Additional Hetero Ring Containing Patents (Class 544/96)
  • Patent number: 5145856
    Abstract: Compounds having the formula (I): ##STR1## in which any two of K, L and M are nitrogen and the other is CE; X and Y are independently hydrogen, halogen, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, C.sub.2-4 alkynyloxy, phenyl, benzyloxy, cyano, isocyano, isothiocyanato, nitro, NR.sup.1 R.sup.2, NR.sup.1 OR.sup.2, N.sub.3, NHCOR.sup.1, NR.sup.1 CO.sub.2 R.sup.2, NHCONR.sup.1 R.sup.2, N.dbd.CHNR.sup.1 R.sup.2, NHSO.sub.2 R.sup.1, OR.sup.1, OCOR.sup.1, OSO.sub.2 R.sup.1, SR.sup.1, SOR.sup.1, SO.sub.2 R.sup.1, SO.sub.2 OR.sup.1, SO.sub.2 NR.sup.1 R.sup.2, COR.sup.1, CR.sup.1 .dbd.NOR.sup.2, CHR.sup.1 CO.sub.2 R.sup.2, CO.sub.2 R.sup.1, CONR.sup.1 R.sup.2, CSNR.sup.1 R.sup.2, CH.sub.3 O.sub.2 C.C:CH.OCH.sub.
    Type: Grant
    Filed: December 27, 1991
    Date of Patent: September 8, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey, Ian T. Streeting, Rex Cheetham
  • Patent number: 5137886
    Abstract: The invention provides insecticidally active compounds of formula (I): ##STR1## wherein X is nitrogen or carbon bearing a hydrogen atom; R.sup.1 is a group of formula --S(O).sub.n --Y, wherein Y is an optionally substituted heterocyclic ring containing at least one nitrogen atom, the point of attachment of the group Y being at a ring nitrogen atom, and n is 0, 1 or 2; R.sup.2 is a group of formula --OSO.sub.2 R.sup.3 wherein R.sup.3 is selected from C.sub.1-8 alkyl, C.sub.1-4 alkyl substituted by an optionally substituted phenyl or heterocyclic ring, C.sub.1-8 haloalkyl, C.sub.2-6 alkenyl, C.sub.2-4 alkenyl substituted by an optionally substituted phenyl or heterocyclic ring, C.sub.2-4 alkynyl, C.sub.2-4 alkynyl substituted by an optionally substituted phenyl or heterocyclic ring, optionally substituted aryl, and a group of formula --N(R.sup.4)(R.sup.5) wherein R.sup.4 and R.sup.5 are independently selected from hydrogen and C.sub.1-6 alkyl or wherein R.sup.4 and R.sup.5 together represent --(CH.sub.2).sub.
    Type: Grant
    Filed: December 6, 1990
    Date of Patent: August 11, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: Robin A. E. Carr, Donn W. Moseley, Nan C. Sillars
  • Patent number: 5136034
    Abstract: Thioacids, thiols, an acid, and an aldehyde are used to produce chiral thioacetals of the general formula. ##STR1## The compounds are leukotriene antagonists.
    Type: Grant
    Filed: October 5, 1990
    Date of Patent: August 4, 1992
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert N. Young, Michel Therien, Jacques-Yves Gauthier, Robert Zamboni, Michel L. Belley
  • Patent number: 5135563
    Abstract: The present invention relates to a pyrimidine derivative having the formula ##STR1## (wherein the variables are defined in the full text of the patent), a method for producing the same, and its use as a herbicide.
    Type: Grant
    Filed: July 5, 1991
    Date of Patent: August 4, 1992
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Mitsunori Hiratsuka, Naonori Hirata, Kazuo Saitoh, Hideyuki Shibata
  • Patent number: 5125957
    Abstract: A pyrimidine derivative represented by the formula ##STR1## wherein the variables are defined below in the specification, and their production and herbicidal activities are described.
    Type: Grant
    Filed: October 24, 1990
    Date of Patent: June 30, 1992
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Mitsunori Hiratsuka, Naonori Hirata, Kazuo Saito, Hideyuki Shibata
  • Patent number: 5120843
    Abstract: The aromatic amines (I), alkyl amines (II), bicyclic amines (III). ##STR1## cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).
    Type: Grant
    Filed: October 23, 1989
    Date of Patent: June 9, 1992
    Assignee: Upjohn
    Inventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer
  • Patent number: 5110938
    Abstract: Chloro- and fluorosubstituted dioxolane containing oxazolines and oxazines, and their polymers are disclosed. The polymers are useful for surface modification of other polymers.
    Type: Grant
    Filed: November 30, 1990
    Date of Patent: May 5, 1992
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Ming-Hong Hung, Mureo Kaku
  • Patent number: 5096914
    Abstract: Benzopyran derivatives of the general formula I ##STR1## wherein the substituents are as defined herein are provided. The compounds show vasodilating and vascular spasmolytic activity and are useful in treating hypertension.
    Type: Grant
    Filed: November 30, 1990
    Date of Patent: March 17, 1992
    Assignee: Beiersdorf Aktiengesellschaft
    Inventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
  • Patent number: 5081197
    Abstract: This invention provides novel azlactone-functional oligomers of 2-alkenyl azlactones in which oligomerization has occurred predominantly via the 2-alkenyl group. Oligomerization of the 2-alkenyl group provides oligomers having 2 to 15 mer units with predominantly carbon-carbon backbone segments. Oligomerized in this fashion, the novel compositions possess azlactone groups which can be reacted with nucleophiles in the normal ring-opening sense. The oligomers are prepared by a novel process in which both Lewis and Bronsted acidic catalysts are effective. The reactive oligomers find utility as crosslinking agents for polymers containing azlactone-reactable nucleophilic groups.
    Type: Grant
    Filed: October 23, 1990
    Date of Patent: January 14, 1992
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Steven M. Heilmann, Dean M. Moren, Jerald K. Rasmussen, Larry R. Krepski, Sadanand V. Pathre
  • Patent number: 5075316
    Abstract: Novel compounds of the formula ##STR1## in which: R.sub.1 and R.sub.2 independently of one another are hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.2 halogenoalkyl, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 halogenoalkoxy; R.sub.3 is C.sub.3 -C.sub.6 cycloalkyl or C.sub.3 -C.sub.6 cycloalkyl which is substituted by up to three identical or different methyl or halogen groups; R.sub.4 is halogen, thiocyano, --OR.sub.5, --SR.sub.5 or --NR.sub.5 R.sub.6, in which R.sub.5 and R.sub.6 are halogen groups; R.sub.4 is halogen, thiocyano, --OR.sub.5, --SR.sub.5 or --NR.sub.5 R.sub.6, in which R.sub.5 and R.sub.6 are as defined herein, are novel active compounds for preventing attack of plants by microorganisms. The compounds can be employed as microbicides as such or in the form of suitable agents.
    Type: Grant
    Filed: March 20, 1990
    Date of Patent: December 24, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Adolf Hubele
  • Patent number: 5071871
    Abstract: New benz[b]pyranes and pyranopyridines of formula I, ##STR1## wherein the significances of substituents V, T, W, R.sub.3 to R.sub.5, R.sub.9, R.sub.10, m, X, Y and Z are given in claim 1 and their N-oxides and their salts and their use in the treatment of raised blood pressure in the treatment of vascular disorders and other disorders in which a reduction in tension of the smooth muscles is therapeutically useful, as well as in the treatment of hair loss and baldness. Further the compounds are useful in the treatment of asthma and obstructive disorders of the respiratory system as well as in the prophylactic treatment of obstructive or inflammatory airways disease, for example asthma, as well as novel pharmaceutical compositions comprising said K.sup.+ channel activators suitable for such use.
    Type: Grant
    Filed: July 10, 1990
    Date of Patent: December 10, 1991
    Assignee: Sandoz Ltd.
    Inventors: Stefan Blarer, John Morley, Ian D. Chapman
  • Patent number: 5055579
    Abstract: Compounds of general formula I are disclosed ##STR1## wherein L denotes a hydrogen atom, an aryl radial or a substituent of the formula ##STR2## M denotes an alkylene radical or alkenylene radical or a 1,2-arylene radical,Q denotes a sulfur, selenium or oxygen atom, a dialkylmethylene group, an alken 1,2-ylene radical, a 1,2-phenylene radical or an N-R.sup.1 group,denotes an alkyl, aralkyl, aryloxyalkyl or alkoxyalkyl radical,R.sup.2 and R.sup.3 denote a hydrogen atom or a 4,6-bis-trichloromethyl-s-triazin-2-yl group, andn is 0 or 1.The compounds are suitable for use as photoinitiators in photosensitive systems that are induced to reaction by free radicals or acid cations. The compounds are characterized by high sensitivity in the visible spectral region.
    Type: Grant
    Filed: March 1, 1989
    Date of Patent: October 8, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Georg Pawlowski, Heidrun Lutz
  • Patent number: 5028711
    Abstract: Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: July 2, 1991
    Assignee: Beiersdorf Aktiengesellschaft
    Inventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
  • Patent number: 5021578
    Abstract: Compounds of the formula ##STR1## in which R.sup.1 denotes haloalkyl, haloalkenyl or haloalkynyl, (R.sup.2).sub.n denotes H or up to 3 halogens, A denotes N or N.fwdarw.0, R.sup.3 denotes H or alkyl, and Z denotes, inter alia, a carboxyl group or a functional derivative thereof, are valuable herbicides and growth regulators.
    Type: Grant
    Filed: February 22, 1989
    Date of Patent: June 4, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Volker Koch, Lothar Willms, Andreas Fuss, Klaus Bauer, Hermann Bieringer, Helmut Burstell
  • Patent number: 5017586
    Abstract: Derivatives of 5-aminomethyl-2-furanomethanol represented by formula (I), or pharmaceutically acceptable salts thereof, which possess calcium-antagonistic activity and are effective in lowering blood pressure, and a process for preparing and using the same: ##STR1## wherein R, R.sub.1, R.sub.2 and R.sub.2 ' each represent a lower alkyl group containing 1 to 4 carbon atoms, with the proviso that R.sub.2 and R.sub.2 ', together with N, may form a 5- or 6-membered saturated heterocyclic ring which may contain an additional heteroatom, selected from the group consisting of as O, N and S, or R.sub.2 ' represents an aralkyl group;wherein R.sub.3 and R.sub.4 are each selected from the group consisting of a hydrogen atom, a halogen, a nitro group and a methoxy group; andwherein R.sub.5 is selected from the group consisting of a halogen, a difluoromethoxy group, a trifluoromethyl group, a nitro group, a carbamylmethoxy group, a cyanomethoxy group and a mesyloxy group.
    Type: Grant
    Filed: May 12, 1989
    Date of Patent: May 21, 1991
    Assignee: Gerot-Pharmazeutika Gesellschaft m.b.H.
    Inventor: Ludwig H. Schlager
  • Patent number: 5015284
    Abstract: Compounds of the formula I, their stereoisomers or their salts ##STR1## wherein A denotes >C(R.sup.4).sub.2 or >C.dbd.C(R.sup.5).sub.2 ; R.sup.1 denotes H, an optionally substituted aliphatic or cycloaliphatic radical, forfuryl, tetrahydrofurfuryl or (substituted) phenyl; R.sup.2 denotes H, alkyl, alkenyl, alkynyl or alkoxy; R.sup.3 denotes a radical of the formulae ##STR2## X denotes O, S or NR.sup.12 and Y denotes O or S, possess excellent herbicidal and plant-growth regulating properties.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: May 14, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
  • Patent number: 5002960
    Abstract: Compounds of the formulas: ##STR1## wherein Het is an oxazole or oxazine moiety; X is O, S or SO, n is an integer from 3 to 9, Y is an aliphatic bridge; and the various R groups represent hydrogen or various substituents as described herein, are useful as antiviral agents, especially against picornaviruses. N-(Chloroalkyl)amide intermediates for the compounds of Formula I are also active as antiviral agents. Related compounds outside the scope of the above formulas are also disclosed. Also disclosed are novel intermediates, N-halo-alkyl-4-(isoxazol-5-yl)alkoxybenzamides, also useful as antiviral agents.
    Type: Grant
    Filed: June 12, 1989
    Date of Patent: March 26, 1991
    Assignee: Sterling Drug, Inc.
    Inventor: Guy D. Diana
  • Patent number: 5001138
    Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.
    Type: Grant
    Filed: May 4, 1989
    Date of Patent: March 19, 1991
    Assignee: Nihon Tokushu Noyaku Seizo, K.K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
  • Patent number: 4994569
    Abstract: Compounds of formula: ##STR1## in which R.sub.1 denotes 2-indolyl, 2-thienyl, 3-furyl, naphthyl, phenyl, or phenyl substituted with one or two halogen atoms, with alkoxy, alkyl, nitro, acylamino, alkylthio, acyl, trifluoromethoxy, morpholino, piperidino, amino, mono- or dialkylamino or, at the 3- and 4-positions, with methylenedioxyR.sub.2 denotes phenyl or phenyl substituted with one or two halogen atoms, with one or two alkyl radicals, with alkoxy, nitro, trifluoromethyl or hydroxy or, at the 3- and 4-positions, with methylenedioxy andeither X denotes oxygen andR.sub.3 denotes phenyl R.sub.4, R.sub.5 and R.sub.6 denote hydrogen, orR.sub.3 and R.sub.4 denote hydrogen, R.sub.5 denotes hydrogen or methyl and R.sub.6 denotes phenyl or one of R.sub.3 and R.sub.4 denotes methyl and the other hydrogen, R.sub.5 denotes hydrogen and R.sub.6 denotes phenyl,or X denotes sulphur, R.sub.3 denotes phenyl and R.sub.4, R.sub.5 and R.sub.
    Type: Grant
    Filed: November 1, 1989
    Date of Patent: February 19, 1991
    Assignee: Rhone-Poulenc Sante
    Inventors: Jean-Dominique Bourzat, Claude Cotrel, Claude Guyon, Philippe Pitchen
  • Patent number: 4992433
    Abstract: Novel pyridazinamine derivatives having antiviral activity, compositions containing these compounds as active ingredient, and a method of destructing viruses or preventing the growth thereof in warm-blooded animals suffering from diseases caused by these viruses. Processes for preparing said compounds and compositions.
    Type: Grant
    Filed: November 9, 1988
    Date of Patent: February 12, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Raymond A. Stokbroekx, Marcel J. M. Van der Aa, Marcel G. M. Luyckx, Gilbert A. J. Grauwels
  • Patent number: 4990174
    Abstract: R.sup.2 is halogen,R.sup.3 is hydrogen, halogen or a C.sub.1 -C.sub.4 -alkyl,R.sup.4, R.sup.5 are hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.2 -C.sub.4 -alkyl which carries a hydroxyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -alkylthio radical, C.sub.1 -C.sub.6 -alkoxy, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.3 -C.sub.6 -alkenyloxy and/or C.sub.3 -C.sub.6 -alkynyloxy, or together with the nitorgen atom form a 5- or 6-membered aliphatic ring in which a methylene group may be replaced by an oxygen atom, andR.sup.6 is hydrogen, C.sub.1 -C.sub.6 -alkyl which is unsubstituted or substituted by one or two C.sub.1 -C.sub.4 -alkoxy groups, or is C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl or benzyl,processes for their manufacture, and their herbicidal use.
    Type: Grant
    Filed: January 9, 1990
    Date of Patent: February 5, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Lothar Rueb, Karl Eicken, Peter Plath, Karl-Otto Westphalen, Bruno Wuerzer
  • Patent number: 4988723
    Abstract: Benzopyran derivatives of formula (I) wherein the substituents are as defined herein are provided. The compounds possess vasodilating activity and are useful in the treatment of hypertension. Pharmaceutical compositions and methods of treating hypertension are also provided.
    Type: Grant
    Filed: May 17, 1989
    Date of Patent: January 29, 1991
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Youichi Shiokawa, Koichi Takimoto, Kohei Takenaka, Takeshi Kato
  • Patent number: 4988384
    Abstract: Disclosed herein are herbicidal pyridine compounds substituted at the 3- and/or 5-position with a carboxylic acid-derived heterocyclic moiety, as well as herbicidal compositions and use of these compounds.
    Type: Grant
    Filed: December 24, 1987
    Date of Patent: January 29, 1991
    Assignee: Monsanto Company
    Inventors: Yuen-Lung L. Sing, Len F. Lee
  • Patent number: 4987132
    Abstract: A saturated heterocyclic carboxamide derivative of the following general formula (I) and salts thereof which have platelet activating factor (PAF) antagonizing activity.
    Type: Grant
    Filed: August 16, 1988
    Date of Patent: January 22, 1991
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Toshiyasu Mase, Hiromu Hara, Hitoshi Nagaoka, Takumi Takahashi, Takeshi Suzuki, Kenichi Tomioka, Toshimitsu Yamada
  • Patent number: 4981962
    Abstract: Substituted tetrathiotetracenes and tetraselenotetracenes of the formula I ##STR1## in which Z is --S-- or --Se-- and (a) R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H and R.sup.5 to R.sup.8 are each H and at least one of the radicals R.sup.5 to R.sup.8 independently of one another is a substituent belonging to the group comprising C.sub.1 -C.sub.20 alkyl--X--.sub.p which is unsubstituted or substituted by halogen, --CN, --CONR.sup.9 R.sup.10, --OR.sup.9, --SR.sup.9 or --COOR.sup.9, with the exception of C.sub.1 -C.sub.4 alkyl and methoxy, C.sub.2 -C.sub.18 alkenyl--X--.sub.p, C.sub.2 -C.sub.18 -alkynyl--X--.sub.p, C.sub.3 -C.sub.8 cycloalkyl--X--.sub.p, (C.sub.1 -C.sub.12 alkyl)--C.sub.3 -C.sub.8 cycloalkyl--X--.sub.p, C.sub.3 -C.sub.8 cycloalkyl-C.sub.r H.sub.2r --X--.sub.p, (C.sub.1 -C.sub.12 alkyl)-C.sub.3 -C.sub.8 -cyclo alkyl-C.sub.r H.sub.2r --X--.sub.p, phenyl--X--.sub.p, (C.sub.1 -C.sub.12)alkyl)-phenyl--X--, phenyl-C.sub.r H.sub. 2r --X--.sub.p and (C.sub.1 -C.sub.12 alkyl)-phenyl-C.sub.r H.sub.
    Type: Grant
    Filed: May 24, 1989
    Date of Patent: January 1, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Marcus Baumann, Walter Fischer, Vratislav Kvita, Carl W. Mayer, Wolfgang Wernet
  • Patent number: 4959374
    Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereif, wherein: Z represents a residue of a substituted or unsubstituted aryl group,X represents o or NR.sup.o wherein R.sup.0 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, an alkanoyl group substituted or unsubstituted in the alkyl moiety, or an arylalkyl moiety substituted or unsubstituted in the aryl moiety,n represents an integer 1 or 2,m represents an integer 1 or 2,p represents an integer 2 or 3,andq represents an integer in the range of from 1 to 12; pharmaceutical compositions containing such compounds and the use of such compounds and compositions in medicine.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: September 25, 1990
    Assignee: Beecham Group P.L.C.
    Inventor: John M. Berge
  • Patent number: 4954509
    Abstract: A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4 -12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl, or R.sub.3 together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group; R.sub.4 and R.sub.5, which may be the same or different and may be attached to the same or different carbon atoms of the isoquinoline nucleus, are each hydrogen, halogen, hydroxy, C.sub.1-6 alkyl, aryl, or R.sub.4 together with R.sub.5 form a --(CH.sub.2).sub.p -- group, where p is an integer of from 1 to 5 and one or more of the --(CH.sub.2)-- moieties is optionally substituted by a C.
    Type: Grant
    Filed: February 17, 1989
    Date of Patent: September 4, 1990
    Assignee: Dr. Lo. Zambeletti S.p.A.
    Inventors: Vittorio Vecchietti, Giuseppe Giardina
  • Patent number: 4939140
    Abstract: A heterocyclic oxophthalazinyl acetic acid having aldose reductast inhibitory activity of the formula ##STR1## wherein X is oxygen or sulfur; Z is a covalent bond, O, S, NH or CH.sub.2 or CHR.sub.5 Z is vinyl; R.sub.1 is hydroxy, or a prodrug group; R.sub.2 is a heterocyclic group, R.sub.3 and R.sub.4 are hydrogen or the same or a different substituent, and R.sub.5 is hydrogen, methyl or trifluoromethyl. The pharmaceutically acceptable acid addition salts of the above compounds wherein R.sub.1 is di(C.sub.1 -C.sub.4)alkylamino or (C.sub.1 -C.sub.4)alkoxy substituted by N-morpholino or di(C.sub.1 -C.sub.4)alkylamino and the pharmaceutically active base addition salts of the above compounds wherein R.sub.1 is hydroxy are also aldose reductase inhibitors.
    Type: Grant
    Filed: October 27, 1988
    Date of Patent: July 3, 1990
    Assignee: Pfizer Inc.
    Inventors: Eric R. Larson, Banavara L. Mylari
  • Patent number: 4931444
    Abstract: 4-(4-phenyl-1-piperazinyl)phenols for use as 5-lipoxygenase inhibitors and a method of treating warm-blooded animals suffering from leukotriene mediated diseases and disorders using the same. Pharmaceutical compositions containing the same as active ingredient. Novel compounds used in said method and processes for preparing said novel compounds.
    Type: Grant
    Filed: January 12, 1989
    Date of Patent: June 5, 1990
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean P. F. Van Wauwe, Jan Heeres, Leo J. J. Backx
  • Patent number: 4923858
    Abstract: Compounds of the general formula: ##STR1## wherein the radicals R.sub.1 and R.sub.2 are the same or different and represent hydrogen or C.sub.1 -C.sub.6 -alkyl, the radicals R.sub.3 and R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkanoyloxy, halogen or C.sub.2 -C.sub.6 -alkanoyl, X is oxygen, sulphur or the group --NR.sub.5 and R.sub.5 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkanoyl or benzoyl, m and n in each case may represent the integers 1, 2 or 3 and the phenyl radical A is unsubsituted or is substituted by halogen, nitro, C.sub.1 -C.sub.6 -alkyl, trifluoromethyl, C.sub.3 -C.sub.7 -cycloalkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkanoyloxy, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, C.sub.2 -C.sub.6 -alkanoylamino, CN, carboxy, C.sub.1 -C.sub.6 -alkoxycarbonyl, phenyl, C.sub.1 -C.sub.
    Type: Grant
    Filed: May 16, 1989
    Date of Patent: May 8, 1990
    Assignee: Asta Pharma Aktiengesellschaft
    Inventors: Jurgen Engel, Peter Emig, Bernd Nickel, Istvan Szelenyi
  • Patent number: 4916124
    Abstract: Novel indoloquinoxalines having substituents in 6-position containing cyclic groups, of the general formula I ##STR1## wherein R.sub.1 represents hydrogen or one or several preferably 1 to 4, similar or different substituents in the positions 1-4 and/or 7-10, selected from halogen, lower alkyl-/alkoxy group having not more than 4 carbon atoms, trifluoromethyl group, trichloromethyl group;X is a group ##STR2## wherein Y is CH.sub.2, NH, O or S and a is 2, 3 or 4 and wherein also the bond --C.dbd.N-- can be saturated; Z is alkyl having 1-6 carbon atoms, Cl, Br or CF.sub.3 andR.sub.3 represents hydrogen, lower alkyl-/cycloalkyl group having not more than 4 carbon atoms,and the physiologically acceptable addition products of the compounds with acids and halogen adducts are described. Also methods for preparing said compounds by reaction of a compound of the formula II ##STR3## with a reactive compound containing the residue --CHR.sub.
    Type: Grant
    Filed: November 18, 1987
    Date of Patent: April 10, 1990
    Assignee: Lief Lundblad
    Inventors: Jan O. E. Bergman, Stig G. Akerfeldt
  • Patent number: 4908356
    Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 may be the same of different and are each independently hydrogen or lower alkyl which may be unsubstituted or monosubstituted with halogen, lower alkoxy or hydroxy with the proviso that the substituent is not the .alpha.-carbon or R.sup.1 and R.sup.2 taken together with the carbon to which they are attached form a morpholino ring;each R.sup.3 is independently hydrogen, lower alkyl, carboxy or carbalkoxy;n is an integer from 0, 1, 2 or 3 andR is hydrogen, lower alkyl, cycloalkyl, arylalkyl aryl or a nitrogen, sulfur or oxygen containing heterocyclic or a heterocyclic lower alkyl and pharmacuetically acceptable salts thereof.
    Type: Grant
    Filed: May 25, 1988
    Date of Patent: March 13, 1990
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Richard F. Borch, Ronald R. Valente
  • Patent number: 4908056
    Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.
    Type: Grant
    Filed: February 17, 1989
    Date of Patent: March 13, 1990
    Assignee: E. I. Du Pont De Nemours and Company
    Inventor: Chi-Ping Tseng
  • Patent number: 4904300
    Abstract: Imidazole derivatives of formula I ##STR1## and the stereochemically isomeric forms thereof, and salts thereof, have useful herbicidal properties. The substituents R.sup.1, L and X have the meanings defined herein.
    Type: Grant
    Filed: August 17, 1988
    Date of Patent: February 27, 1990
    Assignee: Ciba-Geigy Corp.
    Inventors: Hans-Dieter Schneider, William R. Lutz, Henry Szczepanski, Werner Topfl
  • Patent number: 4902339
    Abstract: The invention relates to certain sulfonylurea compounds having a carbocyclic or heterocyclic ring ortho to the sulfonylurea linkage, compositions thereof and a method of their use as herbicides or plant growth regulants.
    Type: Grant
    Filed: August 30, 1988
    Date of Patent: February 20, 1990
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Joel R. Christensen, Morris P. Rorer
  • Patent number: 4897105
    Abstract: A compound of the general formula ##STR1## wherein R.sub.1 is a phenyl group which may be substituted, R.sub.2 and R.sub.3 respectively are a lower alkyl or lower alkoxy group, Z is CH or N and n is 0 or 1, or a salt thereof which is useful as a herbicide.
    Type: Grant
    Filed: March 20, 1987
    Date of Patent: January 30, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yoshiyuki Okada, Isao Aoki, Nobuyuki Okajima, Takashi Kuragano
  • Patent number: 4886794
    Abstract: 4-[(.alpha.,.alpha.-Diaryl)-hydroxymethyl]-1-piperidinylalkylcyclic carbamate derivatives having the formula: ##STR1## wherein; R is hydrogen, loweralkyl, cycloalkyl, phenyl and substituted phenyl;Ar and Ar.sup.1 are phenyl, substituted phenyl or pyridinyl;alk is a straight or branched hydrocarbon chain;R.sup.1 is loweralkyl substituted for hydrogen on a ring carbon.The compounds are useful antihistamines and in controlling allergic response.
    Type: Grant
    Filed: June 3, 1988
    Date of Patent: December 12, 1989
    Assignee: A. H. Robins Company, Incorporated
    Inventor: David A. Walsh
  • Patent number: 4861791
    Abstract: Compounds of the formula ##STR1## wherein the substituents are as defined herein are useful as antiviral agents, in particular against picornaviruses.
    Type: Grant
    Filed: December 3, 1987
    Date of Patent: August 29, 1989
    Assignee: Sterling Drug Inc.
    Inventors: Guy D. Diana, Philip M. Carabateas
  • 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: 4849432
    Abstract: Novel heterocyclic compounds of the formula ##STR1## wherein, R.sup.1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group ##STR2## in which R.sup.2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R.sup.3 represents a hydrogen atom or an alkyl group, and Z represents an optionally sibstituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group.The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.
    Type: Grant
    Filed: February 24, 1987
    Date of Patent: July 18, 1989
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hattori
  • Patent number: 4846875
    Abstract: A herbicidal compound which is a Q-substituted 1-aryl-4,5-dihydro-1,2,4-triazol-5(1H)-one in which the Q-substituent is on the ring-carbon atom at the 5-position of the aryl group and in which: Q is(a) --CH(R.sup.1)ZR in which Z is O or S(O).sub.n and n is zero, one or two; or(b) --CH(R.sup.1)N(R.sup.4)(R.sup.5); or(c) --C(R.sup.9).dbd.NR.sup.
    Type: Grant
    Filed: July 21, 1987
    Date of Patent: July 11, 1989
    Assignee: FMC Corporation
    Inventor: Jun H. Chang
  • Patent number: 4840957
    Abstract: A pyran derivative represented by a general formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, cycloalkyl or phenyl, R.sub.2 is alkyl having 8 to 20 carbon atoms, R.sub.3 is hydrogen, halogen, ##STR2## or --CH.sub.2 N A, R.sub.4 and R.sub.5 being each lower alkyl or cycloalkyl, A being --CH.sub.2 13 , oxygen or nitrogen atom, N A forms five or six-member ring (the ring may have no substitutent or have at least one substituent selected from lower alkyl, lower alkoxy and halogen atom), or an acid salt thereof, are useful as agricultural miticides.
    Type: Grant
    Filed: January 21, 1988
    Date of Patent: June 20, 1989
    Assignee: Otsuka Kagaku Kabushiki Kaisha
    Inventors: Hisashi Takao, Norio Osaki, Norio Yasudomi
  • Patent number: 4838925
    Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.
    Type: Grant
    Filed: September 25, 1987
    Date of Patent: June 13, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Chi-Ping Tseng
  • Patent number: 4835280
    Abstract: The present invention provides Indolines of the formula: ##STR1## ps useful to provide pharmaceutically active pyrrolobenzimidazoles or tautomers thereof, of the formula: These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.
    Type: Grant
    Filed: July 14, 1987
    Date of Patent: May 30, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Alfred Martens, Jens-Peter Holck, Herbert Berger, Bernd Muller-Beckman, Klaus Strein, Egon Roesch
  • Patent number: 4832732
    Abstract: Novel herbicidal 1-methyl-1H-imidazole -5-carboxylic acid derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Further the invention also relates to a process for making these novel compounds.
    Type: Grant
    Filed: December 17, 1987
    Date of Patent: May 23, 1989
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: William R. Lutz, Guy R. E. Van Lommen, Victor Sipido, Wim G. Verschueren
  • Patent number: 4831032
    Abstract: The present invention provides benzimidazoles of the general formula: ##STR1## wherein R.sub.1, X, A, and R.sub.2 are as defined in the specification. The present invention also provides processes for the preparation of these new benzimidazoles and pharmaceutical compositions containing them, as well as intermediates for the preparation thereof.The new benzimidazoles are useful to treat heart or circulatory diseases which respond to a lowering of blood pressure, a positive inotropic action and/or an improvement in microcirculation.
    Type: Grant
    Filed: July 3, 1986
    Date of Patent: May 16, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein
  • Patent number: 4824472
    Abstract: Novel herbicidal 1-cyclyl or polycyclyl substituted 1H-imidazole-5-carboxylic acid derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Processes for making these novel compounds.
    Type: Grant
    Filed: December 23, 1987
    Date of Patent: April 25, 1989
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Guy R. E. Van Lommen, Victor Sipido, Wim G. Verschueren, William R. Lutz
  • Patent number: 4820842
    Abstract: The present invention provides a process for preparing a 5-cyano-2-substituted-1,4-dihydropyridine compound having cardiovascular activity.
    Type: Grant
    Filed: September 11, 1987
    Date of Patent: April 11, 1989
    Assignee: Warner-Lambert Company
    Inventors: Kevin R. Anderson, Ila Sircar
  • Patent number: 4818754
    Abstract: A compound of the formula (1) or a salt or solvate thereof: ##STR1## in which: R.sub.0 is hydrogen or C.sub.1-6 alkyl;R.sub.1 and R.sub.2 are both hydrogen; orR.sub.1 is hydrogen, C.sub.1-6 alkyl; and R.sub.2 is CN; CR.sub.5 R.sub.6 Y where R.sub.5 and R.sub.6 are independently selected from hydrogen and C.sub.1-4 alkyl and Y is selected from hydrogen, OR.sub.7 or SR.sub.7 where R.sub.7 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkanoyl, and NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkanoyl or together are C.sub.4-6 polymethylene; or COR.sub.10 is OH or C.sub.1-4 alkyl, or COR.sub.10 is a pharmaceutically acceptable ester or amide; orR.sub.2 is hydrogen, C.sub.1-6 alkyl, or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; and R.sub.1 is CN, CR.sub.5 R.sub.6 Y or COR.sub.10 as defined for R.sub.2 above; orR.sub.1 and R.sub.2 together form C.sub.3 -C.sub.
    Type: Grant
    Filed: April 16, 1987
    Date of Patent: April 4, 1989
    Assignee: Beecham Group p.l.c. of Beecham House
    Inventors: Robert W. Ward, Roger E. Markwell, Ian Hughes
  • Patent number: 4792547
    Abstract: Novel pyrazine derivatives useful for treatment of bronchial asthma, allergic gastorenteric trouble, hay fever urticaria, allertic rhinitis, and allergic conjunctivitis, and pharmaceutical compositions thereof, are disclosed. The compounds have the formula I as follows: ##STR1## wherein R represents hydrogen or ##STR2## wherein R.sub.1 and R.sub.2 may be the same or different and each independently represents hydrogen, straight or branched-chain lower-alkyl, or cycloalkyl having three to six carbon atoms inclusive, phenyl which may be substituted with halogen, lower-alkyl, or lower-alkoxy, or wherein R.sub.1 and R.sub.2 together represent alkylene of four to six carbon atoms, inclusive, optionally interrupted by one or two nitrogen atoms or one oxygen atom and said ring being optionally substituted by straight or branched-chain lower-alkyl having one to six carbon atoms inclusive, hydroxy, or phenyl,and pharmaceutically-acceptable salts thereof.
    Type: Grant
    Filed: December 15, 1986
    Date of Patent: December 20, 1988
    Assignee: Hokuriku Pharmaceutical Co., Ltd.
    Inventors: Yasuo Itoh, Hideo Kato, Eiichi Koshinaka, Nobuo Ogawa, Kazuya Mitani