 represents hydrogen; alkyl which is optionally monosubstituted or polysubstituted by identical or different substituents; alkenyl which is optionally monosubstituted or polysubstituted by identical or different substituents; alkinyl which is optionally monosubstituted or polysubstituted; cycloalkenyl or cycloalkyl which is optionally monosubstituted or polysubstituted by identical or different substituents; aryl or aralkyl which is optionally monosubstituted or polysubstituted by identical or different substituents; or a heterocyclic structure which is monosubstituted or polysubstituted by identical or different substituents;R.sup.
    Type: Grant
    Filed: August 27, 1984
    Date of Patent: February 4, 1986
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wilhelm Brandes, Rolf Bunnenberg, Gerd Hanssler, Paul Reinecke, Karlfried Wedemeyer
  • Patent number: 4563452
    Abstract: This invention relates to new derivatives of oxazinobenzothiazine-6,6-dioxide, to a process for the production thereof and to the use thereof as medicaments.The new derivatives according to the present invention correspond to the general formula I: ##STR1## wherein: R represents a linear or branched lower C.sub.1 -C.sub.4 alkyl radical, in particular the methyl and ethyl radicals,X represents an oxygen atom or a sulphur atom, andHet represents a mono- or bicyclic unsaturated heterocycle containing a nitrogen heteroatom in the ortho position relative to the link between the said heterocycle and the nitrogen atom of the oxazine ring, the said heterocycle optionally containing one or two other additional heteroatoms selected from nitrogen, oxygen and sulphur, and also being able to be substituted by one or two methyl radicals.
    Type: Grant
    Filed: June 8, 1983
    Date of Patent: January 7, 1986
    Assignee: Provesan S.A.
    Inventor: Jose Esteve Soler
  • Patent number: 4558045
    Abstract: Heterocyclic compounds of the formula: ##STR1## wherein A is a direct link, or is alkylene of 1 to 4 carbon atoms or alkenylene of 2 to 4 carbon atoms; wherein either X is --CR.sup.1 R.sup.2 -- and Y is --O--, --S-- or --NR.sup.3 --, wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each is hydrogen or alkyl of up to 4 carbon atoms;or X is --O--, --S-- or --NH-- and Y is --CR.sup.1 R.sup.2 -- wherein R.sup.1 and R.sup.2 have the meanings stated above;and wherein Het is a 5- or 6- membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from nitrogen, oxygen or sulphur atoms, which ring may be unsubstituted or may bear one or two substituents as set out in claim 1, provided that when X is --CR.sup.1 R.sup.2 -- and A is a direct link, Het is not unsubstituted 2-furyl; and salts thereof where appropriate; processes for their manufacture and pharmaceutical compositions containing them. The compounds possess cardiotonic and/or antihypertensive activity.
    Type: Grant
    Filed: October 12, 1984
    Date of Patent: December 10, 1985
    Assignee: Imperial Chemical Industries, PLC
    Inventors: Rodney B. Hargreaves, Bernard J. McLoughlin, Stuart D. Mills
  • Patent number: 4555261
    Abstract: This invention relates to a novel class of sulfonamides and their use as herbicides and plant growth regulants.
    Type: Grant
    Filed: November 1, 1984
    Date of Patent: November 26, 1985
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Wallace C. Petersen
  • Patent number: 4544742
    Abstract: 1,2,6-Thiadiazine-3,5-dione-1,1-dioxides of the general formula ##STR1## wherein each R and R.sub.3 independently may be substituted or unsubstituted alkyl, alkenyl or substituted cycloalkyl are described. These compounds, as well as those wherein the R substituents additionally may be cycloalkyl or substituted or unsubstituted aryl, are useful as accelerators for the peroxidic polymerization of ethylenically unsaturated compounds, such as methacrylic acid compounds, and have particular utility in dental compositions.
    Type: Grant
    Filed: February 28, 1984
    Date of Patent: October 1, 1985
    Inventors: Werner Schmitt, Robert Purrmann, Peter Jochum, Heinz-Joachim Hubner, Bernd Burger
  • Patent number: 4542132
    Abstract: A series of novel 4-piperidino-6,7-dimethoxyquinazoline compounds, further substituted on the piperidino group, and the pharmaceutically-acceptable salts thereof, possess cardiac stimulating activity in mammals. They are useful in the curative or prophylactic treatment of cardiac conditions, in particular heart failure.
    Type: Grant
    Filed: July 31, 1984
    Date of Patent: September 17, 1985
    Assignee: Pfizer Inc.
    Inventors: Simon F. Campbell, Albert A. Jaxa-Chamiec, David A. Roberts
  • Patent number: 4532252
    Abstract: 3,5-Substituted-2-pyridylalkylamino derivatives are disclosed which are useful as histamine H.sub.1 -antagonists.
    Type: Grant
    Filed: December 9, 1983
    Date of Patent: July 30, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: George S. Sach
  • Patent number: 4497807
    Abstract: Thiadiazinones, such as 3-chloro-5-phenylthio-4H-1,2,6-thiadiazin-4-one, useful for control of certain fungus plant diseases such as scab of apple, late blight of tomato and downy mildew of grape.
    Type: Grant
    Filed: March 31, 1978
    Date of Patent: February 5, 1985
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Robert C. Portnoy
  • Patent number: 4496563
    Abstract: Thiadiazinones of the formula ##STR1## where R.sup.1 and R.sup.2 are identical or different and are each hydrogen, alkyl, cycloalkyl, phenyl or substituted aryl and R.sup.3 is phenyl or haloalkyl-substituted, alkyl-substituted, alkoxy-substituted or haloalkoxy-substituted or alkyl- or halo-substituted phenyl, are used in fungicides.
    Type: Grant
    Filed: August 18, 1983
    Date of Patent: January 29, 1985
    Assignee: BASF Aktiengesellschaft
    Inventors: Rolf-Dieter Acker, Eberhard Ammermann, Ernst-Heinrich Pommer
  • Patent number: 4493835
    Abstract: Heterocyclic compounds of the formula: ##STR1## wherein either X is --CR.sup.1 R.sup.2 -- and Y is --O--, --S-- or--NHR.sup.3 --, wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each is hydrogen or alkyl of up to 4 carbon atoms;or X is --O--, --S-- or --NH-- and Y is --CR.sup.1 R.sup.2 -- wherein R.sup.1 and R.sup.2 have the meanings stated above; wherein R.sup.4 and R.sup.5, which may be the same or different, each is hydrogen (but provided that R.sup.4 and R.sup.5 are not both hydrogen), or each is a group defined in claim 1 which is readily convertible into a carboxy group; processes for their manufacture; and pharmaceutical compositions containing them. The compounds possess cardiotonic and/or antihypertensive activity.
    Type: Grant
    Filed: October 26, 1982
    Date of Patent: January 15, 1985
    Assignee: Imperial Chemical Industries PLC
    Inventors: Rodney B. Hargreaves, Bernard J. McLoughlin
  • Patent number: 4489074
    Abstract: Heterocyclic compounds of the formula ##STR1## wherein either X is --CR.sup.1 R.sup.2 and Y is --O--, --S-- or --NR.sup.3 --, wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each is hydrogen or alkyl of up to 4 carbon atoms;or X is --O--, --S-- or --NH-- and Y is --CR.sup.1 R.sup.2 -- wherein R.sup.1 and R.sup.2 have the meanings stated above;wherein either R.sup.4 is hydrogen, fluoro or chloro, or alkyl, alkenyl, halogenoalkyl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or alkoxy each of up to 6 carbon atom, and R.sup.5, R.sup.6 and R.sup.7, which may be the same or different, each is hydrogen, fluoro, chloro, bromo or iodo, or alkyl, alkenyl, halogenoalkyl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or alkoxy each of up to 6 carbon atoms, provided that R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are not all hydrogen;or R.sup.4 is bromo and R.sup.5, R.sup.6 and R.sup.7 have the meanings stated above, provided that R.sup.5, R.sup.6 and R.sup.7 are not all hydrogen;or R.sup.4 and R.sup.
    Type: Grant
    Filed: November 12, 1982
    Date of Patent: December 18, 1984
    Assignee: Imperial Chemical Industries, PLC
    Inventors: David Brown, Rodney B. Hargreaves, Bernard J. McLoughlin, Stuart D. Mills
  • Patent number: 4489075
    Abstract: 6,7-Dialkoxy-4-[4-(cyclic-sulfonamidoalkyl)piperidino]quinazolines and method of use as cardiac stimulants.
    Type: Grant
    Filed: April 27, 1983
    Date of Patent: December 18, 1984
    Assignee: Pfizer Inc.
    Inventors: Simon F. Campbell, David A. Roberts, John K. Stubbs
  • Patent number: 4489073
    Abstract: Heterocyclic compounds of the formula: ##STR1## wherein A is a direct link, or is alkylene of 1 to 4 carbon atoms or alkenylene of 2 to 4 carbon atoms; wherein either X is --CR.sup.1 R.sup.2 -- and Y is --O--, --S-- or --NR.sup.3 --, wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each is hydrogen or alkyl of up to 4 carbon atoms;or X is --O--, --S-- or --NH-- and Y is --CR.sup.1 R.sup.2 -- wherein R.sup.1 and R.sup.2 have the meanings stated above;and wherein Het is a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from nitrogen, oxygen or sulphur atoms, which ring may be unsubstituted or may bear one or two substituents as set out in claim 1, provided that when X is --CR.sup.1 R.sup.2 -- and A is a direct link, Het is not unsubstituted 2-furyl; and salts thereof where appropriate; processes for their manufacture and pharmaceutical compositions containing them. The compounds possess cardiotonic and/or antihypertensive activity.
    Type: Grant
    Filed: November 3, 1982
    Date of Patent: December 18, 1984
    Assignee: Imperial Chemical Industries, PLC
    Inventors: Rodney B. Hargreaves, Bernard J. McLoughlin, Stuart D. Mills
  • Patent number: 4456565
    Abstract: Acyl cyanides of the general formula ##STR1## in which R represents alkyl or substituted alkyl of from 1 to 8 carbon atoms; cycloalkyl or substituted cycloalkyl with 3 to 12 carbon atoms; aryl or substituted aryl; or an optionally substituted 5-membered or 6-membered heterocyclic radical which can additionally also be fused with a benzene ring, are prepared by reacting the corresponding carboxylic acid anhydride in the liquid phase with anhydrous hydrocyanic acid, at a temperature of between 50.degree. to 250.degree. C.
    Type: Grant
    Filed: July 14, 1983
    Date of Patent: June 26, 1984
    Assignee: Bayer Aktiengesellschaft
    Inventors: Kurt Findeisen, Herbert Schwarz
  • Patent number: 4452795
    Abstract: The invention relates to novel substituted 5-phenoxyphenyl-tetrahydro-1,3,5-thiadiazin-4-ones of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, trifluoromethyl, methoxy, ethoxy, benzyl, phenoxy, phenylthio, or phenoxy or phenylthio substituted by a radical selected from the group consisting of halogen, C.sub.1 -C.sub.4 -alkyl, methoxy and ethoxy; each of R.sub.2 and R.sub.3 independently of the other is hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, trifluoromethyl, methoxy or ethoxy; each of R.sub.4 and R.sub.5 independently of the other is hydrogen or C.sub.1 -C.sub.6 -alkyl; and each of R.sub.6 and R.sub.7 independently of the other is C.sub.1 -C.sub.4 -alkyl, trifluoromethyl, C.sub.3 -C.sub.6 -cycloalkyl, alkoxyalkyl containing a total of 2 to 6 carbon atoms, benzyl, phenyl or phenyl which is substituted by a member selected from the group consisting of halogen, C.sub.1 -C.sub.
    Type: Grant
    Filed: August 26, 1982
    Date of Patent: June 5, 1984
    Assignee: Ciba-Geigy Corporation
    Inventors: Saleem Farooq, Hans-Peter Streibert
  • Patent number: 4450269
    Abstract: Selected mono-5-substituted-3-chloro-4H-1,2,6 thiadiazin-4-ones having the general formula ##STR1## are described which are useful for control of fungal disease in plants.
    Type: Grant
    Filed: December 18, 1980
    Date of Patent: May 22, 1984
    Assignee: FMC Corporation
    Inventors: Clinton J. Peake, Wayne N. Harnish, Bruce L. Davidson
  • Patent number: 4436549
    Abstract: N-(1,3,4-Thiadiazin-2-yl)-2,6-dialkoxybenzamide derivatives useful as herbicides.
    Type: Grant
    Filed: October 28, 1982
    Date of Patent: March 13, 1984
    Assignee: Eli Lilly and Company
    Inventor: Thomas D. Thibault