Additional Hetero Ring Containing Patents (Class 544/96)
  • Patent number: 4785016
    Abstract: Indole derivatives are disclosed of formula (I): ##STR1## wherein R.sub.1 represents H, alkyl or alkenyl;R.sub.2 represents H, alkyl, alkenyl, cycloalkyl or phenyl or phenyl alkyl the phenyl ring being optionally substituted by halogen, alkyl, alkoxy, hydroxyl or by a group --NR.sub.a R.sub.b, or --CONR.sub.a R.sub.b, wherein R.sub.a and R.sub.b are H, alkyl, alkenyl, or with the nitrogen atom form a saturated monocyclic ring;R.sub.3 and R.sub.4 are H, alkyl or propenyl or together form an aralkylidene group;Alk represents a Cf.sub.2-3 alkyl chain optionally substituted by one or two alkyl groups; andA.sup.1 represents a C.sub.2-5 alkenyl chain and salts and solvates thereof.The compounds have selective vasoconstrictor activity and are useful in treating and/or preventing pain resulting from dilatation of the cranial vasculature, particularly migraine. The compounds may be formulated in conventional manner with pharmaceutically acceptable carriers or excipients.
    Type: Grant
    Filed: December 3, 1985
    Date of Patent: November 15, 1988
    Assignee: Glaxo Group Limited
    Inventors: Brian Evans, Alexander W. Oxford, Darko Butain
  • 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: 4772706
    Abstract: An improved process for the preparation of 7-substituted amino-1-alkyl- or cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids is described where tetrafluorobenzoyl chloride is converted in three operations via 1-alkyl or 1-cycloalkyl-1,4-dihydro-6,7,8-trifluoro-4-oxoquinoline-3-carbonitrile which in a separate step or in situ is displaced and hydrolyzed to the desired product.
    Type: Grant
    Filed: January 13, 1986
    Date of Patent: September 20, 1988
    Assignee: Warner-Lambert Company
    Inventors: James N. Wemple, James R. Zeller, John M. Domagala
  • 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: 4767443
    Abstract: There are described novel, microbicidally active 5-(arylmethylimino)-pyrimidines of the formula I ##STR1## wherein R.sub.n --A-- is an unsubstituted or substituted phenyl, naphthyl, biphenyl, phenoxyphenyl or phenylthiophenyl, and R.sub.1 is an ether, thioether or amino function, these substances being produced according to the invention by substitution of the halogen atom in the claimed intermediates of the formula II ##STR2## The use of these substances in plant protection, and also further important intermediates, are likewise described.
    Type: Grant
    Filed: September 13, 1985
    Date of Patent: August 30, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Helmut Zondler, Wolfgang Eckhardt, Robert Nyfeler
  • 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: 4755599
    Abstract: The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl,either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl,or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and(i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6 C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.
    Type: Grant
    Filed: February 3, 1987
    Date of Patent: July 5, 1988
    Assignee: Rhone-Poulenc Sante
    Inventors: Jean-Claude Barriere, Jean-Pierre Corbet, Claude Cotrel, Daniel Farge, Jean-Marc Paris
  • Patent number: 4743294
    Abstract: A selective herbicide of the formula ##STR1## in which m is 0, 1 or 2,R.sup.5 is an organic radical,R.sup.3 is hydrogen or an organic radical,R.sup.9 is hydrogen or an optionally substituted alkyl radical,R.sup.10 is an organic radical or forms a ring with R.sup.9,R.sup.40 and R.sup.41 are alkyl or alkoxy, andM is hydrogen or a metal or ammonium radical, or an acid adduct thereof.
    Type: Grant
    Filed: April 22, 1987
    Date of Patent: May 10, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Joachim Diehr, Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Theodor Pfister, Uwe Priesnitz, Hans-Jochem Riebel, Wolfgang Roy, Hans-Joachim Santel, Robert R. Schmidt, Koichi Moriya, Ludwig Eue, Klaus Lurssen
  • 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: 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: 4735942
    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: June 2, 1986
    Date of Patent: April 5, 1988
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jan Heeres, Raymond A. Stokbroekx, Leo J. J. Backx
  • Patent number: 4732898
    Abstract: The present invention are 2-(2-aryl-2-oxo-alkylidene) analogs of 1,2,3,4-tetrahydropyridine-3,5-pyridinecarboxylic acids and particularly esters thereof having valuable calcium antagonist and positive inotropic activity useful in the treatment of cardiovascular disorders, pharmaceutical compositions and methods of use therefor.
    Type: Grant
    Filed: March 3, 1987
    Date of Patent: March 22, 1988
    Assignee: Warner-Lambert Company
    Inventors: Edward W. Badger, Michael D. Taylor
  • Patent number: 4725679
    Abstract: The novel 2-amino-alkenylsulfonylureas of the formula (I) ##STR1## in which R.sub.1 and R.sub.2 denote hydrogen, alkyl, cycloalkyl or (substituted) phenyl, or R.sub.1 and R.sub.2, together with the common nitrogen atom, form a 5-membered to 7-membered (hetero)aliphatic ring, R.sub.3 denotes hydrogen, cycloalkyl, alkyl, alk(en)(yn)yloxy, alkylsulfen(in)(on)yl, --SO.sub.2 (N)(mono- or di-alkyl), (substituted) phenyl, benzyl, substituted hydroxycarbonyl or (substituted) aminocarbonyl, R.sub.4 has the meaning of R.sub.3 and additionally denote formyl, alkanoyl, (substituted) benzoyl, cycloalkylcarbonyl or C.sub.6 H.sub.5 --CH.sub.2 --O--CO--, or R.sub.3 and R.sub.4, together with the olefinic carbon atoms connecting them, form a 5-membered to 8-membered aliphatic ring system, R.sub.5 denotes H, alkyl, alkenyl, alkynyl, alkoxy or alkoxycarbonyl and R.sub.
    Type: Grant
    Filed: February 7, 1986
    Date of Patent: February 16, 1988
    Assignee: Hoechst Aktiengesellschaft
    Inventor: Lothar Willms
  • 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: 4715984
    Abstract: Dihydroazines of the formula IR.sub.1 --A.sup.1 --Z.sub.1 --A.sub.2 --R.sup.2 Iwherein R.sup.1, R.sup.2, A.sup.1, A.sup.2 and Z.sub.1 have the meanings specified herein may be used as components of liquid crystalline phases.
    Type: Grant
    Filed: January 22, 1986
    Date of Patent: December 29, 1987
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Joachim Krause, Wachtler, Bernhard Scheuble
  • 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: 4710500
    Abstract: The present invention relates to novel indole derivatives which have interesting pharmacodynamic effects indicating pronounced activity in the treatment of psychic disorders, especially psychoses and, at the same time, a low degree of undesired side effects.Moreover, the invention relates to methods for the preparation of said indole derivatives, pharmaceutical compositions containing same, and methods for the treatment of psychic disorders, especially psychoses, by administering a therapeutically active amount of one of said derivatives to a living animal body, including human beings.The novel indole derivatives of the present invention are represented by the following formula: ##STR1## wherein R is phenyl, optionally substituted with halogen, lower alkyl or trifluoromethyl, or a hetero aromatic group, such as 2-thienyl, 3-thienyl, 2-furoyl, 3-furoyl, 2-thiazol, 2-oxazol, 2-imidazole, 2-pyridyl, 3-pyridyl or 4-pyridyl; R.sup.
    Type: Grant
    Filed: April 1, 1986
    Date of Patent: December 1, 1987
    Assignee: H. Lundbeck A/S
    Inventor: Jens K. Perregaard
  • Patent number: 4707479
    Abstract: 1,4-Dihyropyridinecarboxamides of the formula ##STR1## and salts thereof, are effective for treating cardiac insufficiency, thromboses, thromboembolisms and ischaemias, for influencing the blood-sugar level and the circulation and as coronary therapeutic agents and anti-arrhythmic agents.
    Type: Grant
    Filed: December 5, 1985
    Date of Patent: November 17, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Horst Meyer, Gerhard Franckowiak, Ulrich Rosentreter, Rainer Gross, Gunter Thomas, Matthias Schramm, Michael Kayser, Friedel Seuter, Elisabeth Perzborn, Martin Bechem
  • Patent number: 4699647
    Abstract: This invention relates to herbicidal benzene sulfonamides containing a five or six membered heterocyclic ring consisting of 2-3 heteroatoms and 1-2 carbonyl groups as a substituent on benzene.
    Type: Grant
    Filed: March 27, 1986
    Date of Patent: October 13, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Morris P. Rorer
  • Patent number: 4696927
    Abstract: This invention relates to 4-(2-pyrimidinyl)-1-piperazinyl heterocyclic carbonyl derivatives, to a process for their preparation, and to their use as anxiolytic agents.
    Type: Grant
    Filed: December 17, 1986
    Date of Patent: September 29, 1987
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Maurice W. Gittos, Marcel Hibert
  • 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: 4684650
    Abstract: The present invention relates to indane derivatives with the following formula: ##STR1## wherein R.sub.1 is H, Halogen, an alkyl group having from one to three carbon atoms inclusive, methoxy, a methylthio-group, or a trifluoromethyl group,n is 2-4X is O or S,Y is O, CH.sub.2 or N--R.sub.2, where R.sub.2 is hydrogen or an (1-6 C) alkyl, (2-6 C) alkenyl or cycloalkyl-methyl group having from three to six carbon atoms,Z is --(CH.sub.2).sub.n --, n is 2 or 3 or Z is 1,2-phenylene optionally substituted with halogen or trifluoromethyl or Z=1,2--C.sub.6 H.sub.4 CO-- (to form a quinazolidinone or -thione ring system). U=N or C.Each compound exists as geometric isomers and each of these as a pair of optical isomers; and the separation and isolation of these are also within the scope of the invention.Moreover, pharmaceutically acceptable acid addition salts of the compounds of Formula I are within the scope of the present invention.
    Type: Grant
    Filed: October 10, 1985
    Date of Patent: August 4, 1987
    Assignee: H. Lundbeck A/S
    Inventor: Klaus P. Bogeso
  • 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: 4672062
    Abstract: 3-amino-2,3-dihydro-1-benzoxepine compounds corresponding to the general Formula I ##STR1## wherein R.sub.1 and R.sub.2 may each be hydrogen, halogen, lower alkyl or lower alkoxy, or if one of R.sub.1 and R.sub.2 is hydrogen, the other may also be nitro or trifluoromethyl, R.sub.3 represents hydrogen or a lower alkyl group which optionally may be substituted by hydroxy, lower alnoxy, an optionally substituted phenyl group or an optionally substituted amino group, and R.sub.4 represents hydrogen or lower alkyl, or R.sub.3 and R.sub.4 together with the nitrogen atom form a 5 or 6 member heterocycle. The compounds exhibit pharmacological, especially antidepressive, activity.
    Type: Grant
    Filed: November 4, 1985
    Date of Patent: June 9, 1987
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Heinrich-Wilhelm Ohlendorf, Michael Ruhland, Klaus-Ullrich Wolf
  • Patent number: 4668690
    Abstract: This invention relates to 1,2,3,4,4a,9b-hexahydro-4a-aminoalkyldibenzofurans of the formula ##STR1## where X is hydrogen, loweralkyl, F and Cl; R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, loweralkenyl, loweralkoxyloweralkyl, aryloxyloweralkyl, cycloalkylloweralkyl and heteroarylloweralkyl: R.sub.2 is hydrogen, lower alkyl or R.sub.1 and R.sub.2 taken together with the N ring atom constitute a saturated or unsaturated heterocyclic ring having 5 or 6 members; R.sub.3 is hydrogen, lower alkyl; n is an interger of 1 to 3; and the pharmaceutically acceptable acid addition salts thereof and where applicable the stereo, optical and geometrical isomers of the foregoing.
    Type: Grant
    Filed: December 30, 1985
    Date of Patent: May 26, 1987
    Assignee: Hoechst Roussel Pharmaceuticals Inc.
    Inventor: Gregory M. Shutske
  • 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: 4666902
    Abstract: Tetrahydropyridazinones of the formula I ##STR1## wherein R denotes an optionally substituted carbocyclic or heterocyclic radical, R.sup.1 denotes hydrogen; alkyl; aralkyl, which is optionally substituted in the aryl part; or acyl, and R.sup.2 denotes hydrogen; alkyl, which can optionally be substituted; or optionally substituted phenyl; and their acid addition compounds, if these can be prepared.The tetrahydropyridazinone derivatives of the formula I according to the invention and their physiologically acceptable salts exhibit useful pharmacological actions.
    Type: Grant
    Filed: June 8, 1984
    Date of Patent: May 19, 1987
    Assignee: Cassella Aktiengesellschaft
    Inventors: Gerhard Zoller, Rudi Beyerle, Melitta Just, Piero Martorana, Helmut Bohn, Rolf-Eberhard Nitz
  • 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: 4652649
    Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula: ##STR1## wherein the substituents are defined hereinbelow.
    Type: Grant
    Filed: February 20, 1985
    Date of Patent: March 24, 1987
    Assignee: United Pharmaceuticals, Inc.
    Inventor: William M. Davis
  • Patent number: 4647557
    Abstract: This invention relates to novel heterocyclic derivatives bearing an amino group and to processes for making said compounds.More particularly this invention provides novel heterocyclic compounds the hetero ring of which has two hetero atoms, the same or different, substituted with a free or substituted amino group.These compounds are useful as active ingredients of drugs.
    Type: Grant
    Filed: December 23, 1983
    Date of Patent: March 3, 1987
    Inventors: Gerard Moinet, Michel Schaeffer, Pierre Bessin, Jacqueline Bonnet
  • Patent number: 4640800
    Abstract: This invention provides a novel class of quinodimethane compounds which can exhibit nonlinear optical response.
    Type: Grant
    Filed: June 25, 1985
    Date of Patent: February 3, 1987
    Assignee: Celanese Corporation
    Inventors: Eui W. Choe, Alan Buckley, Anthon F. Garito
  • Patent number: 4639436
    Abstract: The invention includes certain 3,4,5-trihydroxypiperidine compounds, methods for their preparation, compositions containing said 3,4,5-trihydroxypiperidine compounds and methods for the use of said compounds and compositions.The subject matter of the invention is useful against diabetes, hyperlipaemia and adiposity as well as in animal nutrition.
    Type: Grant
    Filed: August 23, 1978
    Date of Patent: January 27, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Hans P. Krause, Lutz Muller, Walter Puls
  • Patent number: 4638066
    Abstract: Compounds of formula (I), ##STR1## or an N-oxide or pharmaceutically acceptable salt thereof, wherein R.sub.1 is hydrogen, C.sub.1-7 alkyl, C.sub.3-7 cycloalkyl, C.sub.4-7 cycloalkenyl or C.sub.1-4 alkyl substituted by C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, C.sub.3-7 cycloalkyl, hydroxy, thiol, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, carboxy, C.sub.1-4 alkoxycarbonyl, C.sub.1-4 alkanoyl, amino optionally substituted by one or two C.sub.1-4 alkyl or by C.sub.4-6 polymethylene optionally containing an oxygen or nitrogen atom, aminocarbonyl optionally N-substituted by one or two C.sub.1-4 alkyl, or benzoyl or phenyl either being optionally ring-substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or trifluoromethyl, R.sub.2 and R.sub.3 are the same or different and are hydrogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen or trifluoromethyl, m is 1 to 3 and n is 1 or 2, the hydrogen atom bonded to the C.sub.a carbon atom being trans to the hydrogen atom bonded to the C.sub.
    Type: Grant
    Filed: December 20, 1984
    Date of Patent: January 20, 1987
    Assignee: Beecham Group p.l.c.
    Inventors: Laramie M. Gaster, Barry S. Orlek
  • Patent number: 4631276
    Abstract: Compounds of Formula I ##STR1## wherein R.sub.1 is a prostaglandin or prostacyclin residue;Y is oxygen, sulfur, imino, or N-(C.sub.1 -C.sub.4 -alkyl) imino;Q is (CR.sub.6 R.sub.7).sub.p wherein p is an integer of 0 to 3;R.sub.2 is hydrogen; alkyl of 1-6 carbon atoms optionally substituted by hydroxy or amino; C.sub.1 -C.sub.4 -alkoxycarbonyl; benzyloxycarbonyl; cyano; or di-C.sub.1 -C.sub.4 -alkylamino-carbonyl;R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 each independently is hydrogen; alkyl of 1-6 carbon atoms optionally substituted by hydroxy or amino; or aryl; andR.sub.3 and R.sub.4 together form a trimethylene, tetramethylene, or 1,3-butadienylene group when R.sub.2 and R.sub.5 together represent a direct bond;have valuable pharmacological properties, e.g., as blood-pressure-lowering or abortive agents.
    Type: Grant
    Filed: July 3, 1984
    Date of Patent: December 23, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Vorbruggen, Walter Elger, Michael-Harold Town, Ekkehard Schillinger
  • 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: 4616002
    Abstract: Compounds of the formula I ##STR1## in which n represents 1, 2 or 3, Ar represents a carbocyclic or heterocyclic aryl radical, Ac represents the acyl radical of an acid, Z represents a radical --OR.sub.7 or --NR.sub.8 R.sub.9, R.sub.1 represents hydrogen, unsubstituted or substituted lower alkyl, a carbocyclic or heterocyclic aryl radical or free, etherified or esterified hydroxy, R.sub.2 and R.sub.3, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl, formyl or functionally modified formyl, carboxy or functionally modified carboxy, a carbocyclic or heterocyclic aryl radical or unsubstituted or mono- or di-substituted amino, R.sub.4 represents hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl or a carbocyclic or heterocyclic aryl radical, R.sub.7, R.sub.8 and R.sub.
    Type: Grant
    Filed: January 6, 1986
    Date of Patent: October 7, 1986
    Assignee: Ciba-Geigy Corporation
    Inventors: Bruno Kamber, Thomas Leutert, Hans Kuhnis, Kurt Eichenberger
  • Patent number: 4607031
    Abstract: An ethyl benzylphosphinate derivative represented by the general formula (I) ##STR1## wherein Y represents a hydrogen or fluorine atom, X represents a methylene group or an oxygen atom, and n is 2, 3 or 4.The said compounds can be produced by reacting a compound represented by the following formula (II) ##STR2## wherein Y is as defined above, with a compound represented by the following formula (III) ##STR3## wherein X and n are as defined, and M is an alkali metal atom, in an inert medium. These compounds are useful as a calcium antagonist.
    Type: Grant
    Filed: May 22, 1985
    Date of Patent: August 19, 1986
    Assignee: Kanebo Ltd.
    Inventors: Koichiro Yoshino, Tominori Morita, Masaru Moriyama, Keizo Ito, Goro Tsukamoto
  • Patent number: 4602940
    Abstract: This invention relates to ortho-heterocyclic benzene sulfonylureas which are useful as herbicides and growth regulants.
    Type: Grant
    Filed: May 20, 1985
    Date of Patent: July 29, 1986
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Anthony D. Wolf
  • Patent number: 4595539
    Abstract: Certain 2-substituted-2-penem-3-carboxylic acid compounds and pharmaceutically-acceptable salts thereof can be prepared from the appropriate xanthate or trithiocarbonate by desulfurization and addition of an electrophilic sulfur compound followed by halogenation and ring closure. The corresponding desulfurized and halogenated olefinic intermediates are disclosed.
    Type: Grant
    Filed: June 10, 1983
    Date of Patent: June 17, 1986
    Assignee: Pfizer Inc.
    Inventor: Ernest S. Hamanaka
  • Patent number: 4576749
    Abstract: Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and a 1-substituent of the formula ##STR1## (or a salt or ester thereof).
    Type: Grant
    Filed: April 13, 1984
    Date of Patent: March 18, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Robert Zahler, William H. Koster, William A. Slusarchyk
  • Patent number: 4567276
    Abstract: Novel substituted imidazoles and methods for their preparation are disclosed. These imidazoles, and their salts, exhibit pharmacological activity which includes antihypertensive activity and .beta.-adrenergic blocking activity.
    Type: Grant
    Filed: June 13, 1983
    Date of Patent: January 28, 1986
    Assignee: Merck & Co., Inc.
    Inventor: John J. Baldwin
  • Patent number: 4556654
    Abstract: Substituted anthra[1,9-cd]pyrazol-6(2H-ones have antimicrobial activity. Methods for their preparation, use and pharmaceutical compositions are disclosed.
    Type: Grant
    Filed: June 28, 1983
    Date of Patent: December 3, 1985
    Assignee: Warner-Lambert Company
    Inventors: Howard D. H. Showalter, Judith L. Johnson, Leslie M. Werbel, Edward F. Elslager
  • Patent number: 4556658
    Abstract: The invention relates to 7-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-quinoline-3-carboxyli c acids, processes for their preparation and compositions containing them as antibacterial agents. Also included in the invention are methods for treating bacterial infection using the compounds and compositions of the invention.
    Type: Grant
    Filed: April 24, 1984
    Date of Patent: December 3, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Grohe, Uwe Petersen, Hans-Joachim Zeiler, Karl G. Metzger
  • 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: 4521597
    Abstract: A novel process for producing sulfonylureas of the formula I having a herbicidal action and an action regulating plant growth ##STR1## wherein A is an unsubstituted or substituted phenyl, naphthyl, furan, thiophene or pyridine group, E is a nitrogen atom or the methine group, R.sub.a is hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -haloalkyl, C.sub.1 -C.sub.5 -alkoxy, C.sub.1 -C.sub.5 -haloalkoxy, C.sub.1 -C.sub.5 -alkylthio or C.sub.2 -C.sub.10 -alkoxyalkoxy, and R.sub.b is the same as R.sub.
    Type: Grant
    Filed: October 14, 1983
    Date of Patent: June 4, 1985
    Assignee: Ciba Geigy Corporation
    Inventors: Haukur Kristinsson, Werner Topfl
  • Patent number: 4521599
    Abstract: This invention relates to the use of 6-aryluracils as antiinflammatory and antiarthritic agents and also to both novel intermediates and novel processes for the preparation of selected 6-aryluracils.
    Type: Grant
    Filed: September 17, 1984
    Date of Patent: June 4, 1985
    Assignee: The Upjohn Company
    Inventors: Harvey I. Skulnick, Herman W. Smith, Robert J. Smith, Wendell Wierenga
  • Patent number: 4515946
    Abstract: This invention relates to 6,11-dihydro-11-oxo-dibenz[b,e]oxepin derivatives of the formula ##STR1## where Y is alkyl, alkoxy, halogen or trifluoromethyl, n is 0, 1, 2 or 3; R is ##STR2## where Hal is a halogen; ##STR3## where n is 0, 1, 2 or 3; p is 1 or 2; q is 0, 1, or 2; R.sup.1 to R.sup.7 are the same or different and are hydrogen and alkyl and R.sup.8 is hydrogen, alkyl and phenyl; and R.sup.9 is alkyl and the pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: December 23, 1981
    Date of Patent: May 7, 1985
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Lawrence L. Martin, Linda L. Setescak