N-c(=x)-x-c Containing Patents (Class 514/478)
  • Patent number: 5945315
    Abstract: The present invention provides novel cryptophycin compounds having the following structure: ##STR1## The present invention also provides methods for producing cryptophycins from the Nostoc sp. of blue-green algae (cyanobacteria). Pharmaceutical compositions comprising novel cryptophycins are also provided by the present invention, as are methods for using cryptophycins to inhibit the proliferation of hyperproliferative cells. The present invention further provides methods for using cryptophycins to inhibit the proliferation of hyperproliferative cells with drug resistant phenotypes, and to treat pathological conditions, such as neoplasia.
    Type: Grant
    Filed: November 4, 1996
    Date of Patent: August 31, 1999
    Assignee: University of Hawaii
    Inventors: Richard E. Moore, Gregory M. L. Patterson
  • Patent number: 5942548
    Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of cardiovascular disorders. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.
    Type: Grant
    Filed: March 24, 1998
    Date of Patent: August 24, 1999
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5939357
    Abstract: This invention provides a novel fungicide composition which has a bicarbonate-containing inorganic salt ingredient which enhances the efficacy of a fungicide ingredient for the treatment of cultivated crops. An invention fungicide composition also contains a surfactant ingredient, and a water-soluble organic compound which functions as a compatibility enhancing ingredient in aqueous formulations, and the ingredients improve the spreadability and adhesiveness of the composition when applied to foliage. An invention fungicide composition also contains a fertilizer-effective ratio of nitrogen, phosphorus and potassium.
    Type: Grant
    Filed: June 7, 1993
    Date of Patent: August 17, 1999
    Assignee: Church & Dwight Co., Inc.
    Inventors: Keith A. Jones, Anthony E. Winston, M. Stephen Lajoie, Amy L. Joseph
  • Patent number: 5939458
    Abstract: Mammalian hair growth is reduced by applying an inhibitor of aminoacyl-tRNA synthetase to the skin.
    Type: Grant
    Filed: September 22, 1997
    Date of Patent: August 17, 1999
    Inventors: James P. Henry, Gurpreet S. Ahluwalia
  • Patent number: 5935997
    Abstract: The present invention relates to O-thiocarbamoyl-aminoalkanol compound represented by the following structural formula (VI), (VIII) and (IX) which are a racemic or enantiomerically enriched and pharmaceulically acceptable salts thereof to treat diseases of the central nervous system: ##STR1## wherein Ar is a phenyl group as described as follows: ##STR2## wherein R is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br, and I, alkoxy containing 1 to 3 carbon atoms, thioalkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, or taifluorocarbon, and x is an integer from 1 to 3, with the proviso that R is the same or different when x is 2 or 3. R.sub.1 and R.sub.2 may be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, 3 to 7-membered aliphatic cyclic compounds and R.sub.1 and R.sub.
    Type: Grant
    Filed: January 13, 1998
    Date of Patent: August 10, 1999
    Assignee: Yukong Limited
    Inventors: Yong Moon Choi, Yong Kil Kim
  • Patent number: 5925674
    Abstract: This invention relates to cycloalkylcarboxanilides of the formula ##STR1## which are used to combat pests.
    Type: Grant
    Filed: October 26, 1995
    Date of Patent: July 20, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd-Wieland Krueger, Klaus Sasse, Thomas Schenke, Michael Negele, Heinz-Wilhelm Dehne
  • Patent number: 5906981
    Abstract: A biocidal composition which comprises an inclusion complex of a halopropargyl compound and a cyclodextrin or a modified cyclodextrin, useful broadly in industrial systems and more particularly in aqueous compositions used in connection with paints, coatings, stucco, concrete, stone, cementaceous surfaces, wood, caulking, sealants, textiles, and the like.
    Type: Grant
    Filed: June 4, 1996
    Date of Patent: May 25, 1999
    Assignee: Troy Corporation
    Inventor: Kamlesh D. Gaglani
  • Patent number: 5889047
    Abstract: N-(alkyloxycarbonyl)-N-(2-hydroxy-3-alkyloxypropyl)ethanolamine derivatives corresponding to the following formula: ##STR1## in which R.sub.1 and R.sub.2, which may be identical or different, represent a linear or branched, saturated or unsaturated and optionally hydroxylated alkyl radical having from 8 to 26 carbon atoms; as well as to their use in, and for the preparation of, cosmetic or dermatological compositions. These compositions are used in particular as moisturizers in skincare products or as conditioners in hair products.
    Type: Grant
    Filed: August 13, 1997
    Date of Patent: March 30, 1999
    Assignee: L'Oreal
    Inventor: Michel Philippe
  • Patent number: 5886031
    Abstract: Disclosed herein is hair-care cosmetic compositions comprising iodopropynyl butylcarbamate and/or a solution of zinc pyrithione in N-acyl ethylenediamine triacetate.
    Type: Grant
    Filed: May 22, 1997
    Date of Patent: March 23, 1999
    Assignee: Pacific Corporation
    Inventors: Moon Sam Shin, Sang Cho Choi, Yong Duk Kwak, Seong Hwan Seo, Han Il Jeong, Kyung Hee Seo
  • Patent number: 5882731
    Abstract: A method is disclosed for applying a mildewcide compound laden film to surfaces by applying an aqueous, film-depositing composition onto said surfaces, allowing to stand momentarily, and rinsing with water. After rinsing, a residual, durable, virtually invisible film remains. This film is mildew resistant, paintable and its sheen closely mimics that of the surfaces prior to application of the aqueous composition. The aqueous composition comprises a mildewcide compound, a non-ionic surfactant, water, and at least one film-former.
    Type: Grant
    Filed: July 23, 1997
    Date of Patent: March 16, 1999
    Inventor: Richard L. Owens
  • Patent number: 5874465
    Abstract: Compounds having the structural formula: ##STR1## wherein: R is C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.9 aralkyl, or nitroso; R' is C.sub.1 -C.sub.4 alkyl; and R" is C.sub.1 -C.sub.4 alkyl. These compounds exhibit insecticidal and miticidal activity.
    Type: Grant
    Filed: October 24, 1996
    Date of Patent: February 23, 1999
    Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.
    Inventors: Mark Achiel Dekeyser, Paul Thomas McDonald
  • Patent number: 5863950
    Abstract: HIV protease inhibitors, obtainable by chemical synthesis, block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and possibly other anti-viral agents as ingredients, are thus suitable for the treatment of the HIV virus known to cause AIDS.
    Type: Grant
    Filed: October 27, 1994
    Date of Patent: January 26, 1999
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Siegfried H. Reich, Kathleen Lewis, Michael Melnick, Mary Ann M. Fuhry, Stephen Warren Kaldor
  • Patent number: 5856354
    Abstract: The invention concerns tachykinin antagonists. The compounds are neopeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included. The compounds are expected to be especially useful in asthma and rheumatoid arthritis.
    Type: Grant
    Filed: October 17, 1997
    Date of Patent: January 5, 1999
    Assignee: Warner-Lambert Company
    Inventors: David Christopher Horwell, William Howson, Martyn Clive Pritchard, Edward Roberts, David Charles Rees
  • Patent number: 5846997
    Abstract: The present invention relates to water-emulsifiable liquid formulations of insecticidal active compounds, characterized in that they containa) 2.5 to 30% of active compound,b) 5 to 77.5% of a mixture of benzyl acetate and an alcohol in the ratio 25-95% to 5-75%,c) 2.5 to 20% of formulation auxiliary.
    Type: Grant
    Filed: April 29, 1996
    Date of Patent: December 8, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Kirkor Sirinyan, Rainer Sonneck, Klaus Mrusek
  • Patent number: 5846959
    Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: December 8, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
  • Patent number: 5840661
    Abstract: The present invention relates to novel 2-aryl-3-hydroxy-cyclopent-2-en-1-one derivatives of the formula (I) ##STR1## in which X represents halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy,Y represents hydrogen, halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy,Z represents halogen, nitro, cyano, alkyl, alkoxy or halogenoalkoxy andA, B, D.sup.1, D.sup.2, G and n have the meaning given in the description,several processes for their preparation and their use as compositions for controlling pests and as herbicides.
    Type: Grant
    Filed: December 31, 1996
    Date of Patent: November 24, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Jacques Dumas, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Andreas Turberg, Norbert Mencke
  • Patent number: 5824705
    Abstract: Carbamates of the formula I ##STR1## where the substituents have the following meanings: Z is methoxy, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2, CH.sub.3, C.sub.2 H.sub.5, CF.sub.3 or CCl.sub.3,X and Y are identical or different and each is hydrogen, F, Cl, Br, CF.sub.3, CN, NO.sub.2, alkoxy, alkenyloxy, alkynyloxy, alkyl, alkenyl or alkynyl or may be condensed together to form a substituted or unsubstituted aromatic or heteroaromatic, alicyclic or heterocyclic, partially or completely hydrogenated ring,R.sup.1 may also be substituted or unsubstituted and is O-alkyl, O-alkenyl, O-alkynyl, O-cycloalkyl, O-cycloalkenyl or O--CO.sub.2 -alkyl,A is --O--, --S--, --CR.sup.2 .dbd.CR.sup.3 --, CHR.sup.2 --O--, --CHR.sup.2 --S--, --CHR.sup.2 --O--N.dbd.C(R.sup.4)--, --CR.sup.2 .dbd.N--O--, --O--N.dbd.C(R.sup.4)--, --C.tbd.C--, --CHR.sup.2 --CHR.sup.3 --, --CHR.sup.2 --O--CO--, --O--CHR.sup.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: October 20, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Mueller, Hubert Sauter, Franz Roehl, Reinhard Doetzer, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5821260
    Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 13, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, Margaret K. Offermann, R. Wayne Alexander, Sampath Parthasarathy
  • Patent number: 5814659
    Abstract: The present invention comprises a topical analgesic composition comprising an analgesic agent, an alcohol, a chaotropic agent and an unsaturated fatty acid. The composition is preferably in the form of a stable gel and may further comprise a pharmaceutically acceptable emulsifier, a pharmaceutically acceptable gelling and/or thickening agent, and a pharmaceutically acceptable preservative. The pH of the composition is adjusted to 7.5-8.0 by the addition of a pharmaceutically acceptable organic base, such as triethanolamine.The invention also comprises a method for inducing topical analgesia. The composition is absorbed on an absorbent material, for example a cotton strip inserted into typical skin-wipe packet; brought in contact with the skin of a person in need of such an analgesia; and maintained in contact with the skin for a period of time sufficient to induce and maintain topical analgesia.
    Type: Grant
    Filed: April 23, 1996
    Date of Patent: September 29, 1998
    Assignee: DTR Dermal Therapy (Barbados) Inc.
    Inventor: Harry Richardson Elden
  • Patent number: 5807957
    Abstract: A mixture of lipophilic and amphiphilic/hydrophilic film-forming polymers of the formula (I)R--(CO).sub.m Y.sup.1 --(CH.sub.2 CHR.sup.1 O).sub.n --?CONH--Z--NHCO(OCH.sub.2 CHR.sup.2).sub.n' --Y.sup.2 --(CH.sub.2 CHR.sup.2 O).sub.n" !.sub.p --CONH--Z--NHCO--(OCH.sub.2 CHR.sup.1).sub.n --Y.sup.1 (CO).sub.m R (I)where R represents (i) an alkyl, alkenyl or alkaryl group of from 1 to 30 carbon atoms or (ii) a polypropylene oxide group or polybutylene oxide group; R.sup.1 and R.sup.2, each, independently, represent a hydrogen atom, or a methyl or ethyl group; Z represents a divalent linking hydrocarbyl group; m is 0 or 1; when m=0, Y.sup.1 represents O, NR.sup.3 or N.sup.+ R.sup.3 R.sup.4 X.sup.- and when m=1 Y.sup.1 represents O; Y.sup.2 represents O, NR.sup.3, N.sup.+ R.sup.3 R.sup.4 X.sup.-, (R.sup.3 NCH.sub.2 CH.sub.2).sub.t, or ?(R.sup.3 R.sup.4 N.sup.+ CH.sub.2 CH.sub.2)X.sup.- !.sub.t ; R.sup.3 and R.sup.4, independently, represent C.sub.1 -C.sub.
    Type: Grant
    Filed: December 23, 1996
    Date of Patent: September 15, 1998
    Assignee: MacroChem Corporation
    Inventors: Carlos M. Samour, Scott F. Krauser
  • Patent number: 5807884
    Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.
    Type: Grant
    Filed: October 4, 1994
    Date of Patent: September 15, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
  • Patent number: 5792787
    Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 11, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Margaret K. Offermann
  • Patent number: 5783596
    Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 21, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, Margaret K. Offermann, R. Wayne Alexander, Sampath Parthasarathy
  • Patent number: 5773231
    Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 30, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
  • Patent number: 5773209
    Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 30, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
  • Patent number: 5773466
    Abstract: A pharmaceutical product is disclosed which interferes with pathologies of human sensitivity and of the motor system. This product comprises parasympathomimetic drugs, in particular carbachol, methacholine or bethanechol and it has a broad application in the medical and neurological clinical fields.
    Type: Grant
    Filed: November 1, 1996
    Date of Patent: June 30, 1998
    Inventor: Maurizio Santini
  • Patent number: 5773465
    Abstract: Tartronic acid acetalic ethers and esters of the general formula: ##STR1## are provided and are useful in treatment of bone dysmetabolism. As examples, Ra and Rb may be hydrogen, B is a C.sub.2 -C.sub.12 acyl group, R is phenyl and n is 0-12.
    Type: Grant
    Filed: March 12, 1997
    Date of Patent: June 30, 1998
    Assignee: Dompe Farmaceutici S.p.A.
    Inventors: Carmelo A. Gandolfi, Lorella Cotini, Marco Mantovanini, Gianfranco Caselli, Gaetano Clavenna, Claudio Omini
  • Patent number: 5763364
    Abstract: The invention relates to thixotropic aqueous suspension concentrates of plant protection agents. The invention furthermore relates to the use of these agents in plant protection and the use of saponites as auxiliaries in the preparation of plant protection agent suspensions by wet grinding of the solid constituents.
    Type: Grant
    Filed: September 19, 1995
    Date of Patent: June 9, 1998
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Frisch, Thomas Maier
  • Patent number: 5763462
    Abstract: A herbicidal composition comprising an effective amount of a herbicide and an effective amount of a herbicide activator selected from the group consisting of an alkyl phosphate, an alkenyl phosphate, a hydroxyalkyl phosphate, a polyoxyalkylene alkyl ether phosphate, a salt thereof, a polyoxyalkylene alkenyl ether phosphate, a salt thereof, a polyoxyalkylene hydroxyalkyl ether phosphate and a salt thereof.
    Type: Grant
    Filed: February 18, 1997
    Date of Patent: June 9, 1998
    Assignee: Kao Corporation
    Inventor: Tetsuji Iwasaki
  • Patent number: 5750351
    Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 12, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
  • Patent number: 5733935
    Abstract: A hydroxylamine derivatives of formula (I): ##STR1## wherein R represents ##STR2## in which R.sup.1 and R.sup.2 represents alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkynyl group, alkoxy - alkyl group, phenoxy - alkyl group, alkylthio - alkyl group, alkylsulfonyl - alkyl group, alkylamino - alkyl group, phenyl group, benzyl group, phenethyl group, cinnamyl group, pyridyl group, furyl group, thienyl group, X represents CO.sub.2, CO or SO.sub.2, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom or a lower alkyl group, and n represents 0 or 1, and fungicides contain said compound as an active ingredient.The compounds of the present invention have excellent effects for controlling wood-rot fungi, plant diseases and fungi of humans and animals, and are useful as industrial, agricultural and medical fungicides.
    Type: Grant
    Filed: June 17, 1996
    Date of Patent: March 31, 1998
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Nobuharu Andoh, Tsutomu Nishiguchi, Katsutoshi Endo
  • Patent number: 5733928
    Abstract: The present invention relates to a novel compound selected from the group consisting of:(i) the compounds of the formula ##STR1## in which: A is a group --CO--NH-- or a group --NH--CO--,R is a hydrogen atom or a methyl group, and*C, if R is not the hydrogen atom, is an asymmetric carbon of (R,S) or (R) configuration; and(ii) their addition salts.It further relates to the method of preparing this compound and to its use in therapeutics.
    Type: Grant
    Filed: May 15, 1996
    Date of Patent: March 31, 1998
    Assignee: Fournier Industrie et Sante
    Inventors: Luc Lebreton, Patrice Renaut, Christine Dumas
  • Patent number: 5733924
    Abstract: DC107 derivatives represented by the formula (I): ##STR1## or pharmacologically acceptable slats thereof, ?wherein R.sup.1 is hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR.sup.4 or the like; R.sup.2 represents hydrogen or COR.sup.5 ; R.sup.3 represents lower alkyl, lower alkenyl, aralkyl which may be substituted with substituted or unsubstituted aryl, lower alkoxyalkyl, aralkyloxyalkyl, substituted or unsubstituted aryloxyalkyl, lower alkoxycarbonylalkyl, lower alkanoyloxyalkyl, alicyclic alkanoyloxyalkyl or the like, or bonds to Y to represent a single bond; Y bonds to R.sup.3 to represent a single bond, or bonds to Z to represent a single bond; Z represents hydrogen or bonds to Y to represent a single bond; W represents oxygen or NR.sup.6, with the proviso that the compound wherein R.sup.1, R.sup.2 and Z each represents hydrogen, R.sup.3 bonds to Y to represent a single bond, and W represents oxygen (DC107) is excluded.
    Type: Grant
    Filed: April 17, 1997
    Date of Patent: March 31, 1998
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Yutaka Kanda, Yutaka Saitoh, Hiromitsu Saito, Tadashi Ashizawa, Kazuyo Sugiyama, Katsushige Gomi, Shingo Kakita, Yuichi Takahashi, Chikara Murakata
  • Patent number: 5728729
    Abstract: 3-Methoxy-2-phenyl-acrylic esters of the formula ##STR1## in which R represents optionally substituted alkyl, cycloalkyl or aryl andn represents a number 0 or 1,a process for their preparation and their use as pesticides.
    Type: Grant
    Filed: November 13, 1995
    Date of Patent: March 17, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Gayer, Peter Gerdes, Heinz-Wilhelm Dehne
  • Patent number: 5723490
    Abstract: The present invention relates to a class of THF-containing sulfonamides which are aspartyl protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention.
    Type: Grant
    Filed: April 19, 1995
    Date of Patent: March 3, 1998
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventor: Roger D. Tung
  • Patent number: 5714518
    Abstract: HIV protease inhibitors, obtainable by chemical synthesis, block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and possibly other anti-vital agents as ingredients, are thus suitable for the treatment of the HIV virus known to cause AIDS.
    Type: Grant
    Filed: October 27, 1994
    Date of Patent: February 3, 1998
    Assignee: Agouron Pharmaceuticals
    Inventors: Siegfried H. Reich, Mark J. Pino, Dzuy T. Nguyen, Anthony J. Trippe
  • Patent number: 5709890
    Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.
    Type: Grant
    Filed: March 20, 1997
    Date of Patent: January 20, 1998
    Assignee: Donlar Corporation
    Inventor: J. Larry Sanders
  • Patent number: 5707929
    Abstract: This invention is directed to a broad spectrum fungicide/algaecide composition which comprises a mixture of (a) at least one halopropynyl compound and (b) at least one sulfur-containing s-triazine, said mixture provided in an amount to prevent and/or protect a substrate from attack by one or more fungal and/or algael organisms. The composition can be used broadly in industrial systems and more particularly with substrates such as paints, coatings, stucco, concrete, stone, cementaceous surfaces, wood, caulking, sealants, textiles, and the like.
    Type: Grant
    Filed: May 8, 1995
    Date of Patent: January 13, 1998
    Assignee: Troy Chemical Corporation
    Inventors: Eeva-Liisa Kuusisto, Kurt Laurits Hansen
  • Patent number: 5698569
    Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 16, 1997
    Assignee: G. D. Searle & Co.
    Inventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
  • Patent number: 5684178
    Abstract: Lysine derivatives, the salts of the derivatives, their optical isomers of D or L configuration, or their mixtures, the derivatives containing an N.sup..epsilon. -alkoxy or N.sup..epsilon. -alkenoxycarbonyl group of formula: ##STR1## in which: R represents a linear or branched C.sub.13 -C.sub.24 alkyl radical, the C.sub.16 radical being branched, or a linear or branched C.sub.8 -C.sub.24 alkenyl radical. The lysine derivatives are used in cosmetic, pharmaceutical hygiene or food compositions.
    Type: Grant
    Filed: November 2, 1994
    Date of Patent: November 4, 1997
    Assignee: L'Oreal
    Inventors: Michel Philippe, Thierry Bordier
  • Patent number: 5658944
    Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein Ar is a mono- or bicyclic aromatic group optionally containing one or two heteroatoms independently selected from nitrogen, oxygen and sulphur, said group being optionally substituted by one or more atoms or groups independently selected from halogen, nitro, amino, --NRR.sup.1 where R and R.sup.1 are independently selected from hydrogen, C.sub.1-8 alkyl and C.sub.1-8 alkanoyl, cyano, carboxyalkoxy, alkoxycarbonylalkoxy, C.sub.1-8 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.1-8 alkoxy (including cycloalkoxy and cycloalkylalkoxy), C.sub.
    Type: Grant
    Filed: April 14, 1995
    Date of Patent: August 19, 1997
    Assignee: The University of South Carolina
    Inventors: James Mood Chapman, Jr., Roy Lee Hawke, Karl Witold Franzmann, Kevin Julian O'Connor
  • Patent number: 5658945
    Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: August 19, 1997
    Assignee: American Cyanamid Company
    Inventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
  • Patent number: 5656660
    Abstract: The present invention describes compounds, methods and compositions effective to treat mast cell mediated inflammatory conditions, such as conjunctivitis, asthma and allergic rhinitis. The compounds of the invention comprise novel mono- and di-aminomethylbenzyl, aminobenzyl, guanidylbenzyl and benzyl tryptase inhibitors. The compositions for treating mast cell mediated inflammatory conditions include oral, inhalant and topical preparations as well as devices comprising such preparations.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: August 12, 1997
    Assignee: Arris Pharmaceutical Corporation
    Inventors: Robert T. Lum, Heinz W. Gschwend, Barr E. Bauer, Elaine Kuo, Ken Rice
  • Patent number: 5650423
    Abstract: New active compound combinations of valinamide derivatives of the formula (I) ##STR1## in which R.sup.1 and R.sup.2 has the meaning given in the description,with known fungicidal active substances, and their use for combating phytopathogenic fungi are described.
    Type: Grant
    Filed: November 6, 1995
    Date of Patent: July 22, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz-Wilhelm Dehne, Wilhelm Brandes, Karl-Heinz Kuck, Thomas Seitz
  • Patent number: 5648085
    Abstract: Pest populations that have developed pesticide resistance can be treated and killed with an inhibitor for ATP-dependent 150-180 kDa membrane P-glycoprotein as a pretreatment or simultaneously with application of a pesticide at doses which, by themselves, are not toxic to the pests.
    Type: Grant
    Filed: March 15, 1995
    Date of Patent: July 15, 1997
    Assignee: Duke University
    Inventors: Christine L. Lanning, Mohammed B. Abou-Donia, Robert L. Fine, James J. Corcoran
  • Patent number: 5646133
    Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.
    Type: Grant
    Filed: March 14, 1996
    Date of Patent: July 8, 1997
    Assignee: Donlar Corporation
    Inventor: J. Larry Sanders
  • Patent number: 5639768
    Abstract: The invention relates to the compounds of formula (I) wherein the C(.dbd.NH)--NHR.sub.3 group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which: R.sub.1 is amino which is mono- or disubstituted by a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical or a said radical interrupted by oxygen; R.sub.2 is hydroxy which is etherified by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy; R.sub.3 is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid; X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--); and X.sub.2 is a divalent aliphatic hydrocarbon radical which may be interrupted by an aromatic radical.
    Type: Grant
    Filed: July 25, 1995
    Date of Patent: June 17, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Michael M. Morrissey, Hongsuk Suh
  • Patent number: 5633280
    Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: May 27, 1997
    Assignee: American Cyanamid Company
    Inventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
  • Patent number: 5631273
    Abstract: A water soluble preservative antimicrobial composition for addition to commercial use products at predetermined use levels to provide synergistic biocidal activity against a wide range of fungi and gram-negative and gram-positive bacteria, comprising an active liquid blend of(1) an admixture of(a) one or more methylol compounds selected from the group consisting of N-[1,3-bis (hydroxymethyl)-2,5-dioxo-4-imidazolidinyl]-N,N'-bis (hydroxymethyl) urea; 1,3-dimethylol-5,5-dimethyl hydantoin; sodium hydroxymethyl glycinate; 1,1-methylene bis[3-[3-(hydroxymethyl)-2,5-dioxo-4-imidazolidinyl]urea]; and glycine anhydride dimethylol; and(b) 3-iodo-2-propynylbutyl carbamate, in a weight ratio of (a):(b) of 100:1 to 2000:1, and(2) propylene glycol or 1,3-butylene glycol.
    Type: Grant
    Filed: May 23, 1996
    Date of Patent: May 20, 1997
    Assignee: ISP Chemicals Inc.
    Inventor: John J. Merianos
  • Patent number: 5631293
    Abstract: Amino acid-substituted benzoylguanidines, a process for their preparation, their use as a medicament or diagnostic agent and a medicament containing themBenzoylguanidines of the formula I ##STR1## in which the radicals R(1) to R(5) have the meanings given in the description, are described. They are prepared by reacting a compound of the formula II ##STR2## in which R(1) to R(5) and L have the meanings given in the description, with guanidine. The compound I is suitable for the preparation of cardiovascular medicaments.
    Type: Grant
    Filed: September 8, 1995
    Date of Patent: May 20, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus